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5-aminosalicylic acid

Jinke Xu, Mifong Tam, Sepideh Samadei, Sophie Lerouge, Jake Barralet, Mary M Stevenson, Marta Cerruti
Mucoadhesive drug delivery systems stick to mucosal tissues and prolong the local retention time of drugs. Since the colon is covered by a mucosal layer, mucoadhesive rectal formulations may improve treatment of such diseases as hypertension or colon cancer. Ulcerative colitis (UC) is an inflammatory bowel disease characterized by chronic inflammation of the colonic mucosa. It is commonly treated with sulfasalazine (SSZ), which is metabolized by the intestinal flora into the therapeutic 5-aminosalicylic acid (5-ASA) and a toxic by-product sulfapyridine (SP)...
October 18, 2016: Acta Biomaterialia
Tim Smeets, Florence van Hunsel
A 38-year-old male and a 36-year-old female experienced red-brown urine discolouration after 2 and 3 days, respectively, during the use of mesalamine for inflammatory bowel disease. Both patients mentioned that the urine discoloured after contact with sodium hypochlorite detergent in toilet water. Mesalamine and the inactive metabolite N-acetyl-5-aminosalicylic acid are primarily excreted in the urine. We hypothesised a possible reaction with sodium hypochlorite and/or light. Naranjo assessment scores of 9 and 6 were obtained for the reports, indicating a certain and probable relationship, respectively, between the red-brown urine discolouration and the use of the suspect drug mesalamine...
December 2016: Drug Saf Case Rep
Avnish Kumar Seth, Pawan Rawal, Ruchika Bagga, Priti Jain
Forty-four-year-old male with ulcerative colitis (UC) for 11 years reported frequent relapse despite daily sulfasalazine 4 g, azathioprine 125 mg, and rectal 5-aminosalicylic acid. Repeated use of corticosteroids led to cataract. At enrollment, he was passing eight stools a day with blood with a Mayo score of 9 (3+1+3+2). Stool was negative for ova/cysts/acid fast bacilli and Clostridium difficile toxin assay. Rectal biopsy showed cryptitis, crypt abscess, and crypt distortion with no inclusion bodies, and cytomegalovirus DNA was negative...
September 2016: Indian Journal of Gastroenterology: Official Journal of the Indian Society of Gastroenterology
Makoto Naganuma, Shinta Mizuno, Kosaku Nanki, Shinya Sugimoto, Takanori Kanai
Recently, several medical treatments for ulcerative colitis (UC) have been developed, including 5-aminosalicylic acids (5-ASAs), corticosteroids, thiopurine, calcineurin inhibitors, and anti-tumor necrosis factor (TNF) α treatments. Treatment options including calcineurin inhibitors and anti-TNF treatment for refractory UC are discussed in this article. Furthermore, upcoming treatments are introduced, such as golimumab, vedolizumab, AJM300, tofacitinib. Budesonide foamwill be used as one treatment option in patients with distal colitis...
October 3, 2016: Clinical Journal of Gastroenterology
Anthony K Akobeng, Dongni Zhang, Morris Gordon, John K MacDonald
BACKGROUND: The prevention of relapse is a major issue in the management of Crohn's disease. Corticosteroids, the mainstay of treatment of acute exacerbations, are not effective for maintenance of remission and its chronic use is limited by numerous adverse events. Randomised controlled trials assessing the efficacy of oral 5-aminosalicylic acid (5-ASA) agents for maintenance of medically-induced remission in Crohn's disease have produced conflicting results. OBJECTIVES: To conduct a systematic review to evaluate the efficacy and safety of oral 5-ASA agents for the maintenance of medically-induced remission in Crohn's disease...
September 28, 2016: Cochrane Database of Systematic Reviews
Takuya Yoshino, Makoto Sono, Shujiro Yazumi
BACKGROUND: Patients with refractory-ulcerative colitis (UC) require therapy escalation. Sulfasalazine (SASP) could deliver a high concentration of 5-aminosalicylic acid to the colon. The usefulness of SASP for refractory-UC patients, however, is unclear. AIM: The aim was to evaluate the usefulness of SASP for refractory-UC patients. METHOD: We retrospectively analysed 36 (11.4%) of 316 patients with refractory-UC who had been treated with SASP...
2016: BMJ Open Gastroenterology
Mei-Sing Ong, Richard J Grand, Kenneth D Mandl
BACKGROUND: Prophylactic treatment of postoperative Crohn's disease (CD) plays a critical role in maintaining clinical remission. We performed the first study in the last decade to examine secular trends in the use of pharmacologic interventions after ileocolonic resection in the United States, to understand whether clinical practice converges with recent advances in scientific knowledge. METHODS: A retrospective study of a U.S. national claims database was performed...
