Meagher Alison K, Ambrose Paul G, Grasela Thaddeus H, Ellis-Grosse Evelyn J
Cognigen Corporation, Buffalo, New York, USA.
Clin Infect Dis. 2005 Sep 1;41 Suppl 5:S333-40. doi: 10.1086/431674.
Tigecycline, a first-in-class expanded-spectrum antimicrobial agent, has demonstrated efficacy in the treatment of complicated intra-abdominal and skin and skin-structure infections. This new antibiotic is available as an intravenous formulation and exhibits linear pharmacokinetics. It is rapidly distributed and has a large volume of distribution, indicating extensive tissue penetration. After a 100-milligram loading dose, followed by 50 milligrams every 12 h, the steady-state maximum concentration in serum after a 1-h infusion is approximately 0.6 microg/mL, the 24-h steady-state area under the concentration-time curve is approximately 5-6 microg.h/mL, and the terminal elimination half-life is approximately 40 h. The major route of elimination of tigecycline is through the feces, primarily as unchanged drug. The pharmacokinetic profile is not affected by severe or end-stage renal disease, nor is it significantly altered by hemodialysis. The pharmacokinetics of tigecycline are also not affected by food, although tolerability is increased if the drug is administered following a meal.
替加环素是首个新型的广谱抗菌药物，已证明其在治疗复杂性腹腔内感染及皮肤和皮肤结构感染方面具有疗效。这种新型抗生素有静脉注射剂型，呈现线性药代动力学特征。它分布迅速，分布容积大，表明其能广泛渗透到组织中。在给予100毫克负荷剂量后，随后每12小时给予50毫克，在1小时输注后的血清稳态最大浓度约为0.6微克/毫升，24小时稳态浓度-时间曲线下面积约为5 - 6微克·小时/毫升，终末消除半衰期约为40小时。替加环素的主要消除途径是通过粪便，主要以原形药物形式排出。其药代动力学特征不受严重或终末期肾病的影响，血液透析也不会使其发生显著改变。替加环素的药代动力学也不受食物影响，不过如果在餐后给药，耐受性会有所提高。
