Amchek - Amchek is a long-acting 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, Amchek prevents calcium-dependent myocyte contraction and vasoconstriction. A second proposed mechanism for the drugâ€™s vasodilatory effects involves pH-dependent inhibition of calcium influx via inhibition of smooth muscle carbonic anhydrase. Some studies have shown that Amchek also exerts inhibitory effects on voltage-gated N-type calcium channels. N-type calcium channels located in the central nervous system may be involved in nociceptive signaling and pain sensation. Amchek is used to treat hypertension and chronic stable angina.|
Indication: For the treatment of hypertension and chronic stable angina.
Amchek belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. It was widely accepted that DHP CCBs target L-type calcium channels, the major channel in muscle cells that mediate contraction; however, some studies have indicated that Amchek also binds to and inhibits N-type calcium channels. Similar to other DHP CCBs, Amchek binds directly to inactive L-type calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives Amchek additional arterial selectivity. At therapeutic sub-toxic concentrations, Amchek has little effect on cardiac myocytes and conduction cells.