Avelox (Moxifloxacin HCL)
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Avelox (Moxifloxacin HCL)

AVELOX
(moxifloxacin)

WARNING

Fluoroquinolones, including AVELOX® , are associated with an increased risk of tendinitis and tendon rupture in all ages. This risk is further increased in older patients usually over 60 years of age, in patients taking corticosteroid drugs, and in patients with kidney, heart or lung transplants [see WARNINGS AND PRECAUTIONS].

Fluoroquinolones, including AVELOX, may exacerbate muscle weakness in persons with myasthenia gravis. Avoid AVELOX in patients with known history of myasthenia gravis [see WARNINGS AND PRECAUTIONS].

DRUG DESCRIPTION

AVELOX (moxifloxacin) hydrochloride is a synthetic broad spectrum antibacterial agent for oral and intravenous administration. Moxifloxacin, a fluoroquinolone, is available as the monohydrochloride salt of 1-cyclopropyl-7-[(S,S)2,8-diazabicyclo[4.3.0]non-8-yl]-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3 quinoline carboxylic acid. It is a slightly yellow to yellow crystalline substance with a molecular weight of 437.9. Its empirical formula is C21H24FN3O4*HCl and its chemical structure is as follows:

AVELOX (moxifloxacin) Structural Formula Illustration

AVELOX Tablets

  • AVELOX Tablets are available as film-coated tablets containing moxifloxacin hydrochloride (equivalent to 400 mg moxifloxacin).
  • The inactive ingredients are microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, hypromellose, titanium dioxide, polyethylene glycol and ferric oxide.

AVELOX IV

  • AVELOX IV is available in ready-to-use 250 mL latex-free flexibags as a sterile, preservative free, 0.8% sodium chloride aqueous solution of moxifloxacin hydrochloride (containing 400 mg moxifloxacin) with pH ranging from 4.1 to 4.6.
  • The appearance of the intravenous solution is yellow. The color does not affect, nor is it indicative of, product stability.
  • The inactive ingredients are sodium chloride, USP, Water for Injection, USP, and may include hydrochloric acid and/or sodium hydroxide for pH adjustment.
  • AVELOX IV contains approximately 34.2 mEq (787 mg) of sodium in 250 mL.

What are the possible side effects of moxifloxacin (Avelox)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using moxifloxacin and call your doctor at once if you have a serious side effect such as:

  • severe dizziness, fainting, fast or pounding heartbeats;
  • sudden pain, snapping or popping sound, bruising, swelling, tenderness, stiffness, or loss of movement in any of your joints;
  • diarrhea that is watery or bloody;
  • confusion, hallucinations, depression, insomnia or nightmares, unusual...

Read All Potential Side Effects and See Pictures of Avelox »

What are the precautions when taking moxifloxacin hcl (Avelox)?

Before taking moxifloxacin, tell your doctor or pharmacist if you are allergic to it; or to other quinolone antibiotics (e.g., ciprofloxacin, levofloxacin); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, heart problems (e.g., recent heart attack), joint/tendon problems (e.g., tendonitis, bursitis), liver disease, myasthenia gravis, nervous system disorder (e.g., peripheral neuropathy), seizure disorder, conditions that increase your risk of seizures (e.g., brain/head injury, brain tumors, cerebral atherosclerosis).

Moxifloxacin may cause...

Read All Potential Precautions of Avelox »

Last reviewed on RxList: 10/9/2012
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

To reduce the development of drug-resistant bacteria and maintain the effectiveness of AVELOX® and other antibacterial drugs, AVELOX should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

AVELOX® Tablets and IV are indicated for the treatment of adults ( ≥ 18 years of age) with infections caused by susceptible isolates of the designated microorganisms in the conditions listed below [see DOSAGE AND ADMINISTRATION and Use In Specific Populations].

Culture and Susceptibility Testing

Appropriate culture and susceptibility tests should be performed before treatment in order to isolate and identify organisms causing infection and to determine their susceptibility to moxifloxacin [see CLINICAL PHARMACOLOGY]. Therapy with AVELOX may be initiated before results of these tests are known; once results become available, appropriate therapy should be continued.

Acute Bacterial Sinusitis

AVELOX is indicated for the treatment of Acute Bacterial Sinusitis caused by Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis [see Clinical Studies].

Acute Bacterial Exacerbation of Chronic Bronchitis

AVELOX is indicated for the treatment of Acute Bacterial Exacerbation of Chronic Bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, methicillin-susceptible Staphylococcus aureus, or Moraxella catarrhalis [see Clinical Studies].

Community Acquired Pneumonia

AVELOX is indicated for the treatment of Community Acquired Pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant isolates*), Haemophilus influenzae, Moraxella catarrhalis, methicillin-susceptible Staphylococcus aureus, Klebsiella pneumoniae, Mycoplasma pneumoniae, or Chlamydophila pneumoniae.

* MDRSP, Multi-drug resistant Streptococcus pneumoniae includes isolates previously known as PRSP (Penicillinresistant S. pneumoniae), and are isolates resistant to two or more of the following antibiotics: penicillin (minimum inhibitory concentrations [MIC] ≥ 2 mcg/mL), 2nd generation cephalosporins (for example, cefuroxime), macrolides, tetracyclines, and trimethoprim/sulfamethoxazole [see Clinical Studies].

Uncomplicated Skin and Skin Structure Infections

AVELOX is indicated for the treatment of Uncomplicated Skin and Skin Structure Infections caused by methicillinsusceptible Staphylococcus aureus or Streptococcus pyogenes [see Clinical Studies].

Complicated Skin and Skin Structure Infections

AVELOX is indicated for the treatment of Complicated Skin and Skin Structure Infections caused by methicillinsusceptible Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, or Enterobacter cloacae [see Clinical Studies].

Complicated Intra-Abdominal Infections

AVELOX is indicated for the treatment of Complicated Intra-Abdominal Infections including polymicrobial infections such as abscess caused by Escherichia coli, Bacteroides fragilis, Streptococcus anginosus, Streptococcus constellatus, Enterococcus faecalis, Proteus mirabilis, Clostridium perfringens, Bacteroides thetaiotaomicron, or Peptostreptococcus species [see Clinical Studies].

DOSAGE AND ADMINISTRATION

Dosage in Adult Patients

The dose of AVELOX is 400 mg (orally or as an intravenous infusion) once every 24 hours. The duration of therapy depends on the type of infection as described in Table 1.

Table 1: Dosage and Duration of Therapy in Adult Patients

Type of Infectiona Dose Every 24 hours Durationb (days)
Acute Bacterial Sinusitis (1.1) 400 mg 10
Acute Bacterial Exacerbation of Chronic Bronchitis (1.2) 400 mg 5
Community Acquired Pneumonia 400 mg 7-14
Uncomplicated Skin and Skin Structure Infections (SSSI ) (1.4) 400 mg 7
Complicated SSSI (1.5) 400 mg 7-21
Complicated Intra-Abdominal Infections (1.6) 400 mg 5-14
aDue to the designated pathogens [see INDICATIONS AND USAGE, for IV use, see Use In Specific Populations].
bSequential therapy (intravenous to oral) may be instituted at the discretion of the physician

Intravenous formulation is indicated when it offers a route of administration advantageous to the patient (for example, patient cannot tolerate an oral dosage form). When switching from intravenous to oral formulation, no dosage adjustment is necessary. Patients whose therapy is started with AVELOX IV may be switched to AVELOX Tablets when clinically indicated at the discretion of the physician.

Drug interactions with Multivalent Cations

Oral doses of AVELOX should be administered at least 4 hours before or 8 hours after products containing magnesium, aluminum, iron or zinc, including antacids, sucralfate, multivitamins and VIDEX® (didanosine) chewable/buffered tablets or the pediatric powder for oral solution [see DRUG INTERACTIONS and CLINICAL PHARMACOLOGY].

Administration Instructions

AVELOX Film-Coated Tablets

AVELOX Tablets can be taken with or without food, drink fluids liberally.

AVELOX IV Solution for Infusion

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

AVELOX IV should be administered by INTRAVENOUS infusion only. It is not intended for intra-arterial, intramuscular, intrathecal, intraperitoneal, or subcutaneous administration.

AVELOX IV should be administered by intravenous infusion over a period of 60 minutes by direct infusion or through a Y-type intravenous infusion set which may already be in place. Caution: rapid or bolus intravenous infusion must be avoided.

Because only limited data are available on the compatibility of AVELOX intravenous injection with other intravenous substances, additives or other medications should not be added to AVELOX IV or infused simultaneously through the same intravenous line. If the same intravenous line or a Y-type line is used for sequential infusion of other drugs, or if the “piggyback” method of administration is used, the line should be flushed before and after infusion of AVELOX IV with an infusion solution compatible with AVELOX IV as well as with other drug(s) administered via this common line.

AVELOX IV is compatible with the following intravenous solutions at ratios from 1:10 to 10:1

0.9% Sodium Chloride Injection, USP Sterile Water for Injection, USP
1M Sodium Chloride Injection 10% Dextrose for Injection, USP
5% Dextrose Injection, USP Lactated Ringer's for Injection

Preparation for Administration of AVELOX IV

To prepare AVELOX IV injection premix in flexible containers:

  1. Close flow control clamp of administration set.
  2. Remove cover from port at bottom of container.
  3. Insert piercing pin from an appropriate transfer set (for example, one that does not require excessive force, such as ISO compatible administration set) into port with a gentle twisting motion until pin is firmly seated.

NOTE: Refer to complete directions that have been provided with the administration set.

HOW SUPPLIED

Dosage Forms And Strengths

AVELOX Tablets
  • Containing moxifloxacin hydrochloride (equivalent to 400 mg moxifloxacin)
  • Oblong, dull red film-coated tablets
  • Imprinted with BAYER on one side and M400 on the other
AVELOX IV
  • Containing 400 mg moxifloxacin in 0.8% saline (moxifloxacin hydrochloride in sodium chloride injection) with pH ranging from 4.1 to 4.6.
  • Ready-to-use 250 mL latex-free flexibags. No further dilution is necessary
  • Sterile, preservative free, 0.8% sodium chloride aqueous solution of moxifloxacin hydrochloride

Storage And Handling

AVELOX Tablets

AVELOX (moxifloxacin) hydrochloride tablets are available as oblong, dull red film-coated tablets containing 400 mg moxifloxacin.

The tablet is coded with the word “BAYER” on one side and “M400” on the reverse side.

Package NDC Code
Bottles of 30: 0085-1733-01
Unit Dose Pack of 50: 0085-1733-02
ABC Pack of 5: 0085-1733-03

Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F) [see USP Controlled Room Temperature]. Avoid high humidity.

AVELOX Intravenous Solution – Premix Bags

AVELOX IV (moxifloxacin) hydrochloride in sodium chloride injection is available in ready-to-use 250 mL latex-free flexible bags containing 400 mg of moxifloxacin in 0.8% saline. NO FURTHER DILUTION OF THIS PREPARATION IS NECESSARY.

Package NDC Code
250 mL flexible container 0085-1737-01

Parenteral drug products should be inspected visually for particulate matter prior to administration. Samples containing visible particulates should not be used.

Because the premix flexible containers are for single-use only, any unused portion should be discarded.

Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F) [see USP Controlled Room Temperature].

DO NOT REFRIGERATE – PRODUCT PRECIPITATES UPON REFRIGERATION.

Revised August 2012. Manufactured for: Bayer HealthCare Pharmaceuticals Inc. Wayne, NJ 07470 AVELOX Tablets manufactured in Germany AVELOX IV manufactured in Germany or AVELOX IV manufactured in Norway by Fresenius Kabi Norge AS NO-1753 Halden, Norway. Distributed by: Merck Sharp & Dohme Corp., a subsidiary of Whitehouse Station, NJ 08889, USA

Last reviewed on RxList: 10/9/2012
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

Serious and Otherwise Important Adverse Reactions

The following serious and otherwise important adverse reactions are discussed in greater detail in the WARNINGS AND PRECAUTIONS section of the label:

Clinical Trial Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The data described below reflect exposure to AVELOX in 14981 patients in 71 active controlled Phase II- IV clinical trials in different indications [see INDICATIONS AND USAGE]. The population studied had a mean age of 50 years (approximately 73% of the population was < 65 years of age), 50% were male, 63% were Caucasian, 12% were Asian and 9% were Black. Patients received AVELOX 400 mg once daily PO, IV, or sequentially (IV followed by PO). Treatment duration was usually 6-10 days, and the mean number of days on therapy was 9 days.

