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Relative Potency and Selectivity of Calcium Antagonists Used in the Treatment of Migraine
Author(s) -
Peroutka Stephen J.,
Banghart Suzanne B.,
Allen George S.
Publication year - 1984
Publication title -
headache: the journal of head and face pain
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.14
H-Index - 119
eISSN - 1526-4610
pISSN - 0017-8748
DOI - 10.1111/j.1526-4610.1984.hed2402055.x
Subject(s) - flunarizine , cinnarizine , nimodipine , cyproheptadine , nifedipine , calcium channel , pharmacology , dihydropyridine , potency , medicine , calcium , anesthesia , chemistry , in vitro , serotonin , biochemistry , receptor
SYNOPSIS Calcium channel antagonists selectively block intracerebral vasoconstriction and appear clinically effective in the treatment of migraine. The in vitro method described in the present report measured both the absolute and relative potencies of a group of calcium blockers. The dihydropyridine drugs, nimodipine and nifedipine, were both the most potent and selective of the calcium antagonists studied. Cinnarizine and flunarizine were essentially equipotent in both basliar and femoral arteries while the traditional therapeutic agents, cyproheptadine and amitriptyline, were 10‐fold more potent in femoral than basilar artery. This rapid in vitro method may provide pharmacologic information which can be used as a guide in the selection of calcium channel antagonists for future clinical trials.