Comparative Pharmacology
Head-to-head clinical analysis: PROZAC WEEKLY versus SARAFEM.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PROZAC WEEKLY versus SARAFEM.
PROZAC WEEKLY vs SARAFEM
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective serotonin reuptake inhibitor (SSRI); potentiates serotonergic activity by blocking reuptake of serotonin at the presynaptic neuronal membrane.
SARAFEM (fluoxetine) is a selective serotonin reuptake inhibitor (SSRI). It potentiates serotonergic activity in the CNS by inhibiting the reuptake of serotonin at the presynaptic neuronal membrane, enhancing serotonin effects in the synaptic cleft.
90 mg orally once weekly
10-20 mg orally once daily initially, may increase to 40 mg/day after 3 weeks if needed; maximum 80 mg/day
None Documented
None Documented
Fluoxetine: 4-6 days after single dose, 4-6 days (extended to 7-9 days with chronic dosing due to autoinhibition of CYP2D6); norfluoxetine: 9-31 days. Steady state achieved after 2-4 weeks.
Fluoxetine: 4-6 days after single dose, 4-16 days after chronic dosing; norfluoxetine: 4-16 days after single dose, up to 16-20 days after chronic dosing. The long half-life minimizes withdrawal symptoms and allows for once-weekly dosing.
Renal excretion of metabolites (primarily fluoxetine glucuronide and norfluoxetine glucuronide) accounts for approximately 80% of elimination; fecal excretion accounts for approximately 15%.
Primarily renal excretion of fluoxetine (10%) and its active metabolite norfluoxetine (7.5%) as unchanged drug; the remainder is excreted as conjugates and other metabolites. Approximately 2.5% is excreted in feces.
Category C
Category C
SSRI Antidepressant
SSRI Antidepressant