NUCYNTA ER (Tapentadol Extended-Release Tablets)
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NUCYNTA ER (tapentadol extended-release tablets) is an oral analgesic taken twice daily for the management of moderate to severe chronic pain in adults when a continuous, around-the-clock opioid analgesic is required for an extended period of time.
NUCYNTA ER was approved by the U.S. Food and Drug Administration in August 2011. NUCYNTA (Tapentadol immediate-release tablets) was approved by the FDA on November 20, 2008 for the relief of moderate to severe acute pain in patients 18 years of age or older.
Tapentadol is a centrally-acting synthetic analgesic. The tapentadol molecule is classified as Schedule II of the Controlled Substances Act.
Both NUCYNTA and NUCYNTA ER are available by prescription only and have an abuse liability similar to other opioid analgesics.
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Important Safety Information for NUCYNTA ER
Potential for Abuse
NUCYNTA ER contains tapentadol, a mu-opioid agonist and a Schedule II controlled substance with a high risk for abuse. NUCYNTA ER can be abused in a manner similar to other opioid agonists, whether legal or illicit. Such risks should be considered when doctors prescribe or dispense NUCYNTA ER in situations where the doctor or pharmacist is concerned about an increased risk of misuse, abuse, or diversion of the medication. Schedule II opioid substances, including morphine, hydromorphone, oxycodone, fentanyl, oxymorphone, and methadone, have the highest potential for abuse and risk of fatal overdose due to respiratory depression.
Proper Patient Selection
NUCYNTA ER, an extended-release formulation of tapentadol, is indicated for the management of moderate-to-severe chronic pain in adults when a continuous, round-the-clock opioid analgesic is required for an extended period of time.
Limitations of Use
NUCYNTA ER is not intended for use as an as-needed analgesic. NUCYNTA ER is not intended for the management of acute or postoperative pain.
NUCYNTA ER tablets are to be swallowed whole. They are not to be broken, chewed, split, dissolved, or crushed. Taking broken, chewed, split, dissolved, or crushed NUCYNTA ER tablets could lead to rapid release and absorption of a potentially fatal dose of tapentadol.
Patients must not consumer alcoholic beverages, or prescription or nonprescription medications that contain alcohol. Combining alcohol with NUCYNTA ER may result in a potentially fatal dose of tapentadol.
Contraindications
• NUCYNTA ER is contraindicated in patients with significant respiratory depression, acute or severe bronchial asthma or hypercapnia in unmonitored settings or in the absence of equipment used to resuscitate patients.
• NUCYNTA ER is contraindicated in any patient who is or is suspected of having a paralytic ileus (obstruction of the intestine due to paralysis of the intestinal muscles).
• NUCYNTA ER is contraindicated in patients receiving monoamine oxidase inhibitors (MAOIs) 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.
• NUCYNTA ER is contraindicated in patients with known hypersensitivity to the active substance, tapentadol, or any component of the product. Angioedema (a swelling, similar to hives, but beneath the skin, most often around the lips and eyes) has been reported in association with use of tapentadol.
Warnings and Precautions
• NUCYNTA ER tablets are to be swallowed whole and are not to be broken, chewed, split, dissolved, or crushed. Taking broken, chewed, split, dissolved, or crushed NUCYNTA ER tablets leads to rapid release and absorption of a potentially fatal dose of tapentadol.
• NUCYNTA ER tablets must be kept in a secure place out of the reach of children. Accidental consumption of the medicine, especially in children, can result in a fatal dose of tapentadol.
• Respiratory depression is the primary risk with mu-opioid agonists. This occurs more frequently in elderly and debilitated patients and those suffering from conditions accompanied by hypoxia, hypercapnia, or upper airway obstruction, in whom even moderate therapeutic doses of NUCYNTA ER may significantly decrease pulmonary ventilation.
• Use NUCYNTA ER with caution in patients with conditions accompanied by hypoxia, hypercapnia, or decreased respiratory reserve, such as: asthma, chronic obstructive pulmonary disease (COPD) or cor pulmonale, severe obesity, sleep apnea syndrome, myxedema, kyphoscoliosis, central nervous system (CNS) depression, or coma. In such patients, even the usual therapeutic doses of the medicine may increase airway resistance and decrease respiratory drive to the point of apnea. Alternative non-mu-opioid agonist analgesics should be considered. NUCYNTA ER should only be employed 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.
• Patients receiving other opioid agonist analgesics, general anesthetics, phenzothiazines, other tranquilizers, hypnotics, sedatives, centrally acting muscle relaxants, or other CNS depressants (including alcohol) concomitantly with NUCYNTA ER 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 ER. When such combined therapy is contemplated, a dose reduction of one or both agents should be considered.
