奥美沙坦酯(Olmesartan Medoxomi I)由日本Sankyo(三共公司)和美国Forestaboratories开发，2002年5月以商品名Benicar在美国上市，同年8月在德国获批准并在10月初上市。
奥美沙坦疗效优于洛沙坦等较早上市的沙坦类药物，为一种较理想的抗高I血压药物，对各型高压均有较好疗效，其突出特点是半衰期较长，可以在一天内有效控制血压，因此服用较为方便。同时与其它的血管紧张素 II受体拮抗剂类药物相比。具有剂量小、起效快、降压作用更强而持久、不良反应的发生率低等明显优点。临床研究表明：奥美沙坦酯还可以与其它的降压药同时服用以达到更理想的治疗效果。此外，奥美沙坦对动脉硬化、心肌肥厚、心力衰竭、糖尿病、肾病等均具有较好作用。
药品英文名
Olmesartan Medoxomil
药品别名
Benicar、Olmetec
【药品特性】
1.强效：降压幅度更大，达标率更高
2.快速：二周达最大疗效
3.独特：双链结构和反向激动机制, 保证更出色的降压, 达标率更高
4.放心：药物相互作用少, 使用患者群广，不经P450代谢，肝、肾双通道排泄
傲坦 （奥美沙坦酯）作为最新的 ARB, 于 2002 年 5 月在美国率先上市。目前 , 其美国市场的处方量已升至ARB类药物的第 3位 , 仅次于缬沙坦和氯沙坦。
药理作用
本药为非肽类血管紧张素Ⅱ(AngⅡ)受体(AT1型)阻滞药。与血管紧张素转换酶抑制药(ACEI)相比，本药不引起ACEI所致的干咳、皮疹和血管神经性水肿等，不良反应小，具有强而持久的降压作用。AngⅡ为肾素-血管紧张素-醛固酮系统中重要的物质，有收缩血管、刺激醛固酮合成，激动心脏、促进肾脏对钠的再吸收等功能。本药通过选择性阻断AugⅡ与血管平滑肌AT1受体结合，从而拮抗AngⅡ的作用，抑制肾素分泌的负反馈调节，导致血浆肾素活性升高和循环AngⅡ浓度升高，但这对本药的降压效果无明显影响。
药动学
本药口服后1周开始起效，最大降压效应的时间为2～4周。单次或多次用药，持续时间均约24h。健康受试者一次口服本药20mg、40mg、80mg后，血药浓度达峰时间为1.4～2.8h，峰浓度分别为450ng/ml、725ng/ml、1200ng/ml，谷浓度分别为19ng/ml、35ng/ml、62ng/ml，平均曲线下面积(AUC)分别为2613(ng·h)/ml、4229(ng·h)/ml、9330(ng·h)/ml。健康受试者静脉注射2mg、4mg、8mg、16mg后，血药浓度达峰时间为10min，峰浓度分别为543ng/ml、1092ng/ml、2078ng/ml、4829ng/ml。静脉给药4mg、8mg后，AUC分别为2906(ng·h)/ml、5370(ng·h)/ml。本药口服生物利用度为26%，进食不影响生物利用度。动物研究资料表明，少量药物可通过血-脑脊液屏障和胎盘。分布容积为17L。总蛋白结合率为99%。药物主要通过肠壁代谢，其代谢产物为有活性的脱酯奥美沙坦。口服后，肾脏清除率为0.5～0.8L/h，排泄率为35%～50%，胆汁排泄率为50%～65%，半衰期为12～18h。静脉给药1～32mg后，肾脏清除率为0.5～0.6L/h，排泄率为35%～49%，半衰期为8～13h。
适应证
用于高血压。
禁忌证
1.对本药过敏者。
2.孕妇。
注意事项
1.慎用：
(1)对ACEI、阿司匹林和(或)青霉素过敏者。
(2)有发生血管性水肿的危险的患者。
(3)有因喉部喘鸣，面部、舌部或声门血管性水肿而停药的病史者。
(4)主动脉或二尖瓣狭窄、肥大性心肌病、左心室流出通道阻塞的患者。
(5)肾损害(单肾或双肾动脉狭窄)、肝损害(胆汁性肝硬化或胆道阻塞)患者。
(6)糖尿病患者。
(7)同时使用保钾利尿药或补钾药的患者。
2.药物对儿童的影响：尚无18岁以下患者用药的研究资料，不推荐使用。
3.药物对妊娠的影响：妊娠中、晚期用药，可造成胎儿(或新生儿)损伤(如血压降低、高血钾，新生儿贫血、颅骨发育不全、无尿和肾衰竭等)或死亡。美国药品和食品管理局(FDA)对本药的妊娠安全性分级为C级(妊娠早期)和D级(妊娠中、晚期)。
4.药物对哺乳的影响：动物试验表明，本药可少量经乳汁分泌。尚不清楚是否经人乳分泌。
5.需全身麻醉的外科手术、导致血压降低的药可能阻断继发于代偿性肾素释放的AngⅡ的形成。
6.心力衰竭、低钠血症、近期加强利尿(增加利尿药用量)、肾透析、严重血容量或钠盐摄入不足的患者，可致血压过低的危险性增加。
7.如患者存在血容量或钠盐摄入不足，可降低初始用量。
不良反应
1.心血管系统：可见心律减慢(轻微)。未观察到严重血压下降(按一日80mg给药)。
2.中枢神经系统：可见头晕、头痛。
3.代谢/内分泌系统：可见血糖、三酰甘油升高。
4.呼吸系统：可见支气管炎、咽炎、鼻窦炎、上呼吸道感染，包括流感样症状。
5.肌肉骨骼系统：可见肌酸磷酸激酶(CPK)升高。有报道可出现肌痛、骨骼痛，尤其是背部疼痛或僵直。
6.泌尿生殖系统：可见血尿。
7.肝脏：少见氨基转移酶升高(尚不确定是否由本药引起)。
用法用量
成人常规剂量：口服给药初始用量，一次20mg，一日1次，共2周。一般用量，一次20～40mg，一日1次。最大用量，一次40mg，一日1次。肾功能不全时剂量：无需调整剂量。肝功能不全时剂量：无需调整剂量。
药物相应作用
1.与甘草合用，可降低AngⅡ受体拮抗药的疗效，可能的机制是甘草可引起高盐皮质激素效应。2.与麻黄合用，可降低AngⅡ受体拮抗药的疗效，可能的机制是麻黄中麻黄碱和伪麻黄碱的拟交感活性可产生拮抗作用。
3.与育亨宾合用，可降低AngⅡ受体拮抗药的疗效，可能的机制是育亨宾可增加去甲肾上腺素的释放。
4.与抗酸药合用，本药的生物利用度未发生显著改变。
5.与地高辛、华法林合用，尚未出现明显相互作用的报道。

Generic Name: olmesartan (OL me SAR tan)
Brand Names: Benicar
What is Benicar?
