Loxapine

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Loxapine
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Systematic (IUPAC) name
2-Chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine
Pharmacokinetic data
Metabolism Gastrointestinal, peak concn. occur between 1-2 hours.
Biological half-life Oral-4 hours
Excretion Majority are excreted within 24 hours. Main route through urine(conjugated metabolites); Small amounts through the faeces(unconjugated metabolites)
Identifiers
CAS Number 1977-10-2
ATC code N05AH01 (WHO)
PubChem CID 3964
IUPHAR/BPS 205
DrugBank APRD00574
Chemical data
Formula C18H18ClN3O
Molar mass 327.808 g/mol[[Script error: No such module "String".]]
Physical data
Melting point 109 to 110 °C (228 to 230 °F)
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Loxapine (Loxapac, Loxitane) is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. It is a member of the dibenzoxazepine class and as a dibenzazepine derivative, it is structurally related to clozapine (which belongs to the chemically closely akin class of dibenzodiazepines). Several researchers have argued that Loxapine may behave as an atypical antipsychotic.[1]

Loxapine may be metabolized by N-demethylation to amoxapine, a tetracyclic antidepressant.[2]

Precautions

Care should be taken with consumption. At least 3 cases were reported of loxapine succinate abuse.[3]

Side effects

The most significant side-effects of loxapine are excessive salivation and indifference to surroundings. Loxapine, if administered to individuals without schizophrenia, causes emotional quieting and insensitivity. In persons with psychosis, it may control aggressive behaviour and restlessness, and reduce the severity of hallucinations and delusions. Other Side effects include tardive dyskinesia, neuroleptic malignant syndrome, extrapyramidal side effects, tremor, gynecomastia and sedation.

Dosage

The typical starting dosage is 10mg twice daily; usual dose range 30-50mg twice daily; maximum recommended dosage is 250mg per day.

A brief review of loxapine[4] found no conclusive evidence that it was particularly effective in patients with paranoid schizophrenia. A subsequent systematic review considered that the limited evidence did not indicate a clear difference in its effects from other antipsychotics.[5]

Chemistry

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Schmutz, J.; Kunzle, F.; Hunziker, F.; Gauch, R.; Helv. Chim. Acta 1967, 50, 245.

References

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External links



fr:Loxapine
  1. Glazer WM (1999). "Does loxapine have "atypical" properties? Clinical evidence". The Journal of Clinical Psychiatry. 60 (Suppl 10): 42–6. PMID 10340686. 
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  5. Chakrabarti A, Bagnall A, Chue P; et al. (2007). "Loxapine for schizophrenia". Cochrane Database of Systematic Reviews (Online) (4): CD001943. doi:10.1002/14651858.CD001943.pub2. PMID 17943763.