Drug Guide
Loxapine Hydrochloride
Classification
Therapeutic: Antipsychotic
Pharmacological: Thioxanthene derivative
FDA Approved Indications
- Schizophrenia
- Locally established off-label uses (e.g., agitation in certain settings)
Mechanism of Action
Loxapine acts by antagonizing dopamine D2 receptors and, to a lesser extent, serotonin receptors, which reduces psychotic symptoms.
Dosage and Administration
Adult: Typically, 10-50 mg daily in divided doses; dosage individualized based on response and tolerability.
Pediatric: Use is not well-established; generally reserved for adult patients.
Geriatric: Start at lower doses; monitor closely for side effects.
Renal Impairment: Use with caution; adjust dose based on clinical response and tolerability.
Hepatic Impairment: Use with caution; hepatic function should be monitored.
Pharmacokinetics
Absorption: Well-absorbed orally, but bioavailability is reduced due to first-pass metabolism.
Distribution: Widely distributed; crosses the blood-brain barrier.
Metabolism: Primarily hepatic; metabolized via CYP450 enzymes.
Excretion: Excreted mainly in urine and feces as metabolites.
Half Life: Approximately 16 hours
Contraindications
- Comcomitant use with certain medications that prolong QT interval
- Hypersensitivity to loxapine or other phenothiazines
Precautions
- History of epilepsy
- Cardiovascular disease
- Liver disease
- History of seizures
- Pregnancy category C; risk-benefit assessment advised
Adverse Reactions - Common
- Sedation (Common)
- Orthostatic hypotension (Common)
- Dry mouth (Common)
- Extrapyramidal symptoms (Common)
Adverse Reactions - Serious
- Neuroleptic malignant syndrome (Rare)
- QT prolongation and arrhythmias (Rare)
- Agranulocytosis (Rare)
Drug-Drug Interactions
- Other CNS depressants
- Medications prolonging QT interval (e.g., certain antiarrhythmics, antibiotics)
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor mental status, extrapyramidal symptoms, cardiovascular status, and blood counts.
Diagnoses:
- Risk for falls
- Impaired skin integrity (due to sedation)
- Risk for cardiac arrhythmias
Implementation: Administer as prescribed; monitor for side effects; educate patient about potential adverse effects.
Evaluation: Assess therapeutic effectiveness and adverse reactions; adjust dose as necessary.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Avoid alcohol and CNS depressants unless advised by the healthcare provider.
- Report any signs of dehydration, fever, or abnormal movements.
- Be aware of potential sedation and orthostatic hypotension.
Special Considerations
Black Box Warnings:
- Increased mortality in elderly patients with dementia-related psychosis
Genetic Factors: Pharmacogenetic variations may affect metabolism; consider genetic testing if treatment failure or adverse effects occur.
Lab Test Interference: May increase prolactin levels; can induce leukopenia or neutropenia.
Overdose Management
Signs/Symptoms: Severe hypotension, extrapyramidal symptoms, sedation, seizures, coma.
Treatment: Supportive care; gastric lavage; activated charcoal; management of cardiac dysrhythmias; IV fluids; monitoring and correction of electrolytes.
Storage and Handling
Storage: Store at room temperature, away from light and moisture.
Stability: Stable for typical shelf life; check specific product labeling.