Benicar (olmesartan) is in a group of drugs called angiotensin II receptor antagonists.
Benicar keeps blood vessels from narrowing, which lowers blood pressure and improves blood flow.
Benicar is used to treat high blood pressure (hypertension) inadults and children who are at least 6 years old. It is sometimes given together with other blood pressure medications.
Benicar may also be used for other purposes not listed in this medication guide.
---------------------------------------------------
Important information about Benicar
Stop using Benicar and tell your doctor right away if you become pregnant.
Benicar can cause injury or death to the unborn baby if you take the medicine during your second or third trimester.
You should not use Benicar if you are allergic to olmesartan.
Drinking alcohol can further lower your blood pressure and may increase certain side effects of Benicar. Do not use potassium supplements or salt substitutes while you are taking Benicar, unless your doctor has told you to.
Your blood pressure will need to be checked often. Visit your doctor regularly.
Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.
---------------------------------------------------
Before taking Benicar
You should not take Benicar you are allergic to olmesartan.
If you have any of these other conditions, you may need a dose adjustment or special tests:
kidney disease;
liver disease;
congestive heart failure; or
if you are dehydrated.
FDA pregnancy category D. Do not use Benicar if you are pregnant.
Stop using Benicar and tell your doctor right away if you become pregnant.
Benicar can cause injury or death to the unborn baby if you take the medicine during your second or third trimester.
Use effective birth control while taking Benicar.
It is not known whether olmesartan passes into breast milk or if it could harm a
nursing baby. You should not breast-feed while you are taking olmesartan.
---------------------------------------------------
How should I take Benicar?
Take Benicar exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Your doctor may occasionally change your dose to make sure you get the best results.
You may take Benicar with or without food.
Your blood pressure will need to be checked often. Visit your doctor regularly.
Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.
Store Benicar at room temperature away from moisture and heat.
---------------------------------------------------
What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
---------------------------------------------------
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
Overdose symptoms may include extreme dizziness, fast or slow heartbeat, or fainting.
---------------------------------------------------
What should I avoid while taking Benicar?
Drinking alcohol can further lower your blood pressure and may increase certain side effects of Benicar. Do not use potassium supplements or salt substitutes while you are taking Benicar, unless your doctor has told you to.
Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.
---------------------------------------------------
Benicar side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Benicar: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:
feeling like you might pass out;
urinating less than usual or not at all;
chest pain, fast heart rate; or
swelling in your hands or feet.
Less serious Benicar side effects may include:
dizziness;
joint or muscle pain;
back pain;
stomach pain, nausea, diarrhea;
mild itching or skin rash; or
weakness.
This is not a complete list of Benicar side effects and others may occur. Tell your doctor about any unusual or bothersome side effect.
You may report side effects to FDA at 1-800-FDA-1088.
---------------------------------------------------
What other drugs will affect Benicar?
Tell your doctor about all other medicines you use, especially blood pressure medications such as a diuretic (water pill).
There may be other drugs that can interact with Benicar. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.
---------------------------------------------------
Where can I get more information?
Your pharmacist can provide more information about Benicar.
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses
outside of the United States are appropriate, unless specifically indicated otherwise.
Multum's drug information does not endorse drugs, diagnose patients or recommend therapy.
Multum's drug information is an informational resource designed to assist licensed
healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.
The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.
------------------------------------------------
注：以下产品不同规格和不同价格，购买以咨询为准！
-----------------------------------------------
产地国家: 美国
原产地英文商品名:
BENICAR DS PK 40mg/Tablet 100Tablets/box
原产地英文药品名:
OLMESARTAN MEDOXOMIL
中文参考商品译名:
傲坦板装 40毫克/片 100片/盒
中文参考药品译名:
奥美沙坦酯
生产厂家中文参考译名:
第一三共
生产厂家英文名:
DAIICHI SANKYO
-----------------------------------------------
产地国家: 美国
原产地英文商品名:
BENICAR DS PK 20mg/Tablet 100Tablets/box
原产地英文药品名:
OLMESARTAN MEDOXOMIL
中文参考商品译名:
傲坦板装 20毫克/片 100片/盒
中文参考药品译名:
奥美沙坦酯
生产厂家中文参考译名:
第一三共
生产厂家英文名:
DAIICHI SANKYO
该药品相关信息网址1:
http://www.benicar.com/
该药品相关信息网址2:
http://www.drugs.com/benicar.html
该药品相关信息网址3:
http://www.rxlist.com/benicar-drug.htm