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吩噻嗪光毒性:有毒的氯丙嗪光产物。

Phenothiazine phototoxicity: toxic chlorpromazine photoproducts.

作者信息

Ljunggren B

出版信息

J Invest Dermatol. 1977 Oct;69(4):383-6. doi: 10.1111/1523-1747.ep12510313.

DOI:10.1111/1523-1747.ep12510313
PMID:20478
Abstract

The effect of preirradiated chlorpromazine (CPZ) solutions has been studied in vivo in the guinea pig and in vitro in a yeast culture. With intracutaneous administration of CPZ solutions preirradiated with long-wave ultraviolet radiation (UVA), an inflammatory response was attained equaling the response achieved when nonirradiated solutions were injected and the skin of the animals was subsequently irradiated with UVA. Preirradiated CPZ was not toxic to the yeast culture. During irradiation the pH of the CPZ solution changed, indicating an accumulation of acid photoproducts. Nonphototoxic phenothiazines and related tricyclic drugs failed to change their pH following irradiation whereas phototoxic compounds behaved like CPZ. The low pH alone could not account for the inflammatory response in vivo, as neutralized irradiated CPZ solutions still induced inflammation, and acidified, nonirradiated solutions failed to cause a reaction. CPZ phototoxicity seems mainly to be due to the effect of photoproducts. The nature of these is not known, but it is suggested that the stable free radical of CPZ might be an active principle.

摘要

已在豚鼠体内和酵母培养物中对预先照射的氯丙嗪(CPZ)溶液的作用进行了研究。对用长波紫外线(UVA)预先照射的CPZ溶液进行皮内给药时,所产生的炎症反应与注射未照射溶液且随后对动物皮肤进行UVA照射时所产生的反应相当。预先照射的CPZ对酵母培养物无毒。照射期间CPZ溶液的pH发生了变化,表明酸性光产物有所积累。非光毒性吩噻嗪类药物及相关三环类药物在照射后pH未发生变化,而光毒性化合物的表现与CPZ类似。仅低pH值无法解释体内的炎症反应,因为经中和的照射后CPZ溶液仍会引发炎症,而酸化的未照射溶液则不会引起反应。CPZ的光毒性似乎主要归因于光产物的作用。这些光产物的性质尚不清楚,但有人认为CPZ的稳定自由基可能是活性成分。

相似文献

1
Phenothiazine phototoxicity: toxic chlorpromazine photoproducts.吩噻嗪光毒性:有毒的氯丙嗪光产物。
J Invest Dermatol. 1977 Oct;69(4):383-6. doi: 10.1111/1523-1747.ep12510313.
2
Phenothiazine phototoxicity: an experimental study on chlorpromazine and its metabolites.吩噻嗪光毒性:关于氯丙嗪及其代谢产物的实验研究
J Invest Dermatol. 1977 May;68(5):313-7. doi: 10.1111/1523-1747.ep12494582.
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Phenothiazine phototoxicity: an experimental study on chlorpromazine and related tricyclic drugs.吩噻嗪类光毒性:关于氯丙嗪及相关三环类药物的实验研究
Acta Derm Venereol. 1977;57(4):325-9.
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引用本文的文献

1
Experimental studies on the mechanism of benoxaprofen photoreactions.
Arch Dermatol Res. 1983;275(5):318-23. doi: 10.1007/BF00417205.
2
Inhibition of riboflavin metabolism in rat tissues by chlorpromazine, imipramine, and amitriptyline.氯丙嗪、丙咪嗪和阿米替林对大鼠组织中核黄素代谢的抑制作用。
J Clin Invest. 1981 May;67(5):1500-6. doi: 10.1172/jci110180.
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Photochemical inactivation of deoxyribonucleic and ribonucleic acid viruses by chlorpromazine.氯丙嗪对脱氧核糖核酸病毒和核糖核酸病毒的光化学灭活作用。
Antimicrob Agents Chemother. 1979 Mar;15(3):461-4. doi: 10.1128/AAC.15.3.461.