Discontinuation of AVELOX due to adverse events occurred in 5.0% of patients overall, 4.1% of patients treated with 400 mg PO, 3.9% with 400 mg IV and 8.2% with sequential therapy 400 mg PO/IV. The most common adverse events leading to discontinuation with the 400 mg PO doses were nausea (0.8%), diarrhea (0.5%), dizziness (0.5%), and vomiting (0.4%). The most common adverse event leading to discontinuation with the 400 mg IV dose was rash (0.5%). The most common adverse events leading to discontinuation with the 400 mg IV/PO sequential dose were diarrhea (0.5%), pyrexia (0.4%).

Adverse reactions occurring in ≥ 1% of AVELOX-treated patients and less common adverse reactions, occurring in 0.1 to < 1% of AVELOX-treated patients, are shown in Tables 2 and Table 3, respectively. The most common adverse drug reactions ( ≥ 3%) are nausea, diarrhea, headache, and dizziness.

Table 2 : Common ( ≥ 1.0%) Adverse Reactions Reported in Active-Controlled Clinical Trials with AVELOX

System Organ Class Adverse Reactionsa % (N=14,981)
Blood and Lymphatic System Disorders Anemia 1.1
Nausea 6.9
Diarrhea 6.0
Vomiting 2.4
Constipation 1.9
Abdominal pain 1.5
Abdominal pain upper 1.1
Gastrointestinal Disorders Dyspepsia 1.0
General Disorders and Administration Site Conditions Pyrexia 1.1
Investigations Alanine aminotransferase increased 1.1
Metabolism and Nutritional Disorder Hypokalemia 1
Headache 4.2
Nervous System Disorders Dizziness 3.0
Psychiatric Disorders Insomnia 1.9
aMedDRA Version 12.0

Table 3: Less Common (0.1 to < 1.0%) Adverse Reactions Reported in Active-Controlled Clinical Trials with AVELOX (N=14,981)

System Organ Class Adverse Reactionsa
Blood and Lymphatic System Disorders Thrombocythemia
Eosinophilia
Neutropenia
Thrombocytopenia
Leukopenia
Leukocytosis
Cardiac Disorders Atrial fibrillation
Palpitations
Tachycardia
Cardiac failure congestive
Angina pectoris
Cardiac failure
Cardiac arrest
Bradycardia
Ear and Labyrinth Disorders Vertigo Tinnitus
Eye Disorders Vision blurred
Gastrointestinal Disorders Dry mouth
Abdominal discomfort
Flatulence
Abdominal distention
Gastritis
Gastroesophageal reflux disease
General Disorders and Administration Site Conditions Fatigue
Chest pain
Asthenia
Edema peripheral
Pain
Malaise
Infusion site extravasation
Edema
Chills
Chest discomfort
Facial pain
Hepatobiliary disorders Hepatic function abnormal
Infections and Infestations Vulvovaginal candidiasis
Oral candidiasis
Vulvovaginal mycotic infection
Candidiasis
Vaginal infection
Oral fungal infection
Fungal infection
Gastroenteritis
Investigations Aspartate aminotransferase increased
Gamma-glutamyltransferase increased
Blood alkaline phosphatase increased
Hepatic enzyme increased
Electrocardiogram QT prolonged
Blood lactate dehydrogenase increased
Platelet count increased
Blood amylase increased
Blood glucose increased
Lipase increased
Hemoglobin decreased
Blood creatinine increased
Transaminases increased
White blood cell count increased
Blood urea increased
Liver function test abnormal
Hematocrit decreased
Prothrombin time prolonged
Eosinophil count increased
Activated partial thromboplastin time prolonged
Blood bilirubin increased
Blood triglycerides increased
Blood uric acid increased
Blood pressure increased
Metabolism and Nutrition Disorders Hyperglycemia
Anorexia
Hypoglycemia
Hyperlipidemia
Decreased appetite
Dehydration
Musculoskeletal and Connective Tissue Disorders Back pain
Pain in extremity
Arthralgia
Myalgia
Muscle spasms
Musculoskeletal chest pain
Musculoskeletal pain
Nervous System Disorders Dysgeusia
Somnolence
Tremor
Lethargy
Paresthesia
Tension headache
Hypoesthesia
Syncope
Psychiatric Disorders Anxiety
Confusional state
Agitation
Depression
Nervousness
Restlessness
Hallucination
Disorientation
Renal and Urinary Disorders Renal failure
Dysuria
Renal failure acute
Reproductive System and Breast Disorders Vulvovaginal pruritus
Respiratory, Thoracic, and Mediastinal Disorders Dyspnea
Asthma
Wheezing
Bronchospasm
Skin and Subcutaneous Tissue Disorders Rash
Pruritus
Hyperhidrosis
Erythema
Urticaria
Dermatitis allergic
Night sweats
Vascular disorders Hypertension Hypotension Phlebitis
aMedDRA Version 12.0

Laboratory Changes

Changes in laboratory parameters, without regard to drug relationship, which are not listed above and which occurred in ≥ 2% of patients and at an incidence greater than in controls included: increases in MCH, neutrophils, WBCs, PT ratio, ionized calcium, chloride, albumin, globulin, bilirubin; decreases in hemoglobin, RBCs, neutrophils, eosinophils, basophils, PT ratio, glucose, pO2, bilirubin, and amylase. It cannot be determined if any of the above laboratory abnormalities were caused by the drug or the underlying condition being treated.

Postmarketing Experience

Table 4 lists adverse reactions that have been identified during post-approval use of AVELOX. Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Table 4: Postmarketing Reports of Adverse Drug Reactions

System/Organ Class Adverse Reaction
Blood and Lymphatic System Disorders Agranulocytosis Pancytopenia [see WARNINGS AND PRECAUTIONS]
Cardiac Disorders Ventricular tachyarrhythmias (including in very rare cases cardiac arrest and torsade de pointes, and usually in patients with concurrent severe underlying proarrhythmic conditions)
Ear and Labyrinth Disorders Hearing impairment, including deafness (reversible in majority of cases)
Eye Disorders Vision loss (especially in the course of CNS reactions, transient in majority of cases)
Hepatobiliary Disorders Hepatitis (predominantly cholestatic) Hepatic failure (including fatal cases) Jaundice Acute hepatic necrosis [see WARNINGS AND PRECAUTIONS]
Immune System Disorders Anaphylactic reaction Anaphylactic shock Angioedema (including laryngeal edema) [see WARNINGS AND PRECAUTIONS]
Musculoskeletal and Connective Tissue Disorders Tendon rupture [see WARNINGS AND PRECAUTIONS)]
Nervous System Disorders Altered coordination Abnormal gait [see WARNINGS AND PRECAUTIONS] Myasthenia gravis (exacerbation of) [see WARNINGS AND PRECAUTIONS] Muscle weakness Peripheral neuropathy, polyneuropathy [see WARNINGS AND PRECAUTIONS]
Psychiatric Disorders Psychotic reaction (very rarely culminating in self-injurious behavior, such as suicidal ideation/thoughts or suicide attempts [see WARNINGS AND PRECAUTIONS]
Renal and Urinary Disorders Renal dysfunction Interstitial nephritis [see WARNINGS AND PRECAUTIONS]
Respiratory, Thoracic and Mediastinal Disorders Allergic pneumonitis [see WARNINGS AND PRECAUTIONS]
Skin and Subcutaneous Tissue Disorders Photosensitivity/phototoxicity reaction [see WARNINGS AND PRECAUTIONS] Stevens-Johnson syndrome Toxic epidermal necrolysis [see WARNINGS AND PRECAUTIONS]

Read the Avelox (moxifloxacin hcl) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

Antacids, Sucralfate, Multivitamins and other products containing Multivalent Cations

Quinolones form chelates with alkaline earth and transition metal cations. Oral administration of quinolones with antacids containing aluminum or magnesium, with sucralfate, with metal cations such as iron, or with multivitamins containing iron or zinc, or with formulations containing divalent and trivalent cations such as VIDEX® (didanosine) chewable/buffered tablets or the pediatric powder for oral solution, may substantially interfere with the absorption of quinolones, resulting in systemic concentrations considerably lower than desired. Therefore, AVELOX should be taken at least 4 hours before or 8 hours after these agents. [see DOSAGE AND ADMINISTRATION, Pharmacokinetics, and PATIENT INFORMATION.]

Warfarin

Quinolones, including AVELOX, have been reported to enhance the anticoagulant effects of warfarin or its derivatives in the patient population. In addition, infectious disease and its accompanying inflammatory process, age, and general status of the patient are risk factors for increased anticoagulant activity. Therefore the prothrombin time, International Normalized Ratio (INR), or other suitable anticoagulation tests should be closely monitored if a quinolone is administered concomitantly with warfarin or its derivatives. [see ADVERSE REACTIONS, Pharmacokinetics, and PATIENT INFORMATION.]

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

Although not observed with AVELOX in preclinical and clinical trials, the concomitant administration of a nonsteroidal anti-inflammatory drug with a quinolone may increase the risks of CNS stimulation and convulsions [see WARNINGS AND PRECAUTIONS, and PATIENT INFORMATION].

Drugs that Prolong QT

There is limited information available on the potential for a pharmacodynamic interaction in humans between AVELOX and other drugs that prolong the QTc interval of the electrocardiogram. Sotalol, a Class III antiarrhythmic, has been shown to further increase the QTc interval when combined with high doses of intravenous (IV) AVELOX in dogs. Therefore, AVELOX should be avoided with Class IA and Class III antiarrhythmics. [see WARNINGS AND PRECAUTIONS, Nonclinical Toxicology, and PATIENT INFORMATION.]

Last reviewed on RxList: 10/9/2012
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

Tendinopathy and Tendon Rupture

Fluoroquinolones, including AVELOX, are associated with an increased risk of tendinitis and tendon rupture in all ages. This adverse reaction most frequently involves the Achilles tendon, and rupture of the Achilles tendon may require surgical repair. Tendinitis and tendon rupture in the rotator cuff (the shoulder), the hand, the biceps, the thumb, and other tendon sites have also been reported. The risk of developing fluoroquinolone-associated tendinitis and tendon rupture is further increased in older patients usually over 60 years of age, in patients taking corticosteroid drugs, and in patients with kidney, heart or lung transplants. Factors, in addition to age and corticosteroid use, that may independently increase the risk of tendon rupture include strenuous physical activity, renal failure, and previous tendon disorders such as rheumatoid arthritis. Tendinitis and tendon rupture have also occurred in patients taking fluoroquinolones who do not have the above risk factors. Tendon rupture can occur during or after completion of therapy; cases occurring up to several months after completion of therapy have been reported. AVELOX should be discontinued if the patient experiences pain, swelling, inflammation or rupture of a tendon. Patients should be advised to rest at the first sign of tendinitis or tendon rupture, and to contact their healthcare provider regarding changing to a non-quinolone antimicrobial drug. [see ADVERSE REACTIONS and PATIENT INFORMATION.]

Exacerbation of Myasthenia Gravis

Fluoroquinolones, including AVELOX, have neuromuscular blocking activity and may exacerbate muscle weakness in persons with myasthenia gravis. Postmarketing serious adverse events, including deaths and requirement for ventilatory support, have been associated with fluoroquinolone use in persons with myasthenia gravis. Avoid AVELOX in patients with known history of myasthenia gravis [see PATIENT INFORMATION].

QT Prolongation

AVELOX has been shown to prolong the QT interval of the electrocardiogram in some patients. Following oral dosing with 400 mg of AVELOX the mean (± SD) change in QTc from the pre-dose value at the time of maximum drug concentration was 6 msec (± 26) (n = 787). Following a course of daily intravenous dosing (400 mg; 1 hour infusion each day) the mean change in QTc from the Day 1 pre-dose value was 10 msec (±22) on Day 1 (n=667) and 7 msec (± 24) on Day 3 (n = 667).

The drug should be avoided in patients with known prolongation of the QT interval, patients with uncorrected hypokalemia and patients receiving Class IA (for example, quinidine, procainamide) or Class III (for example, amiodarone, sotalol) antiarrhythmic agents, due to the lack of clinical experience with the drug in these patient populations.

Pharmacokinetic studies between AVELOX and other drugs that prolong the QT interval such as cisapride, erythromycin, antipsychotics, and tricyclic antidepressants have not been performed. An additive effect of AVELOX and these drugs cannot be excluded; therefore caution should be exercised when AVELOX is given concurrently with these drugs. In premarketing clinical trials, the rate of cardiovascular adverse events was similar in 798 AVELOX and 702 comparator treated patients who received concomitant therapy with drugs known to prolong the QTc interval.

