Chemical structure of fluoxetine
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Fluoxetine

Fluoxetine hydrochloride is an antidepressant drug used medically in the treatment of depression, obsessive-compulsive disorder, bulimia nervosa, premenstrual dysphoric disorder and panic disorder. Fluoxetine is also used (off-label) to treat many other conditions, such as ADHD. more...

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It is sold under the brand names Prozac®, Symbyax® (compounded with olanzapine), Sarafem®, Fontex® (Sweden), Foxetin® (Argentina), Ladose® (Greece), Fluctin® (Austria, Germany), Prodep® (India), Fludac*® (India) and Lovan® (Australia). Fluoxetine was derived from diphenhydramine, an antihistamine found to inhibit reuptake of the neurotransmitter serotonin.

Compared to other popular selective serotonin reuptake inhibitors, fluoxetine has a strong energizing effect. This makes fluoxetine highly effective in treatment of clinical depression cases where symptoms like depressed mood and lack of energy prevail. Although stimulating, it is also approved for a variety of anxiety disorders, including panic disorder and obsessive compulsive disorder.

Eli Lilly's Prozac was approved by the FDA on December 29, 1987 and introduced in the US at the beginning of 1988. The drug became very popular, with millions around the world having taken the medication. In the fall of 2001, Eli Lilly lost a patent dispute with Barr Laboratories and now fluoxetine hydrochloride is manufactured by many companies.

Uses

Approved

Fluoxetine hydrochloride is approved in the United States to treat depression, obsessive-compulsive disorder, bulimia nervosa, premenstrual dysphoric disorder and panic disorder. In the United Kingdom, it is approved to treat depression with or without anxiety, bulimia nervosa, and obsessive-compulsive disorder.

In December 2003 the FDA approved Symbyax® to treat bipolar depression. Symbyax is a combination of fluoxetine and olanzapine. (However, the pure form of fluoxetine can cause mania, mixed-states, rapid cycling and psychosis in bipolar patients, particularly if the patient is not also taking a mood stabilizer.)

Unapproved/Off-label/Investigational

In 2003, Michel Harper, Fukodome Takayasu, and Andrew G. Engel reported that fluoxetine given over a period of three years at doses of up to 80-120 mg/day to two patients with slow-channel congenital myasthenic syndrome who were allergic to quinidine resulted in substantial subjective and objective improvement in muscle strength.

Mechanism of action

Recent research indicates that fluoxetine may increase the production of new neurons (brain cells) in adult brain (adult neurogenesis), and that it interacts with the system of "clock genes", the transcription factors involved in drug abuse and possibly obesity ,.

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Fluoxetine for Premenstrual Dysphoric Disorder
From American Family Physician, 4/15/01 by Monica Preboth

The U.S. Food and Drug Administration has approved a new indication for fluoxetine, a selective serotonin reuptake inhibitor (SSRI), for the treatment of premenstrual dysphoric disorder (PMDD). Fluoxetine was previously sold only under the brand name Prozac. It is now marketed as Sarafem for treatment of PMDD.

PMDD causes depression, anxiety, irritability, anger and other symptoms in the two weeks before menses. The severity of symptoms of PMDD interfere with a patient's occupational and social functioning.

According to the January 22, 2001 issue of The Medical Letter, clinical trials of women with PMDD showed that fluoxetine taken in a dosage of 20 to 60 mg per day through six menstrual cycles improved mood symptoms in 53 percent of participants, compared with improvement in 28 percent of those who took placebo. Results of another trial suggest that taking 20 mg per day of fluoxetine only for the two weeks before menses might be as effective as taking it throughout the cycle.

The Medical Letter reports that the most common side effects associated with SSRIs are nausea, headache, nervousness, insomnia, rash, fatigue and sexual dysfunction, including decreased libido and anorgasmia. Prolonged use may lead to weight gain. Fluoxetine also inhibits cytochrome P450 enzymes 2D6 and 3A4 and interacts with many other drugs.

Sarafem and Prozac are both available in 10- and 20-mg capsules, but in different colors and different packaging. According to The Medical Letter, generic fluoxetine is expected to be available sometime in 2001.

COPYRIGHT 2001 American Academy of Family Physicians
COPYRIGHT 2001 Gale Group

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