| 简介：
部份中文替米沙坦处方资料（仅供参考）
商品名：Micardis Tablets
英文名：Telmisartan
中文名：替米沙坦
生产商：日本勃林格殷格翰公司
ミカルディス錠20mg/ミカルディス錠40mg/ミカルディス錠80mg
药用类别名称
胆汁排泄型持久性AT1受体阻滞剂
批准日期：2004年12月
商標名
Micardis Tablets 20mg
Micardis Tablets 40mg
Micardis Tablets 80mg
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)
操作注意事项
包装后, 可以吸收水分, 软化和变黄, 以避免高温和潮湿保存。
药用药理学
1. 作用机制
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。
2. 降压作用
该制剂为4天连续口服1mgkg 给肾血管性高血压大鼠, 显示低血压效果高达55mmHg, 4天连续口服给高血压大鼠0.3, 1, 3mgkg, 每次可达 23, 22, 表现为38mmHg 的降压作用。此外, 通过21天对转基因大鼠进行0.5, 1, 2mgkg的逐渐口服, 显示出分别高达33、57、72毫米汞柱的降压作用。在每一种模型中, 都没有观察到管理结束后的反弹现象。单次口服1mgg/kg 对肾血管性高血压大鼠在21小时内表现出明显的降压作用。 口服0.3mg/kg对缺钠的降压作用也有显著的降压作用, 经口服注射为, 降压作用持续7小时。此外, 对正常血压动物的降压作用较弱。该制剂与利尿剂和钙拮抗剂联合使用, 增强了该药物的降压作用。
适应症
高血压
用法与用量
成人每天口服一次40毫克作为终端苏丹。然而, 它是逐渐增加的开始给药从每天20毫克。虽然根据年龄和症状适当增加或减少, 但一天的最大剂量高达80毫克。
包装
片
20mg:140片(14片x10)PTP, 500片(10片x50) PTP, 700片(14片x50) PTP, 500片
40mg:140片(14片x10) PTP, 500片(10片x50) PTP, 700片(14片 x50) PTP, 500片
80m: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://www.info.pmda.go.jp/go/pack/2149042F1025_1_22/
Micardis Tablets 20mg（Telmisartan ミカルディス錠）
Brand name:Micardis Tablets 20mg
Active ingredient:Telmisartan
Dosage form:white to palish yellow tablet (diameter: ca. 6mm, thickness: ca. 2.5mm)
Print on wrapping:(Face) Micardis 20mg, ミカルディス 20mg, 50H (Back) ミカルディス20mg,Boehringer Ingelheim, astellas, 高血圧治療剤
Effects of this medicine
This medicine reduces blood pressure by acting on the intravascular angiotensin receptor to suppress thevasoconstrictive effect of angiotensin II, hypertensive substance.
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 two tablets (40 mg of telmisartan) at a time orally once daily, but the dose may begradually increased from one tablet (20 mg). The dosage may be adjusted according to the patient's age andseverity of symptoms, but the maximum daily dose is 4 tablets (80 mg). Strictly follow the instructions.
・This medicine is influenced by meal. If you are instructed to take this medicine before meal, you should take itbefore meal. If you are instructed to take this medicine after meal, you should take it after meal.
・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.
You should never take two doses at one time.
・If you accidentally take more than your prescribed dose, you may feel dizzy due to hypotension. Consult with yourdoctor 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.
The medicine may cause dizziness or light-headedness due to decrease in blood pressure.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include hypotension, dizziness, light-headed feeling, rash, headache,itchiness, urticaria and erythema. 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 impairment]
・dry cough, fever, difficulty breathing (shortness of breath on exertion) [interstitial pneumonia]
・lassitude, muscle pain, brown urin [rhabdomyolysis]
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 the reach of children. Store away from heat, moisture and direct sunlight.
・Discard the remainder. Do not store them.
Internal
Revised: 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. |