AVELOX should be used with caution in patients with ongoing proarrhythmic conditions, such as clinically significant bradycardia, acute myocardial ischemia. The magnitude of QT prolongation may increase with increasing concentrations of the drug or increasing rates of infusion of the intravenous formulation. Therefore the recommended dose or infusion rate should not be exceeded. QT prolongation may lead to an increased risk for ventricular arrhythmias including torsade de pointes. No excess in cardiovascular morbidity or mortality attributable to QTc prolongation occurred with AVELOX treatment in over 15,500 patients in controlled clinical studies, including 759 patients who were hypokalemic at the start of treatment, and there was no increase in mortality in over 18,000 AVELOX tablet treated patients in a postmarketing observational study in which ECGs were not performed. Elderly patients using IV AVELOX may be more susceptible to drug-associated QT prolongation. [see Use In Specific Populations.] In addition, AVELOX should be used with caution in patients with mild, moderate, or severe liver cirrhosis. [see CLINICAL PHARMACOLOGY and PATIENT INFORMATION.]

Hypersensitivity Reactions

Serious anaphylactic reactions, some following the first dose, have been reported in patients receiving quinolone therapy, including AVELOX . Some reactions were accompanied by cardiovascular collapse, loss of consciousness, tingling, pharyngeal or facial edema, dyspnea, urticaria, and itching. Serious anaphylactic reactions require immediate emergency treatment with epinephrine. AVELOX should be discontinued at the first appearance of a skin rash or any other sign of hypersensitivity. Oxygen, intravenous steroids, and airway management, including intubation, may be administered as indicated. [see ADVERSE REACTIONS and PATIENT INFORMATION.]

Other Serious and Sometimes Fatal Reactions

Other serious and sometimes fatal events, some due to hypersensitivity, and some due to uncertain etiology, have been reported rarely in patients receiving therapy with quinolones, including AVELOX . These events may be severe and generally occur following the administration of multiple doses. Clinical manifestations may include one or more of the following:

The drug should be discontinued immediately at the first appearance of a skin rash, jaundice, or any other sign of hypersensitivity and supportive measures instituted [see PATIENT INFORMATION and ADVERSE REACTIONS.

Central Nervous System Effects

Fluoroquinolones, including AVELOX, may cause central nervous system (CNS) events, including: nervousness, agitation, insomnia, anxiety, nightmares or paranoia. [See ADVERSE REACTIONS.]

Convulsions and increased intracranial pressure (including pseudotumor cerebri) have been reported in patients receiving fluoroquinolones. Fluoroquinolones may also cause central nervous system (CNS) events including: dizziness, confusion, tremors, hallucinations, depression, and, rarely, suicidal thoughts or acts. These reactions may occur following the first dose. If these reactions occur in patients receiving AVELOX , the drug should be discontinued and appropriate measures instituted. As with all fluoroquinolones, AVELOX should be used with caution in patients with known or suspected CNS disorders (for example, severe cerebral arteriosclerosis, epilepsy) or in the presence of other risk factors that may predispose to seizures or lower the seizure threshold. [see DRUG INTERACTIONS, ADVERSE REACTIONS and PATIENT INFORMATION.]

Clostridium Difficile-Associated Diarrhea

Clostridium difficile-associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including AVELOX, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.

C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.

If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated [see ADVERSE REACTIONS and PATIENT INFORMATION].

Peripheral Neuropathy

Rare cases of sensory or sensorimotor axonal polyneuropathy affecting small and/or large axons resulting in paresthesias, hypoesthesias, dysesthesias and weakness have been reported in patients receiving quinolones including AVELOX. AVELOX should be discontinued if the patient experiences symptoms of neuropathy in order to prevent the development of an irreversible condition [see ADVERSE REACTIONS and PATIENT INFORMATION].

Arthropathic Effects in Animals

The oral administration of AVELOX caused lameness in immature dogs. Histopathological examination of the weight-bearing joints of these dogs revealed permanent lesions of the cartilage. Related quinolone-class drugs also produce erosions of cartilage of weight-bearing joints and other signs of arthropathy in immature animals of various species. [see Animal Toxicology and/or Pharmacology.]

Photosensitivity/Phototoxicity

Moderate to severe photosensitivity/phototoxicity reactions, the latter of which may manifest as exaggerated sunburn reactions (for example, burning, erythema, exudation, vesicles, blistering, edema) involving areas exposed to light (typically the face, “V” area of the neck, extensor surfaces of the forearms, dorsa of the hands), can be associated with the use of quinolone antibiotics after sun or UV light exposure. Therefore, excessive exposure to these sources of light should be avoided. Drug therapy should be discontinued if phototoxicity occurs. [see ADVERSE REACTIONS and Pharmacokinetics.]

Development of Drug Resistant Bacteria

Prescribing AVELOX in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria [see PATIENT INFORMATION].

Patient Counseling Information

See FDA-Approved Medication Guide

Antibacterial Resistance

Antibacterial drugs including AVELOX should only be used to treat bacterial infections. They do not treat viral infections (for example, the common cold). When AVELOX is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by AVELOX or other antibacterial drugs in the future.

Administration With Food, Fluids, and Drug Products Containing Multivalent Cations

Patients should be informed that AVELOX tablets may be taken with or without food. Patients should be advised to drink fluids liberally.

AVELOX tablets should be taken at least 4 hours before or 8 hours after multivitamins (containing iron or zinc), antacids (containing magnesium or aluminum), sucralfate, or VIDEX® (didanosine) chewable/buffered tablets or the pediatric powder for oral solution.

Serious and Potentially Serious Adverse Reactions

To assure safe and effective use of AVELOX, patients should be informed of the following serious adverse reactions that have been associated with AVELOX and other fluoroquinolone use:

  • Tendon Disorders: Patients should contact their healthcare provider if they experience pain, swelling, or inflammation of a tendon, or weakness or inability to use one of their joints; rest and refrain from exercise; and discontinue AVELOX treatment. The risk of severe tendon disorder with fluoroquinolones is higher in older patients usually over 60 years of age, in patients taking corticosteroid drugs, and in patients with kidney, heart or lung transplants.
  • Exacerbation of Myasthenia Gravis: fluoroquinolones like AVELOX may cause worsening of myasthenia gravis symptoms, including muscle weakness and breathing problems. Patients should call their healthcare provider right away if they have any worsening muscle weakness or breathing problems.
  • Prolongation of the QT interval: AVELOX may produce changes in the electrocardiogram (QTc interval prolongation). AVELOX should be avoided in patients receiving Class IA (for example quinidine, procainamide) or Class III (for example amiodarone, sotalol) antiarrhythmic agents. AVELOX may add to the QTc prolonging effects of other drugs such as cisapride, erythromycin, antipsychotics, and tricyclic antidepressants. The patients should inform their physician of any personal or family history of QTc prolongation or proarrhythmic conditions such as recent hypokalemia, significant bradycardia, and acute myocardial ischemia. Patients should contact their physician if they experience palpitations or fainting spells while taking AVELOX.
  • Hypersensitivity Reactions: Patients should be advised that AVELOX may be associated with hypersensitivity reactions, including anaphylactic reactions, even following a single dose. Patients should discontinue AVELOX at the first sign of a skin rash or other signs of an allergic reaction.
  • Convulsions: Convulsions have been reported in patients receiving quinolones, and they should notify their physician before taking AVELOX if there is a history of this condition. Patients should also inform their physician if they are taking NSAIDs concurrently with AVELOX.
  • Neurologic Adverse Effects (for example, dizziness, lightheadedness): AVELOX may cause dizziness, lightheadedness and vision disorders therefore, patients should know how they react to this drug before they operate an automobile or machinery or engage in activities requiring mental alertness or coordination.
  • Psychotic Reaction: Psychotic reactions sometimes resulting in self-injurious behavior have been reported in patients receiving quinolones. Patients should notify their physician if they have a history of psychiatric illness before taking AVELOX.
  • Peripheral Neuropathies: If symptoms of peripheral neuropathy including pain, burning, tingling, numbness, and/or weakness develop, patients should discontinue AVELOX and contact their physician.
  • Photosensitivity/Phototoxicity: Patients should be informed that photosensitivity/phototoxicity has been reported in patients receiving quinolones. Patients should minimize or avoid exposure to natural or artificial sunlight (tanning beds or UVA/B treatment) while taking quinolones. If patients need to be outdoors while using quinolones, they should wear loose-fitting clothes that protect skin from sun exposure and discuss other sun protection measures with their physician. If a sunburn-like reaction or skin eruption occurs, patients should contact their physician.
  • Diarrhea: Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long term studies in animals to determine the carcinogenic potential of moxifloxacin have not been performed.

Moxifloxacin was not mutagenic in 4 bacterial strains (TA 98, TA 100, TA 1535, TA 1537) used in the Ames Salmonella reversion assay. As with other quinolones, the positive response observed with moxifloxacin in strain TA 102 using the same assay may be due to the inhibition of DNA gyrase. Moxifloxacin was not mutagenic in the CHO/HGPRT mammalian cell gene mutation assay. An equivocal result was obtained in the same assay when v79 cells were used. Moxifloxacin was clastogenic in the v79 chromosome aberration assay, but it did not induce unscheduled DNA synthesis in cultured rat hepatocytes. There was no evidence of genotoxicity in vivo in a micronucleus test or a dominant lethal test in mice.

Moxifloxacin had no effect on fertility in male and female rats at oral doses as high as 500 mg/kg/day, approximately 12 times the maximum recommended human dose based on body surface area (mg/m2), or at intravenous doses as high as 45 mg/kg/day, approximately equal to the maximum recommended human dose based on body surface area (mg/m2). At 500 mg/kg orally there were slight effects on sperm morphology (head-tail separation) in male rats and on the estrous cycle in female rats.

Use In Specific Populations

Pregnancy

Pregnancy Category C

Because no adequate or well-controlled studies have been conducted in pregnant women, AVELOX should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Moxifloxacin was not teratogenic when administered to pregnant rats during organogenesis at oral doses as high as 500 mg/kg/day or 0.24 times the maximum recommended human dose based on systemic exposure (AUC), but decreased fetal body weights and slightly delayed fetal skeletal development (indicative of fetotoxicity) were observed. Intravenous administration of 80 mg/kg/day (approximately 2 times the maximum recommended human dose based on body surface area (mg/m2) to pregnant rats resulted in maternal toxicity and a marginal effect on fetal and placental weights and the appearance of the placenta. There was no evidence of teratogenicity at intravenous doses as high as 80 mg/kg/day. Intravenous administration of 20 mg/kg/day (approximately equal to the maximum recommended human oral dose based upon systemic exposure) to pregnant rabbits during organogenesis resulted in decreased fetal body weights and delayed fetal skeletal ossification. When rib and vertebral malformations were combined, there was an increased fetal and litter incidence of these effects. Signs of maternal toxicity in rabbits at this dose included mortality, abortions, marked reduction of food consumption, decreased water intake, body weight loss and hypoactivity. There was no evidence of teratogenicity when pregnant cynomolgus monkeys were given oral doses as high as 100 mg/kg/day (2.5 times the maximum recommended human dose based upon systemic exposure). An increased incidence of smaller fetuses was observed at 100 mg/kg/day. In an oral pre- and postnatal development study conducted in rats, effects observed at 500 mg/kg/day included slight increases in duration of pregnancy and prenatal loss, reduced pup birth weight and decreased neonatal survival. Treatment-related maternal mortality occurred during gestation at 500 mg/kg/day in this study.

Nursing Mothers

Moxifloxacin is excreted in the breast milk of rats. Moxifloxacin may also be excreted in human milk. Because of the potential for serious adverse reactions in infants who are nursing from mothers taking AVELOX, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness in pediatric patients and adolescents less than 18 years of age have not been established. AVELOX causes arthropathy in juvenile animals [see BOXED WARNING, WARNINGS AND PRECAUTIONS, and CLINICAL PHARMACOLOGY].

Geriatric Use

Geriatric patients are at increased risk for developing severe tendon disorders including tendon rupture when being treated with a fluoroquinolone such as AVELOX. This risk is further increased in patients receiving concomitant corticosteroid therapy. Tendinitis or tendon rupture can involve the Achilles, hand, shoulder, or other tendon sites and can occur during or after completion of therapy; cases occurring up to several months after fluoroquinolone treatment have been reported. Caution should be used when prescribing AVELOX to elderly patients especially those on corticosteroids. Patients should be informed of this potential side effect and advised to discontinue AVELOX and contact their healthcare provider if any symptoms of tendinitis or tendon rupture occur. [see BOXED WARNING, WARNINGS AND PRECAUTIONS, and ADVERSE REACTIONS.]

