Nucynta (Tapentadol Immediate-Release Oral Tablets)
برای این دارو، اطلاعات عمومی (فارسی) یافت نشد . برای افزودن اطلاعات فارسی به این دارو کلیک نمایید.
Nucynta (Tapentadol Immediate-Release Oral Tablets)

NUCYNTA®
(tapentadol) Immediate-Release Oral Tablets

DRUG DESCRIPTION

NUCYNTA® (tapentadol) Tablets are immediate-release film-coated tablets for oral administration. The chemical name is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2- methylpropyl]phenol monohydrochloride. The structural formula is:

NUCYNTA® (tapentadol) Structural Formula Illustration

The molecular weight of tapentadol HCl is 257.80, and the molecular formula is C14H23NO·HCl. The n-octanol:water partition coefficient log P value is 2.87. The pKa values are 9.34 and 10.45. In addition to the active ingredient tapentadol HCl, tablets also contain the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, and Opadry® II, a proprietary film-coating mixture containing polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and aluminum lake coloring.

What are the possible side effects of tapentadol (Nucynta, Nucynta ER)?

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.

Call your doctor at once if you have a serious side effect such as:

  • weak or shallow breathing, weak pulse, slow heartbeat;
  • seizure (convulsions);
  • severe drowsiness or dizziness;
  • confusion, problems with speech or balance; or
  • agitation, hallucinations, fever, fast heart rate, overactive reflexes, nausea, vomiting, diarrhea, loss of coordination,...

Read All Potential Side Effects and See Pictures of Nucynta »

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

NUCYNTA® (tapentadol) is indicated for the relief of moderate to severe acute pain in patients 18 years of age or older.

DOSAGE AND ADMINISTRATION

As with many centrally-acting analgesic medications, the dosing regimen should be individualized according to the severity of pain being treated, the previous experience with similar drugs and the ability to monitor the patient.

The dose is 50 mg, 75 mg, or 100 mg every 4 to 6 hours depending upon pain intensity.

On the first day of dosing, the second dose may be administered as soon as one hour after the first dose, if adequate pain relief is not attained with the first dose. Subsequent dosing is 50 mg, 75 mg, or 100 mg every 4 to 6 hours and should be adjusted to maintain adequate analgesia with acceptable tolerability.

Daily doses greater than 700 mg on the first day of therapy and 600 mg on subsequent days have not been studied and are not recommended.

NUCYNTA® may be given with or without food [see CLINICAL PHARMACOLOGY].

Renal Impairment

No dosage adjustment is recommended in patients with mild or moderate renal impairment [see CLINICAL PHARMACOLOGY].

NUCYNTA® has not been studied in patients with severe renal impairment. The use in this population is not recommended.

Hepatic Impairment

No dosage adjustment is recommended in patients with mild hepatic impairment [see CLINICAL PHARMACOLOGY].

NUCYNTA® should be used with caution in patients with moderate hepatic impairment. Treatment in these patients should be initiated at 50 mg with the interval between doses no less than every 8 hours (maximum of three doses in 24 hours). Further treatment should reflect maintenance of analgesia with acceptable tolerability, to be achieved by either shortening or lengthening the dosing interval [see CLINICAL PHARMACOLOGY].

NUCYNTA® has not been studied in patients with severe hepatic impairment and use in this population is not recommended [see WARNINGS AND PRECAUTIONS].

Elderly Patients

In general, recommended dosing for elderly patients with normal renal and hepatic function is the same as for younger adult patients with normal renal and hepatic function. Because elderly patients are more likely to have decreased renal and hepatic function, consideration should be given to starting elderly patients with the lower range of recommended doses.

HOW SUPPLIED

Dosage Forms And Strengths

NUCYNTA® Tablets are round, biconvex and film-coated and are available in the following strengths, colors, and debossings: 50 mg of tapentadol (yellow with “O-M” on one side and “50” on the other side), 75 mg of tapentadol (yellow-orange with “O-M” on one side and “75” on the other side), and 100 mg of tapentadol (orange with “O-M” on one side and “100” on the other side).

Storage And Handling

NUCYNTA® Tablets are available in the following strengths and packages. All tablets are round and biconvex-shaped.

50 mg tablets are yellow and debossed with “O-M” on one side and “50” on the other side, and are available in bottles of 100 (NDC 50458-820-04) and hospital unit dose blister packs of 10 (NDC 50458-820-02).

75 mg tablets are yellow-orange and debossed with “O-M” on one side and “75” on the other side, and are available in bottles of 100 (NDC 50458-830-04) and hospital unit dose blister packs of 10 (NDC 50458-830-02).

100 mg tablets are orange and debossed with “O-M” on one side and “100” on the other side, and are available in bottles of 100 (NDC 50458-840-04) and hospital unit dose blister packs of 10 (NDC 50458-840-02).

Store up to 25°C (77°F); excursions permitted to 15° - 30°C (59° - 86°F) [see USP Controlled Room Temperature]. Protect from moisture.

Keep out of reach of children.

Revised: July 2011. Manufactured by: Janssen Ortho, LLC, Gurabo, PR 00778. Manufactured for: Janssen Pharmaceuticals, Inc., Titusville, NJ 08560. Rev: July 2011

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

The following treatment-emergent adverse events are discussed in more detail in other sections of the labeling:

Because clinical studies are conducted under widely varying conditions, adverse event rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in clinical practice. A treatment-emergent adverse event refers to any untoward medical event associated with the use of the drug in humans, whether or not considered drug-related.

Based on data from nine Phase 2/3 studies that administered multiple doses (seven placebo- and/or active-controlled, one noncontrolled and one Phase 3 activecontrolled safety study) the most common adverse events (reported by ≥ 10% in any NUCYNTA® dose group) were: nausea, dizziness, vomiting and somnolence.

The most common reasons for discontinuation due to adverse events in the studies described above (reported by ≥ 1% in any NUCYNTA® dose group) were dizziness (2.6% vs. 0.5%), nausea (2.3% vs. 0.6%), vomiting (1.4% vs. 0.2%), somnolence (1.3% vs. 0.2%) and headache (0.9% vs. 0.2%) for NUCYNTA®- and placebo-treated patients, respectively.

Seventy-six percent of NUCYNTA®-treated patients from the nine studies experienced adverse events.

NUCYNTA® was studied in multiple-dose, active- or placebo-controlled studies, or noncontrolled studies (n = 2178), in single-dose studies (n = 870), in open-label study extension (n = 483) and in Phase 1 studies (n = 597). Of these, 2034 patients were treated with doses of 50 mg to 100 mg of NUCYNTA® dosed every 4 to 6 hours.

The data described below reflect exposure to NUCYNTA® in 3161 patients, including 449 exposed for 45 days. NUCYNTA® was studied primarily in placebo- and active-controlled studies (n = 2266, and n = 2944, respectively). The population was 18 to 85 years old (mean age 46 years), 68% were female, 75% white and 67% were postoperative. Most patients received NUCYNTA® doses of 50 mg, 75 mg, or 100 mg every 4 to 6 hours.

Commonly-Observed Treatment-Emergent Adverse Events in Double-Blind Controlled Clinical Trials

Table 1 lists the adverse events reported in ≥ 1% or more of NUCYNTA®-treated patients with acute moderate to severe pain in the pooled safety data from nine Phase 2/3 studies that administered multiple doses (seven placebo- and/or active-controlled, one noncontrolled, and one Phase 3 active-controlled safety study).

Table 1 : Treatment-Emergent Adverse Events* Reported by ≥ 1% of NUCYNTA®- Treated Patients In Seven Phase 2/3 Placebo- and/or Oxycodone- Controlled, One Noncontrolled, and One Phase 3 Oxycodone-Controlled Safety, Multiple-Dose Clinical Studies

System/Organ Class MedDRA Preferred Term NUCYNTA® 21 mg - 120 mg
(n=2178) %
Placebo
(n=619) %
Gastrointestinal disorders
  Nausea  30 13
  Vomiting 18 4
  Constipation 8 3
  Dry mouth 4 < 1
  Dyspepsia 2 < 1
General disorders and administration site conditions
  Fatigue 3 < 1
  Feeling hot 1 < 1
Infections and infestations
  Nasopharyngitis 1 < 1
  Upper respiratory tract infection 1 < 1
  Urinary tract infection 1 < 1
Metabolism and nutrition disorders
  Decreased appetite 2 0
Musculoskeletal and connective tissue disorders
  Arthralgia 1 < 1
Nervous system disorders
  Dizziness 24 8
  Somnolence 15 3
  Tremor 1 < 1
  Lethargy 1 < 1
Psychiatric disorders
  Insomnia 2 < 1
  Confusional state 1 0
  Abnormal dreams 1 < 1
  Anxiety 1 < 1
Skin and subcutaneous tissue disorders
  Pruritus 5 1
  Hyperhidrosis 3 < 1
  Pruritus generalized 3 < 1
  Rash 1 < 1
Vascular disorders 
  Hot flush 1 < 1
* A treatment-emergent adverse event refers to any untoward medical event associated with the use of the drug in humans, whether or not considered drug-related.

Other Adverse Reactions Observed During the Premarketing Evaluation of NUCYNTA®

The following adverse drug reactions occurred in < 1% of NUCYNTA®-treated patients in the pooled safety data from nine Phase 2/3 studies that administered multiple doses (seven were placebo- and/or active-controlled, one noncontrolled, and one Phase 3 active-controlled safety study):

Cardiac disorders: heart rate increased, heart rate decreased

Eye disorders: visual disturbance

Gastrointestinal disorders: abdominal discomfort, impaired gastric emptying

General disorders and administration site conditions: irritability, edema, drug withdrawal syndrome, feeling drunk

Immune system disorders: hypersensitivity

Investigations: gamma-glutamyltransferase increased, alanine aminotransferase increased, aspartate aminotransferase increased

Musculoskeletal and connective tissue disorders: involuntary muscle contractions, sensation of heaviness

Nervous system disorders: hypoesthesia, paresthesia, disturbance in attention, sedation, dysarthria, depressed level of consciousness, memory impairment, ataxia, presyncope, syncope, coordination abnormal, seizure

Psychiatric disorders: euphoric mood, disorientation, restlessness, agitation, nervousness, thinking abnormal

Renal and urinary disorders: urinary hesitation, pollakiuria

Respiratory, thoracic and mediastinal disorders: oxygen saturation decreased, cough, dyspnea, respiratory depression

Skin and subcutaneous tissue disorders: urticaria

Vascular disorders: blood pressure decreased

In the pooled safety data, the overall incidence of adverse reactions increased with increased dose of NUCYNTA®, as did the percentage of patients with adverse reactions of nausea, dizziness, vomiting, somnolence, and pruritus.

