Loxapine
- Atc Codes:N05AH01
- CAS Codes:1977-10-2#27833-64-3
- PHARMGKB ID:1977-10-2#27833-64-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
France: Loxapac; Luxembourg: Loxapac.
North America
Canada: Loxapac, Loxapine; USA: Loxapine.
Drug combinations
Chemistry
Loxapine: C~18~H~18~ClN~3~O. Mw: 327.81. (1) Dibenz[b,f][1,4]oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-; (2) 2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine. CAS-1977-10-2 (1969).
Loxapine Succinate: C~18~H~18~ClN~3~O C~4~H~6~O~4~. Mw: 445.90. Butanedioic acid, compd. with 2-chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine (1:1). CAS-27833-64-3 (1969).
Pharmacologic Category
Antipsychotics, Miscellaneous. (ATC-Code: N05AH01).
Mechanism of action
Dibenzoxazepine antipsychotic which blocks postsynaptic mesolimbic D~1~ and D~2~ receptors in brain; also possesses serotonin 5-HT~2~-blocking activity.
Therapeutic use
Management of psychotic disorders.
Pregnancy and lactiation implications
Unlabeled use
Psychosis/agitation related to Alzheimer’s dementia.
Contraindications
Hypersensitivity to loxapine or any component of the formulation. Severe CNS depression. Coma.
Warnings and precautions
Might alter cardiac conduction (avoid use in underlying QT prolongation, in patients taking medicines which prolong QT interval, or cause polymorphic ventricular tachycardia). Might cause anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention)(use with caution in decreased gastrointestinal motility, paralytic ileus, urinary retention, benign prostatic hypertrophy, xerostomia, or visual problems). Blood dyscrasias (e.g. leukopenia, agranulocytosis) observed with antipsychotic use. Antipsychotic use associated with esophageal dysmotility and aspiration (use with caution in risk of pneumonia (e.g. Alzheimer’s disease)). Might cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Use may be associated with neuroleptic malignant syndrome. Might cause orthostatic hypotension (use with caution in cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). Might be associated with pigmentary retinopathy. Might be sedating. Impaired core body temperature regulation might occur. Use with caution in severe cardiovascular disease. Increased mortality risk with typical and atypical antipsychotic drugs when used in elderly patients with dementia-related psychosis (loxapine not approved for this indication). Use with caution in narrow-angle glaucoma (might be exacerbated by cholinergic blockade), in hepatic and renal impairment, in myasthenia gravis (might be exacerbated by cholinergic blockade), in Parkinson’s disease, in breast cancer or other prolactin-dependent tumors (elevates prolactin levels), in respiratory disease, and in patients at risk of seizures, including those with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Might mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects.