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Paramethadione | CAS No: 115-67-3 | GMP-certified suppliers
A medication that controls refractory absence (petit mal) seizures by reducing their frequency through central nervous system modulation, requiring stringent quality and safety standards for API sourcing.
Therapeutic categories
AnticonvulsantsCentral Nervous System DepressantsCytochrome P-450 CYP2C8 SubstratesCytochrome P-450 CYP2C9 SubstratesCytochrome P-450 CYP2E1 SubstratesCytochrome P-450 CYP3A Substrates
Generic name
Paramethadione
Molecule type
small molecule
CAS number
115-67-3
DrugBank ID
DB00617
Approval status
Approved drug
ATC code
N03AC01
Primary indications
- Used for the control of absence (petit mal) seizures that are refractory to treatment with other medications
Product Snapshot
- Paramethadione is an oral small molecule formulation
- It is primarily indicated for the control of refractory absence (petit mal) seizures
- The compound has received regulatory approval for this indication
Clinical Overview
Paramethadione (CAS number 115-67-3) is an anticonvulsant belonging to the oxazolidinedione class. It is specifically indicated for the control of absence (petit mal) seizures that are refractory to other therapies. Absence seizures are characterized by brief episodes of impaired consciousness, during which the individual appears vacant and unresponsive, typically lasting up to 30 seconds.
Pharmacologically, paramethadione acts on the central nervous system to reduce the frequency of these absence seizures. Its action is localized primarily in the thalamic reticular nucleus, a region implicated in the generation of absence seizures. Mechanistically, paramethadione and related dione anticonvulsants inhibit T-type calcium channels in thalamic neurons, including relay neurons. This inhibition disrupts corticothalamic transmission and elevates the threshold for repetitive neuronal firing in the thalamus. The net effect is a suppression of abnormal thalamocortical rhythmicity, which underpins the characteristic 3-Hz spike-and-wave discharges observed in electroencephalogram recordings during absence seizures.
Paramethadione is metabolized via multiple cytochrome P450 enzymes, including CYP2C8, CYP2C9, CYP2E1, and CYP3A4 isoforms, indicating the potential for drug-drug interactions through these metabolic pathways. Its classification includes anticonvulsants and central nervous system depressants.
Safety considerations are critical due to the association of paramethadione with fetal trimethadione syndrome, also termed paramethadione syndrome. This teratogenic risk necessitates careful evaluation of benefit versus risk in women of childbearing potential and highlights the importance of contraceptive measures during treatment.
From a sourcing and quality perspective, procurement of paramethadione active pharmaceutical ingredient (API) requires adherence to rigorous quality standards including purity, batch consistency, and compliance with relevant pharmacopeial monographs. Given its teratogenic potential and CNS activity, traceability and control of impurities are essential to ensure safety and efficacy in finished pharmaceutical products.
Pharmacologically, paramethadione acts on the central nervous system to reduce the frequency of these absence seizures. Its action is localized primarily in the thalamic reticular nucleus, a region implicated in the generation of absence seizures. Mechanistically, paramethadione and related dione anticonvulsants inhibit T-type calcium channels in thalamic neurons, including relay neurons. This inhibition disrupts corticothalamic transmission and elevates the threshold for repetitive neuronal firing in the thalamus. The net effect is a suppression of abnormal thalamocortical rhythmicity, which underpins the characteristic 3-Hz spike-and-wave discharges observed in electroencephalogram recordings during absence seizures.
Paramethadione is metabolized via multiple cytochrome P450 enzymes, including CYP2C8, CYP2C9, CYP2E1, and CYP3A4 isoforms, indicating the potential for drug-drug interactions through these metabolic pathways. Its classification includes anticonvulsants and central nervous system depressants.
Safety considerations are critical due to the association of paramethadione with fetal trimethadione syndrome, also termed paramethadione syndrome. This teratogenic risk necessitates careful evaluation of benefit versus risk in women of childbearing potential and highlights the importance of contraceptive measures during treatment.
From a sourcing and quality perspective, procurement of paramethadione active pharmaceutical ingredient (API) requires adherence to rigorous quality standards including purity, batch consistency, and compliance with relevant pharmacopeial monographs. Given its teratogenic potential and CNS activity, traceability and control of impurities are essential to ensure safety and efficacy in finished pharmaceutical products.
Identification & chemistry
| Generic name | Paramethadione |
|---|---|
| Molecule type | Small molecule |
| CAS | 115-67-3 |
| UNII | Z615FRW64N |
| DrugBank ID | DB00617 |
Pharmacology
| Summary | Paramethadione, an oxazolidinedione anticonvulsant, targets voltage-dependent T-type calcium channels in thalamic neurons to inhibit corticothalamic transmission. This action increases the threshold for repetitive thalamic activity, reducing abnormal thalamocortical rhythmicity associated with absence seizures. It is primarily indicated for managing treatment-resistant absence (petit mal) seizures. |
|---|---|
| Mechanism of action | Dione anticonvulsants such as paramethadione reduce T-type calcium currents in thalamic neurons (including thalamic relay neurons). This inhibits corticothalamic transmission and raises the threshold for repetitive activity in the thalamus. This results in a dampening of the abnormal thalamocortical rhythmicity proposed to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram (EEG) during absence seizures. |
| Pharmacodynamics | Paramethadione is an oxazolidinedione anticonvulsant similar to trimethadione that acts on the central nervous system (CNS) to reduce the number of absence seizures (often seen in epileptics). Absence seizures involve an interruption to consciousness where the person experiencing the seizure seems to become vacant and unresponsive for a short period of time (usually up to 30 seconds). Paramethadione acts on thalamic neurons in the thalamic reticular nucleus (which studies have shown to be associated with absence seizures, von Krosigk et al., 1993). |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent T-type calcium channel subunit alpha-1I | Humans | inhibitor |
ADME / PK
| Absorption | Rapid via the digestive tract. |
|---|---|
| Half-life | 12 to 24 hours (however the half-life for the active metabolite is not known) |
| Protein binding | Not significant |
| Metabolism | Primarily hepatic (mainly via cytochrome P450 isozyme 2C9), paramethadione is completely demethylated to 5-ethyl-5-methyl-2,4-oxazolidinedione, the active metabolite. |
Formulation & handling
- Paramethadione is a small molecule suitable for oral formulation due to its moderate logP and high water solubility.
- It is chemically stable under standard handling conditions, but formulation should consider its liquid state for accurate dosing.
- No peptide or biologic properties are present, and sensitivity to food intake has not been indicated.
Regulatory status
Supply Chain
| Supply chain summary | Paramethadione is manufactured by a limited number of originator companies, with Abbott Laboratories Pharmaceutical Products Division identified as a key manufacturer. The branded product has a presence primarily in the US and EU markets. Given the patent status, paramethadione is likely subject to existing generic competition in these regions. |
|---|
Safety
| Toxicity | Symptoms of overdose include clumsiness or unsteadiness, coma, severe dizziness, severe drowsiness, severe nausea, and problems with vision. |
|---|
High Level Warnings:
- Overexposure may result in central nervous system depression, including severe dizziness and drowsiness
- Ingestion of excessive quantities can cause coma and impaired motor coordination
- Visual disturbances have been reported in cases of overdose
