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  • Verapamil hydrochloride: pharmacological properties and role in cardiovascular therapeutics.

Verapamil hydrochloride: pharmacological properties and role in cardiovascular therapeutics.

Pharmacotherapy (1982-11-01)
S H Baky, B N Singh
摘要

Verapamil hydrochloride, a prototype calcium antagonist, is now marketed in the United States for the acute treatment of supraventricular tachyarrhythmias and for chronic management of vasospastic and chronic stable angina. It inhibits the slow inward channel in in the heart and blocks calcium influx in smooth muscle. Its intrinsic negative inotropic action, which is apparent in isolated tissues, is offset in vivo by peripheral vasodilation. It has a mild, noncompetitive sympathetic antagonist effect; its most important electrophysiologic action is a depression of AV nodal conduction, accounting for its effect in supraventricular tachyarrhythmias. Its hemodynamic actions are characterized by a complex interplay of changes in preload, afterload, contractility, heart rate, and coronary blood flow. It does not depress cardiac function, except in severe heart failure. The drug has a mild dilator action on coronary arteries and reverses ergonovine-induced vasoconstriction. Controlled trials have established its role in Prinzmetal's variant angina, unstable angina, and chronic stable angina. It has also been found to be effective in obstructive cardiomyopathies. The potential role of verapamil in such conditions as hypertension, cardioprotection, and Raynaud's phenomenon needs further evaluation; at present these indications have not been approved by the Food and Drug Administration. The most common side effects include constipation, skin rash, and dizziness; AV block, heart failure, and sinus arrest may occasionally be encountered, especially when ventricular function is compromised or conduction system disease is present.

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Sigma-Aldrich
(±)-维拉帕米 盐酸盐, ≥99% (titration), powder
USP
维拉帕米 盐酸盐, United States Pharmacopeia (USP) Reference Standard
Supelco
Verapamil hydrochloride solution, 1.0 mg/mL in methanol (as free base), ampule of 1 mL, certified reference material, Cerilliant®
维拉帕米, European Pharmacopoeia (EP) Reference Standard
Supelco
(±)-维拉帕米 盐酸盐, Pharmaceutical Secondary Standard; Certified Reference Material