Bunazosin in patients with impaired hepatic or renal function

Halabi, A.; Nokhodian, A.; Kirch, W.

European Journal of Drug Metabolism and Pharmacokinetics 18(3): 309-313


ISSN/ISBN: 0378-7966
PMID: 7908631
DOI: 10.1007/bf03188813
Accession: 008247983

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Following a single oral dose of 6 mg bunazosin, a novel alpha-1-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 (AUC-0- infin ) of bunazosin increased from 96.6 +- 48.7 mu-g.ml-1.h in the normals to 157.0 +- 101.0 mu-g.ml-1.h in the liver patients and to 298.2 +- 199.4 mu-g.ml-1.h in patients with impaired renal function (P lt 0.05). As there was a close correlation between plasma levels and antihypertensive activity of bunazosin in the present study, dosage adjustment of the alpha-1-receptor blocker in patients with impaired liver and kidney function appears to be mandatory.

Bunazosin in patients with impaired hepatic or renal function