Brogden R N, Carmine A A, Heel R C, Speight T M, Avery G S
Drugs. 1982 Jun;23(6):405-30. doi: 10.2165/00003495-198223060-00001.
Trimethoprim, which has been widely available for several years in combination with sulphamethoxazole as co-trimoxazole, is now available for use alone in the treatment of acute uncomplicated urinary tract infections. Trimethoprim, which is active against a wide range of Gram-positive and Gram-negative aerobic bacteria, is readily absorbed by the oral route and is widely distributed in body fluids and tissues. In therapeutic trials, trimethoprim 200 to 400mg daily has been shown to be comparable in efficacy with co-trimoxazole, ampicillin 2g, cephalexin 2g, oxolinic acid 1.5g and nitrofurantoin 200mg daily in the treatment of acute urinary tract infection. Similarly, in long term prophylaxis of recurrent urinary tract infection, trimethoprim 100mg daily given as a single dose at night was comparable with nitrofurantoin 50 to 100mg, methenamine 1g, oxolinic acid 375mg or co-trimoxazole (80mg trimethoprim/400mg sulphamethoxazole) each given as a single daily dose. Emergence of acquired resistance has been infrequent during years of therapeutic use of co-trimoxazole. Nevertheless, results of serial laboratory surveys suggest that resistance to trimethoprim among enterobacteria is increasing. However, at present, there is no conclusive evidence that there will be a more rapid increase following the introduction of trimethoprim for use alone in the treatment of urinary tract infections. At the dosages used, trimethoprim has generally been well tolerated and in studies comparing it with co-trimoxazole overall, skin rashes and gastrointestinal upset have occurred less frequently with trimethoprim than with co-trimoxazole.
甲氧苄啶与磺胺甲恶唑联合使用作为复方新诺明已广泛应用数年，现在可单独用于治疗急性单纯性尿路感染。甲氧苄啶对多种革兰氏阳性和革兰氏阴性需氧菌有活性，口服后易于吸收，广泛分布于体液和组织中。在治疗试验中，已表明每日服用200至400毫克甲氧苄啶在治疗急性尿路感染方面的疗效与每日服用复方新诺明、2克氨苄西林、2克头孢氨苄、1.5克恶喹酸和200毫克呋喃妥因相当。同样，在复发性尿路感染的长期预防中，每晚单剂量服用100毫克甲氧苄啶与每日单剂量服用50至100毫克呋喃妥因、1克乌洛托品、375毫克恶喹酸或复方新诺明（80毫克甲氧苄啶/400毫克磺胺甲恶唑）相当。在复方新诺明多年的治疗使用中，获得性耐药的出现并不常见。然而，系列实验室调查结果表明，肠杆菌对甲氧苄啶的耐药性正在增加。然而，目前尚无确凿证据表明在单独使用甲氧苄啶治疗尿路感染后耐药性会更快增加。在所使用的剂量下，甲氧苄啶一般耐受性良好，在将其与复方新诺明进行总体比较的研究中，甲氧苄啶引起的皮疹和胃肠道不适比复方新诺明更少。
