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Pharmacology: Pharmacodynamics: Desvenlafaxine succinate is a selective serotonin and norepinephrine reuptake inhibitor (SNRI) that potentiates these neurotransmitters in the CNS. Desvenlafaxine is the major active metabolite of venlafaxine, which is also used to treat major depressive disorders.
Pharmacokinetics: Absorption: The absolute oral bioavailability of Desvenlafaxine is approximately 80%. Food has no clinically significant effect. The mean time to peak plasma concentrations of Desvenlafaxine after oral administration of extended-release tablets was approximately 7.5 hours.
Distribution: The protein binding of Desvenlafaxine is low (30%) and is not dependent on drug concentration. Volume of distribution is 3.4 L/kg.
Metabolism: Desvenlafaxine is principally metabolized via conjugation by uridine disphosphoglucuronosyl-transferase (UGT) isoenzymes and, to a lesser extent through oxidation (by the cytochrome P-450 [CYP] 3A4 isoenzyme). The drug minimally inhibits CYP2D6 isoenzyme and does not inhibit the CYP1A2, 2A6, 2C8, 2C9, or 2C19 isoenzymes. Desvenlafaxine is not an inhibitor of CYP3A4. Nor is it an inducer of CYP3A4.
Excretion: The mean terminal half-life of Desvenlafaxine is approximately 11 hours. Approximately 45% of a single oral dose of Desvenlafaxine is eliminated unchanged in the urine at 72 hours, approximately 19% of the dose is excreted as the glucuronide metabolite, and less than 5% is excreted as the oxidative metabolite (N,O-didesmethylvenlafaxine).
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