Tramadol how is it metabolized




















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The data presented were ancillary data generated with support of a previous project from the Department of Defense DoD to Parabon Computation, Inc. The opinions and findings presented here are those of the authors and do not necessarily reflect those of the DoD, Parabon Computation, Inc. Frank R. Tramadol and its metabolites are mainly excreted via the kidneys. The mean elimination half-life is about 6 hours. The wide variability in the pharmacokinetic properties of tramadol can partly be ascribed to CYP polymorphism.

O- and N-demethylation of tramadol as well as renal elimination are stereoselective. Pharmacokinetic-pharmacodynamic characterisation of tramadol is difficult because of differences between tramadol concentrations in plasma and at the site of action, and because of pharmacodynamic interactions between the two enantiomers of tramadol and its active metabolites.

Tramadol provides postoperative pain relief comparable with that of pethidine, and the analgesic efficacy of tramadol can further be improved by combination with a non-opioid analgesic. Tramadol may prove particularly useful in patients with a risk of poor cardiopulmonary function, after surgery of the thorax or upper abdomen and when non-opioid analgesics are contraindicated.

Tramadol is an effective and well tolerated agent to reduce pain resulting from trauma, renal or biliary colic and labour, and also for the management of chronic pain of malignant or nonmalignant origin, particularly neuropathic pain.

Tramadol appears to produce less constipation and dependence than equianalgesic doses of strong opioids.



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