+ Site Statistics
+ Search Articles
+ Subscribe to Site Feeds
EurekaMag Most Shared ContentMost Shared
EurekaMag PDF Full Text ContentPDF Full Text
+ PDF Full Text
Request PDF Full TextRequest PDF Full Text
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter
Follow on LinkedInFollow on LinkedIn

+ Translate

Disposition of 5 amino salicylic acid the active metabolite of sulfasalazine in man

Disposition of 5 amino salicylic acid the active metabolite of sulfasalazine in man

European Journal of Clinical Pharmacology 25(4): 511-516

The disposition of 5-aminosalicylic acid (5-AS), the therapeutically active metabolite of sulfasalazine (SZ), was studied in patients with active inflammatory bowel disease, in patients with biliary tract disease and postoperative T-tube drainage, and in healthy volunteers. Subjects were treated 3 times a day either with 5-AS 0.5 g suppositories and a slow-release preparation or with SZ 1 g tid [3 times a day] (equivalent to 5-AS 1.14 g/day). Plasma and urine concentrations of 5-AS and its acetylated major metabolite (AcAS) were monitored during one dosing interval. In a cross-over trial in 5 patients with ulcerative colitis, no difference was found in the dose-corrected mean (.+-. SD) steady-state plasma levels (.hivin.Css) of 5-AS and AcAS between treatment with 5-AS suppositories (0.10 .+-. 0.07 and 0.50 .+-. 0.20 .mu.g/ml, respectively) and SZ (0.12 .+-. 0.14 and 0.67 .+-. 0.14 .mu.g/ml, respectively). Urinary excretion of total AS (5-AS + AcAS) was similar (192 .+-. 70 and 179 .+-. 79 mg/day) with both forms of treatment. The oral slow-release form of 5-AS produced slightly higher .hivin.Css in 5 patients with Crohn's disease (5-AS 0.21 .+-. 0.22 .mu.g/ml; AcAS 0.83 .+-. 0.40 .mu.g/ml) and in 5 healthy volunteers (5-AS 0.28 .+-. 0.14 .mu.g/ml and AcAS 1.10 .+-. 0.43 .mu.g/ml). Urinary recovery of total AS averaged 20 .+-. 6% (patients ) and 27 .+-. 10% ( volunteers). The cross-over trial in 7 patients with a biliary T-tube revealed that after single doses of 5-AS 1 g and SZ 2 g between 0.01% and 0.75% could be recovered in collected bile (85-500 ml/day) as total As (traces of free 5-AS, and acetylated and glucuronidated 5-AS), indicating some enterohepatic circulation.

(PDF 0-2 workdays service: $29.90)

Accession: 005170715

Download citation: RISBibTeXText

PMID: 6140167

Related references

Soybean lip oxygenase ec inhibition studies with the sulfasalazine metabolites n acetylamino salicylic acid 5 amino salicylic acid and sulfapyridine. European Journal of Clinical Pharmacology 26(4): 449-452, 1984

Effect of sulfasalazine and its active metabolite 5 aminosalicylic acid on toxic oxygen metabolite production by neutrophils. Gut 30(11): 1581-1587, 1989

Poly n acryloyl 4 amino salicylic acid and poly n acyloly 5 amino salicylic acid part 2 anti bacterial properties and uses for the preparation of active insoluble antibiotics. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 3(1): 29-32, 1973

Effect of sulfasalazine and 5 amino salicylic acid on the human colonic prostaglandin system. Gut 23(5): A444, 1982

Steady state pharmaco kinetics of the 5 amino salicylic acid moiety of sulfasalazine. Scandinavian Journal of Gastroenterology Supplement 18(86): 56, 1983

Sulfasalazine and 5 amino salicylic acid inhibit calcium ionophore induced leukotriene formation in rat peritoneal cells. Journal of Allergy & Clinical Immunology 73(1 PART 2): 194, 1984

The effect of di sodium azo bis on water and electrolyte transfer of the rat ileum and colon in vivo compared with sulfasalazine 5 amino salicylic acid and sulfapyridine. Gastroenterology 86(5 PART 2): 1091, 1984

Capacity-limited gut wall metabolism of 5-aminosalicylic acid, a therapeutically active metabolite of sulfasalazine, in rats. Journal of Pharmaceutical Sciences 68(10): 1323-1325, 1979

A double blind clinical trial the compare the effects of 4 amino salicylic acid to 5 amino salicylic acid in topical treatment of ulcerative colitis. Digestion 29(4): 204-208, 1984

Comparative randomized open study of the efficacy and tolerance of enemas with 2 gr of 4-amino-salicylic acid (4-ASA) and 1 gr of 5-amino-salicylic acid (5-ASA) in distal forms of hemorrhagic rectocolitis. Gastroenterologie Clinique et Biologique 19(1): 31-35, 1995