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Trifluoperazine | CAS No: 117-89-5 | GMP-certified suppliers
A medication that treats anxiety disorders, agitation, and depressive symptoms secondary to anxiety, offering antipsychotic and antiemetic benefits for central nervous system conditions.
Therapeutic categories
Primary indications
- For the treatment of anxiety disorders, depressive symptoms secondary to anxiety and agitation
Product Snapshot
- Trifluoperazine is available primarily as oral tablets and syrup formulations, with an injectable solution for intramuscular administration
- It is indicated for the treatment of anxiety disorders, depressive symptoms secondary to anxiety, and agitation
- The product is approved and marketed in Canada and the United States
Clinical Overview
Clinically, trifluoperazine is indicated for the treatment of anxiety disorders, including depressive symptoms secondary to anxiety and agitation. It is also employed in the management of schizophrenia and other psychotic disorders. However, its efficacy has not been demonstrated in addressing behavioral complications associated with mental retardation.
The pharmacological activity of trifluoperazine is attributed to its antagonism of postsynaptic dopaminergic receptors, specifically dopamine D1 and D2 receptors within the mesolimbic pathways of the brain. In blocking these receptors, it modulates dopaminergic neurotransmission, which contributes to its antipsychotic effects. Additional pharmacodynamic actions include suppression of hypothalamic and hypophyseal hormone release and depression of the reticular activating system, influencing basal metabolism, body temperature regulation, wakefulness, vasomotor tone, and emesis control.
Key pharmacokinetic considerations include its metabolism as a substrate of cytochrome P450 enzymes, notably CYP1A2, and involvement with UGT1A4-mediated pathways. Trifluoperazine also interacts with P-glycoprotein transport mechanisms as both an inhibitor and substrate. These factors are relevant for potential drug-drug interactions and dosing considerations.
Safety and toxicity profiles of trifluoperazine encompass neurotoxic risks common to typical antipsychotics, including extrapyramidal symptoms and photosensitivity reactions. The compound’s classification under photosensitizing agents and neurotoxic agents necessitates vigilance in clinical monitoring. Its antiadrenergic activities may contribute to vascular side effects such as hypotension or hypertension.
Trifluoperazine is marketed under various global brands and remains in approved clinical use despite the availability of newer atypical antipsychotics. Its procurement as an active pharmaceutical ingredient (API) requires adherence to stringent quality standards, with emphasis on purity, impurity profiling, and compliance with regulatory guidelines for phenothiazine derivatives. Due to its metabolism via CYP pathways, consistent API quality is critical to ensure predictable pharmacokinetics and therapeutic outcomes.
Identification & chemistry
| Generic name | Trifluoperazine |
|---|---|
| Molecule type | Small molecule |
| CAS | 117-89-5 |
| UNII | 214IZI85K3 |
| DrugBank ID | DB00831 |
Pharmacology
| Summary | Trifluoperazine is a phenothiazine antipsychotic that primarily antagonizes postsynaptic mesolimbic dopamine D1 and D2 receptors, modulating dopaminergic neurotransmission. It also depresses hypothalamic and hypophyseal hormone release and influences the reticular activating system, affecting basal metabolism, wakefulness, and autonomic functions. The compound targets multiple proteins including dopamine receptors, calmodulin, and adrenergic receptors, and is used for managing schizophrenia, psychotic disorders, and anxiety-related symptoms. |
|---|---|
| Mechanism of action | Trifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. |
| Pharmacodynamics | Trifluoperazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Trifluoperazine has not been shown effective in the management of behaviorial complications in patients with mental retardation. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine D2 receptor | Humans | antagonist |
| Neuron-specific vesicular protein calcyon | Humans | antagonist |
| Alpha-1A adrenergic receptor | Humans | antagonist |
ADME / PK
| Half-life | 10-20 hours |
|---|---|
| Metabolism | Hepatic. |
Formulation & handling
- Trifluoperazine is a small molecule phenothiazine available for oral and intramuscular administration, primarily formulated as tablets and injections.
- Low water solubility and high lipophilicity (LogP 4.66) should be considered during formulation development to optimize bioavailability.
- Avoid concurrent use with alcohol due to potentiation of CNS depressant effects; stability under normal storage conditions is typical for solid oral dosage forms.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has reached patent expiry in both the US and Canada, allowing for generic competition. As a result, the product is in a mature market phase in these regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for trifluoperazine includes multiple originator and generic manufacturers such as GlaxoSmithKline, Sandoz, and Mylan, indicating a well-established supply base. Branded products are predominantly marketed in North America, specifically the US and Canada. Given the presence of numerous generic manufacturers and the availability of various dosages under different brand names, patent expiry has likely enabled established generic competition in this market. |
|---|
Safety
| Toxicity | Symptoms of overdose include agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, and restlessness. |
|---|
- Exposure may cause central nervous system depression and respiratory difficulties
- Ensure adequate ventilation during handling
- In case of accidental overdose, symptoms can include convulsions, irregular heart rate, and hypotension
Trifluoperazine 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.
Trifluoperazine (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.
Trifluoperazine API manufacturers & distributors
Compare qualified Trifluoperazine API suppliers worldwide. We currently have 2 companies offering Trifluoperazine API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Anphar Labs. | Producer | India | India | CoA, WC | 5 products |
| ZCL Chemicals | Producer | India | India | CoA, Other, FDA, ISO9001 | 30 products |
When sending a request, specify which Trifluoperazine 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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