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Methotrimeprazine | CAS No: 60-99-1 | GMP-certified suppliers
A medication that treats psychosis, including schizophrenia, and manages manic phases of bipolar disorder with antipsychotic and central nervous system effects.
Therapeutic categories
Primary indications
- For the treatment of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder
Product Snapshot
- Methotrimeprazine is available as oral tablets and liquid solutions, as well as injectable formulations for intramuscular and intravenous administration
- It is indicated for the treatment of psychosis, including schizophrenia and manic phases of bipolar disorder
- The product is approved and investigational in the Canadian market
Clinical Overview
Clinically, methotrimeprazine is indicated primarily for the management of psychotic disorders, including schizophrenia, and for controlling manic episodes within bipolar disorder. Its antipsychotic efficacy is primarily attributed to antagonism of dopamine D2 receptors in the brain, which modulates dopaminergic neurotransmission implicated in psychosis. Additionally, methotrimeprazine exhibits affinity for serotonin 5-HT2 receptors, which may contribute to its therapeutic profile. The compound also antagonizes alpha-1 adrenergic receptors and exhibits anticholinergic and antihistaminic actions, influencing its safety and side effect profile.
Absorption, distribution, metabolism, and excretion (ADME) parameters for methotrimeprazine are aligned with those typical of phenothiazine derivatives. It undergoes hepatic metabolism, involving cytochrome P450 isoenzymes such as CYP2D6 and CYP2E1, functioning both as substrate and inhibitor, which may impact drug-drug interaction potential. Renal and hepatic clearance contribute to elimination.
Safety considerations include risk of neurotoxic effects, potential QTc interval prolongation, photosensitivity reactions, and metabolic disturbances like hyperglycemia. Anticholinergic and adrenergic blockade can lead to side effects such as sedation, orthostatic hypotension, and tachycardia. These factors necessitate careful dose optimization and monitoring during therapy.
Notable formulations containing methotrimeprazine may be positioned within therapy regimens in regions where it is approved for use, though its availability varies globally. It is classified as a first-generation (typical) antipsychotic agent.
From an API sourcing perspective, methotrimeprazine requires stringent quality control due to its narrow therapeutic index and complex pharmacology. Suppliers should ensure compliance with pharmacopeial standards and provide comprehensive impurity profiles. Stability, batch-to-batch consistency, and adherence to Good Manufacturing Practices (GMP) are critical to guarantee reliable supply for pharmaceutical formulation development.
Identification & chemistry
| Generic name | Methotrimeprazine |
|---|---|
| Molecule type | Small molecule |
| CAS | 60-99-1 |
| UNII | 9G0LAW7ATQ |
| DrugBank ID | DB01403 |
Pharmacology
| Summary | Methotrimeprazine is a phenothiazine antipsychotic that primarily antagonizes dopamine receptors (D1-D5) and serotonin 5-HT2 receptors, contributing to its efficacy in treating psychosis and manic episodes. It also exhibits affinity for histamine H1, muscarinic acetylcholine, and alpha-adrenergic receptors, underlying its broad central nervous system effects. |
|---|---|
| Mechanism of action | Methotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role. |
| Pharmacodynamics | Methotrimeprazine is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604) |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine D2 receptor | Humans | antagonist |
| Dopamine D1 receptor | Humans | antagonist |
| Dopamine D5 receptor | Humans | antagonist |
ADME / PK
| Absorption | Methotrimeprazine has an incomplete oral bioavailability, because it undergoes considerable first-pass-metabolism in the liver. Oral bioavailability is approximately 50 to 60%. |
|---|---|
| Half-life | Approximately 20 hours. |
| Metabolism | Hepatic. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxid-, a glucuronid- and a demethyl-moiety. |
Formulation & handling
- Methotrimeprazine is a small molecule phenothiazine available for oral, intramuscular, and intravenous administration.
- Formulations include coated and film-coated tablets and solutions, with oral forms advised to be taken with food to minimize gastrointestinal irritation.
