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Results for “AMINOSALICYLIC ACID”

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At least 379 records · Page 21Linked to original sources
PubMed1992

Retrograde distribution of a new 5-aminosalicylic acid enema in patients with ulcerative colitis.

Retrograde colonic distribution of a new 4 g 5-aminosalicylic acid enema (mesalazine) was investigated in seven patients with ulcerative colitis, five of whom were in remission. The enema was labeled with 99m-technetium and imaged by a gamma camera. A median of 86 percent (range 57-90) of the enema had spread beyond the rectum during the first two hours after administration. In four of the five examined patients with left-sided ulcerative colitis, the diseased mucosa was covered within the first 4 hours. In the fifth patient, with involvement of the descending colon, the enema did not spread beyond the very tortuous sigmoid colon 4 or even 8 hours after enema administration.

Adult↗
PubMed1992

Topical 5-aminosalicylic acid: a treatment for aphthous ulcers.

A double-blind placebo controlled trial of 5% 5-aminosalicylic acid (5-ASA) cream for the treatment of oral aphthous ulcers was carried out on 22 subjects. The cream or a placebo (11 patients each) was applied to the ulcers three times daily for up to 14 days. Daily discomfort was reduced by half (P less than 0.01) and less pain (P less than 0.05) was experienced by the treated group. Treatment with 5-ASA shortened healing time (7 vs. 11 days, P less than 0.01) and reduced the difficulty in eating (P less than 0.05). No significant side-effects were reported. We believe 5-ASA cream to be an effective treatment for aphthous ulcers.

Administration, Topical↗
PubMed2005

Free radical scavenging reactions of sulfasalazine, 5-aminosalicylic acid and sulfapyridine: mechanistic aspects and antioxidant activity.

Reactions of sulfasalazine (SAZ) and its metabolites, 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP), with various oxidizing and reducing free radicals (hydroxyl, haloperoxyl, one-electron oxidizing, lipid peroxyl, glutathiyl, superoxide, tryptophanyl, etc.) have been studied to understand the mechanistic aspects of its action against free radicals produced during inflammation. Nanosecond pulse radiolysis technique coupled with transient spectrophotometry has been used for in situ generation of free radicals and to follow their reaction pathways. The transients produced in these reactions have been assigned and radical scavenging rate constants have been measured. In addition to scavenging of various primary and secondary free radicals by SAZ, 5-ASA and SP, 5-ASA has also been observed to efficiently scavenge radicals of biomolecules. 5-ASA has been found to be the active moiety of SAZ involved in the scavenging of oxidizing free radicals whereas reduction of SAZ produced molecular radical anion. The study suggests that free radical scavenging activity of 5-ASA may be a major path of pharmacological action of SAZ against inflammatory bowel diseases (IBD).

Aminosalicylic Acids↗
PubMed1987

Coated oral 5-aminosalicylic acid therapy for mildly to moderately active ulcerative colitis. A randomized study.

We assessed oral 5-aminosalicylic acid (5-ASA) prepared with a pH-sensitive polymer coating in 87 patients with mildly to moderately active ulcerative colitis in a double-blind, placebo-controlled trial. Patients were randomly assigned to receive 5-ASA at a dosage of either 4.8 or 1.6 g per day or placebo for six weeks. The outcome was monitored by flexible proctosigmoidoscopic examinations and physicians' assessments at three-week intervals and by patients' recordings of daily symptoms. Results showed 24 percent complete and 50 percent partial responses in those receiving 4.8 g of 5-ASA per day as compared with 5 percent complete and 13 percent partial responses in those receiving placebo (P less than 0.0001, rank-sum test). At a dosage of 1.6 g per day, the response was twice as good as with placebo, but the difference did not reach statistical significance (P = 0.51). Age, sex, duration of disease, duration of active symptoms, or extent of disease did not affect the clinical outcome. We conclude that oral 5-ASA administered in a dosage of 4.8 g per day is effective therapy, at least in the short term, for mildly to moderately active ulcerative colitis.