In controlled multiple-dose clinical trials, 23% of patients receiving oral AVELOX were greater than or equal to 65 years of age and 9% were greater than or equal to 75 years of age. The clinical trial data demonstrate that there is no difference in the safety and efficacy of oral AVELOX in patients aged 65 or older compared to younger adults.

In trials of intravenous use, 42% of AVELOX patients were greater than or equal to 65 years of age, and 23% were greater than or equal to 75 years of age. The clinical trial data demonstrate that the safety of intravenous AVELOX in patients aged 65 or older was similar to that of comparator-treated patients. In general, elderly patients may be more susceptible to drug-associated effects of the QT interval. Therefore, AVELOX should be avoided in patients taking drugs that can result in prolongation of the QT interval (for example, class IA or class III antiarrhythmics) or in patients with risk factors for torsade de pointes (for example, known QT prolongation, uncorrected hypokalemia). [see WARNINGS AND PRECAUTIONS, DRUG INTERACTIONS, and CLINICAL PHARMACOLOGY.]

Renal Impairment

The pharmacokinetic parameters of moxifloxacin are not significantly altered in mild, moderate, severe, or end-stage renal disease. No dosage adjustment is necessary in patients with renal impairment, including those patients requiring hemodialysis (HD) or continuous ambulatory peritoneal dialysis (CAPD) [see DOSAGE AND ADMINISTRATION, and CLINICAL PHARMACOLOGY.]

Hepatic Impairment

No dosage adjustment is recommended for mild, moderate, or severe hepatic insufficiency (Child-Pugh Classes A, B, or C). However, due to metabolic disturbances associated with hepatic insufficiency, which may lead to QT prolongation, AVELOX should be used with caution in these patients [see WARNINGS AND PRECAUTIONS, and CLINICAL PHARMACOLOGY].

Last reviewed on RxList: 10/9/2012
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

Single oral overdoses up to 2.8 g were not associated with any serious adverse events. In the event of acute overdose, the stomach should be emptied and adequate hydration maintained. ECG monitoring is recommended due to the possibility of QT interval prolongation. The patient should be carefully observed and given supportive treatment. The administration of activated charcoal as soon as possible after oral overdose may prevent excessive increase of systemic moxifloxacin exposure. About 3% and 9% of the dose of moxifloxacin, as well as about 2% and 4.5% of its glucuronide metabolite are removed by continuous ambulatory peritoneal dialysis and hemodialysis, respectively.

Single oral AVELOX doses of 2000, 500, and 1500 mg/kg were lethal to rats, mice, and cynomolgus monkeys, respectively. The minimum lethal intravenous dose in mice and rats was 100 mg/kg. Adverse clinical signs included CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting and diarrhea.

CONTRAINDICATIONS

AVELOX is contraindicated in persons with a history of hypersensitivity to moxifloxacin or any member of the quinolone class of antimicrobial agents.

Last reviewed on RxList: 10/9/2012
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

Mechanism of Action

AVELOX is a member of the fluoroquinolone class of antibacterial agents [see Microbiology].

Pharmacokinetics

Absorption

Moxifloxacin, given as an oral tablet, is well absorbed from the gastrointestinal tract. The absolute bioavailability of moxifloxacin is approximately 90 percent. Co-administration with a high fat meal (that is, 500 calories from fat) does not affect the absorption of moxifloxacin.

Consumption of 1 cup of yogurt with moxifloxacin does not significantly affect the extent or rate of systemic absorption (AUC).

Table 5: Mean (± SD) Cmax and AUC values following single and multiple doses of 400 mg moxifloxacin given orally

  Cmax (mg/L) AUC (mg•h/L) Half-life (hr)
Single Dose Oral
  Healthy (n = 372) 3.1 ± 1 36.1 ± 9.1 11.5 - 15.6a
Multiple Dose Oral
  Healthy young male/female (n = 15) 4.5 ± 0.5 48 ± 2.7 12.7 ± 1.9
  Healthy elderly male (n = 8) 3.8 ± 0.3 51.8 ± 6.7  
  Healthy elderly female (n = 8) 4.6 ± 0.6 54.6 ± 6.7  
  Healthy young male (n = 8) 3.6 ± 0.5 48.2 ± 9  
  Healthy young female (n = 9) 4.2 ± 0.5 49.3 ± 9.5  
a Range of means from different studies

Table 6: Mean (± SD) Cmax and AUC values following single and multiple doses of 400 mg moxifloxacin given by 1 hour IV infusion

  Cmax (mg/L) AUC (mg•h/L) Half-life (hr)
Single Dose IV
  Healthy young male/female (n = 56) Patients (n = 118) 3.9 ± 0.9 39.3 ± 8.6 8.2 - 15.4a
  Male (n = 64) 4.4 ± 3.7    
    Female (n = 54) 4.5 ± 2    
     < 65 years (n = 58) 4.6 ± 4.2    
     ≥ 65 years (n = 60) 4.3 ± 1.3    
Multiple Dose IV
  Healthy young male (n = 8) 4.2 ± 0.8 38 ± 4.7 14.8 ± 2.2
  Healthy elderly (n =12; 8 male, 4 female) Patientsb (n = 107) 6.1 ± 1.3 48.2 ± 0.9 10.1 ± 1.6
    Male (n = 58) 4.2 ± 2.6    
    Female (n = 49) 4.6 ± 1.5    
     < 65 years (n = 52) 4.1 ± 1.4    
     ≥ 65 years (n = 55) 4.7 ± 2.7    
a Range of means from different studies
b Expected Cmax (concentration obtained around the time of the end of the infusion)

Plasma concentrations increase proportionately with dose up to the highest dose tested (1200 mg single oral dose). The mean (± SD) elimination half-life from plasma is 12 ± 1.3 hours; steady-state is achieved after at least three days with a 400 mg once daily regimen.

Mean Steady-State Plasma Concentrations of Moxifloxacin Obtained With Once Daily Dosing of 400 mg Either Orally (n=10) or by IV Infusion (n=12)

Mean Steady-State Plasma Concentrations - Illustration

Distribution

Moxifloxacin is approximately 30-50% bound to serum proteins, independent of drug concentration. The volume of distribution of moxifloxacin ranges from 1.7 to 2.7 L/kg. Moxifloxacin is widely distributed throughout the body, with tissue concentrations often exceeding plasma concentrations. Moxifloxacin has been detected in the saliva, nasal and bronchial secretions, mucosa of the sinuses, skin blister fluid, subcutaneous tissue, skeletal muscle, and abdominal tissues and fluids following oral or intravenous administration of 400 mg. Moxifloxacin concentrations measured post-dose in various tissues and fluids following a 400 mg oral or IV dose are summarized in Table 7. The rates of elimination of moxifloxacin from tissues generally parallel the elimination from plasma.

Table 7: Moxifloxacin Concentrations (mean ± SD) in Tissues and the Corresponding Plasma Concentrations After a Single 400 mg Oral or Intravenous Dosea

Tissue or Fluid N Plasma Concentration (mcg/mL) Tissue or Fluid Concentration (mcg/mL or mcg/g) Tissue Plasma Ratio
Respiratory
Alveolar Macrophages 5 3.3 ± 0.7 61.8 ± 27.3 21.2 ± 10
Bronchial Mucosa 8 3.3 ± 0.7 5.5 ± 1.3 1.7 ± 0.3
Epithelial Lining Fluid 5 3.3 ± 0.7 24.4 ± 14.7 8.7 ± 6.1
Sinus
Maxillary Sinus Mucosa 4 3.7 ± 1.1b 7.6 ± 1.7 2 ± 0.3
Anterior Ethmoid 3 3.7 ± 1.1b 8.8 ± 4.3 2.2 ± 0.6
Mucosa Nasal Polyps 4 3.7 ± 1.1b 9.8 ± 4.5 2.6 ± 0.6
Skin, Musculoskeletal
Blister Fluid 5 3 ± 0.5c 2.6 ± 0.9 0.9 ± 0.2
Subcutaneous Tissue 6 2.3 ± 0.4d 0.9 ± 0.3e 0.4 ± 0.6
Skeletal Muscle 6 2.3 ± 0.4d 0.9 ± 0.2e 0.4 ± 0.1
Intra-Abdominal
Abdominal tissue 8 2.9 ± 0.5 7.6 ± 2 2.7 ± 0.8
Abdominal exudate 10 2.3 ± 0.5 3.5 ±1.2 1.6 ± 0.7
Abscess fluid 6 2.7 ± 0.7 2.3 ±1.5 0.8±0.4
a All moxifloxacin concentrations were measured 3 hours after a single 400 mg dose, except the abdominal tissue and exudate concentrations which were measured at 2 hours post-dose and the sinus concentrations which were measured 3 hours post-dose after 5 days of dosing.
b N = 5
c N = 7
d N = 12
e Reflects only non-protein bound concentrations of drug.

Metabolism

Approximately 52% of an oral or intravenous dose of moxifloxacin is metabolized via glucuronide and sulfate conjugation. The cytochrome P450 system is not involved in moxifloxacin metabolism, and is not affected by moxifloxacin. The sulfate conjugate (M1) accounts for approximately 38% of the dose, and is eliminated primarily in the feces. Approximately 14% of an oral or intravenous dose is converted to a glucuronide conjugate (M2), which is excreted exclusively in the urine. Peak plasma concentrations of M2 are approximately 40% those of the parent drug, while plasma concentrations of M1 are generally less than 10% those of moxifloxacin.

In vitro studies with cytochrome (CYP) P450 enzymes indicate that moxifloxacin does not inhibit CYP3A4, CYP2D6, CYP2C9, CYP2C19, or CYP1A2, suggesting that moxifloxacin is unlikely to alter the pharmacokinetics of drugs metabolized by these enzymes.

Excretion

Approximately 45% of an oral or intravenous dose of moxifloxacin is excreted as unchanged drug (~20% in urine and ~25% in feces). A total of 96% ± 4% of an oral dose is excreted as either unchanged drug or known metabolites. The mean (± SD) apparent total body clearance and renal clearance are 12 ± 2 L/hr and 2.6 ± 0.5 L/hr, respectively.

Pharmacokinetics in Specific Populations

Geriatric

Following oral administration of 400 mg moxifloxacin for 10 days in 16 elderly (8 male; 8 female) and 17 young (8 male; 9 female) healthy volunteers, there were no age-related changes in moxifloxacin pharmacokinetics. In 16 healthy male volunteers (8 young; 8 elderly) given a single 200 mg dose of oral moxifloxacin, the extent of systemic exposure (AUC and Cmax) was not statistically different between young and elderly males and elimination half-life was unchanged. No dosage adjustment is necessary based on age. In large phase III studies, the concentrations around the time of the end of the infusion in elderly patients following intravenous infusion of 400 mg were similar to those observed in young patients. [see Use In Specific Populations.]

Pediatric

The pharmacokinetics of moxifloxacin in pediatric subjects has not been studied [see Use In Specific Populations].

Gender

Following oral administration of 400 mg moxifloxacin daily for 10 days to 23 healthy males (19-75 years) and 24 healthy females (19-70 years), the mean AUC and Cmax were 8% and 16% higher, respectively, in females compared to males. There are no significant differences in moxifloxacin pharmacokinetics between male and female subjects when differences in body weight are taken into consideration.

A 400 mg single dose study was conducted in 18 young males and females. The comparison of moxifloxacin pharmacokinetics in this study (9 young females and 9 young males) showed no differences in AUC or Cmax due to gender. Dosage adjustments based on gender are not necessary.

Race

Steady-state moxifloxacin pharmacokinetics in male Japanese subjects were similar to those determined in Caucasians, with a mean Cmax of 4.1 mcg/mL, an AUC24 of 47 mcg•h/mL, and an elimination half-life of 14 hours, following 400 mg p.o. daily.

Renal Insufficiency

The pharmacokinetic parameters of moxifloxacin are not significantly altered in mild, moderate, severe, or end-stage renal disease. No dosage adjustment is necessary in patients with renal impairment, including those patients requiring hemodialysis (HD) or continuous ambulatory peritoneal dialysis (CAPD).

