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- Antipsychotics
- Classic antipsychotics
- Zuclopenthixol
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Zuclopenthixol | CAS No: 53772-83-1 | GMP-certified suppliers
A medication that manages acute psychoses including mania and schizophrenia, providing antipsychotic benefits primarily for short-term clinical use in psychiatric settings.
Therapeutic categories
Primary indications
- Used in the management of acute psychoses such as mania or schizophrenia
- However, the use of zuclopenthixol acetate in psychiatric emergencies as an alternative to standard treatments (haloperidol, clotiapine, etc
- ) should be cautioned, since well executed and documented trials of zuclopenthixol acetate for this use have yet to be conducted
- Zuclopenthixol acetate is not intended for long-term use
Product Snapshot
- Zuclopenthixol is available in multiple formulation types including oral film-coated tablets and parenteral injections
- It is primarily indicated for managing acute psychoses such as mania and schizophrenia
- The product is approved for use in the Canadian market and remains investigational elsewhere
Clinical Overview
Pharmacologically, zuclopenthixol acts mainly through antagonism of dopamine receptors D1 and D2, which underlies its antipsychotic effects. Additionally, it exhibits significant affinity for alpha-1 adrenergic and serotonin 5-HT2 receptors, while displaying weaker activity at histamine H1 receptors and minimal binding to muscarinic cholinergic and alpha-2 adrenergic receptors. This receptor interaction profile contributes to both therapeutic outcomes and side effect considerations.
Zuclopenthixol is metabolized predominantly by cytochrome P450 isoenzyme 2D6. This metabolic pathway may have implications for drug-drug interactions and variability in patient responses. Due to its pharmacodynamic properties, zuclopenthixol has been associated with adverse effects typical of first-generation antipsychotics, including extrapyramidal symptoms and potential QTc interval prolongation. These safety concerns necessitate careful clinical monitoring.
The drug has been marketed under brand names such as Cisordinol, Acuphase, and Clopixol. Notably, while approved for clinical use in countries including Canada since 2011, zuclopenthixol is not authorized for use in the United States.
From an API procurement perspective, ensuring compliance with international quality standards is essential given the compound’s complex synthesis and pharmacological potency. Manufacturers should verify that supplied zuclopenthixol meets stringent purity, identity, and stability criteria aligned with pharmacopeial specifications. Additionally, attention to regulatory acceptance in target markets and an understanding of metabolic liabilities are important for formulation and sourcing decisions.
Identification & chemistry
| Generic name | Zuclopenthixol |
|---|---|
| Molecule type | Small molecule |
| CAS | 53772-83-1 |
| UNII | 47ISU063SG |
| DrugBank ID | DB01624 |
Pharmacology
| Summary | Zuclopenthixol is a typical antipsychotic of the thioxanthene class that primarily exerts its effects through antagonism of dopamine D1 and D2 receptors. It also interacts with alpha1-adrenergic, 5-HT2 serotonin, histamine H1, and muscarinic cholinergic receptors to a lesser extent. These receptor interactions contribute to its therapeutic use in managing acute psychotic disorders. |
|---|---|
| Mechanism of action | Zuclopenthixol is a typical antipsychotic neuroleptic drug of the thioxanthene class. It mainly acts by antagonism of D1 and D2 dopamine receptors. Zuclopenthixol also has high affinity for alpha1-adrenergic and 5-HT2 receptors. It has weaker histamine H1 receptor blocking activity, and even lower affinity for muscarinic cholinergic and alpha2-adrenergic receptors. |
| Pharmacodynamics | Zuclopenthixol is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine D1 receptor | Humans | antagonist |
| Dopamine D5 receptor | Humans | antagonist |
| Dopamine D2 receptor | Humans | antagonist |
ADME / PK
| Absorption | Upon reaching the body water phase, the decanoate ester is slowly released from the oil depot, which is resultantly hydrolyzed to the active substance, zuclopenthixol. The decanoate ester provides a means of slow release since zuclopenthixol itself is a short-acting drug. |
|---|---|
| Half-life | 20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form. |
| Protein binding | 98-99% |
| Metabolism | The metabolism of zuclopenthixol is mainly by sulphoxidation, side chain N-dealkylation and glucuronic acid conjugation. The metabolites are devoid of pharmacological activity. |
| Route of elimination | Primarily in the feces with approximately 10% in the urine. |
| Volume of distribution | 20 L/kg. |
| Clearance | approximately 0.9 L/min. |
Formulation & handling
- Zuclopenthixol is a small molecule available in both oral and intramuscular injectable formulations, including extended-release suspensions.
- Low water solubility and high LogP suggest formulation challenges in aqueous systems and potential need for solubilizing agents or suitable excipients.
- Oral administration can be with or without food, but alcohol should be strictly avoided due to contraindications associated with acute intoxication.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is currently marketed in Canada with patent protection set to expire within the next 12 months, indicating an upcoming transition from exclusive rights towards a more competitive generic marketplace. Post-patent expiry, the API is expected to experience increased market maturity and broader availability. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | Zuclopenthixol is manufactured by a limited number of originator companies, with branded products primarily present in the Canadian market. The available formulations include oral tablets and injectable liquids in varying dosages. Patent expiry has allowed for existing generic competition within these markets. |
|---|
Safety
| Toxicity | Although there have not been any cases of overdosage reported, the symptoms are likely to be somnolence, coma, extrapyramidal symptoms, convulsions, hypotension, shock, or hyper- or hypothermia. Neuroleptic malignant syndrome may occur. Zuclopenthixol may potentiate anticholinergic effects of concurrent medications. Zuclopenthixol has a demonstrated antiemetic effect in animals, and may mask signs of toxicity due to other drug overdoses, or may mask symptoms of disease. |
|---|
- Exposure to zuclopenthixol may result in central nervous system depression characterized by somnolence, coma, and extrapyramidal symptoms
- Neuroleptic malignant syndrome, a potentially life-threatening reaction, has been reported with zuclopenthixol use
- Zuclopenthixol can potentiate anticholinergic effects of co-administered drugs and may mask toxicity signs of other substances, requiring careful monitoring during handling
Zuclopenthixol 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.
Zuclopenthixol (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.
