Atorvastatin
Atorvastatin. Competitively inhibits HMG-CoA reductase (cholesterol synthesis) — the rate-limiting enzyme of cholesterol biosynthesis. ldl… Oral half-life 7 h.
Competitively inhibits HMG-CoA reductase (Cholesterol synthesis) — the rate-limiting enzyme of cholesterol biosynthesis. LDL receptor + PCSK9 axis LDLR upregulation → 40–60% LDL reduction at high-intensity doses. Pleiotropic effects (plaque stabilisation, endothelial function, anti-inflammation) contribute to CV benefit beyond LDL alone. Long t½ → any-time-of-day dosing (vs Simvastatin evening).
PK: CLASS 12, AND THE FIX IS TO PUT THE WHOLE BLOCK ON ONE SELF-CONSISTENT ABSTRACT. The stored half-life of 11.4 h is verbatim, but from a DIFFERENT dataset — a terminal t1/2z for parent acid — while the volume belongs with a 7 h effective half-life. Bolting the terminal slope onto that volume dropped implied clearance to 23.1 L/h against the review own "The total plasma clearance of atorvastatin acid is 625 mL/min", and inflated exposure 2.24x AGAINST THE VERY PAPER THE RECORD CITED. CLASS 6 IS ACQUITTED, AND PROVABLY SO: no human intravenous atorvastatin study exists, but three numbers in one abstract are mutually consistent ONLY if the volume is true — "The volume of distribution of atorvastatin acid is 381L" with that clearance and "the half-life is about 7 hours" reproduce each other to 0.6%, whereas a V/F reading would imply a 0.98 h half-life and contradict the same sentence. The stored 380 was off by one from the verbatim 381. THE ANALYTE IS CORRECT WITH A SCOPE CAVEAT: the mass and both sources are the acid, so there is no acid-versus-lactone confusion, but the same paper shows the ortho-hydroxy metabolite carrying 1.8 times the parent exposure, so the prose claim that a long half-life permits any-time-of-day dosing is METABOLITE-DRIVEN and the record models the minority species.
Pharmacokinetics
- Oral — t½ 7 h · F 14% · Vd 381 L
Related compounds
- CoQ10 — caution
- Colchicine — caution
- Ezetimibe — synergistic
- Fenofibrate — caution
Sources: PMID:14531725, PMID:15572716, PMID:22801271