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Loxapine information from DrugsUpdate  

See Available Brands of Loxapine in India

P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *
LI - Lab *

Loxapine (sold as Loxapac, Loxitane) is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. It is a member of the dibenzoxazepine class and as a dibenzazepine derivative, it is structurally related to clozapine (which belongs to the chemically closely akin class of dibenzodiazepines). Several researchers have argued that Loxapine may behave as an atypical antipsychotic .

Loxapine may be metabolized by N-demethylation to amoxapine, a tricyclic antidepressant.

Pharmacodynamics

Pharmacologically, Loxapine is an antipsychotic for which the exact mode of action has not been established. However, changes in the level of excitability of subcortical inhibitory areas have been observed in several animal species in association with such manifestations of tranquilization as calming effects and suppression of aggressive behavior.

In normal human volunteers, signs of sedation were seen within 20 to 30 minutes after administration, were most pronounced within 1½ to 3 hours, and lasted through 12 hours. Similar timing of primary pharmacologic effects was seen in animals.

Pharmacokinetics

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 hours.

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 hours (terminal elimination half-life).

Loxapine Indications / Loxapine Uses

Information Not Available

Loxapine Adverse Reactions / Loxapine Side Effects

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.

Precautions

Care should be taken with consumption. At least 3 cases were reported of loxapine succinate abuse.

Overdosage

Symptoms: Deep sleep, dystonia, agitation, dysrhythmias, extrapyramidal reactions, hypotension, seizures. Management: Symptomatic and supportive.

Special 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.

Other Drug Interactions

Inhibits vasopressor effect of epinephrine.

Potentially Fatal: Additive CNS depression with other CNS depressants (e.g. benzodiazepines, barbiturates, alcohol).

Other Interactions

Food Interaction
CNS depression may be increased with kava kava, gotu kola, valerian, St John's wort.

Dosage

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.

Food(before/after)

Should be taken with food

List of Contraindications

Loxapine and Pregnancy

Caution when used during pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Loxapine and Lactation

Caution when used during lactation

Loxapine and Children

Safety and efficacy not established

Loxapine and Geriatic

Information Not Available

Loxapine and Other Contraindications

Severe CNS depression, coma

Storage

Oral
Store at 20-25°C (68-77°F)

Lab interference

Oral
Store at 20-25°C (68-77°F)

Loxapine brands in India:

Dibeta-SR Enipaxol Loxapac Loxaris

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