Metabolism and Toxicology of Nitroimidazole Drugs

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2 Metabolism and Toxicology

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1 Metabolic processes in the body

The main metabolic pathways and metabolites of this class of drugs are the methyl group on the imidazole ring C ₂ that is oxidized to hydroxymethyl.
For example, the metabolites of DMZ and RNZ are the same, both are HMMNI.
Ipranidazole is metabolized to IPZOH and MNZ metabolites.
For MNZOH
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Figure 16-1 Metabolic pathways and main metabolites of representative drugs

Oral MNZ is absorbed rapidly, and its bioavailability is 60%-100%.
It reaches a peak concentration within 1 to 2 hours.
Only a small amount is bound to plasma protein, and the plasma protein binding rate is less than 20%
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TNZ is taken orally and is well absorbed through the gastrointestinal tract, reaching the peak blood level in 2 hours
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16.
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2 Toxicology and adverse reactions

In vivo and in vitro experiments have confirmed that nitroimidazoles have genotoxic, teratogenic and suspected carcinogenic effects
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3 Maximum allowable residue limit

The nitroheterocyclic structure contained in nitroimidazole drugs has cell mutagenicity, which leads to carcinogenic and potential teratogenic effects, which has attracted clinical attention.
The problem of drug residues in edible animal tissues has attracted worldwide attention.
Attention
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