loxapine
Brands: Loxitane, Adasuve
Last reviewed 2025-12-29
Reviewed by PsychMed Editorial Team.
Quick answers
What is loxapine?
Loxapine is a mid-potency first-generation antipsychotic with serotonergic antagonism resembling second-generation antipsychotics (SGAs), available orally and as inhaled powder for acute agitation.
What is Loxitane?
Loxitane is a brand name for loxapine (other brands: Adasuve).
What is Loxitane (loxapine) used for?
Label indications include: Schizophrenia (oral); Acute agitation in schizophrenia/bipolar I (inhaled).
What drug class is Loxitane (loxapine)?
Antipsychotic.
What is the mechanism of action of Loxitane (loxapine)?
Mid-potency typical antipsychotic antagonizing dopamine D2 and serotonin 5-HT2A receptors with additional H1 and M1 blockade.
What strengths does Loxitane (loxapine) come in?
Oral capsules: 5–50 mg; oral concentrate 5 mg/mL.
Is Loxitane (loxapine) a controlled substance?
No — it is not scheduled as a controlled substance under U.S. federal law.
Snapshot
- Class: Antipsychotic
- Common US brands: Loxitane, Adasuve
- Therapeutic drug monitoring not routinely recommended.
- Last reviewed: 2025-12-29
Clinical Highlights
Loxapine is a mid-potency first-generation antipsychotic with serotonergic antagonism resembling second-generation antipsychotics (SGAs), available orally and as inhaled powder for acute agitation. Used in adult schizophrenia and bipolar agitation (inhaled formulation under REMS controls).
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- Inhaled loxapine (Adasuve) is designed for rapid tranquilization in supervised settings; bronchospasm risk and monitoring requirements make it a niche option rather than a routine outpatient PRN.
- For oral maintenance, expect sedation and dizziness early; bedtime dosing, slow titration, and fall-risk planning help patients stay on therapy when cost limits SGA access.
- Selected for cost-sensitive maintenance regimens or when inhaled rapid-acting therapy is desirable; Adasuve’s bronchospasm risk and REMS observation requirements shape patient selection and follow-up via the bipolar disorder hub.
- The compare tool and loxapine evidence feed can help weigh EPS, metabolic, and inhaled-versus-oral trade-offs when considering therapy changes.
- Schizophrenia (oral) (FDA 1975)
- Acute agitation in schizophrenia/bipolar I (inhaled) (FDA 2012)
- Generic: Oral products available generically; inhaled formulation remains brand-only (REMS).
Dosing & Formulations
Oral capsules: 5–50 mg; oral concentrate 5 mg/mL. Inhaled powder (Adasuve) 10 mg single-use device.
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- Oral: start 10 mg BID; titrate to 60–100 mg/day divided (max 250 mg/day).
- Inhaled (Adasuve): 10 mg per administration; may repeat once ≥2 h later (max 20 mg/day) under REMS monitoring.
Monitoring & Risks
Boxed warning: Increased mortality in elderly patients with dementia-related psychosis. Sedation: Frequent due to H1 blockade.
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- Dizziness: Notable during initiation.
- Orthostatic hypotension: From α1 antagonism.
- Anticholinergic effects: Dry mouth and constipation.
- Extrapyramidal symptoms: Dose dependent (~10–15%).
- AIMS screening for tardive dyskinesia is commonly used, and weight, lipids, and glucose are typically tracked over time even when average metabolic risk is lower than with clozapine/olanzapine.
- Adasuve (inhaled) can cause bronchospasm and is contraindicated in asthma/COPD; administration is limited to REMS-certified settings with rescue bronchodilator availability and ≥1 hour observation.
Drug Interactions
CYP1A2/CYP3A4 inhibitors increase levels; smoking or enzyme inducers reduce exposure. Additive CNS depression with alcohol or benzodiazepines.
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- Potentiates antihypertensives via α1 blockade.
- Other QT-active or orthostasis-promoting medications can compound risk; baseline ECG is commonly considered when cardiac risk factors are present.
Practice Notes
EPS and metabolic monitoring often follow patterns used for other antipsychotics. REMS certification required for Adasuve; patients are observed ≥1 h post dose for bronchospasm.
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- SGAs are often considered if metabolic or EPS burden is problematic long-term.
- Agitation pathways often include a clear escalation plan (e.g., when to switch to IM antipsychotic/benzodiazepine, airway monitoring, and follow-up) rather than repeat PRN dosing alone.
- Acute agitation plans typically include a clear transition strategy to maintenance treatment (oral antipsychotic optimization, LAI consideration, and follow-up on the bipolar disorder hub when relevant).