Lamotrigine API Manufacturers & Suppliers
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Lamotrigine | CAS No: 84057-84-1 | GMP-certified suppliers
A medication that supports control of partial and generalized seizures, including Lennox‑Gastaut syndrome, and helps maintain stability in bipolar I disorder.
Therapeutic categories
Primary indications
- Lamotrigine is indicated as adjunctive therapy for the following seizure types in patients ≥2 years of age: partial seizures, primary generalized tonic-clonic seizures, and generalized seizures due to Lennox-Gastaut syndrome
- It is also indicated for the process of conversion to drug monotherapy for those at least 16 years of age or older with partial seizures and currently are receiving treatment with carbamazepine, phenytoin, phenobarbital, primidone, or valproate as the single antiepileptic drug (AED)
Product Snapshot
- Lamotrigine is an oral small‑molecule API supplied primarily in multiple tablet presentations, including immediate‑release, chewable/dispersible, soluble, and extended‑release forms
- It is used for epilepsy management across several seizure types and for maintenance treatment of bipolar I disorder
- It is approved in the US and Canada, with both approved and investigational statuses noted for specific formulations
Clinical Overview
Lamotrigine exerts antiseizure and mood‑stabilizing effects primarily through inhibition of voltage‑sensitive sodium channels, promoting stabilization of presynaptic neuronal membranes and reducing pathologic glutamate release. Its pharmacologic profile also includes weak affinity for several neurotransmitter receptors at high micromolar concentrations, along with evidence for inhibition of R‑type calcium currents, which may contribute to its anticonvulsant activity.
Absorption following oral administration is generally efficient, and lamotrigine undergoes predominant hepatic glucuronidation with renal elimination of metabolites. Conditions that reduce glucuronidation, such as hepatic impairment or coadministration with valproate, increase systemic exposure. Enzyme‑inducing antiepileptic drugs enhance clearance. The drug’s 2‑N‑methyl metabolite can prolong PR and QRS intervals at high concentrations; although typically present at trace levels, accumulation is possible in impaired metabolism.
Safety considerations include risk of severe cutaneous adverse reactions, particularly with rapid dose escalation or concomitant valproate. Central nervous system effects such as dizziness or diplopia are dose related. Cardiovascular conduction effects are uncommon but clinically relevant in susceptible populations.
Lamotrigine is marketed in many regions as immediate‑release and extended‑release formulations. When procuring the active pharmaceutical ingredient, sourcing teams should verify compliance with current pharmacopoeial specifications, control of polymorphic form, and confirmed impurity profiles supporting consistent glucuronidation pathways and stability.
Identification & chemistry
| Generic name | Lamotrigine |
|---|---|
| Molecule type | Small molecule |
| CAS | 84057-84-1 |
| UNII | U3H27498KS |
| DrugBank ID | DB00555 |
Pharmacology
| Summary | Lamotrigine primarily modulates neuronal excitability by inhibiting voltage‑gated sodium channels, stabilizing presynaptic membranes, and reducing glutamate release. It also exhibits weaker interactions with multiple receptor families and may inhibit R‑type calcium currents, contributing to its anticonvulsant and mood‑stabilizing effects. Minor metabolites have been associated with cardiac conduction effects, though these are typically present at low levels under normal metabolic conditions. |
|---|---|
| Mechanism of action | The exact mechanism of action of lamotrigine is not fully elucidated, as it may exert cellular activities that contribute to its efficacy in a range of conditions. Although chemically unrelated, lamotrigine actions resemble those of phenytoin and carbamazepine, inhibiting voltage-sensitive sodium channels, stabilizing neuronal membranes, thereby modulating the release of presynaptic excitatory neurotransmitters. Lamotrigine likely acts by inhibiting sodium currents by selective binding to the inactive sodium channel, suppressing the release of the excitatory amino acid, glutamate. The mechanism of action of lamotrigine in reducing anticonvulsant activity is likely the same in managing bipolar disorder. Studies on lamotrigine have identified its binding to sodium channels in a fashion similar to local anesthetics, which could explain the demonstrated clinical benefit of lamotrigine in some neuropathic pain states. Lamotrigine displays binding properties to several different receptors. In laboratory binding assays, it demonstrates weak inhibitory effect on the serotonin 5-HT3 receptor. Lamotrigine also weakly binds to Adenosine A1/A2 receptors, α1/α2/β adrenergic receptors, dopamine D1/D2 receptors, GABA A/B receptors, histamine H1 receptors, κ-opioid receptor (KOR), mACh receptors and serotonin 5-HT2 receptors with an IC50>100 µM. Weak inhibitory effects were observed at sigma opioid receptors.An in vivo study revealed evidence that lamotrigine inhibits Cav2.3 (R-type) calcium currents, which may also contribute to its anticonvulsant effects. |
