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Clinical Pharmacokinetics of Urapidil

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Summary

Urapidil is a selective α1adrenoceptor antagonist with central antihypertensive action which is increasingly used in the treatment of hypertension. Urapidil is readily absorbed, is subject to moderate first-pass metabolism and is eliminated primarily as metabolites of much lower antihypertensive activity than the parent drug.

The influences of age, renal and hepatic disease on the disposition of urapidil are reviewed. Studies on the relationship between pharmacodynamics and pharmacokinetics show that the optimum use of urapidil in clinical practice depends on an understanding of the pharmacokinetic properties of the drug.

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References

  • Bories P, Ampelas M, Bauret P, Michel H. The pharmacokinetics of urapidil in liver impairment. In Amery (Ed.) Treatment of hypertension with urapidil: preclinical and clinical update, pp. 53–56, ICSS 101, Royal Society of Medicine Services Limited, London, 1986

    Google Scholar 

  • Fischer R, Haerlin R, Steinijans VW, Zech K, Bruckschen EG. Preliminary results on the correlation between serum level and antihypertensive effect of urapidil (Ebrantil). Methods and Findings in Experimental and Clinical Pharmacology 3: 89S–93S, 1981

    PubMed  Google Scholar 

  • Fozard JR, Mir AK. Are 5-HT receptors involved in the antihypertensive effects of urapidil. British Journal of Pharmacology 90: 24P, 1987

    Google Scholar 

  • Franke N, Schmucker P, van Ackern K, Reichert B. Anti-hypertensive Therapie mit Urapidil wä hrend der Narkose. Therapiewoche 30: 880–886, 1980

    Google Scholar 

  • Gemeiner M, Zech K. Development of a radioimmunoassay for urapidil. (Manuscript in preparation), 1987

  • Gillis RA, Dretchen KL, Namath I, Anastasi N, Souza JD, et al. Hypotensive effect of urapidil: CNS site and relative contribution. Journal of Cardiovascular Pharmacology 9: 103–109, 1987

    PubMed  CAS  Google Scholar 

  • Godehardt E, Wambach G, Heitz W, Steinijans VW, Haerlin R, et al. Pharmacokinetics of urapidil in patients with normal and impaired renal function. In Amery (Ed.) Treatment of hypertension with urapidil: preclinical and clinical update, pp. 71–86, ICSS 101, Royal Society of Medicine Services Limited, London, 1986

    Google Scholar 

  • Haerlin R. Bioavailability of urapidil from sustained-release capsules. Byk Gulden Research Report 109-110/84, 1984

  • Haerlin R, Engelstätter R, Henze F, Radtke HW. Treatment of primary and secondary hypertension: long-term use of urapidil (Ebrantil®). Clinical Trials Journal 22: 215–223, 1985

    Google Scholar 

  • Israili ZH. Correlation of pharmacological effects with plasma levels of antihypertensive drugs in man. Annual Review of Pharmacology and Toxicology 19: 25–52, 1979

    Article  PubMed  CAS  Google Scholar 

  • Junger H, van Deyk K, Kopp M. Hä modynamik unter antihypertensiver Therapie mit Urapidil und Nitroprussid-Natrium. In Kaufmann & Bruckschen (Eds) Urapidil — Darstellung einer neuen antihypertensiven Substanz, pp. 139–146, Excerpta Medica, 1982

    Google Scholar 

  • Kirsten R, Nelson K, Molz KH, Haerlin R, Steinijans VW. Pharmacodynamics and pharmacokinetics of urapidil in hypertensive patients: a crossover study comparing infusion with an infusion-capsule combination. European Journal of Clinical Pharmacology 32: 61–65, 1987

    Article  PubMed  CAS  Google Scholar 

  • Kirsten R, Nelson K, Neff J, Haerlin R, Steinijans VW, et al. Pharmacodynamics and pharmacokinetics of three different doses of urapidil infused in hypertensive patients. European Journal of Clinical Pharmacology 30: 549–552, 1986

