Loxapine Brand names: Loxapac, Loxitane
Drug monograph Contents Indications Contraindications Warnings ... Research Pharmacology Antipsychotic Agent Loxapine, a tricyclic dibenzoxazepine antipsychotic agent, which is chemically distinct from the phenothiazines, thioxanthenes and butyrophenones, produces pharmacological responses in various animal species which are characteristic of those seen with the majority of antipsychotic drugs. Although the precise mechanism of action is not known, loxapine succinate administration results in strong inhibition of spontaneous motor activity. Absorption following orally administered loxapine succinate is virtually complete. Following oral administration of a single 25 mg dose of loxapine, the onset of sedative effect occurs in 15 to 30 minutes; peak effect occurs within 1.0 to 3 hours. The duration of sedative effect is approximately 12 hours. Loxapine is metabolized rapidly and extensively in animals and man and excreted both in the urine and feces. There appear to be 3 reactions, other than phenol conjugation, involved in the metabolism of loxapine: aromatic hydroxylation, N-oxidation and N-demethylation. Unmetabolized drug has not been recovered in urine and feces though metabolites are excreted in urine mainly in the form of conjugates and in feces mainly in the unconjugated form. In rats, 86 to 96% of orally administered doses of loxapine has been recovered in urine and feces. In dogs, 92 to 104% has been similarly recovered. Approximately 50% of the drug is recovered within the first 24 hours. | |
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