Post-marketing Experience

The following additional adverse reactions have been identified during post-approval use of NUCYNTA®. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate their frequency reliably.

Gastrointestinal disorders: diarrhea

Immune system disorders: angioedema

Nervous system disorders: headache

Psychiatric disorders: hallucination

Cardiac disorders: palpitations

Read the Nucynta (tapentadol immediate-release oral tablets) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

NUCYNTA® is mainly metabolized by glucuronidation. The following substances have been included in a set of interaction studies without any clinically significant finding: acetaminophen, acetylsalicylic acid, naproxen and probenecid [see CLINICAL PHARMACOLOGY].

The pharmacokinetics of tapentadol were not affected when gastric pH or gastrointestinal motility were increased by omeprazole and metoclopramide, respectively [see CLINICAL PHARMACOLOGY].

Drugs Metabolized by Cytochrome P450 Enzymes

In vitro investigations indicate that NUCYNTA® does not inhibit or induce P450 enzymes. Thus, clinically relevant interactions mediated by the cytochrome P450 system are unlikely to occur [see CLINICAL PHARMACOLOGY].

Drugs That Inhibit or Induce Cytochrome P450 Enzymes

The major pathway of tapentadol metabolism is conjugation with glucuronic acid to produce glucuronides. To a lesser extent, tapentadol is additionally metabolized to N-desmethyl tapentadol (13%) by CYP2C9 and CYP2C19 to hydroxy tapentadol (2%) by CYP2D6, which are further metabolized by conjugation. Since only a minor amount of NUCYNTA® is metabolized via the oxidative pathway clinically relevant interactions mediated by the cytochrome P450 system are unlikely to occur [see CLINICAL PHARMACOLOGY].

Centrally-Acting Drugs and Alcohol

Patients receiving other opioid agonist analgesics, general anesthetics, phenothiazines, antiemetics, other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with NUCYNTA® may exhibit an additive CNS depression. Interactive effects resulting in respiratory depression, hypotension, profound sedation, or coma may result if these drugs are taken in combination with NUCYNTA®. When such combined therapy is contemplated, a dose reduction of one or both agents should be considered [see WARNINGS AND PRECAUTIONS].

Monoamine Oxidase Inhibitors

NUCYNTA® is contraindicated in patients who are receiving monoamine oxidase (MAO) inhibitors or who have taken them within the last 14 days due to potential additive effects on norepinephrine levels which may result in adverse cardiovascular events [see CONTRAINDICATIONS].

Drug Abuse And Dependence

Controlled Substance

NUCYNTA® contains tapentadol, a mu-opioid agonist and is a Schedule II controlled substance. NUCYNTA® has an abuse potential similar to hydromorphone, can be abused and is subject to criminal diversion.

Abuse

Addiction is a primary, chronic, neurobiologic disease, with genetic, psychosocial, and environmental factors influencing its development and manifestations. It is characterized by behaviors that include one or more of the following: impaired control over drug use, compulsive use, continued use despite harm, and craving. Drug addiction is a treatable disease, utilizing a multidisciplinary approach, but relapse is common.

Concerns about abuse and addiction should not prevent the proper management of pain. However, all patients treated with opioids require careful monitoring for signs of abuse and addiction, because use of opioid analgesic products carries the risk of addiction even under appropriate medical use.

“Drug seeking” behavior is very common in addicts, and drug abusers. Drug-seeking tactics include emergency calls or visits near the end of office hours, refusal to undergo appropriate examination, testing or referral, repeated claims of loss of prescriptions, tampering with prescriptions and reluctance to provide prior medical records or contact information for other treating physician(s). “Doctor shopping” (visiting multiple prescribers) to obtain additional prescriptions is common among drug abusers and people suffering from untreated addiction. Preoccupation with achieving adequate pain relief can be appropriate behavior in a patient with poor pain control.

Abuse and addiction are separate and distinct from physical dependence and tolerance. Physicians should be aware that addiction may not be accompanied by concurrent tolerance and symptoms of physical dependence in all addicts. In addition, abuse of mu-opioid agonists can occur in the absence of true addiction and is characterized by misuse for non-medical purposes, often in combination with other psychoactive substances. Careful recordkeeping of prescribing information, including quantity, frequency, and renewal requests is strongly advised.

Abuse of NUCYNTA® poses a risk of overdose and death. This risk is increased with concurrent abuse of NUCYNTA® with alcohol and other substances. In addition, parenteral drug abuse is commonly associated with transmission of infectious diseases such as hepatitis and HIV.

Proper assessment of the patient, proper prescribing practices, periodic re-evaluation of therapy, and proper dispensing and storage are appropriate measures that help to limit abuse of drugs with mu-opioid agonist properties.

Infants born to mothers physically dependent on opioids will also be physically dependent and may exhibit respiratory difficulties and withdrawal symptoms [see WARNINGS AND PRECAUTIONS]. Use of NUCYNTA® in this population has not been characterized. As NUCYNTA® has mu-opioid agonist activity, infants whose mothers have taken NUCYNTA®, should be carefully monitored.

Dependence

Tolerance is the need for increasing doses of opioids to maintain a defined effect such as analgesia (in the absence of disease progression or other external factors). Physical dependence is manifested by withdrawal symptoms after abrupt discontinuation of a drug or upon administration of an antagonist.

The opioid abstinence or withdrawal syndrome is characterized by some or all of the following: restlessness, lacrimation, rhinorrhea, yawning, perspiration, chills, myalgia, and mydriasis. Other symptoms also may develop, including irritability, anxiety, backache, joint pain, weakness, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhea, increased blood pressure, respiratory rate, or heart rate.

Generally, tolerance and/or withdrawal are more likely to occur the longer a patient is on continuous opioid therapy. In a safety study where drug was administered up to 90 days, 82.7% of patients taking NUCYNTA® who stopped abruptly without initiating alternative therapy and were assessed 2 to 4 days after discontinuation, did not have objective signs of opioid withdrawal using the Clinical Opiate Withdrawal Scale. Moderate withdrawal symptoms were seen in 0.3% of patients with the rest (17%) experiencing mild symptoms. Withdrawal symptoms may be reduced by tapering NUCYNTA®.

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

Respiratory Depression

Respiratory depression is the primary risk of mu-opioid agonists. Respiratory depression occurs more frequently in elderly or debilitated patients and in those suffering from conditions accompanied by hypoxia, hypercapnia, or upper airway obstruction, in whom even moderate therapeutic doses may significantly decrease pulmonary ventilation.

NUCYNTA® should be administered with caution to patients with conditions accompanied by hypoxia, hypercapnia or decreased respiratory reserve such as: asthma, chronic obstructive pulmonary disease or cor pulmonale, severe obesity, sleep apnea syndrome, myxedema, kyphoscoliosis, central nervous system (CNS) depression, or coma. In such patients, even usual therapeutic doses of NUCYNTA® may increase airway resistance and decrease respiratory drive to the point of apnea. Alternative non-mu-opioid agonist analgesics should be considered and NUCYNTA® should be employed only under careful medical supervision at the lowest effective dose in such patients. If respiratory depression occurs, it should be treated as any mu-opioid agonist-induced respiratory depression [see OVERDOSAGE].

CNS Depression

Patients receiving other mu-opioid agonist analgesics, general anesthetics, phenothiazines, other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with NUCYNTA® may exhibit additive CNS depression. Interactive effects resulting in respiratory depression, hypotension, profound sedation, coma or death may result if these drugs are taken in combination with NUCYNTA®. When such combined therapy is contemplated, a dose reduction of one or both agents should be considered.

Head Injury and Increased Intracranial Pressure

Opioid analgesics can raise cerebrospinal fluid pressure as a result of respiratory depression with carbon dioxide retention. Therefore, NUCYNTA® should not be used in patients who may be susceptible to the effects of raised cerebrospinal fluid pressure such as those with evidence of head injury and increased intracranial pressure. Opioid analgesics may obscure the clinical course of patients with head injury due to effects on pupillary response and consciousness. NUCYNTA® should be used with caution in patients with head injury, intracranial lesions, or other sources of preexisting increased intracranial pressure.

Misuse and Abuse

Tapentadol is a mu-opioid agonist and is a Schedule II controlled substance. Such drugs are sought by drug abusers and people with addiction disorders. Diversion of Schedule II products is an act subject to criminal penalty.

NUCYNTA® can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing NUCYNTA® in situations where the physician or pharmacist is concerned about an increased risk of misuse and abuse. Concerns about abuse and addiction should not prevent the proper management of pain. However, all patients treated with mu-opioid agonists require careful monitoring for signs of abuse and addiction, since use of mu-opioid agonist analgesic products carry the risk of addiction even under appropriate medical use [see Drug Abuse and Dependence].

NUCYNTA® may be abused by crushing, chewing, snorting or injecting the product. These practices pose a significant risk to the abuser that could result in overdose and death [see Drug Abuse and Dependence].

Driving and Operating Machinery

Patients should be cautioned that NUCYNTA®may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks such as driving a car or operating machinery. This is to be expected especially at the beginning of treatment, at any change of dosage as well as in combination with alcohol or tranquilizers [see DRUG INTERACTIONS].

