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Reproductive Toxicology (Elmsford, N.Y.) 1995
Review
Topics: Animals; Fertility; Humans; Male; Sulfasalazine
PubMed: 7579905
DOI: 10.1016/0890-6238(95)00002-r -
Zeitschrift Fur Rheumatologie Apr 2002
Review
Topics: Antirheumatic Agents; Clinical Trials as Topic; Humans; Meta-Analysis as Topic; Spondylitis, Ankylosing; Sulfasalazine; Treatment Outcome
PubMed: 12056292
DOI: 10.1007/s003930200023 -
Scandinavian Journal of... 1988Sulphasalazine was first produced nearly 50 years ago through the inspiration of a Swedish doctor, Dr Nanna Svartz. Later, in controlled trials, this compound was shown... (Clinical Trial)
Clinical Trial Review
Sulphasalazine was first produced nearly 50 years ago through the inspiration of a Swedish doctor, Dr Nanna Svartz. Later, in controlled trials, this compound was shown to reduce substantially the frequency of recurrent attacks of ulcerative colitis when used as long-term maintenance therapy. Studies into the metabolism of sulphasalazine have shown that, when taken orally, most of the ingested dose reaches the colon intact, and within the colonic lumen, bacteria split sulphasalazine into two breakdown products, sulphapyridine and 5-ASA. 5-ASA was shown to be the active therapeutic moiety while sulphapyridine served simply as a carrier. Olsalazine was developed to retain the property of sulphasalazine of reaching the colon intact, but also to liberate two molecules of 5-ASA with no residual carrier.
Topics: Aminosalicylic Acids; Clinical Trials as Topic; Colitis, Ulcerative; History, 20th Century; Humans; Sulfasalazine; Sweden
PubMed: 2906475
DOI: 10.3109/00365528809101538 -
British Journal of Rheumatology Nov 1995Sulphasalazine a drug used for the treatment of rheumatoid arthritis (RA) shows a wide range of biological activities all of which might contribute to the beneficial... (Review)
Review
Sulphasalazine a drug used for the treatment of rheumatoid arthritis (RA) shows a wide range of biological activities all of which might contribute to the beneficial clinical effect seen during treatment of RA. This review summarizes some of the biological activities and discusses these in context of possible modes of action of the drug. Sulphasalazine has been described as an antibacterial drug, an anti-inflammatory drug or as an immunomodulator. From the reviewed data it is concluded that the effects of sulphasalazine on various immunological processes, are of outstanding importance for its mode of action.
Topics: Anti-Inflammatory Agents; Antirheumatic Agents; Arthritis, Rheumatoid; Humans; Sulfasalazine
PubMed: 8535652
DOI: No ID Found -
Alimentary Pharmacology & Therapeutics Feb 1996The choice of medical therapies for Crohn's disease continues to grow. Although our understanding of the mechanisms of the disease is incomplete, increasing knowledge of... (Review)
Review
The choice of medical therapies for Crohn's disease continues to grow. Although our understanding of the mechanisms of the disease is incomplete, increasing knowledge of the pathogenesis of inflammation in general and Crohn's disease in particular allows targeting of therapies at various points in the immunoinflammatory cascade. In addition, the division of Crohn's disease into subtypes by location, aggressiveness, and the presence or absence of perianal and fistulizing disease allows the tailoring of medical therapy to the individual patient. For those patients with moderate to severe symptoms or frequent flares of disease activity, and those who have required surgical resection, maintenance therapy can substantially reduce the rate of recurrence. Despite these advances, available medical therapies for Crohn's disease remain imperfect, as evidenced by their sometimes substantial toxicities and the continued frequent need for surgery.
Topics: Anti-Infective Agents; Anti-Inflammatory Agents; Clinical Trials as Topic; Crohn Disease; Enteral Nutrition; Humans; Parenteral Nutrition, Total; Steroids; Sulfasalazine
PubMed: 8871440
DOI: 10.1111/j.1365-2036.1996.tb00173.x -
Lancet (London, England) Jun 1987
Topics: Aminosalicylic Acids; Colitis, Ulcerative; Humans; Male; Mesalamine; Sulfasalazine
PubMed: 2884417
DOI: No ID Found -
The American Journal of Gastroenterology May 1988
Topics: Animals; Arthritis, Rheumatoid; Colitis, Ulcerative; Crohn Disease; History, 20th Century; Humans; Sulfasalazine
PubMed: 2896458
DOI: No ID Found -
International Journal of Andrology Feb 1986Salicylazosulfapyridine (SASP), a drug used in the treatment of inflammatory bowel diseases, has been reported to depress the fertility in males. Therefore, some authors... (Review)
Review
Salicylazosulfapyridine (SASP), a drug used in the treatment of inflammatory bowel diseases, has been reported to depress the fertility in males. Therefore, some authors have proposed SASP as a new lead in the search for a contraceptive for men. Based on a review of the literature, our conclusion is that SASP taken in tolerable doses has not sufficient antifertility effect. Additionally, the drug has too serious and too many side effects to be accepted as a contraceptive. However, the effect on male fertility of other sulfa drugs and related compounds remains to be investigated.
