Pimozidum

Pimozidum Uses, Dosage, Side Effects, Food Interaction and all others data.

A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to haloperidol for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)

Pimozidum is an orally active antipsychotic drug product which shares with other antipsychotics the ability to blockade dopaminergic receptors on neurons in the central nervous system. However, receptor blockade is often accompanied by a series of secondary alterations in central dopamine metabolism and function which may contribute to both pimozide's therapeutic and untoward effects. In addition, pimozide, in common with other antipsychotic drugs, has various effects on other central nervous system receptor systems which are not fully characterized. Pimozidum also has less potential for inducing sedation and hypotension as it has more specific dopamine receptor blocking activity than other neuroleptic agents (and is therefore a suitable alternative to haloperidol).

Trade Name Pimozidum
Availability Prescription only
Generic Pimozide
Pimozide Other Names Pimozida, Pimozide, Pimozidum
Related Drugs haloperidol, Haldol, Haldol Decanoate, Orap, Permax, pergolide
Type
Formula C28H29F2N3O
Weight Average: 461.5462
Monoisotopic: 461.227868975
Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Pimozidum
Pimozidum

Uses

Pimozidum is an antipsychotic used to manage debilitating motor and phonic tics in patients with Tourette's Disorder.

Used for the suppression of motor and phonic tics in patients with Tourette's Disorder who have failed to respond satisfactorily to standard treatment.

Pimozidum is also used to associated treatment for these conditions: Delusional Parasitosis, Tics

How Pimozidum works

The ability of pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be primarily a function of its dopaminergic blocking activity. Pimozidum binds and inhibits the dopamine D2 receptor in the CNS.

Toxicity

LD50 = 1100 mg/kg (rat, oral), 228 mg/kg (mouse, oral)

Food Interaction

  • Avoid grapefruit products. Grapefruit inhibits CYP3A4 and, therefore, may increase pimozide serum levels.
  • Exercise caution with St. John's Wort.

[Major] GENERALLY AVOID: Theoretically, the coadministration with grapefruit juice may increase the plasma concentrations of pimozide.

The mechanism is decreased clearance of pimozide due to inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.

The use of pimozide alone has been associated with dose-dependent prolongation of the QT interval.

Although clinical data are lacking, this interaction may result in potentiation of the proarrhythmic effect of pimozide and consequently an increased risk of ventricular arrhythmias such as ventricular tachycardia and torsade de pointes.

In addition, alcohol may potentiate some of the pharmacologic effects of pimozide.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: The manufacturer recommends avoiding grapefruit juice (and probably grapefruits) during therapy with pimozide.

Patients should also be advised to avoid or limit consumption of alcohol.

Elimination Route

Greater than 50% absorption after oral administration. Serum peak appears 6-8 hours post ingestion.

Half Life

29 ± 10 hours (single-dose study of healthy volunteers).

Innovators Monograph

You find simplified version here Pimozidum

*** Taking medicines without doctor's advice can cause long-term problems.
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