orap forte
orap forte 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 forte 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 forte 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 | orap forte |
Availability | Prescription only |
Generic | Pimozide |
Pimozide Other Names | Pimozida, Pimozide, Pimozidum |
Related Drugs | haloperidol, Haldol, Haldol Decanoate, Orap, Permax, pergolide |
Weight | 4mg, |
Type | Tablet |
Formula | C28H29F2N3O |
Weight | Average: 461.5462 Monoisotopic: 461.227868975 |
Groups | Approved |
Therapeutic Class | |
Manufacturer | Janssen Pharmaceutica N,v, |
Available Country | Saudi Arabia, Portugal |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
orap forte 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 forte is also used to associated treatment for these conditions: Delusional Parasitosis, Tics
How orap forte 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 forte 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.
orap forte Drug Interaction
Major: amphetamine / dextroamphetamine, acetaminophen / oxycodone, methylphenidate, atomoxetine, lisdexamfetamineModerate: aripiprazole, buspirone, fenfluramineMinor: armodafinilUnknown: multivitamin with minerals, guaifenesin / phenylephrine, apixaban, omega-3 polyunsaturated fatty acids, clopidogrel, aldesleukin, budesonide nasal, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol
orap forte Disease Interaction
Major: dementia, CNS depression/coma, previous neuroleptic malignant syndrome (NMS), seizure disorders, acute alcohol intoxication, CNS depression, NMS, tardive dyskinesia, pituitary tumors, QT interval prolongation, ticsModerate: seizure, hyperprolactinemia/breast cancer, neutropenia, anticholinergic effects, hyperprolactinemia, parkinsonism, renal/liver disease
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
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