Rhinocort Aqua Nasal Spray

Budesonide is a synthetic corticosteroid having potent glucocorticoid activity and weak mineralocorticoid activity. The precise mechanism of corticosteroid actions in seasonal and perennial allergic rhinitis is not known. Corticosteroids have been shown to have a wide range of inhibitory activities against multiple cell types (e.g. mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (e.g. histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic mediated inflammation. Overall, the results of clinical trials showed that RHINOCORT AQUA Nasal Spray administered once daily provides statistically significant reduction in the severity of nasal symptoms of seasonal and perennial allergic rhinitis including runny nose, sneezing, and nasal congestion. In some studies, improvement versus placebo has been shown to occur within 24 hours of initiating treatment with RHINOCORT AQUA Nasal Spray. Maximum benefit is generally not achieved until 2 weeks after initiation of treatment.

In standard in-vitro and animal models, budesonide has approximately a 200-fold higher affinity for the glucocorticoid receptor and a 1000-fold higher topical anti-inflammatory potency than cortisol (rat croton oil ear edema assay). As a measure of systemic activity, budesonide is 40 times more potent than cortisol when administered subcutaneously and 25 times more potent when administered orally in the rat thymus involution assay. In glucocorticoid receptor affinity studies, the 22R form was twice as active as the 22S epimer. The therapeutic efficacy of RHINOCORT AQUA Nasal Spray has been evaluated in placebo-controlled clinical trials of seasonal and perennial allergic rhinitis of 3-6 weeks duration. The number of patients treated with budesonide in these studies was 90 males and 51 females aged 6-12 years and 691 males and 694 females 12 years and above. The patients were predominantly Caucasian.

Rarely, immediate and/or delayed hypersensitivity reactions may occur after the intranasal administration of budesonide. Rare instances of wheezing, nasal septum perforation, and increased intraocular pressure have been reported following the intranasal application of corticosteroids, including budesonide.

Budesonide is a white to off-white, odorless powder that is practically insoluble in water and in heptane, sparingly soluble in ethanol, and freely soluble in chloroform. Its partition coefficient between octanol and water at pH 5 is 1.6 x 10 3. RHINOCORT AQUA is an unscented, metered-dose, manual-pump spray formulation containing a micronized suspension of budesonide in an aqueous medium. Microcrystalline cellulose and carboxymethyl cellulose sodium, dextrose anhydrous, polysorbate 80, disodium edetate, potassium sorbate and purified water are contained in this medium; hydrochloric acid is added to adjust the pH to a target of 4.5. RHINOCORT AQUA Nasal Spray is available in two dose strengths which deliver 32 mcg and 64 mcg, respectively, of budesonide per spray.

RHINOCORT AQUA Nasal Spray should be stored at controlled room temperature, 20 to 25°C (68 to 77°F) with the valve up. Do not freeze. Protect from light. Shake gently before use. Do not spray in eyes.