Escitalopram
Escitalopram. Pure S-enantiomer of citalopram — the pharmacologically active stereoisomer. Cleaner side-effect profile (lower QT risk at… Oral half-life 27 h.
Pure S-enantiomer of citalopram — the pharmacologically active stereoisomer. Cleaner side-effect profile (lower QT risk at therapeutic doses) and best-tolerated SSRI in head-to-head network meta-analyses (Cipriani 2018).
PK: THE HEALTHIEST RECORD OF THE BATCH, AND BOTH PAIR TESTS PASS. V 1100 L is verbatim and INTRAVENOUS-DERIVED — "After intravenous infusion of escitalopram, the mean systemic clearance and volume of distribution were 31 L/h and 1,100 L" — so class 6 does not apply despite the surface shape, and the model own clearance of 28.2 L/h agrees with the published 31 to within 9%. A FALSE POSITIVE IS PRE-EMPTED: a later review, by a CO-AUTHOR of that primary, restates the same 1100 L as an oral Vz/F; do not "correct" it to 880. THE ENANTIOMER DIRECTION TEST PASSES WITH A SOURCE: 27 h against the racemate 35 h is correct chemistry, because "the latter two phenotypes eliminated S-CT more rapidly via CYP2C19" makes R-citalopram the slower half. ka 0.7 is refuted by its own source Tmax, implying 4.90 h against "attained after 3 to 4 hours". F 0.8 is unsourced here — the abstract only paraphrases "a high absolute bioavailability" — and is carried on the racemate measurement. Its only reference was a MISFILE: a January 2000 review of five SSRIs published two years before this drug was marketed, which never mentions it.
Pharmacokinetics
- Oral — t½ 27 h · F 80% · Vd 1100 L
Related compounds
- Citalopram — synergistic
Sources: PMID:17375980