In a single oral dose study of 24 patients with varying degrees of renal function from normal to severely impaired, the mean peak concentrations (Cmax) of moxifloxacin were reduced by 21% and 28% in the patients with moderate (CLCR ≥ 30 and ≤ 60 mL/min) and severe (CLCR < 30 mL/min) renal impairment, respectively. The mean systemic exposure (AUC) in these patients was increased by 13%. In the moderate and severe renally impaired patients, the mean AUC for the sulfate conjugate (M1) increased by 1.7-fold (ranging up to 2.8-fold) and mean AUC and Cmax for the glucuronide conjugate (M2) increased by 2.8-fold (ranging up to 4.8-fold) and 1.4-fold (ranging up to 2.5-fold), respectively. [see Use In Specific Populations.]

The pharmacokinetics of single dose and multiple dose moxifloxacin were studied in patients with CLCR < 20 mL/min on either hemodialysis or continuous ambulatory peritoneal dialysis (8 HD, 8 CAPD). Following a single 400 mg oral dose, the AUC of moxifloxacin in these HD and CAPD patients did not vary significantly from the AUC generally found in healthy volunteers. Cmax values of moxifloxacin were reduced by about 45% and 33% in HD and CAPD patients, respectively, compared to healthy, historical controls. The exposure (AUC) to the sulfate conjugate (M1) increased by 1.4- to 1.5-fold in these patients. The mean AUC of the glucuronide conjugate (M2) increased by a factor of 7.5, whereas the mean Cmax values of the glucuronide conjugate (M2) increased by a factor of 2.5 to 3, compared to healthy subjects. The sulfate and the glucuronide conjugates of moxifloxacin are not microbiologically active, and the clinical implication of increased exposure to these metabolites in patients with renal disease including those undergoing HD and CAPD has not been studied.

Oral administration of 400 mg QD AVELOX for 7 days to patients on HD or CAPD produced mean systemic exposure (AUCss) to moxifloxacin similar to that generally seen in healthy volunteers. Steady-state Cmax values were about 22% lower in HD patients but were comparable between CAPD patients and healthy volunteers. Both HD and CAPD removed only small amounts of moxifloxacin from the body (approximately 9% by HD, and 3% by CAPD). HD and CAPD also removed about 4% and 2% of the glucuronide metabolite (M2), respectively.

Hepatic Insufficiency

No dosage adjustment is recommended for mild, moderate, or severe hepatic insufficiency (Child-Pugh Classes A, B, or C). However, due to metabolic disturbances associated with hepatic insufficiency, which may lead to QT prolongation, AVELOX should be used with caution in these patients [see WARNINGS AND PRECAUTIONS, Use In Specific Populations].

In 400 mg single oral dose studies in 6 patients with mild (Child-Pugh Class A) and 10 patients with moderate (Child-Pugh Class B) hepatic insufficiency, moxifloxacin mean systemic exposure (AUC) was 78% and 102%, respectively, of 18 healthy controls and mean peak concentration (Cmax) was 79% and 84% of controls.

The mean AUC of the sulfate conjugate of moxifloxacin (M1) increased by 3.9-fold (ranging up to 5.9-fold) and 5.7-fold (ranging up to 8-fold) in the mild and moderate groups, respectively. The mean Cmax of M1 increased by approximately 3fold in both groups (ranging up to 4.7- and 3.9-fold). The mean AUC of the glucuronide conjugate of moxifloxacin (M2) increased by 1.5-fold (ranging up to 2.5-fold) in both groups. The mean Cmax of M2 increased by 1.6- and 1.3-fold (ranging up to 2.7- and 2.1-fold), respectively. The clinical significance of increased exposure to the sulfate and glucuronide conjugates has not been studied. In a subset of patients participating in a clinical trial, the plasma concentrations of moxifloxacin and metabolites determined approximately at the moxifloxacin Tmax following the first intravenous or oral AVELOX dose in the Child-Pugh Class C patients (n=10) were similar to those in the Child-Pugh Class A/B patients (n=5), and also similar to those observed in healthy volunteer studies.

Photosensitivity Potential

A study of the skin response to ultraviolet (UVA and UVB) and visible radiation conducted in 32 healthy volunteers (8 per group) demonstrated that AVELOX does not show phototoxicity in comparison to placebo. The minimum erythematous dose (MED) was measured before and after treatment with AVELOX (200 mg or 400 mg once daily), lomefloxacin (400 mg once daily), or placebo. In this study, the MED measured for both doses of AVELOX were not significantly different from placebo, while lomefloxacin significantly lowered the MED.

It is difficult to ascribe relative photosensitivity/phototoxicity among various fluoroquinolones during actual patient use because other factors play a role in determining a subject's susceptibility to this adverse event such as: a patient's skin pigmentation, frequency and duration of sun and artificial ultraviolet light (UV) exposure, wearing of sunscreen and protective clothing, the use of other concomitant drugs and the dosage and duration of fluoroquinolone therapy [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS, and PATIENT INFORMATION].

Drug-Drug Interactions

The following drug interactions were studied in healthy volunteers or patients.

Antacids and iron significantly reduced bioavailability of moxifloxacin, as observed with other quinolones [see DRUG INTERACTIONS].

Calcium, digoxin, itraconazole, morphine, probenecid, ranitidine, theophylline, and warfarin did not significantly affect the pharmacokinetics of moxifloxacin. These results and the data from in vitro studies suggest that moxifloxacin is unlikely to significantly alter the metabolic clearance of drugs metabolized by CYP3A4, CYP2D6, CYP2C9, CYP2C19, or CYP1A2 enzymes.

Moxifloxacin had no clinically significant effect on the pharmacokinetics of atenolol, digoxin, glyburide, itraconazole, oral contraceptives, theophylline, and warfarin [see DRUG INTERACTIONS].

Antacids

When moxifloxacin (single 400 mg tablet dose) was administered two hours before, concomitantly, or 4 hours after an aluminum/magnesium-containing antacid (900 mg aluminum hydroxide and 600 mg magnesium hydroxide as a single oral dose) to 12 healthy volunteers there was a 26%, 60% and 23% reduction in the mean AUC of moxifloxacin, respectively. Moxifloxacin should be taken at least 4 hours before or 8 hours after antacids containing magnesium or aluminum, as well as sucralfate, metal cations such as iron, and multivitamin preparations with zinc, or VIDEX® (didanosine) chewable/ buffered tablets or the pediatric powder for oral solution. [see DOSAGE AND ADMINISTRATION, DRUG INTERACTIONS].

Atenolol

In a crossover study involving 24 healthy volunteers (12 male; 12 female), the mean atenolol AUC following a single oral dose of 50 mg atenolol with placebo was similar to that observed when atenolol was given concomitantly with a single 400 mg oral dose of moxifloxacin. The mean Cmax of single dose atenolol decreased by about 10% following co-administration with a single dose of moxifloxacin.

Calcium

Twelve healthy volunteers were administered concomitant moxifloxacin (single 400 mg dose) and calcium (single dose of 500 mg Ca++ dietary supplement) followed by an additional two doses of calcium 12 and 24 hours after moxifloxacin administration. Calcium had no significant effect on the mean AUC of moxifloxacin. The mean Cmax was slightly reduced and the time to maximum plasma concentration was prolonged when moxifloxacin was given with calcium compared to when moxifloxacin was given alone (2.5 hours versus 0.9 hours). These differences are not considered to be clinically significant.

Digoxin

No significant effect of moxifloxacin (400 mg once daily for two days) on digoxin (0.6 mg as a single dose) AUC was detected in a study involving 12 healthy volunteers. The mean digoxin Cmax increased by about 50% during the distribution phase of digoxin. This transient increase in digoxin Cmax is not viewed to be clinically significant. Moxifloxacin pharmacokinetics were similar in the presence or absence of digoxin. No dosage adjustment for moxifloxacin or digoxin is required when these drugs are administered concomitantly.

Glyburide

In diabetics, glyburide (2.5 mg once daily for two weeks pretreatment and for five days concurrently) mean AUC and Cmax were 12% and 21% lower, respectively, when taken with moxifloxacin (400 mg once daily for five days) in comparison to placebo. Nonetheless, blood glucose levels were decreased slightly in patients taking glyburide and moxifloxacin in comparison to those taking glyburide alone, suggesting no interference by moxifloxacin on the activity of glyburide. These interaction results are not viewed as clinically significant.

Iron

When moxifloxacin tablets were administered concomitantly with iron (ferrous sulfate 100 mg once daily for two days), the mean AUC and Cmax of moxifloxacin was reduced by 39% and 59%, respectively. Moxifloxacin should only be taken more than 4 hours before or 8 hours after iron products. [see DOSAGE AND ADMINISTRATION, DRUG INTERACTIONS].

Itraconazole

In a study involving 11 healthy volunteers, there was no significant effect of itraconazole (200 mg once daily for 9 days), a potent inhibitor of cytochrome P4503A4, on the pharmacokinetics of moxifloxacin (a single 400 mg dose given on the 7th day of itraconazole dosing). In addition, moxifloxacin was shown not to affect the pharmacokinetics of itraconazole.

Morphine

No significant effect of morphine sulfate (a single 10 mg intramuscular dose) on the mean AUC and Cmax of moxifloxacin (400 mg single dose) was observed in a study of 20 healthy male and female volunteers.

Oral Contraceptives

A placebo-controlled study in 29 healthy female subjects showed that moxifloxacin 400 mg daily for 7 days did not interfere with the hormonal suppression of oral contraception with 0.15 mg levonorgestrel/0.03 mg ethinylestradiol (as measured by serum progesterone, FSH, estradiol, and LH), or with the pharmacokinetics of the administered contraceptive agents.

Probenecid

Probenecid (500 mg twice daily for two days) did not alter the renal clearance and total amount of moxifloxacin (400 mg single dose) excreted renally in a study of 12 healthy volunteers.

Ranitidine

No significant effect of ranitidine (150 mg twice daily for three days as pretreatment) on the pharmacokinetics of moxifloxacin (400 mg single dose) was detected in a study involving 10 healthy volunteers.

Theophylline

No significant effect of moxifloxacin (200 mg every twelve hours for 3 days) on the pharmacokinetics of theophylline (400 mg every twelve hours for 3 days) was detected in a study involving 12 healthy volunteers. In addition, theophylline was not shown to affect the pharmacokinetics of moxifloxacin. The effect of co-administration of a 400 mg dose of moxifloxacin with theophylline has not been studied, but it is not expected to be clinically significant based on in vitro metabolic data showing that moxifloxacin does not inhibit the CYP1A2 isoenzyme.

Warfarin

No significant effect of moxifloxacin (400 mg once daily for eight days) on the pharmacokinetics of R- and S-warfarin (25 mg single dose of warfarin sodium on the fifth day) was detected in a study involving 24 healthy volunteers. No significant change in prothrombin time was observed. [see ADVERSE REACTIONS, DRUG INTERACTIONS].

Microbiology

Mechanism of Action

The bactericidal action of moxifloxacin results from inhibition of the topoisomerase II (DNA gyrase) and topoisomerase IV required for bacterial DNA replication, transcription, repair, and recombination. It appears that the C8-methoxy moiety contributes to enhanced activity and lower selection of resistant mutants of Gram-positive bacteria compared to the C8-H moiety. The presence of the bulky bicycloamine substituent at the C-7 position prevents active efflux, associated with the NorA or pmrA genes seen in certain Gram-positive bacteria.

Mechanism of Resistance

The mechanism of action for fluoroquinolones, including moxifloxacin, is different from that of macrolides, beta-lactams, aminoglycosides, or tetracyclines; therefore, microorganisms resistant to these classes of drugs may be susceptible to moxifloxacin. Resistance to fluoroquinolones occurs primarily by a mutation in topoisomerase II (DNA gyrase) or topoisomerase IV genes, decreased outer membrane permeability or drug efflux. In vitro resistance to moxifloxacin develops slowly via multiple-step mutations. Resistance to moxifloxacin occurs in vitro at a general frequency of between 1.8 x 10-9 to < 1 x 10-11 for Gram-positive bacteria.

Cross Resistance

Cross-resistance has been observed between moxifloxacin and other fluoroquinolones against Gram-negative bacteria. Gram-positive bacteria resistant to other fluoroquinolones may, however, still be susceptible to moxifloxacin. There is no known cross-resistance between moxifloxacin and other classes of antimicrobials.

Moxifloxacin has been shown to be active against most isolates of the following bacteria, both in vitro and in clinical infections . [see INDICATIONS AND USAGE].

