Kauffman Carol A, Carver Peggy L
Division of Infectious Diseases, Department of Internal Medicine, Veterans Affairs Ann Arbor Healthcare System, University of Michigan Medical School, Ann Arbor, Michigan 48105, USA.
Semin Respir Crit Care Med. 2008 Apr;29(2):211-9. doi: 10.1055/s-2008-1063859.
Echinocandins are semisynthetic lipopeptides that competitively inhibit an essential cell wall component of Candida and aspergillus. They are generally inactive against other fungi. Resistance to these agents is infrequent to date. Echinocandins exhibit low oral bioavailability and are available only as parenteral formulations that are dosed once daily. None of the echinocandins serve as major substrates, inducers, or inhibitors of cytochrome P450 enzymes or the P-glycoprotein transport system; thus they have a low potential for serious drug-drug interactions. In candidemia trials, all echinocandins showed similar rates of success and were as efficacious as fluconazole, amphotericin B, or lipid formulations of amphotericin B. Caspofungin and micafungin have been studied as single-agent therapy in patients with invasive aspergillosis and will likely remain as second-line agents. However, because of their unique mechanism of action, echinocandins are ideally suited for use in combination with polyenes or azoles and are likely to be used increasingly in immunosuppressed hosts despite a current lack of controlled trials demonstrating efficacy. Limited experience suggests that caspofungin and micafungin are safe to use in pediatric patients. Hospital formulary committees are likely to view the three echinocandins as equivalent agents and place the least expensive agent on formulary.
棘白菌素类是半合成脂肽,可竞争性抑制念珠菌和曲霉菌细胞壁的一种重要成分。它们通常对其他真菌无活性。迄今为止,对这些药物产生耐药的情况并不常见。棘白菌素类口服生物利用度低,仅可采用每日给药一次的肠胃外制剂。没有一种棘白菌素类是细胞色素P450酶或P-糖蛋白转运系统的主要底物、诱导剂或抑制剂;因此,它们发生严重药物相互作用的可能性较低。在念珠菌血症试验中,所有棘白菌素类的成功率相似,且与氟康唑、两性霉素B或两性霉素B脂质制剂的疗效相当。卡泊芬净和米卡芬净已作为侵袭性曲霉病患者的单药治疗进行了研究,可能仍作为二线药物。然而,由于其独特的作用机制,棘白菌素类非常适合与多烯类或唑类联合使用,尽管目前缺乏证明其疗效的对照试验,但在免疫抑制宿主中可能会越来越多地使用。有限的经验表明,卡泊芬净和米卡芬净在儿科患者中使用是安全的。医院药事委员会可能会将这三种棘白菌素类视为等效药物,并将最便宜的药物列入药品目录。