Multiple‐Dose, Linear, Dose‐Proportional Pharmacokinetics of Retigabine in Healthy Volunteers

@article{Ferron2002MultipleDoseLD,
  title={Multiple‐Dose, Linear, Dose‐Proportional Pharmacokinetics of Retigabine in Healthy Volunteers},
  author={G{\'e}raldine M. Ferron and Jeffrey Paul and Richard J. Fruncillo and Lyette S Richards and Norbert G Knebel and John Getsy and Steven Troy},
  journal={The Journal of Clinical Pharmacology},
  year={2002},
  volume={42}
}
  • G. FerronJ. Paul S. Troy
  • Published 1 February 2002
  • Medicine, Biology
  • The Journal of Clinical Pharmacology
Retigabine, a first‐in‐class selective M‐current potassium channel opener, is a novel antiepileptic compound currently in clinical development. The purpose of this randomized placebo‐controlled study was to assess retigabine oral safety and pharmacokinetics in healthy male volunteers (N = 45). Subjects received one dose on day 1 and doses every 12 hours for the next 14 days. Fixed doses were given to the first four groups (200, 400, 500, and 600 mg per day). Titrated doses were given to group 5… 

Lack of pharmacokinetic interaction between retigabine and phenobarbitone at steady-state in healthy subjects.

No dosage adjustment is likely to be necessary when retigabine and phenobarbitone are coadministered to patients, and no clinically relevant changes were observed in the electrocardiograms, vital signs or laboratory measurements.

Pharmacokinetic interaction between retigabine and lamotrigine in healthy subjects

The induction of LTG clearance due to retigabine was unexpected since RGB did not show enzyme induction in various other drug–drug interaction studies, and RGB and LTG exhibit a modest pharmacokinetic interaction on each other.

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Randomized, double-blind, placebo-controlled trial of ezogabine (retigabine) in partial epilepsy

This study demonstrates that EZG(RTG) 1,200 mg/day is effective as add-on therapy for reducing seizure frequency in patients with drug-resistant partial-onset seizures.

Lack of effect of ezogabine/retigabine on the pharmacokinetics of digoxin in healthy individuals: results from a drug–drug interaction study

Co-administration of EZG/RTG across the therapeutic range resulted in small, non-dose-dependent and non-clinically relevant increases in digoxin systemic exposure, suggesting that digoxin dose adjustment is not necessary.

Retigabine: in partial seizures.

When used as adjunctive therapy in patients with partial seizures, retigabine 600-1200 mg/day (200-400 mg three times daily) was associated with significant linear dose-dependent reductions in monthly seizure frequency compared with placebo in a large 16-week randomised phase II trial.

Efficacy of Retigabine in Adjunctive Treatment of Partial Onset Seizures in Adults

  • M. Y. Splinter
  • Medicine, Biology
    Journal of central nervous system disease
  • 2013
Retigabine has been shown to have efficacy when used as adjunctive therapy in partial-onset seizures, and has less drug interactions than many other anticonvulsants because it is not metabolized through the P-450 system.
...

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