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Pimozide information from DrugsUpdate  

See Available Brands of Pimozide in India

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

Pimozide (sold as Orap) is an antipsychotic drug. It was discovered at Janssen Pharmaceutica in 1963. It has a high potency compared to chlorpromazine (ratio 50-70:1). On a weight basis it is even more potent than haloperidol. It also has special neurologic indications for Tourette syndrome and resistant tics. The side effects include akathisia, tardive dyskinesia, and, more rarely, neuroleptic malignant syndrome and long QT syndrome.

Pharmacodynamics

Pimozide blocks the following postsynaptic receptors according to Bezchlinyk-Butler and Jeffries:

    * Extremely strong: D2
    * Strong: D3, ALPHA1, 5-HT2A
    * Moderate to moderately strong: DE1, D4, ALPHA2
    * Weak: ACH, H1
    * Extremely weak: 5-HT1A


Pimozide also inhibits moderately the dopamine-reuptake from the synaptic cleft, accounting for the stimulant properties of the drug. The inhibition of dopamine-reuptake may also explain the synergistic effects of pimozide in the treatment of ADHD when given together with a stimulant.

Pharmacokinetics

Pimozide is a long-acting antipsychotic structurally similar to butyrophenones which blocks dopaminergic receptors in the CNS. It also exhibits some calcium-blocking activity.

Absorption
>50% absorbed (oral); peak plasma levels after 4-12 hr.

Metabolism
Extensively hepatic via N-dealkylation.

Excretion

Urine and faeces (as unchanged drug and metabolites).

Pimozide Indications / Pimozide Uses

Information Not Available

Pimozide Adverse Reactions / Pimozide Side Effects

Extrapyramidal reactions, insomnia, drowsiness, dizziness. ECG changes, dry mouth, constipation, urinary difficulty and blurred vision.

Potentially Fatal: Neuroleptic malignant syndrome.

Precautions

Information Not Available

Special Precautions

Parkinson's syndrome; epilepsy, pregnancy, lactation; hepatic or renal impairment; monitor ECG before and during treatment; review the need for continuing treatment if repolarisation changes occur. Monitor cardiac function in patients taking >16 mg daily. Electrolytes disturbances such as hypomagnesaemia or hypokalaemia may increase risk of cardiotoxicity.

Other Drug Interactions

Propranolol and cimetidine decrease hepatic metabolism and increase efficacy and toxicity. Concurrent use with SSRIs may increase risk of extrapyramidal adverse effects and potentially fatal torsades de pointes arrhythmias.

Potentially Fatal: Potentiates other CNS depressants eg, alcohol and benzodiazepines. Increased risk of arrhythmias due to prolonged QT interval with TCAs, terfenadine, astemizole, antimalarial and cisapride. Concurrent use with inhibitors of CYP3A4 or CYP2D6 may lead to increased plasma concentrations leading to cardiac arrhythmias. Imatinib may also raise the plasma concentrations of pimozide. Avoid use with drugs that cause electrolyte disturbances eg, diuretics.

Other Interactions

Food Interaction
Concurrent use with grapefruit juice may increase the blood concentrations of pimozide.

Dosage

Oral
Schizophrenia
Adult: Initially, 2 mg daily adjusted according to response by increments of 2-4 mg at intervals of not <1 week. Max dose: 20 mg/day.
Child: 12-18 years: Initial dose: 1 mg daily.

Oral
Monosymptomatic hypochondria
Adult: Initially, 4 mg daily adjusted according to response by increments of 2-4 mg at intervals of not <1 week. Max dose: 16 mg/day.
Elderly: Half the usual initial dose.

Oral
Paranoid states
Adult: Initially, 4 mg daily adjusted according to response by increments of 2-4 mg at intervals of not <1 week. Max dose: 16 mg/day.
Elderly: Half the usual initial dose.

Oral
Tourette's syndrome
Adult: Initially, 1-2 mg or 200 mcg/kg daily. Max dose: 10 mg/day.
Child: >12 years: initial dose: 50 mcg/kg.

Food(before/after)

May be taken with or without food

List of Contraindications

Pimozide 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.

Pimozide and Lactation

Caution when used during lactation

Pimozide and Children

Limited information regarding use, efficacy, and safety in patients younger than 12 years of age.

Pimozide and Geriatic

Information Not Available

Pimozide and Other Contraindications

Prolonged QT interval, family history of congenital QT prolongation, history of cardiac arrhythmias.

Storage

Information Not Available

Lab interference

Information Not Available

Pimozide brands in India:

Larap Mozep Neurap Notic Orap Pimodac Pimoz R Zep

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