Interactions with Alcohol and Drugs of Abuse

Due to its mu-opioid agonist activity, NUCYNTA® may be expected to have additive effects when used in conjunction with alcohol, opioids, or illicit drugs that cause central nervous system depression, respiratory depression, hypotension, and profound sedation, coma or death [see DRUG INTERACTIONS].

Seizures

NUCYNTA® has not been systematically evaluated in patients with a seizure disorder, and such patients were excluded from clinical studies. NUCYNTA® should be prescribed with care in patients with a history of a seizure disorder or any condition that would put the patient at risk of seizures.

Serotonin Syndrome Risk

The development of a potentially life-threatening serotonin syndrome may occur with use of Serotonin and Norepinephrine Reuptake Inhibitor (SNRI) products, including NUCYNTA®, particularly with concomitant use of serotonergic drugs such as Selective Serotonin Reuptake Inhibitors (SSRIs), SNRIs, tricyclic antidepressants (TCAs), MAOIs and triptans, and with drugs that impair metabolism of serotonin (including MAOIs). This may occur within the recommended dose. Serotonin syndrome may include mental-status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination) and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea).

Withdrawal

Withdrawal symptoms may occur if NUCYNTA® is discontinued abruptly. These symptoms may include: anxiety, sweating, insomnia, rigors, pain, nausea, tremors, diarrhea, upper respiratory symptoms, piloerection, and rarely, hallucinations. Withdrawal symptoms may be reduced by tapering NUCYNTA® [see Drug Abuse and Dependence

Hepatic Impairment

A study of NUCYNTA® in subjects with hepatic impairment showed higher serum concentrations than in those with normal hepatic function. NUCYNTA® should be used with caution in patients with moderate hepatic impairment [see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY].

NUCYNTA® has not been studied in patients with severe hepatic impairment and, therefore, use in this population is not recommended.

Use in Pancreatic/Biliary Tract Disease

Like other drugs with mu-opioid agonist activity, NUCYNTA® may cause spasm of the sphincter of Oddi and should be used with caution in patients with biliary tract disease, including acute pancreatitis.

Patient Counseling Information

Physicians are advised to discuss the following issues with patients for whom they prescribe NUCYNTA®:

Instructions for Use

Patients should be advised NUCYNTA® should be taken only as directed and to report episodes of breakthrough pain and adverse experiences occurring during therapy to their physician. Individualization of dosage is essential to make optimal use of this medication. Patients should be advised not to adjust the dose of NUCYNTA® without consulting their physician [see DOSAGE AND ADMINISTRATION]. Patients should be advised that it may be appropriate to taper dosing when discontinuing treatment with NUCYNTA® as withdrawal symptoms may occur [see Drug Abuse and Dependence]. The physician can provide a dose schedule to accomplish a gradual discontinuation of the medication.

Misuse and Abuse

Patients should be advised that NUCYNTA® is a potential drug of abuse. Patients should protect NUCYNTA® from theft, and NUCYNTA® should never be given to anyone other than the individual for whom NUCYNTA® was prescribed [see WARNINGS AND PRECAUTIONS].

Interference with Cognitive and Motor Performance

As NUCYNTA® has the potential to impair judgment, thinking, or motor skills, patients should be cautioned about operating hazardous machinery, including automobiles [see WARNINGS AND PRECAUTIONS].

Pregnancy

Patients should be advised to notify their physician if they become pregnant or intend to become pregnant during treatment with NUCYNTA® [see Use In Specific Populations].

Nursing

Patients should be advised not to breast-feed an infant during treatment with NUCYNTA® [see Use In Specific Populations].

Monoamine Oxidase Inhibitors

Patients should be informed not to take NUCYNTA® while using any drugs that inhibit monoamine oxidase. Patients should not start any new medications while taking NUCYNTA® until they are assured by their healthcare provider that the new medication is not a monoamine oxidase inhibitor.

Seizures

Patients should be informed that NUCYNTA® could cause seizures if they are at risk for seizures or have epilepsy. Such patients should be advised to use NUCYNTA® with care [see WARNINGS AND PRECAUTIONS]. Patients should be advised to stop taking NUCYNTA® if they have a seizure while taking NUCYNTA® and call their healthcare provider right away.

Serotonin Syndrome

Patients should be informed that NUCYNTA® could cause rare but potentially life-threatening conditions resulting from concomitant administration of serotonergic drugs (including Serotonin Reuptake Inhibitors, Serotonin and Norepinephrine Reuptake Inhibitors and tricyclic antidepressants) [see WARNINGS AND PRECAUTIONS].

Patients should be advised to inform their physicians if they are taking, or plan to take, any prescription or over-the-counter drugs as there is a potential for interactions [see DRUG INTERACTIONS].

Alcohol

Patients should be advised to avoid alcohol while taking NUCYNTA® [see DRUG INTERACTIONS].

Medication Guide

See Medication Guide.

Non-Clinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis

Tapentadol was administered to rats (diet) and mice (oral gavage) for two years. In mice, tapentadol HCl was administered by oral gavage at dosages of 50, 100 and 200 mg/kg/day for 2 years (up to 0.2 times the plasma exposure at the maximum recommended human dose [MRHD] on an area under the time-curve [AUC] basis).

No increase in tumor incidence was observed at any dose level.

In rats, tapentadol HCl was administered in diet at dosages of 10, 50, 125 and 250 mg/kg/day for two years (up to 0.2 times in the male rats and 0.6 times in the female rats the MRHD on an AUC basis). No increase in tumor incidence was observed at any dose level.

Mutagenesis

Tapentadol did not induce gene mutations in bacteria, but was clastogenic with metabolic activation in a chromosomal aberration test in V79 cells. The test was repeated and was negative in the presence and absence of metabolic activation. The one positive result for tapentadol was not confirmed in vivo in rats, using the two endpoints of chromosomal aberration and unscheduled DNA synthesis, when tested up to the maximum tolerated dose.

Impairment of Fertility

Tapentadol HCl was administered intravenously to male or female rats at dosages of 3, 6, or 12 mg/kg/day (representing exposures of up to approximately 0.4 times the exposure at the MRHD on an AUC basis, based on extrapolation from toxicokinetic analyses in a separate 4-week intravenous study in rats). Tapentadol did not alter fertility at any dose level. Maternal toxicity and adverse effects on embryonic development, including decreased number of implantations, decreased numbers of live conceptuses, and increased pre- and post-implantation losses occurred at dosages ≥ 6 mg/kg/day.

Use In Specific Populations

Pregnancy

Pregnancy Category C

Tapentadol HCl was evaluated for teratogenic effects in pregnant rats and rabbits following intravenous and subcutaneous exposure during the period of embryofetal organogenesis. When tapentadol was administered twice daily by the subcutaneous route in rats at dose levels of 10, 20, or 40 mg/kg/day [producing up to 1 times the plasma exposure at the maximum recommended human dose (MRHD) of 700 mg/day based on an area under the time-curve (AUC) comparison], no teratogenic effects were observed. Evidence of embryofetal toxicity included transient delays in skeletal maturation (i.e. reduced ossification) at the 40 mg/kg/day dose which was associated with significant maternal toxicity. Administration of tapentadol HCl in rabbits at doses of 4, 10, or 24 mg/kg/day by subcutaneous injection [producing 0.2, 0.6, and 1.85 times the plasma exposure at the MRHD based on an AUC comparison] revealed embryofetal toxicity at doses ≥ 10 mg/kg/day. Findings included reduced fetal viability, skeletal delays and other variations. In addition, there were multiple malformations including gastroschisis/thoracogastroschisis, amelia/phocomelia, and cleft palate at doses ≥ 10 mg/kg/day and above, and ablepharia, encephalopathy, and spina bifida at the high dose of 24 mg/kg/day. Embryofetal toxicity, including malformations, may be secondary to the significant maternal toxicity observed in the study.

In a study of pre- and postnatal development in rats, oral administration of tapentadol at doses of 20, 50, 150, or 300 mg/kg/day to pregnant and lactating rats during the late gestation and early postnatal period [resulting in up to 1.7 times the plasma exposure at the MRHD on an AUC basis] did not influence physical or reflex development, the outcome of neurobehavioral tests or reproductive parameters. Treatment-related developmental delay was observed, including incomplete ossification, and significant reductions in pup body weights and body weight gains at doses associated with maternal toxicity (150 mg/kg/day and above). At maternal tapentadol doses ≥ 150 mg/kg/day, a dose-related increase in pup mortality was observed through postnatal Day 4.

There are no adequate and well controlled studies of NUCYNTA® in pregnant women. NUCYNTA® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Labor and Delivery

The effect of tapentadol on labor and delivery in humans is unknown. NUCYNTA® is not recommended for use in women during and immediately prior to labor and delivery. Due to the mu-opioid receptor agonist activity of NUCYNTA®, neonates whose mothers have been taking NUCYNTA® should be monitored for respiratory depression. A specific opioid antagonist, such as naloxone, should be available for reversal of opioid induced respiratory depression in the neonate.

Nursing Mothers

There is insufficient/limited information on the excretion of tapentadol in human or animal breast milk. Physicochemical and available pharmacodynamic/toxicological data on tapentadol point to excretion in breast milk and risk to the suckling child cannot be excluded. NUCYNTA® should not be used during breast-feeding.

Pediatric Use

The safety and effectiveness of NUCYNTA® in pediatric patients less than 18 years of age have not been established. NUCYNTA® is not recommended in this population.

Geriatric Use

Of the total number of patients in Phase 2/3 double-blind, multiple-dose clinical studies of NUCYNTA®, 19% were 65 and over, while 5% were 75 and over. No overall differences in effectiveness were observed between these patients and younger patients. The rate of constipation was higher in subjects greater than or equal to 65 years than those less than 65 years (12% vs. 7%).

In general, recommended dosing for elderly patients with normal renal and hepatic function is the same as for younger adult patients with normal renal and hepatic function. Because elderly patients are more likely to have decreased renal and hepatic function, consideration should be given to starting elderly patients with the lower range of recommended doses [see CLINICAL PHARMACOLOGY].

