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Clinical Pharmacokinetics of Quinidine

 

作者: Hermann R. Ochs,   David J. Greenblatt,   Elaine Woo,  

 

期刊: Clinical Pharmacokinetics  (ADIS Available online 1980)
卷期: Volume 5, issue 2  

页码: 150-168

 

ISSN:0312-5963

 

年代: 1980

 

出版商: ADIS

 

数据来源: ADIS

 

摘要:

The elimination of quinidine in humans is accomplished by a combination of renal excretion of the intact drug (15 to 40% of total clearance) and hepatic biotransformation to a variety of metabolites (60 to 85% of total clearance). Many of the metabolites appear to be pharmacologically active. Typical ranges for kinetic properties of quinidine in healthy persons are: apparent volume of distribution 2.0 to 3.5 litres/kg; elimination half-life 5 to 12 hours; clearance, 2.5 to 5.0ml/min/kg. Quinidine clearance is reduced in the elderly, in patients with cirrhosis, and in those with congestive heart failure.Oral quinidine is available either as relatively rapidly absorbed conventional tablets (usually quinidine sulphate) or as a variety of slowly absorbed sustained release preparations. Absolute systemic availability generally is 70% or greater.Quinidine is 70 to 95% bound to plasma protein, primarily to albumin but also to a number of other plasma constituents. Binding is reduced in patients with cirrhosis, partly because of hypoalbuminaemia, but is not influenced by renal insufficiency. Clinical interpretation of total serum or plasma quinidine concentrations must be altered in patients with reduced or increased binding, since it is the unbound fraction which is pharmacologically active.

 

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