Tindall William N
Department of Family Medicine, Boonshoft School of Medicine, Wright State University, Dayton, OH 45459, USA.
Am J Health Syst Pharm. 2009 Mar 1;66(5):451-7. doi: 10.2146/ajhp070442.
Adherence issues with the use of available aminosalicylates for the treatment of ulcerative colitis (UC) are discussed.
In the clinical setting, adherence to aminosalicylate therapy has been less than optimal. Topical formulations are associated with poor retention, abdominal bloating, and discomfort during administration. Although oral formulations are more convenient than topical formulations, many require multiple-daily-dosing regimens and have a high pill burden, which make patient adherence poor. A number of oral aminosalicylate formulations use colonic bacteria to release the active drug. Although these oral formulations are effective for the treatment of active UC, therapy is not optimal with regard to clinical outcome. Because of the short half-life, the vast majority of current therapies require multiple daily dosing. In addition, the dose strength of these formulations ranges from 250 to 500 mg, which requires patients to take several tablets at a time. Some patients may also require additional topical aminosalicylate to maintain treatment efficacy. However, many patients dislike topical formulations, and refill rates have been shown to be much lower than with oral formulations. New aminosalicylate formulations are now being designed to improve dosing schedules and increase patient adherence, potentially improving clinical and economic outcomes. High-dose, oral mesalamine formulations have been designed to reduce pill burden.
While aminosalicylates are recommended as first-line treatment for the reduction of symptoms and the prevention of relapse in patients with mild-to-moderate UC, many available formulations require patients to take multiple tablets or capsules two to four times daily, which may affect adherence. New dosage regimens and delivery systems have been developed or are under development to improve convenience of dosing and potentially improve adherence.
讨论现有氨基水杨酸制剂用于治疗溃疡性结肠炎（UC）时的依从性问题。
在临床环境中，氨基水杨酸治疗的依从性一直不太理想。局部用制剂存在保留性差、腹部胀气以及给药时不适等问题。虽然口服制剂比局部用制剂更方便，但许多口服制剂需要每日多次给药方案且药片负担重，这导致患者依从性差。一些口服氨基水杨酸制剂利用结肠细菌来释放活性药物。虽然这些口服制剂对治疗活动性UC有效，但就临床结果而言治疗效果并不理想。由于半衰期短，目前绝大多数疗法都需要每日多次给药。此外，这些制剂的剂量强度在250至500毫克之间，这要求患者一次服用几片。一些患者可能还需要额外的局部用氨基水杨酸来维持治疗效果。然而，许多患者不喜欢局部用制剂，而且续方率已显示远低于口服制剂。现在正在设计新的氨基水杨酸制剂以改善给药方案并提高患者依从性，这可能改善临床和经济结果。高剂量口服美沙拉嗪制剂已被设计用于减轻药片负担。
虽然氨基水杨酸被推荐作为轻至中度UC患者减轻症状和预防复发的一线治疗药物，但许多现有制剂要求患者每天服用多次片剂或胶囊，这可能会影响依从性。已开发或正在开发新的给药方案和给药系统，以提高给药便利性并可能改善依从性。
