New therapeutic trends in calcium antagonism. Are they meaningful?
Recent advances in the field of calcium antagonism include the development of long-acting calcium antagonists, some of which have a slow onset of action. Some of these newly developed calcium antagonists are dihydropyridine derivatives. Others, including monatepil (AJ-2615), are chemically unrelated to either the dihydropyridine (nifedipine), phenylalkylamine (verapamil), or benzothiazepine (diltiazem) prototypes of the group. Irrespective of their chemistry, however, vascular selectivity is a prominent feature of the more recently developed calcium antagonists. This, coupled with their long duration and slow onset of action, properties that facilitate continuous protection rather than the intermittent protection of short-acting calcium antagonists, makes them suitable for use as blood pressure-lowering agents that provide "vascular protection"--as indicated by their ability to slow experimentally induced atherosclerotic lesion formation. Long-acting vasculoprotective calcium antagonists can be used to treat other disorders, including angina pectoris. Their efficacy as antiatherosclerotic agents, proven in experimental models, needs to be confirmed by clinical trials on natural atherosclerosis.
Nayler
W G
WG
Department of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Victoria, Australia.
D000818:Animals; D001161:Arteriosclerosis / Q000517:prevention & control*; D002121:Calcium Channel Blockers / Q000494:pharmacology* / Q000627:therapeutic use; D003988:Dibenzothiepins / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D010879:Piperazines / Q000494:pharmacology / Q000627:therapeutic use
D002121:Calcium Channel Blockers; D003988:Dibenzothiepins; D010879:Piperazines; C067818:monatepil