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PubMedDate not supplied

Spontaneous formation of immunogenic conjugates by 5-aminosalicylic acid--a biotransformation product of salicylazosulfapyridine.

5-Aminosalicylic acid (5-ASA) reacts readily with proteins at alkaline pH and forms conjugates capable to induce hapten specific antibodies in rabbits. Extensive immunological cross reactions have been found between 5-ASA and para-aminophenol (PAP) immunological systems, but no cross reactions were found between 5-ASA and orto-aminophenol (OAP) immunological systems. Moderate cross reactions were found, occasionally between 5-ASA, 3-hydroxy-sulfanilamide (3-HS) and alpha-methyldopa (alpha MD) immunological systems. Antibodies directed against normal rabbit serum (NRS) proteins, which served as carrier in the 5-ASA conjugates used for immunization, were found in the sera of three out of the six rabbits inoculated with such conjugates. Antibodies directed against heterologous proteins were found in all of these sera, including one serum which lacked hapten specific antibodies and the three sera lacking antibodies directed against NRS proteins. The significance of these findings for the interpretation of the immuno-allergic reactions induced by sulfasalazine is discussed.

Aminosalicylic Acids↗
PubMed2004

Inflammatory bowel diseases, 5-aminosalicylic acid and sulfasalazine treatment and risk of acute pancreatitis: a population-based case-control study.

OBJECTIVES: Patients with inflammatory bowel diseases are suggested to have an increased risk of acute pancreatitis. Although azathioprine and glucocorticoids are risk factors for acute pancreatitis, the relation is poorly understood, in particular the role of 5-aminosalicylic acid and sulfasalazine treatment. To clarify these relations, we conducted a population-based case-control study. METHODS: We identified 1,590 incident cases of acute pancreatitis from the Hospital Discharge Registry of the North Jutland County of Denmark from 1991 to 2002, and selected 10 controls per case (N = 15,913) from the Central Personal Registry, matched by age and gender. Among cases and controls, we identified patients with inflammatory bowel diseases. Data on drug use were extracted from a Pharmaco-epidemiological Prescription Database. RESULTS: Adjusted odds ratios for acute pancreatitis in patients with Crohn's disease and ulcerative colitis were 3.7 (95% confidence interval (CI), 1.9-7.6) and 1.5 (95% CI, 0.7-3.6), respectively. In all patients treated with 5-aminosalicylic acid and sulfasalazine the adjusted odds ratios for acute pancreatitis were 0.7 (95% CI, 0.4-2.2) and 1.5 (95% CI, 0.4-5.2), respectively. Restricted to patients with inflammatory bowel diseases only, the adjusted odds ratios for acute pancreatitis in patients exposed to 5-aminosalicylic acid and sulfasalazine were 0.7 (95% CI, 0.1-3.8) and 0.6 (95% CI, 0.1-6.7), respectively. CONCLUSION: We found a nearly four-fold increased risk of acute pancreatitis in patients with Crohn's disease and a 1.5-fold increased risk for ulcerative colitis. In patients with inflammatory bowel diseases, the use of 5-aminosalicylic acid or sulfasalazine was not associated with increased risk of acute pancreatitis.

Acute Disease↗
PubMed1999

Mesalazine (5-aminosalicylic acid) induced chronic hepatitis.

BACKGROUND: Treatment of ulcerative colitis or Crohn's disease with sulphasalazine causes several adverse effects, including hepatitis. Sulphasalazine is cleaved by colonic bacteria into 5-aminosalicylic acid and sulphapyridine. Received wisdom was that 5-aminosalicylic acid was topically active, whereas sulphapyridine was absorbed and caused immunoallergic side effects. Mesalazine, a slow release formulation of 5-aminosalicylic acid, was expected to be a safe alternative. However, several cases of acute hepatitis have been reported. CASE REPORT: A 65 year old man had increased liver enzymes, anti-nuclear and anti-smooth muscle autoantibodies and IgG levels, and lesions of chronic hepatitis after 21 months of mesalazine treatment. Although liver dysfunction had been identified eight months earlier, simvastatin rather than mesalazine had been withdrawn, without any improvement. In contrast, liver enzyme and IgG levels became normal and autoantibodies disappeared after discontinuation of mesalazine administration. CONCLUSION: Contrary to initial expectations, mesalazine can cause most of the sulphasalazine induced adverse effects, and hepatic side effects may be almost as frequent. When liver dysfunction occurs, mesalazine administration should be discontinued to avoid the development of chronic hepatitis and liver fibrosis.

Aged↗
PubMed1997

Determination of p-aminosalicylic acid and its N-acetylated metabolite in human urine by capillary zone electrophoresis as a measure of in vivo N-acetyltransferase 1 activity.

A capillary zone electrophoresis method has been developed for the determination of p-aminosalicylic acid (PAS) and its metabolite, N-acetyl-p-aminosalicylic acid (N-acetyl-PAS), in urine. A linear relationship was observed between time-normalized peak area and the concentration of the parent and metabolite with correlation coefficients greater than 0.9990. The method could be applied to the determination of PAS and N-acetyl-PAS in human urine without any sample pretreatment. A good separation of the analytes is achieved in a run time of 12 min (15 min total, including capillary wash). Using PAS as a probe for N-acetyltransferase 1 activity, 20 healthy volunteers were phenotyped after oral administration of a 1 g dose. The preliminary results seem to indicate a bimodal distribution of N-acetyl-PAS/PAS molar ratios.

