Pharmacokinetics of vigabatrin following single and multiple oral doses in normal volunteers
| Autor: | Neil M. Sussman, Kelly K. Antony, John F. Hoke, Lianng Yuh, James M. Elberfeld, Richard A. Okerholm |
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| Rok vydání: | 1993 |
| Předmět: |
Adult
Male genetic structures Urinalysis Adolescent Metabolic Clearance Rate medicine.medical_treatment Administration Oral Pharmacology Vigabatrin Drug Administration Schedule Pharmacokinetics Oral administration medicine Humans Pharmacology (medical) Dosing Adverse effect Aminocaproates medicine.diagnostic_test business.industry Half-life Anticonvulsant Anticonvulsants business medicine.drug Half-Life |
| Zdroj: | Journal of clinical pharmacology. 33(5) |
| ISSN: | 0091-2700 |
| Popis: | The pharmacokinetics of vigabatrin were investigated after single and multiple oral doses in two groups of 24 healthy male volunteers. Vigabatrin was well tolerated by the volunteers; headache was the most frequently reported adverse event. There were no clinically remarkable changes in serum chemistry, urinalysis, or hematology attributable to vigabatrin. For the single-dose study, a stepwise linear contrast method was used to assess dose proportionality. The results showed that vigabatrin exhibited dose linear pharmacokinetics after single oral doses ranging from 0.5 to 4.0 g. Slight changes in the terminal phase half-life and renal clearance were evident in the higher dosage groups. These changes with increasing dose of vigabatrin were relatively minor and not considered to be clinically important. Evaluation of the multiple-dose pharmacokinetics indicated that vigabatrin exhibited dose linearity over the range of 0.5 to 2.0 g administered every 12 hours. The terminal phase half-life and renal clearance of vigabatrin during multiple dosing were consistent with that after single doses. During multiple dosing, steady-state concentrations of vigabatrin were reached on the second day of dosing, and drug accumulation was minimal. |
| Databáze: | OpenAIRE |
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