Loxapine
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| Trade names | Several trade names worldwide |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682311 |
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Oral, powder for inhalation |
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| Pharmacokinetic data | |
| Protein binding | 96.8% |
| Metabolism | Extensive hepatic; active metabolites include amoxapine and 8-hydroxyloxapine. Inhibits P-gp and is a substrate of CYP1A2, CYP3A4 and CYP2D6<re name = "DrugPoint" /> |
| Biological half-life | 4 hours (oral); 7.61 hours (inhalation) |
| Excretion | Majority are excreted within 24 hours, main route through urine (conjugated metabolites), small amounts through the feces (unconjugated metabolites) |
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| ECHA InfoCard | 100.016.215 |
| Chemical and physical data | |
| Formula | C18H18ClN3O |
| Molar mass | 327.808 g/mol |
| 3D model (Jmol) | |
| Melting point | 109 to 110 °C (228 to 230 °F) |
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Loxapine (several trade names worldwide) is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines). Several researchers have argued that loxapine may behave as an atypical antipsychotic.
Loxapine may be metabolized by N-demethylation to amoxapine, a tetracyclic antidepressant.
The typical starting dosage is 10 mg twice daily; usual dose range 30–50 mg twice daily; maximum recommended dosage is 250 mg per day. The US Food and Drug Administration (FDA) has approved loxapine inhalation powder 10 mg (Adasuve, Alexza Pharmaceuticals) for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults.
A brief review of loxapine 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.
This drug is unrelated to the habit-forming benzodiazepines, and misuse is rare. The risks and side effect profile are comparable to other antipsychotics.
Note: Percentages given after possible adverse effects refer to the incidence of said adverse effects, according to DrugPoint.
The data in the following table was obtained from the PDSP Ki database and they are for binding towards human cloned proteins (receptor and transporter) unless otherwise specified.
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