——Dymista喷鼻剂获准用于治疗季节性过敏性鼻炎

2012年5月2日，Meda宣布美国食品药品管理局(FDA)已批准Dymista(盐酸氮卓斯汀和丙酸氟替卡松)用于治疗年龄≥12岁的季节性过敏性鼻炎(SAR)患者。Dymista是一种喷鼻剂，含有1种H1受体拮抗剂和1种皮质激素。用法为每次对两侧鼻孔各喷1下，每日给药2次。
Dymista的有效性与安全性已在多项研究中得到了评估，这些研究共招募4,000多例患者，其中一项长期安全性研究招募了超过600例患者。
共招募853例患者的3项随机、多中心、双盲、安慰剂对照临床试验的结果，帮助确定了Dymista的安全性和有效性。受试患者被随机分为4个治疗组：Dymista喷鼻剂、盐酸氮卓斯汀喷鼻剂、丙酸氟替卡松喷鼻剂或安慰剂；各组均每次对两侧鼻孔各喷1下，每日给药2次。基于反射性鼻部症状总评分(rTNSS)、瞬时鼻部症状总评分和其他支持性次要疗效参数，对疗效进行评估。在这些试验中，Dymista喷鼻剂组的rTNSS减少程度显著多于另外三组。2种单药治疗的疗效与安慰剂相比，差异也分别具有统计学显著性。
Dymista使用者报告的最常见不良反应包括味觉障碍、鼻出血和头痛。

制造商：
梅达制药

药理分类：
抗组胺剂+皮质类固醇。

“活性成分”（词）：
盐酸氮卓斯汀（HCL），氟替卡松137mcg/50mcg;每0.137mL计量喷鼻剂;水悬浮液。

指示（S）：
季节性过敏性鼻炎。

药理作用：
盐酸氮卓斯汀是一种抗组胺剂，H1-受体拮抗活性的干扰与炎症反应的过敏原。主要活性代谢物的氮卓斯汀盐酸desmethylazelastine，还具有H1-受体拮抗活性。

替卡松丙酸酯是一种合成的三氟化皮质类固醇抗炎活性。通过丙酸氟替卡松的影响过敏性鼻炎的症状的确切机制尚不清楚。

临床试验：
在3个随机，多中心，双盲，安慰剂对照的临床试验中，853例≥12岁季节性过敏性鼻炎的Dymista季节性过敏性鼻炎的疗效和安全性进行了评估。患者被随机分配到四个治疗组之一：每个鼻孔一喷，每日两次，氮卓斯汀盐酸鼻喷雾剂，丙酸氟替卡松鼻喷雾剂，车辆安慰剂Dymista。

疗效评估的基础上的反射总鼻部症状的得分（rTNSS），另外的瞬时总鼻部症状的得分（iTNSS）和其他支持的次要疗效变量。 TNSS的计算公式为患者的得分总和的4个人鼻部症状（流涕，鼻塞，打喷嚏，鼻痒）在0到3个明确的严重程度量表（0 =无，1 =轻度，2 =中度， 3 =重度）。患者被要求每天记录症状的严重程度，反映了在过去12小时（AM和PM）。主要疗效终点，合并AM +：PM rTNSS（最高24分）的每一天为从基线的变化进行了评估，然后平均在2周的治疗期。主要疗效终点是从基线的平均变化联合AM + PM rTNSS超过2周。录得的iTNSS紧接的下一个剂量。

在这些试验中，Dymista表现出统计学显著下降（从基线的变化）在rTNSS（-5.6）相比，盐酸氮卓斯汀（-4.3）和丙酸氟替卡松（-4.7），以及安慰剂组（-2.9）。

在这些试验中，Dymista也表现出统计上显著，大幅度降低（从基线的变化）iTNSS（-5.2）相比安慰剂（-2.7），做了盐酸氮卓斯汀（-3.9）和丙酸氟替卡松（-4.5）比较。

法律分类：
接收

成人：
每个鼻孔喷1次，每日两次。

儿童：
不成立的。

警告/注意事项：
避免在最近鼻腔溃疡，鼻腔手术或鼻外伤的使用。呼吸道结核。感染（例如，真菌，细菌，病毒，眼单纯疱疹）。避免接触水痘和麻疹，如果暴露，应考虑抗感染的预防性治疗。如果存在肾上腺皮质功能不全，全身性皮质类固醇治疗后，更换外用皮质类固醇可能会加剧肾上腺皮质功能不全（例如，精神不振，抑郁症）的症状。监控经常在孩子的成长。监测亢进和抑制丘脑 - 垂体 - 肾上腺轴（如果逐渐发生中断），念珠菌感染或其他鼻腔黏膜的变化。历史，青光眼，眼压增高和/或白内障;监控任何视力变化。避免眼睛。妊娠（部件C）。哺乳期的母亲。

