The disposition and protein binding of batanopride and its metabolites in subjects with renal impairment
| Autor: | K. A. Dandekar, M. E. Brady, Charles E. Halstenson, L. Smaldone, Edward F. Foote, William F. Keane, J. V. St. Peter, J. L. Pykkonen |
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| Rok vydání: | 1993 |
| Předmět: |
Adult
Male medicine.medical_specialty medicine.drug_class Metoclopramide Renal function Plasma protein binding chemistry.chemical_compound Pharmacokinetics Internal medicine medicine Antiemetic Humans Pharmacology (medical) Aged Pharmacology business.industry Antagonist General Medicine Metabolism Disposition Blood Proteins Middle Aged Endocrinology chemistry Female Kidney Diseases Serotonin Antagonists business Batanopride Protein Binding |
| Zdroj: | European journal of clinical pharmacology. 45(1) |
| ISSN: | 0031-6970 |
| Popis: | We have studied the disposition of batanopride and its three major metabolites (the erythro-alcohol, threo-alcohol, and N-desethyl metabolites) in 27 subjects with various degrees of renal function after intravenous infusion of a single dose of 3.6.mg.kg-1 of batanopride over 15 min. The subjects were assigned to one of three treatment groups: group 1, normal renal function (creatinine clearanceor = 75 ml.min-1 x 1.73 m-2; n = 13); group 2, moderate renal impairment (creatine clearance 30-60 ml.min-1 x 1.73 m-2; n = 8); group 3, severe renal impairment (creatinine clearanceor = 30 ml.min-1 x 1.73 m-2; n = 6). The terminal half-life of batanopride was significantly prolonged from 2.7 h in group 1 to 9.9 h in group 3. The renal clearance of batanopride was significantly lower in group 3 (25 ml.min-1) compared with group 1 (132 ml.min-1). There were no differences in plasma protein binding or steady-state volume of distribution of batanopride among the groups. There were significantly lower renal clearances for all three metabolites in groups 2 and 3 compared with group 1. The half-lives of all three metabolites were significantly prolonged in group 3 compared with group 1. The dose of batanopride may need to be reduced in patients with creatinine clearances less than 30 ml.min-1 x 1.73 m-2 to prevent drug accumulation and avoid possible dose-related adverse effects. |
| Databáze: | OpenAIRE |
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