部份中文替米沙坦/苯磺酸氨氯地平处方资料（仅供参考）
商品名：Micamlo Combination
英文名：Telmisartan/Amlodipine Besilate
中文名：替米沙坦/苯磺酸氨氯地平
生产商：日本勃林格殷格翰公司
药品介绍
安斯泰来(Astellas)宣布，降压药Micamlo片获日本卫生劳动福利部（MHLW）批准。该药是首个高剂量血管紧张素II-1型受体阻断剂（ARB）替米沙坦（telmisartan，80mg）和长效钙通道阻滞剂（CCB）氨氯地平（amlodipine，5mg）的组合药物，具有强大的降压作用，持续时间可达24h。
ミカムロ配合錠AP／ミカムロ配合錠BP
药用类别名称
胆汁排泄型持久性AT1受体阻滞剂/持久性钙拮抗剂混合物
批准日期：
商標名
Micamlo Combination Tablets AP
Micamlo Combination Tablets BP
一般名
テルミサルタン（JAN）
Telmisartan（JAN，INN）
化学名
4’-{[4-Methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazol-1-yl]methyl}biphenyl-2-carboxylic acid
化学構造式
raster
分子式
C33H30N4O2
分子量
514.62
性状
它是一种白色到小黄色的结晶粉末。
易溶于甲酸, 不易溶于甲醇, 很易溶于乙醇 (99.5), 不易溶于水。
多态性被观察。
熔点
269°c
分布系数
LogP = 3.2 (正辛醇/ph 7.4 磷酸盐缓冲液)
一般名
アムロジピンベシル酸塩（Amlodipine Besilate）
化学名
3-Ethyl 5-methyl(4RS)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate monobenzenesulfonate
化学構造式
raster
分子式
C20H25ClN2O5・C6H6O3S
分子量
567.05
性状
它是一种白色带淡黄色的结晶粉末。
甲醇易溶, 不易溶于乙醇 (99.5), 难以溶于水。
甲醇溶液 (1→100) 不显示光学旋转。
熔点
约 198°c (分解)
操作注意事项
由于包装后吸湿可能会使其软化, 因此应加以保存, 以避免高温和高湿。
药用药理学
1. 作用机制
作为维特斯苏丹, 有以下报道。
本剂主要是血管紧张素II. 1型(AT1) 受体, 血管紧张素II是一种生理助推器(A-II), 特别是拮抗剂, 通过抑制血管收缩作用来表达降压作用。AT1受体亲和力较高(Ki = 3.7nM), 不容易与 AT1 受体分离。该制剂在浓度范围为10~1000nM 时, 采用A-II对切除兔主动脉标本的血管收缩反应曲线, 以抑制最大收缩40至50%, 并将浓度相关的方式向右移动。也显示出一个显着的血管收缩抑制, 即使在标本洗涤120分钟后, 该作用是持续的。此外, 它不直接影响ACE(激酶II)是一种缓激肽降解酶。
作为苯甲酸氨氯地平酸盐, 下面有一个报告。
具体结合膜电位依赖性细胞膜的钙通道, 通过减少钙流入细胞, 放松冠状动脉和外周血管的平滑肌。钙拮抗的表达缓慢, 是持续的。此外, 心脏抑制效果较弱, 血管选择性被观察。
2. 降压作用
对于替米沙坦或氨氯地平单独或结合使用的效果, 以下报告。
使用男性Shr在Arousal下, 每天给1mg/kg T何时何地使用, 每天服用一次, 在压力下测量超过5天的血压, 1mg kg telmisartan和5mg kg氨氯地平, 单次给药平均血压降低约25毫米汞柱, 血压降低效果基本相同。然后, 测量1mgkg替米沙坦, 每天5天口服一次, 结合5mg/kg氨氯地平, 随着时间的推移血压。与单次给药降血压 (降低约25毫米汞柱) 相比, 对端叶磺胺和氨氯地平同时给药对血压的影响, 观察到显著的降压作用(降低约50mmHg)。
适应症
高血压
用法与用量
成人1片每天一次(40mgsp/或80mgsg)口服为末端Sultans氨氯地平。这种药物不作为高血压治疗的首选药物。
包装
配合錠AP: 100 片(10片x10) PTP, 500片(10片x50) PTP, 700片(14片x50) PTP, 500片
配合錠BP: 100 片(10片x10) PTP
制造和销售
日本勃林格殷格翰公司
销售
安斯泰来制药公司
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整资料附件：http://bij-kusuri.jp/medicine_data/mca_t/mca_t_tenpu.htm
Micamlo Combination Tablets AP（Telmisartan/Amlodipine Besilate ミカムロ配合錠AP）
Brand name:Micamlo Combination Tablets AP
Active ingredient:Telmisartan
Amlodipine besilate
Dosage form:pale red tablets (diameter: ca. 8.5mm, thickness: ca. 4.0mm)
Print on wrapping:(Face) Micamlo 配合錠 AP, テルミサルタン 40mg アムロジピン 5mg,ミカムロ AP, A1 (Back) ミカムロ配合錠 AP, Boehringer Ingelheim,astellas, テルミサルタン 40mg アムロジピン 5mg, 高血圧治療剤
Effects of this medicine
Micamlo is a combination drug of an angiotensin receptor blocker (ARB) and calcium blocker: the ARB inhibits
vasoconstriction caused by angiotensin II in vascular smooth muscle to lower blood pressure and the calcium blockerdecreases Ca2+ inflow into the cell and relaxes the vascular smooth muscle to lower blood pressure.
Usually, this medicine is used in the treatment of hypertension.
Before using this medicine, be sure to tell your doctor and pharmacist
If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
If you have a hepatic disorder, poor bile secretion or diabetes mellitus.
If you are pregnant, possibly pregnant or breastfeeding.
If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinaleffects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
Your dosing schedule prescribed by your doctor is<< to be written by a healthcare professional>>In general, for adults, take 1 tablet at a time, once daily. Strictly follow the instructions.
For patients taking the medicine before meals, if you miss a dose, take as soon as possible. If it is almost time for thenext dose, skip the missed dose and continue your regular dosing schedule.
For patients taking the medicine after meals, if you miss a dose, take as soon as possible after taking a snack. Youshould never take two doses at one time.
If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
Use caution when driving, operating machinery, working at high places or engaging in other hazardous activities.
This medicine may cause dizziness or light-headedness due to decrease in blood pressure.
Do not take grapefruit juice and the medicine together as it may intensify the effect of the medicine.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include dizziness, eczema and rash. If any of these symptoms occur,consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicatedin brackets. If any of these symptoms occur, stop taking this medicine and see your doctorimmediately.
・swelling of the eyelids, lips, tongue, or throat; breathing difficulty, decrease in blood pressure [angioedema,anaphylaxis]
・numbness of the hands and lips, muscle weakness, paralysis of limbs [hyperkalemia]
・cold sensation, vomiting, faint [shock, syncope, loss of consciousness]
・lassitude, hunger, cold sweat [hypoglycemia]
・a decrease in urine volume, edema, general fatigue [renal dysfunction]
・dry cough, fever, difficulty breathing (shortness of breath on exertion) [interstitial pneumonia]
・lassitude, muscle pain, brown urin [rhabdomyolysis]
・bradycardia, dizziness [atrioventricular block]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with yourdoctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other informationKeep out of the reach of children. Store away from heat, moisture and direct sunlight.
Discard unused medicine. Ask the pharmacy or medical institutions how to discard.
04/2014
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approvaldetails may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It isimportant to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response,
patients should understand their medication and cooperate with the treatment.