Namzaric每日用药一次的胶囊，获FDA批准为首个固定剂量复方药Namzaric(TM)（以前称 MDX-8704），用于治疗稳定的阿尔茨海默病型中重度痴呆
2014年12月24日，全球仿制药巨头阿特维斯（Actavis）与合作伙伴Adamas制药公司近日宣布，复方新药Namzaric已获FDA批准用于正接受盐酸美金刚和盐酸多奈哌齐治疗且病情稳定的中度至重度阿尔茨海默氏型老年性痴呆（Alzheimer's type dementia）的治疗。
Namzaric是一种每日一次的口服胶囊，由固定剂量美金刚和多奈哌齐（memantine ER/donepezil）组成，适用于目前正在服用美金刚（10mg每日2次；或28mg缓释片每日1次）和多奈哌齐（10mg）的患者。此外，该胶囊可以被打开，将内容物撒在食物上，以方便可能有吞咽困难的患者。
美金刚（memantine）和多奈哌齐（donepezil）联合用药，是用于中度至重度阿尔茨海默氏型老年性痴呆患者的一套行之有效的治疗方案。Namzaric（缓释美金刚ER/多奈哌齐），有助于帮助减轻患者日常用药的负担，并改善患者的依从性和合规性（compliance，即遵医行为）。
Namzaric包括2种剂量，28mg/10mg和14mg/10mg，后者可用于有严重肾功能损害的患者。目前，美金刚缓释（memantine ER）胶囊已以品牌名NAMENDA XR上市销售，适用于中度至重度阿尔茨海默型老年痴呆的治疗。多奈哌齐品牌名为ARICEPT，适用于轻度至重度阿尔茨海默型老年痴呆的治疗。
如何提供
14毫克/10毫克：浅绿色，不透明胶囊采用了黑色“FL14/10”放射状的印记。
一瓶30：NDC  0456-1214-30
一瓶90：NDC  0456-1214-90
28毫克/10毫克：蓝色，不透明胶囊采用了黑色“FL28/10”放射状的印记。
一瓶30：NDC  0456-1228-30
一瓶90：NDC  0456-1228-90
存储和处理
商店在25°C（77°F）;15°C和30°C（59°F和86°F）

NAMZARIC（DONEPEZIL HYDROCHLORIDE; MEMANTINE HYDROCHLORIDE）CAPSULE, EXTENDED RELEASE;ORAL
General Information
Namzaric is a fixed-dose combination of memantine hydrochloride extended-release, a NMDA receptor antagonist, and donepezil hydrochloride, an acetylcholinesterase inhibitor.
Namzaric is specifically indicated for the treatment of moderate to severe dementia of the Alzheimer's type in patients stabilized on memantine hydrochloride and donepezil hydrochloride.
Namzaric is supplied as a capsule for once daily oral administration. The capsules can also be opened to allow the contents to be sprinkled on food to facilitate dosing for patients who may have difficulty swallowing.
Clinical Results
FDA Approval
The FDA approval of Namzaric was based on the results of a randomized, double-blind, placebo-controlled trial of 677 outpatients on a stable dose of acetylcholinesterase inhibitors (AChEIs). The clinical study was not conducted with Namazaric; however, bioequivalence of Namazaric with coadministered memantine HCl extended release and donepezil HCl was demonstrated. Approximately 68% of the patients randomized to receive either memantine HCl extended release 28 mg or placebo were taking donepezil as the AchEI at Baseline and throughout the study. The results demonstrated statistically significant improvement in cognition and global function for patients treated with Namenda XR 28 mg plus an AChEI compared to placebo plus an AChEI.
Side Effects
Adverse effects associated with the use of Namzaric may include, but are not limited to, the following:
•headache
•diarrhea
•dizziness
Mechanism of Action
Namzaric is a fixed-dose combination of memantine hydrochloride extended-release, a NMDA receptor antagonist, and donepezil hydrochloride, an acetylcholinesterase inhibitor.
NAMZARIC Rx
Pharmacological Class:
N-methyl-D-aspartate (NMDA) receptor antagonist + acetylcholinesterase inhibitor.

