Trade Names:Nucynta- Tablets 50 mg- Tablets 75 mg- Tablets 100 mg
Binds to certain opioid receptors and inhibits reuptake of norepinephrine; exact mechanism of action unknown.
Mean absolute bioavailability is 32%. High-fat meals increased C max and AUC 16% and 25%, respectively. T max is 1.25 h.
Vd is approximately 540 L. Protein binding is approximately 20%.
Tapentadol is mainly metabolized by conjugation with glucuronic acid to produce glucuronides. Tapentadol is also metabolized to a lesser extent by CYP2C9 (13%) and CYP2C19 (2%). None of the metabolites contribute to its pharmacologic activity.
99% of a dose is excreted in urine; 3% is unchanged drug. The half-life is 4 h. Total Cl is 1,530 mL/min.
In patients with renal function impairment, there is an increase in exposure (AUC) of the metabolite tapentadol-0-glucuronide. Tapentadol has not been studied and is not recommended in patients with severe renal impairment.Hepatic Function Impairment
Metabolism of tapentadol is reduced in patients with hepatic impairment. In patients with moderate hepatic impairment, dose adjustment is recommended. Tapentadol has not been studied and is not recommended in patients with severe impairment.Elderly
C max is 16% lower than in younger subjects.
Relief of moderate to severe acute pain.
Significant respiratory depression in unmonitored settings or in the absence of resuscitative equipment; acute or severe bronchial asthma or hypercapnia in unmonitored settings or in the absence of resuscitative equipment; paralytic ileus; concomitant use with MAOIs or within the last 14 days.
PO 50, 75, or 100 mg every 4 to 6 h, depending on pain intensity. On first day of dosing, the second dose may be given as soon as 1 h after the first dose, if adequate pain relief is not achieved. Max dose is 700 mg on day 1, and 600 mg on subsequent days.Hepatic Function Impairment
PO For patients with moderate hepatic impairment, initiate at 50 mg, not more frequently than every 8 h (max, 3 doses in 24 h). Adjust subsequent doses by shortening or lengthening the dosing interval to maintain adequate analgesia and acceptable tolerability. Not recommended for use in patients with severe hepatic impairment.
Store at 59° to 86°F. Protect from moisture.
Risk of CNS and respiratory depression may be increased.MAOIs
Concomitant use or use within 14 days of each other is contraindicated.Serotonergics (eg, SNRIs, SSRIs, tricyclic antidepressants, triptans)
Serotonin syndrome (eg, agitation, coma, hallucinations, hyperreflexia, hyperthermia, tachycardia) may occur with coadministration.
None well documented.
Dizziness (24%); somnolence (15%); fatigue (3%); insomnia (2%); abnormal dreams, anxiety, confusional state, lethargy, tremor (1%).
Hyperhidrosis, pruritus (3%); rash (1%).
Nausea (30%); vomiting (18%); constipation (8%); dry mouth (4%); dyspepsia (2%).
Decreased appetite (2%).
Upper respiratory tract infection (1%).
Feeling hot, hot flush (1%).
Monitor patients for breakthrough pain and adverse effects of tapentadol.
Category C .
Safety and efficacy not established in children younger than 18 yr of age.
Consider starting at the low end of the dosage range because of the greater frequency of hepatic or renal impairment.
Not recommended in patients with severe renal function impairment.
Use with caution in patients with moderate hepatic impairment; dosage adjustments required. Not recommended in patients with severe hepatic impairment.
Use with caution in patients with conditions accompanied by hypoxic, hypercapnia, or decreased respiratory reserve such as asthma, COPD, cor pulmonae, obesity, sleep apnea, myxedema, kyphoscoliosis, CNS depression, or coma.
May impair judgment, thinking, or motor skills.
Tapentadol is a controlled substance and may cause addiction. Use with caution in opioid-dependent patients.
Do not use in patients with increased intracranial pressure or head trauma; use with caution in patients with intracranial lesions.
May cause spasm of the sphincter of Oddi; use with caution in patients with biliary tract disease, including acute pancreatitis.
Potentially life-threatening serotonin syndrome may develop, particularly when combined with serotinergic agents (eg, SNRIs, SSRIs, triptans).
Use with caution in patients with a history of a seizure disorder or any condition that would put the patient at risk of seizures.
If tapentadol is discontinued abruptly, withdrawal symptoms may occur.
Coma, convulsions, CV collapse, miosis, respiratory arrest, respiratory depression, vomiting.
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