Renal Impairment

In patients with severe renal impairment, the safety and effectiveness of NUCYNTA® has not been established. NUCYNTA® is not recommended in this population [see DOSAGE AND ADMINISTRATION].

Hepatic Impairment

Administration of NUCYNTA® resulted in higher exposures and serum levels to tapentadol in subjects with impaired hepatic function compared to subjects with normal hepatic function [see CLINICAL PHARMACOLOGY]. NUCYNTA® should be used with caution in patients with moderate hepatic impairment [see DOSAGE AND ADMINISTRATION].

NUCYNTA® has not been studied in patients with severe hepatic impairment, therefore, use of NUCYNTA® is not recommended in this population [see WARNINGS AND PRECAUTIONS].

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

Human Experience

Experience with NUCYNTA® overdose is very limited. Preclinical data suggest that symptoms similar to those of other centrally acting analgesics with mu-opioid agonist activity are to be expected upon intoxication with tapentadol. In principle, these symptoms may particularly appear in the clinical setting: miosis, vomiting, cardiovascular collapse, consciousness disorders up to coma, convulsions and respiratory depression up to respiratory arrest.

Management of Overdose

Management of overdose should be focused on treating symptoms of mu-opioid agonism. Primary attention should be given to re-establishment of a patent airway and institution of assisted or controlled ventilation when overdose of NUCYNTA® is suspected. Supportive measures (including oxygen and vasopressors) should be employed in the management of circulatory shock and pulmonary edema accompanying overdose as indicated. Cardiac arrest or arrhythmias may require cardiac massage or defibrillation.

Pure opioid antagonists, such as naloxone, are specific antidotes to respiratory depression resulting from opioid overdose. Respiratory depression following an overdose may outlast the duration of action of the opioid antagonist. Administration of an opioid antagonist is not a substitute for continuous monitoring of airway, breathing, and circulation following an opioid overdose. If the response to opioid antagonists is suboptimal or only brief in nature, an additional antagonist should be administered as directed by the manufacturer of the product.

Gastrointestinal decontamination may be considered in order to eliminate unabsorbed drug. Gastrointestinal decontamination with activated charcoal or by gastric lavage is only recommended within 2 hours after intake. Gastrointestinal decontamination at a later time point may be useful in case of intoxication with exceptionally large quantities. Before attempting gastrointestinal decontamination, care should be taken to secure the airway.

CONTRAINDICATIONS

Impaired Pulmonary Function

Like other drugs with mu-opioid agonist activity, NUCYNTA® is contraindicated in patients with significant respiratory depression in unmonitored settings or the absence of resuscitative equipment. NUCYNTA® is also contraindicated in patients with acute or severe bronchial asthma or hypercapnia in unmonitored settings or the absence of resuscitative equipment [see WARNINGS AND PRECAUTIONS].

Paralytic Ileus

Like drugs with mu-opioid agonist activity, NUCYNTA® is contraindicated in any patient who has or is suspected of having paralytic ileus.

Monoamine Oxidase Inhibitors

NUCYNTA® is contraindicated in patients who are receiving monoamine oxidase (MAO) inhibitors or who have taken them within the last 14 days due to potential additive effects on norepinephrine levels which may result in adverse cardiovascular events [see DRUG INTERACTIONS].

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

Mechanism of Action

Tapentadol is a centrally-acting synthetic analgesic. Although its exact mechanism is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.

Pharmacodynamics

Tapentadol is a centrally-acting synthetic analgesic. It is 18 times less potent than morphine in binding to the human mu-opioid receptor and is 2-3 times less potent in producing analgesia in animal models. Tapentadol has been shown to inhibit norepinephrine reuptake in the brains of rats resulting in increased norepinephrine concentrations. In preclinical models, the analgesic activity due to the mu-opioid receptor agonist activity of tapentadol can be antagonized by selective mu-opioid antagonists (e.g., naloxone), whereas the norepinephrine reuptake inhibition is sensitive to norepinephrine modulators. Tapentadol exerts its analgesic effects without a pharmacologically active metabolite.

Effects on the cardiovascular system

There was no effect of therapeutic and supratherapeutic doses of tapentadol on the QT interval. In a randomized, double-blind, placebo- and positive-controlled crossover study, healthy subjects were administered five consecutive doses of NUCYNTA® 100 mg every 6 hours, NUCYNTA® 150 mg every 6 hours, placebo and a single oral dose of moxifloxacin. Similarly, NUCYNTA® had no relevant effect on other ECG parameters (heart rate, PR interval, QRS duration, T-wave or U-wave morphology).

Pharmacokinetics

Absorption

Mean absolute bioavailability after single-dose administration (fasting) is approximately 32% due to extensive first-pass metabolism. Maximum serum concentrations of tapentadol are typically observed at around 1.25 hours after dosing. Dose-proportional increases in the Cmax and AUC values of tapentadol have been observed over the 50 to 150 mg dose range. A multiple (every 6 hour) dose study with doses ranging from 75 to 175 mg tapentadol showed a mean accumulation factor of 1.6 for the parent drug and 1.8 for the major metabolite tapentadol-O-glucuronide, which are primarily determined by the dosing interval and apparent half-life of tapentadol and its metabolite.

Food Effect

The AUC and Cmax increased by 25% and 16%, respectively, when NUCYNTA® was administered after a high-fat, high-calorie breakfast. NUCYNTA® may be given with or without food.

Distribution

Tapentadol is widely distributed throughout the body. Following intravenous administration, the volume of distribution (Vz) for tapentadol is 540 +/- 98 L. The plasma protein binding is low and amounts to approximately 20%.

Metabolism and Elimination

In humans, the metabolism of tapentadol is extensive. About 97% of the parent compound is metabolized. Tapentadol is mainly metabolized via Phase 2 pathways, and only a small amount is metabolized by Phase 1 oxidative pathways. The major pathway of tapentadol metabolism is conjugation with glucuronic acid to produce glucuronides. After oral administration approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) of the dose is excreted in urine in the conjugated form.

A total of 3% of drug was excreted in urine as unchanged drug. Tapentadol is additionally metabolized to N-desmethyl tapentadol (13%) by CYP2C9 and CYP2C19 and to hydroxy tapentadol (2%) by CYP2D6, which are further metabolized by conjugation. Therefore, drug metabolism mediated by cytochrome P450 system is of less importance than phase 2 conjugation.

None of the metabolites contributes to the analgesic activity.

Tapentadol and its metabolites are excreted almost exclusively (99%) via the kidneys. The terminal half-life is on average 4 hours after oral administration. The total clearance is 1530 +/- 177 ml/min.

Special Populations

Elderly

The mean exposure (AUC) to tapentadol was similar in elderly subjects compared to young adults, with a 16% lower mean Cmax observed in the elderly subject group compared to young adult subjects.

Renal Impairment

AUC and Cmax of tapentadol were comparable in subjects with varying degrees of renal function (from normal to severely impaired). In contrast, increasing exposure (AUC) to tapentadol-O-glucuronide was observed with increasing degree of renal impairment. In subjects with mild, moderate, and severe renal impairment, the AUC of tapentadol-O-glucuronide are 1.5-, 2.5-, and 5.5-fold higher compared with normal renal function, respectively.

Hepatic Impairment

Administration of NUCYNTA® resulted in higher exposures and serum levels to tapentadol in subjects with impaired hepatic function compared to subjects with normal hepatic function. The ratio of tapentadol pharmacokinetic parameters for the mild and moderate hepatic impairment groups in comparison to the normal hepatic function group were 1.7 and 4.2, respectively, for AUC; 1.4 and 2.5, respectively, for Cmax; and 1.2 and 1.4, respectively, for t1/2. The rate of formation of tapentadol-O-glucuronide was lower in subjects with increased liver impairment.

Pharmacokinetic Drug Interactions

Tapentadol is mainly metabolized by Phase 2 glucuronidation, a high capacity/low affinity system, therefore, clinically relevant interactions caused by Phase 2 metabolism are unlikely to occur. Naproxen and probenecid increased the AUC of tapentadol by 17% and 57%, respectively. These changes are not considered clinically relevant and no change in dose is required.

No changes in the pharmacokinetic parameters of tapentadol were observed when acetaminophen and acetylsalicylic acid were given concomitantly.

In vitro studies did not reveal any potential of tapentadol to either inhibit or induce cytochrome P450 enzymes. Thus, clinically relevant interactions mediated by the cytochrome P450 system are unlikely to occur.

The pharmacokinetics of tapentadol were not affected when gastric pH or gastrointestinal motility were increased by omeprazole and metoclopramide, respectively.

Plasma protein binding of tapentadol is low (approximately 20%). Therefore, the likelihood of pharmacokinetic drug-drug interactions by displacement from the protein binding site is low.

Animal Toxicology and/or Pharmacology

In toxicological studies with tapentadol, the most common systemic effects of tapentadol were related to the mu-opioid receptor agonist and norepinephrine reuptake inhibition pharmacodynamic properties of the compound. Transient, dose-dependent and predominantly CNS-related findings were observed, including impaired respiratory function and convulsions, the latter occurring in the dog at plasma levels (Cmax) which are in the range associated with the maximum recommended human dose (MRHD).

Clinical Studies

The efficacy and safety of NUCYNTA® in the treatment of moderate to severe acute pain has been established in two randomized, double-blind, placebo- and active-controlled studies of moderate to severe pain from first metatarsal bunionectomy and end-stage degenerative joint disease.

Orthopedic Surgery – Bunionectomy

A randomized, double-blind, parallel-group, active- and placebo-controlled, multiple-dose study demonstrated the efficacy of 50 mg, 75 mg, and 100 mg NUCYNTA® given every 4 to 6 hours for 72 hours in patients aged 18 to 80 years experiencing moderate to severe pain following unilateral, first metatarsal bunionectomy surgery. Patients who qualified for the study with a baseline pain score of ≥ 4 on an 11-point rating scale ranging from 0 to 10 were randomized to 1 of 5 treatments. Patients were allowed to take a second dose of study medication as soon as 1 hour after the first dose on study Day 1, with subsequent dosing every 4 to 6 hours. If rescue analgesics were required, the patients were discontinued for lack of efficacy. Efficacy was evaluated by comparing the sum of pain intensity difference over the first 48 hours (SPID48) versus placebo. NUCYNTA® at each dose provided a greater reduction in pain compared to placebo based on SPID48 values.