互动（补）：
避免酒精或其他中枢神经系统抑制剂。伴随利托那韦：不推荐。注意与其他强效的CYP3A4抑制剂（如酮康唑）。

不良反应（S）：
味觉异常，鼻出血，头痛，嗜睡。

如何提供：
泵（23G）-120喷射的

最后更新：
2012年10月5日

Manufacturer:
Meda Pharmaceuticals

Pharmacological Class:
Antihistamine + corticosteroid.

Active Ingredient(s):
Azelastine hydrochloride (HCl), fluticasone propionate 137mcg/50mcg; per 0.137mL metered nasal spray; aqueous suspension.

Indication(s):
Seasonal allergic rhinitis.

Pharmacology:
Azelastine HCl is an antihistamine that antagonizes H1-receptor activity by interfering with the inflammatory response to the allergens. The major active metabolite of azelastine HCl, desmethylazelastine, also possesses H1-receptor antagonist activity.

Fluticasone propionate is a synthetic trifluorinated corticosteroid with anti-inflammatory activity. The precise mechanism through which fluticasone propionate affects allergic rhinitis symptoms is not known.

Clinical Trials:
The efficacy and safety of Dymista in seasonal allergic rhinitis was evaluated in 3 randomized, multicenter, double-blind, placebo-controlled clinical trials in 853 patients ≥12 years with seasonal allergic rhinitis. Patients were randomized to one of four treatment groups: one spray per nostril twice daily of Dymista, azelastine HCl nasal spray, fluticasone propionate nasal spray, and vehicle placebo.

Assessment of efficacy was based on the reflective total nasal symptom score (rTNSS), in addition to the instantaneous total nasal symptom score (iTNSS) and other supportive secondary efficacy variables. TNSS is calculated as the sum of the patients’ scoring of the 4 individual nasal symptoms (rhinorrhea, nasal congestion, sneezing, and nasal itching) on a 0 to 3 categorical severity scale (0 = absent, 1 = mild, 2 = moderate, 3 = severe). Patients were required to record symptom severity daily reflecting over the previous 12 hours (AM and PM). For the primary efficacy endpoint, the combined AM+PM rTNSS (maximum score of 24) was assessed as a change from baseline for each day and then averaged over a 2 week treatment period. The primary efficacy endpoint was the mean change from baseline in combined AM+PM rTNSS over 2 weeks. The iTNSS was recorded immediately prior to the next dose.

In these trials, Dymista demonstrated statistically significant greater decreases (change from baseline) in rTNSS (-5.6) as compared to azelastine HCl (-4.3) and to fluticasone propionate (-4.7), as well as to placebo (-2.9).

In these trials, Dymista also demonstrated statistically significant, greater decreases (change from baseline) in iTNSS (-5.2) as compared to placebo (-2.7), as did the azelastine HCl (-3.9) and fluticasone propionate (-4.5) comparators.

Legal Classification:
Rx

Adults:
1 spray per nostril twice daily.

Children:
Not established.

Warnings/Precautions:
Avoid use in recent nasal ulcers, nasal surgery, or nasal trauma. Respiratory tract tuberculosis. Infections (eg, fungal, bacterial, viral, ocular herpes simplex). Avoid exposure to chickenpox and measles; if exposed, consider anti-infective prophylactic therapy. If adrenal insufficiency exists following systemic corticosteroid therapy, replacement with topical corticosteroids may exacerbate symptoms of adrenal insufficiency (eg, lassitude, depression). Monitor growth routinely in children. Monitor for hypercorticism and HPA axis suppression (if occur discontinue gradually), and Candida infection or other nasal mucosal changes. History of increased intraocular pressure, glaucoma, and/or cataracts; monitor any change in vision. Avoid eyes. Pregnancy (Cat. C). Nursing mothers.

Interaction(s):
Avoid alcohol or other CNS depressants. Concomitant ritonavir: not recommended. Caution with other potent CYP3A4 inhibitors (eg, ketoconazole).

Adverse Reaction(s):
Dysgeusia, epistaxis, headache; somnolence.

How Supplied:
Pump (23g)—120 sprays

Last Updated:
10/5/2012