Candesartan
Candesartan. AT1 receptor blocker — cilexetil ester prodrug rapidly hydrolyzed during absorption. Long half-life supports once-daily dosing.… Oral half-life 9.3 h.
AT1 receptor blocker — cilexetil ester prodrug rapidly hydrolyzed during absorption. Long half-life supports once-daily dosing. Used for hypertension, HFrEF, and migraine prophylaxis (off-label).
PK: THE HALF-LIFE IS EXACTLY RIGHT AND ITS CITATION NEVER STATED IT. The old source says the half-life "were assessed" and then never reports it; the replacement gives "the elimination half-life was 9.3 h in healthy volunteers and 12 h in the patients", and whoever stored 9.3 correctly avoided the hepatic-impairment arm. The analyte declaration is confirmed - "Candesartan cilexetil is the prodrug of candesartan ... Absorbed candesartan cilexetil is completely metabolised to candesartan" - so modelling the acid at mw 440.45 is right. WHAT IS NOT FIXED HERE, DELIBERATELY: this record over-predicts candesartan exposure six- to eightfold and I will not close it with an invented number. {V 9, F 0.4, 9.3 h} imply CL/F 1.68 L/h against three independent measurements of 13.2, 9.9 and 17.5 L/h, and simulated Cmax at the typical 16 mg is about 710 ng/mL against an observed "160.91". The individual values are not the problem: 9 L is candesartan genuine small intravenous-derived volume and 9.3 h is a genuine terminal half-life, and they cannot coexist in one compartment. FIXING F ALONE MAKES IT WORSE - the tablet figure is about 15%, not the 40% that belongs to the oral SOLUTION, and F 0.15 would cut CL/F to 0.63 L/h. Reproducing the observed AUC needs V/F near 132 L, which no abstract states. Logged to AUTHORING_GAPS.
Pharmacokinetics
- Oral — t½ 9.3 h · F 40% · Vd 9 L
Sources: PMID:29746726, PMID:8331552, PMID:11825094, PMID:9696961