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Topiramate | CAS No: 97240-79-4 | GMP-certified suppliers
A medication that treats epilepsy seizures, Lennox-Gastaut syndrome, and migraine prophylaxis in patients aged 2 years and older, supporting diverse therapeutic needs.
Therapeutic categories
Primary indications
- Topiramate is indicated for the following conditions: 1)Monotherapy for partial onset or primary generalized tonic-clonic seizures for patients 2 years of age and above 2)Adjunctive therapy for partial onset seizures or primary generalized tonic-clonic seizures for both adult and pediatric patients above 2 years old 3)Adjunctive therapy for seizures associated with Lennox-Gastaut syndrome in patients above 2 years of age 4)Prophylaxis of migraine in children 12 years of age and older and adults
- Topiramate is also used off-label as an adjunct therapy for weight management and for mood disorders
Product Snapshot
- Topiramate is available as oral formulations including tablets, capsules, and extended-release capsules
- It is primarily indicated for treatment of various seizure disorders and migraine prophylaxis
- The API is approved for use in major regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, topiramate reduces neuronal excitability by modulating multiple targets. It enhances GABA-A receptor-mediated inhibitory neurotransmission at non-benzodiazepine sites and inhibits excitatory glutamate receptors, specifically AMPA and kainate subtypes. It also blocks voltage-dependent sodium channels, further decreasing abnormal neuronal firing associated with seizures. Topiramate’s activity as a carbonic anhydrase inhibitor is noted, but the clinical relevance of this remains uncertain. The compound belongs to the dioxolopyran chemical class, characterized structurally by a fused dioxole and pyran ring, with a unique monosaccharide-like configuration containing a sulfamate group.
Absorption of topiramate is typically rapid and complete, with moderate protein binding and a half-life allowing twice-daily dosing in most formulations. It is predominantly eliminated unchanged via renal excretion. Topiramate is known to interact with cytochrome P450 enzymes, including CYP2C19 inhibition and CYP3A4 induction, affecting its own metabolism and potential drug-drug interactions.
Safety considerations include risks of metabolic acidosis, nephrolithiasis, cognitive and mood disturbances including potential for suicidal ideation, and hypothermia when combined with valproic acid. Careful monitoring is essential in clinical use, especially in pediatric populations and individuals with renal impairment.
Topiramate APIs should be sourced with attention to stringent quality controls ensuring consistent purity, polymorphic form, and compliance with regulatory standards. Given its widespread global use and multiple indications, reliable suppliers with validated analytical methods and robust supply chains are critical for formulation development and regulatory submissions.
Identification & chemistry
| Generic name | Topiramate |
|---|---|
| Molecule type | Small molecule |
| CAS | 97240-79-4 |
| UNII | 0H73WJJ391 |
| DrugBank ID | DB00273 |
Pharmacology
| Summary | Topiramate exerts anticonvulsant and antimigraine effects primarily through modulation of neuronal excitability by enhancing GABA-A receptor activity and inhibiting glutamate-mediated neurotransmission at AMPA and kainate receptors. It also blocks voltage-dependent sodium channels, contributing to decreased seizure propagation. Additionally, topiramate inhibits several carbonic anhydrase isozymes, though the clinical relevance of this action remains unclear. |
|---|---|
| Mechanism of action | A seizure is an abnormal and unregulated electrical discharge occurring in the brain. This leads to transient interruption in brain function, manifested by reduced alertness, abnormal sensations, and focal involuntary movements or convulsions. Several types of seizures exist, with common types including tonic-clonic seizures and partial onset seizures. The exact mechanisms by which topiramate exerts pharmacological actions on seizures and migraines are currently not fully characterized. Several properties of this drug, however, are likely to contribute to its therapeutic effects. Topiramate has been observed to exert actions on voltage-dependent sodium channels, GABA receptors, and glutamate receptors. Topiramate stimulates GABA-A receptor activity at brain non-benzodiazepine receptor sites and reduces glutamate activity at both AMPA and kainate receptors. Normally, GABA-A receptors are inhibitory and glutaminergic receptors are stimulatory for neuronal activity. By increasing GABA activity and inhibiting glutamate activity, topiramate blocks neuronal excitability, preventing seizures and migraines. Additionally, it blocks the voltage-dependent sodium channels, further blocking seizure activity. Topiramate has been shown to inhibit various carbonic anhydrase isozymes, but the clinical significance of this is unknown at this time. |
| Pharmacodynamics | Topiramate prevents the occurrence of seizures and prevents migraine symptoms by reducing neural pathway excitability. It is important to note that this drug may cause metabolic acidosis, mood changes, suicidal thoughts and attempts, as well as kidney stones. When topiramate is combined with [valproic acid], it is known to cause hypothermia. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-1 | Humans | agonist |
| Voltage-gated sodium channel alpha subunit | Humans | inhibitor |
| Kainate receptors | Humans | antagonist |
