Telmisartan
Telmisartan. AT1 receptor blocker + partial PPAR-γ agonist — unique among ARBs in modest insulin-sensitizing activity. Long half-life supports… Oral half-life 24 h.
AT1 receptor blocker + partial PPAR-γ agonist — unique among ARBs in modest insulin-sensitizing activity. Long half-life supports once-daily dosing. Research interest as a longevity / metabolic compound goes beyond standard ARB use.
PK: MY PRIOR HELD AND THE OUTLIER-LOOKING VALUES ARE REAL. F 0.43 is verbatim - "Absolute bioavailability was 43%" - with a matched intravenous arm, and V 500 L is verbatim in a review as an explicitly STEADY-STATE volume, "a high of 500 L (telmisartan)", so pairing the two is CORRECT and class 6 is acquitted. I could NOT source my own claim of 42% at 40 mg rising to 58% at 160 mg from any abstract, and it is deliberately not stored; what is sourceable is only "maximum plasma concentrations increasing disproportionately with dose", and the verbatim 43% was measured on a 40 mg oral SOLUTION rather than a tablet. t-half 24 IS THE DOSING INTERVAL: no abstract states 24 h for telmisartan, and the one that comes closest contains both "a prolonged terminal elimination phase (> 20 h in healthy and hypertensive subjects)" and, in the same abstract, "the full 24-h dosing interval". No clean scalar replacement exists - the only point values are 27 to 42 hours in HEPATIC IMPAIRMENT - so 24 is retained with its true provenance stated and the verbatim inequality recorded, because the model needs an elimination rate. ka 1.4 is removed for being too SLOW: observed tmax is "0.5 to 1 hour" and 1.4 predicts 2.8 h. Telmisartan is "reversibly distributed into erythrocytes", which is noted but is not a matrix defect.
Pharmacokinetics
- Oral — t½ 24 h · F 43% · Vd 500 L
Sources: PMID:8220885, PMID:23471702, PMID:11185629, PMID:10854085, PMID:11014323