بوسپیرون
Buspirone (Buspar)
بوسپیرون

نام ژنریک

Buspirone

شکل دارویی

اشكال دارويي:


Tablet: 5,10mg

موارد مصرف

موارد و مقدار مصرف


درمان اختلالات اضطرابي


بزرگسالان: ابتدا 5/7 ميلي‌گرم دو بار در روز از راه خوراكي مصرف مي‌شود. مقدار مصرف را مي‌توان هر دو تا سه روز به ميزان mg5 افزايش داد. مقدار معمول نگهدارنده mg/day30-20 به‌صورت منقسم است. مقدار مصرف نبايد از mg/day60 تجاوز كند.




مكانيسم اثر: اثر ضد اضطراب


بوسپيرون رفتار تهاجمي و كشمكش‌ زا را فرو مي‌نشاند و واكنشهاي گريز يا اجتناب (conditioned avoidance) را مهار مي‌كند. مكانيسم دقيق اثر دارو مشخص نيست، اما به نظر مي‌رسد به اثرات همزمان بر چندين نوروترانسميتر و گيرنده‌ مربوط مي‌شود. فعاليت عصبي سروتونين را كاهش و متابوليسم نوراپي‌نفرين را افزايش مي‌دهد و به طور نسبي به‌عنوان يك آنتاگونيست پيش‌سيناپسي دوپامين عمل مي‌كند. مطالعات به عمل آمده يك اثر غير مستقيم بر روي مجموعه گيرنده هاي بنزوديازپيني و GABA دارد.


بوسپيرون از نظر فارماكولوژيك ربطي به بنزوديازپينها، باربيتوراتها، يا ساير داروهاي ضداضطراب و تسكين بخش ندارد. اين دارو اثر باليني برجسته‌اي دارد و به طور منحصر به فردي ضد اضطراب است. اثر شل‌كنندة عضلاني يا ضد تشنج ندارد و به نظر نمي‌رسد سبب وابستگي جسمي يا تسكين‌بخشي قابل توجه شود.

موارد منع مصرف

تداخل دارويي


در صورت مصرف همزمان با مهاركننده‌هاي MAO، بوسپيرون ممكن است فشار خون را افزايش دهد. از مصرف همزمان آنها خودداري شود.


با فرآورده‌هاي حاوي الكل يا ساير داروهاي مضعف CNS با احتياط مصرف شود، زيرا ممكن است رخوت، بخصوص با مقادير بيش از mg/day30، بروز كند. بوسپيرون اختلال ذهني و عملكرد حركتي ناشي از الكل را افزايش نمي دهد. با اين وجود، اثرات CNS دارو در افراد قابل پيش‌بيني نيست. غلظت سرمي هالوپريدول ممكن است افزايش يابد.


مصرف همزمان مهاركننده‌ها يا القاكننده‌هاي سيتوكروم 3A4 مي‌تواند باعث تغيير سطح بوسپيرون شود.


مصرف همزمان با ديگوكسين مي‌تواند ديگوكسين را از محل اتصال آن جابجا نمايد. سطح ديگوكسين بايد ارزيابي شود.


بوسپيرون مي‌تواند سطح هالوپريدول را افزايش دهد، بنابراين در مصرف همزمان دوز هالوپريدول بايد كاهش داده شود.


ضد قارچ‌هاي آزولي باعث مهار متابوليسم گذر اول بوسپيرون مي‌شود.

موارد قابل توجه

-

تداخل دارویی

عوارض جانبي


اعصاب مركزي: سرگيجه، خواب آلودگي، عصبانيت، بيخوابي، سردرد، منگي، كرختي.


چشم: تاري ديد.


دستگاه گوارش: خشكي دهان، ‌تهوع، اسهال، ديسترس شكمي.




مسموميت و درمان


تظاهرات باليني: سرگيجه، خواب آلودگي، تنگي غيرمعمول مردمكها، تهوع و استفراغ.


درمان: علامتي و حمايتي است. محتويات معده با شستشوي سريع معده تخليه شود. تنفس، نبض و فشار خون بيمار پيگري گردد. پادزهر خاصي ندارد. اثر دياليز معلوم نيست.

مکانیزم اثر

عوارض جانبي


اعصاب مركزي: سرگيجه، خواب آلودگي، عصبانيت، بيخوابي، سردرد، منگي، كرختي.


چشم: تاري ديد.


دستگاه گوارش: خشكي دهان، ‌تهوع، اسهال، ديسترس شكمي.




مسموميت و درمان


تظاهرات باليني: سرگيجه، خواب آلودگي، تنگي غيرمعمول مردمكها، تهوع و استفراغ.


درمان: علامتي و حمايتي است. محتويات معده با شستشوي سريع معده تخليه شود. تنفس، نبض و فشار خون بيمار پيگري گردد. پادزهر خاصي ندارد. اثر دياليز معلوم نيست.

فارماكوكینتیك

موارد منع مصرف و احتياط


موارد منع مصرف: حساسيت مفرط به دارو يا تا 14 روز پس از مصرف مهاركننده‌هاي MAO.


موارد احتياط: اختلال كار كليه يا كبد.

سایر اطلاعات

طبقه‌بندي فارماكولوژيك: آزاسپيرودكانديون


طبقه‌بندي درماني: ضد اضطراب


طبقه‌بندي مصرف در بارداري: ردة B




نام‌هاي تجاري: BUSP

ملاحظات اختصاصي


1- بيماراني كه قبلاً با بنزوديازپين ها تحت درمان بوده اند، ممكن است پاسخ باليني خوبي به اين دارو ندهند.


2- اگرچه به نظر نمي‌رسد بوسپيرون سبب وابستگي جسمي يا رواني شود، ولي اين احتمال وجود دارد كه بيمار براي تجربهاين اثرات به سوء مصرف دارو دست بزند.


3- بوسپيرون سندرم قطع مصرف ناشي از بنزوديازپين ها يا ساير داروهاي خواب‌‌آور و تسكين‌بخش را مسدود نمي‌كند. از اين رو، مصرف اين داروها پيش از جايگزيني با بوسپيرون به تدريج قطع شود.


4- وضعيت عملكرد كبد و كليه بيمار پيگيري شود؛ اختلال كار كليه و كبد متابوليسم و دفع دارو را مختل كرده و ممكن است به تجمع سمي دارو منجر شود. كاهش مقدار مصرف ممكن است ضروري باشد.


5- بوسپيرون به صورت تحقيقاتي در درمان افسردگي غيرملانكوليك و سندرم پاركينسون استفاده شده است.


6- بعلت احتمال بروز اختلال شناختي توصيه مي‌شود بيماران از فعاليتهايي كه هوشياري كامل نياز دارند خودداري نمايند.


7- سندرم پاي بيقرار در برخي بيماران گزارش شده است كه مي‌تواند در ارتباط با اثرات آنتاگونيستي دوپاميني بوسپيرون باشد. بيمار از جهت علائم ديستوني، بي قراري و سودوپاركينسونيسم بررسي شود.


8- در بيماران با نارسايي كليه و كبد با احتياط مصرف شود.


9- در مصرف همزمان با MAOI‌ها ممكن است افزايش فشار خون رخ دهد، مصرف همزمان توصيه نمي‌شود.


