生物活性

• 描述Cimetidine is a histamine H2 receptor blocker with Ki and IC50 values of about 0.75 and 0.85 uM, respectively. It inhibits acid release from stomach and is used for gasterointestinal diseases and could inhibit converting hydrogen peroxide (H2O2) in a non-competitive manner. Cimetidine could non-competitively inhibit the liver catalase with high affinity. Binding of cimetidine to the enzyme induced conformational alteration in the enzyme^[3]. Cimetidine, an H2-receptor antagonist, has been shown to enhance a variety of immunologic functions both in vivo and in vitro because of its inhibitory effects on suppressor-cell function. Patients receiving cimetidine have been shown to exhibit enhanced cell-mediated immunity as evaluated by increased response to skin-test antigens, restoration of sensitivity following development of acquired tolerance, and increased responses of lymphocytes to mitogen stimulation^[4]. The clearance (Cl) of CsA (Cyclosporine) was significantly reduced following treatment with cimetidine when compared to the Cl value obtained in the control group (15.46 versus 10.36 ml/min/kg). Cimetidine is an inhibitor of the mixed function oxidase system enzyme system, it inhibits the metabolism of CsA^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00588887	-	-	Terminated	-	United States, Indiana ... more >> Biomet Orthopedics, Inc. Warsaw, Indiana, United States, 46581 Collapse <<
  NCT02175576	Osteoarthritis ... more >> Rheumatoid Arthritis Traumatic Arthritis Lower Limb Deformity Post-traumatic Deformity Complications, Arthroplasty Collapse <<	Not Applicable	Active, not recruiting	October 2026	United States, Illinois ... more >> Midwest Orthopaedics at Rush University Medical Center Chicago, Illinois, United States, 60605 United States, Michigan DeClaire LaMacchia Orthopaedic Institute Rochester Hills, Michigan, United States, 48307 United States, Missouri Missouri Orthopaedic Institute Columbia, Missouri, United States, 65212 United States, Ohio Joint Implant Surgeons, Inc. New Albany, Ohio, United States, 43054 United States, Texas Texas Center for Joint Replacement Plano, Texas, United States, 75093 United States, Utah University of Utah Orthopaedic Center Salt Lake City, Utah, United States, 84108 Collapse <<
  NCT02036931	-	-	Active, not recruiting	April 2025	United States, Arizona ... more >> University Orthopedic Specialists Tucson, Arizona, United States, 85718 France Clermont-Ferrand Hospital Clermont-Ferrand, France Germany University of Würzburg, Orthopedic Würzburg, Germany Ireland Midwestern Regional Orthopaedic Hospital Limerick, Ireland Netherlands Reinier de Groep Delft, Netherlands Spain Hospital El Bierzo Ponferrada, Spain Collapse <<

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• 参考文献

• [1] Sprowl JA, van Doorn L, et al. Conjunctive therapy of cisplatin with the OCT2 inhibitor cimetidine: influence on antitumor efficacy and systemic clearance. Clin Pharmacol Ther. 2013 Nov;94(5):585-92.

  [2] Takahashi HK, Watanabe T, et al. Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol. 2006 Aug;70(2):450-3.

  [3] Jahangirvand M, Minai-Tehrani D, Yazdi F, Minai-Tehrani A, Razmi N. Binding of Cimetidine to Balb/C Mouse Liver Catalase; Kinetics and Conformational Studies. Curr Clin Pharmacol. 2016;11(1):21-7

  [4] Kumar A. Cimetidine: an immunomodulator. DICP. 1990 Mar;24(3):289-95

  [5] D'Souza MJ, Pollock SH, Solomon HM. Cyclosporine-cimetidine interaction. Drug Metab Dispos. 1988 Jan-Feb;16(1):57-9

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