Each week we will aim to bring out a concise email that provides 4-5 key pieces of information addressing a specific issue in clinical therapeutics.
This week: Focus on tapentadol
Tapentadol is a centrally acting synthetic opioid which exerts its analgesic effect by binding to the mu opioid receptor and also inhibiting noradrenaline reuptake. It is currently approved by the Therapeutic Goods Administration in Australia for treatment of moderate-to-severe chronic pain unresponsive to non-opioid analgesics.
- Maximum serum concentrations from the immediate-release formulation are achieved about 1.25 hours after administration, but for sustained-release formulations peak levels are seen approximately 3 to 6 hours after administration. The sustained-release formulation (Palexia®) is recommended for twice daily administration. Sustained-release formulations currently available include oral dose forms of 50 mg, 100 mg, 150 mg, 200 mg and 250 mg.
- The most common adverse effects of tapentadol include nausea, vomiting, dizziness, constipation, somnolence and pruritus. Most of these effects are dose related.
- Medications which result in respiratory depression (e.g. general anaesthetics, alcohol, sedatives, hypnotics) may cause an additive effect if used concomitantly with tapentadol: reduction of the dose of one or both of the agents should be considered. As tapentadol increases noradrenaline reuptake; patients who are also currently receiving monoamine oxidase inhibitors (MAOIs) or those who received MAOIs within the last 14 days should be treated with caution.
Please consider these issues when preparing or interpreting RMMR reports or education sessions. Contributions of content or suggested topics are welcome and should be sent directly to firstname.lastname@example.org.