10- ايمني و كارآيي دارو در كودكان زير 6 سال شناسايي نشده است. مطالعات در مورد مصرف طولاني دارو در كودكان در دسترس نيست.


11- بوسپيرون تحمل متقاطع با بنزوديازپين‌ها ندارد.




نكات قابل توصيه به بيمار


1- دارو را طبق دستور پزشك مصرف و از دو برابر كردن مقدار مصرف دارو خودداري كنيد. در صورت فراموشي يك نوبت مصرف مقدار فراموش شده را هرچه زودتر مصرف كنيد، مگر آنكه نوبت مصرف بعدي رسيده باشد.


2- تا مشخص شدن اثر دارو از انجام فعاليت هاي خطرناك اجتناب كنيد. اثرات الكل و ساير مضعفهاي CNS (مانند آنتي هيستامينها، تسكين‌بخشها، آرام‌بخشها، داروهاي خواب‌آور، ضد درد، باربيتوراتها، داروهاي ضد تشنج، شل كننده‌هاي عضلاني، داروهاي ضد سرماخوردگي، ضد سرفه يا آلرژي) ممكن است با رخوت و خواب‌آلودگي اضافي ناشي از بوسپيرون افزايش يابند.


3- دارو را دور از گرما و نور و دسترس كودكان نگهداري كنيد.


4- هرگونه عوارض جانبي را فوراً اطلاع دهيد.


مصرف در شيردهي: مطالعات بر روي حيوانات نشان داده است كه بوسپيرون و متابوليتهاي آن در شير موش صحرايي ترشح مي‌شوند. ميزان ترشح دارو در شير انسان مشخص نيست. در زنان شيرده نبايد تجويز شود.

Buspirone (Buspar)

BuSpar®
(buspirone HCl, USP)

DRUG DESCRIPTION

BuSpar® (buspirone hydrochloride tablets, USP) is an antianxiety agent that is not chemically or pharmacologically related to the benzodiazepines, barbiturates, or other sedative/anxiolytic drugs.

Buspirone hydrochloride is a white crystalline, water soluble compound with a molecular weight of 422.0. Chemically, buspirone hydrochloride is 8-[4-[4-(2-pyrimidinyl)-1piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione monohydrochloride. The empirical formula C21H31N5O2 •HCl is represented by the following structural formula:

BuSpar® (buspirone HCl, USP) Structural Formula Illustration

BuSpar (buspirone) is supplied as tablets for oral administration containing 5 mg, 10 mg, 15 mg, or 30 mg of buspirone hydrochloride, USP (equivalent to 4.6 mg, 9.1 mg, 13.7 mg, and 27.4 mg of buspirone free base, respectively). The 5 mg and 10 mg tablets are scored so they can be bisected. Thus, the 5 mg tablet can also provide a 2.5 mg dose, and the 10 mg tablet can provide a 5 mg dose. The 15 mg and 30 mg tablets are provided in the DIVIDOSE® tablet design. These tablets are scored so they can be either bisected or trisected. Thus, a single 15 mg tablet can provide the following doses: 15 mg (entire tablet), 10 mg (two thirds of a tablet), 7.5 mg (one half of a tablet), or 5 mg (one third of a tablet). A single 30 mg tablet can provide the following doses: 30 mg (entire tablet), 20 mg (two thirds of a tablet), 15 mg (one half of a tablet), or 10 mg (one third of a tablet). BuSpar (buspirone) Tablets contain the following inactive ingredients: colloidal silicon dioxide, lactose, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. The 30 mg tablet also contains iron oxide.

What are the possible side effects of buspirone (BuSpar, BuSpar Dividose)?

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

Call your doctor at once if you have any of these serious side effects:

  • feeling light-headed, fainting;
  • fast or uneven heart rate;
  • depressed mood, unusual thoughts or behavior; or
  • lack of balance or coordination.

Less serious side effects may be more likely to occur, such as:

  • drowsiness, dizziness, blurred vision;
  • feeling...

Read All Potential Side Effects and See Pictures of Buspar »

What are the precautions when taking buspirone (Buspar)?

Before taking buspirone, tell your doctor or pharmacist if you are allergic to it; 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.

This medication should not be used if you have certain medical conditions. Before using this medication, consult your doctor if you have: kidney problems, liver problems.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: bipolar disorder (manic-depression), Parkinson's disease.

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

Read All Potential Precautions of Buspar »

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

BuSpar (buspirone) is indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic.

The efficacy of BuSpar (buspirone) has been demonstrated in controlled clinical trials of outpatients whose diagnosis roughly corresponds to Generalized Anxiety Disorder (GAD). Many of the patients enrolled in these studies also had coexisting depressive symptoms and BuSpar (buspirone) relieved anxiety in the presence of these coexisting depressive symptoms. The patients evaluated in these studies had experienced symptoms for periods of 1 month to over 1 year prior to the study, with an average symptom duration of 6 months. Generalized Anxiety Disorder (300.02) is described in the American Psychiatric Association's Diagnostic and Statistical Manual, III1 as follows:

Generalized, persistent anxiety (of at least 1 month continual duration), manifested by symptoms from three of the four following categories:

  1. Motor tension: shakiness, jitteriness, jumpiness, trembling, tension, muscle aches, fatigability, inability to relax, eyelid twitch, furrowed brow, strained face, fidgeting, restlessness, easy startle.
  2. Autonomic hyperactivity: sweating, heart pounding or racing, cold, clammy hands, dry mouth, dizziness, lightheadedness, paresthesias (tingling in hands or feet), upset stomach, hot or cold spells, frequent urination, diarrhea, discomfort in the pit of the stomach, lump in the throat, flushing, pallor, high resting pulse and respiration rate.
  3. Apprehensive expectation: anxiety, worry, fear, rumination, and anticipation of misfortune to self or others.
  4. Vigilance and scanning: hyperattentiveness resulting in distractibility, difficulty in concentrating, insomnia, feeling “on edge,” irritability, impatience.

The above symptoms would not be due to another mental disorder, such as a depressive disorder or schizophrenia. However, mild depressive symptoms are common in GAD.

The effectiveness of BuSpar (buspirone) in long-term use, that is, for more than 3 to 4 weeks, has not been demonstrated in controlled trials. There is no body of evidence available that systematically addresses the appropriate duration of treatment for GAD. However, in a study of long-term use, 264 patients were treated with BuSpar (buspirone) for 1 year without ill effect. Therefore, the physician who elects to use BuSpar (buspirone) for extended periods should periodically reassess the usefulness of the drug for the individual patient.

DOSAGE AND ADMINISTRATION

The recommended initial dose is 15 mg daily (7.5 mg b.i.d.). To achieve an optimal therapeutic response, at intervals of 2 to 3 days the dosage may be increased 5 mg per day, as needed. The maximum daily dosage should not exceed 60 mg per day. In clinical trials allowing dose titration, divided doses of 20 mg to 30 mg per day were commonly employed.

The bioavailability of buspirone is increased when given with food as compared to the fasted state (see CLINICAL PHARMACOLOGY). Consequently, patients should take buspirone in a consistent manner with regard to the timing of dosing; either always with or always without food.

When buspirone is to be given with a potent inhibitor of CYP3A4, the dosage recommendations described in the PRECAUTIONS: DRUG INTERACTIONS section should be followed.

