Tapenta75 mg

Tapenta is an opioid analgesic indicated for the relief of pain, with evidence-based use classified as follows:

Established/FDA-Approved Uses

• Acute pain (immediate-release formulation): Management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate, in adults and in pediatric patients 6 years of age and older weighing at least 40 kg.
• Chronic pain (extended-release formulation): Management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatments are inadequate, in adults.
• Neuropathic pain associated with diabetic peripheral neuropathy (extended-release formulation): Management of moderate to severe chronic neuropathic pain associated with diabetic peripheral neuropathy in adults, when a continuous, around-the-clock opioid analgesic is needed for an extended period.

Important Note

Tapenta is reserved for pain severe enough to require opioid treatment and for which alternative, non-opioid treatment options are inadequate or not tolerated; it is not intended for use on an as-needed basis for mild pain.

Each tablet contains Tapentadol Hydrochloride equivalent to 50 mg, 75 mg, or 100 mg of tapentadol base in immediate-release form, or 50 mg to 250 mg of tapentadol base in extended-release form, depending on product strength and manufacturer, along with standard pharmaceutical excipients.

Tapenta is a centrally-acting synthetic opioid analgesic with a dual mechanism of action: it is a mu-opioid receptor agonist and also inhibits norepinephrine reuptake in the central nervous system. This combined mechanism allows Tapenta to provide effective analgesia for moderate to severe pain, often at lower opioid-receptor activity than conventional pure opioid agonists.

Tapenta is available as immediate-release tablets for acute pain and extended-release tablets for chronic, around-the-clock pain management, including neuropathic pain associated with diabetic peripheral neuropathy.

As with all opioid analgesics, Tapenta carries a serious risk of addiction, abuse, misuse, and life-threatening respiratory depression, and should be used only under close medical supervision.

Opioid analgesic (centrally-acting synthetic analgesic); combined mu-opioid receptor agonist and norepinephrine reuptake inhibitor.

Tapentadol Hydrochloride exerts its analgesic effect through two complementary mechanisms: agonism at the mu-opioid receptor and inhibition of norepinephrine reuptake in descending inhibitory pain pathways of the central nervous system. This dual action contributes to pain relief while potentially allowing a lower degree of pure opioid-receptor binding compared with conventional opioids.

Pharmacokinetics

• Absorption: Absolute oral bioavailability is approximately 32% due to extensive first-pass metabolism; peak plasma concentrations occur about 1.25 hours (immediate-release) after dosing.
• Metabolism: Predominantly hepatic, chiefly via glucuronidation, with minor contribution from CYP2C9 and CYP2C19 pathways.
• Elimination: Mainly renal, as inactive metabolites; elimination half-life is approximately 4 hours.

Tapenta tablets should be taken orally, with or without food, exactly as prescribed. Extended-release tablets must be swallowed whole, one at a time, with enough water to ensure complete swallowing, and must not be crushed, chewed, dissolved, or split, as doing so can cause rapid release and absorption of a potentially fatal dose.

Tapenta has several clinically significant drug interactions:

• Monoamine oxidase inhibitors (MAOIs): Contraindicated with concurrent use or within 14 days of MAOI discontinuation, due to risk of serotonin syndrome and unpredictable, severe potentiation of opioid effects.
• Other CNS depressants (benzodiazepines, sedatives, alcohol, other opioids): Concomitant use increases the risk of profound sedation, respiratory depression, coma, and death; combined use should be reserved for situations where alternatives are inadequate, using the lowest effective doses.
• Serotonergic drugs (SSRIs, SNRIs, tricyclic antidepressants, triptans, tramadol): Increased risk of serotonin syndrome; see Precautions and Warnings.
• Mixed opioid agonist/antagonists (e.g., butorphanol, nalbuphine, pentazocine) or partial agonists (buprenorphine): May reduce analgesic effect and/or precipitate withdrawal symptoms; avoid concurrent use.
• Muscle relaxants: May potentiate CNS and respiratory depressant effects; dose reduction of either agent may be needed.

The most common adverse effects of Tapenta (occurring in 10% or more of adult patients) are:

• Nausea
• Dizziness
• Vomiting
• Somnolence (drowsiness)

Other commonly reported effects include constipation, headache, pruritus (itching), dry mouth, and fatigue. In pediatric patients, vomiting, constipation, nausea, pruritus, and fever have been reported.

Serious but less common effects include respiratory depression, serotonin syndrome, seizures, severe hypotension, and adrenal insufficiency; see Precautions and Warnings for details.

Pregnancy: Data on Tapenta use in pregnant women are limited. Prolonged use of opioid analgesics, including Tapenta, during pregnancy can cause neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated. Tapenta should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, and only under close medical supervision; consult a physician before use.

