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Pharmacokinetics of an Immediate‐Release Oral Formulation of Fampridine (4‐Aminopyridine) in Normal Subjects and Patients with Spinal Cord Injury
Author(s) -
Hayes K. C.,
Katz M. A.,
Devane J. G.,
Hsieh J. T. C.,
Wolfe D. L.,
Potter P. J.,
Blight A. R.
Publication year - 2003
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270003251388
Subject(s) - cmax , pharmacokinetics , 4 aminopyridine , spinal cord injury , high performance liquid chromatography , oral administration , medicine , plasma concentration , spinal cord , anesthesia , chemistry , pharmacology , chromatography , potassium channel , psychiatry
Plasma concentration profiles of the K + channel‐blocking compound Fampridine were obtained from (1) control subjects ( n = 6) following oral administration of doses of 10, 15, 20, and 25 mg and (2) patients with spinal cord injury (SCI) ( n = 11) following a single oral dose of 10 mg of an immediate‐release formulation. Plasma concentrations were determined using a reversed‐phase ion‐pair high‐performance liquid chromatography (HPLC) assay with ultraviolet light detection employing liquid extraction. The drug was rapidly absorbed with a t max ∼1 hour for both groups; t max was independent of dose. C max and AUC 0‐∞ were linearly related to dose, and t 1/2 was 3 to 4 hours for both groups. There were no obvious differences in the (10‐mg) plasma concentration profiles between control subjects and SCI patients. The drug was well tolerated, with only mild and transient side effects of light‐headedness, dysesthesias, and dizziness.