Retigabin 2025-09-26 11:18:51

Clinical summary of the Retigabin

Clinical Summary of Retigabine (Ezogabine)

Introduction

Retigabine (also known as ezogabine) is a first-in-class antiepileptic drug (AED) approved for the adjunctive treatment of partial-onset seizures in adults. Its unique mechanism—modulation of neuronal potassium channels—sets it apart from other AEDs. Despite initial promise and regulatory approvals in both Europe and the United States, its clinical use was discontinued in 2017 due to serious adverse effects. This summary provides a comprehensive overview of retigabine’s pharmacology, efficacy, safety, clinical trial data, and its ultimate clinical fate.

Pharmacology

Mechanism of Action

Retigabine acts primarily as an opener of neuronal voltage-gated potassium channels of the KCNQ (Kv7.2–7.5) family, stabilizing the open state and enhancing the M-current. This hyperpolarizes neuronal membranes, reduces excitability, and suppresses epileptiform activity (Blackburn-Munro et al., 2005) (Czuczwar et al., 2010) (Medical Dialogues, 2022). Additionally, retigabine may enhance GABAergic neurotransmission via GABA_A receptors and has weak inhibitory effects on sodium and calcium channels (Czuczwar et al., 2010).

Pharmacokinetics

Bioavailability: Approximately 50–60% after oral administration.
Time to peak plasma concentration (Tmax): 0.5–2 hours.
Volume of distribution: 2–3 L/kg.
Protein binding: 60–80%.
Metabolism: Undergoes extensive hepatic N-glucuronidation (major) and N-acetylation (minor). Cytochrome P450 enzymes are not involved.
Major metabolites: N-glucuronides (inactive) and N-acetyl metabolite (NAMR, less potent than parent drug).
Elimination half-life: Mean ~8 hours (range 6–11 hours).
Excretion: Primarily renal—~85% via urine (36% unchanged, 18% as NAMR, 24% as N-glucuronides); ~14% via feces (Wikipedia, 2025) (Medical Dialogues, 2022).

Clinical Efficacy

Indication

Retigabine was approved as an adjunctive therapy for adults (≥18 years) with partial-onset seizures, with or without secondary generalization, who were refractory to other AEDs (Harris & Murphy, 2011) (Martyn-St James et al., 2012).

Key Clinical Trials

Three pivotal randomized, double-blind, placebo-controlled trials evaluated retigabine as adjunctive therapy:

| Study | Sample Size | Doses (mg/day) | Median % Seizure Reduction vs. Placebo | 50% Responder Rate vs. Placebo |
|------------------------|-------------|---------------|----------------------------------------|-------------------------------|
| Porter et al. (2007b) | n = 396 | 600/900/1200 | 23.4 / 29.3 / 35.2 (p<0.001) | 23.2 / 31.6 / 33.0 |
| Brodie et al. (RESTORE 2, 2010) | n = 538 | 600/900 | 27.9 / 39.9 (p=0.007, <0.001) | 31.5 / 39.3 |
| French et al. (RESTORE 1, 2011) | n = 305 | 1200 | 44.3 (p<0.001) | 44.4 |

Placebo groups had median reductions in seizure frequency ranging from 5.1% to 17.5% and responder rates from 15.6% to 18.9%.
Dose-response relationship: Higher doses led to greater efficacy (Harris & Murphy, 2011).

Meta-Analytic Evidence

A systematic review and network meta-analysis of 20 trials (including 1,242 retigabine patients) found that retigabine had similar risks and benefits to other newer AEDs (e.g., eslicarbazepine, lacosamide, tiagabine, zonisamide, pregabalin) as adjunctive therapy for refractory partial-onset seizures (Martyn-St James et al., 2012).

Responder rate (≥50% reduction in seizures): No significant difference compared to other AEDs except for pregabalin (OR 0.65, 95% CrI 0.41–0.96; favoring pregabalin).
Seizure freedom, adverse event withdrawals: Comparable to other AEDs.
Limitations: Heterogeneity in dosing, patient populations, short trial durations, and few head-to-head comparisons.

Safety and Tolerability

Common Adverse Effects

Adverse effects reported in ≥10% of subjects included:

Dizziness: 14.6–40.5%
Somnolence: 20.3–31.4%
Fatigue: 15.7–16.2%
Confusion: 12.3–14.4%
Headache: 12.4–14.2%
Nausea: 6.4–10.5%
Speech disorder: 8.5–12.4%
Abnormal gait, tremor, blurred vision, memory impairment, urinary tract infection also observed (Harris & Murphy, 2011).

Unique and Serious Adverse Effects

Urinary retention and bladder dysfunction: Retigabine can cause dose-related urinary retention, dysuria, and hesitation, likely due to its effect on peripheral Kv7 channels (Ciliberto et al., 2012). FDA review highlighted this as a significant concern.
Skin and retinal discoloration: Blue skin and retinal pigmentation, potentially irreversible, were observed, especially with long-term use.
Other: Chromaturia (discoloration of urine), psychiatric effects (e.g., confusion, hallucinations).

Discontinuation and Regulatory Status

Due to these adverse effects—particularly skin and retinal pigmentation and urinary retention—retigabine was withdrawn from the market in 2017 (IUPHAR Guide to Pharmacology, 2021).

Dosage and Administration

Initial dose: 300 mg/day (100 mg three times daily).
Titration: Increase by 150 mg/day (50 mg tid) at weekly intervals.
Target dose: 600–1200 mg/day, divided into three doses, depending on response and tolerability.
Dose adjustments: Required for renal impairment; lower starting and maximum doses recommended (Medical Dialogues, 2022).

Drug Interactions

Minimal CYP involvement: Low potential for pharmacokinetic drug–drug interactions.
Lamotrigine: May reduce retigabine clearance and increase metabolism of lamotrigine.
Other AEDs: No significant interactions with valproic acid, topiramate, phenytoin, or carbamazepine.
Oral contraceptives: No clinically significant interactions (Harris & Murphy, 2011).

Clinical Utility and Comparisons

Efficacy Compared to Other AEDs

Effectiveness: Comparable to other new-generation AEDs in terms of responder rate and seizure freedom.
Withdrawal rates: Higher than eslicarbazepine acetate (OR 1.91, CrI 1.18–2.89).
Somnolence: Higher incidence than tiagabine (OR 2.38, CrI 1.03–7.14).
Pregabalin: Lower responder rate compared to pregabalin (Martyn-St James et al., 2012).

Place in Therapy

Retigabine was considered an option for adults with refractory partial-onset seizures when other treatments had failed. Its unique mechanism offered an alternative for patients unresponsive to other AEDs. However, safety concerns limited its use and led to its discontinuation.

Conclusion

Retigabine was a novel antiepileptic drug with a unique potassium-channel opening mechanism and demonstrated efficacy as adjunctive therapy in refractory partial-onset seizures. While it provided seizure reduction comparable to other modern AEDs, significant safety concerns—especially urinary retention, skin discoloration, and retinal pigmentation—ultimately outweighed its benefits, leading to market withdrawal. The experience with retigabine highlights both the potential and the challenges of targeting new ion channel mechanisms in epilepsy.

