Cenobamate
Cenobamate Uses, Dosage, Side Effects, Food Interaction and all others data.
Cenobamate, or YKP-3089, is an antiepileptic drug developed by SK Pharmaceuticals and used to treat partial onset seizures. The exact mechanism of action has not been described in the literature, though it positively modulates GABAA and inhibits voltage gated sodium channels.
Cenobamate was granted FDA approval on 21 November 2019.
The mechanism of cenobamate is unknown, however it modulates GABAA and inhibit voltage gated sodium channels. Cenobamate is given once daily and so it has a long duration of action. The therapeutic window is wide as doses of 750mg can be well tolerated. Patients should be counselled regarding the risk of DRESS syndrome, QT interval shortening, suicidal behavior, and neurological adverse effects.
Trade Name | Cenobamate |
Availability | Prescription only |
Generic | Cenobamate |
Cenobamate Other Names | Cenobamate, Cénobamate, Cenobamato, Cenobamatum |
Related Drugs | diazepam, topiramate, levetiracetam, Keppra, Topamax, Valium |
Type | Oral tablet |
Formula | C10H10ClN5O2 |
Weight | Average: 267.67 Monoisotopic: 267.0523023 |
Protein binding | Cenobamate is 60% protein bound in plasma, mainly serum albumin. |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cenobamate is a small molecule drug indicated to treat partial onset seizures in adults.
Cenobamate is indicated for the treatment of partial onset seizures in adults.
Cenobamate is also used to associated treatment for these conditions: Partial-Onset Seizures
How Cenobamate works
Cenobamate inhibits voltage gated sodium channels and is a positive GABAA modulator. However, the exact mechanism of action remains unknown. Inhibition of voltage gated sodium channels increases the threshold for generating action potentials and decreases the number of action potentials.
Toxicity
There is limited information regarding the signs, symptoms, and treatment of a cenobamate overdose. Symptomatic and supportive treatment is recommended and there is limited data on the utility of dialysis to remove cenobamate from blood.
Food Interaction
- Avoid alcohol. Alcohol may increase somnolence and sedation.
- Take with or without food.
Cenobamate Alcohol interaction
[Moderate] GENERALLY AVOID:
Alcohol may potentiate some of the pharmacologic effects of central nervous system (CNS)-active agents.
Use in combination may result in additive CNS depression and/or impairment of judgment, thinking, and psychomotor skills.
Patients receiving CNS-active agents should be advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled against driving, operating machinery, or engaging in potentially hazardous activities requiring mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Cenobamate Drug Interaction
Moderate: perampanel, lamotrigine, atorvastatin, dextromethorphan / guaifenesin, esomeprazole, clobazam, topiramate, ubrogepantUnknown: fremanezumab, naproxen, albuterol / ipratropium, fluticasone, metoprolol, albuterol, acetaminophen, albuterol, lacosamide, cyanocobalamin
Volume of Distribution
The apparent volume of distribution of cenobamate is 40-50L.
Elimination Route
Cenobamate is 88% orally bioavailable with a Tmax of 1-4 hours. A high fat meal does not significantly impact the pharmacokinetics of cenobamate.
Half Life
The terminal half life of cenobamate is 50-60h.
Clearance
The apparent oral clearance of cenobamate is 0.45-0.63L/h for a 100-400mg/day dose.
Elimination Route
Cenobamate is 87.8% eliminated in the urine and 5.2% in the feces.
Innovators Monograph
You find simplified version here Cenobamate