• Opioid analgesics can raise cerebrospinal fluid pressure as a result of respiratory depression with carbon dioxide retention. Therefore, NUCYNTA ER 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 the effects on papillary response and consciousness. Use NUCYNTA ER with caution in patients with head injury, intracranial lesions, or other sources of pre-existing increased intracranial pressure.
• Tapentadol is a mu-opioid agonist and is a Schedule II controlled substance. Such drugs are sought by drug abusers and those with addiction disorders. Diversion of Schedule II products is an act that is subject to criminal penalties.
• Patients should be assessed for their clinical risks for opioid abuse or addiction prior to being prescribed opioids.
• NUCYNTA ER can be abused in a manner similar to other opioid agonists, whether legal or illicit. This should be considered when prescribing or dispensing NUCYNTA ER in situations where the doctor or pharmacist is concerned about an increased risk of misuse and abuse. Concerns about abuse and addiction should not prevent proper management of pain, but all patients treated with mu-opioid agonists require careful monitoring to detect signs of abuse and addiction – since use of mu-opioid agonist analgesic products carries the risk of addiction even under appropriate medical use.
• Drug abusers may attempt to abuse NUCYNTA ER by chewing, snorting, crushing or injecting the medication. Any of these practices may result in the uncontrolled delivery of NUCYNTA ER and pose a significant risk to the abuser that could result in overdose and death.
• NUCYNTA ER may cause severe hypotension. Patients at higher risk of hypotension include those with hypovolemia or those taking concurrent products that compromise vasomotor tone (for example, those taking phenothiazines or general anesthetics).
• Patients taking NUCYNTA ER should be cautioned that it may impair mental and/or physical abilities required for the performance of potentially hazardous tasks such as operating machinery or drive a car. This is to be expected, especially at the beginning of treatment, at any change of dosage, as well as in combination with tranquilizers or alcohol.
• NUCYNTA ER may be expected to have additive effects when used in conjunction with alcohol, other opioids, or illicit drugs that cause CNS depression, because respiratory depression, hypotension, hypertension, and profound sedation, coma, or death may result.
• NUCYNTA ER has not been evaluated in patients with a predisposition to a seizure disorder, and such patients were excluded from clinical studies. As with other opioids, NUCYNTA ER should be prescribed with care in patients with a history of seizure disorder or any condition that would put them at risk of seizures.
• Cases of life-threatening serotonin syndrome have been reported with the concurrent use of tapentadol and serotonergic drugs. Serotonergic drugs compromise selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptans, drugs that affect the serotonergic neurotransmitter system (for example, mirtazapine, tramadol, and trazodone), and drugs that impair metabolism of serotonin (including MAOIs). This may occur within the recommended dose. Serotonin syndrome may include changes in mental status (for example, agitation, hallucinations, coma), autonomic instability (tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (hyperreflexia, incoordination) and/or gastrointestinal symptoms (nausea, diarrhea, vomiting), and can be fatal.
• Withdrawal symptoms may occur if NUCYNTA ER is abruptly discontinued. Symptoms may include: anxiety, diarrhea, insomnia, nausea, pain, piloerection, rigors, sweating, upper respiratory symptoms, and rarely, hallucinations. Withdrawal symptoms may be reduced by tapering off NUCYNTA ER.
• A study with the immediate-release formulation of tapentadol in subjects with hepatic impairment showed higher serum concentrations of tapentadol than in those with normal hepatic function. Tapentadol should be used in caution in patients with moderate hepatic impairment.
• NUCYNTA ER has not been studied in patients with severe hepatic impairment and use in this population is not recommended.
• Like other drugs with mu-opioid agonist activity, NUCYNTA ER may cause spasm of the sphincter of Oddi and should be used with caution in patients with biliary tract disease, including acute pancreatitis.
• NUCYNTA ER should be used with caution in the following conditions: adrenocortical insufficiency (for example, Addison’s disease), delirium tremens (DTs), myxedema or hypothyroidism, prostatic hypertrophy or urethral stricture, and toxic psychosis.
• There are no adequate and well-controlled studies of NUCYNTA ER in pregnant women. Therefore, NUCYNTA ER should be used during pregnancy ONLY of the potential benefit justifies the potential risk to the fetus.
Adverse Reactions
The most common adverse reactions – greater than or equal to 10 percent – were nausea, constipation, headache, dizziness, and somnolence (drowsiness).
--Suzannekane 14:28, 27 August 2011 (MDT)
