Budesonide rectal

Corticosteroids for rectal use betamethasone sodium phosphate budesonide... 

Corticosteroids and adrenocorticotropic hormone have been widely used for the treatment of ulcerative cohtis and Crohn s disease, given parenterally, orally, or rectally. Corticosteroids are believed to modulate the immune system and inhibit production of cytokines and mediators. It is not clear whether the most important steroid effects are systemic or local (mucosal). Budesonide is a corticosteroid that is administered orally in a controlled-release formulation. The drug undergoes extensive first-pass metabolism, so systemic exposure is thought to be minimized. Immunosuppressive agents such as azathioprine, mercaptopurine (a metabolite of azathioprine), methotrexate, or cyclosporine are sometimes used for the treatment of IBD. ... 

The choice of rectally administered steroid is a subject of debate, as there is varying potential for systemic steroid absorption with different products. Although many steroids have been administered rectally, certain agents such as betamethasone-17-valerate, beclomethasone dipropionate, prednisolone metasulfobenzoate, prednisolone-21-phosphate, and budesonide have been used in attempts to reduce systemic steroid effects. Systemic side effects may be the least severe with beclomethasone dipropionate, because... 

Grapefruit juice increases plasma levels of methylprednisolone and is predicted to increase plasma levels of rectal budesonide. Grapefruit juice does not affect the pharmacokinetics of prednisone or prednisolone. 

Budenofalk Rectal Foam (Budesonide). Dr. Falk Wiarma UK Ltd UK Summary of product characteristics, June 2006. 

One case report indicates that clarithromycin may enhance the effects of inhaled budesonide and although the authors suggest that prolonged use of clarithromycin and the terminal condition of the patient may have been factors, they advise close monitoring if the combination is used. Note that rectal budesonide produces higher plasma levels than the oral or inhaled use. The manufacturers of one UK rectal preparation advise that potent inhibitors of CYP3A4 (they name clarithromycin) should be avoided. However, given the evidence available, this seems a very cautious approach. 

Some suspensions have such a limited stability, that they have to be prepared just before use. An example is an enema with budesonide, where the active substance is incorporated in a dispersible tablet, that has to be added to a solution for rectal suspension. Here again, correct instruction of the user or caregiver is important. 

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See also in sourсe #XX -- [ ]

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