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Trimethadione | CAS No: 127-48-0 | GMP-certified suppliers
A medication that manages refractory absence seizures by reducing abnormal central nervous system electrical activity to help control epileptic episodes.
Therapeutic categories
Primary indications
- Used in the control of absence (petit mal) seizures that are refractory to treatment with other medications
Product Snapshot
- Trimethadione is an oral small molecule available in tablet and chewable tablet formulations
- It is primarily indicated for the management of refractory absence (petit mal) seizures
- The compound is FDA-approved and marketed in the United States
Clinical Overview
Pharmacodynamically, trimethadione and its closely related compound paramethadione act on the central nervous system to reduce the frequency of epileptic seizures. Their therapeutic effect is attributed to modulation of CNS electrical activity, specifically targeting abnormal rhythmic discharge patterns observed in absence seizures.
The mechanism of action involves inhibition of voltage-dependent T-type calcium channels located in thalamic neurons, including thalamic relay neurons. By reducing T-type calcium currents, trimethadione elevates the threshold for repetitive neuronal firing within the thalamus and suppresses corticothalamic transmission. This modulation dampens the abnormal thalamocortical oscillations associated with the characteristic 3-Hz spike-and-wave EEG pattern of absence seizures.
From an ADME perspective, trimethadione is a substrate for multiple cytochrome P450 isoenzymes, including CYP2C19, CYP2C8, CYP2C9, CYP2E1, and CYP3A4. This implicates potential for drug-drug interactions mediated through hepatic metabolism. Trimethadione’s impact on cardiac electrophysiology includes a potential for QTc interval prolongation, warranting consideration in patients with cardiac risk factors.
Safety and toxicity profiles limit the use of trimethadione to refractory absence seizures. Adverse effects can be significant, and chronic administration requires careful monitoring. The drug is also categorized among agents capable of causing hyperkalemia and bradycardia, emphasizing the need for clinical vigilance.
Trimethadione remains a specialized therapeutic option primarily in settings where newer antiepileptics fail or are contraindicated. It is referenced in legacy clinical practice and older epilepsy management protocols.
For API sourcing, manufacturers should prioritize purity and consistency due to trimethadione’s narrow therapeutic index and toxicity concerns. Compliance with pharmacopeial standards and verification of impurity profiles, particularly for potential genotoxic or teratogenic contaminants, is essential to ensure product quality and patient safety.
Identification & chemistry
| Generic name | Trimethadione |
|---|---|
| Molecule type | Small molecule |
| CAS | 127-48-0 |
| UNII | R7GV3H6FQ4 |
| DrugBank ID | DB00347 |
Pharmacology
| Summary | Dione anticonvulsants target voltage-dependent T-type calcium channels in thalamic neurons, inhibiting T-type calcium currents and raising the threshold for repetitive thalamic activity. This modulation disrupts abnormal thalamocortical rhythmicity associated with absence seizures. These agents are utilized in the management of refractory absence epilepsy by reducing seizure frequency through central nervous system effects. |
|---|---|
| Mechanism of action | Dione anticonvulsants reduce T-type calcium currents in thalamic neurons, including thalamic relay neurons. It does so via the inhibition of voltage dependent T-type calcium channels. This raises the threshold for repetitive activity in the thalamus, and inhibits corticothalamic transmission. Thus, the abnormal thalamocortical rhythmicity, which is thought to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram(EEG) with absence seizures, is dampened. |
| Pharmacodynamics | Paramethadione and trimethadione are anticonvulsants indicated in the control of absence (petit mal) seizures that are refractory to treatment with other medications. Dione anticonvulsants are used in the treatment of epilepsy. They act on the central nervous system (CNS) to reduce the number of seizures. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent T-type calcium channel subunit alpha-1G | Humans | inhibitor |
ADME / PK
| Protein binding | 90% |
|---|
Formulation & handling
- Trimethadione is formulated for oral administration as a chewable tablet and is not intended for injectable use.
- As a small molecule with moderate water solubility, it is suitable for solid oral dosage forms requiring controlled release considerations.
- Avoid co-administration with alcohol due to potential central nervous system depressant effects affecting patient safety.
Regulatory status
| Lifecycle | The API is currently marketed in the US, with patent protection recently expired, allowing for the introduction of generic alternatives. This transition marks the product's shift from exclusive patent protection to a more competitive market phase. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Trimethadione is currently manufactured and packaged primarily by a single originator company, with branded products available in the US market. There is no indication of a broader global presence in the EU or other regions. Patent expiry status is not specified, suggesting limited or no generic competition in the immediate market. |
|---|
Safety
| Toxicity | Symptoms of overdose include clumsiness or unsteadiness, coma, dizziness (severe), drowsiness (severe), nausea (severe), and problems with vision. |
|---|
- Overdose may result in severe CNS depression, including coma and impaired motor coordination
- Exposure can cause pronounced dizziness, drowsiness, and visual disturbances
- Handle with appropriate protective measures to minimize risk of systemic toxicity
Trimethadione is a type of Anticonvulsants
Anticonvulsants are a vital category of pharmaceutical Active Pharmaceutical Ingredients (APIs) used for the treatment of seizures and epilepsy. These APIs play a crucial role in managing and preventing convulsions, which are characterized by abnormal electrical activity in the brain. With a significant demand for effective anticonvulsant medications, these APIs hold immense importance in the pharmaceutical industry.
Anticonvulsant APIs work by stabilizing the excessive electrical activity in the brain, preventing or reducing seizures. They achieve this by targeting specific receptors or channels involved in the regulation of neuronal excitability. Some commonly used anticonvulsant APIs include phenytoin, valproic acid, carbamazepine, and lamotrigine.
Pharmaceutical companies utilize these APIs to formulate various dosage forms, such as tablets, capsules, and oral suspensions, ensuring convenient administration for patients. Additionally, anticonvulsant APIs may also be employed in the development of extended-release formulations, providing sustained and controlled drug release.
The market for anticonvulsant APIs continues to grow due to the rising prevalence of epilepsy and other seizure disorders. Moreover, ongoing research and development efforts aim to enhance the efficacy, safety, and tolerability of these APIs, ensuring better treatment outcomes for patients.
In conclusion, anticonvulsant APIs are a crucial pharmaceutical category used to manage seizures and epilepsy. With their ability to stabilize brain activity, these APIs play a pivotal role in improving the quality of life for individuals living with these conditions. The pharmaceutical industry's continued focus on research and development in this area ensures the availability of advanced and effective anticonvulsant medications for patients in need.
Trimethadione API manufacturers & distributors
Compare qualified Trimethadione API suppliers worldwide. We currently have 1 companies offering Trimethadione API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Aesica Queenborough | Producer | United Kingdom | United Kingdom | CoA, GMP | 4 products |
When sending a request, specify which Trimethadione API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Trimethadione API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
