Nonlinear Elimination of Methyprylon (Noludar) in an Overdosed Patient: Correlation of Clinical Effects with Plasma Concentration
| Autor: | Nicholas Gerber, D C Mays, Denise A. Contos, Robert M. Guthrie, Kimberly F. Dixon |
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| Rok vydání: | 1991 |
| Předmět: |
Adult
Drug Methyprylon Pyridones medicine.drug_class Metabolite media_common.quotation_subject medicine.medical_treatment Pharmaceutical Science Pharmacology Hypnotic chemistry.chemical_compound Therapeutic index Pharmacokinetics medicine Humans Biotransformation Chromatography High Pressure Liquid Piperidones media_common business.industry Gastric lavage Suicide chemistry Anesthesia Sedative Female Spectrophotometry Ultraviolet business Half-Life medicine.drug |
| Zdroj: | Journal of Pharmaceutical Sciences. 80:768-771 |
| ISSN: | 0022-3549 |
| Popis: | This is a report of the pharmacokinetics of methyprylon and its major plasma metabolite, 5-methylpyrithyldione, in an overdosed patient using a reversed-phase HPLC assay. The decline in the concentration of plasma methyprylon was nonlinear between 66 and 30 micrograms/mL and linear at concentrations less than 30 micrograms/mL, with an apparent half-life of 4.4 h. The concentration of 5-methylpyrithyldione reached a maximum of 17 micrograms/mL approximately 13 h after admission and declined with a half-life of 8 h. Treatment of the patient was conservative, consisting of gastric lavage and supportive therapy. The patient regained consciousness when the methyprylon concentration fell below 43 micrograms/mL, and recovered from the overdose within 24 h. These results indicate that the pharmacokinetics of methyprylon are nonlinear (concentration dependent) in this overdosed patient; explanations include saturation of one or more of the metabolic pathways and/or product inhibition. The 4-h half-life of methyprylon, generally accepted for a therapeutic dose of 300 mg, is not appropriate in intoxicated patients and would greatly underestimate the time required to reach a safe therapeutic concentration of the drug. |
| Databáze: | OpenAIRE |
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