    Article  PubMed  CAS  Google Scholar 

  • Kolassa N, Bischler P, Beller KD, Sanders KH. Inhibition of the hypotensive effect of urapidil and 8-OH-DPAT by the 5-HT receptor antagonist spiroxatrine in cats. Abstract 23P. Serotonin Satellite Meeting, 10th IUPHAR Congress, Sydney, Australia, 1987

  • Liebau H, Haehn KD, Wurst W, Solleder P. Efficacy, safety and tolerability of urapidil: results of a multicentre trial. Journal of Hypertension 4: S141–S143, 1986

    Article  Google Scholar 

  • Leibetseder F. Beziehung zwischen Blutdruck und Serumspiegel von Urapidil. In Kaufmann & Bruckschen (Eds) Urapidil — Darstellung einer neuen antihypertensiven Substanz, pp. 71–80, Excerpta Medica, Amsterdam, 1982

    Google Scholar 

  • Michel JP, Hessel L, Zech K, Steinijans VW. Pharmacokinetics and pharmacodynamics of urapidil in the elderly. In Amery (Ed.) Treatment of hypertension with urapidil: preclinical and clinical update, pp. 39–45 ICSS 101, Royal Society of Medicine Services Limited, London, 1986

    Google Scholar 

  • Mönch E, Jäckel R, Kohlen W, Diel H. Serumkonzentrationen von Urapidil bei Normo- und Hypertonikern. In Kaufmann & Brickschen (Eds) Urapidil — Darstellung einer neuen antihypertensiven Substanz, pp. 65–70, Excerpta Medica, Amsterdam, 1982

    Google Scholar 

  • Nieder M, Dilger C, Haerlin R. Quantitation of urapidil and its metabolites in human serum by high performance liquid chromatography. Journal of High Resolution Chromatography and Chromatography Communications 8: 224–229, 1985

    Article  CAS  Google Scholar 

  • Puchstein C, Van Aken H, Zander J, Lawin P. Die Anwendung von Urapidil in der perioperativen Phase. Anaesthesist 33: 224–227, 1984

    PubMed  CAS  Google Scholar 

  • Ramage AG. A comparison of the effects of doxazosin and alfuzosin with those of urapidil on preganglionic sympathetic nerve activity in anaesthetised cats. European Journal of Pharmacology 129: 307–314, 1986

    Article  PubMed  CAS  Google Scholar 

  • Rosenthal J, Haerlin R. Hypertonie-Behandlung mit Alpha-Blockade oder ACE-Hemmung. Fortschritte der Medizin 104: 763–766, 1986

    PubMed  CAS  Google Scholar 

  • Sanders KH, Jurna I. Effects of urapidil, clonidine, prazosin and propranolol on autonomic nerve activity, blood pressure and heart rate in anaesthetized rats and cats. European Journal of Pharmacology 110: 181–190, 1985

    Article  PubMed  CAS  Google Scholar 

  • Sanders KH, Kilian U, Kolassa N, Schoetensack W. Influence of urapidil on α-and β-adrenoreeeptors in pithed rats. Journal of Autonomic Pharmacology 5: 307–316, 1985

    Article  PubMed  CAS  Google Scholar 

  • Schöber JG, Pilossoff W, Bühlmeyer K. Urapidil therapy for acute hypertensive crises in infants and children. European Journal of Pediatrics 143: 87–91, 1984

    Article  PubMed  Google Scholar 

  • Slingeneyer A, Mourad G, Zech K, Mion C. Pharmacokinetics of urapidil in end stage renal failure. In Amery (Ed.) Treatment of hypertension with urapidil: preclinical and clinical update, pp. 57–61, ICSS 101, Royal Society of Medicine Services Limited, London, 1986

    Google Scholar 

  • Solleder P, Haerlin R, Zech K. Assessment of potential pharmacokinetic interaction of urapidil on digoxin. Byk Gulden Research Report 223/87, 1987

  • Somogyi A, Muirhead M. Pharmacokinetic interactions of cimetidine 1987. Clinical Pharmacokinetics 12: 321–366, 1987

