Literature DB >> 2454374

Mechanism of the vasodilatory effect of carvedilol in normal volunteers: a comparison with labetalol.

L X Cubeddu1, N Fuenmayor, F Varin, V G Villagra, R E Colindres, J R Powell.   

Abstract

In a single blind parallel design, saline (n = 9), labetalol i.v. (40 mg n = 4, 80 mg n = 3), and carvedilol i.v. (15 mg n = 8) were given to volunteers with blood pressure (BP) recorded intraarterially. The effect of these treatments on the response to challenge doses of angiotensin II (to give a rise in mean BP of 20-25 mm Hg), isoproterenol (to give an increase in heart rate of 30-35 beats/min), and phenylephrine (to give a rise in mean BP of 20-25 mm Hg) were studied. The dose of i.v. carvedilol employed gave a greater fall in BP than the dose of labetalol used. Carvedilol appeared to be about four times more potent than labetalol in inhibiting the tachycardia to isoprenaline. Likewise, from inhibition of the pressor response to phenylephrine, it is concluded that carvedilol is four times more effective at the alpha receptor than labetalol. Neither drug was found to antagonize the pressor effects of angiotensin. Calculation of the half-life of carvedilol gave values of 2.2 to 9 h. The volume of distribution was found to be 1.54 l/kg and the total body clearance was 0.521 l/h/kg.

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Year:  1987        PMID: 2454374

Source DB:  PubMed          Journal:  J Cardiovasc Pharmacol        ISSN: 0160-2446            Impact factor:   3.105


  13 in total

1.  Antihypertensive effect of carvedilol: a preliminary dose-response study.

Authors:  B Casadei; J Conway; A J Coats; R Bird
Journal:  Clin Investig       Date:  1992

2.  Dose-effect relationship of carvedilol in essential hypertension. An open study.

Authors:  T Ogihara; Y Goto; K Yoshinaga; Y Kumahara; O Iimura; M Ishii; E Murakami; T Takeda; T Kokubu; K Arakawa
Journal:  Drugs       Date:  1988       Impact factor: 9.546

3.  Vasodilating mechanism and response to physiological pressor stimuli of acute doses of carvedilol compared with labetalol, propranolol and hydralazine.

Authors:  B Tomlinson; F Bompart; B R Graham; J B Liu; B N Prichard
Journal:  Drugs       Date:  1988       Impact factor: 9.546

Review 4.  Progress in antihypertensive therapy with a multiple-action drug.

Authors:  B N Prichard; B Tomlinson
Journal:  Drugs       Date:  1988       Impact factor: 9.546

5.  Haemodynamic effects of new beta-blockers with vasodilatory properties in essential hypertension.

Authors:  H Tsukiyama; K Otsuka; M Horii
Journal:  Drugs       Date:  1988       Impact factor: 9.546

6.  The dose dependency of the alpha- and beta-adrenoceptor antagonist activity of carvedilol in man.

Authors:  T C Tham; S Guy; B J McDermott; R G Shanks; J G Riddell
Journal:  Br J Clin Pharmacol       Date:  1995-07       Impact factor: 4.335

Review 7.  Antihypertensive profile of carvedilol.

Authors:  W Meyer-Sabellek; B Agrawal
Journal:  Clin Investig       Date:  1992

8.  Clinical pharmacology of carvedilol.

Authors:  B Tomlinson; B N Prichard; B R Graham; R J Walden
Journal:  Clin Investig       Date:  1992

Review 9.  Clinical pharmacokinetics and pharmacodynamics of carvedilol.

Authors:  T Morgan
Journal:  Clin Pharmacokinet       Date:  1994-05       Impact factor: 6.447

10.  Single and repeated doses of the vasodilator/beta-adrenergic antagonist, carvedilol, block cirazoline- and isoproterenol-mediated hemodynamic responses in the conscious rat.

Authors:  E F Smith; M J Slivjak; R Gagnon
Journal:  Cardiovasc Drugs Ther       Date:  1992-10       Impact factor: 3.727

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