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NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diazepines, oxazepines, thiazepines and oxepines
loxapine
N05AH01
Forms & Strengths
- Capsule: 5 mg, 10 mg, 25 mg, 50 mg
- Inhalation powder: 10 mg (Adasuve)
- Concentrate: 25 mg/mL (historical/discontinued in some regions)
Adult Dosing
- Oral (Schizophrenia): Initial 10 mg twice daily, titrate up to 20-50 mg twice daily; maintenance range 20-250 mg/day in divided doses
- Inhalation (Agitation associated with schizophrenia or bipolar disorder): 10 mg single dose via dedicated inhaler; max 1 dose per 24 hours
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 18 years of age
Indications
- Management of manifestations of schizophrenia
- Rapid treatment of acute agitation associated with schizophrenia or bipolar I disorder (inhalation form)
Mechanism of Action
- Dibenzo-oxazepine dibenzodiazepine derivative classified as a typical (first-generation) antipsychotic
- Exerts antipsychotic activity primarily through strong antagonism at central dopamine D2 and serotonin 5-HT2 receptors
Contraindications
- Hypersensitivity to loxapine or amoxapine
- Comatose or severely depressed states from any cause
- History of bronchospasm, asthma, or active airway disease (for inhalation formulation due to risk of severe bronchospasm)
Adverse Reactions
- Extrapyramidal symptoms including akathisia, dystonia, and parkinsonism
- Sedation, somnolence, and dizziness
- Anticholinergic effects such as dry mouth, constipation, and blurred vision
- Tardive dyskinesia with long-term use
- Neuroleptic Malignant Syndrome (rare)
- Bronchospasm, wheezing, and dyspnea (specifically with inhalation route)
Drug Interactions
- Central nervous system (CNS) depressants and alcohol: additive sedation and respiratory depression
- Anticholinergic agents: increased risk of severe anticholinergic adverse effects
- Dopamine agonists (e.g., levodopa): mutual antagonism of therapeutic effects
- Drugs lowering the seizure threshold: increased risk of seizures
Curated Content: Needs Vetting Before Put to Clinical Use