2955 Perphenazine An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine. [PubChem] 58-39-9 4748 C21H26ClN3OS 403.148510 White powder. 97°C 278-281°C at 1.00E+00 mm Hg 28.3 mg/L (at 24°C) Absolute bioavailability is 40% following oral administration. Binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone and vomiting centre. Perphenazine also binds the alpha andrenergic receptor. This receptor's action is mediated by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Hepatic. Route of Elimination: Perphenazine is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation. Half Life: 8-12 hours, but ranges up to 20 hours. LD50:318 mg/kg (Oral, Rat) (A308) LD50: 64 mg/kg (Intraperitoneal, Mouse) (A308) No indication of carcinogenicity to humans (not listed by IARC). For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults. Symptoms of overdose include stupor or coma, and children may have convulsive seizures. Signs of arousal may not occur for 48 hours. Treatment is symptomatic and supportive. Induction of emesis is not recommended because of the possibility of a seizure, CNS depression, or dystonic reaction of the head or neck and subsequent aspiration. Gastric lavage (after intubation, if the patient is unconscious) and administration of activated charcoal together with a laxative should be considered. There is no specific antidote. Standard measures (oxygen, intravenous fluids, corticosteroids) should be used to manage circulatory shock or metabolic acidosis. An open airway and adequate fluid intake should be maintained. Body temperature should be regulated. Hypothermia is expected, but severe hyperthermia may occur and must be treated vigorously. An electrocardiogram should be taken and close monitoring of cardiac function instituted if there is any sign of abnormality. Close monitoring of cardiac function is advisable for not less than five days. Vasopressors such as norepinephrine may be used to treat hypotension, but epinephrine should NOT be used. (L1712) 2009-07-21T20:27:49Z 2026-03-27T00:50:37Z Perphenazine C07427 8028 Perphenazine DB00850 true OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(Cl)C=C3)CC1 C21H26ClN3OS InChI=1S/C21H26ClN3OS/c22-17-6-7-21-19(16-17)25(18-4-1-2-5-20(18)27-21)9-3-8-23-10-12-24(13-11-23)14-15-26/h1-2,4-7,16,26H,3,8-15H2 RGCVKNLCSQQDEP-UHFFFAOYSA-N 403.969 403.148510866 Exogenous Solid 4.2 HMDB14988 CHEMBL567 4586 <p><a href="http://www.drugsyn.org/Perphenazine.htm">DrugSyn.org</a></p> CHEM002289 DTXSID1023441 NS00006492 2-{4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl}ethan-1-ol