tapentadol hydrochloride: clinical use

Prescribing considerations

• Agree treatment goals, review continued need and plan eventual discontinuation before starting.
• Assess respiratory risk, concurrent sedatives, seizure history, mental-health history and current or previous substance misuse.
• Use caution with head injury or raised intracranial pressure, biliary or pancreatic disease and sleep-related breathing disorders.
• Avoid abrupt cessation after repeated use because withdrawal may occur.
• Tapentadol can impair cognition and driving; counsel patients not to drive when impaired.

Contraindications and cautions

• Hypersensitivity to tapentadol or formulation excipients.
• Significant respiratory depression in an unmonitored setting or without resuscitation facilities.
• Acute or severe bronchial asthma or hypercapnia where mu-opioid agonists are contraindicated.
• Known or suspected paralytic ileus.
• Acute intoxication with alcohol, hypnotics, centrally acting analgesics or psychotropic substances.

Monitoring

• Analgesic benefit, function and ongoing clinical need.
• Sedation, respiratory depression and sleep-related breathing symptoms.
• Constipation and other gastrointestinal adverse effects.
• Tolerance, dependence, opioid use disorder, early refill requests and withdrawal symptoms.
• Seizures and features of serotonin syndrome, especially with interacting psychotropic medicines.
• Renal and hepatic status where impairment is present or suspected.

Clinical pharmacology

Tapentadol combines mu-opioid receptor agonism with noradrenaline reuptake inhibition. It is directly active, undergoes predominantly glucuronide conjugation and has limited involvement of major CYP enzymes.

Formulation and product differences

• Immediate-release film-coated tablets are licensed for acute pain in adults.
• Oral solution is licensed for acute pain in adults and eligible paediatric patients; paediatric treatment is restricted to hospital use with respiratory-support facilities. It may be diluted in a non-alcoholic drink and is measured with the supplied device.
• Prolonged-release tablets are licensed for severe chronic pain in adults and eligible paediatric patients. They must remain whole to preserve controlled release.
• Selected formulations differ in excipients, including lactose in tablets and propylene glycol and sodium benzoate in oral solution.

Modified-release tablet

Route: Oral

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