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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. 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.

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. 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.
Fluoxetine Drug

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.

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 ,.

Interactions
Fluoxetine has a wide range of published interactions, notably with monoamine oxidase inhibitors (serotonin syndrome).

Fluoxetine along with several SSRI's are known to augment the effects of cannabis in multiples. One specific case of this interaction once rendered a 200+ pound male temporarily unconscious upon one "hit". Such interactions are ill-advised and highly dangerous.

Side effects
Common adverse effects include anxiety, which is possibly associated with an interaction of fluoxetine with the pineal gland, in addition to restlessness and insomnia. Weight loss, trembling, weakness, skin rash, anorgasmia, itching, and a decrease in sexual drive, have also been reported. Finally it has been reported to cause subsequent weight gain .

Like other SSRIs, an overdose of fluoxetine or combining it with other antidepressants can lead to serotonin syndrome.

Metabolism
Fluoxetine is eliminated very slowly by the body. The half-life of fluoxetine after a single dose is two days and, after multiple dosing, four days. The liver then metabolizes fluoxetine into norfluoxetine, a desmethyl metabolite, which is also a serotonin reuptake inhibitor; norfluoxetine has an even longer half-life, i.e. 8.6 and 9.3 days for single and repeated dosage respectively. These long half-lives may be helpful in those patients with compliance issues, but fluoxetine is most effective when taken daily. Other SSRIs have, by comparison, a very short half-life.

Some professionals feel that it is fluoxetine's long half-life that gives it much of its therapeutic utility, however this has never been proven under rigorous scientific study. Nevertheless, its long half life is also relevant because suddenly discontinuing SSRIs is known to produce both somatic and psychological withdrawal symptoms, a phenomenon known as "SSRI discontinuation syndrome". It is generally accepted that fluoxetines withdrawal symptoms are much smoother than with other SSRIs, as the substance takes several days to completely leave the system. Fluoxetine is a potent CYP2D6 inhibitor, which can decrease metabolism of other medications.

Formulations
Fluoxetine is sold in capsules containing 10, 20, 40 or 90 mg of active ingredient, in tablets containing 10 mg, or in an oral solution with concentration of 20 mg/5 ml. Dosages in the range of 20-60 mg per day are standard, with 80 mg considered a maximum.

Prozac Weekly is 90 mg of regular enteric-coated fluoxetine, taken every 7 days. The coating causes the fluoxetine to be dissolved in the intestines instead of the stomach. 4 or 5 regular 20mg doses taken at once will have a similar effect to Prozac Weekly with significantly lower costs, especially when using generic versions.

Other useful drug information: Demerol | Luvox | Synthroid | Norco | Nortriptyline | Lamictal | Carbamazepine

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