Summary
The kinetics of absorption, distribution and excretion of pindolol have been investigated in 17 volunteers after an oral dose or intravenous infusion of 5 mg. The calculated absorption was 92%. The time course of the plasma levels appeared to follow first order kinetics with an apparent half life of 3.6 (oral) and 3.1 (i.v.) hours. The cumulative urinary excretion att=∞ was 36.1% and 39.2% of the dose administered, respectively, indicating extensive metabolism of the drug. The distribution volume was 136 l. Peak plasma levels were found 80 min after oral administration and they showed up to 4-fold variation after identical doses. Renal clearance was 216 ml×min−1 and total clearance was 483 ml×min−1. In plasma 57% of pindolol was bound to protein.
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Åblad, B., Ervik, M., Hallgren, J., Johnsson, G., Sölvell, L.: Pharmacological effects and serum levels of orally administered alprenolol in man. Europ. J. clin. Pharmacol.5, 44–52 (1972)
Barrett, A.M., Carter, J.: Comparative chronotropic activity of β-adrenoceptive antagonists. Brit. J. Pharmacol.40, 373 (1970)
Bodem, G., Chidsey, C.A.: Studies of practolol, a beta adrenergic antagonist, in man. Clin. Pharmacol. Ther.14, 26 (1973)
Brodie, B.B., Reid, W.D.: The value of determining the plasma concentration of drugs in animals and man. In: Fundamentals of drug metabolism and drug disposition, pps. 328–339. (Eds. LaDu, B.N., Mandel, H.G., Way, E.L.). Baltimore: Williams and Wilkins Company 1971
Dengler, H.J., Eichelbaum, M., Hengstmann, H., Wieber, J.: Pharmacokinetic studies in man with sparteine. Pharmacol. Clin.2, 189–195 (1970)
Dengler, H. J., Bodem, G., Wirth, K.: Pharmakokinetische Untersuchungen mit H3-Digoxin und H3-Lanatosid beim Menschen. Arzneimittel-Forsch.23, 64–74 (1973)
Diller, W.: In: Bünger, P., Diller, W., Führ, J. Arzneimittel-Forsch.11, 247 (1961)
Fitzgerald, J.D., Scales, B.: Effect of a new adrenergic beta-blocking agent (ICI 50, 172) on heart rate in relation to its blood levels. Int. J. clin. Pharmacol.1, 6, 467–474 (1968)
George, C.F., Fenyvesi, T., Conolly, M.E., Dollery, C.T.: Pharmacokinetics of dextro-, laevo-, and racemic propranolol in man. Europ. J. clin. Pharmacol.4, 74–76 (1972)
Gibaldi, M., Nagashima, R., Levy, G.: Relationship between drug concentration in plasma or serum and amount of drug in the body. J. Pharm. Sci.58, 193–197 (1969)
Giudicelli, J., Schmitt, H., Boissier, J.: Studies on DL-4-(2-hydroxy-3-isopropylaminopropoxy)-indole, a new potent beta adrenergic blocking drug. J. Pharmacol. exp. Ther.168, 345 (1969)
Gugler, R., Höbel, W., Bodem, G., Dengler, H.J.: Relationship between β-adrenergic blockade and plasma level of pindolol in man (In preparation)
Hicks, D.C., Arbab, A.G., Turner, P., Hills, M.: A comparison of intravenous pindolol and propranolol in normal man. J. clin. Pharmacol.12, 212–216 (1972)
Hill, R.C., Turner, P.: The effect of a new beta-adrenoceptive receptor blocking drug on heart rate in man. Brit. J. Pharmacol.32, 663 (1967)
Hill, R.C., Turner, P.: Preliminary investigations of a new beta-adrenoceptive receptor blocking drug LB 46, in man. Brit. J. Pharmacol.36, 368 (1969)
Johnsson, G., Sjögren, J., Sölvell, L.: Beta-blocking effect and serum levels of alprenolol in man after administration of ordinary and sustained release tablets. Europ. J. clin. Pharmacol.3, 74–81 (1971)
Koch-Weser, J.: Serum drug concentrations as therapeutic guides. New Engl. J. Med.287, 227–231 (1972)
Krieglstein, J., Kuschinsky, G.: Quantitative Bestimmungen der Eiweißbindung von Pharmaka durch Gelfiltration. Arzneimittel-Forsch.18, 287–289 (1968)
Levy, J.V.: Cardiovascular effects of prinodolol (LB 46), a potent beta-adrenergic receptor antagonist. J. Clin. Pharmacol.11, 249–260 (1971)
Lubawski, J., Wale, J.: Studies with LB 46, a new β-receptor blocking drug. Europ. J. Pharmacol.6, 345 (1969)
Martin, B.K.: Drug urinary excretion data — some aspects concerning their interpretation. Brit. J. Pharmac. Chemother.29, 181–193 (1967)
Nüesch, E.: Proof of the general validity of Dost's law of corresponding areas. Europ. J. clin. Pharmacol.6, 33–43 (1973)
Olsson, B.S., Varnauskas, E.: Duration of beta-receptor blockade after oral administration of LB-46. Europ. J. clin. Pharmacol.5, 214–217 (1973)
Pacha, W.L.: A method for the fluorometric determination of 4-(2-hydroxy-3-isopropylaminopropoxy)-indole, a β-blocking agent, in plasma and urine. Experientia25, 802–803 (1969)
Paterson, J.W., Conolly, M.E., Dollery, C.T., Hayes, A., Cooper, R.G.: The pharmacodynamics and metabolism of propranolol in man. Pharmacol. Clin.2, 127–133 (1970)
Saameli, K.: Comparative studies with β-receptor blocking agents and quinidine. Helv. physiol. pharmacol. Acta25, CR 432 (1967)
Shand, D.G., Nuckolls, E.M., Oates, J.A.: Plasma propranolol levels in adults, with observations in four children. Clin. Pharmacol. Ther.11, 112–120 (1970)
Wagner, J.G.: Pharmacokinetics. J.M. Richards Laboratory, Grosse Pointe Park, Michigan, USA, 1969; pp. 5–10
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Gugler, R., Herold, W. & Dengler, H.J. Pharmacokinetics of pindolol in man. Eur J Clin Pharmacol 7, 17–24 (1974). https://doi.org/10.1007/BF00614385
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DOI: https://doi.org/10.1007/BF00614385