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QuickView for Loxapine (compound)

Name: Loxapine
PubChem Compound ID: 3964
Description: An antipsychotic agent used in schizophrenia.
Molecular formula: C18H18ClN3O
Molecular weight: 327.808 g/mol
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.
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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
Indication: For the management of the manifestations of psychotic disorders such as schizophrenia
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 ...
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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 ...
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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
Food interaction:
Take with food to reduce irritation. Avoid alcohol.
Drug interaction:
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
TriprolidineTriprolidine 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.
TrimethobenzamideTrimethobenzamide and Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
TetrabenazineMay cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
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