Pimozide drug data and news

Pimozide drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Pimozide
Brand Names/Synonyms 6238; Haldol Decanoate; Halomonth; KD-136; Mcn-Jr 6238; Neoperidole; Opiran; Orap; Pimozide; Pimozide [Usan:Ban:Inn:Jan]; Pimozidum [Inn-Latin]; Primozida [Inn-Spanish]; R 6238
Indication Used for the suppression of motor and phonic tics in patients with Tourette's Disorder who have failed to respond satisfactorily to standard treatment.
Sponsored links
Description Not Available
Pharmacology Pimozide 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. Although its exact mode of action has not been established, the ability of Pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be a function of its dopaminergic blocking activity. 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.
Mechanism Of Action Although its exact mode of action has not been established, the ability of Pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be a function of its dopaminergic blocking activity. Pimozide binds to the dopamine D2 receptor
Pimozide News
(When available)
Dosage Forms TABLET
Drug_Category Antidyskinetics; Antipsychotics; Antipsychotics; ATC:N05AG02
Absorption >50% absorption after oral administration, serum peak appears 6-8 hours post ingestion.
Interactions -->Interactions for Pimozide:

Because ORAP prolongs the QT interval of the electrocardiogram, an additive effect on QT interval would be anticipated if administered with other drugs, such as phenothiazines, tricyclic antidepressants or antiarrhythmic agents, which prolong the QT interval. Accordingly, pimozide should not be given with dofetilide, sotalol, quinidine, other Class Ia and III anti-arrhythmics, mesoridazine, thioridazine, chlorpromazine, droperidol, sparfloxacin, gatifloxacin, moxifloxacin, halofantrine, mefloquine, pentamidine, arsenic trioxide, levomethadyl acetate, dolasetron mesylate, probucol, tacrolimus, ziprasidone, or other drugs that have demonstrated QT prolongation as one of their pharmacodynamic effects. Also, the use of macrolide antibiotics in patients with prolonged QT intervals has been rarely associated with ventricular arrhythmias. Such concomitant administration should not be undertaken.

Since ORAP is partly metabolized via CYP 3A4, it should not be administered concomitantly with inhibitors of this metabolic system, such as azole antifungal agents and protease inhibitor drugs.

As CYP 1A2 may also contribute to the metabolism of ORAP, prescribers should be aware of the theoretical potential for drug interactions with inhibitors of this enzymatic system

ORAP may be capable of potentiating CNS depressants, including analgesics, sedatives, anxiolytics, and alcohol.

Rare case reports have suggested possible additive effects of pimozide and fluoxetine leading to bradycardia.

Concomitant administration of pimozide and sertraline should be contraindicated.

Interaction with Food

Patients should avoid grapefruit juice because it may inhibit the metabolism of pimozide by CYP 3A4.

Toxicity LD50 = 1100 mg/kg (rat, oral), 228 mg/kg (mouse, oral)
Organisms Affected Humans and other mammals
Chemical IUPAC Name 1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidyl]-1,3-dihydrobenzoimidazol-2-one
Chemical Formula C28H29F2N3O
Molecular Weight 461.546 g/mol
Smiles String C1CN(CCC1N2C3=CC=CC=C3NC2=O)CCCC(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F
Melting Point 214-218 °C
Water Solubility 10 mg/L
State Solid
LogP/Hphobicity 5.849
Isoelectric Point 8.63
Biotransformation Primarily hepatic
Half Life 55 hours
Protein Binding [%] Not Available
RxList Link RXlist
Sponsored links
Drug Reference http://www.drugs.com/cons/Pimozide.html
http://www.rxlist.com/cgi/generic3/orap.htm
Drug Type Approved Drug
Accession No APRD00218
CAS Registry Number 2062-78-4
KEGG Compound ID C07566
PubChem ID SID:159615
PharmGKB ID PA450965
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2245433

Home | About | Cancers | Treatment | Medications
Copyright onconews.org 2005.
All Rights Reserved.
Google
 
Web onconews.org