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At least 19 recordsLinked to original sources
PubMed1995

Orocecal transit time in humans assessed by sulfapyridine appearance in saliva after sulfasalazine intake.

PURPOSE: We propose a noninvasive method for the measurement of orocecal transit time assessed by the sulfapyridine appearance time in saliva after ingestion of sulfasalazine. METHOD: In 12 healthy volunteers, we studied the correlation between plasma and saliva sulfapyridine appearance times and then the sulfapyridine appearance times in saliva under various experimental conditions to assess the reproducibility, the effects of meals, and the role of the formulation, and the effects of gastrointestinal kinetic drugs. RESULTS: The correlation between saliva and plasma sulfapyridine appearance times was strong (r = 0.84; p = 0.0004). The sulfapyridine saliva appearance time was significantly delayed by the meal. Compared with placebo, the saliva sulfapyridine appearance time was reduced by cisapride (312 +/- 128 versus 551 +/- 97 minutes; p = 0.0001) and increased by loperamide (674 +/- 267 versus 501 +/- 131 minutes; p = 0.044). CONCLUSION: We propose the salivary sample method as a validated simplification of the plasma sulfasalazine-sulfapyridine test for the measurement of orocecal transit time.

Adult↗
PubMedDate not supplied

Antifertility effects of sulfapyridine on male hamsters.

Sulfapyridine was administered to mature male golden hamsters either by impregnation in feed pellets, or by subcutaneous injection as a solution in dimethylsulfoxide. The average litter size for control males was 8.3 +/- 3.3 (n = 13) vs. 4.2 +/- 2.7 (n = 11) for sulfapyridine-fed treated animals. Histology of the testis and epididymis was normal and sperm were normal in morphology and motility. Subcutaneous injection of sulfapyridine caused much more dramatic inhibition of male fertility than was achieved by feeding the drug. Sulfapyridine (750 mg/kg body weight in 0.2 ml DMSO) injected subcutaneously for 60 days was effective in reducing testis size and sperm quality. Histology of testes showed spermatogenic arrest at young spermatids. Two classes of animals were found in both sulfapyridine-fed and -injected treatment groups. One class was relatively resistant to the antifertility effects of the drugs. This difference may reflect differing abilities of the animals to convert sulfapyridine to an active form or to excrete its metabolites.

Animals↗
PubMed2000

Inhibitory effect of mast cell-mediated immediate-type allergic reactions by sulfapyridine.

We examined the effect of sulfapyridine on mast cell-mediated immediate-type allergic reactions. Sulfapyridine (1 and 10 microg/kg) significantly inhibited systemic allergic reaction induced by compound 48/80 in rats. Sulfapyridine (1 and 10 microg/kg) also inhibited significantly local mast cell-mediated immediate-type allergic reactions activated by anti-dinitrophenyl (DNP) IgE. Moreover, sulfapyridine inhibited histamine release dose-dependently in the rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE. When sulfapyridine was added, the level of cAMP in RPMC, transiently and significantly increased about 4-fold compared with that of basal cells. These results indicate that sulfapyridine inhibits mast cell-mediated immediate-type allergic reactions in vivo and in vitro.

Animals↗
PubMed1979

Relative systemic availability of sulfapyridine from commercial enteric-coated and uncoated sulfasalazine tablets.

The absorption of sulfapyridine after a single 2.0-Gm oral dose of sulfasalazine, the drug of choice in the treatment of inflammatory bowel disease, as commercial uncoated and enteric-coated and uncoated tablets was evaluated in four healthy male adults. The peak plasma concentration of sulfapyridine after the enteric-coated tablets occurred at 20 hours on the average (compared to 14 hours for the uncoated tablets) and was only 50% of that attained from the uncoated tablets (P less than 0.05). The low relative extent of systemic availability of sulfapyridine from the enteric-coated tablets (65.5 +/- 6.3 per cent, mean +/- S.E.) compared to uncoated tablets may be due to absorption rate-dependent presystemic metabolism, since the relative extent of sulfapyridine absorption was 92.7 +/- 6.2 per cent compared to uncoated tablets. These findings suggest that enteric-coated and uncoated tablets of sulfasalazine are not bioequivalent. It remains to be determined whether the clinical efficacy of sulfasalazine from enteric-coated tablets is affected.

Adult↗
PubMed1986

Inhibition of cytotoxicity by sulfasalazine. II. Sulfasalazine and sulfapyridine inhibit different stages of the NK and NKCF lytic processes.

