Cbz (Carbamazepine) API Manufacturers & Suppliers
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Carbamazepine | CAS No: 298-46-4 | GMP-certified suppliers
A medication that supports management of epilepsy, relieves trigeminal neuralgia pain, and stabilizes acute manic or mixed episodes in bipolar I disorder for clinical use.
Therapeutic categories
Primary indications
- Carbamazepine is indicated for the treatment of epilepsy and pain associated with true trigeminal neuralgia
- In particular, carbamazepine has shown efficacy in treating mixed seizures, partial seizures with complex symptoms, and generalized tonic-clonic seizures
- Carbamazepine is also indicated for the treatment of manic episodes and mixed manic-depressive episodes caused by bipolar I disorder
- Some off-label, unapproved uses of carbamazepine include the treatment of alcohol withdrawal syndrome and restless leg syndrome
Product Snapshot
- Carbamazepine is an oral small‑molecule drug available in multiple solid and liquid formulations, with limited use as an injectable powder for solution
- It is used for epilepsy, trigeminal neuralgia pain, and mood stabilization in bipolar I disorder
- It is approved in the US and Canada, with additional investigational status in some regions
Clinical Overview
Its therapeutic effect in epilepsy and neuropathic pain is primarily attributed to activity at voltage‑dependent sodium channels. Carbamazepine decreases high‑frequency neuronal firing, lowers polysynaptic responses, and reduces post‑tetanic potentiation. Experimental models have shown diminished action potentials in thalamic nuclei and inhibition of reflex pathways that modulate facial pain signaling. In bipolar disorder, evidence suggests increased dopamine turnover and enhanced GABAergic tone, although the complete mechanism remains unresolved.
Carbamazepine exhibits dose‑dependent pharmacokinetics with a narrow therapeutic index. It is extensively metabolized, involving multiple CYP isoforms including CYP3A4, CYP1A2, CYP2B6, and CYP2C19, and it acts as both an inducer and substrate for several of these pathways. Autoinduction is clinically relevant and influences steady‑state concentrations. It is also a P‑glycoprotein substrate and inducer. Renal elimination accounts for a substantial portion of metabolite clearance.
Safety considerations include risks of central nervous system depression, hematologic toxicity, hepatic enzyme induction, and clinically significant drug interactions due to broad CYP and UGT induction profiles. A strong association between the HLA‑B*1502 allele and severe cutaneous adverse reactions, including Stevens‑Johnson syndrome and toxic epidermal necrolysis, has been documented in individuals of certain Asian ancestries, warranting genotype screening where applicable.
Common global brand contexts include Tegretol and related formulations.
For API procurement, manufacturers and sourcing teams should verify compliance with pharmacopeial specifications, control of polymorphic form, residual solvent limits, and consistency of particle size distribution, as these parameters can influence bioavailability and regulatory acceptance.
Identification & chemistry
| Generic name | Carbamazepine |
|---|---|
| Molecule type | Small molecule |
| CAS | 298-46-4 |
| UNII | 33CM23913M |
| DrugBank ID | DB00564 |
Pharmacology
| Summary | Carbamazepine primarily modulates neuronal excitability by binding to voltage‑dependent sodium channels and limiting repetitive action‑potential firing. These actions reduce seizure activity and trigeminal neuralgia symptoms, and the drug may also influence dopaminergic and GABAergic pathways relevant to bipolar disorder. Its pharmacology includes additional interactions with other neuronal receptor targets, alongside known variability in response linked to genetic factors. |
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| Mechanism of action | Carbamazepine's mechanism of action is not fully elucidated and is widely debated.One major hypothesis is that carbamazepine inhibits sodium channel firing, treating seizure activity. Animal research studies have demonstrated that carbamazepine exerts its effects by lowering polysynaptic nerve response and inhibiting post-tetanic potentiation. In both cats and rats, carbamazepine was shown to decrease pain caused by infraorbital nerve stimulation. A decrease in the action potential in the nucleus ventralis of the thalamus in the brain and inhibition of the lingual mandibular reflex were observed in other studies after carbamazepine use. Carbamazepine causes the above effects by binding to voltage-dependent sodium channels and preventing action potentials, which normally lead to stimulatory effects on nerves.In bipolar disorder, carbamazepine is thought to increase dopamine turnover and increase GABA transmission, treating manic and depressive symptoms. A common issue that has arisen is resistance to this drug in up to 30% of epileptic patients, which may occur to altered metabolism in patients with variant genotypes.A potential therapeutic target to combat carbamazepine resistance has recently been identified as the EPHX1 gene promoter, potentially conferring resistance to carbamazepine through methylation. |