Lactation: There is no adequate data on the presence of tapentadol in human milk. Because of the potential for serious adverse reactions, including excess sedation and respiratory depression, in a breastfed infant, breastfeeding is generally not recommended during treatment with Tapenta unless a physician determines the benefit outweighs the risk; infants should be monitored closely if exposure occurs.

Boxed Warning

• Addiction, abuse, and misuse: Tapenta exposes patients to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Assess each patient's risk before prescribing and monitor regularly.
• Life-threatening respiratory depression: Risk is greatest during initiation of therapy or following dose increases; monitor closely, especially in the first 24-72 hours.
• Accidental ingestion: Accidental ingestion of even one dose, especially by children, can result in fatal overdose.
• Concomitant use with benzodiazepines or other CNS depressants: May result in profound sedation, respiratory depression, coma, and death.
• Neonatal opioid withdrawal syndrome: Prolonged use during pregnancy can result in withdrawal in the newborn; see Pregnancy and Lactation.

Serotonin Syndrome

Concomitant use of Tapenta with serotonergic drugs (SSRIs, SNRIs, MAOIs, triptans, tricyclic antidepressants) may result in serotonin syndrome, a potentially life-threatening condition. Symptoms include agitation, hallucinations, tachycardia, fever, tremor, and gastrointestinal symptoms. Discontinue immediately if suspected.

Seizures

Tapenta may increase the frequency of seizures in patients with seizure disorders, and may increase seizure risk in other clinical settings associated with seizures. Monitor patients with a history of seizure disorder.

Dependence and Withdrawal

Tolerance and physical dependence may develop with repeated use of Tapenta. Do not discontinue abruptly after prolonged use; taper the dose gradually under medical supervision to reduce the risk of withdrawal symptoms.

Other Precautions

• Avoid alcohol while taking Tapenta, as it increases the risk of dangerous, potentially fatal side effects.
• May impair mental and physical abilities; caution when driving or operating machinery until effects are known.
• Use with caution in elderly, cachectic, or debilitated patients, and in those with head injury, increased intracranial pressure, or biliary tract disease.
• Tapenta is a controlled substance with potential for diversion; store securely and out of reach of children and others.

Overdose of Tapenta may present with respiratory depression, extreme somnolence progressing to stupor or coma, muscle flaccidity, cold and clammy skin, constricted (pinpoint) pupils, bradycardia, hypotension, and in severe cases, circulatory collapse or death.

Overdose is a medical emergency. Seek immediate medical attention or contact emergency services or a poison control center. Do not attempt to manage a suspected overdose at home. Treatment involves securing the airway, providing ventilatory support, and administration of an opioid antagonist (e.g., naloxone) by trained medical personnel; patients should be monitored closely, as the duration of antagonist effect may be shorter than that of Tapenta.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children and store securely, as Tapenta is a controlled substance with potential for misuse or diversion.

• Elderly: No overall differences in safety or efficacy compared with younger patients have been established, but greater sensitivity to opioid effects cannot be ruled out; use the lowest effective dose with close monitoring.
• Hepatic impairment: Dose adjustment required for moderate impairment (immediate-release); not recommended in severe hepatic impairment or for extended-release use in any hepatic impairment.
• Renal impairment: Not recommended in severe renal impairment; use with caution and close monitoring in mild to moderate impairment.
• Pediatric patients: Immediate-release Tapenta is approved for acute pain in patients 6 years and older weighing at least 40 kg; safety and effectiveness of extended-release formulations have not been established in pediatric patients. See Pediatric Uses.
• Pregnancy and lactation: See Pregnancy and Lactation section.

Tapenta should be used at the lowest effective dose for the shortest duration consistent with treatment goals for acute pain. For chronic pain, the ongoing need for opioid therapy should be reassessed periodically by the prescribing physician, and treatment should not be continued longer than medically necessary.

Opioid Analgesics; Centrally Acting Synthetic Analgesics; Mu-Opioid Receptor Agonists.

Tapentadol Hydrochloride acts via a dual mechanism: agonism at the mu-opioid receptor combined with inhibition of norepinephrine reuptake, which together produce analgesia for moderate to severe pain.

Immediate-release Tapenta is approved for the management of acute pain in pediatric patients 6 years of age and older weighing at least 40 kg, using weight-based dosing (see Dosage and Administration); it has not been studied in pediatric patients with hepatic or renal impairment, and use in these populations is not recommended. Safety and effectiveness of extended-release Tapenta have not been established in patients younger than 18 years, and it should not be used in this population.