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Home , Chlorproethazine

Hydrochloride/ 969

2. Stubb S, et al. Fixed eruptions: 77 cases from 1981 to 1985. Chlorpromazine Embonate (BANM, rINNM) mazine. Photosensitivity reactions are more common Br J Dermatol 1989; 120: 583. 3. Roujeau J-C, et al. Medication use and the risk of Stevens-John- Chlorpromazine, Embonate de; Chlorpromazine Pamoate; with chlorpromazine than with other . son syndrome or toxic epidermal necrolysis. N Engl J Med 1995; Chlorpromazini Embonas; Embonato de clorpromazina. Haematological disorders, including haemolytic anae- 333: 1600–7. Хлорпромазина Эмбонат mia, aplastic anaemia, thrombocytopenic purpura, Porphyria. Chlormezanone has been associated with acute at- (C H ClN S) ,C H O = 1026.1. tacks of porphyria and is considered unsafe in porphyric patients. 17 19 2 2 23 16 6 eosinophilia, and a potentially fatal agranulocytosis ATC — N05AA01. have occasionally been reported; they may be manifes- Preparations ATC Vet — QN05AA01. tations of a hypersensitivity reaction. Most cases of Proprietary Preparations (details are given in Part 3) agranulocytosis have occurred within 4 to 10 weeks of Chile: Cardiosedantol; Restoril†. Chlorpromazine Hydrochloride (BANM, rINNM) starting treatment, and symptoms such as sore throat or Multi-ingredient: Chile: Adalgen†; Calmosedan; Diapam; Dioran†; Dol- Aminazine; Chloropromazyny chlorowodorek; Chlorpromazin nix; Dolonase; Dolorelax†; Fibrorelax; Mesolona†; Multisedil; Neo Butar- fever should be watched for and white cell counts insti- trol; Promidan; Sedantol; Sedilit; Silrelax†; Sin-Algin; Hong Kong: Parazone; hydrochlorid; Chlorpromazine, chlorhydrate de; Chlorpromazini S.Afr.: Myoflex. hydrochloridum; Chlorpromazino hidrochloridas; Hidrocloruro tuted should they appear. Mild leucopenia has been de clorpromazina; Klooripromatsiinihydrokloridi; Klorpromazin stated to occur in up to 30% of patients on prolonged Hidroklorür; Klórpromazin-hidroklorid; Klorpromazinhydro- high dosage. Chlorproethazine Hydrochloride (rINNM) klorid. Extrapyramidal dysfunction and resultant disorders in- Chlorproéthazine, Chlorhydrate de; Chlorproethazini Hydro- Хлорпромазина Гидрохлорид clude acute dystonia, a parkinsonism-like syndrome, chloridum; Hidrocloruro de clorproetazina; RP-4909 (chlor- C17H19ClN2S,HCl = 355.3. and akathisia; late effects include tardive dyskinesia proethazine). 3-(2-Chlorophenothiazin-10-yl)-NN-diethylpro- CAS — 69-09-0. and perioral tremor. The neuroleptic malignant syn- ATC — N05AA01. pylamine hydrochloride. drome may also occur. Хлорпроэтазина Гидрохлорид ATC Vet — QN05AA01. In Chin., Eur. (see p.vii), Int., Jpn, US, and Chlorpromazine alters endocrine and metabolic func- C19H23ClN2S,HCl = 383.4. Pharmacopoeias. CAS — 84-01-5 (chlorproethazine); 4611-02-3 (chlo- Viet. tions. Patients have experienced amenorrhoea, galact- rproethazine hydrochloride). Ph. Eur. 6.2 (Chlorpromazine Hydrochloride). A white or al- orrhoea, and gynaecomastia due to hyperprolactinae- ATC — N05AA07. most white crystalline powder. It decomposes on exposure to air mia, weight gain, and hyperglycaemia and altered ATC Vet — QN05AA07. and light. Very soluble in water; freely soluble in . A freshly prepared 10% solution in water has a pH of 3.5 to 4.5. glucose tolerance. Body temperature regulation is im- Store in airtight containers. Protect from light. paired and may result in hypo- or hyperthermia de- S USP 31 (Chlorpromazine Hydrochloride). A white or slightly pending on environment. There have also been reports creamy-white odourless crystalline powder. It darkens on pro- of hypercholesterolaemia. longed exposure to light. Soluble 1 in 1 of water, 1 in 1.5 of alco- There have been isolated reports of sudden death with N Cl hol, and 1 in 1.5 of chloroform; insoluble in ether and in benzene. Store in airtight containers. Protect from light. chlorpromazine; possible causes include cardiac ar- rhythmias or aspiration and asphyxia due to suppres- CH Dilution. Solutions containing 2.5% of chlorpromazine hydro- 3 chloride may be diluted to 100 mL with 0.9% sodium chloride sion of the cough and gag reflexes. solution provided the pH of the saline solution is such that the pH Pain and irritation at the injection site may occur on N of the dilution does not exceed the critical range of pH 6.7 to 6.8.1 injection. Nodule formation may occur after intramus- With saline of pH 7.0 or 7.2, the final solution had a pH of 6.4. cular injection. CH 1. D’Arcy PF, Thompson KM. Stability of chlorpromazine hydro- 3 chloride added to intravenous infusion fluids. Pharm J 1973; do not cause dependence of the type 210: 28. (chlorproethazine) encountered with barbiturates or benzodiazepines. Incompatibility. Incompatibility has been reported between However, withdrawal symptoms have been seen on chlorpromazine hydrochloride injection and several other com- abrupt withdrawal in patients receiving prolonged Profile pounds; precipitation of chlorpromazine base from solution is Chlorproethazine is a derivative differing chemi- particularly likely if the final pH is increased. Compounds re- and/or high-dose maintenance therapy. cally from chlorpromazine by the substitution of a diethyl for a ported to be incompatible with chlorpromazine hydrochloride in- Although the adverse effects of other phenothiazines dimethyl group. It has general properties similar to those of chlor- clude aminophylline, amphotericin