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21.
1.
2 Metabolism and Toxicology
21.
1.
2.
1 Metabolism in the body
AVMs are highly fat-soluble biological antibiotics, which can be widely distributed throughout the body by oral, subcutaneous and intramuscular injection, and body surface administration
.
In the body, the liver and fat are high in content, and the excretion is slow
Radiolabeled IVM metabolism studies have shown that its biotransformation is mainly carried out in the liver and fat
.
The above two tissues have the highest drug concentration content and the longest residence time
DOR has the characteristics of wide distribution and slow tissue elimination in animals
.
Its pharmacokinetic properties are significantly affected by the route of administration, drug formulation, animal species and individual differences
The metabolic characteristics of EPR are similar to other AVMs, but completely different from IVM, its metabolism is mainly carried out in the microsomes of the liver, and N-deacetylation is the main metabolic pathway
.
The milk/blood partition coefficient (KM/p) of EPR is very low.
Due to the high fat solubility of MOX, the drug content in adipose tissue is the highest, followed by the drug secreted into milk by the mammary glands accounting for about 5%
.
21.
1.
2.
2 Toxicology and adverse reactions
Because AVMs block the body’s nerve-muscle signal transmission by increasing GABA to produce anthelmintics, the transmitter of peripheral nerves in mammals is acetylcholine, and GABA is mainly distributed in the central nervous system.
Under normal dosage, due to blood The role of the brain barrier, the number of AVMs entering the central nervous system is very small, and the concentration of AVMs as a GABA agonist is relatively high.
Therefore, AVMs is less toxic to livestock and poultry and has better safety.
Will cause poisoning of livestock and poultry
.
But for young livestock and poultry, because the blood-brain barrier is not yet fully developed, it is more toxic than adult livestock and poultry
Pharmacological tests have shown that there are obvious differences between species and strains in the toxicity of AVMs
.
AVM shows strong toxicity to donkeys and mules, and death can occur when the dose is doubled
It was found through teratogenicity tests that IVM can produce embryo toxicity when given ultra-high doses (close to the maternal toxic dose)
.
The results of Ames test, mammalian cell chromosome aberration analysis and unprogrammed DNA synthesis test show that there is no genetic toxicity
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