Orap 1%

Orap 1% 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)

Orap 1% 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. Orap 1% 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).

Orap 1%
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Orap 1%
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	Japan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Orap 1% 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.

Orap 1% is also used to associated treatment for these conditions: Delusional Parasitosis, Tics

How Orap 1% 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. Orap 1% 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.