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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.
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| 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) |
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| 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 |
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