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Flupentixol | CAS No: 2709-56-0 | GMP-certified suppliers
A medication that supports maintenance therapy in chronic schizophrenia and manages depression and anxiety symptoms in adults, with formulations including oral and long-acting injectable options.
Therapeutic categories
Adrenergic alpha-1 Receptor AntagonistsAdrenergic alpha-AntagonistsAdrenergic AntagonistsAgents producing tachycardiaAgents that produce hypertensionAnticholinergic Agents
Generic name
Flupentixol
Molecule type
small molecule
CAS number
2709-56-0
DrugBank ID
DB00875
Approval status
Approved drug, Investigational drug, Withdrawn drug
ATC code
N05AF01
Primary indications
- Flupentixol is indicated for maintenance therapy of chronic schizophrenic patients whose main manifestations do not include excitement, agitation or hyperactivity
- It is indicated for the management of depression in adult patients who may, or may not, also be showing signs of anxiety
Product Snapshot
- Flupentixol is available as oral tablets (including sugar and film coated) and injectable solutions for intramuscular and parenteral administration
- It is primarily used for maintenance therapy in chronic schizophrenia, management of depression, and treatment of anxiety and asthenia in combination with melitracen
- Flupentixol is approved for use in the Canadian pharmaceutical market
Clinical Overview
Flupentixol is a thioxanthene-class typical antipsychotic agent primarily indicated for maintenance therapy in chronic schizophrenia, notably in patients without prominent excitement, agitation, or hyperactivity. Its clinical use extends to managing depression in adults, with or without concurrent anxiety symptoms. Additionally, flupentixol in combination with melitracen is employed for treating anxiety, depression, and asthenia.
Pharmacologically, flupentixol exists as two geometric isomers; the cis(Z) isomer is pharmacologically active. It acts mainly as an antagonist at dopamine D1 and D2 receptors with similar affinities, contributing to its antipsychotic effects through modulation of dopaminergic neurotransmission. The drug also exhibits antagonistic activity at serotonin 5-HT2A and 5-HT2C receptors, which is linked to its antidepressant and anxiolytic properties. Weak anticholinergic, adrenergic alpha-1 receptor antagonistic, and antiemetic effects have been characterized. Flupentixol decanoate, an esterified form used in intramuscular injections, provides a depot formulation that allows for slow systemic release and sustained action.
Absorption following oral administration is notable, with long-acting injectable forms allowing for extended plasma exposure. Metabolism pathways and detailed pharmacokinetics data are limited, but the esterified intramuscular formulations prolong duration of effect. Safety considerations include the risk of extrapyramidal symptoms, generally observed at doses above 10 mg, which can be managed with anti-Parkinsonian agents. Flupentixol may cause QTc interval prolongation and other cardiovascular risks, including cerebrovascular events and venous thromboembolism. Prolactin elevation is common, with potential long-term effects on bone mineral density related to hypogonadism. Phototoxicity has been reported as an adverse effect. Emerging preclinical findings suggest inhibition of the PI3K/AKT pathway, indicating potential antitumor activity, though this is not clinically established.
Flupentixol is marketed under various brand names, including Depixol and Fluanxol, and is approved in multiple countries except the United States. It is supplied as oral tablets and long-acting intramuscular injections for clinical use.
For sourcing of flupentixol APIs, quality assurance should emphasize stereochemical purity, particularly the enrichment of the active cis(Z) isomer, as well as compliance with pharmacopeial standards. Stability and control of residual solvents and impurities related to the thioxanthene structure must be rigorously monitored to ensure consistent pharmacological activity and safety profiles.
Pharmacologically, flupentixol exists as two geometric isomers; the cis(Z) isomer is pharmacologically active. It acts mainly as an antagonist at dopamine D1 and D2 receptors with similar affinities, contributing to its antipsychotic effects through modulation of dopaminergic neurotransmission. The drug also exhibits antagonistic activity at serotonin 5-HT2A and 5-HT2C receptors, which is linked to its antidepressant and anxiolytic properties. Weak anticholinergic, adrenergic alpha-1 receptor antagonistic, and antiemetic effects have been characterized. Flupentixol decanoate, an esterified form used in intramuscular injections, provides a depot formulation that allows for slow systemic release and sustained action.
Absorption following oral administration is notable, with long-acting injectable forms allowing for extended plasma exposure. Metabolism pathways and detailed pharmacokinetics data are limited, but the esterified intramuscular formulations prolong duration of effect. Safety considerations include the risk of extrapyramidal symptoms, generally observed at doses above 10 mg, which can be managed with anti-Parkinsonian agents. Flupentixol may cause QTc interval prolongation and other cardiovascular risks, including cerebrovascular events and venous thromboembolism. Prolactin elevation is common, with potential long-term effects on bone mineral density related to hypogonadism. Phototoxicity has been reported as an adverse effect. Emerging preclinical findings suggest inhibition of the PI3K/AKT pathway, indicating potential antitumor activity, though this is not clinically established.
