3026 Pimozide 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) 2062-78-4 16362 C28H29F2N3O 461.227870 White powder. 214-218°C 10 mg/L (at 25°C) Greater than 50% absorption after oral administration. Serum peak appears 6-8 hours post ingestion. 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. Pimozide binds and inhibits the dopamine D2 receptor in the CNS. It also appears to block voltage-operated calcium channels and acts as an antagonist at opiate receptors (OP2). Notable first-pass metabolism in the liver, primarily by N-dealkylation via the cytochrome P450 isoenzymes CYP3A and CYP1A2 (and possibly CYP2D6). The activity of the two major metabolites has not been determined. Half Life: 29 ± 10 hours (single-dose study of healthy volunteers). LD50: 1100 mg/kg (Oral, Rat) (A308) LD50: 228 mg/kg (Oral, Mouse) (A308) No indication of carcinogenicity to humans (not listed by IARC). Used for the suppression of motor and phonic tics in patients with Tourette's Disorder who have failed to respond satisfactorily to standard treatment. In the event of overdosage, gastric lavage, establishment of a patent airway and, if necessary, mechanically-assisted respiration are advised. Electrocardiographic monitoring should commence immediately and continue until the ECG parameters are within the normal range. Hypotension and circulatory collapse may be counteracted by use of intravenous fluids, plasma, or concentrated albumin, and vasopressor agents such as metaraminol, phenylephrine and norepinephrine. Epinephrine should not be used. In case of severe extrapyramidal reactions, antiparkinson medication should be administered. Because of the long half-life of pimozide, patients who take an overdose should be observed for at least 4 days. (L1712) 2009-07-21T20:28:22Z 2014-12-24T20:25:54Z Pimozide C07566 8212 Pimozide DB01100 true OC1=NC2=CC=CC=C2N1C1CCN(CCCC(C2=CC=C(F)C=C2)C2=CC=C(F)C=C2)CC1 C28H29F2N3O InChI=1S/C28H29F2N3O/c29-22-11-7-20(8-12-22)25(21-9-13-23(30)14-10-21)4-3-17-32-18-15-24(16-19-32)33-27-6-2-1-5-26(27)31-28(33)34/h1-2,5-14,24-25H,3-4,15-19H2,(H,31,34) InChIKey=YVUQSNJEYSNKRX-UHFFFAOYSA-N 461.5462 461.227868975 Exogenous Solid 6.3 HMDB15232 CHEMBL1423 15520