Loxitane (loxapine) is a first-generation antipsychotic medication belonging to the dibenzoxazepine class, indicated for the management of schizophrenia. It functions primarily as a dopamine D2 and serotonin 5-HT2A receptor antagonist, modulating neurotransmitter activity to alleviate symptoms of psychosis. Clinically, it is recognized for its efficacy in reducing positive symptoms such as hallucinations and delusions, while also demonstrating utility in certain cases for managing agitation. Its well-established pharmacokinetic profile allows for predictable dosing and monitoring, making it a reliable option within a comprehensive treatment plan under specialist supervision.

Features

• Active ingredient: Loxapine (as loxapine succinate or hydrochloride)
• Available formulations: Oral capsules (5 mg, 10 mg, 25 mg, 50 mg); inhalation powder (Adasuve®)
• Receptor affinity: Dopamine D2, serotonin 5-HT2A, adrenergic α1
• Half-life: Approximately 4–12 hours (oral); rapid onset with inhalation
• Metabolism: Hepatic, primarily via CYP1A2 and CYP3A4
• Excretion: Renal and fecal

Benefits

• Effectively reduces positive psychotic symptoms including hallucinations, delusions, and disorganized thinking
• May help improve overall behavioral control and social functioning in patients with schizophrenia
• Available in both oral and inhaled formulations, offering flexibility in administration based on clinical need
• Established safety and efficacy profile supported by decades of clinical use and research
• Can be used as part of a combination therapy regimen under psychiatric guidance

Common use

Loxitane is primarily prescribed for the treatment of schizophrenia in adults. It is used to manage both acute psychotic episodes and for maintenance therapy to prevent relapse. In some cases, it may be used off-label for acute agitation in bipolar disorder or other psychiatric conditions, though such use requires careful risk-benefit assessment. The inhalation form (Adasuve®) is specifically approved for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults.

Dosage and direction

Dosage must be individualized based on symptom severity, patient response, and tolerability. For oral administration in schizophrenia: initial dose is typically 10 mg twice daily, which may be increased gradually over 7–10 days to a therapeutic range of 60–100 mg/day divided into 2–4 doses. Maximum daily dose should not exceed 250 mg. For inhalation powder (Adasuve®): a single 10 mg dose is administered using a proprietary inhaler; not to be repeated within 24 hours. Administration should always follow a healthcare provider’s instructions, and tablets should be taken with food or water to minimize gastrointestinal upset.

Precautions

Patients should be monitored regularly for extrapyramidal symptoms (EPS), tardive dyskinesia, and neuroleptic malignant syndrome (NMS). Use with caution in elderly patients with dementia-related psychosis due to increased risk of mortality and cerebrovascular events. May cause drowsiness or dizziness; advise against operating machinery or driving until response is known. Regular assessments of weight, blood glucose, and lipid levels are recommended due to potential metabolic effects. Avoid abrupt discontinuation; taper under medical supervision.

Contraindications

Hypersensitivity to loxapine or any component of the formulation. Severe central nervous system depression or comatose states. Concurrent use with other potent CNS depressants without careful monitoring. The inhalation form is contraindicated in patients with asthma, chronic obstructive pulmonary disease (COPD), or other underlying lung diseases due to risk of bronchospasm. Not recommended in patients with a history of severe cardiovascular disorders or those with known risk factors for QT prolongation.

Possible side effects

Common side effects may include drowsiness, dizziness, dry mouth, constipation, blurred vision, and weight gain. Extrapyramidal symptoms such as akathisia, dystonia, parkinsonism, and tardive dyskinesia may occur. Less frequently, orthostatic hypotension, tachycardia, seizures, or elevated prolactin levels may be observed. The inhalation form carries a risk of bronchospasm, which requires immediate medical attention. Any signs of NMS (e.g., hyperpyrexia, muscle rigidity, autonomic instability) warrant discontinuation and emergency care.

Drug interaction

Loxitane may potentiate effects of CNS depressants including alcohol, benzodiazepines, and opioids. Concurrent use with other antipsychotics or drugs that prolong QT interval (e.g., certain antiarrhythmics, antibiotics) should be avoided or closely monitored. CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin) may increase loxapine levels, while inducers (e.g., carbamazepine, smoking) may decrease efficacy. Anticholinergic agents may exacerbate certain side effects. Always inform the prescriber of all current medications, including over-the-counter and herbal products.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next dose. In that case, skip the missed dose and resume the regular schedule. Do not double the dose to make up for a missed one. Consistent adherence is important for maintaining therapeutic effect; patients should contact their healthcare provider if multiple doses are missed.

Overdose

Symptoms of overdose may include severe drowsiness, hypotension, tachycardia, extrapyramidal symptoms, convulsions, and coma. Management is supportive and symptomatic; there is no specific antidote. Activated charcoal may be considered if ingestion was recent. Ensure airway protection and provide cardiovascular monitoring. Contact a poison control center or seek emergency medical attention immediately.

Storage

Store at room temperature (20–25°C or 68–77°F), away from light, moisture, and heat. Keep in the original container, tightly closed, and out of reach of children and pets. Do not use beyond the expiration date. The inhalation device is for single use only and should be disposed of properly after administration.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Do not disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

“Loxitane has been a cornerstone in my practice for treatment-resistant schizophrenia. Its predictable pharmacokinetics and dual receptor activity provide a balance of efficacy and tolerability when monitored appropriately.” – Dr. Elena Rostova, MD, Psychiatry

“While newer agents are often preferred first-line, Loxitane remains a valuable option, especially in cases where cost or specific side effect profiles are a concern. The inhalation form offers a rapid alternative for acute agitation.” – Clinical Pharmacologist Review, Journal of Psychiatric Medicine

“Patient response has been generally positive with careful titration. Slower dose escalation helps mitigate early extrapyramidal symptoms, making it a manageable option for long-term therapy.” – Psychiatric Nurse Practitioner Survey