[en] Metronidazole has been shown to be an active radio-sensitiser of hypoxic cells in vivo and in vitro. In this study 120 persons of different types of cancer were given Metrogyl brand of metronidazole prior to radiation treatment and the results were studied. Metronidazole was found to be effective as a chemical radio-sensitiser since more number of patients in the combined treatment showed effective regression of tumors. (author)

No abstract available

[en] Metronidazole is a commonly used antimicrobial drug. When used excessively, it can cause encephalopathy. We report the MRI findings in one such case. A 43-year-old male patient was treated with metronidazole for 2 months, for an amebic liver abscess and presented with neurological signs and symptoms. MRI of the brain showed findings consistent with metronidazole toxicity

[en] Metronidazole-induced neuro-toxicity, though rare, is known. A characteristic spatial distribution of lesions in cerebellar dentate nuclei and dorsal pons is known. However, temporal progression of lesions on magnetic resonance imaging (MRI) has not been described previously. We describe two such cases which presented initially with splenial hyperintesity and showed progression to characterstic lesions. Both cases improved with stoppage of metronidazole.

No abstract available

[en] Metronidazole (MTNZ) is an antiprotozoa drug, could be labeled with the ^99mTc. MTZL could be used as an ideal vehicle to deliver radioactive decay energy of ^99mTc to the sites of tumor, thus facilitate tumor imaging. The process of labeling was done using tin chloride as reducing agent. The optimum conditions required to label 25 μg MTZL were 100 lg stannous chloride, 30 min reaction time, room temperature at pH 7-9 using 0.5 M phosphate buffer. The radiochemical purity of the labeled compound, at the above conditions, was determined using paper chromatography. The yield was about 93%. About 2.5 x 10⁶ of Ehrlich Ascites Carcinoma (EAC) was injected intrapritoneally (i.p) to produce ascites and intramuscularly (i.m) in the right thigh to produce solid tumor in female mice. Biodistribution studies were carried out by injecting solution of ^99mTc-MTZL in normal and tumor bearing mice. The uptake in ascites was over 5% of the injected dose per gram tissue body weight, at 4 h post injection and above 4% in solid tumor. These data revealed localization of the tracer in the tumor tissues with high percentage sufficient to use ^99mTc MTZL as promising tool for diagnosis of tumor. (author)

[en] Full text: The presence of hypoxic cells in cancerous lesions is believed to be one of the major reasons for the failure of radiotherapy. Metronidazole is a nitroimidazole derivative which has a tendency to accumulate in the hypoxic regions. Imidazoles are reduced intracellularly in all cells, but in the absence of adequate supplies of oxygen, they undergo further reduction to more reactive products that bind to cell components. The reduction pathway can proceed in successive steps past the hydroxylamine derivative to terminate at the relatively inactive amine derivative. This leads to the possibility of envisaging these compounds as radiosensitive, the agents, which enhance the lethal effect of ionizing radiations for hypoxic tissues. Materials and Methods: Metronidazole was reacted with 2-iodoxybenzoic acid followed by the subsequent reaction with diethylenetriamine resulting into synthesis of Schiff base derivative which was characterized on the basis of spectroscopic techniques. Radiocomplexation was performed with ^99mTc for in vivo tumor imaging applications, blood kinetics and biodistribution studies of the radiotracer developed. Result: The newly synthesized Schiff base of metronidazole was fully characterized by spectroscopic techniques, ¹H, ¹³C NMR, mass spectroscopy and IR spectroscopy. The radioconjugate was found to be sufficiently stable in vitro as well as in vivo upto 24 h. Blood clearance of the radiotracer in rabbit was found to be more rapid (t1/2(F)=27±1.4 minutes) and (t1/2(S)=3hr 48±8.4 minutes). The biodistribution in athymic mice showed high tumor uptake (4.93 ± 0.22% ID/g) and low normal organs uptake. Conclusion: Above results showed that ^99mTc labeled compound acts as a specific marker accumulated in hypoxic tumor. Excellent biodistribution characteristics support the concept of its utility as specific radiopharmaceutical for imaging hypoxic tumors

[en] A conjugate of 6-hydrazinopyridine-3-carboxylic acid (HYNIC) with the amino analogue of metronidazole (MN) was synthesized through a multiple-step reaction. HYNIC-MN could be labeled easily and efficiently with ^99mTc using N-(2-hydroxy-1,1-bis(hydroxymethyl)ethyl)glycine (tricine) and ethylenediamine -N,N'-diacetic acid (EDDA) as coligands to form the ^99mTc-HYNIC-MN complex in high yield (>95%). Its partition coefficient indicated that it was a good hydrophilic complex. The tumor cell experiment showed that the ^99mTc-HYNIC-MN complex had a certain hypoxic selectivity. The biodistribution studies of ^99mTc-HYNIC-MN in Kunming mice bearing S180 tumor showed a favorable tissue distribution profile with high tumor uptake, and low or negligible accumulation in non-target organs, suggesting ^99mTc-HYNIC-MN would be a novel potential tumor hypoxia imaging agent. (author)

[en] The '4+1' mixed-ligand complexes consist of Tc(III) coordinated to a tripodal tetradentate chelator NS3 (2,2′,2″- nitrilotriethanethiol) and a monodentate isocyanide ligand. Neutral '4+1' mixed ligand complexes could be prepared under mild labeling conditions and they exhibit high stability against ligand exchange in vivo. In the present work, a isocyanide derivative of metronidazole was synthesized for radiolabelling with "9"9"mTc using '4+1' mixed ligand approach. Preliminary biodistribution studies in Swiss mice bearing fibrosarcoma tumor showed uptake and retention of the radiolabeled complex in tumor. (author)

[en] Various conservative methods for treatment of labial swelling in patients with granulomatous cheilitis have been attempted, often with only moderate success. We report a case of granulomatous cheilitis who showed excellent sustained response to combination of intralesional steroids, metronidazole and minocycline for initial one month followed by prolonged maintenance treatment with minocycline alone. (author)