Drug intelligence / Profile preview

loxapine

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intramuscular, Inhalation
01

Overview

Loxapine is a tricyclic antipsychotic medication primarily used to treat schizophrenia and acute agitation associated with schizophrenia or bipolar I disorder in adults. It belongs to the dibenzoxazepine class and is structurally similar to clozapine. Loxapine acts mainly as an antagonist at dopamine D2 receptors and serotonin 5-HT2A receptors, helping to rebalance neurotransmitter activity in the brain, which can improve symptoms such as hallucinations, delusions, disorganized thinking, and agitation. The drug is available in oral (capsule), intramuscular injection, and inhalation powder formulations. The inhaled form (Adasuve) is specifically approved for acute agitation. Loxapine may be metabolized into amoxapine (a tricyclic antidepressant). While initially classified as a typical antipsychotic due to its dopamine antagonism and risk of extrapyramidal symptoms at higher doses, it also exhibits properties of atypical antipsychotics due to significant serotonin receptor blockade[1][2][5][7].

Brand names
LoxitaneAdasuve
Other names
loxapine succinate
02

Targets

HTR2A (Serotonin receptor 5-HT2A)DRD2 (Dopamine D2 Receptor)

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