References

REFERENCES

Retigabine - Wikipedia - last accessed: 2025-09-26

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC - last accessed: 2025-09-26

retigabine | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY - last accessed: 2025-09-26

Retigabine: the newer potential antiepileptic drug - PubMed - last accessed: 2025-09-26

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - PubMed - last accessed: 2025-09-26

Clinical utility, safety, and tolerability of ezogabine (retigabine) in the treatment of epilepsy - PMC - last accessed: 2025-09-26

Retigabine : Indications, Uses, Dosage, Drugs Interactions, Side effects - last accessed: 2025-09-26

Retigabine: chemical synthesis to clinical application - PubMed - last accessed: 2025-09-26

Sources used

QUERY: Retigabine AND clinical summary

Practice guideline update summary: Efficacy and tolerability of the new antiepileptic drugs II: Treatment-resistant epilepsy: Report of the Guideline Development, Dissemination, and Implementation Subcommittee of the American Academy of Neurology and the American Epilepsy Society.
Neurology. 2017/3/2; Impact Factor: 4.57, Quartile: Q1
DOI: 10.1212/WNL.0000000000005756
PMID: 29898974
Abstract
To update the 2004 American Academy of Neurology guideline for managing treatment-resistant (TR) epilepsy with second- and third-generation antiepileptic drugs (AEDs).
2004 criteria were used to systemically review literature (January 2003 to November 2015), classify pertinent studies according to the therapeutic rating scheme, and link recommendations to evidence strength.
Forty-two articles were included.
The following are established as effective to reduce seizure frequency (Level A): immediate-release pregabalin and perampanel for TR adult focal epilepsy (TRAFE); vigabatrin for TRAFE (not first-line treatment); rufinamide for Lennox-Gastaut syndrome (LGS) (add-on therapy). The following should be considered to decrease seizure frequency (Level B): lacosamide, eslicarbazepine, and extended-release topiramate for TRAFE (ezogabine production discontinued); immediate- and extended-release lamotrigine for generalized epilepsy with TR generalized tonic-clonic (GTC) seizures in adults; levetiracetam (add-on therapy) for TR childhood focal epilepsy (TRCFE) (1 month-16 years), TR GTC seizures, and TR juvenile myoclonic epilepsy; clobazam for LGS (add-on therapy); zonisamide for TRCFE (6-17 years); oxcarbazepine for TRCFE (1 month-4 years). The text presents Level C recommendations. AED selection depends on seizure/syndrome type, patient age, concomitant medications, and AED tolerability, safety, and efficacy. This evidence-based assessment informs AED prescription guidelines for TR epilepsy and indicates seizure types and syndromes needing more evidence. A recent Food and Drug Administration (FDA) strategy allows extrapolation of efficacy across populations; therefore, for focal epilepsy, eslicarbazepine and lacosamide (oral only for pediatric use) as add-on or monotherapy in persons ≥4 years of age and perampanel as monotherapy received FDA approval.

QUERY: Retigabine AND clinical trial

Effect of Ezogabine on Cortical and Spinal Motor Neuron Excitability in Amyotrophic Lateral Sclerosis: A Randomized Clinical Trial.
JAMA neurology. 2020/11/24; Impact Factor: 11.58, Quartile: Q1
DOI: 10.1001/jamaneurol.2020.4300
PMID: 33226425
Abstract
Amyotrophic lateral sclerosis (ALS) is a progressive neurodegenerative disease of the motor nervous system. Clinical studies have demonstrated cortical and spinal motor neuron hyperexcitability using transcranial magnetic stimulation and threshold tracking nerve conduction studies, respectively, although metrics of excitability have not been used as pharmacodynamic biomarkers in multi-site clinical trials.
To ascertain whether ezogabine decreases cortical and spinal motor neuron excitability in ALS.
This double-blind, placebo-controlled phase 2 randomized clinical trial sought consent from eligible participants from November 3, 2015, to November 9, 2017, and was conducted at 12 US sites within the Northeast ALS Consortium. Participants were randomized in equal numbers to a higher or lower dose of ezogabine or to an identical matched placebo, and they completed in-person visits at screening, baseline, week 6, and week 8 for clinical assessment and neurophysiological measurements.
Participants were randomized to receive 600 mg/d or 900 mg/d of ezogabine or a matched placebo for 10 weeks.
The primary outcome was change in short-interval intracortical inhibition (SICI; SICI-1 was used in analysis to reflect stronger inhibition from an increase in amplitude) from pretreatment mean at screening and baseline to the full-dose treatment mean at weeks 6 and 8. The secondary outcomes included levels of cortical motor neuron excitability (including resting motor threshold) measured by transcranial magnetic stimulation and spinal motor neuron excitability (including strength-duration time constant) measured by threshold tracking nerve conduction studies.
A total of 65 participants were randomized to placebo (23), 600 mg/d of ezogabine (23), and 900 mg/d of ezogabine (19 participants); 45 were men (69.2%) and the mean (SD) age was 58.3 (8.8) years. The SICI-1 increased by 53% (mean ratio, 1.53; 95% CI, 1.12-2.09; P = .009) in the 900-mg/d ezogabine group vs placebo group. The SICI-1 did not change in the 600-mg/d ezogabine group vs placebo group (mean ratio, 1.15; 95% CI, 0.87-1.52; P = .31). The resting motor threshold increased in the 600-mg/d ezogabine group vs placebo group (mean ratio, 4.61; 95% CI, 0.21-9.01; P = .04) but not in the 900-mg/d ezogabine group vs placebo group (mean ratio, 1.95; 95% CI, -2.64 to 6.54; P = .40). Ezogabine caused a dose-dependent decrease in excitability by several other metrics, including strength-duration time constant in the 900-mg/d ezogabine group vs placebo group (mean ratio, 0.73; 95% CI, 0.60 to 0.87; P < .001).
Ezogabine decreased cortical and spinal motor neuron excitability in participants with ALS, suggesting that such neurophysiological metrics may be used as pharmacodynamic biomarkers in multisite clinical trials.
ClinicalTrials.gov Identifier: NCT02450552.

QUERY: Retigabine AND efficacy AND safety

Update on Antiepileptic Drugs 2019.
Continuum (Minneapolis, Minn.). 2019/3/29; Impact Factor: 2.52, Quartile: Q1
DOI: 10.1212/CON.0000000000000715
PMID: 30921021
Abstract
This article is an update from the article on antiepileptic drug (AED) therapy published in the last Continuum issue on epilepsy and is intended to cover the vast majority of agents currently available to the neurologist in the management of patients with epilepsy. Treatment of epilepsy starts with AED monotherapy. Knowledge of the spectrum of efficacy, clinical pharmacology, and modes of use for individual AEDs is essential for optimal treatment for epilepsy. This article addresses AEDs individually, focusing on key pharmacokinetic characteristics, indications, and modes of use.
Since the previous version of this article was published, three new AEDs, brivaracetam, cannabidiol, and stiripentol, have been approved by the US Food and Drug Administration (FDA), and ezogabine was removed from the market because of decreased use as a result of bluish skin pigmentation and concern over potential retinal toxicity.Older AEDs are effective but have tolerability and pharmacokinetic disadvantages. Several newer AEDs have undergone comparative trials demonstrating efficacy equal to and tolerability at least equal to or better than older AEDs as first-line therapy. The list includes lamotrigine, oxcarbazepine, levetiracetam, topiramate, zonisamide, and lacosamide. Pregabalin was found to be less effective than lamotrigine. Lacosamide, pregabalin, and eslicarbazepine have undergone successful trials of conversion to monotherapy. Other newer AEDs with a variety of mechanisms of action are suitable for adjunctive therapy. Most recently, the FDA adopted a policy that a drug's efficacy as adjunctive therapy in adults can be extrapolated to efficacy in monotherapy. In addition, efficacy in adults can be extrapolated for efficacy in children 4 years of age and older. Both extrapolations require data demonstrating that an AED has equivalent pharmacokinetics between its original approved use and its extrapolated use. In addition, the safety of the drug in pediatric patients has to be demonstrated in clinical studies that can be open label. Rational AED combinations should avoid AEDs with unfavorable pharmacokinetic interactions or pharmacodynamic interactions related to mechanism of action.
Knowledge of AED pharmacokinetics, efficacy, and tolerability profiles facilitates the choice of appropriate AED therapy for patients with epilepsy.

Web Sources

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf

ville , R McCool , S Duffy , J Cooper , P Hugel , and PW Lane . Review published: 2012 . CRD summary This review concluded that retigabine provided similar risks and benefits, compared with the other selected anti-epileptic drugs, as additional therapy, for patients with partial-onset seizures, with or without secondary generalisation, but the limitations of the analyses should be considered. These conclusions appear to be reliable. Authors' objectives To evaluate the efficacy and tolerability of retigabine, compared with selected anti-epileptic drugs. Searching Eighteen electronic databases (including MEDLINE, EMBASE, DARE, and HTA database), trial registries, guideline collections, or regulatory authority records, were searched, without language restrictions, up to June 2010. Unpublished data were provided by the manufacturer of retigabine (GlaxoSmithKline). Study selection Parallel or crossover randomised controlled trials of additional anti-epileptic drug therapy were eligible for inclusion if they were of adults (18 years old or older), with partial-onset epileptic seizures, who had failed to respond adequately to previous anti-epileptic drugs. The treatment had to be at target dose (maintenance phase) for eight weeks or more, and the prospective baseline period had to be four weeks or more. Trials had to report the change in seizure frequency and treatment withdrawal, as outcomes. The selected anti-epileptic drugs for comparison were eslicarbazepine acetate, lacosamide, tiagabine, zonisamide and pregabalin. All the included trials were placebo controlled and most evaluated more than one dose of retigabine. The authors did not state how many reviewers selected the trials. Assessment of study quality The quality of the included trials was assessed for appropriateness of randomisation, concealment of treatment allocation, comparability of groups at baseline, blinding procedures, unexpected imbalances in drop-outs, reporting of measured outcomes, and inclusion of an intent-to-treat analysis. The authors did not state how many reviewers performed the assessment. Data extraction The proportions of responders (defined as patients with 50% or greater reduction in seizure frequency), seizure-free patients, withdrawals, and patients reporting anti-epileptic drug-related adverse events (ataxia, dizziness, fatigue, nausea, or somnolence), were extracted from each study to calculate

retigabine | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY

k.github.io/ ) Summary Biological activity Clinical data References Structure Similar ligands No information available. Summary of Clinical Use Retigabine was approved to treat intractable partial-onset epileptic seizures. Use of retigabine was discontinued in 2017 due to serious side-effects including urinary retention, blue skin, and retinal discoloration. The poor selectivity of retigabine among K v 7.2-K v 7.5 channels, and issues around its metabolic degradation products are considered to contribute to these adverse events. Channel activators with improved selectivity for K v 7.2/K v 7.3 are being developed and investigated [ 3 ]. Mechanism Of Action and Pharmacodynamic Effects Retigabine acts as a neuronal voltage activated potassium channel opener but may also affect inhibitory GABA neurotransmission by the GABA A receptor. See the DrugBank link for further details. Clinical Trials Clinical Trial ID Title Type Source Comment References NCT02450552 Clinical Trial of Ezogabine (Retigabine) in ALS Subjects Phase 2 Interventional Massachusetts General Hospital 7 External links For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) Contact us Privacy and Cookie Policy Sponsors list This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License

Retigabine - Wikipedia

oxin . [ 18 ] Researchers hoped this wide-ranging activity would translate to studies in humans as well. [ 8 ] Clinical trials [ edit ] In a double-blind , randomized, placebo-controlled Phase II clinical trial, retigabine was added to the treatment regimen of 399 participants with partial seizures that were refractory to therapy with other antiepileptic drugs. The frequency with which seizures occurred was significantly reduced (by 23 to 35%) in participants receiving retigabine, and approximately one fourth to one third of participants had their seizure frequency reduced by more than 50%. Higher doses were associated with a greater response to treatment. [ 8 ] [ 10 ] [ 9 ] A Phase II trial meant to assess the safety and efficacy of retigabine for treating postherpetic neuralgia was completed in 2009, but failed to meet its primary endpoint . Preliminary results were reported by Valeant as "inconclusive". [ 19 ] Regulatory approval [ edit ] The U.S. Food and Drug Administration accepted Valeant's New Drug Application for retigabine on December 30, 2009. [ 20 ] The FDA Peripheral and Central Nervous System Drugs Advisory Committee met on August 11, 2010, to discuss the process and unanimously recommended approval of Potiga for the intended indication (add-on treatment of partial seizures in adults). [ 21 ] [ 22 ] However, the possibility of urinary retention as an adverse effect was considered a significant concern, and the panel's members recommended that some sort of monitoring strategy be used to identify patients at risk of bladder dysfunction. [ 21 ] Potiga was approved by the FDA on June 10, 2010, but did not become available on the U.S. market until it had been scheduled by the Drug Enforcement Administration . [ 12 ] In December 2011, the U.S. Drug Enforcement Administration (DEA) placed the substance into Schedule V of the Controlled Substances Act (CSA), the category for substances with a comparatively low potential for abuse. This became effective 15 December 2011. [ 23 ] Name [ edit ] The International Nonproprietary Name "retigabine" was initially published as being under consideration by WHO in 1996. [ 24 ] This was later adopted as the recommended International Nonproprietary Name (rINN) for the drug, and, in 2005 or 2006, the USAN Council —a program sponsored by the American Medical Association, the United States Pharmacopeial Convention

Retigabine - Wikipedia

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf

, for any reason, than eslicarbazepine acetate (OR 1.91, CrI 1.18 to 2.89), and a higher incidence of somnolence than tiagabine (OR 2.38, CrI 1.03 to 7.14). The funnel plot inspection was not informative as there were too few trials. Authors' conclusions Retigabine provided similar risks and benefits, compared with the other selected anti-epileptic drugs, as additional therapy, for patients with partial-onset seizures, with or without secondary generalisation, but the limitations of the analyses should be considered. CRD commentary This review appeared to be carefully conducted, with comprehensive searches for relevant evidence and largely reproducible methods for selecting, assessing and combining the retrieved data. The authors pointed out several limitations to their analysis, which were statistical heterogeneity was present for some comparisons; where it was not present, the trials varied in their dosing schedules and participants (age, gender, severity, or concomitant treatment); only a few trials were available for each drug; publication bias could not be excluded for the non-retigabine evidence; most trials had short treatment periods; and not all anti-epileptic drugs were compared. Trial quality was assessed, but the results were not incorporated in the synthesis. The authors conclusions that retigabine was similar to the other included anti-epileptic drugs, but the limitations should be considered, appear to be reliable. Implications of the review for practice and research Practice : The authors did not state any implications for practice. Research : The authors stated that their indirect comparisons should be considered with the direct evidence, and that head-to-head randomised controlled trials, should compare different anti-epileptic drugs for specific patient populations. Funding Funded by GlaxoSmithKline, manufacturer of retigabine. Bibliographic details Martyn-St James M, Glanville J, McCool R, Duffy S, Cooper J, Hugel P, Lane PW. The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison. Seizure 2012; 21(9): 665-678. [ PubMed : 22902288 ] Original Paper URL http://www.seizure-journal.com/article/S1059-1311(12)00188-4/

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

retigabine treatment on vital signs, laboratory measurements (besides the liver enzymes discussed above), electrocardiogram findings (particularly QTc interval), neurologic examinations, or ophthalmologic examinations in the clinical trials discussed [ French et al. 2011 ; Brodie et al. 2010 ; Porter et al. 2007b ]. Contraindications and precautions The clinical trials discussed in this review do not specify any contraindications or precautions for the use of retigabine. The report from the tenth Eilat conference (EILAT X) indicates concern for dose-related bladder dysfunction including dysuria and urinary hesitation [ Bialer et al. 2010 ]. In August 2010, the FDA’s Peripheral and Central Nervous System Drugs Advisory Committee expressed concern over the potential for urinary retention with retigabine [ Lowry, 2010 ]. While the advisory committee believes the urinary retention may be minimized with patient monitoring, it is not known what this monitoring should entail. Dosage and administration In the clinical trials discussed in this review, retigabine was administered orally at a dose of 600–1200 mg/day in three evenly divided doses [ French et al. 2011 ; Brodie et al. 2010 ; Porter et al . 2007b ]. The initial dosage was 300 mg/day (100 mg administered three times daily), which was increased by 150 mg/day (50 mg three times daily) to the target dose. Doses were administered approximately 8 h apart. Conclusion Retigabine (Trobalt ® ) was approved by the EMEA on 28 March 2011 as adjunctive treatment of partial-onset seizures with or without secondary generalization in adults aged 18 years and above with epilepsy. On 10 June 2011, the FDA approved retigabine (USAN, ezogabine, Potiga ® ) for the adjunctive treatment of partial-onset seizures in patients aged 18 years and older [ FDA, 2011 ]. Based on the evidence of retigabine’s effectiveness for the adjunctive treatment of partial-onset seizures in the clinical trials described here, it appears that the drug consistently reduces seizure frequency for this patient population. This, in addition to the drug’s novel mechanism of activating the KCNQ2/KCNQ3 subunits of the potassium channels and a fairly benign side-effect profile, makes retigabine an attractive alternative to other approved AED

