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  1. #101

    23.09.2010
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    http://www.drfalkpharma.ru/Sitkin_GSP_1_2011_p2-5.pdf

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  2. #102

    23.09.2010
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  3. #103
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    02.06.2016
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  4. #104
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    20.07.2008
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  5. #105
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    13.01.2015
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  6. #106

    23.09.2010
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    Sulfasalazine

    Sulfasalazine (Pharmacia & Upjohn Company, Kalamazoo, MI, USA), first developed in 1942, has been the parent aminosalicylate in use for over 60 years (Hanauer 2004) and consists of 5-aminosalyclic acid linked by an azo bond to sulfapyridine (Figure 2). It combines an antibacterial agent (sulfapyridine) with an anti-inflammatory component (5-ASA). The sulfonamide moiety acts as a carrier to deliver the active component 5-ASA to the colon where it is released by bacterial action. Sulfasalazine is metabolized by colonic bacterial enzymes to produce the two active byproducts. Sulfapyraidine is metabolized by the liver and excreted in the urine whereas the 5-ASA component is acetylated by the colonic epithelium (Rochester and Abreu 2005). The original indication for 5-ASA was for rheumatoid arthritis, however it was subsequently found to be efficacious in ulcerative colitis. Misiewicz et al (1965) published the first placebo controlled maintenance trial in 1965 randomizing patients to receive sulfasalazine or placebo for one year. Seventy three percent of patients taking placebo relapsed compared to 21% taking the active drug, thus showing sulfasalazine to be highly efficacious for the treatment of ulcerative colitis.

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    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2376091/
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  7. #107

    23.09.2010
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    Table 2
    Different preparations of mesalamine for UC therapy
    A variety of different mechanisms have been proposed by which aminosalicylates work in inflammatory bowel disease. The main mechanism includes the inhibition of cyclooxygenase and lipoxygenase pathways to reduce the production of prostaglandins and leuokotrienes, respectively (Kaiser et al 1999). Mesalamine also reverses the antiproliferative effects of TNF-alpha thus disrupting the effect of cytokines by reducing intestinal cell transcription of inflammatory mediators (Kaiser et al 1999). Other processes described include inhibition of platelet activating factor and production of oxygen radicals and other anti-inflammatory factors (Egan et al 1999; Hanauer 2004). By reducing inflammatory prostaglandin production and the formation of other potent chemotactic substances including leukotriene B4 and certain hydroxy fatty acids (Grisham 1994), mesalamine plays a significant role in halting the perpetuation of a chronic inflammatory state.
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    The combination therapy of oral and enema mesalamine treatment was shown to be superior to oral alone in terms of both remission and improvement. Improvement was obtained in 89% of mesalamine enema group versus 62% of the placebo group at week 4 (p = 0.0008). At week 8, 86% of the mesalamine enema group versus 68% of the placebo group (p = 0.026) showed improvement (Marteau et al 2005) (see Figure 4).
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  8. #108

    23.09.2010
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    5-
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    In the setting of left-sided distal colitis (proctitis), topical (rectal) formulations were found to be superior to oral aminosalicylates at inducing remission (Cohen et al 2000) and the therapeutic effect of mesalamine was strongly correlated with its mucosal concentration (Frieri et al 2005). In patients with high relapse rate (as measured by at least four moderate to severe relapses in the preceding 2 years), the continuous use of topical mesalamine (4 g/day) with high oral dosage (3.2 g4.8 g/day) significantly decreased the total number of recurrences by increasing the mucosal concentration (Cohen et al 2000). A meta-analysis of five controlled trials comparing rectal mesalamine with placebo for distal colitis showed superiority of mesalamine over placebo (Marshall and Irvine 1995). Slow release 1 g mesalamine suppositories used three times per week was compared with placebo in maintaining remission in patients with proctitis and the data reveled that slow release suppositories were also effective for preventing relaspses in ulcerative proctitis (Marteau et al 1998).

    Go to:
    Adverse effects of 5-ASAs
    5-aminosalicylates have been shown to be in safe in short term use (Loftus et al 2003) with a dose-response efficacy without dose-related toxicity. There is sufficient data to demonstrate long-term safety with mesalamine at doses of up to 5 g daily (Cunliffe and Scott 2002). In clinical trials of active ulcerative colitis comparing mesalamine with placebo, the fraction of patients with adverse events ranged from 13% to 73% with mesalamine vs. 22% to 61% with placebo (Loftus et al 2003). The most commonly reported adverse events with the 5-ASA formulations include headache, GI symptoms such as diarrhea, bloating, nausea. Other rare side effects include interstitial nephritis, hepatitis, pericarditis, pancreatitis, pneumonitis, dermatitis, myocarditis, and hematological disturbances (Ransford and Langman 2002) (Table 3). On occasion, drug holidays may be initiated until diarrheal symptoms resolve. Nephrotoxicity can be seen with any of the 5-ASA compounds. Considering that IBD affects younger population, it is reasonable to also evaluate its safety profile in pregnancy. There has been no evidence of teratogenic effect or fetal toxicity with mesalamine (Diav-Citran et al 1998), placing it into a FDA category B for pregnancy.
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  9. #109

    23.09.2010
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  10. #110

    04.02.2012
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