Gram-positive bacteria
  • Enterococcus faecalis
  • Staphylococcus aureus
  • Streptococcus anginosus
  • Streptococcus constellatus
  • Streptococcus pneumoniae (including multi-drug resistant isolates [MDRSP] **)
  • Streptococcus pyogenes

**MDRSP, Multi-drug resistant Streptococcus pneumoniae includes isolates previously known as PRSP (Penicillinresistant S. pneumoniae), and are isolates resistant to two or more of the following antibiotics: penicillin (MIC) ≥ 2 mcg/mL), 2nd generation cephalosporins (for example, cefuroxime), macrolides, tetracyclines, and trimethoprim/sulfamethoxazole.

Gram-negative bacteria
  • Enterobacter cloacae
  • Escherichia coli
  • Haemophilus influenzae
  • Haemophilus parainfluenzae
  • Klebsiella pneumoniae
  • Moraxella catarrhalis
  • Proteus mirabilis
Anaerobic bacteria
  • Bacteroides fragilis
  • Bacteroides thetaiotaomicron
  • Clostridium perfringens
  • Peptostreptococcus species
  • Other microorganisms
  • Chlamydophila pneumoniae
  • Mycoplasma pneumoniae

The following in vitro data are available, but their clinical significance is unknown. At least 90 percent of the following bacteria exhibit an in vitro minimum inhibitory concentration (MIC) less than or equal to the susceptible breakpoint for moxifloxacin. However, the efficacy of AVELOX in treating clinical infections due to these bacteria has not been established in adequate and well controlled clinical trials.

Gram-positive bacteria
  • Staphylococcus epidermidis
  • Streptococcus agalactiae
  • Streptococcus viridans group
Gram-negative bacteria
  • Citrobacter freundii
  • Klebsiella oxytoca
  • Legionella pneumophila
Anaerobic bacteria
  • Fusobacterium species
  • Prevotella species

Susceptibility Tests Methods

When available, the clinical microbiology laboratory should provide the results of in vitro susceptibility test results for antimicrobial drug products used in resident hospitals to the physician as periodic reports that describe the susceptibility profile of nosocomial and community acquired pathogens. These reports should aid the physician in selecting an antibacterial drug product for treatment.

  • Dilution Techniques:
    Quantitative methods are used to determine antimicrobial minimum inhibitory concentrations (MICs). These MICs provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MICs should be determined using a standardized procedure. Standardized procedures are based on a dilution method (broth and/or agar). 1 The MIC values should be interpreted according to the criteria in Table 8.
  • Diffusion Techniques:
    Quantitative methods that require measurement of zone diameters can also provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. The zone size provides an estimate of the susceptibility of bacteria to antimicrobial compounds. The zone size prove should be determined using a standardized test method.2,3 This procedure uses paper disks impregnated with 5 mcg moxifloxacin to test the susceptibility of bacteria to moxifloxacin. The disc diffusion interpretive criteria are provided in Table 8.
  • Anaerobic Techniques:
    For anaerobic bacteria, the susceptibility to moxifloxacin can be determined by a standardized test method.4 The MIC values obtained should be interpreted according to the criteria provided in Table 8.

Table 8: Susceptibility Test Interpretive Criteria for Moxifloxacin

Species MIC (mcg/mL) Zone Diameter (mm)
S I R S I R
Enterobacteriacae ≤ 2 4 ≥ 8 ≥ 19 16–18 ≤ 15
Enterococcus faecalis ≤ 1 2 ≥ 4 ≥ 18 15–17 ≤ 14
Staphylococcus aureus ≤ 2 4 ≥ 8 ≥ 19 16–18 ≤ 15
Haemophilus influenzaea ≤ 1 - - ≥ 18 -
Haemophilus parainfluenzaea ≤ 1 - ≥ 18 -
Streptococcus pneumoniae ≤ 1 2 ≥ 4 ≥ 18 15–17 ≤ 14d
Streptococcus species ≤ 1 2 ≥ 4 ≥ 18 15–17 ≤ 14d
Anaerobic bacteria ≤ 2 4 ≥ 8 - - -
S=susceptible, I=Intermediate, and R=resistant.
a The current absence of data on moxifloxacin-resistant isolates precludes defining any results other than “Susceptible”. Isolates yielding test results (MIC or zone diameter) other than susceptible, should be submitted to a reference laboratory for additional testing.

A report of “Susceptible” indicates that the antimicrobial is likely to inhibit growth of the pathogen if the antimicrobial compound reaches the concentrations at the infection site necessary to inhibit growth of the pathogen. A report of “Intermediate” indicates that the result should be considered equivocal, and, if the microorganism is not fully susceptible to alternative, clinically feasible drugs, the test should be repeated. This category implies possible clinical applicability in body sites where the drug is physiologically concentrated or in situations where a high dosage of the drug product can be used. This category also provides a buffer zone that prevents small uncontrolled technical factors from causing major discrepancies in interpretation. A report of “Resistant” indicates that the antimicrobial is not likely to inhibit growth of the pathogen if the antimicrobial compound reaches the concentrations usually achievable at the infection site; other therapy should be selected.

  • Quality Control
    Standardized susceptibility test procedures require the use of laboratory controls to monitor and ensure the accuracy and precision of supplies and reagents used in the assay and the techniques of the individuals performing the test.1,2,3,4 Standard moxifloxacin powder should provide the following range of MIC values noted in Table 9. For the diffusion technique using the 5 mcg moxifloxacin disk, the criteria in Table 9 should be achieved.

Table 9: Acceptable Quality Control Ranges for Moxifloxacin

Strains MIC range (mcg/mL) Zone Diameter (mm)
Enterococcus faecalis ATCC 29212 0.06–0.5 -
Escherichia coli ATCC 25922 0.008–0.06 28–35
Haemophilus influenzae ATCC 49247 0.008–0.03 31–39
Staphylococcus aureus ATCC29213 0.015–0.06 -
Staphylococcus aureus ATCC25923 - 28–35
Streptococcus pneumoniae ATCC 49619 0.06–0.25 25–31
Bacteroides fragilis ATCC 25285 0.125–0.5 -
Bacteroides thetaiotaomicron ATCC 29741 1–4 -
Eubacterium lentum ATCC 43055 0.125–0.5 -

Animal Toxicology and/or Pharmacology

Quinolones have been shown to cause arthropathy in immature animals. In studies in juvenile dogs oral doses of moxifloxacin ≥ 30 mg/kg/day (approximately 1.5 times the maximum recommended human dose based upon systemic exposure) for 28 days resulted in arthropathy. There was no evidence of arthropathy in mature monkeys and rats at oral doses up to 135 and 500 mg/kg/day, respectively.

Moxifloxacin at an oral dose of 300 mg/kg did not show an increase in acute toxicity or potential for CNS toxicity (for example, seizures) in mice when used in combination with NSAIDs such as diclofenac, ibuprofen, or fenbufen. Some quinolones have been reported to have proconvulsant activity that is exacerbated with concomitant use of non-steroidal anti-inflammatory drugs (NSAIDs).

A QT-prolonging effect of moxifloxacin was found in dog studies, at plasma concentrations about five times the human therapeutic level. The combined infusion of sotalol, a Class III antiarrhythmic agent, with moxifloxacin induced a higher degree of QTc prolongation in dogs than that induced by the same dose (30 mg/kg) of moxifloxacin alone. Electrophysiological in vitro studies suggested an inhibition of the rapid activating component of the delayed rectifier potassium current (IKr) as an underlying mechanism.

No signs of local intolerability were observed in dogs when moxifloxacin was administered intravenously. After intraarterial injection, inflammatory changes involving the peri-arterial soft tissue were observed suggesting that intra-arterial administration of AVELOX should be avoided.

Clinical Studies

Acute Bacterial Exacerbation of Chronic Bronchitis

AVELOX Tablets (400 mg once daily for five days) were evaluated for the treatment of acute bacterial exacerbation of chronic bronchitis in a randomized, double-blind, controlled clinical trial conducted in the US. This study compared AVELOX with clarithromycin (500 mg twice daily for 10 days) and enrolled 629 patients. Clinical success was assessed at 7-17 days post-therapy. The clinical success for AVELOX was 89% (222/250) compared to 89% (224/251) for clarithromycin.

Table 10: Clinical Success Rates at Follow-Up Visit for Clinically Evaluable Patients by Pathogen (Acute Bacterial Exacerbation of Chronic Bronchitis)

PATHOGEN AVELOX Clarithromycin
Streptococcus pneumoniae 16/16 (100%) 20/23 (87%)
Haemophilus influenzae 33/37 (89%) 36/41 (88%)
Haemophilus parainfluenzae 16/16 (100%) 14/14 (100%)
Moraxella catarrhalis 29/34 (85%) 24/24 (100%)
Staphylococcus aureus 15/16 (94%) 6/8 (75%)
Klebsiella pneumoniae 18/20 (90%) 10/11 (91%)

The microbiological eradication rates (eradication plus presumed eradication) in AVELOX treated patients were Streptococcus pneumoniae 100%, Haemophilus influenzae 89%, Haemophilus parainfluenzae 100%, Moraxella catarrhalis 85%, Staphylococcus aureus 94%, and Klebsiella pneumoniae 85%.

Community Acquired Pneumonia

A randomized, double-blind, controlled clinical trial was conducted in the US to compare the efficacy of AVELOX Tablets (400 mg once daily) to that of high-dose clarithromycin (500 mg twice daily) in the treatment of patients with clinically and radiologically documented community acquired pneumonia. This study enrolled 474 patients (382 of whom were valid for the efficacy analysis conducted at the 14 - 35 day follow-up visit). Clinical success for clinically evaluable patients was 95% (184/194) for AVELOX and 95% (178/188) for high dose clarithromycin.

A randomized, double-blind, controlled trial was conducted in the US and Canada to compare the efficacy of sequential IV/PO AVELOX 400 mg QD for 7-14 days to an IV/PO fluoroquinolone control (trovafloxacin or levofloxacin) in the treatment of patients with clinically and radiologically documented community acquired pneumonia. This study enrolled 516 patients, 362 of whom were valid for the efficacy analysis conducted at the 7-30 day post-therapy visit. The clinical success rate was 86% (157/182) for AVELOX therapy and 89% (161/180) for the fluoroquinolone comparators.

An open-label ex-US study that enrolled 628 patients compared AVELOX to sequential IV/PO amoxicillin/clavulanate (1.2 g IV q8h/625 mg PO q8h) with or without high-dose IV/PO clarithromycin (500 mg BID). The intravenous formulations of the comparators are not FDA approved. The clinical success rate at Day 5-7 for AVELOX therapy was 93% (241/258) and demonstrated superiority to amoxicillin/clavulanate ± clarithromycin (85%, 239/280) [95% C.I. of difference in success rates between moxifloxacin and comparator (2.9%, 13.2%)]. The clinical success rate at the 21-28 days post-therapy visit for AVELOX was 84% (216/258), which also demonstrated superiority to the comparators (74%, 208/280) [95% C.I. of difference in success rates between moxifloxacin and comparator (2.6%, 16.3%)].

The clinical success rates by pathogen across four CAP studies are presented in Table 11.

Table 11: Clinical Success Rates By Pathogen (Pooled CAP Studies)

PATHOGEN AVELOX
Streptococcus pneumoniae 80/85 (94)
Staphylococcus aureus 17/20 (85)
Klebsiella pneumoniae 11/12 (92)
Haemophilus influenzae 56/61 (92)
Chlamydophila pneumoniae 119/128 (93)
Mycoplasma pneumoniae 73/76 (96)
Moraxella catarrhalis 11/12 (-92)

Community Acquired Pneumonia caused by Multi-Drug Resistant Streptococcus pneumoniae (MDRSP)*

AVELOX was effective in the treatment of community acquired pneumonia (CAP) caused by multi-drug resistant Streptococcus pneumoniae MDRSP* isolates. Of 37 microbiologically evaluable patients with MDRSP isolates, 35 patients (95%) achieved clinical and bacteriological success post-therapy. The clinical and bacteriological success rates based on the number of patients treated are shown in Table 12.

* MDRSP, Multi-drug resistant Streptococcus pneumoniae includes isolates previously known as PRSP (Penicillinresistant S. pneumoniae), and are isolates resistant to two or more of the following antibiotics: penicillin (MIC ≥ 2 mcg/mL), 2nd generation cephalosporins (for example, cefuroxime), macrolides, tetracyclines, and trimethoprim/sulfamethoxazole.

