Ganaxolone
Ganaxolone Uses, Dosage, Side Effects, Food Interaction and all others data.
Ganaxolone is the 3β-methylated synthetic analog of allopregnanolone; it belongs to a class of compounds referred to as neurosteroids. Ganaxolone is an allosteric modulator of GABAA receptors acting through binding sites which are distinct from the benzodiazepine binding site. It has activity in a broad range of animal models of epilepsy. Ganaxolone has been shown to be well tolerated in adults and children. In early phase II studies, Ganaxolone has been shown to have activity in adult patients with partial-onset seizures and epileptic children with history of infantile spasms. It is currently undergoing further development in infants with newly diagnosed infantile spasms, in women with catamenial epilepsy, and in adults with refractory partial-onset seizures.
Ganaxolone is a powerful positive allosteric modulator of GABAA receptors with potency and efficacy comparable to its endogenous analog 3a,5a-P (Carter et al., 1997). As with 3a,5a-P, Ganaxolone potentiation of the GABAA receptor occurs at a site distinct from the benzodiazepine site. Ganaxolone has protective activity in diverse rodent seizure models, including clonic seizures induced by pentylenetetrazol (PTZ) and bicuculline (BIC), limbic seizures in the 6 Hz model, and amygdala kindled seizures (Carter et al., 1997; Rogawski and Reddy, 2004; Kaminski et al., 2004).
| Trade Name | Ganaxolone |
| Availability | Prescription only |
| Generic | Ganaxolone |
| Ganaxolone Other Names | Ganaxolone |
| Related Drugs | diazepam, topiramate, levetiracetam, Keppra, Topamax, Valium |
| Type | |
| Formula | C22H36O2 |
| Weight | Average: 332.528 Monoisotopic: 332.271530399 |
| Protein binding | >99% |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Investigated for use/treatment in pediatric indications and seizure disorders.
How Ganaxolone works
Ganaxolone belongs to a novel class of neuroactive steroids called epalons, which specifically modulate the γ-aminobutyric acid type A (GABAA) receptor in the central nervous system (CNS). Chemically related to progesterone but devoid of any hormonal activity, the epalons have potent antiepileptic, anxiolytic, sedative, and hypnotic activities in animals.
Food Interaction
[Moderate] ADJUST DOSING INTERVAL: Food enhances the oral bioavailability of ganaxolone.
When administered with a high-fat meal, ganaxolone peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 3- and 2-fold, respectively, compared to administration under fasted conditions.
Ganaxolone was administered with food in the premarketing study population.
The efficacy of ganaxolone when administered in the fasted state is unknown.
GENERALLY AVOID: Concomitant use of ganaxolone with central nervous system (CNS) depressants, including alcohol, may potentiate adverse effects such as somnolence and sedation.
MANAGEMENT: Ganaxolone must be administered with food according to the manufacturer.
Patients should be advised to avoid or limit consumption of alcohol and to avoid activities requiring mental alertness such as driving or operating hazardous machinery until they know how the medication affects them.
Ganaxolone Disease Interaction
Moderate: suicidal tendency, alcoholism, hepatic impairmentMinor: renal impairment
Half Life
1.3-1.9 hours
Innovators Monograph
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