生物活性

• 描述Trimethoprim (TMP), an inhibitor of dihydrofolate reductase, decreases the level of tetrahydrofolate supplying one-carbon units for biosynthesis of nucleotides, proteins, and panthotenate. TMP caused induction of DnaK, DnaJ, GroEL, ClpB, and IbpA/B Hsps^[3]. Trimethoprim exerts antimicrobial activity by blocking the reduction of dihydrofolate to tetrahydrofolate, the active form of folic acid, by susceptible organisms. It has inhibitory activity for most gram-positive aerobic cocci and some gram-negative aerobic bacilli. Trimethoprim constitutes very effective therapy for women with acute symptomatic urinary tract infections caused by E. coli^[4]. The antimicrobial combination of trimethoprim and sulfamethoxazole is active in vitro against a variety of gram-positive and gram-negative bacteria^[5]. 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^[6].
• 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
  NCT03633643	Antimicrobial Prophylaxis in P... more >>rostate Surgery Collapse <<	Phase 4	Not yet recruiting	March 31, 2022	Switzerland ... more >> St. Claraspital, Department of Urology Not yet recruiting Basel, Basel Stadt, Switzerland, 4058 Contact: Peter Ardelt, Dr. med    +41 61 685 85 23       Kantonsspital Aarau, Department of Urology Not yet recruiting Aarau, Switzerland, 5001 Contact: Maciej Kwiatkowski, Dr. med    +41 62 838 47 47       University Hospital Basel, Division of Infectious Diseases and Hospital Epidemiology Not yet recruiting Basel, Switzerland, 4031 Contact: Andreas Widmer, Prof.Dr.med    +41 61 265 38 51    andreas.widmer@usb.ch    Contact: Kathrin Bausch, Dr.med       kathrin.bausch@usb.ch    Kantonsspital Baselland, Department of Urology Not yet recruiting Liestal, Switzerland, 4410 Contact: Svetozar Subotic, Dr. med    +41 61 925 21 72       University Hospital Zurich, Department of Urology Not yet recruiting Zürich, Switzerland, 8091 Contact: Thomas Hermanns, PD Dr. med    +41 44 255 54 40 Collapse <<
  NCT00126698	Urinary Tract Infection ... more >> Bacteriuria Collapse <<	Phase 4	Completed	-	Netherlands ... more >> Sint Antonius Hospital Nieuwegein, Utrecht, Netherlands, 3430 EM Collapse <<
  NCT00892541	Schizophrenia	Phase 1	Completed	-	-

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• 参考文献

• [1] Vouloumanou EK, Karageorgopoulos DE, et al. Trimethoprim/sulfametrole: evaluation of the available clinical and pharmacokinetic/pharmacodynamic evidence. Int J Antimicrob Agents. 2011 Sep;38(3):197-216.

  [2] Cribb AE, Lee BL, et al. Adverse reactions to sulphonamide and sulphonamide-trimethoprim antimicrobials: clinical syndromes and pathogenesis. Adverse Drug React Toxicol Rev. 1996 Mar;15(1):9-50.

  [3] Laskowska E, Kuczyńska-Wiśnik D, Bak M, Lipińska B. Trimethoprim induces heat shock proteins and protein aggregation in E. coli cells. Curr Microbiol. 2003 Oct;47(4):286-9

  [4] Gleckman R, Blagg N, Joubert DW. Trimethoprim: mechanisms of action, antimicrobial activity, bacterial resistance, pharmacokinetics, adverse reactions, and therapeutic indications. Pharmacotherapy. 1981 Jul-Aug;1(1):14-20

  [5] Cockerill FR 3rd, Edson RS. Trimethoprim-sulfamethoxazole. Mayo Clin Proc. 1987 Oct;62(10):921-9

  [6] Brogden RN, Carmine AA, Heel RC, Speight TM, Avery GS. Trimethoprim: a review of its antibacterial activity, pharmacokinetics and therapeutic use in urinary tract infections. Drugs. 1982 Jun;23(6):405-30

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