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QuickView for Flupenthixol (compound)

Summary
General Info

PubChem

PubChem Compound 17011

PubChem Compound 17011

Name:	Flupenthixol
PubChem Compound ID:	17011
Description:	A thioxanthene neuroleptic that, unlike CHLORPROMAZINE, is claimed to have CNS-activating properties. It is used in the treatment of psychoses although not in excited or manic patients. (From Martindale, The Extra Pharmacopoeia, 30th ed, p595)
Molecular formula:	C₂₃H₂₇Cl₂F₃N₂OS
Molecular weight:	507.44 g/mol

DrugBank

Identification

Name:	Flupenthixol
Name (isomeric):	DB00875
Drug Type:	small molecule
Description:	A thioxanthene neuroleptic that, unlike CHLORPROMAZINE, is claimed to have CNS-activating properties. It is used in the treatment of psychoses although not in excited or manic patients. (From Martindale, The Extra Pharmacopoeia, 30th ed, p595)
Synonyms:	Flupenthixole
Brand:	Fluxanxol, Flupentixol, Siplaril, Emergil, Fluanxol, Flurentixol, Fluanxol Depot, Depixol, Siplarol
Category:	Thioxanthenes, Dopamine Antagonists, Antipsychotic Agents, Antipsychotics
CAS number:	2709-56-0

Pharmacology

Indication:	For use in the treatment of schizophrenia and depression
Pharmacology:	Flupenthixol is an anxiolytic, antidepressive agent and a mood stabilizer. It inhibits the central monoamine receptors, particularly the dopamine D1 and D2 receptors. Therefore, it increases the amount of serotonin and noradrenaline that control mood and thinking, and improves mood.
Mechanism of Action:	Flupenthixol is a thioxanthene antipsychotic. The mechanism of action of Flupenthixol is not completely understood. Flupenthixol is a powerful antagonist of both D1 and D2 dopamine receptors, and an alpha-adrenergic receptor antagonist. It's antipsychotic activity is thought to be related to blocks postsynaptic dopamine receptors in the CNS.
Absorption:	Fairly slow and incomplete after oral administration
Protein binding:	Highly bound to plasma proteins (>95%)
Biotransformation:	Mainly hepatic
Half Life:	19 to 39 hours
Toxicity:	LD₅₀=300 mk/kg (Oral in mice); LD₅₀=791 mg/kg (Oral in rats); LD₅₀=87 mk/kg (IV in mice); LD₅₀=37 mg/kg (IV in rats)
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Avoid alcohol.

Take with food to reduce irritation.

Drug interaction:

Trospium	Trospium and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Thiothixene	May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Triprolidine	Triprolidine and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.

Trospium	Trospium and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Thiothixene	May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Triprolidine	Triprolidine and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Galantamine	Possible antagonism of action
Ziprasidone	Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Artemether	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Trimethobenzamide	Trimethobenzamide and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tacrolimus	Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Donepezil	Possible antagonism of action
Toremifene	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
Zuclopenthixol	Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Trimipramine	Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Rivastigmine	Possible antagonism of action
Voriconazole	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Flupenthixol, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.

Targets

D(2) dopamine receptor

5-hydroxytryptamine 2A receptor

D(1A) dopamine receptor

Alpha-1A adrenergic receptor

Muscarinic acetylcholine receptor M1

Enzymes

Aromatic-L-amino-acid decarboxylase

Transporters

Multidrug resistance protein 1