The Sound of Evolution
Amlodipine
Mechanism of action:
Amlodipine is a dihydropyridine calcium channel blocker. It selectively inhibits L-type Ca²⁺ channels on vascular smooth muscle cell membranes, reducing calcium influx into the cells. As intracellular Ca²⁺ concentration decreases, the interaction between actin and myosin is weakened, leading to vascular smooth muscle relaxation, reduced peripheral vascular resistance, and coronary artery dilation.
Reference(s):
1. Katoh M et al. (2000). Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4. Pharm Res.
2. Darvari R et al. (2004). Concentration dependency of modulatory effect of amlodipine on P-glycoprotein efflux activity of doxorubicin—a comparison with tamoxifen. J Pharm Pharmacol.
3. Kuzuya T et al. (2003). Amlodipine, but not MDR1 polymorphisms, alters the pharmacokinetics of cyclosporine A in Japanese kidney transplant recipients. Transplantation.