Agarwal M B, Rathi S A, Ratho N, Subramanian R
Department of Haematology, Bombay Hospital Institute of Medical Sciences, Marine Lines, Mumbai.
J Assoc Physicians India. 2006 Dec;54:943-8.
Invasive fungal infections are difficult to eradicate especially in immuno-compromised host. Amphotericin B and voriconazole have been the mainstay of treatment but both have significant toxicity. Caspofungin belongs to a new class of antifungal agents, the echinocandins. It acts on the fungal cell wall by selective inhibition of beta-(1,3)-D-glucan syntheses, which is not present in mammalian cells. In vitro data and experimental studies have demonstrated that it has antifungal activity against yeasts of the genus Candida (including those resistant to amphotericin B and azoles), severe species of filamentous fungi, including aspergillosis and certain dimorphic fungi. As an empirical antifungal therapy in neutropenic patients, it has comparable clinical efficacy but superior tolerability compared with liposomal amphotericin B. In patients with invasive candidiasis, it is as effective as amphotericin B deoxycholate. In addition, it showed a significantly superior safety profile. Same has been shown in patients with oropharyngeal/oesophageal candidiasis. In patients with invasive aspergillosis refractory to or intolerant to other antifungal agents, 45% showed a partial or complete response to Caspofungin given as a salvage treatment. Caspofungin is cidal for all Candida species and is static against Aspergillus species. It also possesses activity against Pneumocystis jiroveci. In vitro and in animals, Caspofungin shows additive or synergic antifungal activity with amphotericin B and triazoles. Recently, it's use in paediatric patients, including after bone marrow transplantation, has also been shown to be safe. With compare to other antifungal agents known to be effective in systemic fungal infections, Caspofungin has the best safety profile, tolerability with very low potential for drug interactions. This makes Caspofungin an interesting and extremely valuable new antifungal agent that broadens the available therapeutic armamentarium for the treatment of systemic fungal infections.
侵袭性真菌感染难以根除，尤其是在免疫功能低下的宿主中。两性霉素B和伏立康唑一直是主要的治疗药物，但两者都有显著的毒性。卡泊芬净属于一类新型抗真菌药物，即棘白菌素类。它通过选择性抑制β-(1,3)-D-葡聚糖合成来作用于真菌细胞壁，而这种合成在哺乳动物细胞中不存在。体外数据和实验研究表明，它对念珠菌属酵母（包括对两性霉素B和唑类耐药的酵母）、严重的丝状真菌，包括曲霉菌和某些双相真菌具有抗真菌活性。作为中性粒细胞减少患者的经验性抗真菌治疗，与脂质体两性霉素B相比，它具有相当的临床疗效，但耐受性更好。在侵袭性念珠菌病患者中，它与两性霉素B脱氧胆酸盐一样有效。此外，它还显示出显著更好的安全性。在口咽/食管念珠菌病患者中也有同样的情况。在对其他抗真菌药物难治或不耐受的侵袭性曲霉菌病患者中，45%的患者在接受卡泊芬净挽救治疗后显示出部分或完全缓解。卡泊芬净对所有念珠菌属具有杀菌作用，对曲霉菌属具有抑菌作用。它还对耶氏肺孢子菌具有活性。在体外和动物实验中，卡泊芬净与两性霉素B和三唑类药物显示出相加或协同的抗真菌活性。最近，它在儿科患者中的应用，包括骨髓移植后的应用，也已被证明是安全的。与其他已知对系统性真菌感染有效的抗真菌药物相比，卡泊芬净具有最佳的安全性、耐受性，药物相互作用的可能性非常低。这使得卡泊芬净成为一种有趣且极具价值的新型抗真菌药物，拓宽了治疗系统性真菌感染的可用治疗手段。
