Substance
ID:291
Names and Identifiers
Brand Name
LoxapacLoxapinum [INN-Latin]Loxitane COxilapineDibenzoazepineLossapina [Dcit]LoxepineCloxazepineDibenzacepinHydrofluoride 3170LoxapinLoxapina [INN-Spanish]Loxapine [Usan:Ban:Inn]Loxitane Im
IUPAC Traditional name
loxapine
IUPAC name
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaene
Synonyms
Loxapine
Properties
Physical Property
Hydrophobicity(logP)
3.6
Molecule Details
Drug Groups
approved
Description
An antipsychotic agent used in schizophrenia. [PubChem]
Indication
For the management of the manifestations of psychotic disorders such as schizophrenia
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, 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.
Toxicity
LD50=65 mg/kg (Orally in mice)
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic
Absorption
Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers
Half Life
Oral-4 hours
Elimination
Metabolites are excreted in the urine in the form of conjugates and in the feces unconjugated.
References
•
Glazer WM: Does loxapine have "atypical" properties? Clinical evidence. J Clin Psychiatry. 1999;60 Suppl 10:42-6.
[Pubmed]
•
Cheung SW, Tang SW, Remington G: Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography. J Chromatogr. 1991 Mar 8;564(1):213-21.
[Pubmed]
External Links
Molecular Spectra
No Data Available
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References
• Glazer WM: Does loxapine have "atypical" properties? Clinical evidence. J Clin Psychiatry. 1999;60 Suppl 10:42-6. Pubmed
• Cheung SW, Tang SW, Remington G: Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography. J Chromatogr. 1991 Mar 8;564(1):213-21. Pubmed