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QuickView for Loxapine (compound)

Summary
General Info

PubChem

PubChem Compound 3964

PubChem Compound 3964

Name:	Loxapine
PubChem Compound ID:	3964
Description:	An antipsychotic agent used in schizophrenia.
Molecular formula:	C₁₈H₁₈ClN₃O
Molecular weight:	327.808 g/mol
Synonyms:	Loxapine; Dibenzoazepine; Loxapin; LW 3170; Dibenz[b,f][1,4]oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-; Hydrofluoride 3170; Loxitane; EINECS 217-835-3; Loxapina [INN-Spanish]; KBio2_000835. show more » Loxapine; Dibenzoazepine; Loxapin; LW 3170; Dibenz[b,f][1,4]oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-; Hydrofluoride 3170; Loxitane; EINECS 217-835-3; Loxapina [INN-Spanish]; KBio2_000835; BRN 0626753; CL 62362; 54810-23-0; S 805; KBio2_003403; KBio1_001863; Oxilapine; KBioSS_000835; HSDB 3111; HF 3170; SPBio_001814; Dibenzacepin; SPBio_002143; DivK1c_006919; Prestwick0_000132; S-805; Spectrum2_001737; Prestwick1_000132; Loxapine (USAN); D02340; CL-62362; Spectrum_000355; 2-Chloro-11-(4-methylpiperazino)dibenzo(b,f)(1,4)oxazepine; Dibenz(b,f)(1,4)oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-; Loxapinum [INN-Latin]; Loxapine [USAN:BAN:INN]; Spectrum3_001830; KBio2_005971; 2-Chloro-11-(4-methyl-1-piperazinyl)dibenz(b,f)(1,4)oxazepine; Cloxazepine; KBio3_002983; SpecPlus_000823; 1977-10-2; 27833-64-3; C07104; HF3170; Lossapina [DCIT]; SUM 3170 show less «

DrugBank

Identification

Name:	Loxapine
Name (isomeric):	DB00408
Drug Type:	small molecule
Description:	An antipsychotic agent used in schizophrenia.
Brand:	Dibenzoazepine, Dibenzacepin, Oxilapine, Cloxazepine, Loxapina [INN-Spanish], Loxapinum [INN-Latin], Loxapin, Loxitane Im, Loxepine, Loxapac, Loxitane C, Hydrofluoride 3170, Lossapina [Dcit], Loxapine [Usan:Ban:Inn]
Category:	Dopamine Antagonists, Antipsychotic Agents, Antipsychotics
CAS number:	1977-10-2

Pharmacology

Indication:	For the management of the manifestations of psychotic disorders such as schizophrenia
Pharmacology:	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 ... show more » 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. show less «
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 ... show more » 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. show less «
Absorption:	Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers
Biotransformation:	Hepatic
Route of elimination:	Metabolites are excreted in the urine in the form of conjugates and in the feces unconjugated.
Half Life:	Oral-4 hours
Toxicity:	LD₅₀=65 mg/kg (Orally in mice)
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take with food to reduce irritation. Avoid alcohol.

Drug interaction:

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.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Triprolidine	Triprolidine and Loxapine, 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.
Trimethobenzamide	Trimethobenzamide and Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tetrabenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse 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.
Vorinostat	Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Triprolidine	Triprolidine and Loxapine, 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.
Trimethobenzamide	Trimethobenzamide and Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
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.
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).
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Loxapine, 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.
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).
Trospium	Trospium and Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.

Targets

D(2) dopamine receptor

D(1A) dopamine receptor

5-hydroxytryptamine 2A receptor

5-hydroxytryptamine 2C receptor