Amlodipine
Amlodipine. Long-acting dihydropyridine calcium-channel blocker — preferential vascular smooth-muscle Cav1.2 blockade with minimal cardiac… Oral half-life 36 h.
Long-acting dihydropyridine calcium-channel blocker — preferential vascular smooth-muscle Cav1.2 blockade with minimal cardiac effect. Lowers blood pressure via peripheral vasodilation. CYP3A4 substrate; weak inhibitor at higher doses. Pedal edema dose-related.
PK: THE CLEANEST RECORD IN ITS GROUP — THREE OF FOUR FIELDS VERIFY, AND THE OUTLIER-LOOKING NUMBERS ARE REAL. Verbatim: "Oral administration (single dose, 10 mg) to the same 12 volunteers gave a mean systemic availability of 64% and a mean plasma half-life of 36 h", and the volume is 21 L/kg x 70 stated under "Intravenous administration", so CLASS 6 IS ACQUITTED. Worth recording what the record did NOT do: the same abstract also contains a 45 h steady-state half-life and a 34 h intravenous one, and the record correctly took the single-dose oral value rather than averaging across arms. Only ka 0.3 fails, appearing nowhere; it implies a 9.78 h peak, which lands inside this drug textbook window, so it is consistent with having been tuned rather than measured, though no quoted Tmax exists to prove it.
Pharmacokinetics
- Oral — t½ 36 h · F 64% · Vd 1470 L
Sources: PMID:1711625