tapentadol tartrate: clinical use

Prescribing considerations

• Assess risks of respiratory depression, sedation, falls, tolerance, dependence, opioid use disorder and diversion.
• Review concurrent opioids, sedatives, gabapentinoids, serotonergic medicines and medicines that lower seizure threshold.
• Use caution in respiratory impairment, head injury, seizure disorders, biliary tract disease and moderate hepatic impairment.
• Not recommended in severe renal or severe hepatic impairment, or in children with renal or hepatic impairment.

Contraindications and cautions

• Hypersensitivity to tapentadol or an excipient.
• Significant respiratory depression without appropriate monitoring or resuscitation facilities.
• Acute or severe bronchial asthma or hypercapnia.
• Known or suspected paralytic ileus.
• Acute intoxication with alcohol, hypnotics, centrally acting analgesics or psychotropic substances.

Monitoring

• Pain relief, function, adverse effects and ongoing need for opioid treatment.
• Sedation and respiratory status, especially with other central nervous system depressants.
• Constipation and other gastrointestinal effects.
• Signs of tolerance, withdrawal, opioid use disorder or misuse.
• New seizures or features of serotonin syndrome.

Clinical pharmacology

Tapentadol combines mu-opioid receptor agonism with noradrenaline reuptake inhibition. It is extensively metabolised, mainly by glucuronidation; its metabolites are not analgesically active and elimination is predominantly through the kidneys.

Formulation and product differences

• The selected product is a prolonged-release matrix tablet.
• It must remain intact; dividing, chewing or crushing can cause rapid, potentially fatal exposure.
• The insoluble matrix shell may be visible in stool after absorption.

Modified-release tablet

Route: Oral

Strengths: 25 mg, 50 mg, 100 mg, 150 mg, 200 mg, 250 mg