Sertraline
Sertraline. SSRI with modest dopamine-transporter activity at high doses (σ-1 binding contributes). Weaker CYP interactions than fluoxetine. 26-h… Oral half-life 26 h.
SSRI with modest dopamine-transporter activity at high doses (σ-1 binding contributes). Weaker CYP interactions than fluoxetine. 26-h t½.
PK: t-half 26 IS VERIFIED - "The mean t1/2el was 26.49 +/- 6.45 h for the test formulation" - and the analyte is the PARENT, assayed by HPLC-MS-MS, not desmethylsertraline. F 0.44 IS A FAECAL METABOLITE FRACTION: the SSRI review that carries it says "larger quantities of metabolites of paroxetine (36%) and sertraline (44%) are excreted in FAECES", and the cited bioequivalence study has no intravenous arm and therefore cannot report an absolute bioavailability at all. Because 1400 L is the label 20 L/kg and no human intravenous sertraline study exists, that volume is necessarily apparent, so F is pinned to 1 rather than deleted - which also removes the double-division the old pairing carried. ka 0.4 is removed as unsourced. THE DEFECT IN OUR OWN PROSE: this record effect_compartment note reads "sertraline 69-78% at 4 h", but the cited PET study says "Escitalopram AND sertraline showed high occupancies of 69.1-77.9% at 4h" - a combined two-drug range attributed to one drug - and the note is corrected. Its SERT affinity remains a full-text table value, which the note already discloses honestly; the abstract names only mazindol, sertraline at the DOPAMINE transporter, and nomifensine numerically. THE keo NOTE MERGED TWO DRUGS. It read "sertraline 69-78% at 4 h", but the cited PET study says "Escitalopram and sertraline showed high occupancies of 69.1-77.9% at 4h" — a COMBINED two-drug range attributed to sertraline alone. The 4 h peak-occupancy timing it anchors is unaffected; the range is not sertraline own.
Pharmacokinetics
- Oral — t½ 26 h · F 100% · Vd 1400 L
Sources: PMID:10674711, PMID:27082864, PMID:27738376