Pigrau Carlos, Almirante Benito
Servicio de Enfermedades Infecciosas, Hospital Universitario Vall d'Hebron, Barcelona, España.
Enferm Infecc Microbiol Clin. 2009 Apr;27(4):236-46. doi: 10.1016/j.eimc.2009.02.004. Epub 2009 Apr 29.
A review of the chemical structure, pharmacokinetics, spectrum of activity, clinical use, and adverse effects of oxazolidinones (linezolid), glycopeptides, and cyclic lipopeptides (daptomycin) is presented. Oxazolidinones inhibit protein synthesis, and glycopeptides and cyclic lipopeptides act against the bacterial cell wall. The antibacterial spectrum of these agents covers gram-positive pathogens, including multiresistant microorganisms. Absorption of linezolid is approximately 100% and it can be administered orally or intravenously. Linezolid is cleared by both the kidney and liver; thus, dose adjustments are not needed in patients with renal or hepatic failure. Oral absorption of glycopeptides is minimal, and excretion occurs through the kidneys. Daptomycin has fast, potent bactericidal activity, and can only be administered intravenously. The main clinical indication for these antimicrobial agents is the treatment of infections caused by multiresistant gram-positive pathogens, particularly staphylococci. Linezolid can cause anemia, thrombocytopenia, and gastrointestinal side effects, especially in prolonged therapy. The main side effect of vancomycin is nephrotoxicity, and teicoplanin can cause fever. Daptomycin is a safe antibiotic, with myotoxicity being the most relevant side effect.
本文综述了恶唑烷酮类(利奈唑胺)、糖肽类和环脂肽类(达托霉素)的化学结构、药代动力学、活性谱、临床应用及不良反应。恶唑烷酮类抑制蛋白质合成,糖肽类和环脂肽类作用于细菌细胞壁。这些药物的抗菌谱涵盖革兰氏阳性病原体,包括多重耐药微生物。利奈唑胺的吸收率约为100%,可口服或静脉给药。利奈唑胺经肾和肝清除;因此,肾衰竭或肝衰竭患者无需调整剂量。糖肽类口服吸收极少,经肾脏排泄。达托霉素具有快速、强效的杀菌活性,仅可静脉给药。这些抗菌药物的主要临床适应证是治疗由多重耐药革兰氏阳性病原体,尤其是葡萄球菌引起的感染。利奈唑胺可导致贫血、血小板减少和胃肠道副作用,尤其是在长期治疗时。万古霉素的主要副作用是肾毒性,替考拉宁可引起发热。达托霉素是一种安全的抗生素,最相关的副作用是肌毒性。