Sulfasalazine and sulfapyridine but not 5-aminosalicylate inhibit spontaneous cytotoxicity mediated by human natural killer (NK) cells. The aim of this study was to determine which stage(s) of the NK cytotoxic reaction is inhibited by these compounds. Effector/target cell binding studies performed in parallel with cytotoxicity assays using purified large granular lymphocytes indicated that inhibition is a post-binding event. The kinetic profile of inhibition in a calcium pulse assay showed that inhibition continues long after the effector cell triggering stage and that although sulfasalazine may have some inhibitory effect on the calcium-dependent events of the programming phase, sulfapyridine continues to inhibit during the calcium-independent or lethal hit phase of the cytotoxic sequence. The NK soluble cytotoxic factor (NKCF) assay was used as a measure of the lethal hit since the time course of this assay permits study of the various substages of this terminal event in the lytic sequence. Sulfasalazine and sulfapyridine but not 5-aminosalicylate inhibited NKCF-mediated target cell lysis. Different substages of the NKCF-induced lytic reaction were affected by these agents. Sulfasalazine appears to inhibit binding of NKCF to the target cell whereas sulfapyridine predominantly inhibits early post-binding events.

Aminosalicylic Acids↗
PubMed1988

In vitro susceptibility of diarrhoea producing gram negative enteric bacteria to sulfasalazine, 5-aminosalicylic acid, sulfapyridine and four quinolones. Brief report.

The in vitro susceptibility of diarrhoea producing Gram negative enteric bacteria to sulfasalazine, 5-aminosalicylic acid, sulfapyridine and four quinolones was investigated using an agar dilution method. All strains were resistant to 1600 micrograms/ml of sulfasalazine and 5-aminosalicylic acid. MIC range of sulfapyridine for Y. enterocolitica was 3.1-25 micrograms/ml (median:6.2) and for Salmonella 25-100 micrograms/ml (median: 100) Campylobacter jejuni/coli were less susceptible to sulfapyridine with MIC values ranging from 200 to 800 micrograms/ml. Shigella and three of five E. coli strains were resistant to 1600 micrograms/ml of sulfapyridine. Two strains of E. coli were inhibited by 25 micrograms/ml. All strains were fairly susceptible to enoxacin, ciprofloxacin, pefloxacin and ofloxacin. Cirpofloxacin was the most active drug on weight basis.

Aminosalicylic Acids↗
PubMed1975

Effects of normal alcohols on intestinal absorption of salicylic acid, sulfapyridine, and prednisolone in rats.

The rates of intestinal absorption of salicyclic acid, sulfapyridine, and prednisolone from solutions containing no alcohol or 0.5% ethanol, n-butanol, or n-hexanol were determined. At the concentrations used, ethanol did not significantly affect drug absorption. Butanol reduced the rate of absorption of sulfapyridine but did not significantly affect the absorption rates of prednisolone or salicylic acid. Hexanol reduced the rates of absorption of sulfapyridine and salicylic acid and increased the rate of absorption of prednisolone. The absorption-altering effects of the alcohols were concentration dependent and rapidly reversible. Histological studies indicated that the structure of the epithelium was not altered by the alcohols. While the absorption rate of water from the drug solutions was increased by the alcohols, their absorption-altering effects could not be attributed solely to increased water flux. In addition, the absorption-altering effects of the alcohols could not be attributed to formation of drug-alcohol complexes nor to alcohol-induced alterations in the extent of binding of the drugs to nondialyzable materials in the intestinal drug solution.

Alcohols↗
PubMed1986

Sulfapyridine appearance in plasma after salicylazosulfapyridine. Another simple measure of intestinal transit.

The appearance of sulfapyridine in plasma after oral administration of salicylazosulfapyridine (SASP) was evaluated as a method for defining arrival time in the cecum, an index of small bowel transit. After direct instillation of SASP and lactulose into the cecum, the appearances of their metabolites (sulfapyridine in plasma and hydrogen in breath) were rapid (1-10 min) and simultaneous. When a mixture of SASP and lactulose was taken by mouth, times of the respective "signals" varied among individuals from 40 to 180 min (n = 8) but were correlated within individuals. Salicylazosulfapyridine transit times from duodenum to cecum were also very similar to simultaneous measurements of transit by scintigraphic monitoring of technetium 99m. Timing of the sulfapyridine signal corresponded to the arrival of 5%-13% of technetium 99m DTPA in the cecum. Exemplifying the use of this new technique, simultaneous administration of lactulose into the stomach and SASP into the duodenum yielded consistently longer stomach-to-cecum than duodenum-to-cecum transits, attributable to the delay caused by gastric emptying. Therapeutic doses of morphine delayed small bowel transit of SASP. Transit of SASP offers a second marker technique for the cecal arrival of the "head" of a bolus; the approach may be useful as an inexpensive, noninvasive measurement of transit.

Adult↗
PubMed2001

Dapsone and sulfapyridine.

