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Active ingredient: Loxapine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antipsychotics
  • Dopamine Antagonists

Dosage Forms

  • Tablet
  • Capsule
  • Oral solution
  • IV solution
  • IM solution

Brands / Synonyms

Cloxazepine; Dibenzacepin; Dibenzoazepine; Hydrofluoride 3170; Lossapina [Dcit]; Loxapac; Loxapin; Loxapina [Inn-Spanish]; Loxapine; Loxapine Succinate; Loxapine [Usan:Ban:Inn]; Loxapinum [Inn-Latin]; Loxepine; Loxitane; Loxitane C; Loxitane Im; Oxilapine

Indications

For the management of the manifestations of psychotic disorders

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.

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 of aggressive behavior.

Absorption

Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers

Toxicity

LD50=65 mg/kg (Orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

LOXITANE is contraindicated in comatose or severe drug-induced depressed states (alcohol, barbiturates, narcotics, etc.).

LOXITANE is contraindicated in individuals with known hypersensitivity to dibenzoxazepines.

Drug Interactions

There have been rare reports of significant respiratory depression, stupor and/or hypotension with the concomitant use of loxapine and lorazepam.

The risk of using loxapine in combination with CNS-active drugs has not been systematically evaluated. Therefore, caution is advised if the concomitant administration of loxapine and CNS-active drugs is required.

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