Budesonide is a glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. [PubChem] The extended release oral tablet, marketed as Uceris, was FDA approved on January 14, 2013 for the management of ulcerative colitis. Budesonide is provided as a mixture of two epimers (22R and 22S). Interestingly, the 22R form is two times more active than the 22S epimer. The two forms do not interconvert.
Rhinocort Aqua is a nasal spray containing budesonide, a corticosteroid. It prevents the release of substances in the body that cause inflammation.
Rhinocort Aqua nasal spray is used to treat stuffy nose, sneezing, and runny nose caused by seasonal or year-round allergies.
Rhinocort Aqua is also used to keep nasal polyps from coming back after surgery to remove them.
Before using Rhinocort Aqua, tell your doctor if you have been sick or had an infection of any kind. Also tell your doctor if you have liver disease, glaucoma or cataracts, herpes simplex infection of your eyes, tuberculosis, sores or ulcers in your nose, or if you have recently had injury of or surgery on your nose.
Budesonide has a high glucocorticoid effect and a weak mineralocorticoid effect. It binds to the glucocorticoid receptor with a higher binding affinity than cortisol and prednisolone.
When budesonide is systemically administered, suppression of endogenous cortisol concentrations and an impairment of the hypothalamus-pituitary-adrenal (HPA) axis function has been observed. Furthermore, a decrease in airway reactivity to histamine and other entities has been observed with the inhaled formulation.
Generally, the inhaled formulation has a rapid onset action and improvement in asthma control can occur within 24 hours of initiation of treatment.
Budesonide is an anti-inflammatory corticosteroid that exhibits potent glucocorticoid activity and weak mineralocorticoid activity. The precise mechanism of corticosteroid actions on inflammation in asthma, Crohn's disease, or ulcerative colitis is not known. Inflammation is an important component in the pathogenesis of asthma.
Corticosteroids have been shown to have a wide range of inhibitory activities against multiple cell types (eg, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (eg, histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic and non-allergic-mediated inflammation.
These anti-inflammatory actions of corticosteroids may contribute to their efficacy in the aforementioned diseases. Because budesonide undergoes significant first-pass elimination, the both oral preparations are formulated as an extended release tablet. As a result, budesonide release is delyaed until exposure to a pH ≥ 7 in the small intestine.
Metabolism: Following absorption, budesonide is subject to high first pass metabolism (80-90%). Budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6b-hydroxybudesonide and 16a- hydroxyprednisolone. The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.
Absorption: Absorption is complete following oral administration. The pharmacokinetic parameters of the inhaled powder formulation are as follows: Tmax = 30 minutes;
Route of elimination: Budesonide is excreted in urine and feces in the form of metabolites. Approximately 60% of an intravenous radiolabelled dose was recovered in the urine. No unchanged budesonide was detected in the urine.
Half life: Following IV administration of budesonide, the elimination half-life is 2.0 to 3.6 hours.
All medicines may cause side effects, but many people have no, or minor, side effects.Some medical conditions may interact with Budesonide.
Tell your doctor or pharmacist if you have any medical conditions.
Common Rhinocort Aqua side effects may include: dry or sore throat, cough, irritation in your nose, pain, swelling, burning, itching, or irritation in your throat, sores or white patches inside or around your nose.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider.
