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Pharmacodynamics: Tramadol hydrochloride is a synthetic, centrally active analgesic. The drug (and its active M1 metabolite) acts as an opiate agonist, apparently by selective activity at the μ-receptor. In addition to its opiate agonist activity, tramadol hydrochloride inhibits reuptake of certain monoamines (norepinephrine, serotonin), which appears to contributes to the drug's analgesic effect.
Pharmacokinetics: Absorption: The duration of effects of tramadol hydrochloride and its active metabolite, O-desmethyltramadol (M1), is 2 and 3 hours respectively.
Distribution: Tramadol hydrochloride is 20% bound to plasma proteins. Its volume of distribution is 2.6 - 2.9 L/kg.
Metabolism: Tramadol hydrochloride is metabolized in liver via CYP2D6 and CYP3A4. It is metabolized in the liver to O-desmethyltramadol (M1) as an active metabolite via CYP2D6.
Elimination: Tramadol hydrochloride is eliminated as parent drug and metabolites through the urines in 6.3 and 7.4 hours respectively.
