tramadol hydrochloride: clinical use

Prescribing considerations

• Agree treatment goals and a discontinuation plan before initiating therapy; reassess whether meaningful analgesic and functional benefit continues.
• Consider vulnerability to sedation, respiratory depression, falls, constipation, misuse, dependence, tolerance, withdrawal and opioid-induced hyperalgesia.
• Renal or hepatic impairment and advanced age can delay elimination; follow the relevant product information.
• Use particular caution with impaired respiratory function, head injury, raised intracranial pressure, shock, opioid sensitivity or medicines that depress the central nervous system.
• CYP2D6 poor metabolisers may have reduced analgesia, while ultra-rapid metabolism can increase opioid toxicity.

Contraindications and cautions

• Hypersensitivity to tramadol or product excipients.
• Acute intoxication with alcohol, hypnotics, opioid analgesics or other psychotropic medicines.
• Current monoamine oxidase inhibitor treatment or use within the preceding 14 days.
• Epilepsy not adequately controlled by treatment.
• Use as a substitute treatment for opioid withdrawal.

Monitoring

• Pain relief, function and continued need for treatment.
• Sedation, respiratory rate and signs of opioid toxicity, especially after treatment changes or addition of interacting medicines.
• Constipation, nausea, dizziness, falls risk and urinary retention.
• Dependence, misuse, escalating use, withdrawal, tolerance or hyperalgesia.
• Seizures or serotonin syndrome where relevant risk factors or interacting medicines are present.
• Renal and hepatic function when impairment could affect clearance.

Clinical pharmacology

Tramadol is a centrally acting analgesic with weak mu-opioid receptor agonism and monoamine reuptake inhibition. CYP2D6 forms the active O-desmethyltramadol metabolite; CYP3A4 and renal elimination also influence exposure.

Formulation and product differences

• Standard hard capsules provide immediate-release oral tramadol and are swallowed whole.
• Zamadol Melt is an orodispersible tablet containing aspartame and can dissolve on the tongue.
• Prolonged-release tablets and capsules release tramadol gradually and must not be crushed or chewed.
• The solution for injection or infusion is for professional administration by intramuscular injection, slow intravenous injection or infusion; compatibility requirements must be checked before mixing.

Capsule

Route: Oral

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

Modified-release capsule

Route: Oral

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