Topics: Acrosome; Animals; Bulbourethral Glands; Chemical Phenomena; Chemistry; Contraceptive Agents, Male; Contraceptives, Oral; Disease Models, Animal; Drug Interactions; Fertility; Folic Acid; Hormones; Humans; Male; Sulfasalazine; Testis
PubMed: 2875031
DOI: 10.1111/j.1365-2605.1986.tb00866.x -
Drugs 1986Sulphasalazine, devised by Dr Nana Svartz for the treatment of 'infective polyarthritis', has been used in the treatment of inflammatory bowel disease for more than 40... (Clinical Trial)
Clinical Trial Review
Sulphasalazine, devised by Dr Nana Svartz for the treatment of 'infective polyarthritis', has been used in the treatment of inflammatory bowel disease for more than 40 years. Many controlled trials have shown that sulphasalazine 4g daily will induce remissions in between one-half and three-quarters of patients with acute attacks of ulcerative colitis. When given in a dosage of 2g daily it will prevent relapses in quiescent colitis. Relapses are 5 times more likely in untreated patients. It is less effective in Crohn's disease, where it exerts only a transient benefit in patients with active colonic disease and fails to prevent relapse or recurrence. Sulphasalazine is absorbed from the small intestine, re-excreted in bile and carried to the colon, where its azo bond is split by bacteria to release sulphapyridine, which is absorbed and is responsible for most of the drug's side effects, and 5-aminosalicylic acid, which is the active therapeutic moiety of the drug and exerts a beneficial topical action on the colonic mucosa. Side effects are common but are mainly reversible and not serious. Those related to high concentrations of sulphapyridine and to poor acetylation of the drug include gastrointestinal intolerance, malaise, headache, arthralgia, drug fever, effects on red blood cells and reversible male infertility. More serious, idiosyncratic side effects are skin rashes, leucopenia and agranulocytosis. Rarely, neurotoxicity, hepatotoxicity, polyarteritis, pulmonary fibrosis, a lupus-like syndrome and haemorrhagic colitis are produced. It is possible to desensitise most patients with drug-induced skin rashes. A number of less toxic alternatives to sulphasalazine have been devised and are undergoing trial. They either convey 5-aminosalicylic acid in a coated tablet to the colon or, when conjugated to a non-toxic carrier, release 5-aminosalicylic acid by bacterial cleavage there. Sulphasalazine remains a most useful drug in the treatment of inflammatory bowel disease after 40 years of use.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Clinical Trials as Topic; Colitis, Ulcerative; Crohn Disease; Drug Interactions; Humans; Proctocolitis; Sulfasalazine
PubMed: 2877847
DOI: 10.2165/00003495-198600321-00003 -
ChemMedChem Sep 2021The xCT antiporter is a cell membrane protein involved in active counter-transportation of glutamate (outflux) with cystine (influx) over the human cell membrane. This...
The xCT antiporter is a cell membrane protein involved in active counter-transportation of glutamate (outflux) with cystine (influx) over the human cell membrane. This feature makes the xCT antiporter a crucial element of the biosynthesis of the vital free radical scavenger glutathione. The prodrug sulfasalazine, a medication for the treatment of ulcerative colitis, was previously proven to inhibit the xCT antiporter. Starting from sulfasalazine, a molecular scaffold jumping followed by SAR-assisted design and synthesis provided a series of styryl hydroxy-benzoic acid analogues that were biologically tested in vitro for their ability to decrease intracellular glutathione levels using four different cancer cell lines: A172 (glioma), A375 (melanoma), U87 (glioma) and MCF7 (breast carcinoma). Depletion of glutathione levels varied among the compounds as well as among the cell lines. Flow cytometry using propidium iodide and the annexin V marker demonstrated minimal toxicity in normal human astrocytes for a promising candidate molecule (E)-5-(2-([1,1'-biphenyl]-4-yl)vinyl)-2-hydroxybenzoic acid.
Topics: Amino Acid Transport System y+; Drug Design; Humans; Molecular Structure; Prodrugs; Structure-Activity Relationship; Sulfasalazine
PubMed: 33847044
DOI: 10.1002/cmdc.202100204