Fluoxetine: Difference between revisions
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| bioavailability = 70–90% (oral) | | bioavailability = 70–90% (oral) | ||
| pregnancy = Category C<ref name="lactmed">S0</ref> | | pregnancy = Category C<ref name="lactmed">S0</ref> | ||
| legal = Rx-only in US | | legal = [[USLegal:Prescription only|Rx-only]] in US | ||
| mechanism = TrkB/BDNF<ref name="trkb">S1</ref> <vote slug="ssri-claim">Fluoxetine is a selective serotonin reuptake inhibitor.</vote> | | mechanism = TrkB/BDNF<ref name="trkb">S1</ref> <vote slug="ssri-claim">Fluoxetine is a selective serotonin reuptake inhibitor.</vote> | ||
| intro = Fluoxetine, marketed as Prozac, was the first selective serotonin reuptake inhibitor ([[:Category:Selective_Serotonin_Reuptake_Inhibitors_(SSRIs)|SSRIs]]) brought to market and the medicine that opened the SSRI era. It was discovered at Eli Lilly's laboratories in Indianapolis on 24 July 1972 by a team that included the chemists Bryan Molloy and Klaus Schmiegel and the pharmacologist David Wong,<ref name="wong1974">Wong DT, Horng JS, Bymaster FP, Hauser KL, Molloy BB. A selective inhibitor of serotonin uptake: Lilly 110140, 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine. Life Sciences. 1974;15(3):471-479. PMID: 4549929.</ref> approved by the FDA in December 1987, and launched in the United States as Prozac in January 1988. It is notable for the extremely long half-life of its active metabolite norfluoxetine, which gives the medicine an unusually mild discontinuation profile and makes it useful as a bridge in tapering patients off shorter-acting serotonergic medicines. | | intro = Fluoxetine, marketed as Prozac, was the first selective serotonin reuptake inhibitor ([[:Category:Selective_Serotonin_Reuptake_Inhibitors_(SSRIs)|SSRIs]]) brought to market and the medicine that opened the SSRI era. It was discovered at Eli Lilly's laboratories in Indianapolis on 24 July 1972 by a team that included the chemists Bryan Molloy and Klaus Schmiegel and the pharmacologist David Wong,<ref name="wong1974">Wong DT, Horng JS, Bymaster FP, Hauser KL, Molloy BB. A selective inhibitor of serotonin uptake: Lilly 110140, 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine. Life Sciences. 1974;15(3):471-479. PMID: 4549929.</ref> approved by the FDA in December 1987, and launched in the United States as Prozac in January 1988. It is notable for the extremely long half-life of its active metabolite norfluoxetine, which gives the medicine an unusually mild discontinuation profile and makes it useful as a bridge in tapering patients off shorter-acting serotonergic medicines. | ||
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| pk_absorption = 70–90%<ref name="statpearls">S3</ref> oral bioavailability. | | pk_absorption = 70–90%<ref name="statpearls">S3</ref> oral bioavailability. | ||
| 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_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 ([[ | | pk_metabolism = Fluoxetine's active metabolite is norfluoxetine, produced when the cytochrome P450 enzyme ([[Enzyme:CYP2D6|CYP2D6]]) acts on it. Prescribers must remember that fluoxetine has several med-med interactions due to its metabolism through the CYP2D6 isoenzyme. Additionally, norfluoxetine can have an inhibitory effect on [[Enzyme:CYP3A4|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.<ref name="statpearls"/> | ||
| pk_elimination = | | pk_elimination = | ||
| pharmacodynamics = | | pharmacodynamics = | ||