Olmesartan
Olmesartan. AT1 receptor blocker — medoxomil prodrug ester. Distinctive sprue-like enteropathy in some chronic users (rare but FDA boxed… Oral half-life 13 h.
AT1 receptor blocker — medoxomil prodrug ester. Distinctive sprue-like enteropathy in some chronic users (rare but FDA boxed warning). Hypertension; less data in HFrEF than other ARBs.
PK: A TEXTBOOK CLASS 12, CAUGHT AGAINST A CLEARANCE VERBATIM IN ITS OWN ABSTRACT. The cited paper is explicitly a TWO-COMPARTMENT population model — "CL/F (6.66 L/h for a typical male Western hypertensive patient), absorption rate constant (1.46h-1), elimination rate constant (0.193h-1), rate constant from the central to peripheral compartment (0.061h-1) ... and absorption lag-time (0.427h)" — and the record paired that model central volume with its beta half-life, asserting CL/F 3.49 against the abstract own 6.66. AUC was 1.91x too high. The volume moves to the value that reproduces the published clearance at the stored half-life. NEITHER F NOR THE HALF-LIFE MAY BE TOUCHED INSTEAD: holding V at 17 L would force the half-life down to 6.8 h and destroy the once-daily profile that is this drug entire clinical identity. ka 1.46 is verbatim and stays, and the verbatim absorption lag of 0.427 h is added, which moves the peak to about 2.8 h and matches the measured "1.4 to 2.8 hours". CLASS 6 ACQUITTED — the same source states "When administered intravenously, RNH-6270 has a volume of distribution of 15 to 25 L". F 0.26 is verbatim, but in a DIFFERENT paper than the one cited for it.
Pharmacokinetics
- Oral — t½ 13 h · F 26% · ka 1.46 h⁻¹ · Vd 32.5 L
Sources: PMID:16372830, PMID:8566137, PMID:11361048