Budesonide in the treatment of inflammatory bowel disease

Silverman, Jason A.; Otley, Anthony

doi:10.1586/eci.11.34

Cited by 40 publications

(34 citation statements)

References 63 publications

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“…Both are also applied as topical treatment in mild types of disease. The systemic administration of corticosteroids/prednisolone is of course much more effective in induction of clinical remission [64,65] , but commonly causes more side effects than budesonide [63,64,66] . Two recent studies support this observation even in high dose 5ASA therapy [67] .…”

Section: CDmentioning

confidence: 99%

Pharmacological- and non-pharmacological therapeutic approaches in inflammatory bowel disease in adults

Leitner

Vogelsang

2016

WJGPT

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Inflammatory bowel diseases (IBDs) are a group of chronic inflammatory conditions mainly of the colon and small intestine. Crohn's disease (CD) and ulcerative colitis (UC) are the most frequent types of IBD. IBD is a complex disease which arises as a result of the interaction of environmental, genetic and immunological factors. It is increasingly thought that alterations of immunological reactions of the patients to their own enterable bacteria (microfilm) may contribute to inflammation. It is characterized by mucosal and sub mucosal inflammation, perpetuated by infiltration of activated leukocytes. CD may affect the whole gastrointestinal tract while UC only attacks the large intestine. The therapeutic goal is to achieve a steroidfree long lasting remission in both entities. UC has the possibility to be cured by a total colectomy, while CD never can be cured by any operation. A lifelong intake of drugs is mostly necessary and essential. Medical treatment of IBD has to be individualized to each patient and usually starts with anti-inflammatory drugs. The choice what kind of drugs and what route administered (oral, rectal, intravenous) depends on factors including the type, the localization, and severity of the patient's disease. IBD may require immune-suppression to control symptoms such as prednisolone, thiopurines, calcineurin or sometimes folic acid inhibitors or biologics like TNF-α inhibitors or anti-integrin antibodies. For both types of disease (CD, UC) the same drugs are available but they differ in their preference in efficacy between CD and UC as 5-aminosalicylic acid for UC or budesonide for ileocecal CD. As therapeutic alternative the main mediators of the disease, namely the activated pro-inflammatory cytokine producing leukocytes can be selectively removed via two apheresis systems (Adacolumn and Cellsorba) in steroid-refractory or dependent cases. Extracorporeal photopheresis results in an increase of regulatory B cells, regulatory CD8 + T cells and T-regs Type 1. Both types of apheresis were able to induce clinical remission and mucosal healing accompanied by tapering of steroids.

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Section: CDmentioning

confidence: 99%

Pharmacological- and non-pharmacological therapeutic approaches in inflammatory bowel disease in adults

Leitner

Vogelsang

2016

WJGPT

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“…Budesonide is a glucocorticoid used for the treatment of several inflammatory diseases in the respiratory and gastrointestinal tracts (Ceylan, 2006;Silverman & Otley, 2011). It is available in different formulations, including an inhalation powder (Pulmicort Flexhaler Õ , AstraZeneca, Södertälje, Sweden), a nebulised suspension (Pulmicort Respules TM , AstraZeneca UK Ltd, Luton, UK), an aerosol nasal spray (Rhinocort Aqua Õ , AstraZeneca UK Ltd, Luton, UK), oral tablets (Entocort Õ EC, AstraZeneca, Södertälje, Sweden; Uceris Õ , Salix Pharmaceuticals, Raleigh, NC) and a rectal foam (Uceris Õ , Salix Pharmaceuticals, Raleigh, NC).…”

Section: Introductionmentioning

confidence: 99%

“…On average, 60-80% of an oral dose (capsules) is absorbed in the ileum and colon (Edsbäcker et al, 2003;Lundin et al, 2001). Once absorbed, budesonide is cleared through extensive first-pass metabolism by cytochrome P450 (CYP) 3A4 and, to a lesser extent, CYP3A5 in the liver and intestinal wall, resulting in low systemic bioavailability (Silverman & Otley, 2011). This has been shown to vary depending on the specific formulation with 10-15% systemic bioavailability reported for oral and rectal formulations compared with 13-29% bioavailability for nasally administered formulations (Danielsson et al, 1993;Silverman & Otley, 2011;Thorsson et al, 1999).…”

Section: Introductionmentioning

confidence: 99%

“…Budesonide is primarily metabolised to 16a-hydroxyprednisolone and 6b-hydroxybudesonide ( Figure 1) (Jonsson et al, 1995). The activity of these metabolites is less than 1% of that of the parent compound, and they do not contribute further to the therapeutic effect of budesonide (Silverman & Otley, 2011). In vitro studies of the phase II metabolism of budesonide have demonstrated that it undergoes sulfation by cytosolic sulfotransferase enzyme 1A1 (Meloche et al, 2002); studies in lung tissue slices have also demonstrated the formation of fatty acid esters from budesonide (Nave et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

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In vitro drug–drug interactions of budesonide: inhibition and induction of transporters and cytochrome P450 enzymes

et al. 2017

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Abstract1. Budesonide is a glucocorticoid used in the treatment of several respiratory and gastrointestinal inflammatory diseases. Glucocorticoids have been demonstrated to induce cytochrome P450 (CYP) 3A and the efflux transporter P-glycoprotein (P-gp). This study aimed to evaluate the potential of budesonide to act as a perpetrator or a victim of transporter-or CYP-mediated drug-drug interactions (DDIs). 2. In vitro studies were conducted for P-gp, breast cancer resistance protein and organic anion and cation transporters (OATP1B1, OATP1B3, OAT1, OAT3, OCT2) in transporter-transfected cells. Changes in mRNA expression in human hepatocytes and enzyme activity in human liver microsomes by budesonide were determined for CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A. 3. The data indicated that budesonide is a substrate of P-gp but is not a substrate or an inhibitor of the other transporters investigated. Budesonide is neither an inducer nor an inhibitor of major CYP enzymes. The effect of P-gp on budesonide disposition is anticipated to be low owing to CYP3A-mediated clearance. 4. Collectively, our data indicate there is a low risk of budesonide perpetrating clinical DDIs mediated by the transporters or CYPs studied.

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“…Budesonide is a synthetic corticosteroid that is used for treatment of asthma, allergic rhinitis, autoimmune hepatitis, and inflammatory bowel disease [1][2][3]. The drug is an epimeric mixture of 22S and 22R configurations in a 1:1 ratio [4] and is considered to possess unique favorable pharmacological properties [5].…”

Section: Introductionmentioning

confidence: 99%

Phospholipid removal combined with a semi-automated 96-well SPE application for determination of budesonide in human plasma with LC–MS/MS

Nilsson¹,

Andersson²,

Beck³

2014

Journal of Chromatography B

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Budesonide in the treatment of inflammatory bowel disease

Cited by 40 publications

References 63 publications

Pharmacological- and non-pharmacological therapeutic approaches in inflammatory bowel disease in adults

Pharmacological- and non-pharmacological therapeutic approaches in inflammatory bowel disease in adults

In vitro drug–drug interactions of budesonide: inhibition and induction of transporters and cytochrome P450 enzymes

Phospholipid removal combined with a semi-automated 96-well SPE application for determination of budesonide in human plasma with LC–MS/MS

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