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

Retigabine : Indications, Uses, Dosage, Drugs Interactions, Side effects

Medical Universities News Nursing education News Paramedical Education News Study Abroad Industry Health Investment News Health Startup News Medical Devices News Pharma News CDSCO (Central Drugs Standard Control Organisation) News Pharmacy Education News Industry Perspective Overview Mechanism of Action How To Use Uses Benfits Indications Method of Administration Dosage Strengths Dosage Forms Dietary Restrictions Contraindications Warnings and Precautions for using Adverse Reactions Overdosage Clinical Pharmacology Clinical Studies Authored by Reviewed by References ENG हिंदी Retigabine Indications, Uses, Dosage, Drugs Interactions, Side effects Overview Retigabine Medicine Type : Allopathy Prescription Type: Prescription Required Approval : DCGI (Drugs Controller General of India) Schedule Schedule H Pharmacological Class: Potassium channel opener, Therapy Class: Antiepileptic Drug, About Retigabine Retigabine is an Antiepileptic drug belonging to the potassium channel opener. Retigabine is used in the treatment of Partial-onset seizures. Retigabine is rapidly absorbed and distributed, with an absolute oral bioavailability of 60%. Retigabine is metabolized exclusively via phase II hepatic N-glucuronidation and acetylation. N-glucuronidation is the primary metabolic pathway of the two and forms two major N-glucuronide metabolites.It is excreted via Urine (85%, 36% of total dose as unchanged drug, 18% of total dose as NAMR) and feces (14%, 3% of total dose as unchanged drug) The Tmax of Retigabine was about 0.5 to 2 hours. The common side effects are dizziness, drowsiness, headache, weakness, Nausea, strong irregular heartbeat, swelling, and dizziness upon standing. Retigabine is available in dosage forms, such as tablets. Retigabine is available in Europe, Japan, China, and India. Mechanism of Action of Retigabine Retigabine binds the KCNQ (Kv7.2-7.5) voltage-gated potassium channels, thereby stabilizing the channels in the open formation and enhancing the M-current. As a result, neuronal excitability is regulated, and epileptiform activity is suppressed. In addition

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf Warning: The NCBI web site requires JavaScript to function. more... An official website of the United States government Here's how you know The .gov means it's official. Federal government websites often end in .gov or .mil. Before
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The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - PubMed

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Retigabine - Wikipedia

Retigabine - Wikipedia Jump to content Main menu Main menu move to sidebar hide Navigation Main page Contents Current events Random article About Wikipedia Contact us Contribute Help Learn to edit Community portal Recent changes Upload file Special pages Search Search Appearance Donate Create account Log in Personal tools Donate Create account Log in Pages for logged out editors learn more Contributions Talk Contents move to sidebar hide (Top) 1 Adverse effects 2 Interactions 3 Pharmacology Toggle Pharmacology subsection 3.1 Mechanism of action 3.2 Pharmacokinetics 4 History Toggle History subsection 4.1 Clinical trials 4.2 Regulatory approval 5 Name 6 References 7 Further reading Toggle the table of contents Retigabine 11 languages العربية Deutsch Español فارسی Français Polski Română Српски / srpski Srpskohrvatski / српскохрватски Tiếng Việt 中文 Edit links Article Talk English Read Edit View history Tools Tools move to sidebar hide Actions Read Edit View history General What links here Related changes Upload file Permanent link Page information Cite this page Get shortened URL Download QR code Print/export Download as PDF Printable version In other projects Wikimedia Commons Wikidata item Appearance move to sidebar hide From Wikipedia, the free encyclopedia Anticonvulsant, which works as a potassium-channel opener Pharmaceutical compound Retigabine Clinical data Trade names Trobalt, Potiga Other names D-23129, ezogabine ( USAN US ) AHFS / Drugs.com Professional Drug Facts MedlinePlus a612028 License data EU EMA : by INN US FDA : Ezogabine Routes of administration By mouth ATC code N03AX21 ( WHO ) Legal status Legal status AU : S4 (Prescription only) UK : POM (Prescription only) US : Schedule V Pharmacokinetic data Bioavailability 60% Protein binding 60–80% Metabolism Liver glucuronidation and acetylation . CYP not involved Elimination half-life 8 hours (mean), range: 7–11 hours [ 1 ] Excretion Kidney (84%) Identifiers IUPAC name Ethyl N -[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate

Retigabine - Wikipedia

Clinical utility, safety, and tolerability of ezogabine (retigabine) in the treatment of epilepsy - PMC

Khalil BW, Leroy RF, et al. RESTORE 1/Study 301 Investigators. Randomized double-blind, placebo-controlled trial of ezogabine (retigabine) in partial epilepsy. Neurology. 2011;76(18):1555–1563. doi: 10.1212/WNL.0b013e3182194bd3. [ DOI ] [ PubMed ] [ Google Scholar ] 35. Brodie MJ, Lerche H, Gil-Nagel A, et al. RESTORE 2 Study Group. Efficacy and safety of adjunctive ezogabine (retigabine) in refractory partial epilepsy. Neurology. 2010;75(20):1817–1824. doi: 10.1212/WNL.0b013e3181fd6170. [ DOI ] [ PubMed ] [ Google Scholar ] 36. Porter RJ, Burdette DE, Gil-Nagel A, et al. Retigabine as adjunctive therapy in adults with partial-onset seizures: integrated analysis of three pivotal controlled trials. Epilepsy Res. doi: 10.1016/j.eplepsyres.2012.03.010. Epub April 16, 2012. [ DOI ] [ PubMed ] [ Google Scholar ] 37. Brickel N, Gandhi P, Vanlandingham K, Hammond J, Derossett S. The urinary safety profile and secondary renal effects of retigabine (ezogabine): a first-in-class antiepileptic drug that targets KCNQ (K(v) 7) potassium channels. Epilepsia. 2012;53(4):606–612. doi: 10.1111/j.1528-1167.2012.03441.x. [ DOI ] [ PubMed ] [ Google Scholar ] 38. Ipaveca V, Martirea M, Barreseb V, Taglialatela M, Currò D. KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus. Pharmacol Res. 2011;64(4):397–409. doi: 10.1016/j.phrs.2011.06.016. [ DOI ] [ PMC free article ] [ PubMed ] [ Google Scholar ] 39

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf

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Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

of three phases: a prospective 8-week baseline, 6-week dose titration, and a 12-week maintenance phase. During the 8-week prospective baseline phase, subjects had to experience a minimum of four partial-onset seizures per 28 days while receiving stable doses of one to three AEDs. During the titration phase, the starting dose of 300 mg/day (100 mg every 8 h) was increased by 150 mg/day (50 mg every 8 h) at 1-week intervals, reaching the target dose of 1200 mg/day at week six. A total of 305 subjects were included in the ITT efficacy analysis. The median percentage reduction in 28-day total partial-seizure frequency from baseline and the 50% responder rates for the 18-week treatment period can be found in Table 1 . Adverse events that occurred are addressed in the adverse drug reactions section below. The authors concluded that retigabine is effective as adjunctive therapy for reducing seizure frequency in patients with refractory partial-onset seizures. Adverse drug reactions The adverse effects that occurred in at least 5% of subjects in at least one of the clinical trials discussed are summarized in Table 2 . Table 2. Adverse effects associated with retigabine [ Porter et al. 2007b ; Brodie et al. 2010 ; French et al. 2011 ]. Adverse effects Subjects in trials (%) Abnormal gait 5.6−11.8 Amnesia 5.6 Anxiety 5.2 Asthenia 5.8 Confusion 12.3−14.4 Constipation 5.9 Diplopia 6.1−6.5 Disturbance in attention 5.2−6.4 Dizziness 14.6−40.5 Dysuria 5.2 Fatigue 15.7−16.2 Headache 12.4−14.2 Influenza 7.8 Memory impairment 5.0−7.8 Nausea 6.4−10.5 Somnolence 20.3−31.4 Speech disorder 8.5−12.4 Thinking abnormal 9.0 Tremor 5.3−11.1 Urinary hesitation 5.9 Urinary tract infection 11.8 Vertigo 5.9−9.3 Vision blurred 11.8 Vomiting 5.2 Open in a new tab In the RESTORE 2 trial, chromaturia was reported in one and two subjects in the 600 mg/day