Flupentixol is marketed under various brand names, including Depixol and Fluanxol, and is approved in multiple countries except the United States. It is supplied as oral tablets and long-acting intramuscular injections for clinical use.
For sourcing of flupentixol APIs, quality assurance should emphasize stereochemical purity, particularly the enrichment of the active cis(Z) isomer, as well as compliance with pharmacopeial standards. Stability and control of residual solvents and impurities related to the thioxanthene structure must be rigorously monitored to ensure consistent pharmacological activity and safety profiles.
Identification & chemistry
| Generic name | Flupentixol |
|---|---|
| Molecule type | Small molecule |
| CAS | 2709-56-0 |
| UNII | FA0UYH6QUO |
| DrugBank ID | DB00875 |
Pharmacology
| Summary | Flupentixol is an antipsychotic agent primarily acting as an antagonist at dopamine D1 and D2 receptors with comparable affinity, contributing to its therapeutic effects in schizophrenia. It also exhibits antagonism at serotonin 5-HT2A and 5-HT2C receptors and alpha-1 adrenergic receptors, which may underlie its antidepressant and anxiolytic properties. Additionally, flupentixol demonstrates weak anticholinergic and adrenergic effects, with emerging evidence suggesting inhibition of the PI3K/AKT pathway relevant to potential anticancer activity. |
|---|---|
| Mechanism of action | The mechanism of action of flupentixol is not completely understood. The antipsychotic actions are mainly thought to arise from cis(Z)-flupentixol, the active stereoisomer, acting as an antagonist at both dopamine D<sub>1</sub> and D<sub>2</sub> receptors with equal affinities. Schizophrenia is a mental illness characterized by positive (such as hallucinations and delusions) and negative (such as affect flattening and apathy) symptoms. While several neurotransmitter systems are implicated in the pathophysiologic processes leading to the development of symptoms, the dopamine and glutamate systems have been extensively studied. It is generally understood that positive symptoms of schizophrenia arise from a dysregulated striatal dopamine pathway, leading to hyperstimulation of D<sub>2</sub> receptors. Many antipsychotic agents work by blocking D<sub>2</sub> receptors as antagonists; similarly, cis(Z)-flupentixol, the active stereoisomer, is an antagonist at D<sub>2</sub> receptors. However, there is now evidence that antipsychotic agents can work by blocking other dopamine receptor subtypes, such as D<sub>1</sub>, D<sub>3</sub>, or D<sub>4</sub> receptors.[A229413, A229433, A229438] One study showed that cis(Z)-flupentixol is an antagonist at both dopamine D<sub>1</sub> and D<sub>2</sub> receptors with equal affinities, and binds to D3 and D4 receptors with lower affinities. It also binds to alpha-1 adrenoceptors. Antidepressant effects of flupentixol are understood to be mediated by antagonism at 5-HT<sub>2A</sub> receptors, which are commonly downregulated following repeated antidepressant treatment. Flupentixol also binds to 5-HT<sub>2C</sub> receptors. |
| Pharmacodynamics | Flupentixol is an antipsychotic agent with anxiolytic and mild sedative actions. It exerts weak anticholinergic and adrenergic effects. It possesses antiemetic actions. As flupentixol works by antagonizing dopamine actions, it can cause extrapyramidal effects, mostly at doses greater than 10 mg. In clinical trials, flupentixol-induced extrapyramidal effects have been managed with anti-Parkinsonian drugs. Drug esterification in the intramuscular formulation of the drug results in slow release of the drug from the injection site and a prolonged duration of action. Flupentixol has been investigated for use in mild to moderate depression: compared to other antidepressant agents, flupentixol has a rapid onset of action, where antidepressive effects were observed within the first two to three days after administration. As with other antipsychotic agents, flupentixol can cause QTc prolongation and increase the risk of arrhythmias. In clinical trials, flupentixol was associated with the risk of cardiovascular disease, cerebrovascular adverse events, stroke, and venous thromboembolism. Flupentixol can elevate the levels of prolactin; however, the clinical significance of hyperprolactinemia caused by neuroleptic drugs is unclear. Long-term hyperprolactinemia, when associated with hypogonadism, may lead to decreased bone mineral density in both female and male subjects. Interestingly, recent studies show that flupentixol exhibits anti-tumour properties alone or synergistically with other anticancer drugs like gefitinib. One study demonstrated that _in vitro_, flupentixol docks to the ATP binding pocket of phosphatidylinositol 3-kinase (PI3K), a lipid kinase that activates signalling pathways that are often hyperactivated in some cancers. Flupentixol inhibited the PI3K/AKT pathway and survival of lung cancer cells _in vitro_ and _in vivo_. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine D2 receptor | Humans | antagonist |
| Dopamine D1 receptor | Humans | antagonist |
| 5-hydroxytryptamine receptor 2A | Humans | antagonist |
ADME / PK