HOW SUPPLIED

BuSpar® (buspirone hydrochloride tablets, USP) Tablets, 5 mg and 10 mg (white, ovoid-rectangular with score, MJ logo, strength and the name BuSpar (buspirone) embossed) are available in bottles of 100.

5 mg tablets

NDC 0087-0818-41 Bottles of 100

10 mg tablets

NDC 0087-0819-41 Bottles of 100

Tablets, 15 mg white, in the DIVIDOSE® tablet design imprinted with the MJ logo, are available in bottles of 60 and 180. Tablets, 30 mg pink, in the DIVIDOSE® tablet design imprinted with the MJ logo, are available in bottles of 60. The 15 mg and 30 mg tablets are scored so that they can be either bisected or trisected. The 15 mg tablet has ID number 822 on one side and on the reverse side, the number 5 on each trisect segment. The 30 mg tablet has ID number 824 on one side and on the reverse side, the number 10 on each trisect segment.

15 mg tablets

NDC 0087-0822-32 Bottles of 60
NDC 0087-0822-33 Bottles of 180

30 mg tablets

NDC 0087-0824-81 Bottles of 60

Store at 25° C (77° F); excursions permitted between 15° C to 30° C (59° F to 86° F) [see USP controlled room temperature]. Dispense in a tight, light-resistant container (USP).

REFERENCE

1. American Psychiatric Association, Ed.: Diagnostic and Statistical Manual of Mental Disorders—III, American Psychiatric Association, May 1980.

Bristol-Myers Squibb Company Princeton, NJ 08543 USA. Rev November 2010

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

(See also PRECAUTIONS)

Commonly Observed

The more commonly observed untoward events associated with the use of BuSpar (buspirone) not seen at an equivalent incidence among placebo-treated patients include dizziness, nausea, headache, nervousness, lightheadedness, and excitement.

Associated with Discontinuation of Treatment

One guide to the relative clinical importance of adverse events associated with BuSpar (buspirone) is provided by the frequency with which they caused drug discontinuation during clinical testing. Approximately 10% of the 2200 anxious patients who participated in the BuSpar (buspirone) premarketing clinical efficacy trials in anxiety disorders lasting 3 to 4 weeks discontinued treatment due to an adverse event. The more common events causing discontinuation included: central nervous system disturbances (3.4%), primarily dizziness, insomnia, nervousness, drowsiness, and lightheaded feeling; gastrointestinal disturbances (1.2%), primarily nausea; and miscellaneous disturbances (1.1%), primarily headache and fatigue. In addition, 3.4% of patients had multiple complaints, none of which could be characterized as primary.

Incidence in Controlled Clinical Trials

The table that follows enumerates adverse events that occurred at a frequency of 1% or more among BuSpar (buspirone hydrochloride) patients who participated in 4-week, controlled trials comparing BuSpar (buspirone) with placebo. The frequencies were obtained from pooled data for 17 trials. The prescriber should be aware that these figures cannot be used to predict the incidence of side effects in the course of usual medical practice where patient characteristics and other factors differ from those which prevailed in the clinical trials. Similarly, the cited frequencies cannot be compared with figures obtained from other clinical investigations involving different treatments, uses, and investigators. Comparison of the cited figures, however, does provide the prescribing physician with some basis for estimating the relative contribution of drug and nondrug factors to the side-effect incidence rate in the population studied.

TREATMENT-EMERGENT ADVERSE EXPERIENCE INCIDENCE IN PLACEBO-CONTROLLED CLINICAL TRIALS* (Percent of Patients Reporting)

Adverse Experience BuSpar
(n=477)
Placebo
(n=464)
Cardiovascular
  Tachycardia/Palpitations 1 1
CNS
  Dizziness 12 3
  Drowsiness 10 9
  Nervousness 5 1
  Insomnia 3 3
  Lightheadedness 3
  Decreased Concentration 2 2
  Excitement 2
  Anger/Hostility 2
  Confusion 2
  Depression 2 2
EENT
  Blurred Vision 2
Gastrointestinal
  Nausea 8 5
  Dry Mouth 3 4
  Abdominal/Gastric Distress 2 2
  Diarrhea  2
  Constipation 1 2
  Vomiting 1 2
Musculoskeletal
  Musculoskeletal Aches/Pains 1
Neurological
  Numbness 2
  Paresthesia 1
  Incoordination 1
  Tremor 1
Skin
  Skin Rash 1
Miscellaneous
  Headache 6 3
  Fatigue 4 4
  Weakness 2
  Sweating/Clamminess 1
*Events reported by at least 1% of BuSpar (buspirone) patients are included.
—Incidence less than 1%.

 Other Events Observed During the Entire Premarketing Evaluation of BuSpar (buspirone)

During its premarketing assessment, BuSpar (buspirone) was evaluated in over 3500 subjects. This section reports event frequencies for adverse events occurring in approximately 3000 subjects from this group who took multiple doses of BuSpar (buspirone) in the dose range for which BuSpar (buspirone) is being recommended (ie, the modal daily dose of BuSpar (buspirone) fell between 10 mg and 30 mg for 70% of the patients studied) and for whom safety data were systematically collected. The conditions and duration of exposure to BuSpar (buspirone) varied greatly, involving well-controlled studies as well as experience in open and uncontrolled clinical settings. As part of the total experience gained in clinical studies, various adverse events were reported. In the absence of appropriate controls in some of the studies, a causal relationship to BuSpar (buspirone hydrochloride) treatment cannot be determined. The list includes all undesirable events reasonably associated with the use of the drug.

The following enumeration by organ system describes events in terms of their relative frequency of reporting in this data base. Events of major clinical importance are also described in the PRECAUTIONS section.

The following definitions of frequency are used: Frequent adverse events are defined as those occurring in at least 1/100 patients. Infrequent adverse events are those occurring in 1/100 to 1/1000 patients, while rare events are those occurring in less than 1/1000 patients.

Cardiovascular

Frequent was nonspecific chest pain; infrequent were syncope, hypotension, and hypertension; rare were cerebrovascular accident, congestive heart failure, myocardial infarction, cardiomyopathy, and bradycardia.

Central Nervous System

Frequent were dream disturbances; infrequent were depersonalization, dysphoria, noise intolerance, euphoria, akathisia, fearfulness, loss of interest, dissociative reaction, hallucinations, involuntary movements, slowed reaction time, suicidal ideation, and seizures; rare were feelings of claustrophobia, cold intolerance, stupor, and slurred speech and psychosis.

EENT

Frequent were tinnitus, sore throat, and nasal congestion; infrequent were redness and itching of the eyes, altered taste, altered smell, and conjunctivitis; rare were inner ear abnormality, eye pain, photophobia, and pressure on eyes.

Endocrine

Rare were galactorrhea and thyroid abnormality.

Gastrointestinal

Infrequent were flatulence, anorexia, increased appetite, salivation, irritable colon, and rectal bleeding; rare was burning of the tongue.

Genitourinary

Infrequent were urinary frequency, urinary hesitancy, menstrual irregularity and spotting, and dysuria; rare were amenorrhea, pelvic inflammatory disease, enuresis, and nocturia.

Musculoskeletal

Infrequent were muscle cramps, muscle spasms, rigid/stiff muscles, and arthralgias; rare was muscle weakness.

