It also comes in a delayed-release capsule formulation with dosing at 90 mg per week. When treating bulimia, an efficacious dose is generally 60 mg to 80 mg daily. Generally, 20 mg to 40 mg daily dosing is required to be effective for most individuals. Some individuals may require dosing of 60 to 80 mg daily. For an individual with poorly tolerated side effects, the drug may be dosed in 10 mg tablets instead of 20 mg tablets to help minimize any side effects. Keeping in mind that the medication can be efficacious at doses of 5 milligrams and weighing in on the side effect profile, it is essential to note that the drug can be administered in smaller doses. It is only available in an oral formulation available in oral solution (20 mg/5 ml), tablet (10 mg, 20 mg, 60 mg), capsule (10 mg, 20 mg, 40 mg), and delayed-release capsule (90 mg). įluoxetine should be administered once a day, either in the morning or evening, and started at 20 mg daily. It is also important to remember that fluoxetine has a half-life of 2 to 4 days, and its active metabolite norfluoxetine has a half-life of 7 to 9 days. Additionally, norfluoxetine can have an inhibitory effect on CYP3A4. It is important to remember that fluoxetine has several drug-drug interactions due to its metabolism at the CYP2D6 isoenzyme. Fluoxetine's active metabolite is norfluoxetine, which gets produced when the cytochrome P450 enzyme (CYP2D6) acts on it. Due to its reuptake of serotonin, fluoxetine produces an activating effect, and due to its long half-life, the initial antidepressant effect emerges within 2 to 4 weeks. Fluoxetine also has mild activity at the 5HT2A and 5HT2C receptors.įluoxetine has minimal activity on noradrenergic reuptake. Fluoxetine exerts its effects by blocking the reuptake of serotonin into presynaptic serotonin neurons by blocking the reuptake transporter protein located in the presynaptic terminal. Presynaptic serotonin (5HT1A) receptors are in the dorsal raphe nucleus and project to the prefrontal cortex. Additionally, lower numbers of serotonin uptake sites are located on the platelets of patients with depression. Low concentrations of serotonin appear in the cerebrospinal fluid of patients with depression. Serotonin and norepinephrine, both biological amines, have been shown to play a role in depression.
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