Table 12: Clinical and Bacteriological Success Rates for AVELOX-Treated MDRSP CAP Patients (Population: Valid for Efficacy)

Screening Susceptibility Clinical Success Bacteriological Success
n/Na % n/Nb %
Penicillin-resistant 21/21 100%c 21/21 100%c
2nd generation cephalosporin-resistant 25/26 96%c 25/26 96%c
Macrolide-resistantd 22/23 96% 22/23 96%
Trimethoprim/sulfamethoxazole-resistant 28/30 93% 28/30 93%
Tetracycline-resistant 17/18 94% 17/18 94%
a n = number of patients successfully treated; N = number of patients with MDRSP (from a total of 37 patients)
b n = number of patients successfully treated (presumed eradication or eradication); N = number of patients with MDRSP (from a total of 37 patients)
c One patient had a respiratory isolate that was resistant to penicillin and cefuroxime but a blood isolate that was intermediate to penicillin and cefuroxime. The patient is included in the database based on the respiratory isolate.
d
Azithromycin, clarithromycin, and erythromycin were the macrolide antimicrobials tested.

Not all isolates were resistant to all antimicrobial classes tested. Success and eradication rates are summarized in Table 13.

Table 13: Clinical Success Rates and Microbiological Eradication Rates for Resistant Streptococcus pneumoniae (Community Acquired Pneumonia)

S. pneumoniae with MDRSP Clinical Success Bacteriological Eradication Rate
Resistant to 2 antimicrobials 12/13 (92.3 %) 12/13 (92.3 %)
Resistant to 3 antimicrobials 10/11 (90.9 %)a 10/11 (90.9 %)a
Resistant to 4 antimicrobials 6/6 (100%) 6/6 (100%)
Resistant to 5 antimicrobials 7/7 (100%)a 7/7 (100%)a
Bacteremia with MDRSP 9/9 (100%) 9/9 (100%)
a One patient had a respiratory isolate resistant to 5 antimicrobials and a blood isolate resistant to 3 antimicrobials. The patient was included in the category resistant to 5 antimicrobials.

Acute Bacterial Sinusitis

In a controlled double-blind study conducted in the US, AVELOX Tablets (400 mg once daily for ten days) were compared with cefuroxime axetil (250 mg twice daily for ten days) for the treatment of acute bacterial sinusitis. The trial included 457 patients valid for the efficacy analysis. Clinical success (cure plus improvement) at the 7 to 21 day post-therapy test of cure visit was 90% for AVELOX and 89% for cefuroxime.

An additional non-comparative study was conducted to gather bacteriological data and to evaluate microbiological eradication in adult patients treated with AVELOX 400 mg once daily for seven days. All patients (n = 336) underwent antral puncture in this study. Clinical success rates and eradication/presumed eradication rates at the 21 to 37 day follow-up visit were 97% (29 out of 30) for Streptococcus pneumoniae, 83% (15 out of 18) for Moraxella catarrhalis, and 80% (24 out of 30) for Haemophilus influenzae.

Uncomplicated Skin and Skin Structure Infections

A randomized, double-blind, controlled clinical trial conducted in the US compared the efficacy of AVELOX 400 mg once daily for seven days with cephalexin HCl 500 mg three times daily for seven days. The percentage of patients treated for uncomplicated abscesses was 30%, furuncles 8%, cellulitis 16%, impetigo 20%, and other skin infections 26%. Adjunctive procedures (incision and drainage or debridement) were performed on 17% of the AVELOX treated patients and 14% of the comparator treated patients. Clinical success rates in evaluable patients were 89% (108/122) for AVELOX and 91% (110/121) for cephalexin HCl.

Complicated Skin and Skin Structure Infections

Two randomized, active controlled trials of cSSSI were performed. A double-blind trial was conducted primarily in North America to compare the efficacy of sequential IV/PO AVELOX 400 mg QD for 7-14 days to an IV/PO beta-lactam/betalactamase inhibitor control in the treatment of patients with cSSSI. This study enrolled 617 patients, 335 of which were valid for the efficacy analysis. A second open-label International study compared AVELOX 400 mg QD for 7-21 days to sequential IV/PO beta-lactam/beta-lactamase inhibitor control in the treatment of patients with cSSSI. This study enrolled 804 patients, 632 of which were valid for the efficacy analysis. Surgical incision and drainage or debridement was performed on 55% of the AVELOX treated and 53% of the comparator treated patients in these studies and formed an integral part of therapy for this indication. Success rates varied with the type of diagnosis ranging from 61% in patients with infected ulcers to 90% in patients with complicated erysipelas. These rates were similar to those seen with comparator drugs. The overall success rates in the evaluable patients and the clinical success by pathogen are shown in Tables 14 and 15.

Table 14: Overall Clinical Success Rates in Patients with Complicated Skin and Skin Structure Infections

Study AVELOX n/ N (%) Comparator n/N (%) 95% Confidence Interval*
North America 125/162 (77.2%) 141/173 (81.5%) (-14.4%, 2%)
International 254/315 (80.6%) 268/317 (84.5%) (-9.4%, 2.2%)
*of difference in success rates between Moxifloxacin and comparator (Moxifloxacin – comparator)

Table 15: Clinical Success Rates by Pathogen in Patients with Complicated Skin and Skin Structure Infections

Pathogen AVELOX n/ N (%) Comparator n/N (%)
Staphylococcus aureus (methicillin-susceptible isolates)a 106/129 (82.2%) 120/137 (87.6%)
Escherichia coli 31/38 (81.6 %) 28/33 (84.8 %)
Klebsiella pneumoniae 11/12 (91.7 % ) 7/10 (70%)
Enterobacter cloacae 9/11 (81.8%) 4/7 (57.1%)
a methicillin susceptibility was only determined in the North American Study

Complicated Intra-Abdominal Infections

Two randomized, active controlled trials of cIAI were performed. A double-blind trial was conducted primarily in North America to compare the efficacy of sequential IV/PO AVELOX 400 mg QD for 5-14 days to IV/ piperacillin/tazobactam followed by PO amoxicillin/clavulanic acid in the treatment of patients with cIAI, including peritonitis, abscesses, appendicitis with perforation, and bowel perforation. This study enrolled 681 patients, 379 of which were considered clinically evaluable. A second open-label international study compared AVELOX 400 mg QD for 5-14 days to IV ceftriaxone plus IV metronidazole followed by PO amoxicillin/clavulanic acid in the treatment of patients with cIAI. This study enrolled 595 patients, 511 of which were considered clinically evaluable. The clinically evaluable population consisted of subjects with a surgically confirmed complicated infection, at least 5 days of treatment and a 25-50 day follow-up assessment for patients at the Test of Cure visit. The overall clinical success rates in the clinically evaluable patients are shown in Table 16.

Table 16: Clinical Success Rates in Patients with Complicated Intra-Abdominal Infections

Study AVELOX n/ N (%) Comparator n/N (%) 95% Confidence Interval*
North America (overall) 146/183 (79.8 %) 153/196 (78.1 %) (-7.4%, 9.3%)
  Abscess 40/57 (70.2 %) 49/63 (77.8 %)a NAb
  Non-abscess 106/126 (84.1 %) 104/133 (78.2 %) NA
International (overall) 199/246 (80.9 %) 218/265 (82.3 %) (-8.9 %, 4.2%)
  Abscess 73/93 (78.5 %) 86/99 (86.9 %) NA
  Non-abscess 126/153 (82.4 %) 132/166 (79.5 %) NA
* of difference in success rates between AVELOX and comparator (AVELOX – comparator)
a Excludes 2 patients who required additional surgery within the first 48 hours.
b NA - not applicable

REFERENCES

1. Clinical and Laboratory Standards Institute (CLSI), Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria That Grow Aerobically 9th edition. Approved Standard CLSI Document M7-A9, CLSI, 950 West Valley Rd., Suite 2500, Wayne, PA 19087, 2012.

2. CLSI , Performance Standards for Antimicrobial Susceptibility Testing 22 Informational Supplement. CLSI Document M100-S22, 2012.

3. CLSI , Performance Standards for Antimicrobial Disk Susceptibility Tests 11th edition. Approved Standard CLSI Document M2-A11, 2012.

4. CLSI , Methods for Antimicrobial Susceptibility Testing of Anaerobic Bacteria 8th edition; Approved Standard CLSI Document M11-A8, 2012

Last reviewed on RxList: 10/9/2012
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

Advise patients:

  • To undergo routine blood pressure monitoring and to contact their health care provider if blood pressure is elevated.
  • To immediately contact their health care provider for unusual bleeding, high fever, rigors, sudden onset of worsening neurological function, or persistent or severe abdominal pain, severe constipation, or vomiting.
  • Of increased risk of wound healing complications during and following Avastin.
  • Of increased risk of an arterial thromboembolic event.
  • Of the potential risk to the fetus during and following Avastin and the need to continue adequate contraception for at least 6 months following last dose of Avastin.
  • Of the increased risk for ovarian failure following Avastin treatment.

Last reviewed on RxList: 11/6/2012
This monograph has been modified to include the generic and brand name in many instances.

>

PATIENT INFORMATION

Advise patients:

  • To undergo routine blood pressure monitoring and to contact their health care provider if blood pressure is elevated.
  • To immediately contact their health care provider for unusual bleeding, high fever, rigors, sudden onset of worsening neurological function, or persistent or severe abdominal pain, severe constipation, or vomiting.
  • Of increased risk of wound healing complications during and following Avastin.
  • Of increased risk of an arterial thromboembolic event.
  • Of the potential risk to the fetus during and following Avastin and the need to continue adequate contraception for at least 6 months following last dose of Avastin.
  • Of the increased risk for ovarian failure following Avastin treatment.

Last reviewed on RxList: 11/6/2012
This monograph has been modified to include the generic and brand name in many instances.

Disclaimer

Avelox Consumer

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

MOXIFLOXACIN - ORAL

(mox-ih-FLOX-uh-sin)

COMMON BRAND NAME(S): Avelox

WARNING: This medication may rarely cause tendon damage (e.g., tendinitis, tendon rupture) during or after treatment. Your risk for tendon problems is greater if you are over 60 years of age, if you are taking corticosteroids (such as prednisone), or if you have had a kidney, heart or lung transplant. Stop exercising, rest, and seek immediate medical attention if you develop joint/muscle/tendon pain or swelling.

Moxifloxacin should not be used in patients with myasthenia gravis. It may cause the condition to become worse. Seek immediate medical attention if you develop muscle weakness or trouble breathing.

USES: Moxifloxacin is used to treat a variety of bacterial infections. This medication belongs to a class of drugs called quinolone antibiotics. It works by stopping the growth of bacteria.

This antibiotic treats only bacterial infections. It will not work for virus infections (e.g., common cold, flu). Unnecessary use or overuse of any antibiotic can lead to its decreased effectiveness.

HOW TO USE: Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start using moxifloxacin and each time you get a refill. If you have any questions regarding the information, consult your doctor or pharmacist.

Take this medication by mouth with or without food, usually once daily or as directed by your doctor. The dosage and length of treatment is based on your medical condition and response to treatment. Drink plenty of fluids while taking this drug unless your doctor tells you otherwise.

Take this medication at least 4 hours before or 8 hours after taking any drugs that contain magnesium or aluminum. Some examples include quinapril, certain forms of didanosine (chewable/dispersible buffered tablets or pediatric oral solution), vitamins/minerals, and antacids. Follow the same instructions if you take bismuth subsalicylate, sucralfate, iron, and zinc. These medications bind with moxifloxacin and prevent its full absorption.

Antibiotics work best when the amount of medicine in your body is kept at a constant level. It is important not to miss a dose. To help you remember, take this medication at the same time every day.

Continue to take this medication until the full prescribed amount is finished, even if symptoms disappear after a few days. Stopping the medication too early may allow bacteria to continue to grow, which may result in a return of the infection.

Tell your doctor if your condition persists or worsens.

Disclaimer

Avelox Consumer (continued)

SIDE EFFECTS: See also Warning section.

Nausea, diarrhea, dizziness, lightheadedness, headache, weakness, or trouble sleeping may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these rare but very serious side effects occur: unusual bruising/bleeding, signs of a new infection (e.g., new/persistent fever, persistent sore throat), unusual change in the amount of urine, signs of liver problems (e.g., unusual tiredness, stomach/abdominal pain, persistent nausea/vomiting, yellowing eyes/skin, dark urine).

Seek immediate medical attention if any of these rare but very serious side effects occur: severe/persistent headache, vision changes, shaking (tremors), seizures, severe dizziness, fainting, fast/irregular heartbeat, mental/mood changes (e.g., anxiety, confusion, hallucinations, depression, rare thoughts of suicide).

Moxifloxacin may rarely cause serious nerve problems that may be reversible if identified and treated early. Seek immediate medical attention if you develop any of the following symptoms: pain/numbness/burning/tingling/weakness in any part of the body, changes in how you sense touch/pain/temperature/body position/vibration.

