Ro 31-1118, a new cardioselective beta-adrenoceptor antagonist. Pharmacokinetics and effects on heart rate and blood pressure in mild hypertensives.
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| Abstract |
Five patients with mild hypertension were given single oral doses of Ro 31-1118 (10,20,40, and 80 mg) and placebo in a randomized, double-blind, within-patient study. Plasma concentrations of Ro 31-1118 and supine, standing, exercise, and post-exercise heart rates and blood pressures were measured before and at regular intervals after drug administration. The pharmacokinetic data were consistent with a one-compartment model with first-order absorption and a variable time lag. Peak plasma concentrations and area under curve were linearly related to dose, whereas time to peak concentration, half-time, clearance and apparent volume of distribution were dose-independent. There was a reduction in exercise and post-exercise heart rate of approximately 10% after 10 mg and 20 mg Ro 31-1118, and of approximately 15% after 40 mg and 80 mg. At all doses standing systolic blood pressure was reduced by approximately 5%. A similar fall was seen in exercise and post-exercise systolic blood pressures. There was no substantial effect of Ro 31-1118 on supine or standing heart rates nor on diastolic blood pressure. No adverse effects were reported. It is concluded that Ro 31-1118 has linear pharmacokinetics over the dose range 10-80 mg, and has a weak antihypertensive effect when administered in single doses to patients with mild hypertension.
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| Authors | M Jamieson, J C Petrie, J Webster, A Miller, R I Harris, R J Francis |
| Journal | European journal of clinical pharmacology (Eur J Clin Pharmacol) Vol. 29 Issue 4 Pg. 395-9 ( 1985) ISSN: 0031-6970 [Print] Germany |
| PMID | 2868899 (Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial) |
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