| Pharmacodynamics | **General effects** Carbamazepine treats seizures and the symptoms of trigeminal neuralgia by inhibiting sodium channels. In bipolar 1 disorder, carbamazepine has been found to decrease mania symptoms in a clinically significant manner according to the Young Mania Rating Scale (YMRS).Carbamazepine has a narrow therapeutic index. **A note on genetic variation and carbamazepine use** In studies of Han Chinese ancestry patients, a pronounced association between the HLA-B*1502 genotype and Steven Johnson syndrome and/or toxic epidermal necrolysis (SJS/TEN) resulting from carbamazepine use was observed. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-gated sodium channel alpha subunit | Humans | inhibitor |
| Neuronal acetylcholine receptor subunit alpha-4 | Humans | |
| Nuclear receptor subfamily 1 group I member 2 | Humans | activator |
ADME / PK
| Absorption | The bioavailability of carbamazepine is in the range of 75-85% of an ingested dose.After one 200 mg oral extended-release dose of carbamazepine in a pharmacokinetic study, the Cmax carbamazepine was measured to be 1.9 ± 0.3 mcg/mL. The Tmax was 19 ± 7 hours. After several doses of 800 mg every 12 hours, the peak concentrations of carbamazepine were measured to be 11.0 ± 2.5 mcg/mL. The Tmax was reduced to 5.9 ± 1.8 hours. Extended-release carbamazepine demonstrated linear pharmacokinetics over a range of 200–800 mg. **Effect of food on absorption** A meal containing high-fat content increased the rate of absorption of one 400 mg dose but not the AUC of carbamazepine.The elimination half-life remained unchanged between fed and fasting state. The pharmacokinetics of an extended-release carbamazepine dose was demonstrated to be similar when administered in the fasted state or with food.Based on these findings, food intake is unlikely to exert significant effects on carbamazepine absorption. |
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| Half-life | The mean elimination half-life of carbamazepine was 35 to 40 hours after one dose of carbamazepine extended-release formulations. The half-life ranged from 12-17 hours after several doses of carbamazepine.One pharmacokinetic study determined the elimination half-life of carbamazepine to range between 27 to 36.8 hours in healthy volunteers. |
| Protein binding | Carbamazepine is 75%-80% bound to plasma proteins.One pharmacokinetic study indicates that it is 72% bound to plasma proteins. |
| Metabolism | Carbamazepine is largely metabolized in the liver. CYP3A4 hepatic enzyme is the major enzyme that metabolizes carbamazepine to its active metabolite, carbamazepine-10,11-epoxide, which is further metabolized to its trans-diol form by the enzyme epoxide hydrolase.Other hepatic cytochrome enzymes that contribute to the metabolism of carbamazepine are CYP2C8, CYP3A5, and CYP2B6.Carbamazepine also undergoes hepatic glucuronidation by UGT2B7 enzyme and several other metabolic reactions occur, resulting in the formation of minor hydroxy metabolites and quinone metabolites.Interestingly, carbamazepine induces its own metabolism.This leads to enhanced clearance, reduced half-life, and a reduction in serum levels of carbamazepine. |
| Route of elimination | After an oral dose of radiolabeled carbamazepine, 72% of the administered radioactive dose was detected in the urine and the remainder of the ingested dose was found in the feces. Carbamazepine is mainly excreted as hydroxylated and conjugated metabolites, and minimal amounts of unchanged drug. |
| Volume of distribution | The volume of distribution of carbamazepine was found to be 1.0 L/kg in one pharmacokinetic study.Another study indicates that the volume of distribution of carbamazepine ranges between 0.7 to 1.4 L/kg.. Carbamazepine crosses the placenta, and higher concentrations of this drug are found in the liver and kidney as opposed to lung and brain tissue.Carbamazepine crosses variably through the blood-brain barrier. |
| Clearance | In a pharmacokinetic study, the apparent oral clearance of carbamazepine was 25 ± 5 mL/min after one dose of carbamazepine and 80 ± 30 mL/min after several doses. |
Formulation & handling
- Oral formulations require solubility‑enhancing approaches due to low aqueous solubility, with extended‑release matrices commonly used to moderate dissolution of this lipophilic small molecule.
