Loxapine

Indications
 Oral
Psychoses
Adult: Initially, 20-50 mg daily in 2 divided doses. Increase according to patient response and tolerance over the next 7-10 days to 60-100 mg daily or more, in 2-4 divided doses. Max dose: 250 mg daily. Maintenance dose range: 20-100 mg daily in divided doses.
Elderly: 20-60 mg/day.
Intramuscular
Acute psychosis
Adult: Up to 300 mg daily in 2-3 divided doses.
Elderly: Reduced dose may be required.
Contraindications
 Severe CNS depression, coma.
Warnings / Precautions
 Parkinson's disease. Haemodynamic instability; bone marrow suppression; predisposition to seizures; subcortical brain damage; severe cardiac, hepatic, renal or respiratory impairment. Patients at risk of pneumonia (e.g. Alzheimer's disease). Breast cancer or other prolactin-dependent tumours. Cerebrovascular disease. Decreased GI motility, urinary retention, benign prostatic hyperplasia, xerostomia or visual problems. Narrow-angle glaucoma; myasthenia gravis. May impair ability to drive or operate machinery. Pregnancy and lactation.
Adverse Reactions
 Arrhythmia, BP changes, orthostatic hypotension, tachycardia, syncope; agitation, ataxia, confusion, dizziness, drowsiness, extrapyramidal symptoms, faintness, headache, insomnia, lightheadedness, seizure, slurred speech, tension; sexual dysfunction, urinary retention; agranulocytosis, leukopenia, thrombocytopenia; muscle weakness; alopecia, dermatitis, photosensitivity, pruritus, rash, seborrhoea; amenorrhoea, irregular menstruation, breast enlargement, galactorrhoea, gynaecomastia; ileus, constipation, nausea, vomiting, polydipsia, wt changes, xerostomia; blurred vision; nasal congestion.
Potentially Fatal: Neuroleptic malignant syndrome.
Overdose Reactions
 Symptoms: Deep sleep, dystonia, agitation, dysrhythmias, extrapyramidal reactions, hypotension, seizures. Management: Symptomatic and supportive.
Drug Interactions
 Inhibits vasopressor effect of epinephrine.
Potentially Fatal: Additive CNS depression with other CNS depressants (e.g. benzodiazepines, barbiturates, alcohol).
See Below for More loxapine Drug Interactions
Lab Interactions
 False-positive tests for phenylketonuria, amylase, uroporphyrins, urobilinogen.
Food Interactions
 CNS depression may be increased with kava kava, gotu kola, valerian, St John's wort.
Mechanism of Actions
 Loxapine, a dibenzoxazepine antipsychotic, antagonises central dopaminergic action by blocking postsynaptic mesolimbic D1 and D2 receptors in the brain. It also has serotonin 5-HT2 inhibiting activity.
Absorption: Absorbed readily from the GI tract; peak plasma concentrations within 1-2 hr.
Distribution: Widely distributed; crosses the placenta and distributes into breast milk.
Metabolism: Very rapidly and extensively hepatic. Major metabolites: 7- and 8-hydroxyloxapine.
Excretion: Mainly via urine (as conjugated metabolites); via faeces (small amounts as unconjugated metabolites). 12-19 hr (terminal elimination half-life).
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store at 20-25°C (68-77°F).
ATC Classification
 N05AH01 - loxapine ; Belongs to the class of diazepines, oxazepines and thiazepines antipsychotics.
Storage
 Oral: Store at 20-25°C (68-77°F).
Available As
  • Loxapine 10 mg
  • Loxapine 25 mg
  • Loxapine 50 mg

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