Pryka R D, Rodvold K A, Rotschafer J C
Department of Pharmacy Practice, College of Pharmacy, University of Illinois, Chicago 60612.
Clin Pharm. 1988 Sep;7(9):647-58.
The chemistry, mechanism of action, antimicrobial spectrum, pharmacokinetics, adverse effects, and clinical uses of teicoplanin are reviewed. Teicoplanin, a novel glycopeptide that is similar to vancomycin, was isolated in the mid-1970s. A fermentation product of Actinoplanes teicomyceticus, teicoplanin is a structurally complex compound made up of six fatty-acid components attached to a common aglycone. Teicoplanin's mechanism of action, like that of vancomycin, is inhibition of cell-wall biosynthesis. In vitro activity is comparable to that of vancomycin and includes staphylococci, streptococci, corynebacterium, listeria, and anaerobic cocci. Resistance to teicoplanin has been reported with coagulase-negative staphylococci. Teicoplanin is 50 to 100 times more lipophilic than vancomycin. Teicoplanin is poorly absorbed after oral administration but is 90% bioavailable when administered intramuscularly. The drug distributes widely into body tissue and is eliminated primarily renally. Optimal dosing regimens and therapeutic serum drug concentrations have not been well established. Reported adverse effects have included irreversible ototoxicity, allergic reactions with maculopapular rash and eosinophilia, pain at intramuscular injection site, and elevation of aminotransferases. Initial clinical trials have yielded conflicting results in gram-positive bacteremia, endocarditis, osteomyelitis, and soft-tissue infections. Teicoplanin has shown promise in surgical and dental prophylaxis. Comparative trials with vancomycin and other antimicrobial agents must be completed before teicoplanin's role as a therapeutic agent in the treatment of systemic gram-positive infections is defined.
本文综述了替考拉宁的化学性质、作用机制、抗菌谱、药代动力学、不良反应及临床应用。替考拉宁是一种新型糖肽类抗生素，与万古霉素相似，于20世纪70年代中期被分离出来。它是游动放线菌的发酵产物，是一种结构复杂的化合物，由六个脂肪酸成分连接到一个共同的苷元上组成。替考拉宁的作用机制与万古霉素类似，都是抑制细胞壁生物合成。其体外活性与万古霉素相当，包括对葡萄球菌、链球菌、棒状杆菌、李斯特菌和厌氧球菌。已有凝固酶阴性葡萄球菌对替考拉宁耐药性的报道。替考拉宁的亲脂性比万古霉素高50至100倍。替考拉宁口服吸收差，但肌肉注射时生物利用度为90%。该药广泛分布于身体组织，主要经肾脏排泄。最佳给药方案和治疗性血清药物浓度尚未完全确定。报道的不良反应包括不可逆的耳毒性、伴有斑丘疹和嗜酸性粒细胞增多的过敏反应、肌肉注射部位疼痛以及转氨酶升高。最初的临床试验在革兰氏阳性菌血症、心内膜炎、骨髓炎和软组织感染方面得出了相互矛盾的结果。替考拉宁在外科和牙科预防方面显示出前景。在确定替考拉宁作为治疗全身性革兰氏阳性感染的治疗药物的作用之前，必须完成与万古霉素和其他抗菌药物的对比试验。
