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Pharmacokinetics of the Antianginal Agent Perhexiline: Relationship Between Metabolic Ratio and Steady-state Dose by Benedetta C. Sallustio; Ian S. Westley; Raymond G. Morris is a Medicine article available to read on EtoBox.

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**Aims** 1) To develop an estimate of oral clearance ( /__F__) for the antianginal agent perhexiline based on the ratio of __cis__‐OH‐perhexiline metabolite/parent perhexiline plasma concentrations at steady‐state . 2) To determine whether the ratio measured in the first fortnight of treatment may be used to guide patient dosing with perhexiline, a drug with a narrow therapeutic index, long half‐life and saturable metabolism via CYP2D6. **Methods** Two retrospective studies were conducted reviewing patient records and data obtained from routine monitoring of plasma perhexiline and __cis__‐OH‐perhexiline concentrations. **Results** __Study 1 (n=70)__. At steady‐state, the frequency distributions of /__F__ and / were consistent with CYP2D6 metabolism. Putative poor metabolizers (approximately 8%) were identified by /__F__≤50 ml min^−1^ or /≤0.3. A group of patients with /__F__≥950 ml min^−1^ may have been ultra‐rapid metabolizers. In this group, the high /__F__ values suggest extensive first‐pass metabolism and poor bioavailability. In patients with therapeutic plasma perhexiline concentrations (0.15–0.60 mg l^−1^), the variability in dose appeared directly proportional to /__F__ (__

Who reads Pharmacokinetics of the Antianginal Agent Perhexiline: Relationship Between Metabolic Ratio and Steady-state Dose?

Author

Benedetta C. Sallustio; Ian S. Westley; Raymond G. Morris

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley; Research Square (ISSN 0306-5251)

Published

2002

Language

EN

Field

Medicine (Health Sciences)