For various degrees of improvement from baseline to the 48-hour endpoint, Figure 1 shows the fraction of patients achieving that level of improvement. The figures are cumulative, such that every patient that achieves a 50% reduction in pain from baseline is included in every level of improvement below 50%. Patients who did not complete the 48-hour observation period in the study were assigned 0% improvement.

Figure 1: Percentage of Patients Achieving Various Levels of Pain Relief as Measured by Pain Severity at 48 Hours Compared to Baseline- Post Operative Bunionectomy

Percentage of Patients Achieving Various Levels of Pain Relief - Illustration

The proportions of patients who showed reduction in pain intensity at 48 hours of 30% or greater, or 50% or greater were significantly higher in patients treated with NUCYNTA® at each dose versus placebo.

End-Stage Degenerative Joint Disease

A randomized, double-blind, parallel-group, active- and placebo-controlled, multiple-dose study evaluated the efficacy and safety of 50 mg and 75 mg NUCYNTA® given every 4 to 6 hours during waking hours for 10 days in patients aged 18 to 80 years, experiencing moderate to severe pain from end stage degenerative joint disease of the hip or knee, defined as a 3-day mean pain score of ≥ 5 on an 11-point pain intensity scale, ranging from 0 to 10. Pain scores were assessed twice daily and assessed the pain the patient had experienced over the previous 12 hours. Patients were allowed to continue non-opioid analgesic therapy for which they had been on a stable regimen before screening throughout the study. Eighty-three percent (83%) of patients in the tapentadol treatment groups and the placebo group took such analgesia during the study. The 75 mg treatment group was dosed at 50 mg for the first day of the study, followed by 75 mg for the remaining nine days. Patients requiring rescue analgesics other than study medication were discontinued for lack of efficacy. Efficacy was evaluated by comparing the sum of pain intensity difference (SPID) versus placebo over the first five days of treatment. NUCYNTA® 50 mg and 75 mg provided improvement in pain compared with placebo based on the 5-Day SPID.

For various degrees of improvement from baseline to the Day 5 endpoint, Figure 2 shows the fraction of patients achieving that level of improvement. The figures are cumulative, such that every patient that achieves a 50% reduction in pain from baseline is included in every level of improvement below 50%. Patients who did not complete the 5-day observation period in the study were assigned 0% improvement.

Figure 2: Percentage of Patients Achieving Various Levels of Pain Relief as Measured by Average Pain Severity for the Previous 12 hours, Measured on Study Day 5 Compared to Baseline—End Stage Degenerative Joint Disease

Percentage of Patients Achieving Various Levels of Pain Relief - Illustration

The proportions of patients who showed reduction in pain intensity at 5 days of 30% or greater, or 50% or greater were significantly higher in patients treated with NUCYNTA® at each dose versus placebo.

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

MEDICATION GUIDE

NUCYNTA®
(new-SINN-tah)
(tapentadol) Immediate-Release Oral Tablets

  • NUCYNTA® is a federally controlled substance (C-II) because it can be abused. Keep NUCYNTA® in a safe place to prevent theft. Selling or giving away NUCYNTA® may harm others, and is against the law.
  • Tell your doctor if you (or a family member) have ever abused or been dependent on alcohol, prescription medicines, or street drugs

Read the Medication Guide that comes with NUCYNTA® before you start taking it and each time you get a new prescription. There may be new information. This Medication Guide does not take the place of talking to your doctor about your medical condition or your treatment. Talk to your doctor if you have any questions.

What is the most important information I should know about NUCYNTA®?

NUCYNTA® is a tablet that contains tapentadol, a strong medicine that is a pain medicine.

Use NUCYNTA® exactly how your doctor tells you to. Do not use NUCYNTA® if it has not been prescribed for you.

You should not take NUCYNTA® if your pain is mild and can be controlled with other pain medicines such as non-steroidal anti-inflammatory medicines (NSAIDS) or acetaminophen.

What is NUCYNTA®?

  • NUCYNTA® is a prescription medicine that is used in adults 18 years of age or older to treat moderate to severe pain that is expected to last a short time.
    NUCYNTA® is for short-term use only because the risks for withdrawal symptoms, abuse and addiction are higher when NUCYNTA® is used longer.

Who should not take NUCYNTA®?

Do not take NUCYNTA® if you:

  • have severe lung problems
  • have a gastrointestinal problem called paralytic ileus in which the intestines are not working normally.
  • take a monoamine oxidase inhibitor (MAOI) medicine or have taken an MAOI within the last 14 days. Ask your doctor or pharmacist if any of your medicines is an MAOI.

What should I tell my doctor before taking NUCYNTA®?

NUCYNTA® may not be right for you. Tell your doctor about all your medical conditions, including if you have:

  • trouble breathing or lung problems
  • or had a head injury
  • liver or kidney problems
  • convulsions or seizures
  • dependency problems with alcohol
  • pancreas or gall bladder problems
  • past or present substance abuse or drug addiction. There is a risk of abuse or addiction with narcotic pain medicines. If you have abused drugs in the past, you may have a higher chance of developing abuse or addiction again while using NUCYNTA®.
  • are pregnant or plan to become pregnant
  • are breast-feeding. You should not breast-feed while taking NUCYNTA®.

Tell your doctor about all the medicines you take, including prescription and nonprescription medicines, vitamins, and herbal supplements. Using NUCYNTA® with other medicines can cause serious side effects. The doses of some other medicines may need to be changed. Your doctor can tell you what medicines can be safely taken with NUCYNTA®. Especially tell your doctor if you take:

  • Monoamine Oxidase Inhibitors (MAOIs). See “Who should not take NUCYNTA®.”
  • any medicine that makes you sleepy. NUCYNTA® can make you sleepy and affect your breathing. Taking these medicines together can be dangerous.

How should I take NUCYNTA®?

  • Do not take NUCYNTA® unless it has been prescribed for you by your doctor.
  • Take NUCYNTA® exactly as prescribed by your doctor.
  • Do not change the dose of NUCYNTA® unless your doctor tells you to. Your doctor may change your dose after seeing how the medicine affects you. Do not use NUCYNTA® more often than prescribed. Call your doctor if your pain is not well controlled while taking NUCYNTA®.
  • Follow your doctor's instructions about how to slowly stop taking NUCYNTA® to help lessen withdrawal symptoms.
  • NUCYNTA® can be taken with or without food.

What should I avoid while taking NUCYNTA®?

  • Do not drive, operate machinery, or participate in any other possibly dangerous activities until you know how you react to this medicine. NUCYNTA® can make you sleepy.
  • You should not drink alcohol while using NUCYNTA®. Alcohol increases your chance of having dangerous side effects.

What are the possible side effects of NUCYNTA®?

NUCYNTA® can cause serious side effects including:

  • Life-threatening breathing problems. Call your doctor right away or get emergency medical help if you:
    • have trouble breathing, or have slow or shallow breathing
    • have a slow heartbeat
    • have severe sleepiness
    • have cold, clammy skin
    • feel faint, dizzy, confused, or can not think, walk or talk normally
    • have a seizure
    • have hallucinations
  • Physical Dependence. NUCYNTA® can cause physical dependence. Talk to your doctor about slowly stopping NUCYNTA® to avoid getting sick with withdrawal symptoms. You could become sick with uncomfortable symptoms because your body has become used to the medicine. Tell your doctor if you have any of these symptoms of withdrawal: feeling anxious, sweating, sleep problems, shivering, pain, nausea, tremors, diarrhea, upper respiratory symptoms, hallucinations, hair “standing on end.” Physical dependence is not the same as drug addiction. Your doctor can tell you more about the differences between physical dependence and drug addiction.
  • Serotonin syndrome. Serotonin syndrome is a rare, lifethreatening problem that could happen if you take NUCYNTA® with Selective Serotonin Reuptake Inhibitors (SSRIs), Serotonin and Norepinephrine Reuptake Inhibitors (SNRIs), Monoamine Oxidase Inhibitors (MAOIs), triptans or certain other medicines. Call your doctor or get medical help right away if you have any one or more of the these symptoms: you feel agitated, have hallucinations, coma, rapid heart beat, feel overheated, loss of coordination, over active reflexes, nausea, vomiting, or diarrhea.
  • Seizures. NUCYNTA® can cause seizures in people who are at risk for seizures or who have epilepsy. Tell your doctor right away if you have a seizure and stop taking NUCYNTA®.
  • Low blood pressure. This can make you feel dizzy if you get up too fast from sitting or lying down.

The common side effects with NUCYNTA® are nausea, dizziness, vomiting, sleepiness, and itching.

Constipation is a common side effect of all opioid medicines. Talk to your doctor about the use of laxatives and stool softeners to prevent or treat constipation while taking NUCYNTA®.

Tell your doctor about any side effect that bothers you or that does not go away. These are not all the possible side effects of

NUCYNTA®. For a complete list, ask your doctor or pharmacist.

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

How should I store NUCYNTA®?

  • Store NUCYNTA® at 59°F to 86°F (15°C to 30°C). Keep NUCYNTA® tablets dry.
  • Dispose of NUCYNTA® tablets you no longer need.

Keep NUCYNTA® in a safe place out of the reach of children.

General information about NUCYNTA®

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use NUCYNTA® for a condition for which it was not prescribed. Do not give NUCYNTA® to other people, even if they have the same symptoms you have. Sharing NUCYNTA® could be harmful and is against the law.

This Medication Guide summarizes the most important information about NUCYNTA®. If you would like more information, talk with your doctor. You can ask your doctor or pharmacist for information about NUCYNTA® that is written for doctors. For more information about NUCYNTA® call 1-800-526-7736.

What are the ingredients in NUCYNTA®?