- IV use is limited to reconstituted powder for solution, requiring attention to particulate control and suitable cosolvent or pH‑adjusted systems to maintain solubility.
- Handling should consider photo‑ and thermo‑stability of the solid API and its sensitivity to CYP‑modulating excipients or botanicals that may alter metabolic exposure.
Regulatory status
| Lifecycle | The API shows a mixed lifecycle stage in the US and Canada, with early patents long expired and mid‑term protection ending in 2024 while key later‑expiring patents remain active until 2029. This suggests a partially mature market with continued protection in the near term and fuller generic exposure expected once remaining patents lapse. |
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| Markets | Canada, US |
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Supply Chain
| Supply chain summary | Carbamazepine is supplied by a broad set of manufacturers, with legacy originator involvement alongside numerous generic producers that dominate current commercial supply. Branded and generic products are widely established in North American markets, reflecting long-term global availability beyond the US and EU. Core substance patents have long expired, and remaining later‑dated patents relate to specific formulations, indicating that generic competition is already well established. |
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Safety
| Toxicity | Toxicity information Oral LDLO (female): 1920 mg/kg/17W (intermittent); Oral LDLO (male): 54 mg/kg/9D (intermittent) Oral LD50 (rat): 1957 mg/kg Overdose information The initial signs of carbamazepine overdose occur 1-3 hours post ingestion. These signs and symptoms may vary in case of an overdose between carbamazepine and other drugs. Carbamazepine may cause various cardiovascular, neurological, respiratory, urinary symptoms as well as laboratory abnormalities including leukocytosis, reduced leucocytes, acetonuria, and glycosuria. Neuromuscular symptoms may occur initially, followed by mild cardiac symptoms such as tachycardia, hypertension, or hypotension. Higher doses of carbamazepine may cause more severed cardiovascular effects. Restlessness, muscular twitching, tremor, dilated pupils, nystagmus, psychomotor disturbances, and other neurological symptoms may occur. Hyperreflexia in the initial stages of overdose may be followed by hyporeflexia. Nausea, vomiting, urinary retention, dizziness or drowsiness may also occur.In cases of overdose, contact the local poison control center. Ensure to provide supportive and symptomatic treatment, which may include monitoring and careful supervision by a medical professional. The possibility of overdose with multiple drugs must be considered in the case of carbamazepine overdose. Maintain an adequate airway, oxygen, in addition to ventilation. Vital signs should be monitored. |
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- Oral toxicity varies widely across species and sexes, with reported oral LD₅₀ in rats near 1957 mg/kg and markedly lower LDLO values in humans, indicating potential for severe toxicity at comparatively low exposures
- Overexposure can produce early neuromuscular effects (tremor, twitching, nystagmus) followed by cardiovascular instability, including tachycardia, hypertension, or hypotension
- High systemic levels are associated with multisystem effects such as altered reflexes, leukocyte abnormalities, acetonuria, glycosuria, and CNS disturbances including psychomotor impairment and pronounced drowsiness
Carbamazepine 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.
Carbamazepine API manufacturers & distributors
Compare qualified Carbamazepine API suppliers worldwide. We currently have 13 companies offering Carbamazepine API, with manufacturing taking place in 8 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 |
|---|---|---|---|---|---|
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Arevipharma | Producer | Germany | Unknown | CEP, CoA, FDA | 25 products |
| Arshine Pharmaceutical Co... | Distributor | China | China | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GDP, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC, WHO-GMP | 176 products |
| AXXO GmbH | Distributor | Germany | European Union | CEP, CoA, GMP, GDP, MSDS, USDMF | 243 products |
| BAJAJ HEALTHCARE LTD | Producer | India | India | CoA, GMP, WC | 8 products |
| Indukern Chemie AG | Distributor | Switzerland | Unknown | CoA | 13 products |
| Jubilant Pharmova | Producer | India | India | BSE/TSE, CEP, CoA, GMP, ISO9001, JDMF, MSDS, USDMF | 52 products |
| Katsura Chemical | Producer | Japan | Japan | CoA, JDMF | 7 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, JDMF, KDMF, MSDS | 64 products |
| Shizuoka Coffein Co | Producer | Japan | Japan | CoA, JDMF | 8 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA | 762 products |
| Zhejiang Raybow Pharma | Producer | China | China | CoA, JDMF, USDMF | 2 products |
When sending a request, specify which Carbamazepine 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 Carbamazepine 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.
