METRONIDAZOLE (FLAGYL) - DEGRADATION BY INTESTINAL FLORA

被引：22

作者：

SEARLE, AJF ^{[1
]}

WILLSON, RL ^{[1
]}

机构：

[1] BRUNEL UNIV, DEPT BIOCHEM, UXBRIDGE UB8 3PH, MIDDLESEX, ENGLAND

来源：

XENOBIOTICA | 1976年 / 6卷 / 08期

关键词：

D O I：

10.3109/00498257609151658

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Metronidazole (Flagyl) is reduced exponentially by the contents of the rat cecum in the absence of O2. The rate of removal is highest at pH 7 and 37.degree. C. Reduction of the drug is inhibited by boiling of the cecal contents, CHCl3, Cu2+, Ag+, azodicarboxylic acid bis-dimethylamide, p-chloromercuric benzoate, N-ethylmaleimide and 4,4,4-trifluoro-1,2-thienyl-1,3-butanedione. Nitrate, ethanol (3%), CO, phenol and amytal did not affect the rate of reduction. Fe-S systems are apparently involved in degradation of the drug.

引用

页码：457 / 464

页数：8

共 34 条

[1] METRONIDAZOLE (FLAGYL) - RADIOSENSITIZER OF HYPOXIC CELLS [J].

ASQUITH, JC ;

FOSTER, JL ;

WILLSON, RL ;

INGS, R ;

MCFADZEAN, JA .

BRITISH JOURNAL OF RADIOLOGY, 1974, 47 (560) :474-481

[2]

BEUDING E, 1946, J PHARMACOL EXP THER, V88, P300

[3] SUSCEPTIBILITY OF ANAEROBIC BACTERIA TO METRONIDAZOLE - RELATIVE RESISTANCE OF NON-SPORE-FORMING GRAM-POSITIVE BACCILLI [J].

CHOW, AW ;

PATTEN, V ;

GUZE, LB .

JOURNAL OF INFECTIOUS DISEASES, 1975, 131 (02) :182-185

[4] HUMAN STUDIES WITH HIGH DOSE METRONIDAZOLE - NON-TOXIC RADIOSENSITIZER OF HYPOXIC CELLS [J].

DEUTSCH, G ;

FOSTER, JL ;

MCFADZEAN, JA ;

PARNELL, M .

BRITISH JOURNAL OF CANCER, 1975, 31 (01) :75-80

[5]

DOUGLAS F, 1974, LAB PRACT, V23, P3

[6] METRONIDAZOLE (FLAGYL), A RADIOSENSITIZER OF POSSIBLE CLINICAL USE IN CANCER CHEMOTHERAPY - SOME BIOCHEMICAL AND PHARMACOLOGICAL CONSIDERATIONS [J].

EAKINS, MN ;

CONROY, PJ ;

SEARLE, AJ ;

SLATER, TF ;

WILLSON, RL .

BIOCHEMICAL PHARMACOLOGY, 1976, 25 (10) :1151-1156

[7] SELECTIVE TOXICITY OF ANTIMICROBIAL NITROHETEROCYCLIC DRUGS [J].

EDWARDS, DI ;

DYE, M ;

CARNE, H .

JOURNAL OF GENERAL MICROBIOLOGY, 1973, 76 (MAY) :135-145

[8] MODE OF ACTION OF METRONIDAZOLE AGAINST TRICHOMONAS-VAGINALIS [J].

EDWARDS, DI ;

MATHISON, GE .

JOURNAL OF GENERAL MICROBIOLOGY, 1970, 63 (NOV) :297-&

[9] RADIOSENSITIZATION OF ANOXIC CELLS BY METRONIDAZOLE [J].

FOSTER, JL ;

WILLSON, RL .

BRITISH JOURNAL OF RADIOLOGY, 1973, 46 (543) :234-235

[10] METRONIDAZOLE (FLAGYL) - CHARACTERIZATION AS A CYTOTOXIC DRUG SPECIFIC FOR HYPOXIC TUMOR-CELLS [J].

FOSTER, JL ;

CONROY, PJ ;

SEARLE, AJ ;

WILLSON, RL .

BRITISH JOURNAL OF CANCER, 1976, 33 (05) :485-490

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