FDA批准固定剂量美金刚-多奈哌齐复方制剂Namzaric-预防患老年性痴呆症 美国食品药品监督管理局(FDA)批准固定剂量复方制剂的盐酸美金刚延长释放制剂(XR)和盐酸多奈哌齐(Namzaric,阿特维斯制药 /Adamas Pharm)治疗中度到重度老年痴呆症，患者接受稳定的两种药物剂量。 美金刚XR(Namenda XR, 阿特维斯制药)是一个由N-甲基-D-天门冬氨酸抑制剂，和多奈哌齐(安理申,辉瑞)一种乙酰胆碱酯酶抑制剂(AChEI)。“在一个胶囊里Namzaric组合两个互补疗效的药剂，通常共同规定大约70%使用盐酸美金刚的患者也使用AchEI的治疗”，阿特维斯全球品牌研发部门高级副总裁大卫•尼科尔森，在一次新闻发布会上指出。盐酸美金刚XR和多奈哌齐都证实了其疗效和安全性，用于治疗中度至重度的阿尔茨海默氏症患者。此外，数据显示，盐酸美金刚XR和AchEI的联合疗法对认知上显示了较大的改善，以及全功能的改善相对于单独使用AChEI”，尼克尔森表示。 Namzaric(先前MDX-8704)目前是每日一粒服用的胶囊剂，含有美金刚胺(10毫克每日两次或28毫克XR每日一次)再加上多奈哌齐10毫克。胶囊可以打开，撒在食物上用于有吞咽困难的病人服用。 Namzaric可以采用两方面的特点:28/10毫克(美金刚/多奈哌齐)和14/10毫克(美金刚/多奈哌齐)用于有严重肾功能损害的患者。 “在对阿尔茨海默病的中度到重度的阶段病人做治疗决定时，我会考虑治疗的有效性、安全性及其易于管理的特点，”加州科斯塔梅萨ATP临床研究神经精神病学家和医学主任医学博士Gustavo Alva和加州大学志愿者教员欧文在新闻发布会上说。“FDA批准Namzaric提供新的治疗选择，这为病人提供了一个固定剂量组合的药剂，这种药剂在一个胶囊中实现了两种治疗效果”他补充道。 Namzaric (Memantine Hydrochloride Extended-release and Donepezil Hydrochloride Capsules) INDICATIONS AND USAGE NAMZARIC (memantine hydrochloride extended-release and donepezil hydrochloride) is indicated for the treatment of moderate to severe dementia of the Alzheimer’s type in patients stabilized on: •memantine hydrochloride (10 mg twice daily or 28 mg extended-release once daily) and donepezil hydrochloride 10 mg. •memantine hydrochloride (5 mg twice daily or 14 mg extended-release once daily) and donepezil hydrochloride 10 mg in patients with severe renal impairment. IMPORTANT SAFETY INFORMATION CONTRAINDICATIONS NAMZARIC is contraindicated in patients with known hypersensitivity to memantine hydrochloride, donepezil hydrochloride, piperidine derivatives, or to any excipients used in the formulation. WARNINGS AND PRECAUTIONS Anesthesia NAMZARIC is likely to exaggerate succinylcholine-type muscle relaxation during anesthesia. Cardiovascular Conditions NAMZARIC may have vagotonic effects on the sinoatrial and atrioventricular nodes manifesting as bradycardia or heart block. Bradycardia or heart block may manifest in patients both with and without known underlying cardiac conduction abnormalities. Anesthesia Peptic Ulcer Disease and Gastrointestinal Bleeding Patients treated with NAMZARIC should be monitored closely for symptoms of active or occult gastrointestinal bleeding, especially those at increased risk for developing ulcers, those with a history of ulcer disease, or those receiving concurrent nonsteroidal anti-inflammatory drugs (NSAIDs). Nausea and Vomiting NAMZARIC can cause diarrhea, nausea, and vomiting, although in most cases these effects have been mild and transient, and have resolved during continued treatment. Genitourinary Conditions NAMZARIC may cause bladder outflow obstructions. Conditions that raise urine pH may decrease the urinary elimination of memantine resulting in increased plasma levels of memantine. Seizures Cholinomimetics, including donepezil hydrochloride, are believed to have some potential to cause generalized convulsions. However, seizure activity also may be a manifestation of Alzheimer’s disease. Pulmonary Conditions Cholinesterase inhibitors should be prescribed with care to patients with a history of asthma or obstructive pulmonary disease. ADVERSE REACTIONS •The most common adverse reactions, occurring at a frequency of at least 5% in patients taking memantine hydrochloride extended-release 28 mg/day, and greater than placebo, were headache (6% vs 5%), diarrhea (5% vs 4%), and dizziness (5% vs 1%). •The most common adverse reactions, occurring at a frequency of at least 5% in patients taking donepezil, and at twice or more the rate of placebo, include diarrhea (10% vs 4%), anorexia (8% vs 4%), vomiting (8% vs 4%), nausea (6% vs 2%), and ecchymosis (5% vs 2%). DRUG INTERACTIONS •Alterations of urine pH toward the alkaline condition may lead to an accumulation of memantine with a possible increase in adverse reactions. NAMZARIC should be used with caution under conditions that may be associated with increased urine pH including alterations by diet and the clinical state of the patient. •The combined use of memantine hydrochloride with other NMDA antagonists (amantadine, ketamine, and dextromethorphan) has not been systematically evaluated and such use should be approached with caution. •Inhibitors of CYP450, 3A4 (e.g., ketoconazole) and 2D6 (e.g., quinidine), inhibit donepezil metabolism in vitro. Whether there is a clinical effect of quinidine is not known. •Inducers of CYP3A4 (e.g., phenytoin, carbamazepine, dexamethasone, rifampin, and phenobarbital) could increase the rate of elimination of donepezil. •Cholinesterase inhibitors, including donepezil hydrochloride, have the potential to interfere with the activity of anticholinergic medications. DOSAGE AND ADMINISTRATION •Patients on memantine hydrochloride (10 mg twice daily or 28 mg extended-release once daily) and donepezil hydrochloride 10 mg can be switched to NAMZARIC 28 mg/10 mg, taken once a day in the evening •Severe renal impairment: patients on memantine hydrochloride (5 mg twice daily or 14mg extended-release once daily) and donepezil hydrochloride 10 mg can be switched to NAMZARIC 14mg/10mg