Respiratory

Infrequent were hyperventilation, shortness of breath, and chest congestion; rare was epistaxis.

Sexual Function

Infrequent were decreased or increased libido; rare were delayed ejaculation and impotence.

Skin

Infrequent were edema, pruritus, flushing, easy bruising, hair loss, dry skin, facial edema, and blisters; rare were acne and thinning of nails.

Clinical Laboratory

Infrequent were increases in hepatic aminotransferases (SGOT, SGPT); rare were eosinophilia, leukopenia, and thrombocytopenia.

Miscellaneous

Infrequent were weight gain, fever, roaring sensation in the head, weight loss, and malaise; rare were alcohol abuse, bleeding disturbance, loss of voice, and hiccoughs.

Postmarketing Experience

Postmarketing experience has shown an adverse experience profile similar to that given above. Voluntary reports since introduction have included rare occurrences of allergic reactions (including urticaria), angioedema, cogwheel rigidity, dizziness (rarely reported as vertigo), dystonic reactions (including dystonia), ataxias, extrapyramidal symptoms, dyskinesias (acute and tardive), ecchymosis, emotional lability, serotonin syndrome, transient difficulty with recall, urinary retention, visual changes (including tunnel vision), parkinsonism, akathisia, restless leg syndrome, and restlessness. Because of the uncontrolled nature of these spontaneous reports, a causal relationship to BuSpar (buspirone) treatment has not been determined.

Drug Abuse And Dependence

Controlled Substance Class

BuSpar (buspirone hydrochloride) is not a controlled substance.

Physical and Psychological Dependence

In human and animal studies, buspirone has shown no potential for abuse or diversion and there is no evidence that it causes tolerance, or either physical or psychological dependence. Human volunteers with a history of recreational drug or alcohol usage were studied in two double-blind clinical investigations. None of the subjects were able to distinguish between BuSpar (buspirone) and placebo. By contrast, subjects showed a statistically significant preference for methaqualone and diazepam. Studies in monkeys, mice, and rats have indicated that buspirone lacks potential for abuse.

Following chronic administration in the rat, abrupt withdrawal of buspirone did not result in the loss of body weight commonly observed with substances that cause physical dependency.

Although there is no direct evidence that BuSpar (buspirone) causes physical dependence or drug-seeking behavior, it is difficult to predict from experiments the extent to which a CNS-active drug will be misused, diverted, and/or abused once marketed. Consequently, physicians should carefully evaluate patients for a history of drug abuse and follow such patients closely, observing them for signs of BuSpar (buspirone) misuse or abuse (eg, development of tolerance, incrementation of dose, drug-seeking behavior).

Read the Buspar (buspirone) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

Psychotropic Agents

MAO inhibitors: It is recommended that BuSpar (buspirone) not be used concomitantly with MAO inhibitors (see WARNINGS).

Amitriptyline: After addition of buspirone to the amitriptyline dose regimen, no statistically significant differences in the steady-state pharmacokinetic parameters (Cmax, AUC, and Cmin) of amitriptyline or its metabolite nortriptyline were observed.

Diazepam: After addition of buspirone to the diazepam dose regimen, no statistically significant differences in the steady-state pharmacokinetic parameters (Cmax, AUC, and Cmin) were observed for diazepam, but increases of about 15% were seen for nordiazepam, and minor adverse clinical effects (dizziness, headache, and nausea) were observed.

Haloperidol: In a study in normal volunteers, concomitant administration of buspirone and haloperidol resulted in increased serum haloperidol concentrations. The clinical significance of this finding is not clear.

Nefazodone: (see Inhibitors and Inducers of Cytochrome P450 3A4 [CYP3A4])

Trazodone: There is one report suggesting that the concomitant use of Desyrel® (trazodone hydrochloride) and buspirone may have caused 3- to 6-fold elevations on SGPT (ALT) in a few patients. In a similar study attempting to replicate this finding, no interactive effect on hepatic transaminases was identified.

Triazolam/Flurazepam: Coadministration of buspirone with either triazolam or flurazepam did not appear to prolong or intensify the sedative effects of either benzodiazepine.

Other Psychotropics: Because the effects of concomitant administration of buspirone with most other psychotropic drugs have not been studied, the concomitant use of buspirone with other CNS-active drugs should be approached with caution.

Inhibitors and Inducers of Cytochrome P450 3A4 (CYP3A4)

Buspirone has been shown in vitro to be metabolized by CYP3A4. This finding is consistent with the in vivo interactions observed between buspirone and the following:

Diltiazem and Verapamil: In a study of nine healthy volunteers, coadministration of buspirone (10 mg as a single dose) with verapamil (80 mg t.i.d.) or diltiazem (60 mg t.i.d.) increased plasma buspirone concentrations (verapamil increased AUC and Cmax of buspirone 3.4-fold while diltiazem increased AUC and Cmax 5.5-fold and 4-fold, respectively.) Adverse events attributable to buspirone may be more likely during concomitant administration with either diltiazem or verapamil. Subsequent dose adjustment may be necessary and should be based on clinical assessment.

Erythromycin: In a study in healthy volunteers, coadministration of buspirone (10 mg as a single dose) with erythromycin (1.5 g/day for 4 days) increased plasma buspirone concentrations (5-fold increase in Cmax and 6-fold increase in AUC). These pharmacokinetic interactions were accompanied by an increased incidence of side effects attributable to buspirone. If the two drugs are to be used in combination, a low dose of buspirone (eg, 2.5 mg b.i.d.) is recommended. Subsequent dose adjustment of either drug should be based on clinical assessment.

Grapefruit Juice: In a study in healthy volunteers, coadministration of buspirone (10 mg as a single dose) with grapefruit juice (200 mL double-strength t.i.d. for 2 days) increased plasma buspirone concentrations (4.3-fold increase in Cmax; 9.2-fold increase in AUC). Patients receiving buspirone should be advised to avoid drinking such large amounts of grapefruit juice.

Itraconazole: In a study in healthy volunteers, coadministration of buspirone (10 mg as a single dose) with itraconazole (200 mg/day for 4 days) increased plasma buspirone concentrations (13-fold increase in Cmax and 19-fold increase in AUC). These pharmacokinetic interactions were accompanied by an increased incidence of side effects attributable to buspirone. If the two drugs are to be used in combination, a low dose of buspirone (eg, 2.5 mg q.d.) is recommended. Subsequent dose adjustment of either drug should be based on clinical assessment.

Nefazodone: In a study of steady-state pharmacokinetics in healthy volunteers, coadministration of buspirone (2.5 or 5 mg b.i.d.) with nefazodone (250 mg b.i.d.) resulted in marked increases in plasma buspirone concentrations (increases up to 20-fold in Cmax and up to 50-fold in AUC) and statistically significant decreases (about 50%) in plasma concentrations of the buspirone metabolite 1-PP. With 5 mg b.i.d. doses of buspirone, slight increases in AUC were observed for nefazodone (23%) and its metabolites hydroxynefazodone (HO-NEF) (17%) and meta-chlorophenylpiperazine (9%). Slight increases in Cmax were observed for nefazodone (8%) and its metabolite HO-NEF (11%). Subjects receiving buspirone 5 mg b.i.d. and nefazodone 250 mg b.i.d experienced lightheadedness, asthenia, dizziness, and somnolence, adverse events also observed with either drug alone. If the two drugs are to be used in combination, a low dose of buspirone (eg, 2.5 mg q.d.) is recommended. Subsequent dose adjustment of either drug should be based on clinical assessment.