Dapsone and sulfapyridine are structurally related compounds with anti-microbial and anti-inflammatory effects. Dapsone remains the most important drug for leprosy and is useful in the prophylaxis of Pneumocystis pneumonia in patients with HIV disease. The medical treatment of choice for dermatitis herpetiformis is dapsone; and sulfapyridine also can be used for those patients who are intolerant of dapsone. Other neutrophilic disorders also may respond to these drugs. Toxic side effects of both dapsone and sulfapyridine are mediated through the hydroxylamine metabolite. These include hemolysis, methemoglobinemia, and agranulocytosis. Careful monitoring for possible adverse reactions includes frequently performing complete blood counts and regular blood chemistry profile determinations.

Anti-Infective Agents↗
PubMed1975

Acetylation polymorphism of sulfapyridine in patients with ulcerative colitis and Crohn's disease.

Sulfapyridine (SP) is one of the main metabolites of salicylazosulfapyridine (sulfasalazine) that is used extensively in the management of inflammatory bowel disease. One hundred and twenty-two patients with ulcerative colitis or Crohn's disease were studied, including 21 new, untreated patients and 101 previously treated patients. Patients were studied for at least one year during active disease and remission. It was shown that sulfapyridine shares the same acetylation polymorphism as sulfadimidine. The acetylation capability of each patient as determined in serum and urine was constant irrespective of dose (2 to 8 gm/day) and state of disease. A single study of serum can determine acetylator phenotype in patients on sulfasalazine therapy without using any other drug for this purpose and may help ascertain dosage and assess side effects.

Acetylation↗
PubMed1978

High-performance liquid chromatographic assay of sulfapyridine and acetylsulfapyridine in biological fluids.

A high-pressure liquid chromatographic method for the sensitive, rapid, and specific determination of sulfapyridine and its N-acetyl derivative in plasma and saliva was developed. A cyano-bonded, reversed-phase, high efficiency column was used. The system detected these sulfonamides in serum to 0.25 mg/liter and within only 6 min. Sulfapyridine was separated from its acetyl derivative with little interference from other drugs. The assay reproducibility was within 3%. The assay was highly useful for routine monitoring of patients receiving sulfasalazine for inflammatory bowel disease.

Acetylation↗
PubMed1985

Conformational polymorphism VI: the crystal and molecular structures of form II, form III, and form V of 4-amino-N-2-pyridinylbenzenesulfonamide (sulfapyridine).

The crystal structures of three crystalline forms of 4-amino-N-pyridinylbenzenesulfonamide (sulfapyridine) have been determined by X-ray single crystal structure analysis. Form II crystallizes in space group P2(1)/c with four molecules in the unit cell: a = 0.6722(1) nm, b = 2.0593(5) nm, c = 0.8505(1) nm, beta = 101.14(1) degrees; Form III crystallizes in space group C2/c with eight molecules in the unit cell: a = 1.2830(2) nm, b = 1.1714(3) nm, c = 1.5400(3) nm, beta = 94.12(1) degrees; Form V crystallizes in the orthorhombic space group Pbca with 16 molecules in the unit cell: a = 2.4722(10) nm, b = 1.5710(15) nm, c = 1.2147(7) nm. The three structures were solved by direct methods and refined anisotropically to R factors of 0.045, 0.052, and 0.063, respectively. Bond lengths and bond angles agree well among the molecules in these structures; however, the system exhibits conformational polymorphism since the molecular conformation, as measured by torsion angles, differs significantly among the three forms. Sulfapyridine exhibits the imide configuration in all three structures rather than the amide form present in other sulfonamide compounds. Using the structural data, the powder patterns of the three forms have been computer generated to provide standard diffraction patterns for comparison with the variety of polymorphic forms reported in the literature.

Chemical Phenomena↗
PubMed1990

Simultaneous determination of sulfasalazine and its metabolites sulfapyridine and N-acetylsulfapyridine in human serum by ion-pair high-performance liquid chromatography using a polymer-based column.

An HPLC method is described for the simultaneous and rapid determination of sulfasalazine (salicylazosulfapyridine) and two of its metabolites, sulfapyridine and N-acetylsulfapyridine, in human serum. The range of quantitation is 0.1 to 12 micrograms/mL for sulfasalazine and sulfapyridine and 0.25 to 12 micrograms/mL for N-acetylsulfapyridine. Serum is mixed with acetonitrile containing the internal standard sulfamethazine and the ion-pairing agent tetraethylammonium chloride. The acetonitrile extract is concentrated and analyzed by HPLC, using a new polymer-based column, and detected by UV spectroscopy at 270 nm. This paper is the first both to describe the simultaneous analysis of all three of the compounds from serum and to present sulfasalazine concentration-time data following oral administration to humans.

Acetonitriles↗
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↗