近日，美国食品和药物管理局（FDA）批准Baqsimi（胰高血糖素）鼻粉剂，用于4岁及以上糖尿病患者严重低血糖的紧急治疗。值得一提的是，Baqsimi鼻粉剂是首个无需注射给药治疗严重低血糖的胰高血糖素疗法。在美国，注射用胰高血糖素已被批准使用了数十年。
严重低血糖是指患者血糖水平下降到某一水平，出现困惑或失去知觉，或出现其他需要他人帮助治疗的症状。严重低血糖通常发生在使用胰岛素治疗的糖尿病患者身上。
Baqsimi是一种通过鼻腔给药的粉剂，装在一次性喷雾器中，可以给正在经历严重低血糖症的患者用药。Baqsimi通过刺激肝脏将储存的葡萄糖释放到血液中来增加体内的血糖水平，它具有与胰岛素相反的作用，而胰岛素是降低血糖水平。
批准日期：2019年7月24日 公司：礼来公司
BAQSIMI（胰高血糖素[glucagon]）鼻粉,鼻内装置
最初的美国批准：1960年
作用机制
胰高血糖素通过激活肝脏胰高血糖素受体来增加血糖浓度，从而刺激糖原分解和从肝脏释放葡萄糖。糖原的肝脏储存是胰高血糖素产生抗血糖作用所必需。
适应症和用法
BAQSIMI™是一种抗降血糖药，适用于治疗4岁及以上糖尿病患者的严重低血糖症。
剂量和给药
•BAQSIMI仅供鼻内使用。
•BAQSIMI的推荐剂量为3mg，作为鼻内装置的一个动作进入一个鼻孔。
•根据收缩管标签和使用说明书上的印刷说明管理BAQSIMI。
•通过将尖端插入一个鼻孔并将设备柱塞完全压入直到绿线不再显示来管理剂量。剂量不需要吸入。
•给药后立即呼叫紧急援助。
•当患者对治疗有反应时，给予口服碳水化合物。
•请勿尝试重复使用BAQSIMI。每个BAQSIMI设备都含有一剂胰高血糖素，不能重复使用。
•如果15分钟后没有响应，可在等待紧急援助时再施用3mg剂量。
剂量形式和强度
鼻粉：含有一剂胰高血糖素3mg的鼻内装置
禁忌症
•嗜铬细胞瘤
•胰岛素瘤
•已知对胰高血糖素或任何赋形剂过敏
警告和注意事项
•嗜铬细胞瘤患者的儿茶酚胺释放：嗜铬细胞瘤患者禁用，因为BAQSIMI可能刺激肿瘤中儿茶酚胺的释放。
•胰岛素瘤患者缺乏疗效：对于胰岛素瘤患者，给药可能会使血糖发生初步增加;然而，BAQSIMI可能会刺激胰岛素瘤的过度胰岛素释放并导致低血糖。如果患者在服用BAQSIMI剂量后出现低血糖症状，则口服或静脉注射葡萄糖。
•过敏反应和过敏反应：已报告过敏反应，包括全身性皮疹，在某些情况下还有呼吸困难的过敏性休克和低血压。
•肝糖原减少患者缺乏疗效：只有存在足够的肝糖原时，BAQSIMI才能有效治疗低血糖症。处于饥饿状态，肾上腺功能不全或慢性低血糖状态的患者可能没有足够水平的肝糖原来使BAQSIMI有效。患有这些病症的患者应该用葡萄糖治疗。
不良反应
最常见（≥10％）与BAQSIMI相关的不良反应是恶心，呕吐，头痛，上呼吸道刺激（即鼻漏，鼻子不适，鼻塞，咳嗽和鼻出血），眼睛流泪，眼睛发红，鼻子发痒，喉咙 和眼睛。
要报告疑似不良反应，请联系Eli Lillyand公司，电话1-800-LillyRx（1-800-545-5979）或FDA电话1-800-FDA-1088或www.fda.gov/medwatch。
药物相互作用
•β受体阻滞剂：服用β受体阻滞剂的患者可能会出现短暂的脉搏和血压升高。
•吲哚美辛：在服用吲哚美辛的患者中，BAQSIMI可能会失去升高葡萄糖的能力或可能产生低血糖症。
•华法林：BAQSIMI可能会增加华法林的抗凝血作用。
包装提供/存储和处理
BAQSIMI是一种鼻内装置，含有3毫克剂量的胰高血糖素作为不含防腐剂的白色粉末。
BAQSIMI One Pack™纸盒包含1个鼻内装置（NDC 0002-6145-11）
BAQSIMI Two Pack™纸盒包含2个鼻内装置（NDC 0002-6145-27）
在提供的收缩包装管中，在高达86°F（30°C）的温度下储存。
将BAQSIMI放在收缩包装管中，直到准备使用。 如果管已打开，BAQSIMI可能
已经暴露在潮湿环境中，可能无法正常工作。
使用后丢弃BAQSIMI和管
BAQSIMI(glucagon) Nasal Powder 3mg, the First and Only Nasally Administered Glucagon to Treat Severe Hypoglycemia in Adults and Children with Diabetes Ages Four Years and Older, Approved by FDA
U.S. Food and Drug Administration(FDA)has approved BAQSIMI™ (glucagon) nasal powder 3mg for the treatment of severe hypoglycemia in people with diabetes ages four years and above, announced today. BAQSIMI is the first and only nasally administered glucagon, and it was designed with severe hypoglycemia rescue in mind. It is compact, portable and ready to use (no reconstitution required) in a single, fixed, 3mg dose.
