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中文药名: Exubera(Insulin Human [rDNA origin]-Insulin for Inhalation) 中文药名: 人胰岛素[rDNA源]-吸入用胰岛素 生产厂家: Pfizer Inc. 美国食品与药物管理局（FDA）批准了第一种吸入型胰岛素（Exubera）上市，用于治疗患1型和2型糖尿病的成年患者。FDA称，自19世纪20年代发现胰岛素以来，还是首次采用这种新的胰岛素给药方式——重组人胰岛素（rDNA）吸入粉剂。 FDA建议患者在接受吸入型胰岛素治疗之前应先进行肺功能检查，并在以后的每6至12个月检查一次。 这种新的治疗方式是由辉瑞、赛诺菲-安万特和Nektar制药公司共同努力，经过10年的研究后发明的。本月初辉瑞公司购买了赛诺菲-安万特公司的Exubera使用权。 “在此之前，需要胰岛素治疗的糖尿病患者都只有一种可以选择的治疗方式，” FDA药物审查及研究中心负责人Steven Galson, MD在新的发言中表示，“我们希望吸入型胰岛素的上市可以给患者提供更多的选择以更好地控制血糖。” 吸入型胰岛素地给药装置比治疗哮喘地吸入器大。经过折叠以后体积接近于一个标准的手电筒大小。从装置的体部可以伸出一个可回缩的吸入管，吸入管展开后可以从胸部延伸到口里。在装置启动之前必须先装入泡包装的胰岛素。就Exubera的使用还将对患者和医生进行大量培训。 吸入型胰岛素并不是唯一一种研究中的备选胰岛素剂型。其他的还有胰岛素口喷雾剂、胰岛素贴剂甚至口服剂型的胰岛素。其他制药公司也在加速研制自己的吸入型胰岛素——尤其以Eli Lilly & Co和Alkermes公司合作的研究进展最快。 *对肺安全性的考虑 FDA是在专家咨询小组以7:2的投票结果得出推荐药物的结论后批准药物上市的。咨询小组（投票结果为5:4）还号召对Exubera进行进一步研究考察药物在有潜在肺脏疾病患者中的安全性。 Drug Information for EXUBERA (insulin human [rDNA origin]) Inhalation PowderEXUBERA Inhaler (Pfizer Inc.): DESCRIPTION
EXUBERA® consists of blisters containing human insulin inhalation powder, which are administered using the EXUBERA® Inhaler. EXUBERA blisters contain human insulin produced by recombinant DNA technology utilizing a non-pathogenic laboratory strain of Escherichia coli (K12). Chemically, human insulin has the empirical formula C257H383N65O77S6 and a molecular weight of 5808. Human insulin has the following primary amino acid sequence: EXUBERA(insulin human [rDNA origin]) Inhalation Powder is a white to off-white powder in a unit dose blister (fill mass, see Table 1). Each unit dose blister of EXUBERA contains a 1 mg or 3 mg dose of insulin (see Table 1) in a homogeneous powder formulation containing sodium citrate (dihydrate), mannitol, glycine, and sodium hydroxide. After an EXUBERA blister is inserted into the inhaler, the patient pumps the handle of the inhaler and then presses a button, causing the blister to be pierced. The insulin inhalation powder is then dispersed into the chamber, allowing the patient to inhale the aerosolized powder. Under standardized in vitro test conditions, EXUBERA delivers a specific emitted dose of insulin from the mouthpiece of the inhaler (see Table 1). A fraction of the total particle mass is emitted as fine particles capable of reaching the deep lung. Up to 45% of the 1 mg blister contents, and up to 25% of the 3 mg blister contents, may be retained in the blister. Used For Directions The insulin from Exubera blisters is inhaled into the lungs using the insulin inhaler and is absorbed into the bloodstream through the alveoli in the lungs. It then works in the same way as natural insulin, by binding to insulin receptors on cells in the body. Insulin causes cells in the liver, muscle and fat tissue to increase their uptake of glucose from the bloodstream. It also decreases the production of glucose by the liver, and has various other effects that lower the amount of glucose in the blood. People with type one diabetes will usually still need to use intermediate or longer-acting insulin injections in combination with Exubera. These help control blood glucose levels throughout the day, while the Exubera controls peaks of blood glucose after each meal. People with type two diabetes may use Exubera in combination with their antidiabetic tablets to improve their blood sugar control. Some people with type two diabetes will also still need to use intermediate or longer-acting insulin injections. How It Works People with diabetes have a deficiency or absence of a hormone manufactured by the pancreas called insulin. Insulin is the main hormone responsible for the control of sugar (glucose) in the blood. All people with type one diabetes and some people with type two diabetes need to take insulin to control the amount of glucose in their bloodstream. This acts as a replacement for the deficiency in natural insulin and helps people with diabetes to achieve normal blood glucose levels. When the insulin from Exubera is inhaled into the lungs, it starts to reduce blood sugar rapidly, within 10 to 20 minutes. Its effects last for around six hours. It should be inhaled 10 minutes before a meal to control increasing blood glucose levels after eating. Side Effects The safety of EXUBERA alone, or in combination with subcutaneous insulin or oral agents, has been evaluated in approximately 2500 adult patients with type 1 or type 2 diabetes who were exposed to EXUBERA. Approximately 2000 patients were exposed to EXUBERA for greater than 6 months and more than 800 patients were exposed for more than 2 years. Known side effects are: Low blood sugar levels (hypoglycaemia) Cough Shortness of breath Throat irritation Dry throat Nosebleeds Inflammation of the throat (pharyngitis) Wheezing Breathing difficulties due to a narrowing of the airways (bronchospasm) Alteration in your voice Pain at the back of the throat Dry mouth Tonsil disorder Chest pain Decline in lung function (usually reversible on stopping treatment) Allergy to active ingredients (hypersensitivity) Other Info It is important to monitor your blood glucose regularly and adjust your insulin dose as required. Your doctor or diabetic team will explain how to do this. Keeping your blood glucose level as close to normal as possible, and not too high or too low, significantly reduces the risk of developing late-stage diabetic complications. People with low body weight, as Exubera may not come in a low enough dose People over 75 years of age Heart failure (Exubera is not recommended for people who have breathing difficulties due to heart failure). Not to be used in Low blood sugar levels (hypoglycaemia) People who smoke or have smoked in the last six months Poorly controlled, unstable or severe asthma Severe (GOLD stage III or IV) chronic obstructive pulmonary disease (COPD) Exubera is also not recommended for people with any other kind of lung disease, for example, less severe asthma or COPD. It has not been studied in people with pneumonia. Exubera is not recommended for children and adolescents under 18 years of age, as the long-term safety of inhaled insulin has not been studied in this age group.
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