| 简介：
部份中文替米沙坦/苯磺酸氨氯地平/氢氯噻嗪处方资料（仅供参考）
商品名：Micatrio
英文名：Telmisartan/Amlodipine Besilate/Hydrochlorothiazide
中文名：替米沙坦/苯磺酸氨氯地平/氢氯噻嗪
生产商：日本勃林格殷格翰公司
ミカトリオ配合錠
药用类别名称
胆汁排泄持久性AT1受体阻滞剂/持久性钙拮抗剂/利尿剂混合物
批准日期：2016年9月
商標名
Micatrio Combination Tablets
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
分子式
C33H30N4O2
分子量
514.62
性状
白色至淡黄色结晶性粉末。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
日志 P = 3.2 (N-octanol/Ph-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
分子式
C20H25ClN2O5・C6H6O3S
分子量
567.05
性状
是一种白色带淡黄色的结晶性粉末。 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)
一般名
ヒドロクロロチアジド（Hydrochlorothiazide）
化学名
6-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
化学構造式
分子式
C7H8ClN3O4S2
分子量
297.74
性状
白色的水晶或结晶性粉末, 没有气味, 味道略带苦味。易溶于丙酮, 不易溶于乙腈, 极不溶于水或乙醇 (95), 不易溶于乙醚。它融化成氢氧化钠测试溶液。
熔点
约 267°c (分解)
操作注意事项
打开铝制枕头后, 避免潮湿并保存。
由于包装后可以吸收水分, 降低含量, 因此可以通过避免高温和高湿来屏蔽来保存。
批准条件
制定药品风险管理计划并加以实施。
药用药理学
1. 作用机制
作为维特斯苏丹, 有以下报道。
血管紧张素II. 1型(AT1)受体是一种生理助推器(A-II), 通过抑制血管收缩作用来表达降压作用。AT1受体亲和力高(Ki=3.7nM), 不容易与AT1受体分离。在浓度范围为10 ~1000nM的情况下, 用A-II对切除兔主动脉标本的血管收缩反应曲线进行抑制, 以抑制最大收缩40~ 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, 该行动是持续的。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。
作为氢氯噻嗪, 有以下报告。
它是噻嗪系统的利尿剂, 显示了抗高血压和利尿的作用。利尿作用是基于抑制Na+-c-共输从肾远端曲率的小管, Na+从肾脏,c-, 由水的排泄增加。 低血压作用由早期循环血量的减少引起, 据说是由外周血管的长期扩张引起的。
2. 降压作用
(1)在Rousal、1mgkg T利米沙坦和5mg kg氨氯地平下使用男性高血压自发性大鼠 (SHR), 每天给药一次, 测量血压在一段时间内持续5天, 1mgg终止苏丹和5mg/mmal KG氨氯地平, 单给药平均血压降低约25mmHg, 表现出明显相同的降压作用。 然后, 测量1mg kg 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)。
(2)使用觉醒下的男性SHR, 对3mgkg终点的降压作用进行了检查, 将水硫酰胺或两个10mgg 公斤的水氯噻嗪口服5天。因此, 仅心灵素口服的在第5天的给药显示出最大的降压作用为36mmHg。虽然在单次给药中没有观察到明显的降压作用, 但与身来苏丹联合, 明显增强了端粒磺胺的作用, 最大降压作用为530亿汞柱。
3.利尿作用
用男性SHR在唤醒下, 检查后的利尿作用, 当h、氢氯噻嗪或两个10的终点连续5天口服。 因此, 通过单次给药的的苏丹末端, 观察到尿量和尿电解质浓度(Na +、K+和c-) 的显著变化。另一方面, 单次给药液氯噻嗪为10mg/kg, 观察到尿量、Na +、K + 和氯表观的电解质浓度增加。即使与替米沙坦联合使用, 观察到氢氯噻嗪的利尿活性, 底虫磺胺对氢氯噻嗪的利尿作用影响不大。
适应症
高血压
用法与用量
作为一般规则, 当替米沙坦80mg, 氨氯地平5mg和氢氯噻嗪12.5毫克连续使用相同的使用和剂量在一定时期内, 当获得稳定的血压控制, 切换到该剂考虑。
包装
配合錠：
100片(10片x10), ptp, 140片 (14片x10)
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://www.info.pmda.go.jp/go/pack/2149122F1026_1_02/
Micatrio Combination Tablets（Telmisartan/Amlodipine Besilate/Hydrochlorothiazide ミカトリオ配合錠）
Brand name:Micatrio Combination Tablets
Active ingredient:Telmisartan
Amlodipine besilate
Hydrochlorothiazide
Dosage form:pale orange tablet, diameter: approx. 11 mm, thickness: approx. 4.9
mm Print on wrapping:(Face) Micatrio 配合錠, テルミサルタン 80mg, アムロジピン5mg, ヒドロクロロチアジド 12.5mg, ミカトリオ, C8 (Back) ミカトリオ
配合錠, Boehringer Ingelheim, astellas, テルミサルタン 80mg, アムロジピン 5mg, ヒドロクロロチアジド 12.5mg, 高血圧治療剤
Effects of this medicine
This is a combination drug of an angiotensin receptor blocker (ARB), a calcium channel blocker and thiazide diuretic;the ARB inhibits vasoconstriction caused by angiotensin II in vascular smooth muscle to lower blood pressure, thecalcium blocker decreases Ca2+sup/supinflow into the cell and relaxes the vascular smooth muscle to lower blood pressure, and the diuretic increases urine output via inhibition of sodium and water reabsorption in the kidney tolower blood pressure.
It is usually used to treat 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 hepatic disorder, anuria, acute renal failure, reduction of sodium/potassium in body fluid or diabetesmellitus.
If you are on dialysis.
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, once daily. Strictly follow the instructions.
To avoid possible effects of food, always take the drug at regular dosing schedule, that is, before every meal or afterevery meal.
If you miss a dose, skip the missed dose and follow your regular dosing schedule. You should never take two dosesat one time.
If you accidentally take more than your prescribed dose, you may feel dizzy due to hypotension. Consult with yourdoctor or pharmacist immediately.
Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
The medicine may cause a decrease in blood pressure, dizziness and light headedness. Pay close attention when youwork at heights or perform dangerous operations such as driving a car.
Pay attention that alcohol enhances postural hypotension (dizziness on standing up).
Avoid taking grapefruit juice with this medicine, since it may intensify the effects of this medicine.
Possible adverse reactions to this medicine The most commonly reported adverse reactions include hypotension, postural hypotension (dizziness on standingup), vasculitis, facial flush, respiratory distress, gum hypertrophy, eczema, rash, itchiness, hives, erythema,erythema multiform and solar sensitiveness. 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 eyelids/lips/tongue/throat, respiratory distress, blood pressure falling [angioedema]
numbness of the hands and lips, muscle weakness, paralysis of limbs [hyperkalaemia]
loss of appetite, nausea/vomiting, convulsion [hyponatraemia]
decreased urine output, edema, general malaise [renal dysfunction]
cold feeling, vomiting, loss of consciousness [shock, syncope, loss of consciousness]The above symptoms do not describe all the adverse reactions to this medicine. Consult with your
doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
Keep out of reach of children. Store away from direct sunlight, heat and moisture. Store in a light shielding conditionafter opening a package.
Discard the remainder. Do not store them. Seek advice of your pharmacy or medical institution about properdisposal of the unused medicines.
Internal
Published: 11/2016
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. |
