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. 1980 Jun;9(6):569–575. doi: 10.1111/j.1365-2125.1980.tb01082.x

Cardiovascular effects of single oral doses of the new beta-adrenoceptor blocking agents betaxolol (SL 75212) in healthy volunteers.

P J Cadigan, D R London, B L Pentecost, G Bianchetti, R Gomeni, J R Kilborn, P L Morselli
PMCID: PMC1430003  PMID: 6104498

Abstract

1 The effects of betaxolol (SL 75212), a new beta-adrenoceptor blocking agent, on the cardiovascular response to exercise have been studied in six normal subjects after placebo and single oral doses of 5, 10, 20 and 40 mg given double-blind in a randomized sequence. 2 All doses reduced exercise heart rate, with a significant reduction persisting to 23 h after doses of 20 mg and 40 mg. Systolic blood pressure on exercise was reduced after all doses, with a reduction continuing to 23 h after doses of 10 mg and above. 3 The mean elimination half-life of SL 75212 was 17.5 +/- 3.9 h. The plasma clearance ranged from 0.15--0.48 1 kg-1 h-1 and the volume of distribution from 5.8--13 1 kg-1. 4 There was a significant correlation between the peak blood levels and change in exercise heart rate (r = 0.53, P less than 0.05) and between the area under the blood concentration curve and the effect of the exercise heart rate (r = 0.55, P less than 0.01).

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Bianchetti G., Ganansia J., Morselli P. L. Sensitive gas chromatographic method for the determination in blood and urine of SL 75212 [4-(2-cyclopropylmethoxyethyl)-1-phenoxy-3-isopropylaminopropan-2-ol], a new beta 1 adrenoceptor blocking agent. J Chromatogr. 1979 Aug 1;176(1):134–139. doi: 10.1016/s0021-9673(00)92096-x. [DOI] [PubMed] [Google Scholar]
  2. Boudot J. P., Cavero I., Fénard S., Lefèvre-Borg F., Manoury P., Roach A. G. Preliminary studies on SL 75212, a new potent cardioselective beta-adrenoceptor antagonist [proceedings]. Br J Pharmacol. 1979 Jul;66(3):445P–445P. [PMC free article] [PubMed] [Google Scholar]
  3. Carruthers S. G., Kelly J. G., McDevitt D. G., Shanks R. G. Blood levels of practolol after oral and parenteral administration and their relationship to exercise heart rate. Clin Pharmacol Ther. 1974 May;15(5):497–509. doi: 10.1002/cpt1974155497. [DOI] [PubMed] [Google Scholar]
  4. Dreyfuss J., Brannick L. J., Vukovich R. A., Shaw J. M., Willard D. A. Metabolic studies in patients with nadolol: oral and intravenous administration. J Clin Pharmacol. 1977 May-Jun;17(5-6):300–307. doi: 10.1002/j.1552-4604.1977.tb04609.x. [DOI] [PubMed] [Google Scholar]
  5. Dreyfuss J., Shaw J. M., Ross J. J., Jr Absorption of the beta-adrenergic-blocking agent, nadolol, by mice, rats, hamsters, rabbits, dogs, monkeys, and man: an unusual species difference. Xenobiotica. 1978 Aug;8(8):503–508. doi: 10.3109/00498257809056152. [DOI] [PubMed] [Google Scholar]
  6. Evans G. H., Shand D. G. Disposition of propranolol. VI. Independent variation in steady-state circulating drug concentrations and half-life as a result of plasma drug binding in man. Clin Pharmacol Ther. 1973 Jul-Aug;14(4):494–500. doi: 10.1002/cpt1973144part1494. [DOI] [PubMed] [Google Scholar]
  7. Frithz G. Dose-ranging study of the new beta-adrenergic antagonist nadolol in the treatment of essential hypertension. Curr Med Res Opin. 1978;5(5):383–387. doi: 10.1185/03007997809111902. [DOI] [PubMed] [Google Scholar]
  8. Johnsson G., Regårdh C. G., Sölvell L. Combined pharmacokinetic and pharmacodynammc studies in man of the adrenergic beta1-receptor antagonist metoprolol. Acta Pharmacol Toxicol (Copenh) 1975;36(Suppl 5):31–44. doi: 10.1111/j.1600-0773.1975.tb03320.x. [DOI] [PubMed] [Google Scholar]
  9. McAinsh J. Clinical pharmacokinetics of atenolol. Postgrad Med J. 1977;53 (Suppl 3):74–78. [PubMed] [Google Scholar]
  10. Riess W., Rajagopalan T. G., Imhof P., Schmid K., Keberle H. Metabolic studies on oxprenolol in animals and man by means of radio-tracer techniques and GLC-analysis. Postgrad Med J. 1970 Nov;(Suppl):32–39. [PubMed] [Google Scholar]
  11. Routledge P. A., Shand D. G. Clinical pharmacokinetics of propranolol. Clin Pharmacokinet. 1979 Mar-Apr;4(2):73–90. doi: 10.2165/00003088-197904020-00001. [DOI] [PubMed] [Google Scholar]
  12. Shand D. G. Pharmacokinetic properties of the beta-adrenergic receptor blocking drugs. Drugs. 1974;7(1):39–47. doi: 10.2165/00003495-197407010-00003. [DOI] [PubMed] [Google Scholar]
  13. Shanks R. G., Carruthers S. G., Kelly J. G., McDevitt D. G. Correlation of reduction of exercise heart rate with blood levels of atenolol after oral and intravenous administration. Postgrad Med J. 1977;53 (Suppl 3):70–73. [PubMed] [Google Scholar]
  14. Wan S. H., Koda R. T., Maronde R. F. Pharmacokinetics, pharmacology of atenolol and effect of renal disease. Br J Clin Pharmacol. 1979 Jun;7(6):569–574. doi: 10.1111/j.1365-2125.1979.tb04644.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Watson R. D., Littler W. A. Onset and duration of beta-adrenergic receptor blockade following single oral dose acebutolol hydrochloride (Sectral). Br J Clin Pharmacol. 1979 Jun;7(6):557–561. doi: 10.1111/j.1365-2125.1979.tb04642.x. [DOI] [PMC free article] [PubMed] [Google Scholar]

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