Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Loxapine API Manufacturers & Suppliers
2 verified results
Commercial-scale Suppliers
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Loxapine | CAS No: 1977-10-2 | GMP-certified suppliers
A medication that manages psychotic disorders, such as schizophrenia, by providing antipsychotic effects to control agitation and behavioral symptoms in key markets including the US, EU, and Canada.
Therapeutic categories
Primary indications
- For the management of the manifestations of psychotic disorders such as schizophrenia
Product Snapshot
- Loxapine is available in multiple formulations including oral tablets and capsules, intramuscular injections, and inhalation aerosols
- It is primarily indicated for the management of psychotic disorders such as schizophrenia
- The product is approved for use in major regulatory markets including the US, EU, and Canada
Clinical Overview
Pharmacodynamically, loxapine functions as a typical antipsychotic with a mechanism involving antagonism of dopamine and serotonin receptors. Specifically, it acts as a dopamine D2 receptor antagonist and also blocks serotonin 5-HT2 receptors. The net effect is believed to result in cortical inhibition that manifests clinically as tranquilization and suppression of aggressive behavior. Although the precise mode of action remains incompletely elucidated, preclinical studies indicate modulatory effects on subcortical inhibitory areas of the brain, correlating with observed calming effects.
Following administration, loxapine exhibits central nervous system depressant activity consistent with its receptor binding profile. Key ADME parameters include absorption via the oral route, distribution to the brain and peripheral tissues, hepatic metabolism primarily through the cytochrome P450 system, and renal and fecal elimination. Its metabolism involves oxidative pathways yielding active metabolites, which may contribute to its therapeutic and side effect profile.
Safety considerations with loxapine use include potential neurotoxicity and risks associated with dopamine antagonism, such as extrapyramidal symptoms, sedation, and the possibility of neuroleptic malignant syndrome. Loxapine has been associated with photosensitivity reactions and carries warnings for serotonin syndrome when combined with serotonergic agents. Caution is advised in patients with hepatic impairment or history of seizures.
Among marketed formulations, loxapine is available as oral tablets and inhalation powder for rapid control of agitation in schizophrenia. Notable brand names include Loxapac and Adasuve (inhalation). Usage contexts largely focus on acute management of schizophrenia symptoms and agitation in psychotic disorders.
For API procurement, ensuring compliance with pharmacopeial standards, particularly regarding purity, residual solvents, and stereochemical consistency, is critical. Due to its complex synthesis and sensitive oxidation-prone structure, sourcing from established manufacturers with validated quality control procedures is recommended to ensure batch-to-batch consistency and regulatory compliance.
Identification & chemistry
| Generic name | Loxapine |
|---|---|
| Molecule type | Small molecule |
| CAS | 1977-10-2 |
| UNII | LER583670J |
| DrugBank ID | DB00408 |
Pharmacology
| Summary | Loxapine is a tricyclic antipsychotic agent that primarily acts as an antagonist at dopamine D2 and serotonin 5-HT2 receptors. Its pharmacodynamic effects include cortical inhibition leading to tranquilization and suppression of aggressive behavior. Loxapine’s therapeutic action is utilized in the management of psychotic disorders such as schizophrenia. |
|---|---|
| Mechanism of action | Loxapine is a dopamine antagonist, and also a serotonin 5-HT2 blocker. The exact mode of action of Loxapine has not been established, however changes in the level of excitability of subcortical inhibitory areas have been observed in several animal species in association with such manifestations of tranquilization as calming effects and suppression of aggressive behavior. |
| Pharmacodynamics | Loxapine, a dibenzoxazepine compound, represents a subclass of tricyclic antipsychotic agents, chemically distinct from the thioxanthenes, butyrophenones, and phenothiazines. Pharmacologically, Loxapine is a tranquilizer for which the exact mode of action has not been established, however, it is believed that by antagonising dopamine and serotonin receptors, there is a marked cortical inhibition which can manifest as tranquilization and suppression of aggression. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 2A | Humans | antagonist |
| Dopamine D2 receptor | Humans | antagonist |
| 5-hydroxytryptamine receptor 2C | Humans | antagonist |
ADME / PK
| Absorption | Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers |
|---|---|
| Half-life | Oral-4 hours |
| Metabolism | Hepatic |
| Route of elimination | Metabolites are excreted in the urine in the form of conjugates and in the feces unconjugated. |
Formulation & handling
- Loxapine is a small molecule available for oral, intramuscular, and respiratory inhalation administration, requiring diverse formulation approaches.
- Formulations should consider moderate water solubility and logP of 3.46 to optimize bioavailability and stability.
- Handling instructions include administering oral forms with food to reduce gastrointestinal irritation and avoiding alcohol due to interaction risks.
Regulatory status
| Lifecycle | The API's key patents in the United States expired or will expire between 2021 and 2024, indicating a transition toward a mature market phase in the US, while products remain marketed in the US, EU, and Canada. This suggests increasing generic competition and established market presence across these regions. |
|---|
| Markets | US, EU, Canada |
|---|
Supply Chain
| Supply chain summary | Loxapine is manufactured and packaged by multiple companies, indicating a diversified supply chain with several originator and generic manufacturers. Branded products like Adasuve are present across the US, EU, and Canadian markets, reflecting a broad global presence. Patent expirations ranging from late 2021 to late 2024 suggest existing or imminent opportunities for generic competition. |
|---|
Safety
| Toxicity | LD<sub>50</sub>=65 mg/kg (Orally in mice) |
|---|
- Handle with appropriate personal protective equipment to prevent ingestion and skin contact
- Toxicity observed at an oral LD₅₀ of 65 mg/kg in mice
- Avoid exposure to minimize risk
Loxapine is a type of Atypical antipsychotics
Atypical antipsychotics belong to the subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various mental disorders, particularly schizophrenia and bipolar disorder. These medications are designed to alleviate the symptoms of psychosis by targeting specific neuroreceptors in the brain.
Unlike traditional antipsychotics, atypical antipsychotics exhibit a different pharmacological profile, providing a more favorable side effect profile and improved efficacy. These medications primarily act on dopamine and serotonin receptors, regulating the neurotransmitter levels in the brain to restore the chemical balance.
The mechanism of action of atypical antipsychotics involves blocking dopamine receptors, particularly D2 receptors, as well as modulating serotonin receptors, notably 5-HT2A receptors. By inhibiting excessive dopamine transmission and enhancing serotonin activity, atypical antipsychotics help reduce hallucinations, delusions, and other psychotic symptoms.
Some commonly used atypical antipsychotics include risperidone, olanzapine, quetiapine, and aripiprazole. These APIs are typically formulated into oral tablets or capsules for convenient administration.
Despite their effectiveness, atypical antipsychotics may have potential side effects such as weight gain, metabolic abnormalities, sedation, and extrapyramidal symptoms. Therefore, close monitoring and individualized treatment plans are essential to ensure optimal therapeutic outcomes.
In conclusion, atypical antipsychotics are a crucial subcategory of APIs used in the treatment of mental disorders. Their distinct pharmacological profile and mechanism of action make them valuable in managing psychosis while minimizing adverse effects.
Loxapine (Atypical 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.
Loxapine API manufacturers & distributors
Compare qualified Loxapine API suppliers worldwide. We currently have 2 companies offering Loxapine 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 |
|---|---|---|---|---|---|
| Centaur Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 40 products |
| Medichem | Producer | Spain | Unknown | CoA, USDMF | 39 products |
When sending a request, specify which Loxapine 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 Loxapine 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.