| Pharmacodynamics | Lamotrigine likely prevents seizures and prevents mood symptoms via stabilizing presynaptic neuronal membranes and preventing the release of excitatory neurotransmitters such as glutamate, which contribute to seizure activity. A note on cardiovascular effects The metabolite of lamotrigine, 2-N-methyl metabolite (formed by glucuronidation), is reported to cause dose-dependent prolongations of the PR interval, widening of the QRS complex, and at higher doses, complete AV block. Although this harmful metabolite is only found in trace amounts in humans, plasma concentrations may increase in conditions that cause decreased drug glucuronidation, such as liver disease. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent R-type calcium channel subunit alpha-1E (CACNA1E) | Humans | inhibitor |
| Voltage-gated sodium channel alpha subunit | Humans | inhibitor |
| Adenosine receptor A1 | Humans | inhibitor |
ADME / PK
| Absorption | Lamotrigine is rapidly and entirely absorbed with minimal first-pass metabolism effects, with a bioavailability estimated at 98%. Cmax is reached in the range of 1.4 to 4.8 hours post-dose, but this depends on the dose administered, concomitant medications, and epileptic status. The rate and extent of lamictal absorption is considered equivalent between the compressed tablet form taken with water to that of the chewable dispersible tablets, taken with or without water. |
|---|---|
| Half-life | The average elimination half-life of lamotrigine ranges from approximately 14-59 hours. The value is dependent on the dose administered, concomitant drug therapy, as well as disease status.One pharmacokinetic study revealed a half-life of 22.8 to 37.4 hours in healthy volunteers. It also reported that enzyme-inducing antiepileptic drugs such as pheobarbital, phenytoin, or carbamazepine decrease the half-life of lamotrigine. On the other hand, valproic acid increases the half-life of lamotrigine (in the range of 48-59 hours). |
| Protein binding | The plasma protein binding of lamotrigine is estimated at 55%.This drug is not expected to undergo clinically significant interactions with other drugs via competition for protein binding sites due its lower protein binding. |
| Metabolism | Lamotrigine is mainly glucuronidated, forming 2-N-glucuronide conjugate, a pharmacologically inactive metabolite.The total radioactivity detected after a 240mg radiolabeled dose of lamotrigine during clinical trials were as follows: lamotrigine as unchanged drug(10%), a 2-N-glucuronide (76%), a 5-N-glucuronide (10%), a 2-N-methyl metabolite (0.14%), as well as various other minor metabolites (4%). |
| Route of elimination | Lamotrigine is excreted in both the urine and feces.Following oral administration of 240 mg radiolabelled lamotrigine, about 94% of total drug and its metabolites administered is recovered in the urine and 2% is recovered in the feces.One pharmacokinetic study recovered 43 to 87% of a lamotrigine dose in the urine mainly as glucuronidated metabolites.2-N-glucuronide is mainly excreted in the urine. |
| Volume of distribution | The mean apparent volume of distribution (Vd/F) of lamotrigine following oral administration ranges from 0.9 to 1.3 L/kg and is independent of dose administered. Lamotrigine accumulated in the kidney of the male rat, and likely behaves in a similar fashion in humans. Lamotrigine also binds to tissues containing melanin, such as the eyes and pigmented skin. |
| Clearance | The mean apparent plasma clearance (Cl/F) ranges from 0.18 to 1.21 mL/min/kg. The values vary depending on dosing regimen, concomitant antiepileptic medications, and disease state of the individual.In one study, healthy volunteers on lamictal monotherapy showed a clearance of about 0.44 mL/min/kg after a single dose. |
Formulation & handling
- Oral small‑molecule API with moderate lipophilicity and low aqueous solubility, requiring solubilization or dispersibility strategies for suspension and ODT/chewable formats.
