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Loxapine
Systematic (IUPAC) name
2-Chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine
Identifiers
CAS number 1977-10-2
ATC code N05AH01
PubChem 3964
DrugBank APRD00574
Chemical data
Formula C 18H18ClN3O 
Mol. mass 327.808 g/mol
Physical data
Melt. point 109–110 °C (228–230 °F)
Pharmacokinetic data
Bioavailability  ?
Metabolism Gastrointestinal, peak concn. occur between 1-2 hours.
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)
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?
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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 tricyclic antidepressant.[2]

Contents

Precautions

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

An overdose accident happened with a 8 year old child who swallowed a 375 miligram loxitane pill. 30 minutes later it was treated with activated charcoal. The child became drowsy and was asleep but arousable 1 hour after ingestion. The degree of sedation appeared to peak after 3.75 hours and the child was discharged about 20 hours after ingestion.[4]

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[5] 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.[6]

References

  1. ^ Glazer WM (1999). "Does loxapine have "atypical" properties? Clinical evidence". The Journal of Clinical Psychiatry 60 (Suppl 10): 42–6. PMID 10340686.  
  2. ^ Cheung SW, Tang SW, Remington G (March 1991). "Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography". Journal of Chromatography 564 (1): 213–21. doi:10.1016/0378-4347(91)80083-O. PMID 1860915.  
  3. ^ Sperry L, Hudson B, Chan CH (March 1984). "Loxapine abuse". The New England Journal of Medicine 310 (9): 598. PMID 6694719.  
  4. ^ Tarricone NW (March 1998). "Loxitane overdose". Pediatrics 101 (3 Pt 1): 496. doi:10.1542/peds.101.3.496. PMID 9499203.  
  5. ^ "Clozapine and loxapine for schizophrenia". Drug and Therapeutics Bulletin 29 (11): 41–2. May 1991. PMID 1747161.  
  6. ^ 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.  

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