Rifampin: In a study in healthy volunteers, coadministration of buspirone (30 mg as a single dose) with rifampin (600 mg/day for 5 days) decreased the plasma concentrations (83.7% decrease in Cmax; 89.6% decrease in AUC) and pharmacodynamic effects of buspirone. If the two drugs are to be used in combination, the dosage of buspirone may need adjusting to maintain anxiolytic effect.

Other Inhibitors and Inducers of CYP3A4: Substances that inhibit CYP3A4, such as ketoconazole or ritonavir, may inhibit buspirone metabolism and increase plasma concentrations of buspirone while substances that induce CYP3A4, such as dexamethasone or certain anticonvulsants (phenytoin, phenobarbital, carbamazepine), may increase the rate of buspirone metabolism. If a patient has been titrated to a stable dosage on buspirone, a dose adjustment of buspirone may be necessary to avoid adverse events attributable to buspirone or diminished anxiolytic activity. Consequently, when administered with a potent inhibitor of CYP3A4, a low dose of buspirone used cautiously is recommended. When used in combination with a potent inducer of CYP3A4 the dosage of buspirone may need adjusting to maintain anxiolytic effect.

Other Drugs

Cimetidine: Coadministration of buspirone with cimetidine was found to increase Cmax (40%) and Tmax (2-fold), but had minimal effects on the AUC of buspirone.

Protein Binding

In vitro, buspirone does not displace tightly bound drugs like phenytoin, propranolol, and warfarin from serum proteins. However, there has been one report of prolonged prothrombin time when buspirone was added to the regimen of a patient treated with warfarin. The patient was also chronically receiving phenytoin, phenobarbital, digoxin, and Synthroid®. In vitro, buspirone may displace less firmly bound drugs like digoxin. The clinical significance of this property is unknown.

Therapeutic levels of aspirin, desipramine, diazepam, flurazepam, ibuprofen, propranolol, thioridazine, and tolbutamide had only a limited effect on the extent of binding of buspirone to plasma proteins (see CLINICAL PHARMACOLOGY).

Drug/Laboratory Test Interactions

Buspirone hydrochloride may interfere with the urinary metanephrine/catecholamine assay. It has been mistakenly read as metanephrine during routine assay testing for pheochromocytoma, resulting in a false positive laboratory result. Buspirone hydrochloride should therefore be discontinued for at least 48 hours prior to undergoing a urine collection for catecholamines.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

The administration of BuSpar (buspirone) to a patient taking a monoamine oxidase inhibitor (MAOI) may pose a hazard. There have been reports of the occurrence of elevated blood pressure when BuSpar (buspirone hydrochloride) has been added to a regimen including an MAOI. Therefore, it is recommended that BuSpar (buspirone) not be used concomitantly with an MAOI.

Because BuSpar (buspirone) has no established antipsychotic activity, it should not be employed in lieu of appropriate antipsychotic treatment.

PRECAUTIONS

General

Interference with Cognitive and Motor Performance

Studies indicate that BuSpar (buspirone) is less sedating than other anxiolytics and that it does not produce significant functional impairment. However, its CNS effects in any individual patient may not be predictable. Therefore, patients should be cautioned about operating an automobile or using complex machinery until they are reasonably certain that buspirone treatment does not affect them adversely.

While formal studies of the interaction of BuSpar (buspirone hydrochloride) with alcohol indicate that buspirone does not increase alcohol-induced impairment in motor and mental performance, it is prudent to avoid concomitant use of alcohol and buspirone.

Potential for Withdrawal Reactions in Sedative/Hypnotic/Anxiolytic Drug-Dependent Patients

Because BuSpar (buspirone) does not exhibit cross-tolerance with benzodiazepines and other common sedative/hypnotic drugs, it will not block the withdrawal syndrome often seen with cessation of therapy with these drugs. Therefore, before starting therapy with BuSpar (buspirone) , it is advisable to withdraw patients gradually, especially patients who have been using a CNS-depressant drug chronically, from their prior treatment. Rebound or withdrawal symptoms may occur over varying time periods, depending in part on the type of drug, and its effective half-life of elimination.

The syndrome of withdrawal from sedative/hypnotic/anxiolytic drugs can appear as any combination of irritability, anxiety, agitation, insomnia, tremor, abdominal cramps, muscle cramps, vomiting, sweating, flu-like symptoms without fever, and occasionally, even as seizures.

Possible Concerns Related to Buspirone's Binding to Dopamine Receptors

Because buspirone can bind to central dopamine receptors, a question has been raised about its potential to cause acute and chronic changes in dopamine-mediated neurological function (eg, dystonia, pseudo-parkinsonism, akathisia, and tardive dyskinesia). Clinical experience in controlled trials has failed to identify any significant neuroleptic-like activity; however, a syndrome of restlessness, appearing shortly after initiation of treatment, has been reported in some small fraction of buspirone-treated patients. The syndrome may be explained in several ways. For example, buspirone may increase central noradrenergic activity; alternatively, the effect may be attributable to dopaminergic effects (ie, represent akathisia). See ADVERSE REACTIONS: Postmarketing Experience.

Laboratory Tests

There are no specific laboratory tests recommended.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No evidence of carcinogenic potential was observed in rats during a 24-month study at approximately 133 times the maximum recommended human oral dose; or in mice, during an 18-month study at approximately 167 times the maximum recommended human oral dose.

With or without metabolic activation, buspirone did not induce point mutations in five strains of Salmonella typhimurium (Ames Test) or mouse lymphoma L5178YTK+ cell cultures, nor was DNA damage observed with buspirone in Wi-38 human cells. Chromosomal aberrations or abnormalities did not occur in bone marrow cells of mice given one or five daily doses of buspirone.

Pregnancy

Teratogenic Effects -Pregnancy Category B

No fertility impairment or fetal damage was observed in reproduction studies performed in rats and rabbits at buspirone doses of approximately 30 times the maximum recommended human dose. In humans, however, adequate and well-controlled studies during pregnancy have not been performed. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Labor and Delivery

The effect of BuSpar (buspirone hydrochloride) on labor and delivery in women is unknown. No adverse effects were noted in reproduction studies in rats.

Nursing Mothers

The extent of the excretion in human milk of buspirone or its metabolites is not known. In rats, however, buspirone and its metabolites are excreted in milk. BuSpar (buspirone) administration to nursing women should be avoided if clinically possible.

Pediatric Use

The safety and effectiveness of buspirone were evaluated in two placebo-controlled 6-week trials involving a total of 559 pediatric patients (ranging from 6 to 17 years of age) with GAD. Doses studied were 7.5 mg to 30 mg b.i.d. (15–60 mg/day). There were no significant differences between buspirone and placebo with regard to the symptoms of GAD following doses recommended for the treatment of GAD in adults. Pharmacokinetic studies have shown that, for identical doses, plasma exposure to buspirone and its active metabolite, 1-PP, are equal to or higher in pediatric patients than adults. No unexpected safety findings were associated with buspirone in these trials. There are no long-term safety or efficacy data in this population.