Active Ingredient: tapentadol

Inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, and Opadry® II, a proprietary film-coating mixture containing polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and aluminum lake coloring.

This Medication Guide has been approved by the U.S. Food and Drug Administration.

Medication Guide

NUCYNTA®
(new-SINN-tah)
(tapentadol) oral solution

What is the most important information I should know about NUCYNTA® oral solution?

  • Get emergency help right away if you take too much NUCYNTA® oral solution (overdose). NUCYNTA® oral solution can cause life threatening breathing problems that can lead to death.
  • Never give anyone else your NUCYNTA® oral solution. They could die from taking it. Store NUCYNTA® oral solution away from children and in a safe place to prevent stealing or abuse. Selling or giving away NUCYNTA® oral solution is against the law.
  • Do not change your dose. Take NUCYNTA® oral solution exactly as prescribed by your healthcare provider.
  • Always use the oral syringe provided with NUCYNTA® oral solution, 20 mg/mL to help make sure you measure the right amount.

What is NUCYNTA® oral solution?

NUCYNTA® oral solution is a strong prescription pain medicine that contains an opioid (narcotic) that is used to treat moderate to severe pain that is expected to last a short time.

Who should not take NUCYNTA® oral solution?

Do not take NUCYNTA® oral solution if you:

  • have severe asthma, trouble breathing, or other lung problems
  • have a bowel blockage or narrowing of the stomach or intestines
  • take a monoamine oxidase inhibitor (MAOI) medicine or have taken an MAOI medicine within the last 14 days
  • are allergic to tapentadol or any of its ingredients.

What should I tell my healthcare provider before taking NUCYNTA® oral solution?

Before taking NUCYNTA® oral solution, tell your healthcare provider if you have a history of:

  • head injury, seizures
  • liver, kidney, thyroid problems
  • problems urinating
  • pancreas or gallbladder problems
  • abuse of street or prescription drugs, alcohol addiction, or mental health problems.

Tell your healthcare provider if you are:

  • pregnant or planning to become pregnant. NUCYNTA® oral solution may harm your unborn baby.
  • breastfeeding. NUCYNTA® oral solution may pass into your breast milk and harm your baby.
  • planning to have surgery
  • taking prescription or over-the-counter medicines, vitamins, or herbal supplements.

How should I take NUCYNTA® oral solution?

  • Do not change your dose. Take NUCYNTA® oral solution exactly as prescribed by your healthcare provider.
  • If you miss a dose of NUCYNTA® oral solution you can take the dose when you remember if you have pain, or you can wait for the next dose.
  • You can take NUCYNTA® oral solution with or without food.
  • Make sure you understand exactly how to measure your dose. Always use the oral syringe provided with your NUCYNTA® oral solution to help make sure you measure the right amount. Call your pharmacist if you have difficulties with measuring your medicine.
  • Call your healthcare provider if the dose you are taking does not control your pain.
  • Do not stop taking NUCYNTA® oral solution without talking to your healthcare provider.
  • After you stop taking NUCYNTA® oral solution, flush any unused oral solution down the toilet.

What should I avoid while taking NUCYNTA® oral solution?

While taking NUCYNTA® oral solution do not:

  • Drive or operate heavy machinery, until you know how NUCYNTA® oral solution affects you. NUCYNTA® oral solution can make you sleepy, dizzy, or lightheaded.
  • Drink alcohol or use prescription or over-the-counter medicines that contain alcohol.

What are the possible side effects of NUCYNTA® oral solution?

The possible side effects of NUCYNTA® oral solution are:

  • constipation, nausea, dizziness, vomiting, and sleepiness. Call your healthcare provider if you have any of these symptoms and they are severe.

Get emergency medical help if you:

  • have trouble breathing, shortness of breath, fast heartbeat, chest pain, swelling of your face, tongue or throat, extreme drowsiness, a seizure, or you are feeling faint.
  • are feeling agitated or restless, have hallucinations, pass out (become unconscious), feel overheated, have heavy sweating that is not due to activity, or loss of coordination.

These are not all the possible side effects of NUCYNTA® oral solution.

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

For more information, go to dailymed.nlm.nih.gov

Instructions for Use

NUCYNTA®
(tapentadol), oral solution 20 mg/mL

Read the Instructions for Use before you start taking NUCYNTA® oral solution and each time you get a refill. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.

Important information about measuring NUCYNTA® oral solution

  • Always use the oral syringe provided with your NUCYNTA® oral solution to make sure you measure the right amount.
  • You will be provided (See Figure A.):
    • 1 bottle of NUCYNTA® oral solution
    • 1 oral syringe
    • 1 adapter

If you do not receive an oral syringe with your NUCYNTA® oral solution, ask your pharmacist to give you one.

Figure A

What is provided - Illustration

Before you use NUCYNTA® oral solution for the first time:

1. Remove the child-resistant cap and completely remove the foil seal (See Figure B).

Figure B

Remove the child-resistant cap - Illustration

2. Push the ribbed end of the adapter into the neck of the bottle until it is firmly in place. The bottom edge of the adapter should fully contact the top rim of the bottle (See Figure C). Do not remove the adapter from the bottle after it is inserted.

Figure C

Push the ribbed end of the adapter into the neck of the bottle - Illustration

To prepare a dose of NUCYNTA® oral solution:

3. Hold the oral syringe in one hand. With your other hand, fully push down (depress) the plunger (See Figure D).

Figure D

Push down (depress) the plunger - Illustration

4. Insert the tip of the oral syringe into the adapter (See Figure E).

Figure E

Insert the tip of the oral syringe into the adapter - Illustration

5. Turn the bottle upside down. Pull back slowly on the oral syringe plunger to withdraw the dose prescribed by your healthcare provider (2.5 mL, 3.75 mL, or 5 mL). If you see air bubbles in the oral syringe, fully push in the plunger so that the oral solution flows back into the bottle. Then, withdraw your prescribed dose of oral solution (See Figure F).

Figure F

Withdraw your prescribed dose - Illustration

6. Leave the oral syringe in the bottle adapter and turn the bottle right-side up. Place the bottle onto a flat surface. Remove the oral syringe from the bottle (See Figure G).

Figure G

Remove the oral syringe - Illustration

7. Place the tip of the oral syringe in your mouth. Squirt the oral solution into your mouth by pushing on the plunger until the oral syringe is empty (See Figure H).

Figure H

Place the tip of the oral syringe in your mouth - Illustration

8. Leave the adapter in the bottle. Put the childresistant cap back on the bottle. (See Figure I).

Figure I

Put the childresistant cap back - Illustration

9. Remove the plunger from the oral syringe barrel. Rinse the oral syringe with water after each use and let it air dry. When the oral syringe is dry, put the plunger back into the oral syringe barrel for the next use. Do not throw away the oral syringe.

  • Talk to your pharmacist if you have questions about how to use the oral syringe, or if you lose or misplace the oral syringe.

What are the ingredients in NUCYNTA® oral solution?

Active ingredient: tapentadol

Inactive ingredients: citric acid monohydrate, sucralose, raspberry flavor, sodium hydroxide, and purified water.

How should I store NUCYNTA® oral solution?

  • Store NUCYNTA® oral solution at room temperature between 68°F to 77°F (20°C to 25°C).
  • Store the NUCYNTA® oral solution bottle upright after opening. Keep the oral syringe with your medicine.
  • After you stop taking NUCYNTA® oral solution, flush the unused oral solution down the toilet.

Keep NUCYNTA® oral solution out of the reach of children.

This Instructions for Use has been approved by the U.S. Food and Drug Administration.

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

>

PATIENT INFORMATION

MEDICATION GUIDE

NUCYNTA®
(new-SINN-tah)
(tapentadol) Immediate-Release Oral Tablets

  • NUCYNTA® is a federally controlled substance (C-II) because it can be abused. Keep NUCYNTA® in a safe place to prevent theft. Selling or giving away NUCYNTA® may harm others, and is against the law.
  • Tell your doctor if you (or a family member) have ever abused or been dependent on alcohol, prescription medicines, or street drugs

Read the Medication Guide that comes with NUCYNTA® before you start taking it and each time you get a new prescription. There may be new information. This Medication Guide does not take the place of talking to your doctor about your medical condition or your treatment. Talk to your doctor if you have any questions.

What is the most important information I should know about NUCYNTA®?

NUCYNTA® is a tablet that contains tapentadol, a strong medicine that is a pain medicine.

Use NUCYNTA® exactly how your doctor tells you to. Do not use NUCYNTA® if it has not been prescribed for you.

You should not take NUCYNTA® if your pain is mild and can be controlled with other pain medicines such as non-steroidal anti-inflammatory medicines (NSAIDS) or acetaminophen.

What is NUCYNTA®?

  • NUCYNTA® is a prescription medicine that is used in adults 18 years of age or older to treat moderate to severe pain that is expected to last a short time.
    NUCYNTA® is for short-term use only because the risks for withdrawal symptoms, abuse and addiction are higher when NUCYNTA® is used longer.

Who should not take NUCYNTA®?

Do not take NUCYNTA® if you:

  • have severe lung problems
  • have a gastrointestinal problem called paralytic ileus in which the intestines are not working normally.
  • take a monoamine oxidase inhibitor (MAOI) medicine or have taken an MAOI within the last 14 days. Ask your doctor or pharmacist if any of your medicines is an MAOI.

What should I tell my doctor before taking NUCYNTA®?

NUCYNTA® may not be right for you. Tell your doctor about all your medical conditions, including if you have:

  • trouble breathing or lung problems
  • or had a head injury
  • liver or kidney problems
  • convulsions or seizures
  • dependency problems with alcohol
  • pancreas or gall bladder problems
  • past or present substance abuse or drug addiction. There is a risk of abuse or addiction with narcotic pain medicines. If you have abused drugs in the past, you may have a higher chance of developing abuse or addiction again while using NUCYNTA®.
  • are pregnant or plan to become pregnant
  • are breast-feeding. You should not breast-feed while taking NUCYNTA®.

