Polyether drug metabolism and toxicology

20.
1.
2 Metabolism and Toxicology

20.
1.
2.
1 Metabolism in the body

Except for SAL, which has a bioavailability of 73%, the bioavailability of other PEs is very low, only 1% to 30%
.
PEs are widely distributed in animals.

PEs is quickly eliminated in the body, and the plasma half-life t1/2β is 0.
2-12h
.
The vast majority of drugs and their metabolites (>90%) are excreted in feces, and a small part (<5%) is excreted in urine

Ionophore anticoccidial drugs (such as MON, MAD, etc.
) can be metabolized extensively in the body, and the structure of some metabolites is even very complex
.
In contrast, the structure of non-ionophore substances (such as chlorphenirin hydrochloride , decoquinate, etc.

20.
1.
2.
2 Toxicology and adverse reactions

PEs is more toxic, has a narrow safety range, excessively large doses, uneven mixing of drugs in feed, application to non-target animals or combined application with other drugs can cause poisoning
.
MON, mouse oral LD SAL, LAS and the MAD ₅₀ were 44mg / kg, 50mg / kg, 146mg / kg and 35 mg of / kg

High-dose PEs mainly produce cytotoxic effects by interfering with the ion balance and energy metabolism of animal cells, causing cell degeneration or necrosis
.
Intravenous injection of a small dose of MON can produce a selective coronary vasodilation effect.

The poisoning caused by PEs in the therapeutic dose is caused by the combined use of certain antibacterial drugs
.
Many studies have reported that MON, SAL, NAR and Tiamulin fumarate premix (TFP) have contraindications.

Related links: physical and chemical properties and uses of polyether drugs