desvenlafaxine
Boxed Warning
Suicidality risk in children, adolescents, and young adults under 25 during initial treatment.
Desvenlafaxine is the active metabolite of venlafaxine, formulated as an extended-release SNRI for major depressive disorder. It was designed to provide more predictable pharmacokinetics by bypassing CYP2D6 metabolism.
25mg, 50mg, 100mg
Extended-release tablets: 25mg, 50mg, 100mg
Category C (risk cannot be ruled out)
Serotonin-norepinephrine reuptake inhibitor (SNRI). Inhibits both the serotonin and norepinephrine transporters. Unlike its parent compound venlafaxine, it does not require CYP2D6 activation.
Extended-release tablets cannot be split. Compounding pharmacy needed for doses between available strengths.
Tablets cannot be crushed/split. Compounding pharmacy essential for fine reductions.
Toxicity
Serotonin syndrome with serotonergic combinations. Sustained hypertension. Lipid elevations reported. Severe discontinuation syndrome similar to venlafaxine.
Pharmacokinetics
Bioavailability ~80%. Tmax ~7.5 hours. Food does not significantly affect pharmacokinetics.
~3.4 L/kg
Hepatic conjugation (UGT) and to a minor extent CYP3A4-mediated oxidation. Does not rely on CYP2D6 for activation.
Renal (~45% unchanged, ~24% as glucuronide conjugate). Total urinary recovery ~~70%.
~30%
~215 mL/min (total body clearance)
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