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Drugs reference index «Tapentadol»



Pronunciation: ta-PEN-ta-dolClass: Opioid analgesic

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.

Special Populations

Renal Function Impairment

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.


C max is 16% lower than in younger subjects.

Indications and Usage

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.

Dosage and Administration


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.

General Advice

  • Individualize according to severity of pain, previous experience with similar drugs, and the ability to monitor the patient.
  • May be given with or without food.


Store at 59° to 86°F. Protect from moisture.

Drug Interactions

CNS depressants (eg, alcohol, anesthetics, narcotics, phenothiazines, sedative-hypnotics, tranquilizers)

Risk of CNS and respiratory depression may be increased.


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.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Dizziness (24%); somnolence (15%); fatigue (3%); insomnia (2%); abnormal dreams, anxiety, confusional state, lethargy, tremor (1%).


Hyperhidrosis, pruritus (3%); rash (1%).


Nasopharyngitis (1%).


Nausea (30%); vomiting (18%); constipation (8%); dry mouth (4%); dyspepsia (2%).


UTI (1%).


Decreased appetite (2%).


Arthralgia (1%).


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.

Renal Function

Not recommended in patients with severe renal function impairment.

Hepatic Function

Use with caution in patients with moderate hepatic impairment; dosage adjustments required. Not recommended in patients with severe hepatic impairment.

Special Risk Patients

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.

Hazardous Tasks

May impair judgment, thinking, or motor skills.

Drug abuse

Tapentadol is a controlled substance and may cause addiction. Use with caution in opioid-dependent patients.

Head trauma

Do not use in patients with increased intracranial pressure or head trauma; use with caution in patients with intracranial lesions.

Pancreatic/Biliary tract disease

May cause spasm of the sphincter of Oddi; use with caution in patients with biliary tract disease, including acute pancreatitis.

Serotonin syndrome

Potentially life-threatening serotonin syndrome may develop, particularly when combined with serotinergic agents (eg, SNRIs, SSRIs, triptans).

Respiratory depression

May occur.


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.

Patient Information

  • Instruct patient to take the prescribed dose at the recommended intervals.
  • Instruct patient to report any serious adverse reactions to health care provider.
  • Advise patient not to change the dose of tapentadol without consulting their health care provider.
  • Advise patient to avoid using alcohol or other CNS depressants (eg, sleeping pills).
  • Advise patient that this medication may cause drowsiness and to use caution while driving or using heavy equipment, or performing other tasks requiring mental alertness.
  • Advise patient not to abruptly discontinue this medication; when discontinuing treatment, the drug will be slowly stopped.
  • Advise patient to notify health care provider if pain is not relieved by the medication at prescribed dosage.

Copyright © 2009 Wolters Kluwer Health.

  • Tapentadol MedFacts Consumer Leaflet (Wolters Kluwer)
  • tapentadol Advanced Consumer (Micromedex) - Includes Dosage Information
  • Nucynta Prescribing Information (FDA)
  • Nucynta Consumer Overview

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