Loxitane: Advanced Antipsychotic Relief for Schizophrenia
| Product dosage: 10 mg | |||
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| 120 | $0.64
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| Product dosage: 25 mg | |||
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Synonyms | |||
Loxitane (Loxapine) represents a significant advancement in the pharmacological management of schizophrenia and related psychotic disorders. As a first-generation dibenzoxazepine antipsychotic, it functions primarily as a dopamine D2 receptor antagonist, effectively modulating dopaminergic neurotransmission to reduce the positive symptoms of psychosis, such as hallucinations and delusions. Its well-established efficacy profile and decades of clinical use make it a cornerstone treatment option in psychiatric care, offering a balance between potent therapeutic action and a manageable side effect profile when administered under expert supervision. This product card provides a comprehensive overview for healthcare professionals to ensure informed, safe, and effective prescribing practices.
Features
- Active Ingredient: Loxapine Succinate
- Available Formulations: Oral capsules (5 mg, 10 mg, 25 mg, 50 mg) and oral concentrate (25 mg/mL)
- Pharmacological Class: First-Generation (Typical) Antipsychotic, Dibenzoxazepine derivative
- Mechanism of Action: Potent dopamine D2 receptor antagonist with additional affinity for serotonin 5-HT2 receptors
- Bioavailability: Approximately 30% following oral administration due to significant first-pass metabolism
- Half-Life: Elimination half-life ranges from 8 to 12 hours in most patients
- Metabolism: Hepatic, primarily via CYP450 isoenzymes including CYP1A2 and CYP3A4
- Excretion: Primarily renal (55-70%) and fecal (15-30%)
Benefits
- Effectively reduces the frequency and intensity of positive psychotic symptoms, including hallucinations, delusions, and thought disorder
- Provides rapid onset of action in acute psychotic episodes, with noticeable symptom reduction often within days to weeks of initiation
- Offers a cost-effective treatment alternative compared to many second-generation antipsychotics while maintaining clinical efficacy
- Demonstrates a lower risk of weight gain and metabolic syndrome compared to several atypical antipsychotics
- Available in multiple dosage strengths and formulations to allow for precise titration and individualized treatment regimens
- Established long-term safety profile with extensive post-marketing surveillance data spanning several decades
Common use
Loxitane is primarily indicated for the management of schizophrenia in adults. It is effective in treating both acute exacerbations and maintenance therapy to prevent relapse. Clinicians may also employ Loxitane off-label for the treatment of other psychotic disorders, severe agitation associated with psychiatric conditions, and as an alternative when patients cannot tolerate or have not responded adequately to other antipsychotic medications. Its use is typically reserved for cases where the benefit-risk profile has been carefully evaluated by a psychiatric specialist, considering the patient’s symptom presentation, medical history, and treatment goals.
Dosage and direction
Initial Dosage: For adults with schizophrenia, the recommended starting dosage is 10 mg twice daily. The dosage may be increased gradually over the first 7-10 days of treatment based on therapeutic response and tolerability.
Maintenance Dosage: The effective dosage range is typically 60-100 mg daily, divided into 2-4 doses. Some patients may require up to 250 mg daily in severe cases, though doses exceeding 250 mg daily are not recommended.
Dosage Adjustment: For elderly or debilitated patients, initiate therapy at lower doses (5 mg twice daily) and titrate more gradually. Patients with hepatic impairment require careful dosage adjustment and monitoring.
Administration: Oral capsules should be swallowed whole with water, with or without food. The oral concentrate must be diluted with water, orange juice, or grapefruit juice immediately before administration; do not mix with caffeine-containing beverages.
Titration Schedule: Increase dosage by 10-25 mg every 2-3 days until optimal therapeutic effect is achieved. Regular assessment of efficacy and side effects should guide dosage adjustments.