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

Retigabine: the newer potential antiepileptic drug - PubMed

first Saturday The first day The first weekday Which day? Sunday Monday Tuesday Wednesday Thursday Friday Saturday Report format: Summary Summary (text) Abstract Abstract (text) PubMed Send at most: 1 item 5 items 10 items 20 items 50 items 100 items 200 items Send even when there aren't any new results Optional text in email: Save Cancel Create a file for external citation management software Create file Cancel Your RSS Feed Name of RSS Feed: Number of items displayed: 5 10 15 20 50 100 Create RSS Cancel RSS Link Copy Actions Cite Collections Add to Collections Create a new collection Add to an existing collection Name your collection: Name must be less than 100 characters Choose a collection: Unable to load your collection due to an error Please try again Add Cancel Permalink Permalink Copy Display options Display options Format Abstract PubMed PMID Page navigation Title & authors Abstract Publication types MeSH terms Substances Title & authors Abstract Publication types MeSH terms Substances Review Pharmacol Rep Actions Search in PubMed Search in NLM Catalog Add to Search . 2010 Mar-Apr;62(2):211-9. doi: 10.1016/s1734-1140(10)70260-7. Retigabine: the newer potential antiepileptic drug Piotr Czuczwar 1 , Agnieszka Wojtak , Anna Cioczek-Czuczwar , Jolanta Parada-Turska , Ryszard Maciejewski , Stanisław J Czuczwar Affiliations Expand Affiliation 1 Department of Human Anatomy, Medical University, Jaczewskiego 4, PL 20-090 Lublin, Poland. czuczwarsj@yahoo.com PMID: 20508276 DOI: 10.1016/s1734-1140(10)70260-7 Item in Clipboard Review Retigabine: the newer potential antiepileptic drug Piotr Czuczwar et al. Pharmacol Rep . 2010 Mar-Apr . Show details Display options Display options Format Abstract PubMed PMID Pharmacol Rep Actions Search in PubMed Search in NLM Catalog Add to Search . 2010 Mar-Apr;62(2):211-9. doi: 10.1016/s1734-1140(10)70260-7. Authors Piotr Czuczwar 1 , Agnieszka Wojtak , Anna Cioczek

Retigabine: the newer potential antiepileptic drug - PubMed

):211-9. doi: 10.1016/s1734-1140(10)70260-7. Authors Piotr Czuczwar 1 , Agnieszka Wojtak , Anna Cioczek-Czuczwar , Jolanta Parada-Turska , Ryszard Maciejewski , Stanisław J Czuczwar Affiliation 1 Department of Human Anatomy, Medical University, Jaczewskiego 4, PL 20-090 Lublin, Poland. czuczwarsj@yahoo.com PMID: 20508276 DOI: 10.1016/s1734-1140(10)70260-7 Item in Clipboard Cite Display options Display options Format Abstract PubMed PMID Abstract Retigabine represents an antiepileptic drug possessing a completely different mechanism of action when compared to the existing classical and newer antiepileptic drugs. In the therapeutic range, retigabine enhances potassium currents, very likely via destabilization of a closed conformation or stabilization of the open conformation of the potassium Kv7.2-7.3 channels. There are also data indicating that this drug may be a GABA enhancer. Kainate-induced status epilepticus in rats resulted in massive apoptosis in the pyriform cortex and hippocampal area - retigabine inhibited neurodegeneration only in the former brain structure. The metabolism of retigabine has nothing to do with cytochrome P450 enzymes and the drug undergoes glucuronidation and acetylation. Randomized, placebo-controlled multicenter studies have shown that retigabine produced a considerable improvement as an add-on drug in patients with partial drug-resistant epilepsy. The most prominent adverse effects due to retigabine combined with the existing antiepileptic treatment were dizziness, somnolence and fatigue. The preclinical data indicate that this antiepileptic drug may possibly be applied in patients with neuropathic pain and affective disorders. Initial clinical data suggest that retigabine may be also effective in Alzheimer's disease or stroke. PubMed Disclaimer Publication types Review Actions Search in PubMed Search in MeSH Add to Search MeSH terms Animals Actions Search in PubMed Search in MeSH Add to Search Anticonvulsants / pharmacokinetics Actions Search in PubMed Search in MeSH Add to Search Ant

Retigabine: chemical synthesis to clinical application - PubMed

.1111/j.1527-3458.2005.tb00033.x. Authors G Blackburn-Munro 1 , W Dalby-Brown , N R Mirza , J D Mikkelsen , R E Blackburn-Munro Affiliation 1 Department of Pharmacology, NeuroSearch A/S, Pederstrupvej 93, DK-2750 Ballerup, Denmark. gbm@neurosearch.dk PMID: 15867950 PMCID: PMC6741764 DOI: 10.1111/j.1527-3458.2005.tb00033.x Item in Clipboard Full text links Cite Display options Display options Format Abstract PubMed PMID Abstract Retigabine [D23129; N-(2-amino-4-(4-fluorobenzylamino)-phenyl)carbamic acid ethyl ester] is an antiepileptic drug with a recently described novel mechanism of action that involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels. These channels (primarily K(V)7.2/7.3) enable generation of the M-current, a subthreshold K(+) current that serves to stabilize the membrane potential and control neuronal excitability. In this regard, retigabine has been shown to have a broad-spectrum of activity in animal models of electrically-induced (amygdala-kindling, maximal electroshock) and chemically-induced (pentylenetetrazole, picrotoxin, NMDA) epileptic seizures. These encouraging results suggest that retigabine may also prove useful in the treatment of other diseases associated with neuronal hyperexcitability. Neuropathic pain conditions are characterized by pathological changes in sensory pathways, which favor action potential generation and enhanced pain transmission. Although sometimes difficult to treat with conventional analgesics, antiepileptics can relieve some symptoms of neuropathic pain. A number of recent studies have reported that retigabine can relieve pain-like behaviors (hyperalgesia and allodynia) in animal models of neuropathic pain. Neuronal activation within several key structures within the CNS can also be observed in various animal models of anxiety. Moreover, amygdala-kindled rats, which have a lowered threshold for neuronal activation, also display enhanced

Retigabine : Indications, Uses, Dosage, Drugs Interactions, Side effects

ncbi.nlm.nih.gov/pmc/articles/PMC3538493/ References https://go.drugbank.com/drugs/DB09235 https://www.apollopharmacy.in/salt/RETIGABINE https://pubchem.ncbi.nlm.nih.gov/compound/Retigabine #section=MeSH-Pharmacological-Classification https://www.medplusmart.com/product/efnocar-40mg-tab_efno0001 Authored by Parthika Patel Parthika Patel has completed her Graduated B.Pharm from SSR COLLEGE OF PHARMACY and done M.Pharm in Pharmaceutics. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751 Reviewed by Dr JUHI SINGLA Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow Medical college and done MD pharmacology from SGT UNIVERSITY Gurgaon. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751 Published on: 3 Dec 2022 6:04 PM GMT © 2022 All Rights Reserved. Powered By: Hocalwire X We use cookies for analytics, advertising and to improve our site. You agree to our use of cookies by continuing to use our site. To know more, see our Cookie Policy and Cookie Settings. Ok

Clinical utility, safety, and tolerability of ezogabine (retigabine) in the treatment of epilepsy - PMC

Clinical utility, safety, and tolerability of ezogabine (retigabine) in the treatment of epilepsy - PMC Skip to main content An official website of the United States government Here's how you know Here's how you know Official websites use .gov A .gov website belongs to an official
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the contents by NLM or the National Institutes of Health. Learn more: PMC Disclaimer | PMC Copyright Notice Drug Healthc Patient Saf . 2012 Jul 26;4:81–86. doi: 10.2147/DHPS.S28814 Search in PMC Search in PubMed View in NLM Catalog Add to search Clinical utility, safety, and tolerability of ezogabine (retigabine) in the treatment of epilepsy Michael A Ciliberto Michael A Ciliberto 1 Department of Neurology, Washington University School of Medicine, St Louis, MO, USA Find articles by Michael A Ciliberto 1 , Judith LZ Weisenberg Judith LZ Weisenberg 1 Department of Neurology, Washington University School of Medicine, St Louis, MO, USA Find articles by Judith LZ Weisenberg 1 , Michael Wong Michael Wong 1 Department of Neurology, Washington University School of Medicine, St Louis, MO, USA Find articles by Michael Wong 1, ✉ Author information Article notes Copyright and License information 1 Department