- The compound has low water solubility and moderate lipophilicity (LogP 4.25), requiring consideration of solubilization in parenteral formulations.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is approaching patent expiry in Canada, indicating entry into a mature market phase with potential for generic competition. Market activity is expected to shift towards lifecycle management and cost optimization strategies. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | Methotrimeprazine is supplied by multiple originator companies primarily serving the Canadian market, with several branded products available under similar names. The presence of branded formulations indicates established manufacturing capabilities, though limited global coverage beyond Canada is observed. Patent expiration status suggests the potential for generic competition within this regional market. |
|---|
Safety
| Toxicity | Symptoms of overdose include convulsions, spastic movements, and coma. |
|---|
- Overdose may result in convulsions, spastic movements, and coma
- Handle with care to avoid exposure that could lead to neurotoxic effects
- Use appropriate protective equipment to minimize occupational exposure risk
Methotrimeprazine is a type of Classic antipsychotics
Classic antipsychotics, also known as first-generation antipsychotics (FGAs), are a prominent subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of psychiatric disorders. These medications are primarily prescribed to manage symptoms associated with conditions such as schizophrenia and bipolar disorder.
Classic antipsychotics work by blocking dopamine receptors in the brain, which helps to alleviate symptoms like hallucinations, delusions, and disorganized thinking. Some commonly used classic antipsychotics include chlorpromazine, haloperidol, and fluphenazine.
These APIs exert their therapeutic effects by antagonizing dopamine D2 receptors, thereby reducing the activity of this neurotransmitter in specific brain regions. This mechanism helps to restore the delicate balance of dopamine and other neurotransmitters, leading to an improvement in symptoms of psychosis.
Despite being the first generation of antipsychotics developed, classic antipsychotics still have a significant role in modern medicine. However, their use has somewhat declined due to the advent of second-generation antipsychotics (SGAs) that offer a more favorable side effect profile. Nonetheless, classic antipsychotics remain an essential treatment option, particularly in situations where SGAs may be contraindicated or ineffective.
It is crucial to note that the use of classic antipsychotics requires careful monitoring due to potential side effects, such as extrapyramidal symptoms (EPS), sedation, and tardive dyskinesia. Physicians must assess the risk-benefit ratio and tailor the treatment approach to each patient's specific needs.
In summary, classic antipsychotics represent a notable subcategory of pharmaceutical APIs utilized in the treatment of psychiatric disorders. While their usage has somewhat declined, they continue to play a vital role in managing symptoms associated with conditions like schizophrenia, providing valuable options for healthcare providers and patients alike.
Methotrimeprazine (Classic antipsychotics), classified under Antipsychotics
Antipsychotics belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category used to treat psychiatric disorders such as schizophrenia, bipolar disorder, and other related conditions. These medications play a crucial role in managing symptoms associated with psychosis, including hallucinations, delusions, and disorganized thinking.
Antipsychotics work by modulating the levels of neurotransmitters in the brain, particularly dopamine and serotonin. They can be categorized into two classes: first-generation (typical) antipsychotics and second-generation (atypical) antipsychotics. Typical antipsychotics primarily target dopamine receptors, while atypical antipsychotics also affect serotonin receptors.
The pharmaceutical API category of antipsychotics includes various well-known drugs, such as haloperidol, chlorpromazine, risperidone, quetiapine, and olanzapine. These APIs are often formulated into different dosage forms, including tablets, capsules, injections, and oral suspensions, to provide flexibility in administration and patient-specific needs.
Antipsychotics offer relief from psychotic symptoms by stabilizing the imbalanced neurotransmitter activity in the brain. However, they may also have certain side effects, such as sedation, weight gain, extrapyramidal symptoms, and metabolic disturbances. It is essential for healthcare professionals to carefully monitor patients receiving antipsychotic treatment to optimize therapeutic benefits while minimizing adverse effects.
In summary, antipsychotics are a vital category of pharmaceutical APIs used to manage psychiatric disorders by modulating neurotransmitter activity in the brain. Their effectiveness in treating psychosis has made them a cornerstone of mental health treatment, providing much-needed relief to individuals suffering from these conditions.
Methotrimeprazine API manufacturers & distributors
Compare qualified Methotrimeprazine API suppliers worldwide. We currently have 2 companies offering Methotrimeprazine API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Sanofi | Producer | France | Unknown | CEP, CoA, FDA, GMP | 93 products |
| ZCL Chemicals | Producer | India | India | CEP, CoA, Other, FDA, ISO9001 | 30 products |
When sending a request, specify which Methotrimeprazine 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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