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Toxicological Effects Of Moxifloxacin Hydrochloride

Nov 07, 2023Leave a message

Carcinogenic and mutagenic
Although conventional long-term studies on the carcinogenic effects of moxifloxacin have not been completed, the drug has undergone genotoxicity in vivo and in vitro experiments. In addition, accelerated tests (induction and promotion assays) were conducted on rats for their carcinogenic effects on humans. Four out of five Ames tests were negative, and the mutation test of HPRT in the ovary of Chinese hamsters and the UDS test of primary liver cells in rats were also negative, while Ames tests of other quinolones TA102 were positive. In vitro experiments showed that high-dose (33mg/ml) of other quinolone drugs could cause chromosomal abnormalities in V79 cells of Chinese hamsters. However, in vivo nucleolar assays in mice showed negative results. In addition, in vivo testing showed that its dominant lethality test on mice was negative. In summary, the results of in vivo experiments fully reflect the genetic toxicity in their bodies. No evidence of moxifloxacin carcinogenicity was found in the induction and promotion assays of rats.
Phototoxicity
Moxifloxacin is photostable and has low potential phototoxicity. In vitro and animal experiments have shown that the phototoxicity of moxifloxacin is lower than other quinolone drugs. Oral administration of some quinolone drugs and simultaneous exposure to ultraviolet radiation in mice showed an increased photocarcinogenic effect of ultraviolet radiation.
The study on the photocarcinogenic effect of moxifloxacin has not yet been conducted, and it has been confirmed in the Phase I trial of volunteers that the phototoxicity of moxifloxacin is relatively low.
ElectrocardiogramHigh concentrations of moxifloxacin have an inhibitory effect on delayed regulation of cardiac potassium ion flow, resulting in an extended QT interval. Oral administration of more than 90mg/kg of moxifloxacin to dogs for toxicological studies resulted in a blood concentration greater than 16mg/L, leading to prolonged QT interval, but no arrhythmias were found. However, cumulative intravenous administration of more than 50 times the dosage for individuals (>300mg/kg) can lead to a blood drug concentration of ≥ 200mg/L (30 times higher than the intravenous treatment concentration), and reversible, non-serious ventricular arrhythmias are observed.

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