英文药名: Tekturna HCT Tablets(Aliskiren/Hydrochlorothiazide)

中文药名: 复合阿利吉仑氢氯噻嗪片

生产厂家: 诺华制药公司
药品介绍
Tekturna是10多年来首个新一类获得批准的直接肾素抑制剂，以肾素为靶向目标，有效调节血压有效药
TEKTURNA®HCT（阿利吉仑和氢氯噻嗪）片，供口服使用
美国初步批准：2008年
警告：
阴道毒性查看完整的处方信息，以了解完整的盒装警告。
当检测到怀孕时，尽快停止Tekturna HCT。
直接作用于肾素 - 血管紧张素系统的药物可以对发育中的胎儿造成损伤和死亡。
近期主要变化
禁忌症 3/2015
警告和注意事项 3/2015
作用机制
阿利吉仑
肾素由肾响应于血容量和肾灌注的减少而分泌。肾素裂解血管紧张素原以形成无活性的十肽血管紧张素I（Ang I）。 Ang I通过血管紧张素转换酶（ACE）和非ACE途径转化为活性八肽血管紧张素II（Ang II）。 Ang II是强大的血管收缩剂，并导致从肾上腺髓质和前功能性神经末梢释放儿茶酚胺。它还促进醛固酮分泌和钠重吸收。在一起，这些影响增加血压。 Ang II也抑制肾素释放，从而向系统提供负反馈。这个周期，从肾素通过血管紧张素到醛固酮及其相关的负反馈回路，被称为肾素 - 血管紧张素 - 醛固酮系统（RAAS）。阿利吉仑是直接肾素抑制剂，降低血浆肾素活性（PRA）并抑制血管紧张素原转化为Ang I.阿利吉仑是否影响其它RAAS组分，例如ACE或非ACE途径，是未知的。
所有抑制RAAS的药剂，包括肾素抑制剂，抑制负反馈回路，导致血浆肾素浓度的补偿性升高。当在用ACE抑制剂和ARB治疗期间发生这种上升时，结果是PRA水平增加。然而，在用阿利吉仑治疗期间，阻断增加的肾素水平的作用，使得无论阿利吉仑用作单一疗法还是与其它抗高血压药联合使用，PRA，Ang I和Ang II均降低。
氢氯噻嗪（HCTZ）
HCTZ是噻嗪类利尿剂。噻嗪类影响电解质再吸收的肾小管机制，以大约相等的量直接增加钠和氯化物的排泄。间接地，HCTZ的利尿作用降低血浆体积，随之增加血浆肾素活性，增加醛固酮分泌，增加尿钾损失和血清钾降低。肾素 - 醛固酮联系由血管紧张素II介导，因此阻断血管紧张素II的产生或功能的试剂的共同给药倾向于逆转与这些利尿剂相关的钾损失。
噻嗪类物质的抗高血压作用的作用机制是未知的。
适应症和用法
Tekturna HCT是阿利吉仑，肾素抑制剂和氢氯噻嗪（HCTZ），一种噻嗪类利尿剂，用于治疗高血压，降低血压的组合：
在没有充分控制单一疗法的患者。
作为初始治疗可能需要多种药物以达到其血压目标的患者。
降低血压降低致命和非致命性心血管事件的风险，主要是中风和心肌梗死。
剂量和给药
开始用150/12.5mg每天。根据需要滴定至最大值300/25mg
增加平均效应的顺序：150/12.5mg，150/25mg或300/12.5mg和300/25mg
替代治疗：可替代滴定组分
剂量形式和强度
片剂（mg阿利吉仑/mg HCTZ）：150/12.5,150/25,300/12.5,300 /25。
禁忌症
不要在糖尿病患者中使用血管紧张素受体阻断剂（ARB）或血管紧张素转换酶抑制剂（ACEI）。
阿努里亚
对磺酰胺衍生的药物或任何组分的超敏性。
警告和注意事项
避免同时使用ARB或ACEI，特别是肾损伤患者[肌酐清除率（CrCl）<60mL/ min]。
过敏反应和血管水肿。
低血压：体积和/或盐耗患者的正确不平衡。
受损的肾功能：定期监测血清肌酐。
高钾血症：定期监测钾水平。
急性近视和继发性闭角型青光眼。
不良反应
最常见的不良反应（发生率≥1.5％，比安慰剂更常见）为：头晕和腹泻。
药物相互作用
环孢霉素或伊曲康唑：避免同时使用。
非甾体抗炎药（NSAID）：肾功能损害的风险增加和抗高血压效应的丧失。
抗糖尿病药物：可能需要调整抗糖尿病药物的剂量。
考来烯胺和考来替泊：降低噻嗪类的吸收。
锂：当与利尿剂一起使用时，增加了锂毒性的风险。
在特定人群中使用
护理母亲：护理或药物应停止。
包装规格[注：以下产品不同规格和不同价格，采购以咨询为准]
TEKTURNA HCT TAB 150/12.5MG 30  ALISKIREN/HYDROCHLOROTHIAZIDE     00078-0521-15

