论文部分内容阅读
虽然利福布汀的抗菌谱和抗菌机制与利福平相似,但在药效学和药物动力学特点上却显著优于利福平.利福布汀在药效学方面,它对大多数革兰氏阳性和阴性菌有活性,特别是对结核分枝杆菌和胞内分枝杆菌有活性;对非典型分枝杆菌鸟分枝杆菌一胞内分枝杆菌复合体(MAC)的活性超过利福平;利福平耐药性分枝杆菌对利福布汀无完全交叉耐药性,30%以上菌株对利福布汀仍然敏感.利福布汀与许多抗菌药物包括抗结核药物联用具有累加或协同作用。在治疗结核(包括耐药性分枝杆菌所致)和防治MAC 感染上的卓起效果已彼动物实验和临床观察所证实。利福布汀在药物动力学方面,具有良好的脂溶性,易于透人组织和体液.可迅速透人多型核白细胞,并在其中较长时间保持较高浓度,分布广,半衰期长而具有长效作用.细胞内浓度与细胞外浓度的比值为9~15(利福平为5).利福布汀的血浆蛋白结合率为71%~94%。基于利福布汀的上述特点,可以认为其应用前景看好。
Although the antibacterial spectrum and antibacterial mechanism of rifabutin is similar to rifampicin, its pharmacodynamic and pharmacokinetic properties are significantly better than rifampicin. Rifabutin is pharmacologically active against most Gram-positive and -negative bacteria, especially against Mycobacterium tuberculosis and Mycobacterium intracellulare; against Mycobacterium avium Mycobacterium avium One Mycobacterium complex (MAC) activity than rifampin; rifampicin-resistant Mycobacterium rifabutin no complete cross-resistance, more than 30% of strains are still sensitive to rifabutin . Rifabutin has additive or synergistic effects with many antimicrobials, including anti-TB drugs. The outstanding results in the treatment of tuberculosis (including drug-resistant Mycobacterium) and prevention and treatment of MAC infection have been confirmed in animal experiments and clinical observations. Rifabutin has a good lipid solubility in pharmacokinetics and is readily permeable to tissues and body fluids. It can rapidly penetrate human polymorphonuclear leukocytes and maintain a relatively high concentration for a long time, with a wide distribution, long half-life and long-lasting effect. The ratio of intracellular concentration to extracellular concentration is 9-15 (rifampicin is 5). Rifabutin plasma protein binding rate of 71% to 94%. Based on the above characteristics of rifabutin, it can be considered promising.