Acetamides↗
PubMed1964

KINETICS OF SERUM AMINOSALICYLIC ACID LEVELS.

A mathematical model, involving three consecutive first order reactions, has been applied to already existing experimental material in order to explain the hourly variation in serum levels obtained after administration of varying repeated doses of different preparations of p-aminosalicylic acid to human volunteers. The model closely agrees with the experimental data for all the orally administered preparations concerned, and the differences in blood levels for different preparations can be explained in terms of the values attributed to the parameters involved in the model. The same model adequately describes the elimination of aminosalicylic acid from the blood after a single intravenous infusion provided that the initial blood level attained does not exceed about 11 mg/100 ml., but fails at higher values. In the latter instance a second order model gives a good fit to the experimental curves. The increase in serum levels found experimentally for the same subjects during the first weeks of prolonged treatment with phenyl-p-aminosalicylate corresponds to a change in the values of the parameters for the elimination from the blood only.

Aminosalicylic Acid↗
PubMed1998

Synthesis and evaluation of 5-aminosalicyl-glycine as a potential colon-specific prodrug of 5-aminosalicylic acid.

As a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA), 5-aminosalicyl-glycine (5-ASA-Gly) was prepared by a simple synthetic route in good yield. Apparent partition coefficients of 5-ASA-Gly were lower than those of 5-ASA, which determined in CHCl3/pH 6.8 buffer or n-octanol/pH 6.8 buffer system. Stability of 5-ASA-Gly by peptidases was investigated by incubation of 5-ASA-Gly with the homogenates of tissue and contents of stomach, proximal small intestine or distal small intestine of rats at 37 degrees C. 5-ASA was not detected, indicating that the prodrug was stable in the upper intestine. The amount of 5-ASA liberated from incubation of the prodrug in cecal or colonic contents of rats was about 65% or 27% in 8 hrs, respectively, which indicated that the prodrug activation took place more readily in the rat cecum whose bacterial counts are high like human colon. Results from in vitro experiments suggested 5-ASA-Gly as a promising candidate of a colon-specific prodrug of 5-ASA.

Aminosalicylic Acids↗
PubMed1977

Elimination of para-aminosalicylic acid in patients with liver disease and renal insufficiency.

The elimination of para-aminosalicylic acid (PAS) after the intravenous injection of 20 mg PAS sodium/kg was estimated in patients with liver disease, in uremic patients and in volunteers without damage of the liver or kidneys. The drug was estimated with a colorimetric and fluorometric method. In the volunteers, the half-lives obtained with the fluorometric method were significantly longer than those estimated with the colorimetric method. This is caused by the estimation of more PAS metabolites by the used fluorometric method. In the patients with renal insufficiency (dialysis patients) the elimination rate of unchanged PAS--estimated with the colorimetric method--was not altered, whereas the elimination of PAS and its metabolites extractable by ethyl acetate was markedly slowed in comparison with the results obtained with the volunteers. The clearance of the unchanged PAS was even increased in the uremic patients. The serum protein binding of PAS was lowered significantly in the serum of uremic patients. In patients with liver cirrhosis, acute virus hepatitis and cholangitis the elimination rate of the drug was not altered in comparison with the volunteers. The results show that the dose of PAS in patients with renal insufficiency may not be reduced. The therapeutic level of the drug cannot otherwise be reached in these patients.

Acute Disease↗
PubMed1988

[Pericardial effusion during the therapy of Crohn's disease with 5-aminosalicylic acid].

A 22-year-old woman with Crohn's disease was treated with 5-aminosalicylic acid (Claversal), four times 500 mg daily, because of increased inflammatory activity. Retrosternal pain set in after two weeks; in another two weeks a moderately enlarged heart was noted on the chest X-ray and pericardial effusion diagnosed echocardiographically. After stopping the medication the pericardial effusion resolved without further treatment. Immunoserology failed to demonstrate autoantibodies, but a repeat lymphocyte stimulation test was positive. There is a possible causal relationship between 5-aminosalicylic acid medication and the pericardial effusion, although the pathogenetic mechanisms is not known.

Adult↗
PubMed1987

Inhibition of neutrophil degranulation and superoxide production by sulfasalazine. Comparison with 5-aminosalicylic acid, sulfapyridine and olsalazine.

Sulfasalazine is a potent inhibitor of superoxide production and granule enzyme release by stimulated neutrophils, and modulation of these responses may contribute to its anti-inflammatory properties. It is a composite drug consisting of 5-aminosalicylic acid and sulfapyridine joined through an azo linkage. To investigate which functional groups on the molecule are active against neutrophil responses, 5-aminosalicylic acid, sulfapyridine and olsalazine were added to cells stimulated with fMet-Leu-Phe or immune complexes. The inhibitory effects of sulfasalazine on superoxide production, degranulation and neutrophil-mediated collagen degradation were closely mimicked by olsalazine, with the other two compounds having little effect on either function. Thus the azo link appears to be the important structural feature of sulfasalazine that affects neutrophil responses. This suggests that sulfasalazine could be anti-inflammatory in its own right rather than just acting as a source of 5-aminosalicylic acid. Our findings are also a favourable indication for olsalazine (Dipentum), which is currently under trial as an anti-inflammatory agent.

Aminosalicylic Acids↗