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PharmacodynamicsThe capacity of labetalol HCl to block alpha receptors in man has been demonstrated by attenuation of the pressor effect of phenylephrine and by a significant reduction of the pressor response caused by immersing the hand in ice-cold watercold-pressor testLabetalol HCl’s beta 1receptor blockade in man was demonstrated by a small decrease in the resting heart rateattenuation of tachycardia produced by isoproterenol or exerciseand by attenuation of the reflex tachycardia to the hypotension produced by amyl nitriteBeta 2receptor blockade was demonstrated by inhibition of the isoproterenol-induced fall in diastolic blood pressureBoth the alphaand beta-blocking actions of orally administered labetalol HCl contribute to a decrease in blood pressure in hypertensive patientsLabetalol HCl consistentlyin dose-related fashionblunted increases in exercise-induced blood pressure and heart rateand in their double productThe pulmonary circulation during exercise was not affected by labetalol HCl dosing.

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the oral ld 50 value of trandate hct labetalol hydrochloride in the mouse is approximately 600 mg kg and in the rat is greater than 2 g kg.