Fluoxetine: Sold as Prozac, Sarafem, Fontex etc.
Image Courtesy: "Depressants ." Human Diseases & Conditions. N.p., 2011. Web. 16 Feb. 2011.
This is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class
Fluoxetine is approved for the treatment of
Major depression (including pediatric depression),
Obsessive-compulsive disorder (in both adult and pediatric populations),
Bulimia nervosa,
Panic disorder and
Premenstrual dysphoric disorder.
Fluoxetine's mechanism of action is primarily that of an SSRI.
SSRIs are believed to increase the extracellular level of the neurotransmitter serotonin by inhibiting its reuptake into the presynaptic cell, increasing the level of serotonin in the synaptic cleft available to bind to the postsynaptic receptor.
The bioavailability of fluoxetine is relatively high (72%), and peak plasma concentrations are reached in 6 to 8 hours.
Fluoxetine is metabolized in the liver by isoenzymes of the cytochrome P450 system, including CYP2D6. The role of GYP in the metabolism of fluoxetine may be clinically important, as there is great genetic variability in the function of this enzyme among people. Only one metabolite of fluoxetine, norfluoxetine (N-demethylated fluoxetine), is biologically active. Steady concentration in the blood is achieved only after four weeks The brain concentration of fluoxetine and its metabolites keeps increasing through at least the first five weeks of treatment. That means that the full benefits of the current dose a patient receives are not realized for at least a month since its initiation Likewise, complete excretion of the drug may take several weeks.
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