B, aztreonam, some barbitu- are broadly similar in nature to those of chlorpro- (below) but has been used mainly as a muscle relax- rates, chloramphenicol sodium succinate, chlorothiazide ant in the management of muscle spasm (p.1887). Although ex- sodium, dimenhydrinate, heparin sodium, sulfate mazine, their frequency and pattern tend to fall into 3 posure of the skin to phenothiazines has been associated with (when preserved with chlorocresol), some penicillins, and groups: sensitivity reactions, chlorproethazine hydrochloride has been . • group 1 (e.g. chlorpromazine, , applied topically with the warning to avoid direct exposure to sunlight. It has also been given orally or by intramuscular or slow For a warning about incompatibility between chlorpromazine so- and promazine) are generally characterised by pro- intravenous injection. lution (Thorazine; GSK, USA) and suspension nounced sedative effects and moderate antimus- (Tegretol; Novartis, USA), see p.471. Preparations carinic and extrapyramidal effects Sorption. There was a 41% loss of chlorpromazine hydrochlo- Proprietary Preparations (details are given in Part 3) ride from solution when infused for 7 hours via a plastic infusion • group 2 (e.g. pericyazine, , and thiorid- Fr.: Neuriplege†. set (cellulose propionate burette with PVC tubing), and a 79% azine) are generally characterised by moderate seda- loss after infusion for 1 hour from a glass syringe through silastic tive effects, marked antimuscarinic effects, and few- tubing.1 Loss was negligible after infusion for 1 hour from a sys- er extrapyramidal effects than groups 1 or 3 tem comprising a glass syringe with polyethylene tubing. Chlorpromazine (BAN, rINN) • group 3 (e.g. , , prochlor- 1. Kowaluk EA, et al. Interactions between and intravenous Chlorpromazinum; Clorpromazina; Klooripromatsiini; Klorpro- delivery systems. Am J Hosp Pharm 1982; 39: 460–7. , and ) are generally charac- mazin. 3-(2-Chlorophenothiazin-10-yl)propyldimethylamine. terised by fewer sedative and antimuscarinic effects Хлорпромазин Adverse Effects but more pronounced extrapyramidal effects than C17H19ClN2S = 318.9. Chlorpromazine generally produces less central de- groups 1 or 2 CAS — 50-53-3. pression than the barbiturates or benzodiazepines, and Classical antipsychotics of other chemical groups ATC — N05AA01. tolerance to its initial sedative effects develops fairly tend to resemble the phenothiazines of group 3. They ATC Vet — QN05AA01. quickly in most patients. It has antimuscarinic proper- include the butyrophenones (e.g. and ha- ties and may cause adverse effects such as dry mouth, loperidol); diphenylbutylpiperidines (e.g. ); constipation, difficulty with micturition, blurred vi- CH3 ( and ); substi- sion, and mydriasis. Tachycardia, ECG changes (par- tuted benzamides (e.g. ); oxypertine; and N ticularly Q- and T-wave abnormalities), and, rarely, . CH3 cardiac arrhythmias may occur; hypotension (usually Carcinogenicity. See Effects on Endocrine Function, below. N Cl orthostatic) is common. Other adverse effects include delirium, agitation and, rarely, catatonic-like states, in- Convulsions. Treatment with antipsychotics can result in EEG abnormalities and lowered seizure threshold.1 Seizures can be in- somnia or drowsiness, nightmares, depression, miosis, duced particularly in patients with a history of epilepsy or drug- S EEG changes and convulsions, nasal congestion, mi- induced seizures, abnormal EEG, previous electroconvulsive nor abnormalities in liver function tests, inhibition of therapy, or pre-existing CNS abnormalities. The risk appears to Pharmacopoeias. In Br. and US. ejaculation, impotence, and priapism. be greatest at the start of therapy, or with high dos- BP 2008 (Chlorpromazine). A white or creamy-white powder or es, or abrupt increases of dose, or with the use of more than one waxy solid; odourless or almost odourless. M.p. 56° to 58°. Prac- Hypersensitivity reactions include urticaria, exfoliative antipsychotic. The incidence of antipsychotic-induced convul- tically insoluble in water; freely soluble in alcohol and in ether; dermatitis, erythema multiforme, and contact sensitiv- sions is, however, probably less than 1%. very soluble in chloroform. Protect from light. ity. A syndrome resembling SLE has been reported. In general, the epileptic potential has been correlated with the USP 31 (Chlorpromazine). A white crystalline solid with an Jaundice has occurred, and probably has an immuno- propensity of the antipsychotic to cause sedation. Phenothiazines amine-like odour. It darkens on prolonged exposure to light. logical origin. Prolonged therapy may lead to deposi- with marked sedative effects [group 1] such as chlorpromazine Practically insoluble in water; soluble 1 in 3 of alcohol, 1 in 2 of appear to present a higher risk than those with strong extrapy- chloroform, 1 in 3 of ether, and 1 in 2 of benzene; freely soluble tion of pigment in the skin, or more frequently the eyes; ramidal effects [group 3]. appears to carry a relative- in dilute mineral acids; practically insoluble in dilute alkali hy- corneal and lens opacities have occurred. Pigmentary ly low risk of seizures. The following drugs have been suggested droxides. Store in airtight containers. Protect from light. retinopathy has occurred only rarely with chlorpro- when classical antipsychotic therapy is considered necessary in The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii)