Summary
Following a single oral dose of 6 mg bunazosin, a novel α1-adrenoceptor antagonist, the pharmacokinetics and blood pressure behaviour of 37 patients were studied. 12 subjects had normal renal and hepatic function (mean creatinine clearance (GFR) 107±240 ml/min, antipyrine clearance (AP Cl) 47±10.2 ml/min; x±SD), 13 subjects had impaired renal function (mean GFR 38±11.5 ml/min, AP Cl 39±4.0 ml/min), and 12 patients had liver cirrhosis which was confirmed by liver biopsy (mean AP Cl 18±9.2 ml/min, GFR 92±8.1 ml/min). The groups studied were matched for age and body weight. The area under the plasma level time curve (AUC0−∞) of bunazosin increased from 96.6±48.7 μg.ml−1. h in the normals to 157.0±101.0 μg.ml−1.h in the liver patients and to 298.2±199.4 μg.ml−1.h in patients with impaired renal function (P<0.05). As there was a close correlation between plasma levels and antihypertensive activity of bunazosin in the present study, dosage adjustment of the α1-receptor blocker in patients with impaired liver and kidney function appears to be mandatory.
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Halabi, A., Nokhodian, A. & Kirch, W. Bunazosin in patients with impaired hepatic or renal function. Eur. J. Drug Metab. Pharmacokinet. 18, 309–313 (1993). https://doi.org/10.1007/BF03188813
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DOI: https://doi.org/10.1007/BF03188813