2012年1月20日，美国食品药品管理局（FDA）批准Zetonna（ciclesonide，环索奈德）鼻气雾剂对症治疗成人和12岁以上青少年季节性和常年过敏性鼻炎。 环索奈德是一种皮质类固醇，最初于2006年10月获准的鼻喷雾剂系一种手动泵喷雾计量吸入制剂，配方中含低渗环索奈德水悬浮液，以Omnaris商品名销售。 Zetonna鼻气雾剂使用一种氢氟烷（HFA）作抛射剂，将小体积（50 微升）干燥薄雾状环索奈德输入患者的鼻腔，这样可减少原先的水基制剂吸入时在猴背部产生的不适感觉。 在1111名12岁以上的常年性变应性鼻炎（PAR）患者中开展了一项大型的III期临床研究，对每日一次74微克或148微克剂量环索奈德鼻气雾剂作了试验。这项为期26周的双盲、随机研究表明：经过最初6周双盲治疗，两种剂量治疗与安慰剂组相比PAR患者鼻部症状后有统计学意义的显著改善。26周双盲治疗期结果表明，74微克和148微克剂量的环索奈德鼻气雾剂治疗耐受性与安慰剂组相比效果明显。 ZETONNA Manufacturer: Sunovion Pharmacological Class: Corticosteroid. Active Ingredient(s): Ciclesonide 37micrograms/actuation; metered-dose nasal aerosol; contains HFA. Indication(s): Treatment of symptoms associated with seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR) in patients ≥12 years of age. Pharmacology: Ciclesonide is a prodrug that is enzymatically hydrolyzed to its active metabolite, des-ciclesonide following intranasal application. Des-ciclesonide has anti-inflammatory activity with affinity for the glucocorticoid receptor that is 120 times higher than the parent compound. The precise mechanism through which ciclesonide affects allergic rhinitis symptoms is not known. Clinical Trials: The efficacy of Zetonna Nasal Aerosol was evaluated in one randomized, double-blind, parallel-group, multicenter, placebo-controlled dose-ranging trial (74mcg, 148mcg, and 282mcg once daily) and 3 confirmatory trials (74mcg and 148mcg once daily) involving 3,001 patients with allergic rhinitis. Patients enrolled in the trials were 12–81 years of age with a history of SAR or PAR, a positive skin test to at least one relevant allergen, and active symptoms of allergic rhinitis at study entry. Assessment of efficacy in these trials was based on patient recording of four nasal symptoms (runny nose, nasal itching, sneezing, and nasal congestion) on a 0–3 categorical severity scale (0 = absent, 1 = mild, 2 = moderate, and 3 = severe) as reflective or instantaneous total nasal symptom scores (rTNSS and iTNSS respectively). Additional secondary efficacy variables were assessed, including the total ocular symptom score (TOSS) in the SAR trials and the Rhinoconjunctivitis Quality of Life Questionnaire with Standardized Activities [RQLQ(S)] in both SAR and PAR trials. In the dose-ranging trial, the primary efficacy endpoint was the difference from placebo in the change from baseline of the average of AM and PM rTNSS averaged over the 2-week treatment period. The rTNSS showed a statistically significant estimated treatment difference from placebo of 0.81 (95% CI: 0.32, 1.29); 0.90 (95% CI: 0.40, 1.39); and 0.66 (95% CI: 0.16, 1.16) for 282mcg, 148mcg and 74mcg, respectively. In the confirmatory SAR and PAR trials, Zetonna 74mcg once daily was statistically significantly different from placebo. The rTNSS showed a statistically significant estimated treatment difference from placebo; SAR was 0.9 (95% CI: 0.6, 1.3), and PAR was 0.7 (95% CI: 0.4, 1.0). Statistically significant differences in the AM pre-dose iTNSS indicate that the effect was maintained over the full 24-hour dosing interval for both trials. In the SAR trials, Zetonna 74mcg demonstrated a statistically significant decrease from baseline in the rTOSS compared to placebo. Similarly, a clinically significant decrease (≥ 0.5) from baseline vs. placebo for the RQLQ(S) was also shown. In the PAR trial, Zetonna 74mcg did not demonstrate a clinically significant change from baseline in the overall RQLQ(S) compared to placebo. TOSS was not evaluated in this trial. In both SAR and PAR trials, Zetonna 148mcg once daily did not provide an efficacy benefit over the 74mcg once daily dose. Legal Classification: Rx Adults: One actuation in each nostril once daily (37mcg/actuation); max 74mcg/day. Children: Not established. Warnings/Precautions: Conduct nasal examination before starting treatment. Discontinue if nasal erosion, ulceration, or perforation occurs. Active or quiescent respiratory tract tuberculosis. Infections (eg, ocular herpes simplex). If exposed to measles or chickenpox, consider immunoglobulin prophylactic therapy. If adrenal suppression exists following systemic corticosteroid therapy, replacement with topical steroids may exacerbate symptoms of adrenal insufficiency. Monitor for hypercorticism and HPA axis suppression (if occur discontinue gradually), and for candida infection and other nasal cavity changes. Monitor for growth suppression in children. Monitor for vision changes or if history of increased intraocular pressure, glaucoma or cataracts. Avoid spraying in eyes or directly onto the nasal septum. Pregnancy (Cat. C). Nursing mothers. Interaction(s): May be potentiated by ketoconazole. Adverse Reaction(s): Nasal discomfort, headache, epistaxis; ulcerations, nasal septal perforation, candida infection, impaired wound healing. How Supplied: Nasal aerosol—6.1g (60 actuations) Last Updated: 8/6/2012