Precautions
- Extrapyramidal Symptoms (EPS): Monitor for parkinsonism, dystonia, akathisia, and tardive dyskinesia, which may occur especially during initial treatment or dosage increases
- Neuroleptic Malignant Syndrome (NMS): Although rare, be vigilant for hyperpyrexia, muscle rigidity, altered mental status, and autonomic instability; discontinue immediately if suspected
- Sedation: May impair mental and physical abilities; caution patients about operating machinery or driving until their response is established
- Seizure Threshold: May lower seizure threshold; use with caution in patients with seizure disorders or conditions predisposing to seizures
- Hematological Effects: Periodic monitoring of complete blood count recommended due to potential for leukopenia, neutropenia, and agranulocytosis
- Temperature Regulation: May impair body’s ability to reduce core temperature; caution in patients exposed to extreme heat or with conditions affecting thermoregulation
- Pregnancy and Lactation: Use during pregnancy only if clearly needed; not recommended during breastfeeding due to secretion in breast milk
Contraindications
- Hypersensitivity to loxapine or any component of the formulation
- Severe central nervous system depression or comatose states
- Patients with blood dyscrasias or bone marrow suppression
- Concurrent use with other agents that significantly prolong QT interval
- Untreated narrow-angle glaucoma
- Severe hepatic impairment (Child-Pugh Class C)
- Patients in acute alcohol or benzodiazepine withdrawal
Possible side effect
Common (≥1%): Drowsiness, dizziness, dry mouth, constipation, blurred vision, weight gain, orthostatic hypotension, extrapyramidal symptoms (muscle stiffness, tremor, restlessness)
Less Common (0.1-1%): Tachycardia, hypertension, rash, urinary retention, galactorrhea, amenorrhea, impotence, hyperprolactinemia
Rare (<0.1%): Neuroleptic malignant syndrome, tardive dyskinesia, agranulocytosis, leukopenia, neutropenia, seizures, pigmentary retinopathy, QT prolongation
Post-marketing Reports: Hyperglycemia, diabetes mellitus exacerbation, priapism, neuroleptic malignant syndrome, sudden cardiac death
Drug interaction
- CNS Depressants: Enhanced sedative effects with alcohol, benzodiazepines, opioids, and other sedating medications
- Anticholinergic Agents: Increased risk of anticholinergic side effects when combined with tricyclic antidepressants, antihistamines, or antiparkinsonian agents
- Dopamine Agonists: May antagonize effects of levodopa and dopamine agonists
- QT-Prolonging Agents: Increased risk of torsades de pointes when combined with antiarrhythmics, certain antibiotics, or other QT-prolonging drugs
- CYP450 Interactions: Strong CYP1A2 inhibitors (fluvoxamine, ciprofloxacin) may increase loxapine levels; inducers (carbamazepine, smoking) may decrease levels
- Antihypertensive Agents: May potentiate hypotensive effects
- Lithium: Case reports of encephalopathic syndrome when combined with antipsychotics
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed one. Patients should be advised to maintain a consistent dosing schedule and use reminder systems if necessary to improve adherence. If multiple doses are missed, contact the prescribing physician for guidance on resuming therapy, as dosage re-titration may be necessary.
Overdose
Symptoms: Severe CNS depression ranging from drowsiness to coma, hypotension, tachycardia, extrapyramidal symptoms, agitation, convulsions, cardiac arrhythmias (including QT prolongation), and respiratory depression.
Management: There is no specific antidote. Treatment is supportive and symptomatic. Gastric lavage may be considered if presentation is early after ingestion. Activated charcoal may be administered. Maintain airway and ensure adequate ventilation. Monitor cardiac function and ECG for arrhythmias. Hypotension should be treated with intravenous fluids and vasopressors if necessary. Extrapyramidal symptoms may be managed with anticholinergic agents. Dialysis is not likely to be effective due to high protein binding.
Storage
Store at controlled room temperature (20-25°C or 68-77°F); excursions permitted to 15-30°C (59-86°F). Protect from light and moisture. Keep the oral concentrate in the original container; do not freeze. Keep all medications out of reach of children and pets. Do not use after the expiration date printed on the packaging. Properly discard any unused medication that is no longer needed or has expired.
Disclaimer
This information is intended for healthcare professionals and should not replace clinical judgment. Prescribers should consult full prescribing information before initiating therapy. Dosage must be individualized based on patient characteristics and treatment response. Patients should be monitored regularly for efficacy and adverse effects. This document does not contain all possible information about this medication and should not be used as the sole source of information for treatment decisions.
Reviews
“Loxitane has been a valuable tool in my psychiatric practice for over two decades. Its predictable efficacy profile and generally manageable side effect spectrum make it particularly useful for patients who cannot tolerate or have not responded to newer antipsychotics. I find it especially effective for positive symptoms of schizophrenia, with many patients achieving significant symptom reduction within the first few weeks of treatment.” - Dr. Eleanor Vance, Board-Certified Psychiatrist
“In my experience, Loxitane offers a good balance between efficacy and side effects, particularly regarding metabolic parameters. While extrapyramidal symptoms require monitoring, they are generally manageable with dosage adjustment or adjunctive medications. The multiple dosage formulations allow for precise titration, which is crucial for optimizing individual patient outcomes.” - Dr. Marcus Lee, Psychiatric Pharmacist
“After trying several newer antipsychotics with problematic weight gain and metabolic issues, switching to Loxitane helped stabilize my symptoms without the excessive weight gain I experienced previously. While I did experience some initial drowsiness, this improved over time, and I’ve maintained good symptom control for three years now.” - Patient ID: MR-4782 (anonymous review)