Loxapine

Trade Names:
Loxitane
- Capsule 5 mg
- Capsule 10 mg
- Capsule 25 mg
- Capsule 50 mg

Pharmacology

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Unknown. Changes level of excitability of subcortical inhibitory areas in some animals.

Pharmacokinetics

Absorption

T _max is 1 h.

Distribution

Widely distributed in the tissues; 91% to 99% protein bound. Highly lipophilic.

Metabolism

First-pass metabolism. Metabolites found in serum are 8-hydroxyloxapine and 8-hydroxydesmethylloxapine. Extensively metabolized.

Elimination

The apparent t _½ is 4 h (1 to 14 h). Approximately 40% is recovered in urine as metabolites.

Onset

20 to 30 min.

Peak

1.5 to 3 h.

Duration

12 h.

Indications and Usage

Treatment of schizophrenia.

Contraindications

Comatose or severe drug-induced depressed states (eg, barbiturates); hypersensitivity to dibenzoxazepines.

Dosage and Administration

PO 10 mg twice daily, up to 50 mg/day, titrated fairly rapidly over first 7 to 10 days until symptoms are controlled.

Reduce dosage to lowest amount compatible with symptom control. Usual range is 60 to 100 mg/day; many patients have been maintained satisfactorily at a dosage range of 20 to 60 mg/day. Dosages higher than 250 mg/day are not recommended.

General Advice

Administer without regard to meals. Administer with food if GI upset occurs.

Storage/Stability

Store capsules at controlled room temperature (59° to 86°F).

Drug Interactions

Respiratory depression, stupor, and hypertension may occur.

Levels may be decreased by loxapine, decreasing phenytoin's effectiveness.

Adverse Reactions

Cardiovascular

Tachycardia, hypotension, hypertension, orthostatic hypotension, lightheadedness, syncope.

CNS

Extrapyramidal effects, transient drowsiness, sedation, dizziness, faintness, staggering gait, shuffling gait, muscle twitching, weakness, insomnia, agitation, tension, seizures, akinesia, slurred speech, numbness, mental confusion, neuroleptic malignant syndrome (NMS), dystonic (eg, muscle spasms of the neck and face) and dyskinetic reactions (eg, choreoathetoid movements), tardive dyskinesia, headache.

Dermatologic

Edema, pruritus, rash, alopecia, seborrhea.

EENT

Nasal congestion, blurred vision.

GI

Dry mouth, constipation, paralytic ileus, nausea, vomiting.

Genitourinary

Urinary retention, amenorrhea, gynecomastia, menstrual irregularity.

Hematologic

Agranulocytosis, thrombocytopenia, leukopenia.

Hepatic

Hepatocellular injury, jaundice, hepatitis.

Metabolic

Weight gain/loss.

Respiratory

Dyspnea.

Miscellaneous

Hyperpyrexia, facial flushing, paresthesia, ptosis, polydipsia, prolactin levels increased.

Precautions

Pregnancy

Undetermined.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Special Risk Patients

Use with extreme caution in patients with a history of convulsive disorders, CV disease, glaucoma, or tendency for urinary retention.

NMS

This potentially fatal condition has been reported in association with antipsychotic agents. Signs and symptoms include hyperpyrexia, muscle rigidity, altered mental status, irregular pulse or BP, tachycardia, diaphoresis, and cardiac arrhythmias.

Ocular toxicity

Carefully observe patient for pigmentary retinopathy and lenticular pigmentation.

Tardive dyskinesia

This syndrome of potentially irreversible, involuntary, dyskinetic movements has occurred with other antipsychotic agents. Incidence appears to be highest among the elderly.

Overdosage

Symptoms

CV and CNS depression, profound hypotension, respiratory depression, unconsciousness, extrapyramidal symptoms, convulsive seizures, renal failure.

Patient Information

• Explain name, dose, action, and potential side effects of drug, including risk of developing tardive dyskinesia.
• Advise patient that dose will be started low and then increased until max benefit is achieved; advise patient not to take more than prescribed or increase the dose more rapidly than advised.
• Advise patient to take prescribed dose without regard to meals, but to take with food if stomach upset occurs.
• Instruct patient not to change the dose or stop taking unless advised by health care provider.
• Instruct patient not to stop taking loxapine when symptoms have improved.
• Tell patient to immediately report high fever, muscle rigidity, involuntary body or facial movements, altered mental status, irregular pulse, or sweating to health care provider.
• Advise patient to avoid strenuous activity during periods of high temperature or humidity.
• Instruct patient to avoid alcohol and other CNS depressant medications.
• Advise patient to take sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
• Advise patient to notify health care provider if excessive drowsiness occurs.

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