Active ingredient: Fluoxetine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Antidepressants, Second-Generation
• Selective Serotonin Reuptake Inhibitors (SSRIs)

Dosage Forms

• Capsule
• Liquid
• Solution

Brands / Synonyms

Animex-On; Deprex; Eufor; Fluctin; Fluoxeren; Fluoxetina [Inn-Spanish]; Fluoxetina [Spanish]; Fluoxetine Hcl; Fluoxetine Hydrochloride; Fluoxetine Hydrochloride: Adofen; Fluoxetinum [Inn-Latin]; Fluval; Fontex; Foxetin; Portal; Prozac; Prozac Weekly; Pulvules; Reneuron; Sarafem; Sarafem ; Selfemra; Symbyax

Indications

For the treatment of depression, obsessive compulsive disorder, and bulimia nervosa.

Pharmacology

Fluoxetine, an antidepressant agent belonging to the selective serotonin reuptake inhibitors (SSRIs), is used to treat depression, bulimia nervosa, premenstrual dysphoric disorder, panic disorder and post-traumatic stress. According to the amines hypothesis, a functional decrease in the activity of amines, such as serotonin and norepinephrine, would result in depression; a functional increase of the activity of these amines would result in mood elevation. Fluoxetine's effects are thought to be associated with the inhibition of 5HT receptor, which leads to an increase of serotonin level.

Mechanism of Action

Metabolized to norfluoxetine, fluoxetine is a selective serotonin-reuptake inhibitor (SSRI), it blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT_1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs.

Absorption

72%

Toxicity

Symptoms of overdose include agitation, restlessness, hypomania, and other signs of CNS excitation. LD₅₀=284mg/kg (orally in mice).

Biotrnasformation / Drug Metabolism

Hepatic.

Contraindications

Prozac is contraindicated in patients known to be hypersensitive to it.

Monoamine oxidase inhibitors ¾ There have been reports of serious, sometimes fatal, reactions (including hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes that include extreme agitation progressing to delirium and coma) in patients receiving fluoxetine in combination with a monoamine oxidase inhibitor (MAOI), and in patients who have recently discontinued fluoxetine and are then started on an MAOI. Some cases presented with features resembling neuroleptic malignant syndrome. Therefore, Prozac should not be used in combination with an MAOI, or within a minimum of 14 days of discontinuing therapy with an MAOI. Since fluoxetine and its major metabolite have very long elimination half-lives, at least 5 weeks [perhaps longer, especially if fluoxetine has been prescribed chronically and/or at higher doses ] should be allowed after stopping Prozac before starting an MAOI.

Thioridazine ¾ Thioridazine should not be administered with Prozac or within a minimum of 5 weeks after Prozac has been discontinued .

Drug Interactions

Do not take this medicine with thioridizine, or within 5 weeks of taking fluoxetine.
Talk to your doctor if you are taking certain antibiotics such as erythromycin, clarithromycin
or azithromycin. This medicine should not be taken with MAO inhibitors.
Caution should be exercised when taking this medicine certain antibiotics, such as erythromycin,
clarithromycin, or azithromycin. This medicine should not be taken with MAO inhibitors. If you
think you are taking an MAO inhibitor talk to your doctor or pharmacist. Do not take this medicine
with St. John's Wort because of the additive effects of sertonin.
This medication should not be taken with MAO inhibitors. Your doctor or pharmacist can give you more information
on MAO inhibitors. Wait 5 weeks after stopping escitalopram before starting a non-selective MAO inhibitor. Wait 2
weeks after stopping an MAO inhibitor before starting escitalopram.
If you are taking medications for migraines such as Imitrex, talk to your doctor before starting this medicine.
If you are taking a tricyclic antidepressant, talk to your doctor before taking this medicine.
St. John¡¯s Wort should be avoided while taking this medicine due to the additive effects of serotonin.
Tell your doctor if you are taking any of the following drugs:
blood thinners (Coumadin)
other antidepressants
metoprolol
antihistamines
carbamazepine (Tegretol)
cimetidine (Tagamet)
estrogens
fluoxetine (Prozac)
intraconazole (Sporanox)
ketoconazole (Nizoral)
levodopa
lithium
muscle relaxants
birth control pills
sleeping pills
thyroid medications