October 2016: Inflammatory Bowel Diseases
Hasan Bagheri, Karam Molaei, Ali Akbar Asgharinezhad, Homeira Ebrahimzadeh, Mojtaba Shamsipur
A new method for the selective extraction of p-aminosalicylic acid from aqueous and urine samples has been developed using magnetic molecularly imprinted polymer nanoparticles before determination by high-performance liquid chromatography. The Fe3 O4 nanoparticles were first prepared through the chemical coprecipitation of Fe(2+) and Fe(3+) and then coated with a vinyl shell. Subsequently, a layer of molecularly imprinted polymers was grafted onto the vinyl-modified magnetic nanoparticles by precipitation polymerization...
October 6, 2016: Journal of Separation Science
Joseph Paul Weiner, Andrew Thomas Wong, David Schwartz, Manuel Martinez, Ayse Aytaman, David Schreiber
Pelvic radiation is a commonly utilized treatment for malignancy of the genitourinary and lower gastrointestinal tract. Radiation proctitis and the resultant clinical picture varies from asymptomatic to potentially life threatening. Similarly, treatment options also vary greatly, from medical therapy to surgical intervention. Commonly utilized medical therapy includes sucralfate enemas, antibiotics, 5-aminosalicylic acid derivatives, probiotics, antioxidants, short-chain fatty acids, formalin instillation and fractionated hyperbaric oxygen...
August 21, 2016: World Journal of Gastroenterology: WJG
Suhrid Banskota, Han-Eol Kang, Dong-Guk Kim, Sang Won Park, Hyeonjin Jang, Ujjwala Karmacharya, Byeong-Seon Jeong, Jung-Ae Kim, Tae-Gyu Nam
Although the pathogenesis of inflammatory bowel disease (IBD) is complex, attachment and infiltration of leukocytes to gut epithelium induced by pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α) represents the initial step of inflammation in IBD. Previously, we have reported that some 6-amino-2,4,5-trimethylpyridin-3-ols have significant levels of antiangiogenic activity via PI3K inhibition. Based on the reports that angiogenesis is involved in the aggravation of IBD and that PI3K is a potential target for IBD therapy, we investigated whether the scaffold has inhibitory activity against in vitro and in vivo models of colitis...
October 1, 2016: Bioorganic & Medicinal Chemistry Letters
Yan-Hong Li, Man Zhang, Hai-Bo Fu, Hai-Tao Xiao, Zhao-Xiang Bian
Our previous study demonstrated that a combination of alternative medicine berberine and conventional 5-aminosalicylic acid (5-ASA) showed promise to be a novel therapeutic strategy for ulcerative colitis (UC). This present study aims to sketch the pre-clinical toxicity profile of this combination (1:10 dose ratio) on mice. In acute toxicity test, the determined median lethal dose (LD50) was 278.7 mg/kg berberine plus 2787 mg/kg 5-ASA. The results from subacute toxicity test demonstrated that no toxic signs of clinical symptoms, no significant changes in hematological or biochemical parameters were detected in mice treated with 14 + 140, 28 + 280 or 56 + 560 mg/kg of berberine plus 5-ASA treatment...
August 30, 2016: Food and Chemical Toxicology
Sarika Johari, Chaitanya Joshi, Tejal Gandhi
BACKGROUND: The protective effect of the chloroform extract of Cyperus rotundus (CHCR) is attributed to its anti-inflammatory and antioxidant activities. Cytokines, important regulators of inflammation and repair, play a key role in the pathogenesis of inflammatory bowel disease (IBD). Targeting these cytokines can effectively ameliorate the symptoms of IBD. The aim of the present study was to unravel the molecular mechanism through cytokine regulation in rats in experimental IBD. METHODS: Sprague Dawley rats were randomly allocated to 5 groups (n=6)...
September 2016: Iranian Journal of Medical Sciences
Sofia Vitor, Alexandre Oliveira Ferreira, João Lopes, José Velosa
We present the case of an 18-year-old male patient that was referred to our gastrenterology department with history of intermittent painless hematochezia since childhood. During such instances, he was diagnosed with bowel intussusception, eosinophilic gastroenteritis and inflammatory bowel disease at 4, 6 and 8 years old, respectively. He underwent treatment with 5-aminosalicylic acid for two years, without improvement of symptoms. He was then lost to follow-up until our observation. His physical examination was unremarkable except for digital rectal examination which found a nodular compressible mass by the palpating finger...
August 2016: Revista Española de Enfermedades Digestivas
Md Masud Parvez, Nazia Kaisar, Ho Jung Shin, Jin Ah Jung, Jae-Gook Shin
Currently marketed 22 anti-tuberculosis drugs were comprehensively evaluated for the inhibitory effect on organic anionic (OAT) and cation transporter (OCT)-mediated uptake using stably transfected HEK293 cells in vitro We observed moderate to strong inhibitory effects on OAT1-, OAT3-mediated para-aminohippurate (PAH) and OCT1- and OCT2-mediated N-methyl-4-phenylpylidinium acetate (MPP(+)) uptake. The strong inhibitory effect was observed by ciprofloxacin, linezolid, para-aminosalicylic acid (PAS) and rifampin with IC50 values 35...