- Stable solid suitable for conventional and extended‑release tablets; ER performance depends on controlling its pH‑independent absorption and dissolution‑rate limitations.
- No food‑related absorption impact, allowing flexible administration without special formulation adjustments for fed‑state variability.
Regulatory status
| Lifecycle | Most early Canadian and U.S. patent protection for the API expired in 2012, but several U.S. patents remain active through 2028. As a result, the product is generally mature in Canada while portions of the U.S. market remain under later‑expiring exclusivities. |
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| Markets | Canada, US |
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Supply Chain
| Supply chain summary | Lamotrigine’s supply landscape is mature, with an originator lineage from GlaxoSmithKline and extensive participation by numerous generic manufacturers and repackagers supporting large‑scale distribution. Branded and generic products are widely available in the US and Canada, reflecting well‑established global market penetration. Core substance patents expired more than a decade ago, and although some later‑filed US patents extend into the late 2020s, the market already supports broad generic competition. |
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Safety
| Toxicity | The oral LD50 in mouse and rat is 205 mg/kg and 245 mg/kg, respectively.[MSDS] Fatal cases of overdose of up to 15g of lamotrigine have been reported. Overdose with lamotrigine has been manifested by ataxia, nystagmus, increased seizures, decreased level of consciousness, coma, and intraventricular conduction delay. Though no known antidote exists for lamotrigine, hospitalization and general supportive measures should be employed in the case of a suspected lamotrigine overdose. Gastric lavage and emesis may be warranted with simultaneous protection of the airway. It is uncertain at this time whether hemodialysis is an effective means of removing lamotrigine from the sytemic circulation. |
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- Acute toxicity is moderate, with reported oral LD50 values of 205 mg/kg (mouse) and 245 mg/kg (rat), indicating a defined hazard profile at relatively low gram‑scale exposures
- Documented overdose cases (up to ~15 g) have resulted in CNS depression, ataxia, nystagmus, seizure exacerbation, coma, and intraventricular conduction delay, underscoring the compound’s narrow safety margin at high systemic levels
- No specific antidote is identified
Lamotrigine 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.
Lamotrigine API manufacturers & distributors
Compare qualified Lamotrigine API suppliers worldwide. We currently have 24 companies offering Lamotrigine API, with manufacturing taking place in 9 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 |
| Cipla | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF, WC | 164 products |
| Divis Labs. | Producer | India | India | CoA, FDA, GMP, ISO9001, Other, WC | 47 products |
| Gedeon Richter | Producer | Hungary | Hungary | CoA, GMP | 48 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| GVK Biosciences Pvt Ltd | Producer | India | India | CEP, CoA, FDA, GMP, WC | 10 products |
| Ipca Labs. | Producer | India | India | CoA, GMP | 69 products |
| Jubilant Pharmova | Producer | India | India | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF | 52 products |
| Kromozome | Distributor | India | India | CoA, FDA, GMP, MSDS | 17 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Medichem | Producer | Spain | Unknown | CoA, USDMF | 39 products |
| Menadiona, S.L. | Producer | Spain | Spain | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF, WHO-GMP | 15 products |
| Mylan | Producer | India | India | CEP, CoA, USDMF, WC | 201 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, JDMF, KDMF, MSDS, USDMF | 64 products |
| Praveen Labs | Producer | India | India | CoA, GMP, WC | 3 products |
| Rpg Life Sciences | Producer | India | India | CoA, GMP, WC | 13 products |
| SEDANAH | Distributor | Jordan | World | CoA, GMP | 70 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Sun Pharma | Producer | India | India | CoA, GMP, WC | 219 products |
| Syn-tech Chem | Producer | Taiwan | Taiwan | CoA, JDMF, USDMF | 22 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Torrent Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 34 products |
| Unichem Labs. | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 62 products |
| Zhejiang Supor | Producer | China | China | CoA, USDMF, WC | 13 products |
When sending a request, specify which Lamotrigine 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 Lamotrigine 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.