Tell your doctor about all the medicines you take, including prescription and nonprescription medicines, vitamins, and herbal supplements. Using NUCYNTA® with other medicines can cause serious side effects. The doses of some other medicines may need to be changed. Your doctor can tell you what medicines can be safely taken with NUCYNTA®. Especially tell your doctor if you take:

  • Monoamine Oxidase Inhibitors (MAOIs). See “Who should not take NUCYNTA®.”
  • any medicine that makes you sleepy. NUCYNTA® can make you sleepy and affect your breathing. Taking these medicines together can be dangerous.

How should I take NUCYNTA®?

  • Do not take NUCYNTA® unless it has been prescribed for you by your doctor.
  • Take NUCYNTA® exactly as prescribed by your doctor.
  • Do not change the dose of NUCYNTA® unless your doctor tells you to. Your doctor may change your dose after seeing how the medicine affects you. Do not use NUCYNTA® more often than prescribed. Call your doctor if your pain is not well controlled while taking NUCYNTA®.
  • Follow your doctor's instructions about how to slowly stop taking NUCYNTA® to help lessen withdrawal symptoms.
  • NUCYNTA® can be taken with or without food.

What should I avoid while taking NUCYNTA®?

  • Do not drive, operate machinery, or participate in any other possibly dangerous activities until you know how you react to this medicine. NUCYNTA® can make you sleepy.
  • You should not drink alcohol while using NUCYNTA®. Alcohol increases your chance of having dangerous side effects.

What are the possible side effects of NUCYNTA®?

NUCYNTA® can cause serious side effects including:

  • Life-threatening breathing problems. Call your doctor right away or get emergency medical help if you:
    • have trouble breathing, or have slow or shallow breathing
    • have a slow heartbeat
    • have severe sleepiness
    • have cold, clammy skin
    • feel faint, dizzy, confused, or can not think, walk or talk normally
    • have a seizure
    • have hallucinations
  • Physical Dependence. NUCYNTA® can cause physical dependence. Talk to your doctor about slowly stopping NUCYNTA® to avoid getting sick with withdrawal symptoms. You could become sick with uncomfortable symptoms because your body has become used to the medicine. Tell your doctor if you have any of these symptoms of withdrawal: feeling anxious, sweating, sleep problems, shivering, pain, nausea, tremors, diarrhea, upper respiratory symptoms, hallucinations, hair “standing on end.” Physical dependence is not the same as drug addiction. Your doctor can tell you more about the differences between physical dependence and drug addiction.
  • Serotonin syndrome. Serotonin syndrome is a rare, lifethreatening problem that could happen if you take NUCYNTA® with Selective Serotonin Reuptake Inhibitors (SSRIs), Serotonin and Norepinephrine Reuptake Inhibitors (SNRIs), Monoamine Oxidase Inhibitors (MAOIs), triptans or certain other medicines. Call your doctor or get medical help right away if you have any one or more of the these symptoms: you feel agitated, have hallucinations, coma, rapid heart beat, feel overheated, loss of coordination, over active reflexes, nausea, vomiting, or diarrhea.
  • Seizures. NUCYNTA® can cause seizures in people who are at risk for seizures or who have epilepsy. Tell your doctor right away if you have a seizure and stop taking NUCYNTA®.
  • Low blood pressure. This can make you feel dizzy if you get up too fast from sitting or lying down.

The common side effects with NUCYNTA® are nausea, dizziness, vomiting, sleepiness, and itching.

Constipation is a common side effect of all opioid medicines. Talk to your doctor about the use of laxatives and stool softeners to prevent or treat constipation while taking NUCYNTA®.

Tell your doctor about any side effect that bothers you or that does not go away. These are not all the possible side effects of

NUCYNTA®. For a complete list, ask your doctor or pharmacist.

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

How should I store NUCYNTA®?

  • Store NUCYNTA® at 59°F to 86°F (15°C to 30°C). Keep NUCYNTA® tablets dry.
  • Dispose of NUCYNTA® tablets you no longer need.

Keep NUCYNTA® in a safe place out of the reach of children.

General information about NUCYNTA®

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use NUCYNTA® for a condition for which it was not prescribed. Do not give NUCYNTA® to other people, even if they have the same symptoms you have. Sharing NUCYNTA® could be harmful and is against the law.

This Medication Guide summarizes the most important information about NUCYNTA®. If you would like more information, talk with your doctor. You can ask your doctor or pharmacist for information about NUCYNTA® that is written for doctors. For more information about NUCYNTA® call 1-800-526-7736.

What are the ingredients in NUCYNTA®?

Active Ingredient: tapentadol

Inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, and Opadry® II, a proprietary film-coating mixture containing polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and aluminum lake coloring.

This Medication Guide has been approved by the U.S. Food and Drug Administration.

Medication Guide

NUCYNTA®
(new-SINN-tah)
(tapentadol) oral solution

What is the most important information I should know about NUCYNTA® oral solution?

  • Get emergency help right away if you take too much NUCYNTA® oral solution (overdose). NUCYNTA® oral solution can cause life threatening breathing problems that can lead to death.
  • Never give anyone else your NUCYNTA® oral solution. They could die from taking it. Store NUCYNTA® oral solution away from children and in a safe place to prevent stealing or abuse. Selling or giving away NUCYNTA® oral solution is against the law.
  • Do not change your dose. Take NUCYNTA® oral solution exactly as prescribed by your healthcare provider.
  • Always use the oral syringe provided with NUCYNTA® oral solution, 20 mg/mL to help make sure you measure the right amount.

What is NUCYNTA® oral solution?

NUCYNTA® oral solution is a strong prescription pain medicine that contains an opioid (narcotic) that is used to treat moderate to severe pain that is expected to last a short time.

Who should not take NUCYNTA® oral solution?

Do not take NUCYNTA® oral solution if you:

  • have severe asthma, trouble breathing, or other lung problems
  • have a bowel blockage or narrowing of the stomach or intestines
  • take a monoamine oxidase inhibitor (MAOI) medicine or have taken an MAOI medicine within the last 14 days
  • are allergic to tapentadol or any of its ingredients.

What should I tell my healthcare provider before taking NUCYNTA® oral solution?

Before taking NUCYNTA® oral solution, tell your healthcare provider if you have a history of:

  • head injury, seizures
  • liver, kidney, thyroid problems
  • problems urinating
  • pancreas or gallbladder problems
  • abuse of street or prescription drugs, alcohol addiction, or mental health problems.

Tell your healthcare provider if you are:

  • pregnant or planning to become pregnant. NUCYNTA® oral solution may harm your unborn baby.
  • breastfeeding. NUCYNTA® oral solution may pass into your breast milk and harm your baby.
  • planning to have surgery
  • taking prescription or over-the-counter medicines, vitamins, or herbal supplements.

How should I take NUCYNTA® oral solution?

  • Do not change your dose. Take NUCYNTA® oral solution exactly as prescribed by your healthcare provider.
  • If you miss a dose of NUCYNTA® oral solution you can take the dose when you remember if you have pain, or you can wait for the next dose.
  • You can take NUCYNTA® oral solution with or without food.
  • Make sure you understand exactly how to measure your dose. Always use the oral syringe provided with your NUCYNTA® oral solution to help make sure you measure the right amount. Call your pharmacist if you have difficulties with measuring your medicine.
  • Call your healthcare provider if the dose you are taking does not control your pain.
  • Do not stop taking NUCYNTA® oral solution without talking to your healthcare provider.
  • After you stop taking NUCYNTA® oral solution, flush any unused oral solution down the toilet.

What should I avoid while taking NUCYNTA® oral solution?

While taking NUCYNTA® oral solution do not:

  • Drive or operate heavy machinery, until you know how NUCYNTA® oral solution affects you. NUCYNTA® oral solution can make you sleepy, dizzy, or lightheaded.
  • Drink alcohol or use prescription or over-the-counter medicines that contain alcohol.

What are the possible side effects of NUCYNTA® oral solution?

The possible side effects of NUCYNTA® oral solution are:

  • constipation, nausea, dizziness, vomiting, and sleepiness. Call your healthcare provider if you have any of these symptoms and they are severe.

Get emergency medical help if you:

  • have trouble breathing, shortness of breath, fast heartbeat, chest pain, swelling of your face, tongue or throat, extreme drowsiness, a seizure, or you are feeling faint.
  • are feeling agitated or restless, have hallucinations, pass out (become unconscious), feel overheated, have heavy sweating that is not due to activity, or loss of coordination.

These are not all the possible side effects of NUCYNTA® oral solution.

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

For more information, go to dailymed.nlm.nih.gov

Instructions for Use

NUCYNTA®
(tapentadol), oral solution 20 mg/mL

Read the Instructions for Use before you start taking NUCYNTA® oral solution and each time you get a refill. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.

Important information about measuring NUCYNTA® oral solution

  • Always use the oral syringe provided with your NUCYNTA® oral solution to make sure you measure the right amount.
  • You will be provided (See Figure A.):
    • 1 bottle of NUCYNTA® oral solution
    • 1 oral syringe
    • 1 adapter

If you do not receive an oral syringe with your NUCYNTA® oral solution, ask your pharmacist to give you one.

Figure A

What is provided - Illustration

Before you use NUCYNTA® oral solution for the first time:

1. Remove the child-resistant cap and completely remove the foil seal (See Figure B).

Figure B

Remove the child-resistant cap - Illustration

2. Push the ribbed end of the adapter into the neck of the bottle until it is firmly in place. The bottom edge of the adapter should fully contact the top rim of the bottle (See Figure C). Do not remove the adapter from the bottle after it is inserted.

Figure C

Push the ribbed end of the adapter into the neck of the bottle - Illustration

To prepare a dose of NUCYNTA® oral solution:

3. Hold the oral syringe in one hand. With your other hand, fully push down (depress) the plunger (See Figure D).

Figure D

Push down (depress) the plunger - Illustration

4. Insert the tip of the oral syringe into the adapter (See Figure E).

Figure E

Insert the tip of the oral syringe into the adapter - Illustration

5. Turn the bottle upside down. Pull back slowly on the oral syringe plunger to withdraw the dose prescribed by your healthcare provider (2.5 mL, 3.75 mL, or 5 mL). If you see air bubbles in the oral syringe, fully push in the plunger so that the oral solution flows back into the bottle. Then, withdraw your prescribed dose of oral solution (See Figure F).