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

4588 Parkview Place, St Louis, MO 63110-1088, USA jharris2@stlcop.edu ✉ Julie A. Murphy, PharmD, BCPS Associate Professor of Pharmacy Practice, St Louis College of Pharmacy, St Louis, MO, USA ✉ Corresponding author. Issue date 2011 Nov. © The Author(s) 2011 PMC Copyright notice PMCID: PMC3513894 PMID: 23251762 Abstract Objective The present study reviewed the pharmacology, pharmacokinetics, efficacy, and safety of retigabine (ezogabine), a potential agent for use as adjunctive treatment in refractory partial-onset seizures. Methods A MEDLINE search (1966–May 2011) was conducted using the key words retigabine, ezogabine, D-23129, epilepsy, and anticonvulsant. Bibliographies of all articles retrieved were also reviewed. All studies including humans and published in English with data describing retigabine for the adjunctive treatment of partial-onset seizures were reviewed. Results Retigabine has been shown to interact with the KCNQ2/KCNQ3 subunits of the potassium channels, GABA A receptors, and weakly block sodium and calcium channels. Retigabine is 50–60% bioavailable, metabolized by N-glucuronidation and N-acetylation, 80% protein bound, and has few drug–drug interactions. Recent data suggest that retigabine may have a role as adjunctive treatment for refractory partial-onset seizures. Placebo-controlled trials demonstrated a 23.4–44.3% reduction in seizure frequency with 50% responder rates ranging from 23.2% to 47.0% with varying doses of retigabine. The most common adverse effects, occurring in greater than 10% of subjects in the clinical trials, include abnormal gait, confusion, dizziness, fatigue, headache, nausea, somnolence, speech disorder, tremor, urinary tract infection, and blurred vision. Conclusions Retigabine is a promising agent for adjunctive treatment of refractory partial-onset seizures. Keywords: epilepsy, ezogabine, partial-onset seizures, retigabine Introduction The annual incidence of epilepsy is approximately 40–70 per 100

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf

2012; 21(9): 665-678. [ PubMed : 22902288 ] Original Paper URL http://www.seizure-journal.com/article/S1059-1311(12)00188-4/abstract Indexing Status Subject indexing assigned by NLM MeSH Anticonvulsants /administration & dosage /adverse effects; Carbamates /administration & dosage /adverse effects; Disorders of Excessive Somnolence /chemically induced /epidemiology; Epilepsies, Partial /drug therapy /epidemiology /physiopathology; Humans; Phenylenediamines /administration & dosage /adverse effects; Randomized Controlled Trials as Topic /methods; Treatment Outcome AccessionNumber 12012046228 Database entry date 26/03/2013 Record Status This is a critical abstract of a systematic review that meets the criteria for inclusion on DARE. Each critical abstract contains a brief summary of the review methods, results and conclusions followed by a detailed critical assessment on the reliability of the review and the conclusions drawn. Copyright © 2014 University of York. Bookshelf ID: NBK114414 Share Views PubReader Print View Cite this Page Martyn-St James M, Glanville J, McCool R, et al. The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison. 2012. In: Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews [Internet]. York (UK): Centre for Reviews and Dissemination (UK); 1995-. In this Page CRD summary Authors' objectives Searching Study selection Assessment of study quality Data extraction Methods of synthesis Results of the review Authors' conclusions CRD commentary Implications of the review for practice and research Funding Bibliographic details Original Paper URL Indexing Status MeSH AccessionNumber Database entry date Record Status Similar articles in PubMed Clinical effectiveness, tolerability and cost-effectiveness of newer drugs for epilepsy in adults: a systematic review and economic evaluation. [Health Technol Assess. 2005] Clinical effectiveness, tolerability and cost-effectiveness of newer drugs for epilepsy in adults: a systematic review and economic evaluation. Wilby J, Kainth A, Hawkins N, Epstein D, McIntosh H, McDaid C, Mason A, Golder S, O'M

retigabine | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY

retigabine | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY Home About About The Guide to PHARMACOLOGY About NC-IUPHAR Database Content Contributors Sponsors Citing Linking to us Disclaimer Privacy and Cookie Policy Targets GPCRs Ion channels LGICs VGICs Other channels Nuclear receptors Kinases Catalytic receptors Transporters Enzymes Other protein targets Target search Target search tools BLAST Ligands Ligand list Ligand families Ligand search Diseases Resources Help Tutorial FAQ Terms and symbols Nomenclature guidelines Publications Antibacterials Drug approvals Downloads Download data and reports Web services Slides and posters News Immunopharmacology Meeting 2018 Latest news Hot topics Latest pairings Concise Guide to PHARMACOLOGY Useful links Advanced search Target search Target search tools BLAST Ligand search Pharmacology search Immuno Portal Malaria Portal Home About Help GtoPdb is requesting financial support from commercial users. Please see our sustainability page for more information. Home Ligands retigabine retigabine GtoPdb Ligand ID: 2601 Synonyms: AWD-21360 | D-23129 | ezogabine | Potiga® | Trobalt® | WAY-143841 retigabine is an approved drug (FDA and EMA (2011)) Compound class: Synthetic organic Comment: Retigabine is unique among antiepileptic drugs in that it functions by activating selected voltage-gated potassium channels in the brain ( i.e. K v 7 family channels) [ 4 ] [ 5 ]. Ligand Activity Visualisation Charts These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ View interactive charts of

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

seizures in a dose-dependent manner. Table 1. Summary of placebo-controlled trials for retigabine in partial-onset seizures. Study Sample size Dosage Median reduction inseizure frequency 50% responder rates Porter et al. [2007b] n = 396 Placebo 13.1% 15.6% 600 mg/day 23.4% ( p < 0.001) 23.2% 900 mg/day 29.3% ( p < 0.001) 31.6% ( p = 0.0214) 1200 mg/day 35.2% ( p < 0.001) 33.0% ( p = 0.0214) Brodie et al. [2010] (RESTORE 2) Food and Drug Placebo 15.9% 17.3% Administration population ( n = 538) 600 mg/day 27.9% ( p = 0.007) 31.5% ( p = 0.002) 900 mg/day 39.9% ( p < 0.001) 39.3% ( p < 0.001) European Medicines Placebo 5.1% 18.9% Agency population ( n = 471) 600 mg/day 25.0% ( p = 0.002) 38.6% ( p < 0.001) 900 mg/day 30.9% ( p < 0.001) 47.0% ( p < 0.001) French et al. [2011] (RESTORE 1) n = 305 Placebo 17.5% 17.8% 1200 mg/day 44.3% ( p < 0.001) 44.4% ( p < 0.001) Open in a new tab RESTORE, Retigabine Efficacy and Safety Trials for Partial Onset Epilepsy. The Retigabine Efficacy and Safety Trials for Partial Onset Epilepsy Study 302 (RESTORE 2) was a randomized, double-blind, placebo-controlled, multicenter, parallel-group study that evaluated the efficacy and safety of adjunctive retigabine 600 mg and 900 mg/day, administered at 8-h intervals, in subjects with refractory partial-onset seizures [ Brodie et al. 2010 ]. The study consisted of four phases: a prospective 8-week baseline, 4-week titration, 12-week maintenance, and a 4-

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

Retigabine: chemical synthesis to clinical application - PubMed

day The first weekday Which day? Sunday Monday Tuesday Wednesday Thursday Friday Saturday Report format: Summary Summary (text) Abstract Abstract (text) PubMed Send at most: 1 item 5 items 10 items 20 items 50 items 100 items 200 items Send even when there aren't any new results Optional text in email: Save Cancel Create a file for external citation management software Create file Cancel Your RSS Feed Name of RSS Feed: Number of items displayed: 5 10 15 20 50 100 Create RSS Cancel RSS Link Copy Full text links Wiley Free PMC article Full text links Actions Cite Collections Add to Collections Create a new collection Add to an existing collection Name your collection: Name must be less than 100 characters Choose a collection: Unable to load your collection due to an error Please try again Add Cancel Permalink Permalink Copy Display options Display options Format Abstract PubMed PMID Page navigation Title & authors Abstract References Publication types MeSH terms Substances LinkOut - more resources Title & authors Abstract References Publication types MeSH terms Substances LinkOut - more resources Review CNS Drug Rev Actions Search in PubMed Search in NLM Catalog Add to Search . 2005 Spring;11(1):1-20. doi: 10.1111/j.1527-3458.2005.tb00033.x. Retigabine: chemical synthesis to clinical application G Blackburn-Munro 1 , W Dalby-Brown , N R Mirza , J D Mikkelsen , R E Blackburn-Munro Affiliations Expand Affiliation 1 Department of Pharmacology, NeuroSearch A/S, Pederstrupvej 93, DK-2750 Ballerup, Denmark. gbm@neurosearch.dk PMID: 15867950 PMCID: PMC6741764 DOI: 10.1111/j.1527-3458.2005.tb00033.x Item in Clipboard Review Retigabine: chemical synthesis to clinical application G Blackburn-Munro et al. CNS Drug Rev . 2005 Spring . Show details Display options Display options Format Abstract PubMed PMID CNS Drug Rev Actions Search in PubMed Search in NLM Catalog Add to Search . 2005 Spring;11(1):1-20. doi: 10.1111/j.1527-3458.2005.tb00033.x. Authors G Blackburn-Munro 1 , W Dalby-Brown , N R Mirza , J D Mikkelsen , R E Blackburn-

