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  • A lipophilic, nonselective beta-adrenergic receptor antagonist with anti-anginal and antihypertensive activities. Penbutolol competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. In addition, penbutolol prevents the release of renin, a hormone secreted by the kidneys that causes constriction of blood vessels.
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