Clinical Overview
In adult patients, BAQSIMI had comparable efficacy to injectable glucagon. One hundred percent of pediatric patients (age 4 and above) given BAQSIMI met treatment success and 100% of pediatric patients(age 4 and above) given glucagon for injection met treatment success.
Common cold with nasal congestion did not impair absorption of BAQSIMI.
Most common(≥10%) adverse reactions associated with BAQSIMI are nausea, vomiting, headache, upper respiratory tract irritation (i.e., rhinorrhea, nasal discomfort, nasal congestion, cough, and epistaxis), watery eyes, redness of eyes, itchy nose, throat and eyes.
ABOUT BAQSIMI
BAQSIMI is a portable, dry nasal spray form of glucagon, ready to use with no reconstitution or priming required in a single, fixed 3 mg dose. It is absorbed in the nose, so does not require inhalation. BAQSIMI does not need to be refrigerated and can be stored at temperatures up to 86°F/30°C in the shrink-wrapped tube provided. BAQSIMI was studied in patients as young as age four years.
The device and protective container used for BAQSIMI are supplied by Aptar Pharma, part of AptarGroup, Inc.(Crystal Lake, Illinois).
Indications and Usage
BAQSIMI is indicated for the treatment of severe hypoglycemia in patients with diabetes ages 4 years and above.
Important Safety Information
Contraindications
BAQSIMI is contraindicated in patients with pheochromocytoma, insulinoma, and known hypersensitivity to glucagon or to any of the excipients in BAQSIMI. Allergic reactions have been reported with glucagon and include anaphylactic shock with breathing difficulties and hypotension.
Warnings and Precautions
BAQSIMI is contraindicated in patients with pheochromocytoma because glucagon may stimulate release of catecholamines from the tumor. If the patient develops a dramatic increase in blood pressure and a previously undiagnosed pheochromocytoma is suspected, 5 to 10mg of phentolamine mesylate, administered intravenously, has been shown to be effective in lowering blood pressure.
In patients with insulinoma, administration of glucagon may produce an initial increase in blood glucose; however, BAQSIMI administration may directly or indirectly (through an initial rise in blood glucose) stimulate exaggerated insulin release from an insulinoma and cause hypoglycemia. BAQSIMI is contraindicated in patients with insulinoma. If a patient develops symptoms of hypoglycemia after a dose of BAQSIMI, give glucose orally or intravenously.
Allergic reactions have been reported with glucagon, these include generalized rash, and in some cases anaphylactic shock with breathing difficulties and hypotension. BAQSIMI is contraindicated in patients with a prior hypersensitivity reaction.
BAQSIMI is effective in treating hypoglycemia only if sufficient hepatic glycogen is present. Patients in states of starvation, with adrenal insufficiency or chronic hypoglycemia may not have adequate levels of hepatic glycogen for BAQSIMI administration to be effective. Patients with these conditions should be treated with glucose.
Adverse Reactions
Most common (≥10%) adverse reactions associated with BAQSIMI are nausea, vomiting, headache, upper respiratory tract irritation (i.e., rhinorrhea, nasal discomfort, nasal congestion, cough, and epistaxis), watery eyes, redness of eyes, and itchy nose, throat and eyes.
Drug Interactions
Patients taking beta-blockers may have a transient increase in pulse and blood pressure when given BAQSIMI. In patients taking indomethacin, BAQSIMI may lose its ability to raise blood glucose or may even produce hypoglycemia. BAQSIMI may increase the anticoagulant effect of warfarin.
http://pi.lilly.com/us/baqsimi-uspi.pdf