Figure F

Withdraw your prescribed dose - Illustration

6. Leave the oral syringe in the bottle adapter and turn the bottle right-side up. Place the bottle onto a flat surface. Remove the oral syringe from the bottle (See Figure G).

Figure G

Remove the oral syringe - Illustration

7. Place the tip of the oral syringe in your mouth. Squirt the oral solution into your mouth by pushing on the plunger until the oral syringe is empty (See Figure H).

Figure H

Place the tip of the oral syringe in your mouth - Illustration

8. Leave the adapter in the bottle. Put the childresistant cap back on the bottle. (See Figure I).

Figure I

Put the childresistant cap back - Illustration

9. Remove the plunger from the oral syringe barrel. Rinse the oral syringe with water after each use and let it air dry. When the oral syringe is dry, put the plunger back into the oral syringe barrel for the next use. Do not throw away the oral syringe.

  • Talk to your pharmacist if you have questions about how to use the oral syringe, or if you lose or misplace the oral syringe.

What are the ingredients in NUCYNTA® oral solution?

Active ingredient: tapentadol

Inactive ingredients: citric acid monohydrate, sucralose, raspberry flavor, sodium hydroxide, and purified water.

How should I store NUCYNTA® oral solution?

  • Store NUCYNTA® oral solution at room temperature between 68°F to 77°F (20°C to 25°C).
  • Store the NUCYNTA® oral solution bottle upright after opening. Keep the oral syringe with your medicine.
  • After you stop taking NUCYNTA® oral solution, flush the unused oral solution down the toilet.

Keep NUCYNTA® oral solution out of the reach of children.

This Instructions for Use has been approved by the U.S. Food and Drug Administration.

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

NUCYNTA®
(tapentadol) Immediate-Release Oral Tablets

DRUG DESCRIPTION

NUCYNTA® (tapentadol) Tablets are immediate-release film-coated tablets for oral administration. The chemical name is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2- methylpropyl]phenol monohydrochloride. The structural formula is:

NUCYNTA® (tapentadol) Structural Formula Illustration

The molecular weight of tapentadol HCl is 257.80, and the molecular formula is C14H23NO·HCl. The n-octanol:water partition coefficient log P value is 2.87. The pKa values are 9.34 and 10.45. In addition to the active ingredient tapentadol HCl, tablets also contain the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, and Opadry® II, a proprietary film-coating mixture containing polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and aluminum lake coloring.

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

NUCYNTA®
(tapentadol) Immediate-Release Oral Tablets

DRUG DESCRIPTION

NUCYNTA® (tapentadol) Tablets are immediate-release film-coated tablets for oral administration. The chemical name is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2- methylpropyl]phenol monohydrochloride. The structural formula is:

NUCYNTA® (tapentadol) Structural Formula Illustration

The molecular weight of tapentadol HCl is 257.80, and the molecular formula is C14H23NO·HCl. The n-octanol:water partition coefficient log P value is 2.87. The pKa values are 9.34 and 10.45. In addition to the active ingredient tapentadol HCl, tablets also contain the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, and Opadry® II, a proprietary film-coating mixture containing polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and aluminum lake coloring.

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

NUCYNTA®
(tapentadol) Immediate-Release Oral Tablets

DRUG DESCRIPTION

NUCYNTA® (tapentadol) Tablets are immediate-release film-coated tablets for oral administration. The chemical name is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2- methylpropyl]phenol monohydrochloride. The structural formula is:

NUCYNTA® (tapentadol) Structural Formula Illustration

The molecular weight of tapentadol HCl is 257.80, and the molecular formula is C14H23NO·HCl. The n-octanol:water partition coefficient log P value is 2.87. The pKa values are 9.34 and 10.45. In addition to the active ingredient tapentadol HCl, tablets also contain the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, and Opadry® II, a proprietary film-coating mixture containing polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and aluminum lake coloring.

Last reviewed on RxList: 11/20/2012
This monograph has been modified to include the generic and brand name in many instances.

Nucynta Patient Information Including Side Effects

Brand Names: Nucynta, Nucynta ER

Generic Name: tapentadol (Pronunciation: ta PEN ta dol)

What is tapentadol (Nucynta)?

Tapentadol is in a group of drugs called narcotic pain relievers. It is similar to morphine.

Tapentadol is used to treat moderate to severe chronic pain.

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

Nucynta 100 mg

round, orange, imprinted with O-M, 100

Nucynta 50 mg

round, yellow, imprinted with O-M, 50

Nucynta 75 mg

round, orange, imprinted with O-M, 75

What are the possible side effects of tapentadol (Nucynta)?

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.

Call your doctor at once if you have a serious side effect such as:

  • weak or shallow breathing, weak pulse, slow heartbeat;
  • seizure (convulsions);
  • severe drowsiness or dizziness;
  • confusion, problems with speech or balance; or
  • agitation, hallucinations, fever, fast heart rate, overactive reflexes, nausea, vomiting, diarrhea, loss of coordination, fainting.

Less serious side effects may include:

  • mild nausea or vomiting;
  • constipation;
  • mild dizziness, drowsiness;
  • dry mouth;
  • itching; or
  • increased sweating.

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 Nucynta (tapentadol immediate-release oral tablets) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about tapentadol (Nucynta)?

You should not use this medication if you are allergic to tapentadol, or if you have severe liver or kidney disease, if you are having an asthma attack, or if you have a bowel obstruction called paralytic ileus.

Do not use tapentadol if you have used an MAO inhibitor such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate) in the last 14 days. A dangerous drug interaction could occur, leading to serious side effects.

Tapentadol may be habit-forming and should be used only by the person it was prescribed for. Keep the medication in a secure place where others cannot get to it.

Do not drink alcohol while you are taking tapentadol. Dangerous side effects or death can occur when alcohol is combined with a narcotic pain medicine. Check your food and medicine labels to be sure these products do not contain alcohol.

Never take tapentadol in larger amounts, or for longer than recommended by your doctor. Tell your doctor if the medicine seems to stop working as well in relieving your pain.

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

Do not stop using tapentadol suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to avoid withdrawal symptoms when you stop using tapentadol.

Side Effects Centers

Nucynta Patient Information including How Should I Take

What should I discuss with my healthcare provider before taking tapentadol (Nucynta)?

You should not use this medication if you are allergic to tapentadol, or if you have severe liver or kidney disease, if you are having an asthma attack, or if you have a bowel obstruction called paralytic ileus.

Do not use tapentadol if you have used an MAO inhibitor such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate) in the last 14 days. A dangerous drug interaction could occur, leading to serious side effects.

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

  • asthma, COPD, sleep apnea, or other breathing disorders;
  • liver or kidney disease;
  • curvature of the spine;
  • a history of head injury or brain tumor;
  • epilepsy or other seizure disorder;
  • gallbladder disease or pancreas problems;
  • mental illness; or
  • a history of drug or alcohol addiction.

FDA pregnancy category C. It is not known whether this medication is harmful to an unborn baby. Tapentadol may cause breathing problems and addiction or withdrawal symptoms in a newborn if the mother takes the medication during pregnancy. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

Tapentadol can pass into breast milk and may harm a nursing baby. Do not breast-feed while taking this medication.

Tapentadol may be habit forming and should be used only by the person it was prescribed for. Never share tapentadol with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot get to it.

Older adults may be more sensitive to the effects of this medicine.

Do not give tapentadol to a child.

How should I take tapentadol (Nucynta)?

Take exactly as prescribed. Never take tapentadol in larger amounts, or for longer than recommended by your doctor. Follow the directions on your prescription label. Tell your doctor if the medicine seems to stop working as well in relieving your pain.

Your doctor may occasionally change the timing of your dose to make sure you get the best results.

Take this medicine with a full glass of water.

You may take tapentadol with or without food.

Do not crush, chew, or break an extended-release tablet. Swallow it whole. Breaking or opening the pill may cause too much of the drug to be released at one time.

Tapentadol can cause constipation. Talk to your doctor before using a laxative or stool softener to treat or prevent this side effect.

Do not stop using tapentadol suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to avoid withdrawal symptoms when you stop using tapentadol.

Store at room temperature away from moisture and heat.

Keep track of the amount of medicine used from each new bottle. Tapentadol is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.

Ask a pharmacist about how to dispose of any unused pills after you have stopped taking tapentadol.

Never crush a tablet or other pill to mix into a liquid for snorting tapentadol or injecting the drug into your vein. This practice has resulted in death with the misuse of narcotic pain medicines and similar prescription drugs.

Side Effects Centers

Nucynta Patient Information including If I Miss a Dose

What happens if I miss a dose (Nucynta)?

Since tapentadol is taken as needed, you may not be on a dosing schedule. If you are taking the medication regularly, 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 (Nucynta)?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An overdose of tapentadol can be fatal.

Overdose symptoms may include extreme drowsiness, blurred vision, confusion, vomiting, cold and clammy skin, weak pulse, shallow breathing, fainting, or breathing that stops.

What should I avoid while taking tapentadol (Nucynta)?

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

Do not drink alcohol while you are using tapentadol. Dangerous side effects or death can occur when alcohol is combined with tapentadol. Check your food and medicine labels to be sure these products do not contain alcohol.

What other drugs will affect tapentadol (Nucynta)?

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

There may be other drugs that can interact with tapentadol. 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 tapentadol.


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: 3.01. Revision date: 9/20/2011.

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.

Healthwise

Side Effects Centers

توزیع کنندگان این دارو
شرکت های تولید کننده یا وارد کننده دارو

دارونـــما
نوآوری برای سلامت

طراحی و اجرا M.Ramezani
ارتباط با ما Info@darunama.com