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) |