Sulfamethazine (Sulfadimethyldiazine) 是磺胺类抗感染试剂,用于畜牧业。
Sulfamethazine (80 mg/kg; intravenous injection; healthy female pigs) treatment significantly reduces α, β and AUC
0->∞
, significantly increases t
1/2
α, Vd and CIB, and upon a single intramuscular administration of 80 mg/kg of Sulfamethazine the absolute bioavailability in pigs is 1.01.
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Animal Model:
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19 healthy female pigs (6-week-old, 4.5-6.2 kg)
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Dosage:
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80 mg/kg
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Administration:
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Intravenous injection (Pharmacokinetic study)
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Result:
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The half-life in distribution phase is 0.23 h and half-lifes in eliminations phase is 9.8 h. α, β and the AUC
0->∞
were significantly decreased and t
1/2
α, Vd and CIB were significantly increased, and the absolute bioavailability in pigs is 1.01.
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化学性质
白色或乳白色结晶性粉末,无臭或几乎无臭,易溶于水,略溶于乙醇。
用途
磺胺类药,用于脑膜炎、肺炎球菌、溶血性链球菌及某些革兰氏阴性杆菌所引起的感染。
用途
一种抗菌磺胺药,诱导CYP3A4表达,以及通过N-乙酰转移酶乙酰化
作用方式
磺胺二甲嘧啶钠属磺胺类药,在结构上类似对氨基苯甲酸(PABA),可与PABA竞争性作用于细菌体内的二叶酸合成酶,从而阻止PABA作为原料合成细菌所需要叶酸的过程,减少了具有代谢活性的四氢叶酸的量,而后者则是细菌合成嘌吟、胸腺嘧啶核苷和脱氧核糖核酸(DNA)的必需物质,因此抑制了细菌的生长繁殖。磺胺药的作用可被PABA及其衍生物(普鲁卡因、丁卡因)所拮抗,此外脓液以及组织的分解产物的存在也起拮抗作用,因其可提供细菌生长的必需物质。