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...

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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
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creator Hayes, K. C.
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description 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.
doi_str_mv 10.1177/0091270003251388
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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
title Pharmacokinetics of an Immediate-Release Oral Formulation of Fampridine (4-Aminopyridine) in Normal Subjects and Patients with Spinal Cord Injury
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