Fluoxetine: Difference between revisions
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| halflife = 1–4 days (7–15 days for norfluoxetine) | | halflife = 1–4 days (7–15 days for norfluoxetine) | ||
| bioavailability = 70–90% (oral) | | bioavailability = 70–90% (oral) | ||
| pregnancy = Category C<ref>https://www.ncbi.nlm.nih.gov/books/NBK501186/</ref> | | pregnancy = Category C<ref name ="lactmed">https://www.ncbi.nlm.nih.gov/books/NBK501186/</ref> | ||
| legal = Rx-only | | legal = Rx-only in US | ||
| mechanism = | | mechanism = TrkB/BDNF<ref name="trkb">https://pmc.ncbi.nlm.nih.gov/articles/PMC9666396/</ref> <vote slug="ssri-claim">Fluoxetine is a selective serotonin reuptake inhibitor.</vote> | ||
| intro = Fluoxetine was the first of a long line of SSRIs. It is notable for its extremely long half-life and relative lack of withdrawal syndrome. It can also be useful in helping taper and discontinue other SxRI medicines. | | intro = Fluoxetine was the first of a long line of SSRIs. It is notable for its extremely long half-life and relative lack of withdrawal syndrome. It can also be useful in helping taper and discontinue other SxRI medicines. | ||
| pk_absorption = | | pk_absorption = 70-90%<ref name="statpearls">https://www.ncbi.nlm.nih.gov/books/NBK459223/</ref> Oral bioavailability | ||
| pk_distribution = | | pk_distribution = Fluoxetine has plasma protein binding of approximately 94.5%, bound to albumin and alpha-1 glycoprotein. Fluoxetine readily crosses the blood-brain barrier, with a brain-to-plasma ratio of 2.6:1 in humans. The volume of distribution (Vd) of fluoxetine and its metabolite ranges between 20 to 42 L/kg. Some studies report that fluoxetine has the maximum volume of distribution (Vd) of any SSRI (between 14 and 100 L/kg).<ref name="statpearls"/> | ||
| pk_metabolism = Fluoxetine's active metabolite is norfluoxetine, produced when the cytochrome P450 enzyme (CYP2D6) acts on it. Prescribers must remember that fluoxetine has several drug-drug interactions due to its metabolism through the CYP2D6 isoenzyme. Additionally, norfluoxetine can have an inhibitory effect on CYP3A4. Fluoxetine has a half-life of 2 to 4 days, and its active metabolite norfluoxetine has a half-life of 7 to 9 days. Approximately 7% of individuals definitively exhibit poor metabolism of fluoxetine due to reduced activity of CYP2D6. | | pk_metabolism = Fluoxetine's active metabolite is norfluoxetine, produced when the cytochrome P450 enzyme (CYP2D6) acts on it. Prescribers must remember that fluoxetine has several drug-drug interactions due to its metabolism through the CYP2D6 isoenzyme. Additionally, norfluoxetine can have an inhibitory effect on CYP3A4. Fluoxetine has a half-life of 2 to 4 days, and its active metabolite norfluoxetine has a half-life of 7 to 9 days. Approximately 7% of individuals definitively exhibit poor metabolism of fluoxetine due to reduced activity of CYP2D6. | ||
| pk_elimination = | | pk_elimination = | ||