Geriatric Use

In one study of 6632 patients who received buspirone for the treatment of anxiety, 605 patients were ≥ 65 years old and 41 were ≥ 75 years old; the safety and efficacy profiles for these 605 elderly patients (mean age = 70.8 years) were similar to those in the younger population (mean age = 43.3 years). Review of spontaneously reported adverse clinical events has not identified differences between elderly and younger patients, but greater sensitivity of some older patients cannot be ruled out.

There were no effects of age on the pharmacokinetics of buspirone (see CLINICAL PHARMACOLOGY: Special Populations).

Use in Patients With Impaired Hepatic or Renal Function

Buspirone is metabolized by the liver and excreted by the kidneys. A pharmacokinetic study in patients with impaired hepatic or renal function demonstrated increased plasma levels and a lengthened half-life of buspirone. Therefore, the administration of BuSpar (buspirone) to patients with severe hepatic or renal impairment cannot be recommended (see CLINICAL PHARMACOLOGY).

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

Signs and Symptoms

In clinical pharmacology trials, doses as high as 375 mg/day were administered to healthy male volunteers. As this dose was approached, the following symptoms were observed: nausea, vomiting, dizziness, drowsiness, miosis, and gastric distress. A few cases of overdosage have been reported, with complete recovery as the usual outcome. No deaths have been reported following overdosage with BuSpar (buspirone) alone. Rare cases of intentional overdosage with a fatal outcome were invariably associated with ingestion of multiple drugs and/or alcohol, and a causal relationship to buspirone could not be determined.

Toxicology studies of buspirone yielded the following LD50 values: mice, 655 mg/kg; rats, 196 mg/kg; dogs, 586 mg/kg; and monkeys, 356 mg/kg. These dosages are 160 to 550 times the recommended human daily dose.

Recommended Overdose Treatment

General symptomatic and supportive measures should be used along with immediate gastric lavage. Respiration, pulse, and blood pressure should be monitored as in all cases of drug overdosage. No specific antidote is known to buspirone, and dialyzability of buspirone has not been determined.

CONTRAINDICATIONS

BuSpar is contraindicated in patients hypersensitive to buspirone hydrochloride.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

The mechanism of action of buspirone is unknown. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. In vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models.

Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.

BuSpar (buspirone) is rapidly absorbed in man and undergoes extensive first-pass metabolism. In a radiolabeled study, unchanged buspirone in the plasma accounted for only about 1% of the radioactivity in the plasma. Following oral administration, plasma concentrations of unchanged buspirone are very low and variable between subjects. Peak plasma levels of 1 ng/mL to 6 ng/mL have been observed 40 to 90 minutes after single oral doses of 20 mg. The single-dose bioavailability of unchanged buspirone when taken as a tablet is on the average about 90% of an equivalent dose of solution, but there is large variability.

The effects of food upon the bioavailability of BuSpar (buspirone) have been studied in eight subjects. They were given a 20 mg dose with and without food; the area under the plasma concentration-time curve (AUC) and peak plasma concentration (Cmax) of unchanged buspirone increased by 84% and 116%, respectively, but the total amount of buspirone immunoreactive material did not change. This suggests that food may decrease the extent of presystemic clearance of buspirone (see DOSAGE AND ADMINISTRATION).

A multiple-dose study conducted in 15 subjects suggests that buspirone has nonlinear pharmacokinetics. Thus, dose increases and repeated dosing may lead to somewhat higher blood levels of unchanged buspirone than would be predicted from results of single-dose studies.

An in vitro protein binding study indicated that approximately 86% of buspirone is bound to plasma proteins. It was also observed that aspirin increased the plasma levels of free buspirone by 23%, while flurazepam decreased the plasma levels of free buspirone by 20%. However, it is not known whether these drugs cause similar effects on plasma levels of free buspirone in vivo, or whether such changes, if they do occur, cause clinically significant differences in treatment outcome. An in vitro study indicated that buspirone did not displace highly protein-bound drugs such as phenytoin, warfarin, and propranolol from plasma protein, and that buspirone may displace digoxin.

Buspirone is metabolized primarily by oxidation, which in vitro has been shown to be mediated by cytochrome P450 3A4 (CYP3A4). (See PRECAUTIONS : DRUG INTERACTIONS.) Several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP), are produced. In animal models predictive of anxiolytic potential, 1-PP has about one quarter of the activity of buspirone, but is present in up to 20-fold greater amounts. However, this is probably not important in humans: blood samples from humans chronically exposed to BuSpar (buspirone hydrochloride) do not exhibit high levels of 1-PP; mean values are approximately 3 ng/mL and the highest human blood level recorded among 108 chronically dosed patients was 17 ng/mL, less than 1/200th of 1-PP levels found in animals given large doses of buspirone without signs of toxicity.

In a single-dose study using 14C-labeled buspirone, 29% to 63% of the dose was excreted in the urine within 24 hours, primarily as metabolites; fecal excretion accounted for 18% to 38% of the dose. The average elimination half-life of unchanged buspirone after single doses of 10 mg to 40 mg is about 2 to 3 hours.

Special Populations

Age and Gender Effects

After single or multiple doses in adults, no significant differences in buspirone pharmacokinetics (AUC and Cmax) were observed between elderly and younger subjects or between men and women.

Hepatic Impairment

After multiple-dose administration of buspirone to patients with hepatic impairment, steady-state AUC of buspirone increased 13-fold compared with healthy subjects (see PRECAUTIONS).

Renal Impairment

After multiple-dose administration of buspirone to renally impaired (Clcr = 10– 70 mL/min/1.73 m²) patients, steady-state AUC of buspirone increased 4-fold compared with healthy (Clcr ≥ 80 mL/min/1.73 m²) subjects (see PRECAUTIONS).

Race Effects

The effects of race on the pharmacokinetics of buspirone have not been studied.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

To assure safe and effective use of BuSpar (buspirone) , the following information and instructions should be given to patients:

  1. Inform your physician about any medications, prescription or non-prescription, alcohol, or drugs that you are now taking or plan to take during your treatment with BuSpar (buspirone) .
  2. Inform your physician if you are pregnant, or if you are planning to become pregnant, or if you become pregnant while you are taking BuSpar (buspirone) .
  3. Inform your physician if you are breast-feeding an infant.
  4. Until you experience how this medication affects you, do not drive a car or operate potentially dangerous machinery.
  5. You should take BuSpar (buspirone hydrochloride) consistently, either always with or always without food.
  6. During your treatment with BuSpar (buspirone) , avoid drinking large amounts of grapefruit juice.

BuSpar®
(buspirone HCl, USP)

Patient Instruction Sheet

HOW TO USE:

BuSpar®
(buspirone HCl, USP)

15 mg and 30 mg Tablets in convenient DIVIDOSE® tablet form

Response to buspirone varies among individuals. Your physician may find it necessary to adjust your dosage to obtain the proper response.

This DIVIDOSE tablet design makes dosage adjustments easy. Each tablet is scored and can be broken accurately to provide any of the following dosages.