Acute Disease↗
PubMed1989

Pharmacokinetics of a 5-aminosalicylic acid enteric-coated tablet and suppository dosage form.

An Eudragit-L coated oral 5-aminosalicylic acid (5-ASA; mesalazine) product (Mesasal), has been formulated to deliver 5-ASA to the distal small intestine and colon for the treatment of inflammatory bowel disease. The purpose of this study was to compare the pharmacokinetic profile of this product to sulphasalazine (SASP; Salazopyrin) and to assess the pharmacokinetics of a suppository 5-ASA dosage form. Twelve healthy volunteers randomly received four single doses of 5-ASA delivering formulations not less than 1 week apart. (a) Mesasal tablets, 2 x 250 mg, fasting; (b) Mesasal tablets, 2 x 250 mg, fed; (c) Salazopyrin tablets, 3 x 500 mg (corresponding to 576 mg 5-ASA), fasting; and (d) Mesasal suppository, 1 x 500 mg, fasting. Plasma 5-ASA and acetyl-5-ASA (Ac-5-ASA) concentrations were followed for 48 h and urine and faecal concentrations for 72 h. Mesasal tablets (fasting) produced a greater area under the concentration-time curve (AUC), peak and time to peak for both plasma 5-ASA and Ac-5-ASA than Salazopyrin. Median urinary recovery values were 21.7% for Salazopyrin and 35.5% for Mesasal (fasting) (P less than 0.01). This means that the systemic absorption was higher after Mesasal than after Salazopyrin. The total faecal recovery values were 38.3 and 26.5%, respectively (NS). Except for a delay of 1.5-.3 h in the time to peak of 5-ASA and Ac-5-ASA plasma levels, the pharmacokinetics of Mesasal tablets were essentially the same in fasting or fed subjects. Suppository administration of 5-ASA resulted in a low median urinary recovery of 10.8%.

Adult↗
PubMed1996

Systemic uptake of 5-aminosalicylic acid from olsalazine and eudragit L coated mesalazine in patients with ulcerative colitis in remission.

UNLABELLED: Aminosalicylates are used to maintain remission in patients with ulcerative colitis. Since there are potential systemic side effects of 5-aminosalicylic acid (5-ASA) and long term treatment is necessary for maintenance therapy preparations with low rates of absorption in the small intestine would be optimal for this indication. In this trial olsalazine (Dipentum), a 5-ASA dimer, and an eudragit L coated mesalazine preparation (Salofalk) were compared. PATIENTS AND METHODS: Fifteen patients with ulcerative colitis in clinical and endoscopical remission were randomized in a cross over design. They either received a 2 x 2 capsules of olsalazine 250 mg or 3 x 2 tablets mesalazine 250 mg, these being the doses recommended for maintenance therapy. After a five days equilibration period morning pre-dose serum samples and 24 hour urine were collected on two consecutive days and analyzed for 5-ASA and acetylated 5-ASA. Subsequently, patients were crossed over to receive the alternative preparation and were evaluated after five days correspondingly. RESULTS: Uptake of 5-ASA from mesalazine was significantly higher than from olsalazine (p < 0.0001). Plasma concentrations of 5-ASA were 3.4 times and of acetyl-5-ASA 3.2 times higher after mesalazine administration than after olsalazine. The same applies to the 24 hour 5-ASA and acetyl-5-ASA urinary excretion (median: 3.2 versus 1.0 mmol/24 hr) as well as to the percentage of administered dose (32.4 versus 17.7%). All patients finished the trial and no major systemic side effects occured with either preparation. CONCLUSION: Systemic uptake of 5-ASA from olsalazine was significantly lower than from eudragit L coated mesalazine. Therefore, olsalazine is less likely to produce side effects and seems to be especially suited for maintenance therapy in ulcerative colitis.

Adult↗
PubMed1999

[Salazosulfapyridine and 5-aminosalicylic acid agents for the treatment of ulcerative colitis].

