Home Drug Guide Tapentadol Hydrochloride

Drug Guide

Generic Name

Tapentadol Hydrochloride

Brand Names Nucynta, Nucynta ER

Classification

Therapeutic: Pain reliever (Analgesic)

Pharmacological: Mu-opioid receptor agonist and norepinephrine reuptake inhibitor

FDA Approved Indications

Moderate to severe acute pain in adults
Chronic pain (for Nucynta ER) in adults

Mechanism of Action

Tapentadol acts centrally as a mu-opioid receptor agonist and inhibits norepinephrine reuptake, leading to analgesia through dual mechanisms.

Dosage and Administration

Adult: Immediate-release: Usually 50-100 mg every 4-6 hours as needed, not exceeding 700 mg/day. Extended-release: Typically 100-250 mg twice daily; dosage titration based on response and tolerability.

Pediatric: Not approved for pediatric use.

Geriatric: Start at lower end of dosage range; monitor for increased sensitivity.

Renal Impairment: Adjust dose; avoid in severe impairment.

Hepatic Impairment: Adjust dose; use with caution in moderate to severe impairment.

Pharmacokinetics

Absorption: Rapidly absorbed; peak plasma concentrations in approximately 1 hour for immediate-release.

Distribution: Widely distributed; volume of distribution approximately 113 L.

Metabolism: Primarily via conjugation (glucuronidation) and some oxidative metabolism.

Excretion: Excreted mainly in urine as metabolites; some in feces.

Half Life: Approximately 4 hours for immediate-release; extended formulation varies.

Contraindications

Known hypersensitivity to tapentadol or components

Precautions

History of respiratory depression, head trauma, increased intracranial pressure, conscious sedation, impaired respiratory function, substance abuse history, or in patients using MAO inhibitors within 14 days. Use cautiously in elderly, renal or hepatic impairment.

Adverse Reactions - Common

Nausea (Frequent)
Dizziness (Frequent)
Somnolence (Frequent)
Constipation (Frequent)

Adverse Reactions - Serious

Respiratory depression (Rare)
Seizures (Rare)
Serotonin syndrome (when combined with serotonergic drugs) (Rare)
Severe allergic reactions (Rare)

Drug-Drug Interactions

Other CNS depressants, including benzodiazepines and alcohol; serotonergic drugs like SSRIs, SNRIs, triptans; MAO inhibitors.

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor pain relief efficacy, respiratory status, level of sedation, bowel function.

Diagnoses:

Risk for respiratory depression
Ineffective airway clearance
Risk for constipation

Implementation: Administer with food or milk if GI upset occurs. Monitor for signs of CNS depression.

Evaluation: Assess pain relief, respiratory function, and side effects periodically.

Patient/Family Teaching

Take exactly as prescribed; do not increase dose.
Warn about potential for drowsiness and impaired ability to operate machinery.
Avoid alcohol and sedatives.
Report signs of respiratory depression, dizziness, or allergic reactions.
Follow disposal instructions for unused medication.

Special Considerations

Black Box Warnings:

Risk of respiratory depression, addiction, abuse, and misuse.
Potential for serotonin syndrome when combined with serotonergic drugs.

Genetic Factors: Pharmacokinetics may be influenced by CYP2C9 and CYP2C19 polymorphisms.

Lab Test Interference: May cause increase in serum amylase and lipase; monitor renal and hepatic function during long-term use.

Overdose Management

Signs/Symptoms: Respiratory depression, somnolence, miosis, cyanosis, hypotension, seizures.

Treatment: Support airway and breathing, administer naloxone for opioid overdose, provide cardiovascular support as needed.

Storage and Handling

Storage: Store at room temperature, 20-25°C, protected from moisture, heat, and light.

Stability: Stable under recommended storage conditions.