Ahmad Hilal, Kumar Vijay L
Department of Pharmacology, All India Institute of Medical Sciences, Ansari Nagar, New Delhi, India.
J Basic Clin Physiol Pharmacol. 2018 Nov 27;29(6):581-592. doi: 10.1515/jbcpp-2016-0014.
Ulcerative colitis (UC) is a chronic mucosal inflammation of the large intestine restricted to the rectum and colon. Its clinical course follows an intermittent pattern with episodes of relapse, followed by remission and eventually resulting in mucosal damage. Although there is no permanent cure for UC, the currently available pharmacotherapy aims to induce and maintain clinical remission, promote the healing of colonic mucosa and avert any surgical intervention. The conventional drug therapy comprising of 5-aminosalicylates, thiopurines and corticosteroids has advanced recently in terms of formulations and dosing schedule, resulting in improved efficacy, safety and compliance. Calcineurin inhibitors, such as cyclosporin and tacrolimus, have emerged as steroid sparing agents. The treatment paradigm of UC patients who are refractory to conventional drugs has changed in view of the availability of biologics. Currently, there are four biologics approved by the US FDA for the treatment of UC, namely, infliximab, adalimumab, golimumab and vedolizumab, and several others are undergoing clinical trial. In this comprehensive review, the advantages and limitations of the medical therapy of UC are elaborated with an emphasis on the pharmacokinetic and pharmacodynamic aspects of the drugs.
溃疡性结肠炎（UC）是一种局限于直肠和结肠的大肠慢性黏膜炎症。其临床病程呈间歇性模式，有复发期，随后缓解，最终导致黏膜损伤。虽然UC无法根治，但目前可用的药物治疗旨在诱导并维持临床缓解、促进结肠黏膜愈合并避免任何手术干预。由5-氨基水杨酸、硫嘌呤和皮质类固醇组成的传统药物治疗在制剂和给药方案方面最近有了进展，疗效、安全性和依从性均有所提高。钙调神经磷酸酶抑制剂，如环孢素和他克莫司，已成为类固醇节约剂。鉴于生物制剂的可用性，对传统药物难治的UC患者的治疗模式已经改变。目前，有四种生物制剂被美国食品药品监督管理局（US FDA）批准用于治疗UC，即英夫利昔单抗、阿达木单抗、戈利木单抗和维多珠单抗，还有其他几种正在进行临床试验。在这篇全面综述中，阐述了UC药物治疗的优点和局限性，重点是药物的药代动力学和药效学方面。