If your doctor prescribed the 30 mg tablet: If your doctor prescribed the 15 mg tablet:
30 mg (the entire tablet) 15 mg (the entire tablet)
20 mg (two thirds of a tablet) 10 mg (two thirds of a tablet)
10 mg (one third of a tablet) 5 mg (one third of a tablet)
15 mg (one half of a tablet) 7.5 mg (one half of a tablet)
#822 on 15 mg and 824 on 30 mg tablet

To break a DIVIDOSE tablet accurately and easily, hold the tablet between your thumbs and index fingers close to the appropriate tablet score (groove) as shown in the photo.

Then, with the tablet score facing you, apply pressure and snap the tablet segments apart (segments breaking incorrectly should not be used).

Snap the tablet segments apart - Illustration

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

>

PATIENT INFORMATION

To assure safe and effective use of BuSpar (buspirone) , the following information and instructions should be given to patients:

  1. Inform your physician about any medications, prescription or non-prescription, alcohol, or drugs that you are now taking or plan to take during your treatment with BuSpar (buspirone) .
  2. Inform your physician if you are pregnant, or if you are planning to become pregnant, or if you become pregnant while you are taking BuSpar (buspirone) .
  3. Inform your physician if you are breast-feeding an infant.
  4. Until you experience how this medication affects you, do not drive a car or operate potentially dangerous machinery.
  5. You should take BuSpar (buspirone hydrochloride) consistently, either always with or always without food.
  6. During your treatment with BuSpar (buspirone) , avoid drinking large amounts of grapefruit juice.

BuSpar®
(buspirone HCl, USP)

Patient Instruction Sheet

HOW TO USE:

BuSpar®
(buspirone HCl, USP)

15 mg and 30 mg Tablets in convenient DIVIDOSE® tablet form

Response to buspirone varies among individuals. Your physician may find it necessary to adjust your dosage to obtain the proper response.

This DIVIDOSE tablet design makes dosage adjustments easy. Each tablet is scored and can be broken accurately to provide any of the following dosages.

If your doctor prescribed the 30 mg tablet: If your doctor prescribed the 15 mg tablet:
30 mg (the entire tablet) 15 mg (the entire tablet)
20 mg (two thirds of a tablet) 10 mg (two thirds of a tablet)
10 mg (one third of a tablet) 5 mg (one third of a tablet)
15 mg (one half of a tablet) 7.5 mg (one half of a tablet)
#822 on 15 mg and 824 on 30 mg tablet

To break a DIVIDOSE tablet accurately and easily, hold the tablet between your thumbs and index fingers close to the appropriate tablet score (groove) as shown in the photo.

Then, with the tablet score facing you, apply pressure and snap the tablet segments apart (segments breaking incorrectly should not be used).

Snap the tablet segments apart - Illustration

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

Disclaimer

Buspar 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.

BUSPIRONE - ORAL

(bue-SPYE-rone)

COMMON BRAND NAME(S): Buspar

USES: This medication is used to treat anxiety. It may help you think more clearly, relax, worry less, and take part in everyday life. It may also help you to feel less jittery and irritable, and may control symptoms such as trouble sleeping, sweating, and pounding heartbeat. Buspirone is a medication for anxiety (anxiolytic) that works by affecting certain natural substances in the brain (neurotransmitters).

HOW TO USE: Take this medication by mouth, usually 2 or 3 times a day or as directed by your doctor. You may take this medication with or without food, but it is important to choose one way and always take it the same way so that the amount of drug absorbed will always be the same.

Buspirone may come in a tablet that can be split to get the correct dose for you. Follow the manufacturer's Patient Instruction Sheet or ask your pharmacist how to split the tablet to get your dose.

Limit the amount of grapefruit you may eat or drink (less than one quart a day) while being treated with this medication unless your doctor directs you otherwise. Grapefruit may increase the amount of buspirone in your bloodstream. Consult your pharmacist or doctor for more information.

Dosage is based on your medical condition and response to therapy. Use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same times each day. When this medication is started, symptoms of anxiety (e.g., restlessness) may sometimes get worse before they improve. It may take up to a month or more to get the full effect of this medication.

Inform your doctor if your symptoms persist or worsen.

Disclaimer

Buspar Consumer (continued)

SIDE EFFECTS: Dizziness, drowsiness, headache, nausea, nervousness, lightheadedness, restlessness, blurred vision, tiredness, and trouble sleeping may occur. If any of these effects persist or worsen, notify 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.

Rarely, patients taking buspirone may develop movement disorders such as shakiness (tremors), muscle stiffness, mask-like facial expression, jerky walking movements, or a condition known as tardive dyskinesia. In some cases, these conditions may be permanent. Tell your doctor immediately if you develop any unusual/uncontrolled movements (especially of the face, mouth, tongue, arms, or legs).

Seek immediate medical attention if any of these rare but serious side effects occur: easy bleeding/bruising, shortness of breath, chest pain, fast/irregular heartbeat.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: 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 Buspar (buspirone) Side Effects Center for a complete guide to possible side effects »

PRECAUTIONS: Before taking buspirone, tell your doctor or pharmacist if you are allergic to it; 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.

This medication should not be used if you have certain medical conditions. Before using this medication, consult your doctor if you have: kidney problems, liver problems.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: bipolar disorder (manic-depression), Parkinson's disease.

This drug may make you dizzy or drowsy. 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.

If you are taking other medications for anxiety, do not suddenly stop them unless directed by your doctor. Buspirone will not prevent withdrawal symptoms from other medications, and your dose may need to be lowered slowly when you switch to buspirone. Discuss your treatment plan with your doctor. If you experience withdrawal symptoms, tell your doctor immediately.

During pregnancy, this medication should only be used when clearly needed. Tell your doctor if you are pregnant before using this medication. Discuss the risks and benefits with your doctor.

It is unknown if this drug passes into breast milk. However, similar drugs pass into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breastfeeding.

Disclaimer

Buspar Consumer (continued)

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

Buspirone should not be used with MAO inhibitors (isocarboxazid, linezolid, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, selegiline, tranylcypromine). Do not take buspirone within 2 weeks before, during and after treatment with MAO inhibitors. In some cases, a serious, possibly fatal, drug interaction may occur.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: alcohol, antidepressants (e.g., SSRIs such as fluoxetine, tricyclic antidepressants such as amitriptyline/nortriptyline, trazodone), benzodiazepines (e.g., lorazepam, clonazepam, diazepam), haloperidol, drugs that slow down the removal of buspirone from your body by affecting certain liver enzymes including azole antifungals (e.g., itraconazole, ketoconazole), macrolides (e.g., erythromycin), ritonavir, nefazodone, diltiazem, verapamil, drugs that speed up the removal of buspirone from your body by affecting certain liver enzymes including rifamycins (e.g., rifampin, rifabutin), corticosteroids (e.g., dexamethasone), and certain anticonvulsants (e.g., carbamazepine, phenytoin, phenobarbital).

Tell your doctor or pharmacist if you also take drugs that cause drowsiness such as: certain antihistamines (e.g., diphenhydramine), anti-seizure medications (e.g., valproic acid), medicine for sleep or anxiety (e.g., alprazolam, flurazepam, zolpidem), muscle relaxants, narcotic pain relievers (e.g., codeine), psychiatric medications (e.g., risperidone).

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. Canadian residents should call their local poison control center directly.

NOTES: Do not share this medication with others.

Keep all regular medical and laboratory appointments. If you are also taking trazodone, liver function tests may be performed regularly to 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 the US product in a tightly closed container at room temperature below 86 degrees F (30 degrees C) away from light and moisture.