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC Skip to main content An official website of the United States government Here's how you know Here's how you know Official websites use .gov A .gov website belongs to an official
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the contents by NLM or the National Institutes of Health. Learn more: PMC Disclaimer | PMC Copyright Notice Ther Adv Chronic Dis . 2011 Nov;2(6):371–376. doi: 10.1177/2040622311421542 Search in PMC Search in PubMed View in NLM Catalog Add to search Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians Jacklyn A Harris Jacklyn A Harris Find articles by Jacklyn A Harris ✉ , Julie A Murphy Julie A Murphy Find articles by Julie A Murphy Author information Article notes Copyright and License information ✉ Jacklyn A. Harris, PharmD, BCPS Assistant Professor of Pharmacy Practice, Department of Pharmacy Practice, St Louis College of Pharmacy, 4588 Parkview Place, St Louis, MO 63110-1088, USA jharris2@stlcop.edu ✉ Julie A. Murphy, PharmD, BCPS Associate Professor of Pharmacy Practice, St Louis College

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

Retigabine : Indications, Uses, Dosage, Drugs Interactions, Side effects

(cardiac arrest/asystole or ventricular tachycardia) may occur. Management: Supportive treatment. Ensure an adequate airway, ventilation and oxygenation. Clinical Pharmacology of Retigabine Pharmacodynamics: Retigabine activates specific voltage-gated K channels in the brain known as the KCNQ (Kv7.2-7.5) family of ion channels, thereby stabilising the K channels in open formation, enhancing the M-type current and exerting a hyperpolarising effect on neuronal cells, resulting to stabilisation of the resting membrane potential and suppression of seizure activity. Pharmacokinetics: Absorption: Readily absorbed. Bioavailability: Approx 60%. Time to peak plasma concentration: Approx 0.5-2 hr. Distribution: Well distributed in the body. Volume of distribution: 2-3 L/kg. Plasma protein binding: Approx 80%. Metabolism: Extensively metabolised, mainly via glucuronidation by the uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4) to form inactive N -glucuronides (major metabolites); also undergoes acetylation by N -acetyltransferase 2 (NAT2) to form an active, but less potent, N -acetyl metabolite (NAMR) that is subsequently glucuronidated. Excretion: Via Urine, approx 85% (36% as unchanged drug, 18% as NAMR, and 24% as N -glucuronides); faeces (approx 14%, w/ 3% as unchanged drug). Elimination half-life: Approx 6-11 hr Clinical Studies of Retigabine There are some clinical studies of the drug Retigabine mentioned below: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4053062/ https://www.sciencedirect.com/topics/pharmacology-toxicology-and-pharmaceutical-science/Retigabine https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3538493/ References https://go.drugbank.com/drugs/DB09235 https://www.apollopharmacy.in/s

Retigabine : Indications, Uses, Dosage, Drugs Interactions, Side effects

7.5) voltage-gated potassium channels, thereby stabilizing the channels in the open formation and enhancing the M-current. As a result, neuronal excitability is regulated, and epileptiform activity is suppressed. In addition, Retigabine may also exert therapeutic effects through the augmentation of GABA-mediated currents. How To Use Retigabine Retigabine is available in the form of dosage forms, such as tablets. Retigabine tablets were taken orally with or without food. Uses of Retigabine Retigabine is used in the treatment of Partial-onset seizures. Benefits of Retigabine Retigabine is a first-in-class anticonvulsant that works by activating KCNQ2/3 channels. In vitro studies indicate that ezogabine enhances transmembrane potassium currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels. By activating KCNQ channels, ezogabine is thought to stabilize the resting membrane potential and reduce brain excitability. Indications of Retigabine Retigabine is approved for its use in the following clinical indications: Partial-onset seizures: As adjunctive treatment for partial-onset seizures in patients ≥18 years who have responded inadequately to several alternative treatments and for whom the benefits outweigh the risk of retinal abnormalities and potential decline in visual acuity Dosage Strengths of Retigabine Retigabine is available in various dosage strengths: 50 mg, 100 mg, 200 mg, 300 mg, 400 mg. Dosage Forms of Retigabine Retigabine is available in the form of dosage forms, such as tablets. Dose Adjustment in Kidney Patients ● CrCl ≥50 mL/minute: No dosage adjustment necessary. ● CrCl <50 mL/minute: Initial: 50 mg 3 times daily; may increase at weekly intervals in increments of ≤150 mg per day to a maximum dose of 200 mg 3 times daily (600 mg per day). ● ESRD requiring hemodialysis: Initial: 50 mg 3 times daily; may increase at weekly intervals in increments of ≤150 mg per day to

Retigabine - Wikipedia

07-19 . Further reading [ edit ] Blackburn-Munro G, Dalby-Brown W, Mirza NR, Mikkelsen JD, Blackburn-Munro RE (2005). "Retigabine: chemical synthesis to clinical application" . CNS Drug Reviews . 11 (1): 1– 20. doi : 10.1111/j.1527-3458.2005.tb00033.x . PMC 6741764 . PMID 15867950 . Hempel R, Schupke H, McNeilly PJ, Heinecke K, Kronbach C, Grunwald C, et al. (May 1999). "Metabolism of retigabine (D-23129), a novel anticonvulsant" . Drug Metabolism and Disposition . 27 (5): 613– 622. doi : 10.1016/S0090-9556(24)15258-0 . PMID 10220491 . [ permanent dead link ] v t e Anticonvulsants ( N03 ) GABAergics GABA A R PAMs Barbiturates : Barbexaclone Metharbital Methylphenobarbital Pentobarbital Phenobarbital # Primidone ; Carbamates : Cenobamate Felbamate ; Benzodiazepines : Clobazam Clonazepam Clorazepate Diazepam # Lorazepam # Midazolam Nimetazepam Nitrazepam Temazepam ; Others: Bromide ( potassium bromide , sodium bromide ) Imepitoin Paraldehyde Stiripentol GABA-T inhibitors Fatty acids (and related): Valproate Valpromide Valproate pivoxil Vigabatrin Others GABAR agonists : Progabide ; GAT-1 inhibitors : Tiagabine Channel modulators Sodium blockers Hydantoins : Ethotoin Fosphenytoin Mephenytoin Phenytoin # ; Ureides : Acetylpheneturide Chlorphenacemide Phenacemide ‡ Pheneturide ; Fatty acids : Valproate Valpromide Valproate pivoxil ; Carboxamides : Carbamazepine # Eslicarbazepine acetate Oxcarbazepine ; Others: Lacosamide Lamot

Retigabine - Wikipedia

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf

effectiveness of newer drugs for epilepsy in adults: a systematic review and economic evaluation. Wilby J, Kainth A, Hawkins N, Epstein D, McIntosh H, McDaid C, Mason A, Golder S, O'Meara S, Sculpher M, et al. Health Technol Assess. 2005 Apr; 9(15):1-157, iii-iv. Rufinamide add-on therapy for refractory epilepsy. [Cochrane Database Syst Rev. 2018] Rufinamide add-on therapy for refractory epilepsy. Panebianco M, Prabhakar H, Marson AG. Cochrane Database Syst Rev. 2018 Apr 25; 4(4):CD011772. Epub 2018 Apr 25. Lamotrigine add-on for drug-resistant partial epilepsy. [Cochrane Database Syst Rev. 2016] Lamotrigine add-on for drug-resistant partial epilepsy. Ramaratnam S, Panebianco M, Marson AG. Cochrane Database Syst Rev. 2016 Jun 22; 2016(6):CD001909. Epub 2016 Jun 22. Lamotrigine versus carbamazepine monotherapy for epilepsy: an individual participant data review. [Cochrane Database Syst Rev. 2018] Lamotrigine versus carbamazepine monotherapy for epilepsy: an individual participant data review. Nevitt SJ, Tudur Smith C, Weston J, Marson AG. Cochrane Database Syst Rev. 2018 Jun 28; 6(6):CD001031. Epub 2018 Jun 28. Review Retigabine for the adjunctive treatment of adults with partial-onset seizures in epilepsy with and without secondary generalization : a NICE single technology appraisal. [Pharmacoeconomics. 2013] Review Retigabine for the adjunctive treatment of adults with partial-onset seizures in epilepsy with and without secondary generalization : a NICE single technology appraisal. Craig D, Rice S, Paton F, Fox D, Woolacott N. Pharmacoeconomics. 2013 Feb; 31(2):101-10. See reviews... See all... Recent Activity Clear Turn Off Turn On The efficacy and safety of retigabine and other adjunctive treatments for refrac... The efficacy and safety of retigabine and other adjunctive treatments for refractory

