Pharmacokinetics of an Immediate-Release Oral Formulation of Fampridine (4-Aminopyridine) in Normal Subjects and Patients with Spinal Cord Injury

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‐r...

Full description

Saved in:
Bibliographic Details
Published in:Journal of clinical pharmacology 2003-04, Vol.43 (4), p.379-385
Main Authors: Hayes, K. C., Katz, M. A., Devane, J. G., Hsieh, J. T. C., Wolfe, D. L., Potter, P. J., Blight, A. R.
Format: Article
Language:English
Subjects:
4-aminopyridine
4-Aminopyridine - administration & dosage
4-Aminopyridine - adverse effects
4-Aminopyridine - pharmacokinetics
Administration, Oral
Adult
Area Under Curve
Biological and medical sciences
Biological Availability
Chromatography, High Pressure Liquid
Dose-Response Relationship, Drug
Double-Blind Method
Fampridine
Female
Half-Life
Humans
Male
Medical sciences
Miscellaneous
Neuropharmacology
pharmacokinetics
Pharmacology. Drug treatments
Potassium Channel Blockers - administration & dosage
Potassium Channel Blockers - adverse effects
Potassium Channel Blockers - pharmacokinetics
Spinal Cord Injuries - metabolism
Spinal cord injury
Time Factors
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 tmax ∼1 hour for both groups; tmax was independent of dose. Cmax and AUC0‐∞ were linearly related to dose, and t1/2 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.
ISSN:0091-2700
1552-4604
DOI:10.1177/0091270003251388