Arthur Rebekah R, Drew Richard H, Perfect John R
Campbell University School of Pharmacy, Buies Creek, NC, USA.
Expert Opin Investig Drugs. 2004 Aug;13(8):903-32. doi: 10.1517/13543784.13.8.903.
Administration of antifungals by routes other than that for which the agent was designed or approved have been utilised in attempts to provide directed therapy, reduce adverse effects and improve drug penetration into selected infection sites, such as the central nervous system, lungs and peritoneum. The most widely investigated agent utilising a novel method of drug delivery is amphotericin B. Dose forms for this agent include topicals (aerosol, nasal spray, irrigations, pastes, absorbable sponges, impregnated bone cement and gelatin), oral dosage forms (solutions, suspensions, tablets and so on) and ophthalmic preparations (drops, ointments and injections). Amphotericin B has been administered by routes such as oral, endobronchial, intrathecal, intracisternal, intra-articular, intraperitoneal, ophthalmic and as an antibiotic 'line lock'. Nystatin has been administered as an aerosol, percutaneous paste and bladder washes. Azoles, such as miconazole, fluconazole, ketoconazole and posaconazole, have been administered by novel methods but to a lesser degree. Most of these reports involve miconazole. The dose forms and routes of administration for azoles have included irrigants (bladder, joint), ophthalmic preparations (eye drops, intraocular injections, ointments), impregnated bone cement, endobronchial and intrathecal administration. Finally, both methylene blue (bladder washes) and flucytosine (peritoneal lavage, ophthalmic eye drops) have also been employed. Adequate evaluations of both the safety and efficacy of these therapies are most often hindered by prior or concomitant antifungal therapies, comorbidities and the lack of controlled clinical trials. In addition, the availability of newer treatment options, which demonstrate significant improvement in drug distribution and treatment-related adverse effects make many such novel modes of administration less practical or necessary. In contrast, the inhalation of antifungal aerosols, such as amphotericin B, is rapidly becoming a viable prophylactic option.
为了实现靶向治疗、减少不良反应并提高药物在特定感染部位(如中枢神经系统、肺部和腹膜)的渗透,人们尝试采用药物设计或批准途径以外的方式使用抗真菌药物。两性霉素B是使用新型给药方法研究最为广泛的药物。该药物的剂型包括局部用药(气雾剂、鼻喷雾剂、冲洗剂、糊剂、可吸收海绵、浸渍骨水泥和明胶)、口服剂型(溶液剂、混悬剂、片剂等)和眼科制剂(滴眼液、眼膏和注射剂)。两性霉素B的给药途径包括口服、支气管内、鞘内、脑池内、关节内、腹腔内、眼科给药以及作为抗生素“锁管”用药。制霉菌素已通过气雾剂、经皮糊剂和膀胱冲洗液给药。咪唑类药物,如咪康唑、氟康唑、酮康唑和泊沙康唑,也采用了新型给药方法,但应用程度较低。这些报道大多涉及咪康唑。咪唑类药物的剂型和给药途径包括冲洗剂(膀胱、关节)、眼科制剂(滴眼液、眼内注射、眼膏)、浸渍骨水泥、支气管内给药和鞘内给药。最后,亚甲蓝(膀胱冲洗液)和氟胞嘧啶(腹腔灌洗、眼科滴眼液)也有应用。这些治疗方法的安全性和有效性评估常常受到既往或同时使用的抗真菌治疗、合并症以及缺乏对照临床试验的阻碍。此外,新型治疗选择的出现,在药物分布和治疗相关不良反应方面有显著改善,使得许多此类新型给药方式变得不太实用或不再必要。相比之下,吸入抗真菌气雾剂,如两性霉素B,正迅速成为一种可行的预防选择。
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