ADME / PK
| Absorption | After a 400mg dose in one clinical trial, topiramate reached maximal concentrations within 1.8-4.3 hours and ranged from 1.73-28.7 ug/mL. Food did not significantly affect the extent of absorption, despite delaying time to peak concentration. In patients with normal creatinine clearance, steady state concentrations are reached within 4 days. The bioavailability of topiramate in tablet form is about 80% compared to a topiramate solution. |
|---|---|
| Half-life | The elimination half-life is reported to be in the range of 19-23 hours. If topiramate is given with enzyme-inducers, the half-life can be reduced to 12-15 hours because of increased metabolism. |
| Protein binding | Topiramate is not highly bound to plasma proteins, with an estimated plasma protein binding of 9-17% according to some studies. The FDA label indicates that the protein binding of topiramate is 15-41%. |
| Metabolism | The metabolites of topiramate are not known to be active. The metabolism of topiramate is characterized by reactions of glucuronidation, hydroxylation and hydrolysis that lead to the production of six minor metabolites. Some of topiramate's metabolites include 2,3-desisopropylidene topiramate, 4,5-desisopropylidene topiramate, 9-hydroxy topiramate, and 10-hydroxy topiramate. |
| Route of elimination | Topiramate is mainly eliminated through the kidneys. About 70-80% of the eliminated dose is found unchanged in the urine. |
| Volume of distribution | The mean apparent volume of distribution of topiramate ranges from 0.6-0.8 L/kg when doses of 100mg to 1200mg are given. Topiramate readily crosses the blood-brain barrier. |
| Clearance | The mean oral plasma clearance of topiramate ranges from 22-36 mL/min while the renal clearance is 17-18 mL/min, according to one pharmacokinetic study. The FDA label for topiramate indicates a similar oral plasma clearance of approximately 20 to 30 mL/min in adults. |
Formulation & handling
- Topiramate is a small molecule formulated primarily for oral administration in various solid and liquid dosage forms.
- It does not require specialized handling for peptide or biologic stability but should be protected from moisture due to its solid state.
- Food intake has minimal impact on absorption; however, ketogenic diets should be avoided to reduce the risk of kidney stones.
Regulatory status
| Lifecycle | The API's key patents expired between 2016 and 2019 in the United States and Canada, indicating that the product is currently in a mature market phase with potential for generic competition in these regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Topiramate is manufactured by numerous companies, including both originator and generic producers, reflecting a broad and diversified manufacturing base. Branded products have a notable presence primarily in the US and Canadian markets, with multiple patents that expired around 2016 to 2019, indicating established generic competition in these regions. The supply chain involves extensive packaging and distribution networks supporting various generic manufacturers across North America. |
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Safety
| Toxicity | The LD50 of intraperitoneal topiramate in the rat is above 1500 mg/kg. Overdose information In a study of 4 healthy adult women taking topiramate, the severity of clinical effects following an overdose ranged from asymptomatic to severe, with no deaths reported. According to the FDA prescribing information for topiramate, an overdose may cause hypotension, severe metabolic acidosis, coma, abdominal pain, visual disturbances, convulsions, drowsiness, speech abnormalities, impaired mentation and coordination, stupor, agitation, dizziness, as well as depression. In the case of a recent ingestion of topiramate, the stomach contents should be emptied through the induction of emesis or gastric lavage. Offer supportive treatment, including activated charcoal and hemodialysis. |
|---|
- Topiramate exhibits low acute toxicity with an intraperitoneal LD50 above 1500 mg/kg in rats
- Overdose may result in severe central nervous system effects including coma, convulsions, and metabolic acidosis
- Handling of spills or accidental ingestion requires prompt supportive interventions such as gastric lavage and administration of activated charcoal
Topiramate 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.
Topiramate API manufacturers & distributors
Compare qualified Topiramate API suppliers worldwide. We currently have 13 companies offering Topiramate API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Chr. Olesen Group | Distributor | Denmark | India | USDMF | 252 products |
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Divis Labs. | Producer | India | India | CoA, USDMF | 47 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Glochem | Producer | India | India | CoA, FDA, GMP, WC | 14 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, USDMF, WC | 98 products |
| Janssen Pharma | Producer | Belgium | Unknown | CoA, USDMF | 63 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| MSN Organics | Producer | India | India | CoA, GMP, USDMF, WC | 21 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, KDMF, MSDS, USDMF | 64 products |
| Signa | Producer | Mexico | Mexico | CoA, USDMF | 42 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Torrent Pharma | Producer | India | India | CoA, USDMF | 34 products |
When sending a request, specify which Topiramate 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 Topiramate 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.