August 22, 2016: Antimicrobial Agents and Chemotherapy
Shoya Wada, Hideki Kumagai, Koji Yokoyama, Takane Ito, Akihiko Miyauchi, Saori Sakamoto, Tomoyuki Imagawa, Janyerkye Tulyeu, Masanori Tanaka, Takanori Yamagata
5-Aminosalicylic acid preparations have been used as first-line drugs for treatment of ulcerative colitis (UC). However, some patients with UC present with exacerbation of symptoms because of allergy to mesalazine. Diagnosis of mesalazine allergy in active UC may be challenging because its symptoms mimic those of UC. Here we describe a 13-year-old boy with mesalazine allergy who achieved remission when his medication was changed from mesalazine to salazosulfapyridine. During his clinical course mesalazine was prescribed twice, and on each occasion exacerbation of the symptoms occurred...
October 2016: Clinical Journal of Gastroenterology
Xin Zhao, Nan Li, YiMing Ren, Tao Ma, ChunLi Wang, Jun Wang, ShengYi You
BACKGROUND: Ulcerative colitis (UC) is a chronic and remitting inflammatory disease that is characterized by chronic idiopathic inflammation of the colon and bloody diarrhea. Currently drug treatment is the main intervention for patients with mild to moderate UC. Mesalazine (5-ASA) and beclomethasone dipropionate (BDP) have been widely used for the treatment of UC and have yielded satisfactory results. This study compared the effectiveness of 5-ASA and BDP in the treatment of UC. METHODS: The PubMed, Medline, SinoMed, Embase, and Cochrane Librinary databases were searched for eligible studies...
2016: PloS One
Chao-Yan Ou, Yi-Ni Luo, Sheng-Nan He, Xiang-Fa Deng, Hai-Lan Luo, Zong-Xiang Yuan, Hao-Yang Meng, Yu-Huan Mo, Shao-Jun Li, Yue-Ming Jiang
Excessive intake of manganese (Mn) may cause neurotoxicity. Sodium para-aminosalicylic acid (PAS-Na) has been used successfully in the treatment of Mn-induced neurotoxicity. The γ-aminobutyric acid (GABA) is related with learning and memory abilities. However, the mechanism of PAS-Na on improving Mn-induced behavioral deficits is unclear. The current study was aimed to investigate the effects of PAS-Na on Mn-induced behavioral deficits and the involvement of ultrastructural alterations and γ-aminobutyric acid (GABA) metabolism in the basal ganglia of rats...
August 5, 2016: Biological Trace Element Research
Aurelio Romero-Castro, Mara Gutiérrez-Sánchez, José Correa-Basurto, Martha Cecilia Rosales Hernández, Itzia Irene Padilla Martínez, Jessica Elena Mendieta-Wejebe
5-[(4-carboxybutanoyl)amino]-2-hydroxybenzoic acid (C2) is a novel synthetic derivative of 5-aminosalicylic acid (5-ASA), which is currently being evaluated ex vivo as an anti-inflammatory agent and has shown satisfactory results. This study aimed to obtain the pharmacokinetic profiles, tissue distribution and plasma protein binding of C2 in Wistar Rats. Additionally, an HPLC method was developed and validated to quantify C2 in rat plasma. The pharmacokinetic profiles of intragastric, intravenous and intraperitoneal administration routes at singles doses of 100, 50, and 100 mg/kg, respectively, were studied in Wistar rats...
2016: PloS One
Kyungsoo Oh, Moon-Chang Baek, Wonku Kang
Sulfisoxazole (SFX) is still used in combination with trimethoprim in cattle despite adverse drug reactions (e.g., urolithiasis). Recently, SFX is known to be a promising repositioned drug candidate for pulmonary hypertension and cancer. We developed a simultaneous determination method of SFX and its N-acetylated metabolites (N(1)-acetyl SFX, N1AS; N(4)-acetyl SFX, N4AS; diacetyl SFX, DAS) using HPLC-MS/MS for the first time, and examined the pharmacokinetics of SFX in mice. N1AS and DAS were converted rapidly to SFX and N4AS, respectively, in mouse plasma...
September 10, 2016: Journal of Pharmaceutical and Biomedical Analysis
Brian P Bosworth, William J Sandborn, David T Rubin, Joseph R Harper
BACKGROUND: Rectal budesonide foam is a second-generation corticosteroid efficacious for active mild to moderate ulcerative proctitis and ulcerative proctosigmoiditis. This subgroup analysis examined the impact of baseline oral 5-aminosalicylic acid (5-ASA) on the efficacy and safety of budesonide foam in patients with mild to moderate ulcerative proctitis or ulcerative proctosigmoiditis. METHODS: Patients received budesonide foam 2 mg/25 mL twice daily for 2 weeks, then once daily for 4 weeks, or placebo, with or without continued stable dosing of baseline oral 5-ASAs, for remission induction at week 6 (primary endpoint) in 2 identically designed, randomized, double-blind, phase 3 studies...
August 2016: Inflammatory Bowel Diseases
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