| Absorption | Following oral administration, flupentixol is readily absorbed from the gastrointestinal tract, with oral bioavailability of about 40%. T<sub>max</sub> ranges from three to eight hours. Steady-state plasma levels are achieved in about seven days and following once-daily oral administration of 5 mg flupentixol, the mean minimum steady-state level was about 1.7 ng/mL (3.9 nmol/L). From the site of intramuscular injection, esterified flupentixol diffuses slowly from the oil solution and is slowly released into the extracellular fluid and the circulation to be distributed to different tissues. Peak drug concentrations are reached between four and seven days following intramuscular injection. Intramuscularly administered flupentixol is detectable in the blood three weeks after injection and reaches steady-state concentrations after about three months of repeated administration. |
|---|---|
| Half-life | The elimination half-life is about 35 hours following oral administration and three weeks following intramuscular administration. |
| Protein binding | Flupentixol is 99% bound to plasma proteins. |
| Metabolism | Flupentixol is metabolized in the liver via sulfoxidation, dealkylation, and glucuronidation to form pharmacologically inactive metabolites. Flupentixol decanoate, the active ingredient in the intramuscular formulation, is hydrolyzed to flupentixol. |
| Route of elimination | Fecal excretion is more predominant than renal excretion. In the feces, flupentixol is recovered in the feces mainly as the unchanged form, as well as its lipophilic metabolites, such as dealkyl-flupentixol. Flupentixol is recovered in the urine as the unchanged form as well as its hydrophilic sulfoxide and glucuronide metabolites. |
| Volume of distribution | The apparent volume of distribution is about 14.1 L/kg. Following administration, the highest levels of flupentixol are found in the lungs, liver, and spleen. Lower concentrations of the drug are found in the blood and brain. |
| Clearance | Following oral administration, the mean systemic clearance is about 0.29 L/min. |
Formulation & handling
- Flupentixol is a small molecule suitable for both oral and parenteral (intramuscular) administration as tablets and injection solutions.
- Due to its low water solubility and high logP, formulation strategies should consider solubilization and bioavailability enhancement.
- Food intake does not significantly affect pharmacokinetics, but co-administration with alcohol should be avoided due to enhanced sedation risk.
Regulatory status
| Lifecycle | The API is currently marketed in Canada with patent protection expired, allowing for generic competition and established market availability. Product formulations are in various stages of post-patent lifecycle maturity. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Flupentixol involves multiple originator companies producing branded formulations primarily for the Canadian market. Branded products include various tablet strengths and depot injections, reflecting an established global presence in formulation variety, though with a focus on North America. Patent expiries in this class suggest the availability of generic options, indicating existing or potential generic competition. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> is 423 mg/kg in mice and 791 mg/kg in rats. The intravenous LD<sub>50</sub> is 37 mg/kg in rats. Flupentixol overdose is characterized by sedation, frequently preceded by extreme agitation, excitement, confusion, somnolence, coma, convulsions, and hyperthermia or hypothermia. Extrapyramidal symptoms or respiratory and circulatory collapse may be observed. ECG changes, QT prolongation, Torsades de Pointes, cardiac arrest and ventricular arrhythmias have been reported from the combined use of drugs known to affect the heart with large doses of flupentixol. In case of overdose, symptomatic treatment should be initiated with airway management. In case of severe hypotension, epinephrine should not be used: instead, intravenous vasopressor drugs, such as levarterenol, can be used. Antiparkinsonian medication should be administered only if extrapyramidal symptoms develop. Gastric lavage should be initiated in the case of flupentixol tablet overdose. Further injections of flupentixol should be discontinued in case of an intramuscularly-administered drug overdose until the patient shows signs of relapse, in which the dosage can subsequently be decreased. Neuroleptic malignant syndrome is associated with neuroleptic drugs, which should be responded to with immediate discontinuation of the drug and initiation of symptomatic treatment and medical monitoring. |
|---|
High Level Warnings:
- Flupentixol exhibits moderate acute toxicity with oral LD50 values of 423 mg/kg (mice) and 791 mg/kg (rats), and a significantly lower intravenous LD50 of 37 mg/kg (rats)
- Overdose may cause central nervous system depression, extrapyramidal symptoms, and cardiovascular disturbances including QT prolongation and arrhythmias
- Combined use with other cardiotoxic drugs increases these risks
Flupentixol is a type of 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.
Flupentixol API manufacturers & distributors
Compare qualified Flupentixol API suppliers worldwide. We currently have 2 companies offering Flupentixol 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, WC | 40 products |
| Guangzhou Green Cross Pha... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 15 products |
When sending a request, specify which Flupentixol 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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