This medication may rarely cause a severe intestinal condition (Clostridium difficile-associated diarrhea) due to a type of resistant bacteria. This condition may occur during treatment or weeks to months after treatment has stopped. Do not use anti-diarrhea products or narcotic pain medications if you have any of the following symptoms because these products may make them worse. Tell your doctor immediately if you develop: persistent diarrhea, abdominal or stomach pain/cramping, blood/mucus in your stool.

Use of this medication for prolonged or repeated periods may result in oral thrush or a new vaginal yeast infection. Contact your doctor if you notice white patches in your mouth, a change in vaginal discharge, or other new symptoms.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Read the Avelox (moxifloxacin hcl) Side Effects Center for a complete guide to possible side effects »

PRECAUTIONS: Before taking moxifloxacin, tell your doctor or pharmacist if you are allergic to it; or to other quinolone antibiotics (e.g., ciprofloxacin, levofloxacin); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, heart problems (e.g., recent heart attack), joint/tendon problems (e.g., tendonitis, bursitis), liver disease, myasthenia gravis, nervous system disorder (e.g., peripheral neuropathy), seizure disorder, conditions that increase your risk of seizures (e.g., brain/head injury, brain tumors, cerebral atherosclerosis).

Moxifloxacin may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that require immediate medical attention. The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may affect the heart rhythm (see also Drug Interactions section). Before using moxifloxacin, tell your doctor or pharmacist if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using moxifloxacin safely.

This medication may rarely cause serious changes in blood sugar levels, especially if you have diabetes. Watch for symptoms of high blood sugar including increased thirst and urination. Also watch for symptoms of low blood sugar such as nervousness, shakiness, fast heartbeat, sweating, or hunger. Check your blood sugar regularly as directed by your doctor and report any changes. If you experience symptoms of low blood sugar, you may raise your blood sugar by using glucose tablets/gel or eating a quick source of sugar such as table sugar, honey, or candy, or drink fruit juice or non-diet soda. Tell your doctor immediately about the reaction and the use of this product. To help prevent low blood sugar, eat meals on a regular schedule, and do not skip meals.

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

This medication may make you more sensitive to the sun. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen and wear protective clothing when outdoors.

Caution is advised when using this drug in children because they may be more sensitive to its possible side effects (e.g., joint/tendon problems). Discuss the risks and benefits with the doctor.

Older adults may be more sensitive to the side effects of this medication such as heart problems or tendon problems. The risk for tendon problems is higher if they are also taking corticosteroids (e.g., prednisone, hydrocortisone).

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

Disclaimer

Avelox Consumer (continued)

DRUG INTERACTIONS: See also How to Use section.

Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with them first.

This drug should not be used with the following medication because very serious interactions may occur: strontium.

If you are currently using the medication listed above, tell your doctor or pharmacist before starting moxifloxacin.

Many drugs besides moxifloxacin may affect the heart rhythm (QT prolongation), including amiodarone, dofetilide, procainamide, quinidine, sotalol, certain macrolide antibiotics (e.g., erythromycin, clarithromycin), and certain antipsychotic medications (e.g., pimozide, thioridazine, ziprasidone), among others. Therefore, before using moxifloxacin, report all medications you are currently using to your doctor or pharmacist.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: live bacterial vaccines (e.g., typhoid, BCG), corticosteroids (e.g., prednisone, hydrocortisone), drugs for diabetes (e.g., glyburide, insulin), nonsteroidal anti-inflammatory drugs (NSAIDs such as ibuprofen, naproxen), warfarin.

Also report the use of drugs that might increase seizure risk when combined with this medication such as isoniazid (INH), phenothiazines (e.g., chlorpromazine), theophylline, or tricyclic antidepressants (e.g., amitriptyline), among others. Consult your doctor or pharmacist for details.

Although most antibiotics probably do not affect hormonal birth control such as pills, patch, or ring, some antibiotics may decrease their effectiveness. This could cause pregnancy. Examples include rifamycins such as rifampin or rifabutin. Be sure to ask your doctor or pharmacist if you should use additional reliable birth control methods while using this antibiotic.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Do not share this medication with others.

This medication has been prescribed for your current condition only. Do not use it later for another infection unless told to do so by your doctor. A different medication may be necessary in that case.

Laboratory and/or medical tests (e.g., liver function, complete blood count, blood glucose) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised December 2011. Copyright(c) 2011 First Databank, Inc.

Avelox Patient Information Including Side Effects

Brand Names: Avelox

Generic Name: moxifloxacin (Pronunciation: moxi FLOX a sin)

What is moxifloxacin (Avelox)?

Moxifloxacin is an antibiotic in a group of drugs called fluoroquinolones (flor-o-KWIN-o-lones). Moxifloxacin fights bacteria in the body.

Moxifloxacin is used to treat different types of bacterial infections.

Moxifloxacin may also be used for purposes not listed in this medication guide.

Avelox 400 mg

oblong, red, imprinted with M400, BAYER

What are the possible side effects of moxifloxacin (Avelox)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using moxifloxacin and call your doctor at once if you have a serious side effect such as:

  • severe dizziness, fainting, fast or pounding heartbeats;
  • sudden pain, snapping or popping sound, bruising, swelling, tenderness, stiffness, or loss of movement in any of your joints;
  • diarrhea that is watery or bloody;
  • confusion, hallucinations, depression, insomnia or nightmares, unusual thoughts or behavior, feeling light-headed;
  • seizure (convulsions);
  • pale or yellowed skin, dark colored urine, fever, weakness;
  • urinating less than usual or not at all;
  • easy bruising or bleeding;
  • numbness, tingling, or unusual pain anywhere in your body;
  • the first sign of any skin rash, no matter how mild; or
  • severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Less serious side effects may include:

  • nausea, mild diarrhea;
  • headache, dizziness;
  • blurred vision;
  • feeling nervous, anxious, or agitated;
  • mild skin itching.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the Avelox (moxifloxacin hcl) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about moxifloxacin (Avelox)?

You should not use this medication if you have a history of myasthenia gravis, or if you are allergic to moxifloxacin or similar antibiotics such as ciprofloxacin (Cipro), gemifloxacin (Factive), levofloxacin (Levaquin), ofloxacin (Floxin), norfloxacin (Noroxin), and others.

Before taking moxifloxacin, tell your doctor if you have a heart rhythm disorder, kidney or liver disease, joint problems, a history of seizures, low levels of potassium in your blood (hypokalemia), muscle weakness or trouble breathing, a personal or family history of Long QT syndrome, or if you have ever had an allergic reaction to an antibiotic.

Avoid taking antacids, vitamin or mineral supplements, sucralfate (Carafate), or didanosine (Videx) powder or chewable tablets within 8 hours before or 4 hours after you take moxifloxacin. These other medicines can make moxifloxacin much less effective when taken at the same time.

Taking moxifloxacin can make your skin more sensitive to sunlight. Avoid exposure to sunlight, sun lamps, or tanning beds.

Moxifloxacin may cause swelling or tearing of a tendon (the fiber that connects bones to muscles in the body), especially in the Achilles' tendon of the heel. These effects may be more likely to occur if you are over 60, if you take steroid medication, or if you have had a kidney, heart, or lung transplant. Stop taking moxifloxacin and call your doctor at once if you have sudden pain, swelling, tenderness, stiffness, or movement problems in any of your joints. Rest the joint until you receive medical care or instructions.

Do not share this medication with another person (especially a child), even if they have the same symptoms you do.

Side Effects Centers

Avelox Patient Information including How Should I Take

What should I discuss with my healthcare provider before taking moxifloxacin (Avelox)?

You should not use this medication if you have a history of myasthenia gravis, or if you are allergic to moxifloxacin or similar antibiotics such as ciprofloxacin (Cipro), gemifloxacin (Factive), levofloxacin (Levaquin), ofloxacin (Floxin), norfloxacin (Noroxin), and others.

To make sure you can safely take moxifloxacin, tell your doctor if you have any of these other conditions:

  • a history of allergic reaction to an antibiotic;
  • heart rhythm disorder, especially if you take quinidine (Quin-G), disopyramide (Norpace), bretylium (Bretylol), procainamide (Pronestyl, Procan SR), amiodarone (Cordarone, Pacerone), or sotalol (Betapace);
  • joint problems;
  • kidney or liver disease, cirrhosis;
  • epilepsy or a history of seizures;
  • muscle weakness or trouble breathing;
  • low levels of potassium in your blood (hypokalemia); or
  • a personal or family history of "Long QT syndrome."

FDA pregnancy category C. It is not known whether moxifloxacin will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

It is not known whether moxifloxacin passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are using moxifloxacin.

Moxifloxacin may cause swelling or tearing of a tendon (the fiber that connects bones to muscles in the body), especially in the Achilles' tendon of the heel. These effects may be more likely to occur if you are over 60, if you take steroid medication, or if you have had a kidney, heart, or lung transplant. Stop taking moxifloxacin and call your doctor at once if you have sudden pain, swelling, tenderness, stiffness, or movement problems in any of your joints. Rest the joint until you receive medical care or instructions.

Do not share this medication with another person (especially a child), even if they have the same symptoms you do.

How should I take moxifloxacin (Avelox)?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Take moxifloxacin with a full glass of water (8 ounces). Drink several extra glasses of fluid each day while you are taking moxifloxacin.

Moxifloxacin may be taken with or without food, but take it at the same time each day.

Take this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Moxifloxacin will not treat a viral infection such as the common cold or flu.

Store at room temperature away from moisture and heat.

Side Effects Centers

Avelox Patient Information including If I Miss a Dose

What happens if I miss a dose (Avelox)?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose (Avelox)?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include tremors, nausea, vomiting, diarrhea, and seizures (convulsions).

What should I avoid while taking moxifloxacin (Avelox)?

You may be taking certain other medicines that should not be taken at the same time as moxifloxacin. Avoid taking the following medicines within 8 hours before or 4 hours after you take moxifloxacin. These other medicines can make moxifloxacin much less effective when taken at the same time:

  • antacids that contain magnesium or aluminum (such as Maalox, Mylanta, or Rolaids);
  • the ulcer medicine sucralfate (Carafate);
  • didanosine (Videx) powder or chewable tablets; or
  • vitamin or mineral supplements that contain iron or zinc.

Avoid exposure to sunlight or tanning beds. Moxifloxacin can make you sunburn more easily. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors. Call your doctor if you have severe burning, redness, itching, rash, or swelling after being in the sun.

Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you have diarrhea that is watery or bloody, stop taking moxifloxacin and call your doctor. Do not use anti-diarrhea medicine unless your doctor tells you to.

Moxifloxacin may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

What other drugs will affect moxifloxacin (Avelox)?

Tell your doctor about all other medicines you use, especially:

  • a blood thinner such as warfarin (Coumadin, Jantoven);
  • an antibiotic such as clarithromycin (Biaxin), erythromycin (E.E.S., EryPed, Ery-Tab, Erythrocin, Pediazole), levofloxacin (Levaquin), or pentamidine (NebuPent, Pentam);
  • an antidepressant such as amitriptylline (Elavil, Vanatrip, Limbitrol), clomipramine (Anafranil), or desipramine (Norpramin);
  • anti-malaria medications such as chloroquine (Aralen) or mefloquine (Lariam);
  • medicine to prevent or treat nausea and vomiting such as dolasetron (Anzemet), droperidol (Inapsine), or ondansetron (Zofran);
  • medicines to treat psychiatric disorders, such as chlorpromazine (Thorazine), clozapine (FazaClo, Clozaril), haloperidol (Haldol), pimozide (Orap), thioridazine (Mellaril), or ziprasidone (Geodon);
  • migraine headache medicine such as sumatriptan (Imitrex, Treximet) or zolmitriptan (Zomig);
  • narcotic medication such as methadone (Methadose, Diskets, Dolophine);
  • an NSAID (non-steroidal anti-inflammatory drug) such as ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn, Naprelan, Treximet), celecoxib (Celebrex), diclofenac (Arthrotec, Cambia, Cataflam, Voltaren, Flector Patch, Pennsaid, Solareze), indomethacin (Indocin), meloxicam (Mobic), and others; or
  • steroid medication (prednisone and others).

This list is not complete and other drugs may interact with moxifloxacin. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about moxifloxacin.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 8.01. Revision date: 4/13/2011.

Your use of the content provided in this service indicates that you have read,understood and agree to the End-User License Agreement,which can be accessed by clicking on this link.

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Side Effects Centers

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