Sulfasalazine and 5-aminosalicylic acid are very useful therapeutic agents for the treatment of the inflammatory bowel disease, such as ulcerative colitis or Crohn's disease. However, the mechanism of action of the aminosalicylates remains obscure. Recently, many studies about their mechanism have been performed. As a result, aminosalicylates have been identified to have several antiinflammatory pathways: (1) alterations in eicosanoid metabolism of arachidonic acid; particularly inhibition of leukotrien B4 production, (2)free radical scavengers; scavenging reactive oxygen metabolites or nitric oxide (3)immunologic suppression; inhibition of HLA-DR expression on the intestinal epithelial cells, inflammatory cytokine(IL-1 and IL-2) production, adhesion molecule expression, platelet-activating factor release, or histamine release from mast cell, and so on.

Animals↗
PubMed2001

[Two cases of multi-drug-resistant pulmonary tuberculosis with para-aminosalicylic acid (PAS)-induced hypothyroidism].

Two cases of multi-drug-resistant pulmonary tuberculosis with para-aminosalicylic acid (PAS)-induced hypothyroidism were reported. Case 1; a 73-year-old male, complaining of edema, was admitted to our hospital. He had been treated for his multi-drug-resistant pulmonary tuberculosis during the past 1 year with an antituberculous regimen consisting of ethambutol (EB), ethionamide (ETH) and PAS. A thyroid profile performed when he was admitted to our hospital showed several marked abnormalities: serum thyroid stimulating hormone (TSH) was elevated (69.4 microIU/ml: normal, 0.4-4.2 mIU/ml), free thyroxine level (T4) (0.01 ng/dl; normal, 0.70-1.60 ng/dl) and free triiodothyronine level (Ts) (0.60 pg/ml; normal, 2.3-4.1 pg/ml) were low. PAS was discontinued after he was admitted to our hospital, since PAS was believed to be the cause of the hypothyroidism. A thyroid profile that was repeated after the exclusion of PAS from treatment showed the following results: the TSH level was decreased (13.4 mIU/ml), the free T4 (0.93 ng/dl) were normal. During treatment with PAS, he had never received thyroid replacement therapy. Case 2; A 22-year-old female, complaining of hemosputum. She had been treated for her multi-drug-resistant pulmonary tuberculosis during the past 11 months with an antituberculous regimen consisting of EB, ETH and PAS. A thryoid profile performed when she was admitted to our hospital showed several marked abnormalities: elevated serum TSH (112.7 mIU/ml), and low T4 (2.0 micrograms/dl) and T3 (1.1 ng/ml). A thyroid profile that was repeated after the exclusion of PAS from treatment showed the following results: the TSH level was decreased (5.1 mIU/ml). Drug-induced hypothyroidism is an infrequent side effect of therapy with PAS, and only a few cases of PAS-induced hypothyroidism have been reported so far. In this report, we describe patients with hypothyroidism who were receiving therapy for multi-drug-resistant tuberculosis, tuberculosis namely, resistant to at least isoniazid (INH) and rifampicin (RFP), with a regimen that contained PAS.

Adult↗
PubMed1999

Lupus-like syndrome caused by 5-aminosalicylic acid in patients with inflammatory bowel disease.

BACKGROUND: Although 5-aminosalicylic acid (5-ASA) preparations used to treat inflammatory bowel disease are reported to have fewer side effects than sulphasalazine, increased clinical use of these compounds has resulted in increased reports of significant side effects. OBJECTIVE: To report four patients with antinuclear antibody-positive migratory arthralgias and acute inflammation unrelated to the underlying inflammatory bowel disease, fulfilling the criteria of a drug-induced lupus-like syndrome. SETTING: A university-affiliated teaching hospital. INTERVENTION: Cessation of treatment with 5-ASA compounds. RESULTS: The cases described constitute a drug-induced lupus-like syndrome. All patients improved rapidly after discontinuation of 5-ASA compounds. CONCLUSIONS: Reversible lupus-like syndrome appears to be a rare but significant side effect of 5-ASA compounds. Patients treated with 5-ASA compounds who experience acute inflammatory symptoms or clinical deterioration not related to their gastrointestinal disease should be screened to rule out a lupus-like reaction.

Adult↗