Retigabine - Wikipedia

olum) Monastrol Nicotinic acid Nicotinamide Org 25,435 Phenytoin Propanidid Retigabine (ezogabine) Safranal Seproxetine Stiripentol Sulfonylalkanes (e.g., sulfonmethane (sulfonal) , tetronal , trional ) Terpenoids (e.g., borneol ) Topiramate Valerian constituents (e.g., isovaleric acid , isovaleramide , valerenic acid , valerenol ) Unsorted benzodiazepine site positive modulators: α-Pinene MRK-409 (MK-0343) TCS-1105 TCS-1205 See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators Portal : Medicine Authority control databases : National United States Israel Retrieved from " https://en.wikipedia.org/w/index.php?title=Retigabine&oldid=1296296022 " Categories : Anticonvulsants Carbamates Potassium channel openers 4-Fluorophenyl compounds GABAA receptor positive allosteric modulators Withdrawn drugs Orphan drugs Hidden categories: CS1:Vancouver names with accept markup Articles with short description Short description is different from Wikidata Infobox drug with local INN variant ECHA InfoCard ID from Wikidata Drug has EMA link Articles containing unverified chemical infoboxes All articles with dead external links Articles with dead external links from June 2025 Articles with permanently dead external links This page was last edited on 19 June 2025, at 03:42 (UTC) . Text is available under the Creative Commons Attribution-ShareAlike 4.0 License ;
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Retigabine - Wikipedia

The efficacy and safety of retigabine and other adjunctive treatments for refractory partial epilepsy: a systematic review and indirect comparison - Database of Abstracts of Reviews of Effects (DARE): Quality-assessed Reviews - NCBI Bookshelf

reduction in seizure frequency), seizure-free patients, withdrawals, and patients reporting anti-epileptic drug-related adverse events (ataxia, dizziness, fatigue, nausea, or somnolence), were extracted from each study to calculate odds ratios and related 95% confidence intervals. One reviewer extracted the data, and they were checked by a second reviewer. Methods of synthesis Pooled odds ratios and relative risks were calculated for the drug to placebo comparisons, using both fixed-effect and random-effects models; only odds ratios were presented. Statistical heterogeneity was assessed using Cochran's Q and Ι². Publication bias was investigated by funnel plot inspection. A hierarchical Bayesian network meta-analysis was used to compare the anti-epileptic drugs indirectly with each other, using a fixed-effect logistic regression model. The results were presented as mean odds ratios and 95% credible intervals. Where the trials had multiple treatment arms, evaluating different drug doses, compared with placebo, the results of the different treatment arms were combined to create a pooled comparison of the drug versus placebo. Additional analyses were undertaken to consider clinically relevant dose ranges. Results of the review Twenty trials met the inclusion criteria. Three assessed retigabine (1,242 patients), three assessed eslicarbazepine acetate (1,050 patients), three assessed lacosamide (1,308 patients), three assessed tiagabine (769 patients), and three assessed zonisamide (642 patients). The other five assessed pregabalin (1,487 patients). The double-blind period (following baseline, titration, and maintenance periods) ranged from 12 to 24 weeks. In the network meta-analysis, retigabine was no better and no worse than the other anti-epileptic drugs for responder rate, during the maintenance period; seizure freedom, during maintenance and double-blind periods; withdrawals due to adverse events; and incidences of ataxia, dizziness, fatigue and nausea. Retigabine was associated with a lower responder rate than pregabalin, during the double-blind period (OR 0.65, CrI 0.41 to 0.96), a higher withdrawal rate, for any reason, than eslicarbazepine acetate (OR 1.91, CrI 1.18 to 2.89), and a higher incidence of somnolence than tiagabine (OR 2.38,

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

administration of retigabine with lamotrigine resulted in a small decrease in retigabine clearance, which is thought to be due to competition for renal elimination. Retigabine was also found to increase the metabolism of lamotrigine by an unknown mechanism [ Hermann et al. 2003b ]. The pharmacokinetics of valproic acid, topiramate, phenytoin, or carbamazepine was not clinically altered with concurrent retigabine use. Oral combination contraceptives and retigabine do not result in any pharmacokinetic interactions [ Bialer et al. 2010 ; Luszczki, 2009 ; Hermann et al. 2003b ]. Clinical trials In a parallel-group, double-blind, placebo-controlled, randomized clinical trial, the 16-week (8-week forced titration and 8-week maintenance) efficacy and safety of adjunctive therapy with retigabine 600 mg, 900 mg, and 1200 mg/day in three equally divided doses in subjects with partial-onset seizures was evaluated [ Porter et al. 2007b ]. During the 8-week baseline phase, subjects had to experience a minimum of four partial-onset seizures per month with no 30-day seizure-free period, while maintained on stable doses of one or two AEDs. During week one of the forced titration phase, subjects in the retigabine arms received retigabine 100 mg three times daily. At weekly intervals, thereafter, the dose was increased by 150 mg/day (50 mg three times daily), such that subjects in the 600 mg/day arm reached their target dose by day 15, the 900 mg/day arm by day 29, and the 1200 mg/day arm by day 43. A total of 396 subjects were included in the intention-to-treat (ITT) efficacy analysis. The median percentage reduction in monthly total partial seizure frequency from baseline and the 50% responder rates can be found in Table 1 . Adverse events that occurred are addressed in the adverse drug reactions section below. The authors concluded that adjunctive therapy with retigabine is well tolerated and reduces the frequency of partial-onset seizures in a dose-dependent manner. Table 1. Summary of placebo-controlled trials for retigabine in partial-onset seizures. Study Sample size Dosage Median reduction inseizure frequency 50% responder rates Porter et al.

Retigabine (ezogabine) as add-on therapy for partial-onset seizures: an update for clinicians - PMC

Retigabine - Wikipedia

7–11 hours [ 1 ] Excretion Kidney (84%) Identifiers IUPAC name Ethyl N -[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate CAS Number 150812-12-7 PubChem CID 121892 IUPHAR/BPS 2601 DrugBank DB04953 ChemSpider 108740 UNII 12G01I6BBU KEGG D09569 ChEMBL ChEMBL41355 CompTox Dashboard ( EPA ) DTXSID40164615 ECHA InfoCard 100.158.123 Chemical and physical data Formula C 16 H 18 F N 3 O 2 Molar mass 303.337 g·mol −1 3D model ( JSmol ) Interactive image SMILES O=C(OCC)Nc1ccc(cc1N)NCc2ccc(F)cc2 InChI InChI=1S/C16H18FN3O2/c1-2-22-16(21)20-15-8-7-13(9-14(15)18)19-10-11-3-5-12(17)6-4-11/h3-9,19H,2,10,18H2,1H3,(H,20,21) Key:PCOBBVZJEWWZFR-UHFFFAOYSA-N Retigabine ( INN ) or ezogabine ( USAN ) is an anticonvulsant used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients. [ 2 ] The drug was developed by Valeant Pharmaceuticals and GlaxoSmithKline . It was approved by the European Medicines Agency under the trade name Trobalt on March 28, 2011, and by the United States Food and Drug Administration (FDA), under the trade name Potiga , on June 10, 2011. Production was discontinued in June 2017. [ 3 ] [ 4 ] Retigabine works primarily as a potassium channel opener —that is, by activating a certain family of voltage-gated potassium channels in the brain. [ 5 ] [ 6 ] [ 7 ] This mechanism of action is unique among antiepileptic drugs, and may hold promise for