Store the Canadian product in a tightly closed container at room temperature 59-86 degrees F (15-30 degrees C) away from light and moisture.

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 October 2011. Copyright(c) 2011 First Databank, Inc.

Buspar Patient Information Including Side Effects

Brand Names: BuSpar, BuSpar Dividose

Generic Name: buspirone (Pronunciation: byoo SPYE rone)

What is buspirone (Buspar)?

Buspirone is an anti-anxiety medicine that affects chemicals in your brain that may become unbalanced and cause anxiety.

Buspirone is used to treat symptoms of anxiety, such as fear, tension, irritability, dizziness, pounding heartbeat, and other physical symptoms.

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

BuSpar 10 mg

rectangular, white, imprinted with BUSPAR, MJ 10

BuSpar 15 mg

rectangular, white, imprinted with 5 5 5, MJ 222

BuSpar 5 mg

rectangular, white, imprinted with BUSPAR, MJ 5

Buspirone 10 mg-ETH

oval, yellow, imprinted with 10mg, ETHEX265

Buspirone 10 mg-IVA

oval, white, imprinted with Hourglass Logo 10, 5664

Buspirone 10 mg-MYL

oval, white, imprinted with M B2

Buspirone 10 mg-TEV

round, white, imprinted with 93 54

Buspirone 10 mg-WAT

oval, white, imprinted with WATSON, 658

Buspirone 15 mg-ETH

oblong, yellow, imprinted with 555, ETH 309

Buspirone 15 mg-IVA

oblong, white, imprinted with 5 5 5, Hourglass Logo 56 65

Buspirone 15 mg-MYL

oblong, white, imprinted with M B3, 5 5 5

Buspirone 15 mg-PAR

rectangular, peach, imprinted with 5 5 5, PAR 721

Buspirone 15 mg-TEV

rectangular, white, imprinted with 5 5 5, 93 1003

Buspirone 15 mg-WAT

oval, white, imprinted with LOGO 718

Buspirone 30 mg-MYL

oblong, white, imprinted with M B4, 10 10 10

Buspirone 30 mg-TEV

rectangular, white, imprinted with 10 10 10, 935200

Buspirone 5 mg-ETH

oval, yellow, imprinted with 5mg, ETHEX 264

Buspirone 5 mg-IVA

oval, white, imprinted with Hourglass Logo 5, 5663

Buspirone 5 mg-MYL

oval, white, imprinted with M B1

Buspirone 5 mg-PAR

oval, peach, imprinted with par 707, 5

Buspirone 5 mg-TEV

round, white, imprinted with 93 53

Buspirone 5 mg-WAT

oval, white, imprinted with WATSON, 657

What are the possible side effects of buspirone (Buspar)?

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

Call your doctor at once if you have any of these serious side effects:

  • feeling light-headed, fainting;
  • fast or uneven heart rate;
  • depressed mood, unusual thoughts or behavior; or
  • lack of balance or coordination.

Less serious side effects may be more likely to occur, such as:

  • drowsiness, dizziness, blurred vision;
  • feeling restless;
  • nausea, upset stomach;
  • sleep problems (insomnia); or
  • trouble concentrating.

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

Read the Buspar (buspirone) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about buspirone (Buspar)?

Do not this medication if you are allergic to buspirone, or if you have used an MAO inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam), or tranylcypromine (Parnate) within the past 14 days. Serious, life-threatening side effects can occur if you take buspirone before the MAO inhibitor has cleared from your body.

Buspirone can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Avoid drinking alcohol. It may increase some of the side effects caused by buspirone.

Grapefruit and grapefruit juice may interact with buspirone and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor. Do not increase or decrease the amount of grapefruit products in your diet without first talking to your doctor.

Buspirone is usually taken for only a short time. Do not take this medication for longer than 4 weeks without your doctor's advice.

Side Effects Centers

Buspar Patient Information including How Should I Take

What should I discuss with my healthcare provider before taking buspirone (Buspar)?

Do not this medication if you are allergic to buspirone, or if you have used an MAO inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam), or tranylcypromine (Parnate) within the past 14 days. Serious, life-threatening side effects can occur if you take buspirone before the MAO inhibitor has cleared from your body.

Before taking buspirone, tell your doctor if you are allergic to any drugs, or if you have:

  • kidney disease; or
  • liver disease.

If you have any of these conditions, you may not be able to use buspirone, or you may need a dosage adjustment or special tests during treatment.

FDA pregnancy category B. This medication is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

It is not known whether buspirone passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Do not give this medication to a child younger than 18 years old.

How should I take buspirone (Buspar)?

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.

Buspirone is usually taken for only a short time. Do not take this medication for longer than 4 weeks without your doctor's advice.

You may take buspirone with or without food but take it the same way each time.

Some tablet forms of buspirone (Buspar Dividose) may need to be broken before you take the medicine. These tablets have special scored marks on them to make breaking the tablet easy. Do not use the tablet if it has not broken correctly and the piece is too big or too small. Follow your doctor's instructions about how much of the tablet to take.

If you have been switched to buspirone from another anxiety medication, you may need to slowly decrease your dose of the other medication rather than stopping suddenly. Some anxiety medications can cause withdrawal symptoms when you stop taking them suddenly after long-term use.

Store buspirone at room temperature away from moisture and heat.

Side Effects Centers

Buspar Patient Information including If I Miss a Dose

What happens if I miss a dose (Buspar)?

Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at your next regularly scheduled time. Do not take extra medicine to make up the missed dose.

What happens if I overdose (Buspar)?

Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include nausea, vomiting, dizziness, drowsiness, blurred vision, and stomach pain.

What should I avoid while taking buspirone (Buspar)?

Buspirone can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Avoid drinking alcohol. It may increase some of the side effects caused by buspirone.

Cold or allergy medicine, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, or depression can add to sleepiness caused by buspirone. Tell your doctor if you regularly use any of these other medicines.

Grapefruit and grapefruit juice may interact with buspirone and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor. Do not increase or decrease the amount of grapefruit products in your diet without first talking to your doctor.

What other drugs will affect buspirone (Buspar)?

The following drugs can interact with buspirone. Tell your doctor if you are using any of these:

  • medicines to treat psychiatric disorders, such as chlorpromazine (Thorazine), haloperidol (Haldol), mesoridazine (Serentil), pimozide (Orap), or thioridazine (Mellaril);
  • dexamethasone (Decadron, Hexadrol);
  • erythromycin (E-Mycin, E.E.S., Ery-Tab, Erythrocin);
  • itraconazole (Sporanox), ketoconazole (Nizoral);
  • ritonavir (Norvir);
  • rifampin (Rifadin, Rimactane, Rifater);
  • antibiotics such as capreomycin (Capastat), rifampin (Rifadin, Rimactane, Rifater), vancomycin (Vancocin, Vancoled);
  • a calcium channel blocker such as diltiazem (Tiazac, Cartia, Cardizem) or verapamil (Calan, Covera, Isoptin, Verelan); or
  • seizure medication such as carbamazepine (Carbatrol, Tegretol), phenytoin (Dilantin), phenobarbital (Luminal, Solfoton).

This list is not complete and there may be other drugs that can interact with buspirone. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about buspirone.


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: 3.11. Revision date: 12/15/2010.

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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