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Pharmacokinetics of atenolol in patients with renal impairment

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Summary

The pharmacokinetics of atenolol, a new cardioselective β-adrenoceptor blocking agent, were determined following both acute and chronic dosing in 33 hypertensive patients with widely differing levels of renal impairment. In patients with normal renal function the atenolol half-life was calculated to be about six hours following single 100 mg oral doses. This value increased markedly in patients with renal insufficiency and the blood clearance of atenolol was found to have a significant correlation with the glomerular filtration rate. This demonstrated the importance of the kidneys in the elimination of the drug. After 8 weeks oral treatment with atenolol (100 mg twice daily) a significant decrease in blood pressure, heart rate and plasma renin activity was observed, but no correlation was established between the blood levels of atenolol and any of its pharmacodynamic effects. A positive correlation was found however between the anti-hypertensive action of atenolol and the pretreatment value of the plasma renin activity.

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References

  • Amery, A., McAinsh, J., De Plaen, J-F., Reybrouck, T.: Relationship between the blood level of atenolol and its pharmacological effect. Clin. Pharmacol. Ther.21, 691–699 (1976)

    Google Scholar 

  • Anavekar, S. N., Louis, W. J., Morgan, T. O., Doyle, A. E., Johnston, C. I.: The relationship of plasma levels of pindolol in hypertensive patients to effects on blood pressure, plasma renin and plasma noradrenaline levels. Clin. Exp. Pharmacol. Physiol.2, 203–211 (1975)

    Google Scholar 

  • Barrett, A. M., Carter, J., Fitzgerald, J. D., Hull, R., Le Count, D.: A new type of cardioselective adrenoceptive blocking drug. Brit. J. Clin. Pharmacol.48, 340 P. (1973)

  • Bennett, W. M., Singer, I. and Coggins, C. J.: A guide to drug therapy in renal failure. J. Amer. Med. Ass.230, 1544–1553 (1974)

    Google Scholar 

  • Bodem, G., Chidsey, C. A.: Pharmacokinetic studies of practolol, a beta-adrenergic antagonist in man. Clin. Pharmacol. Ther.14, 26–29, (1973)

    Google Scholar 

  • Bodem, G., Grieser, H., Eichelbaum, M., Gugler, R.: Pharmacokinetics of practolol in renal failure. Europ. J. Pharmacol.7, 249–252 (1974)

    Google Scholar 

  • Bravo, E. L., Tarazi, R. C., Dustan, H. P., Lewis, J. W.: Dissociation between renin and arterial pressure responses to beta adrenergic blockade in human essential hypertension. Circ. Res.35, Suppl. I, I, 241–247 (1975)

    Google Scholar 

  • Brown, H. C., Carruthers, S. G., Johnston, G. D., Kelly, J. G., McAinsh, J., McDevitt, D. G., Shanks, R. G.: Clinical pharmacology of atenolol a new β-adrenoceptor blocking drug. Clin. Pharmacol. Ther.20, 524–534 (1976)

    Google Scholar 

  • Buhler, F. R., Laragh, J. H., Baer, L., Vaughn Jr. E. D., Brunner, H. R.: Propranolol inhibition of renin secretion. New. Engl. J. Med.287, 1209–1214 (1972)

    Google Scholar 

  • Bugler, F. R., Burkart, F., Lutold, B. E., Kung, M., Marbet, G., Pfisterer, M.: Anti-hypertensive beta blocking action as related to renin and age: a pharmacological tool to identify pathogenic mechanisms in essential hypertension. Am. J. Cardiol.36, 653–669 (1975)

    Google Scholar 

  • Conway, F. J., Fitzgerald, J. D., McAinsh, J., Rowlands, D. J., Simpson, W. T.: Human pharmacokinetic and pharmacodynamic studies on atenolol (ICI 66,082) a new cardioselective beta adrenoceptor blocking drug. Brit. J. Clin. Pharmacol.3, 267–272 (1976)

    Google Scholar 

  • Geyskes, C. G., Boer, M., Vos, J., Leenen, F. H. H., Dorhout-Mees, E. J.: Effect of salt depletion and propranolol on blood pressure and plasma renin activity in various forms of hypertension. Circ. Res.35, Sept. I, I. 248–256 (1975)

    Google Scholar 

  • Gysling, E., de Wurstemberger, B.: Effects d'une medication combinee d'hydrochlorothiazide et d'oxprenolol sur la tension arterielle et l'activite de renine plasmatique. Schweiz. Med. Wschr.104, 1797–1798 (1974)

    Google Scholar 

  • Hansson, L., Zweifler, A. J., Julius, S., Ellis, L. N.: Propranolol therapy in essential hypertension: observations on predictability of therapeutic response. Int. J. Clin. Pharmacol.10, 79–89 (1974)

    Google Scholar 

  • Lowenthal, D. T., Briggs, W. A., Gibson, T. P., Nelson, H., Cirksena, W. B.: Pharmacokinetics of oral propranolol in chronic renal disease. Clin. Pharmacol. Ther.16, 761–769 (1974)

    Google Scholar 

  • Ohnhaus, E. E.: The pharmacokinetics of unchanged pindolol in patients with impaired renal function. Brit. J. Pharmacol.47, 11 P (1973)

    Google Scholar 

  • Oie, S., and Levy, G.: Relationship between renal function and elimination kinetics of pindolol in man. Europ. J. clin. Pharmacol.9, 115–116 (1975)

    Google Scholar 

  • Sassard, J., Vincent, M., Annat, G., Bizollon, Ch. A.: Influence of orthostatism on plasma renin and aldosterone in man. J. clin. Endocrinol. Metab.42, 16–21 (1976)

    Google Scholar 

  • Sassard, J., Pozet, N., Vincent, M., Zech, P.: The effects of atenolol on renin release in hypertensives. New Engl. J. Med.294, 787 (1976)

    Google Scholar 

  • Scales, B., Copsey, P. B.: The gas chromatographic determination of atenolol in biological samples. J. Pharm. Pharmacol.51, 169–171 (1975)

    Google Scholar 

  • Stumpe, K. O., Vetter, H., Hessen-Bruch, V., Dusing, R., Kolloch, R., Kruck, F.: Effect of chronic beta adrenergic blockade on blood pressure and release of renin, aldosterone and cortisol in essential HTA. Klin. Wschr.53, 907–912 (1975)

    Google Scholar 

  • Tarazi, R. C., Dustan, H. P.: Beta adrenergic blockade in hypertension practical and theoretical implications of long term haemodynamic variations. Amer. J. Cardiol.29, 633–640 (1972)

    Google Scholar 

  • Thompson, F. D., Joekes, A. M., Foulkes, D. M.: Pharmacodynamics of propranolol in renal failure. Brit. Med. J.1972/2, 434–436

    Google Scholar 

  • Tjandramaga, T. B., Thomas, J., Verbeck, R., Verbesselt, R., Verberokmoes, R., de Schepper, P. J.: The effect of end-stage renal failure and haemodialysis on the elimination kinetics of sotalol. Brit. J. Clin. Pharmacol.3, 259–265 (1976)

    Google Scholar 

  • Vincent, M., Sassard, J., Cier, J. F.: Methode rapide de determination radio-immunochinique de l'activitie renine du plasma. Rev. Europ. Et. Clin. Biol.17, 1001–1006, (1972)

    Google Scholar 

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Sassard, J., Pozet, N., McAinsh, J. et al. Pharmacokinetics of atenolol in patients with renal impairment. Eur J Clin Pharmacol 12, 175–180 (1977). https://doi.org/10.1007/BF00609856

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