<unk> s are well absorbed in the gastrointestinal tract and reach peak plasma levels within 1–8 hours. During absorption<unk> s bind to proteins and are widely distributed throughout the body, including the brain, whereas they are lipophilic. Metabolism and elimination takes place mainly in the liver and most of the<unk> s produce pharmacologically active metabolites, as demonstrated in table 3 among with other pharmacology properties of the<unk> s. Table 3 Comparative pharmacology of<unk> s<unk> tmax (h) Bioavailability (%) VD (L/kg) Protein binding (%) t1/2 Metabolism Active metabolites Excretion Fluoxetine 6–8 60–80 20–45 94.5 Acute administration, 1–3 days. Chronic administration, 4–6 days. Norfluoxetine, acute and chronic administration, 4–16 days Extensive first-pass hepatic mainly by CYP2D6 by desmethylation. Non-linear pharmacokinetic profile Norfluoxetine Mainly (60%) urine Sertraline 4.5–8.4 Absolute bioavailability has not been determined in humans 20 98 25–26 hours Extensive first-pass hepatic primarily by CYP2B6 Desmethyl-sertraline (limited activity) Faeces and urine in equal amount Paroxetine 6–10 30–60 3.1–28 93–95 21–24 hours Extensive first-pass hepatic primarily by CYP2D6. Non-linear pharmacokinetic profile No clinically important metabolites Urine (64%) and faeces (36%) (via the bile) Fluvoxamine 3–8 50 25 77–80 15.6 hours Hepatic by CYP1A2 and CYP3A4 No clinically important metabolites Mainly urine Citalopram 2–4 80 12 50 35 hours Hepatic by CYP3A4 and CYP2C19 mainly via N-demethylation Desmethyl-citalopram 12–23% unchanged in the urine and 10% in faeces Escitalopram 4–5 80 12 56 27–32 hours Hepatic by CYP3A4 and CYP2C19 mainly via N-demethylation (S)-demethylcitalopram. Not clinically important 8–10% (of escitalopram and (S)-demethylcitalopram (S-DCT)) in the urine tmax = Time to peak plasma level after oral dose; VD = Volume of distribution; t1/2 = Elimination half-life
Development and discovery of SSRI drugs
Suicide prevention
Recovered-memory therapy
Chronic fatigue syndrome treatment
Drug rehabilitation
Alternative therapies for developmental and learning disabilities
Experimental cancer treatment
Alternative cancer treatments