Active Ingredient(s):
Memantine HCl extended-release, donepezil HCl; 14mg/10mg, 28mg/10mg; capsules.

Company
Actavis
Indication(s):
Moderate-to-severe dementia of the Alzheimer's type in patients stabilized on memantine HCl and donepezil HCl.

Pharmacology:
Memantine is postulated to exert its therapeutic effect through its action as a low-to-moderate affinity uncompetitive (open channel) NMDA receptor antagonist which binds preferentially to the NMDA ­receptor-operated cation channels. Donepezil is postulated to exert its therapeutic effect by enhancing cholinergic function. This is achieved by increasing the concentration of acetylcholine in the central nervous system through reversible inhibition of its hydrolysis by acetylcholinesterase.

Clinical Trials:
The efficacy of Namzaric as treatment for moderate to severe Alzheimer's disease was shown by its bioequivalence with co-administered memantine HCl ext-rel and donepezil HCl.

The efficacy of memantine HCl ext-rel was evaluated in a randomized, double-blind clinical study (n=677) in patients receiving acetylcholinesterase inhibitor (AChEI) therapy for 3 months prior to screening. Co-primary efficacy parameters of Severe Impairment Battery (SIB) and the Clinician's Interview-Based Impression of Change (CIBIC-Plus) were used. Patients were randomized to memantine HCl ext-rel 28mg/day or placebo, while receiving an AChEI (either donepezil, galantamine, or riva­stigmine). At 24 weeks of treatment, the mean difference in the SIB change scores was 2.6 units and the CIBIC-Plus was 0.3 units for memantine HCl ext-rel vs. placebo. Using an LOCF analysis, memantine HCl ext-rel + AChEI was statistically significantly superior to placebo + AChEI.

The efficacy of donepezil HCl was evaluated in a randomized, double-blind, placebo-controlled study (n=248) in patients with severe Alzheimer's disease. A dual outcome assessment strategy evaluated cognitive function using an instrument designed for more impaired patients and overall function through caregiver-rated assessment. At 6 weeks of treatment, the mean difference in the SIB change scores was 5.9 points and the ADCS-ADL-severe change scores was 1.8 points for donepezil HCl treated patients vs. placebo. Donepezil HCl treatment was statistically significantly superior to placebo.

For more clinical trial data, see full labeling.

Legal Classification:
Rx

Adults:
Start the day after last dose of memantine HCl and donepezil HCl given separately. Swallow whole or may open caps and sprinkle on applesauce, then consume entire contents; do not divide doses. Previously stabilized on both components: 28mg/10mg once daily in the evening. Severe renal impairment (CrCl 5–29mL/min): 14mg/10mg once daily.

Children:
Not established.

Warnings/Precautions:
Cardiac conduction abnormalities. Peptic ulcer. Monitor for GI bleeding. GU obstruction. Alkalinized urine (eg, renal tubular acidosis, severe UTI) increases memantine levels. Seizures. Asthma or COPD. Severe hepatic impairment. Pregnancy (Category C). Nursing mothers.

Interaction(s)
Caution with other NMDA antagonists (eg, amanta­dine, ketamine, dextromethor­phan). Memantine plasma levels may be increased by urinary alkalinizers. Donepezil potentiated by CYP3A4 (eg, ketoconazole) and CYP2D6 (eg, quinidine) inhibitors. CYP3A4 inducers (eg, phenytoin, carbamazepine, dexamethasone, rifampin, phenobarbital) may increase the rate of elimination of donepezil. Antagonizes anticholinergics. May potentiate succinylcholine-type muscle relaxants, other cholinesterase inhibitors, cholinergic agonists (eg, bethanechol). Concomitant NSAIDs may increase risk of GI bleed.

Adverse Reaction(s)
Headache, diarrhea, dizziness, anorexia, vomiting, nausea, ecchymosis.

How Supplied:
Caps—30, 90

LAST UPDATED:
7/31/2015