Pharmacology Of Loxapine

Indication For the management of the manifestations of psychotic disorders such as schizophrenia
Pharmacodynamics 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.
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
Volume of distribution Not Available
Protein binding Not Available
Metabolism 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
Clearance Not Available
Toxicity LD50=65 mg/kg (Orally in mice)