tapentadol maleate hemihydrate: clinical use

Prescribing considerations

• Confirm that severe chronic pain requires opioid therapy and establish treatment goals and review arrangements.
• Assess respiratory function, hepatic and renal impairment, seizure risk, head injury, biliary or pancreatic disease, mental health, substance-use history and concomitant sedatives.
• Discuss impairment, safe storage, overdose, tolerance, dependence, opioid use disorder and withdrawal before prescribing.
• Avoid abrupt discontinuation after ongoing use.
• The selected product is not recommended for children or adolescents and should not be used for acute postoperative pain.

Contraindications and cautions

• Hypersensitivity to tapentadol or an excipient.
• Significant respiratory depression in an unmonitored setting or without resuscitative equipment.
• Acute or severe bronchial asthma or hypercapnia.
• Known or suspected paralytic ileus.
• Acute intoxication with alcohol, hypnotics, centrally acting analgesics or psychotropic substances.
• Rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption because the tablets contain lactose.

Monitoring

• Pain control, function and ongoing clinical need.
• Sedation, respiratory depression and sleep-related breathing disorders.
• Constipation and other gastrointestinal adverse effects.
• Signs of tolerance, misuse, dependence, opioid use disorder or withdrawal.
• Neurological toxicity, including seizures or serotonin syndrome when interacting medicines are used.
• Clinical tolerability in hepatic or renal impairment and in older or frail people.

Clinical pharmacology

Tapentadol combines mu-opioid receptor agonism with noradrenaline reuptake inhibition. It has no pharmacologically active metabolite, is mainly metabolised by glucuronidation through UGT enzymes, has comparatively limited CYP metabolism and is eliminated predominantly in urine as metabolites.

Formulation and product differences

• The selected product is a film-coated prolonged-release matrix tablet intended to be swallowed intact.
• Dividing, chewing or crushing can disrupt prolonged release and cause rapid exposure.
• It contains lactose monohydrate.
• The insoluble matrix may be visible in stool after the active substance has been absorbed.

Modified-release tablet

Route: Oral

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