Patel S S, Spencer C M
Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand.
Drugs. 1996 Jan;51(1):137-60. doi: 10.2165/00003495-199651010-00009.
Enoxacin is a 6-fluoronaphthyridinone antibacterial agent with good in vitro activity against Neisseria gonorrhoeae and most Gram-negative urinary tract pathogens. It is less active in vitro against Acinetobacter spp., Pseudomonas aeruginosa, and most Gram-positive bacteria, than against Gram-negative organisms. Enoxacin is rapidly absorbed, with a high oral bioavailability (87 to 91%). Of the absorbed dose, 44 to 56% is excreted unchanged in the urine, with peak urinary concentrations (>500 mg/L within 4 hours) remaining high (>100 mg/L) for up to 24 hours, sufficient to inhibit most urinary tract pathogens. Single (400 mg) and multiple oral dose regimens (100 to 600 mg twice or 3 times daily for 5 to 14 days) of enoxacin are as effective for the treatment of patients with complicated or uncomplicated urinary tract infections as other antibacterial agents such as amoxicillin, cefuroxime axetil, cotrimoxazole (trimethoprim-sulfamethoxazole) or trimethoprim. Noncomparative data suggest that enoxacin is also an effective agent for the treatment of prostatitis. Single 400 mgoral doses of enoxacin produce >/- 95% bacteriological cure rates in gonococcal infections, comparable to those produced by single intramuscular doses of ceftriaxone 250 mg. Perioperative doses of oral enoxacin 200 mg provide effective prophylaxis against postoperative bacteriuria after transurethral resection of the prostate. Concomitant administration of enoxacin with a number of commonly used therapeutic agents (e.g. antacids, methylxanthines, warfarin) affects the pharmacokinetic properties of either enoxacin or the coadministered agents. Enoxacin is reasonably well tolerated, with the incidence of adverse experiences ranging from 0 to 24%. Adverse events are mainly gastrointestinal, neurological or dermatological and resolve with minimal intervention. Overall, although enoxacin exhibits a number of clinical characteristics that are similar to those of other agents for the treatment of genitourinary tract infections, the advantages offered by this agent generally do not outweigh those of alternative fluoroquinolone agents. Thus, it is likely to prove to be yet another addition to the list of agents available for the management of these infections.
依诺沙星是一种6-氟萘啶酮类抗菌剂，对淋病奈瑟菌和大多数革兰氏阴性泌尿道病原体具有良好的体外活性。它在体外对不动杆菌属、铜绿假单胞菌和大多数革兰氏阳性菌的活性低于对革兰氏阴性菌的活性。依诺沙星吸收迅速，口服生物利用度高（87%至91%）。在吸收剂量中，44%至56%以原形经尿液排泄，尿药浓度峰值（4小时内>500mg/L）在长达24小时内保持较高水平（>100mg/L），足以抑制大多数泌尿道病原体。依诺沙星的单次（400mg）和多次口服给药方案（100至600mg，每日2次或3次，共5至14天）治疗复杂性或非复杂性泌尿道感染患者的疗效与其他抗菌剂如阿莫西林、头孢呋辛酯、复方新诺明（甲氧苄啶-磺胺甲恶唑）或甲氧苄啶相当。非对照数据表明依诺沙星也是治疗前列腺炎的有效药物。依诺沙星单次口服400mg治疗淋菌性感染的细菌学治愈率>/-95%，与单次肌内注射250mg头孢曲松的治愈率相当。围手术期口服依诺沙星200mg可有效预防经尿道前列腺切除术后的菌尿症。依诺沙星与多种常用治疗药物（如抗酸剂、甲基黄嘌呤、华法林）同时给药会影响依诺沙星或同时给药药物的药代动力学特性。依诺沙星耐受性较好，不良反应发生率为0%至24%。不良事件主要为胃肠道、神经或皮肤方面的，经最小干预即可缓解。总体而言，尽管依诺沙星表现出许多与其他治疗泌尿生殖道感染药物相似的临床特征，但该药物的优势通常并不超过其他氟喹诺酮类药物。因此，它可能会被证明是治疗这些感染的可用药物清单中的又一补充药物。
