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Mexiletine | CAS No: 31828-71-4 | GMP-certified suppliers
A medication that treats ventricular tachycardia and premature ventricular beats while preventing ventricular fibrillation to support cardiac arrhythmia management.
Therapeutic categories
Primary indications
- For the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation
Product Snapshot
- Mexiletine is formulated primarily as an oral small molecule available in capsule form, with additional injectable solution presentations
- It is indicated for the management of ventricular tachycardia, symptomatic premature ventricular beats, and prevention of ventricular fibrillation
- Mexiletine holds approved regulatory status in Canada, the US, and the EU, with some investigational uses also noted
Clinical Overview
Pharmacodynamically, mexiletine exhibits a rapid onset and offset of action, with minimal effects on cardiac function at slower heart rates, but increased activity at elevated heart rates. It acts by selectively inhibiting the fast inward sodium current responsible for the initiation and propagation of cardiac action potentials (Phase 0), thereby reducing the maximal rate of depolarization. Mexiletine shortens action potential duration and decreases ventricular refractoriness, specifically lowering the effective refractory period in Purkinje fibers with a lesser magnitude than the reduction in action potential duration. This leads to an increased ERP/APD ratio, which is believed to contribute to its antiarrhythmic efficacy. Importantly, mexiletine does not significantly affect resting membrane potential, sinus node automaticity, left ventricular contractile function, systolic arterial pressure, AV conduction velocity, or QRS and QT intervals.
In terms of metabolism, mexiletine is a substrate for multiple cytochrome P450 enzymes, including CYP1A2, CYP2B6, CYP2D6, CYP2E1, and CYP3A4 isoforms. It also acts as a moderate inhibitor of CYP1A2, which necessitates consideration of potential drug-drug interactions during co-administration with other CYP1A2 substrates or inhibitors.
Safety considerations include monitoring for adverse effects associated with Class Ib antiarrhythmics, such as neurological symptoms or gastrointestinal disturbances. Caution is advised in patients with impaired hepatic function due to metabolic clearance via hepatic CYP enzymes. Mexiletine is approved for clinical use in several countries and is utilized primarily in cardiac arrhythmia management.
From an API sourcing perspective, quality control should focus on stringent verification of chemical identity as a phenol ether compound, purity standards to limit impurities and degradation products, and compliance with pharmacopeial requirements. Supply chain stability and regulatory compliance are critical due to mexiletine’s role as a critical cardiac therapy agent.
Identification & chemistry
| Generic name | Mexiletine |
|---|---|
| Molecule type | Small molecule |
| CAS | 31828-71-4 |
| UNII | 1U511HHV4Z |
| DrugBank ID | DB00379 |
Pharmacology
| Summary | Mexiletine is a Class Ib antiarrhythmic agent that inhibits cardiac sodium channels, reducing the inward sodium current responsible for action potential initiation and conduction. It shortens action potential duration, decreases refractoriness, and modulates impulse conduction in ventricular tissues without significantly impacting resting membrane potential or normal conduction parameters. Mexiletine's pharmacodynamics feature use-dependent sodium channel blockade, with increased effects at higher heart rates, targeting ventricular arrhythmias. |
|---|---|
| Mechanism of action | Mexiletine, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. It achieves this reduced sodium current by inhibiting sodium channels. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals |
| Pharmacodynamics | Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sodium channel protein type 5 subunit alpha | Humans | inhibitor |
| Aryl hydrocarbon receptor | Humans | agonist |
ADME / PK
| Absorption | Well absorbed (bioavailability 90%) from the gastrointenstinal tract. |
|---|---|
| Half-life | 10-12 hours |
| Protein binding | 50-60% |
| Metabolism | Primarily hepatic (85%) via CYP2D6 and CYP1A2 (primarily CYP2D6). |
| Route of elimination | Approximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%. |
| Volume of distribution | * 5 to 7 L/lg |
Formulation & handling
- Mexiletine is a small molecule suitable for oral administration, commonly formulated as capsules.
- It exhibits moderate water solubility and lipophilicity (LogP 2.46), influencing its dissolution and absorption profiles.
- Oral dosing should consider co-administration with food to minimize gastrointestinal irritation.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is currently marketed in Canada, the US, and the EU, with primary patent protections expiring between 2023 and 2025, indicating it is entering a mature market phase with potential for generic competition. Market presence is established, with ongoing regulatory approvals and post-patent lifecycle management activities. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Mexiletine includes multiple originator companies with significant roles, such as Sandoz, Teva, Watson, and Boehringer Ingelheim. Branded products are present across major markets including the US, EU, and Canada. Patent expirations have led to the presence of generic competition from numerous packagers, indicating an established generic market for Mexiletine. |
|---|
Safety
| Toxicity | Symptoms of overdose include nausea, hypotension, sinus bradycardia, paresthesia, seizures, bundle branch block, AV heart block, asystole, ventricular tachyarrythmia, including ventricular fibrillation, cardiovascular collapse, and coma. |
|---|
- Exposure may cause cardiovascular effects including bradycardia and arrhythmias
- Overdose symptoms include neurological and cardiac disturbances such as seizures and heart block
- Handle with appropriate controls to prevent accidental overdose and associated toxicity
Mexiletine is a type of Adrenergic agents
Adrenergic agents are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that target the adrenergic system in the body. This system is responsible for regulating various physiological responses, including heart rate, blood pressure, and smooth muscle contraction.
Adrenergic agents can be further divided into two main groups: adrenergic agonists and adrenergic antagonists. Adrenergic agonists stimulate the adrenergic receptors, leading to an increase in sympathetic nervous system activity. This can result in effects such as vasoconstriction, bronchodilation, and increased heart rate. Adrenergic agonists are commonly used in the treatment of conditions such as asthma, hypotension, and cardiac arrest.
On the other hand, adrenergic antagonists block the adrenergic receptors, thereby inhibiting the effects of sympathetic nervous system activation. These agents are often employed to lower blood pressure, treat certain heart conditions, and manage symptoms associated with conditions like benign prostatic hyperplasia. Adrenergic antagonists can be further classified into alpha-adrenergic antagonists and beta-adrenergic antagonists, based on their selectivity for different adrenergic receptor subtypes.
Pharmaceutical companies extensively utilize adrenergic agents as key components in the development of various medications. Adrenergic APIs offer targeted effects on the adrenergic system, allowing for precise modulation of physiological responses. The understanding of adrenergic agents and their mechanisms of action is vital for the design and optimization of drugs used in the treatment of numerous medical conditions. Researchers and scientists continue to explore and innovate within this subcategory to develop new adrenergic agents with enhanced efficacy and fewer side effects, ultimately improving patient outcomes.
Mexiletine (Adrenergic agents), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Mexiletine API manufacturers & distributors
Compare qualified Mexiletine API suppliers worldwide. We currently have 6 companies offering Mexiletine 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 |
|---|---|---|---|---|---|
| AGC Pharma Chemicals | Distributor | Spain | Spain | CEP, CoA, GMP, USDMF | 4 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Iwaki Seiyaku | Producer | Japan | Japan | CoA, JDMF | 21 products |
| Medichem | Producer | Spain | Unknown | CoA, GMP, USDMF | 39 products |
| Metapharmaceutical Indust... | Producer | Spain | Spain | BSE/TSE, CEP, CoA, GDP, GMP, MSDS | 21 products |
| Tooba Pharmaceuticals Pri... | Producer | India | India | BSE/TSE, CoA, FDA, GMP, HALAL, ISO14001, ISO9001, MSDS, WHO-GMP | 7 products |
When sending a request, specify which Mexiletine 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.).
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