Home Drug Guide Tapentadol

Drug Guide

Generic Name

Tapentadol

Brand Names Nucynta

Classification

Therapeutic: Analgesic

Pharmacological: μ-Opioid receptor agonist and norepinephrine reuptake inhibitor

FDA Approved Indications

Moderate to severe acute pain
Moderate to severe chronic pain in adult patients

Mechanism of Action

Tapentadol relieves pain by activating μ-opioid receptors and inhibiting norepinephrine reuptake, leading to decreased pain transmission in the central nervous system.

Dosage and Administration

Adult: Typically 50-100 mg every 4-6 hours as needed. Maximum dose usually 600 mg/day.

Pediatric: Not approved for pediatric use.

Geriatric: Start with lower doses due to increased sensitivity and risk of respiratory depression.

Renal Impairment: Adjust dose for severe impairment; consult specific guidelines.

Hepatic Impairment: Use cautiously; dose reduction may be necessary.

Pharmacokinetics

Absorption: Rapid absorption; bioavailability approximately 32%.

Distribution: Widely distributed, crosses the blood-brain barrier.

Metabolism: Metabolized primarily in the liver via conjugation and CYP2C19 and CYP2C9 pathways.

Excretion: Excreted mainly in urine; small amount in feces.

Half Life: Approximately 4 hours.

Contraindications

Known hypersensitivity to tapentadol or its components.
Acute or severe bronchial asthma in an unmonitored setting.
Use with monoamine oxidase inhibitors (MAOIs).

Precautions

Risk of respiratory depression, CNS depression, dependence.
Use cautiously in elderly, hepatic or renal impairment, and in patients with history of substance abuse.
Pregnancy category C; risk cannot be ruled out. Use only if benefits outweigh risks.

Adverse Reactions - Common

Nausea (Frequent)
Dizziness (Frequent)
Somnolence (Frequent)
Headache (Frequent)

Adverse Reactions - Serious

Respiratory depression (Uncommon but severe)
Seizures (Rare)
Serotonin syndrome (if combined with serotonergic agents) (Rare)

Drug-Drug Interactions

Central nervous system depressants (e.g., benzodiazepines, alcohol)
Serotonergic drugs (e.g., SSRIs, SNRIs)

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor pain relief effectiveness, respiratory status, blood pressure, and signs of dependency.

Diagnoses:

Risk of respiratory depression
Impaired comfort

Implementation: Administer with food or milk to reduce GI upset; monitor for adverse reactions.

Evaluation: Assess pain relief and side effects regularly; adjust dose accordingly.

Patient/Family Teaching

Do not operate heavy machinery or drive until effects are known.
Take medication exactly as prescribed.
Avoid alcohol and other CNS depressants.
Report any signs of respiratory depression, adverse reactions, or dependency.

Special Considerations

Black Box Warnings:

Risk of addiction, abuse, and misuse leading to overdose and death.
Respiratory depression risk in opioid-naive patients and overdose.
Accidental ingestion can be fatal, especially in children.

Genetic Factors: Polymorphisms in CYP2C19 and CYP2C9 may affect metabolism.

Lab Test Interference: None noted.

Overdose Management

Signs/Symptoms: Respiratory depression, sedation, coma, miosis.

Treatment: Administer naloxone, support respiratory function, provide airway management, continuous monitoring.

Storage and Handling

Storage: Store at room temperature, away from moisture, heat, and light.

Stability: Stable under recommended conditions for the shelf life specified by manufacturer.