    Article  PubMed  CAS  Google Scholar 

  • Storck J, Kirsten R, Haerlin R. Einfluβ von freien Fettsä uren auf die Plasmaproteinbindung von Urapidil. Arzneimittel-Forschung, in press, 1987

    Google Scholar 

  • Sturm E, Zech K. Determination of urapidil in human serum using solid probe chemical ionization mass spectrometry and stable isotope labeling. In Schmidt et al. (Eds) Stable isotopes, pp. 241–246, Elsevier Scientific Publishing Company, Amsterdam, 1982

    Google Scholar 

  • Sturm E, Zech K. Biotransformation of urapidil: isolation and identification of metabolites in mouse, rat, dog and man. Biomedical Mass Spectrometry 11: 211–216, 1984

    Article  PubMed  CAS  Google Scholar 

  • van Zwieten PA, Mathy MJ, Thoolen MJ. Deviating central hypotensive activity of urapidil in the cat. Journal of Pharmacy and Pharmacology 37: 810–811, 1985

    Article  PubMed  Google Scholar 

  • Wambach G, Godehardt E, Lang R, Heitz W, Meurer KA, et al. Pharmacodynamics of urapidil in essential hypertension and in chronic renal failure. In Amery (Ed.) Treatment of hypertension with urapidil: preclinical and clinical update, pp. 63–69, ICSS 101, Royal Society of Medicine Services Limited, London, 1986

    Google Scholar 

  • Zähringer J, Klepzig M, Greif J, Ludwig B, Strauer B. Anti-hypertensive Therapie mit Urapidil bei Hochdruckkrisen. Herz Kreislauf 15: 546–549, 1983

    Google Scholar 

  • Zech K, Arnold P, Liechti H, Ludwig G. HPLC in pharmacokinetics and metabolism studies. Chromatographia 12: 354–358, 1979

    Article  CAS  Google Scholar 

  • Zech K, Eltze M, Kilian U, Sanders KH, Kolassa N. Biotransformation of urapidil: metabolites in serum and urine and theirbiologicalactivity invitroandinvivo. Archiveslnternatio nales de Pharmacodynamie et de Therapie 272: 180–196, 1984

    CAS  Google Scholar 

  • Zech K, Herzog R, Jantke K. In vivo and in vitro protein binding of urapidil. Byk Gulden Research Report 184/87, 1987

  • Zech K, Huber R. Determination of urapidil and its metabolites in human serum and urine: comparison of liquid-liquid and fully automated liquid-solid extraction. Journal of Chromatography 353: 351–360, 1986

    Article  PubMed  CAS  Google Scholar 

  • Zech K, Schilling G, Steinijans VW. Pharmacokinetics and acute hemodynamic effects after a single i.v. administration of 12.5, 25 or 50mg urapidil to patients with essential hypertension. Byk Gulden Research Report 411/85, 1985

  • Zech K, Steinijans VW, Radtke HW. Pharmacokinetics of urapidil in normal subjects. In Amery (Ed.) Treatment of hypertension with urapidil: preclinical and clinical update, pp. 29–38, ICSS 101, Royal Society of Medicine Services Limited, London, 1986

    Google Scholar 

  • Zech K, Sturm E. The pharmacokinetics and metabolism of urapidil (capsules) in the human. Byk Gulden Research Report 189/80, 1980

  • Zech K, Sturm E, Steinijans VW. Pharmakokinetik und Metabolismus von Urapidil (Ebrantil) bei Tier und Mensch. In Kaufmann & Bruckschen (Eds) Urapidil, Darstellung einer neuen antihypertensiven Substanz, pp. 50–64, Excerpta Medica, 1982

    Google Scholar 

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Kirsten, R., Nelson, K., Steinijans, V.W. et al. Clinical Pharmacokinetics of Urapidil. Clin-Pharmacokinet 14, 129–140 (1988). https://doi.org/10.2165/00003088-198814030-00001

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