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Compatibility of commonly used drugs in lactation
Published in Amy Brown, Wendy Jones, A Guide to Supporting Breastfeeding for the Medical Profession, 2019
Sulfasalazine – be alert for bloody diarrhoea. RID 0.3–1.1%; licensed for use in children > 2 years. Mesalazine – be alert for watery diarrhoea. Negligible amounts in milk. RID 0.12–8.76%.Balsalazide – absorbed in colon, not gut, and broken down to mesalazine. No studies located. Be alert for watery diarrhoea.Olsalazine – one case study of 1 patient where RID calculated as 0.9%. Monitor for watery diarrhoea.
Inflammatory bowel disease
Published in Michael JG Farthing, Anne B Ballinger, Drug Therapy for Gastrointestinal and Liver Diseases, 2019
Elizabeth Carty, Anne B Ballinger
Extensive disease cannot be treated adequately using enemas. Mild to moderate disease is treated with mesalazine-containing compounds (Table 5.4) and moderate to severe disease requires oral or intravenous corticosteroids. Oral sulphasalazine 4-6 g/day in four divided doses effectively induces remission in UC21 but its use can be limited by side-effects. Clinical trials have shown that the newer 5-ASA preparations are equally effective as sulphasalazine for inducing remission and that they are associated with fewer side-effects.22, 23 It is unclear if any of these newer compounds have significant benefits over others in the treatment of acute UC. In one study, balsalazide 2.25 mg three times a day was slightly more effective than Asacol (800 mg three times daily) in inducing a remission and there appeared to be fewer side-effects with balsalazide.24 Oral corticosteroids are indicated for moderate to severe UC. Prednisolone 40 mg daily induced remission in about 55% of patients after 3 weeks’ of treatment, which was significantly better than the remission rate obtained with a 20 mg daily dosage. There was further benefit with a 60 mg dosage but this associated with a marked increase in adverse effects.25 Azathioprine or its metabolite, 6-mercaptopurine (6-MP) permits cessation of steroids or a reduction in dose in many patients with persistent symptoms despite prolonged corticosteroid treatment.26, 27 However, onset of action is slow and up to 3-6 months’ of treatment may be required to appreciate an optimal effect.
Medical Treatment of IBD
Published in Peter Sagar, Andrew G. Hill, Charles H. Knowles, Stefan Post, Willem A. Bemelman, Patricia L. Roberts, Susan Galandiuk, John R.T. Monson, Michael R.B. Keighley, Norman S. Williams, Keighley & Williams’ Surgery of the Anus, Rectum and Colon, 2019
Naveen Sharma, Michael R.B. Keighley, Severine Vermeire
Oral mesalazine 2.4 to 4.8 g daily or balsalazide 6.75 g daily is an effective first-line therapy. Topical mesalazine combined with oral mesalazine is more effective than oral therapy alone. Once daily dosing of mesalazine is at least as effective as twice or three times daily regimes.
Successes, failures, and future prospects of prodrugs and their clinical impact
Published in Expert Opinion on Drug Discovery, 2019
The success of prodrugs in the management of GIT conditions is well established. Sulfasalazine (1 in Figure 1) is indicated for the treatment of ulcerative colitis and Crohn’s disease. It is a prodrug metabolized by intestinal bacteria azo-reductase. The azo bond in the prodrug is cleft producing two active metabolites: 5-aminosalicylic acid (5-ASA) and sulfapyridine [33]. Similarly, balsalazide (2 in Figure 1) also contains an azo bond cleavable by intestinal bacteria azo-reductase. Upon metabolism, balsalazide produces 5-ASA and 4-aminoenzoil-β-alanine. While balsalazide exhibits similar therapeutic activity to sulfasalazine, it has been reported to be better tolerated [34]. Olsalazine (3 in Figure 1) also contains the same linkage and is cleft by the same mechanism. Though, it produces 2 molecules of 5-ASA. The therapeutic efficacy of olsalazine is comparable to that of sulfasalazine and balsalazide, however, it is better tolerated [35].
Complications and adverse effects related to surgical and medical treatment in patients with inflammatory bowel disease in a prospectively recruited population-based cohort
Published in Scandinavian Journal of Gastroenterology, 2021
Anders Rönnblom, Östen Ljunggren, Urban Karlbom
Salicylates were the most frequently used group of drugs, the overwhelming majority was mesalamine, but a few individuals used olsalazine or balsalazide. Three patients developed pulmonary complications within weeks after initiation of treatment with mesalamine or after dose adjustment. All recovered uneventfully after discontinuation of the drug. One of these patients was offered treatment with balsalazide but the symptoms recurred. There was no increased risk for surgery among patients with UC intolerant to mesalamine (2/16 vs. 13/274, p = .2).