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効能
抗生物質 (獣医薬), タンパク質合成阻害薬
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使用
Tiamulin is a semi–synthetic analogue of pleuromutilin in which the hydroxyacetyl side chain is replaced with a larger diethylaminoethylthioacetyl moiety, providing greater hydrophobicity and an ionisable group for salt formation and greater water solubility. Tiamulin is a potent and highly selective antibiotic active against a range of Gram positive bacteria, with no cross resistance to existing antibiotic classes due to its unique mode of action. Like pleuromutilin, it inhibits protein synthesis by binding to domain V of 23S rRNA.
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定義
ChEBI: A carbotricyclic compound that is pleuromutilin in which the hydroxyacetate group is replaced by a 2-{[2-(diethylamino)ethyl]sulfanyl}acetate group. An antibacterial drug, tiamulin is used in veterinary medicine (generally as its hydrogen fumarate salt) fo
the treatment of swine dysentery caused by Serpulina hyodysenteriae.
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安全性プロファイル
Poison by
intramuscular and intravenous routes.
Moderately toxic by ingestion and
subcutaneous routes. When heated to
decomposition it emits toxic fumes of SOx
and NOx. See also MERCAPTANS.
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合成
Tiamulin was synthesized by Sandoz Co. in 1973, starting from pleuromutilin produced by Pleurotus mutilus.
