2606 Promazine Promazine is only found in individuals that have used or taken this drug. It is a phenothiazine with actions similar to chlorpromazine but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic. Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine. 58-40-2 4926 C17H20N2S 284.134720 Oily liquid (T50). < 25°C 203-210°C at 3.00E-01 mm Hg 14.2 mg/L (at 24°C) Inhalation; dermal or skin contact; ingestion (MSDS, A308). Absorption may be erratic and peak plasma concentrations show large interindividual differences. Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine. Hepatic, primarily to N-desmethylpromazine and promazine sulfoxide. Absorption may be erratic and peak plasma concentrations show large interindividual differences. The metabolism occurs through oxidative processes mediated largely by hepatic microsomal and other drug metabolizing enzymes. Antoher step is the conjugaion with glucuronic acid. Other reactions include hydroxylation, demetylation, and sulfoxide formation. Moreover, metabolic alterations in side chain may also occur (A308, A631). LD50: 140 mg/kg (Intraperitoneal, Mouse) No indication of carcinogenicity to humans (not listed by IARC). Used as an adjunct for short term treatment of moderate and severe psychomotor agitation. Also used to treat agitation or restlessness in the elderly. It has predominantly anticholinergic side effects, though extrapyramidal side effects are not uncommon either. Other effects include endocrine effects (such as gynaecomastia and menstrual disturbance), sensitivity to sunlight and haemolytic anaemia (A308, L1149). Side effects include: extrapyramidal symptoms, drowsiness, weight gain, dry mouth, constipation, endocrine effects (such as gynaecomastia and menstrual disturbance), sensitivity to sunlight and haemolytic anaemia. In severe cases, consider supportive therapy. Maintain clear airway and adequate hydration. Anti-Parkinson drugs, as well as benztropine mesylate, and barbiturates can be use to relieve extrapyramidal symptoms (A632). 2009-07-05T03:15:17Z 2026-03-31T19:07:43Z Cytochrome P450 2C19 (CYP2C19) (P33261) (A308). Promazine C07379 8459 CPD-7403 Promazine DB00420 true Cytochrome P450 2C19 (P33261) (A308) CN(C)CCCN1C2=CC=CC=C2SC2=CC=CC=C12 C17H20N2S InChI=1S/C17H20N2S/c1-18(2)12-7-13-19-14-8-3-5-10-16(14)20-17-11-6-4-9-15(17)19/h3-6,8-11H,7,12-13H2,1-2H3 ZGUGWUXLJSTTMA-UHFFFAOYSA-N 284.419 284.13471934 Exogenous Liquid 4.55 HMDB14564 CHEMBL564 4757 <p><a href="http://www.drugsyn.org/Promazine.htm">DrugSyn.org</a></p> CHEM002091 DTXSID2023517 NS00010417 dimethyl[3-(10H-phenothiazin-10-yl)propyl]amine