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Budesonide (BUN) is a glucocorticoid with highly potent local anti-inflammatory effects.
It can enhance the stability of endothelial cells, smooth muscle cells and lysosomal membranes, inhibit the immune response and reduce antibody synthesis, thereby reducing the release and activity of allergic mediators such as histamine, and can reduce the enzymatic process stimulated by antigen-antibody binding, inhibit the synthesis and release of bronchoconstrictive substances to reduce the contractile response of smooth muscle.
Acute, subacute and long-term toxicity, it was found that the systemic effects of this product, such as weight loss, lymphoid tissue and adrenal cortex atrophy, are weaker or comparable to other glucocorticoids.
Uses of Budesonide.
For patients with glucocorticoid-dependent or non-dependent bronchial asthma and asthmatic chronic bronchitis.
Mild, moderate colonic Crohn's, ulcerative colitis confined to the sigmoid colon can be used as an enema.
Pharmacological Effect of Budesonide.
1. Inhibit phospholipase A2 by inducing the synthesis of lipocalin, reduce the production and release of platelet-activating factor, leukotrienes, prostaglandins and other lipid-based inflammatory mediators generated by the enzyme-catalysed hydrolysis of membrane phospholipids.
2. Inducing the expression of angiotensin I converting enzyme and neutral peptide chain endonuclease, accelerating the generation of angiotensin II and the degradation and inactivation of bradykinin and tachykinin, respectively; inhibiting the expression of oxidative nitrous oxide synthase, reducing the generation of oxidative nitrous oxide.
Thus, it can constrict blood vessels, or reduce the vasodilatory, inflammatory, and neurogenic inflammatory reaction inducing effects of many other active substances except angiotensin II. In addition, it can also induce the production of vasocortin, a vasoconstrictor substance.
3. Inhibit the expression of a variety of cytokines, such as interleukin 1, 3, 4, 6, 8, tumour necrosis factor, granulocyte colony-stimulating factor. Reduce the role of the above factors in airway inflammation, especially chronic inflammation.
4. Promote the expression of adrenergic β2 receptor and increase the sensitivity to endogenous and exogenous medicinal β2 agonists.
5. Immunosuppressive effect: It has inhibitory effect on the whole immune process from phagocytosis processing of antigen, division and proliferation of lymphocytes, differentiation, to the effector phase.
Drug interactions of Bulk Budesonide Powder.
1, No clinically significant interactions have been reported between budesonide and other drugs used in the treatment of asthma.
2, ketoconazole and cimetidine may affect the in vivo metabolism of budesonide, but the recommended dose of inhalation is not clinically significant.
3, No interactions have been observed between this product and other drugs used to treat asthma or COPD. The metabolic conversion of budesonide can be inhibited by substances metabolised by CYP3A4 (e.g. itraconazole, ketoconazole, ritonavir, nelfinavir, cyclosporine, ethinylestradiol and vinblastine).
Concomitant use of this product with these inhibitors of CYP3A4 increases plasma budesonide concentrations, which is not clinically significant in the short term (1-2 weeks) but should be considered for long-term treatment.
At the recommended dose, cimetidine mildly affects the pharmacokinetics of oral budesonide, but is not clinically significant
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