Summary
The beta-adrenoceptor blocking effects of pindolol were compared with those of a placebo in a double-blind trial in twelve hypertensive Africans. Heart rate and arterial blood pressure were measured at rest and immediately after exercise, before and at intervals up to 8 h after oral administration of the drugs. Plasma levels of pindolol were also determined. Pindolol reduced systolic blood pressure and antagonised exercised-induced tachycardia. The mean time to peak level of pindolol was 1.9 h and the mean half-life was 4.2 h. Comparison of plasma levels of pindolol and beta-adrenoceptor blocking activity showed good correlation between them. It is concluded that the pharmacokinetics and beta-blocking effects of pindolol in Africans are not dissimilar from published data for other races.
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Aellig, W.H., Saameli, K.: Prolonged action of pindolol. Br. Med. J.1973/II, 365
Eckberg, D.L., Drabinsky, M.I., Braunwald, E.: Defective cardiac parasympathetic control in patients with heart disease. N. Engl. J. Med.285, 877–883 (1971)
Falase, A.O., Salako, L.A., and Aderounmu, A.F.: A trial of pindolol in hypertensive Nigerians. Trop. Cardiol.3, 111–120 (1977)
Gugler, R., Bodem, G.: Single and multiple dose pharmacokinetics of pindolol. Europ. J. clin. Pharmacol.3, 13–16 (1978)
Gugler, R., Herold, W., Dengler, H.J.: Pharmacokinetics of pindolol in man. Europ. J. clin. Pharmacol.7, 17–24 (1974)
Gugler, R., Hoebel, W., Bodem, G., Dengler, H.J.: The effect of pindolol on exercise-induced cardiac acceleration in relation to plasma levels in man. Clin. Pharmacol. Ther.17, 127–133 (1975)
Humphreys, G.S., Delvin, D.G.: Ineffectiveness of propranolol in hypertensive Jamaicans. Br. Med. J.1968/II, 601–603
Johnsson, G., Regardh, G.-G.: Clinical pharmacokinetics of B-adrenoceptor blocking drugs. Clin. Pharmacokinet.1, 233–263 (1976)
Lavene, D., Weiss, Y.A., Safar, M.E., Loria, Y., Georges, D., Milliez, P.L.: Pharmacokinetics and hepatic extraction ratio of pindolol in hypertensive patients with normal and impaired renal function. J. clin. Pharmacol.7, 501–508 (1977)
Oh, V.M.S., Kaye, C.M., Warrington, S.J., Taylor, E.A., Wadsworth, J.: Studies of cardioselectivity and partial agonist activity in β-adrenoceptor blockade comparing effects on heart rate and peak expiratory flow rate during exercise. Br. J. clin. Pharmacol.5, 107–120 (1978)
Olsson, S.B., Varnauskas, E.: Duration of B-receptor blockade after oral administration of LB-46. Europ. J. clin. Pharmacol.5, 214–217 (1973)
Pacha, W.L.: A method for the fluorimetric determination of 4-(2-hydroxy-3-isopropylaminopropoxyl-indole (LB 46), a B-blocking agent, in plasma and urine. Experientia258, 802–803 (1969)
Prichard, B.N.C.: β-adrenoceptor blockade in hypertension past, present and future. Br. J. clin. Pharmacol.5, 379–399 (1978)
Richardson, D.W., Freund, Gear, A.S., Mauck, H.P., Preston, L.W.: Effect of propranolol on elevated arterial blood pressure. Circulation37, 534–542 (1968)
Robinson, B.F., Epstein, S.E., Beiser, C.D., and Braunwald, E.: Control of the heart rate by the autonomic nervous system: studies in man between baro-receptor mechanisms and exercise. Circ. Res.19, 400–411 (1966)
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Salako, L.A., Falase, A.O., Ragon, A. et al. Beta-adrenoceptor blocking effects and pharmacokinetics of pindolol. Eur J Clin Pharmacol 15, 299–304 (1979). https://doi.org/10.1007/BF00558431
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DOI: https://doi.org/10.1007/BF00558431