TEKTURNA HCT TAB 150/25MG 30  ALISKIREN/HYDROCHLOROTHIAZIDE     00078-0522-15

TEKTURNA HCT TAB 300/12.5MG 30  ALISKIREN/HYDROCHLOROTHIAZIDE     00078-0523-15

TEKTURNA HCT TAB 300/25MG 30  ALISKIREN/HYDROCHLOROTHIAZIDE     00078-0524-15

TEKTURNA® HCT (aliskiren and hydrochlorothiazide) tablets, for oral use
Medication name
Generic name: Aliskiren/hydrochlorothiazide - Oral
Brand name(s): Tekturna HCT
Warning
This drug can cause serious (possibly fatal) harm to an unborn baby if used during pregnancy. Therefore, it is important to prevent pregnancy while taking this medication. Consult your doctor for more details and to discuss the use of reliable forms of birth control while taking this medication. If you are planning pregnancy, become pregnant, or think you may be pregnant, contact your doctor immediately.
Uses
This product is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems.This product contains 2 medications. Aliskiren works by relaxing blood vessels so blood can flow more easily. Hydrochlorothiazide is called a "water pill" (diuretic) and causes your body to get rid of extra salt and water. This effect may increase the amount of urine you make when you first start the medication. It also helps to relax the blood vessels so that blood can flow through the body more easily.These medications are used together when 1 drug is not controlling your blood pressure. Your doctor may direct you to start taking the individual medications first, and then switch you over to this combination product if this is the best dose combination for you.
How to use
Read the Patient Information Leaflet available from your pharmacist before you start using this product and each time you get a refill. If you have any questions, consult your doctor or pharmacist.Take this medication by mouth, usually once daily or as directed by your doctor. High-fat foods may cause your body to absorb less of this drug. You may take this medication with or without food, but it is important to choose one way and take this medication the same way with every dose. Also, if you take this drug too close to bedtime, you may need to wake up to urinate. Therefore, it is best to take this medication at least 4 hours before your bedtime. If you have any questions about how and when to take this medication, ask your doctor or pharmacist.The dosage is based on your medical condition and response to treatment.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. It is important to continue taking this medication even if you feel well. Most people with high blood pressure do not feel sick. It may take 4 weeks before you get the full benefit of this drug.If you also take certain drugs to lower your cholesterol (bile acid-binding resins such as cholestyramine or colestipol), take this product at least 4 hours before or at least 4 to 6 hours after these medications.Tell your doctor if your condition worsens (e.g., your routine blood pressure readings increase).
Precautions
Before taking this product, tell your doctor or pharmacist if you are allergic to aliskiren or hydrochlorothiazide; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: an inability to make urine (anuria).Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, loss of too much body water (dehydration), kidney disease, liver disease, lupus, gout, untreated mineral imbalance (e.g., high/low potassium, low magnesium, high calcium), high levels of fats in the blood (cholesterol/triglycerides), certain recent nerve surgery (sympathectomy).Before having surgery, tell your doctor or dentist that you are taking this medication.This drug may make you dizzy or cause blurred vision. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position. Significant loss of body water from too much sweating, vomiting, or diarrhea can also lower your blood pressure and worsen dizziness. Drink plenty of fluids to prevent these effects and dehydration. If your doctor has directed you to limit drinking fluids, consult your doctor for further instructions. Contact your doctor if you are unable to drink fluids or if you have persistent diarrhea/vomiting.If you have diabetes, this product may change your blood sugar levels. Check your blood glucose levels regularly as directed by your doctor. Tell your doctor immediately if you have symptoms of high blood sugar such as increased thirst and urination. Your anti-diabetic medication or diet may need to be adjusted.This product may affect your potassium levels. Before using potassium supplements or salt substitutes that contain potassium, consult your doctor or pharmacist.This medication may make you more sensitive to the sun. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen and wear protective clothing when outdoors.Older adults may be more sensitive to the effects of this product, especially dizziness and diarrhea.This medication is not recommended for use during pregnancy. It may harm an unborn baby. Consult your doctor for more details. (See also Warning section.)This medication passes into breast milk. Consult your doctor before breast-feeding.
Drug interactions
See also the How to Use and Precautions sections.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: atorvastatin, cisapride, digoxin, diazoxide, dofetilide, drugs that may increase the level of potassium in the blood (including amiloride, triamterene, ACE inhibitors such as lisinopril/fosinopril/quinapril, ARBs such as irbesartan/candesartan/telmisartan, birth control pills containing drospirenone), furosemide, lithium.Other medications can affect the removal of aliskiren from your body, which may affect how aliskiren works. Examples include azole antifungals (such as itraconazole), cyclosporine, quinidine, among others.Check the labels on all your medicines (such as cough-and-cold products, diet aids, or NSAIDs such as ibuprofen, naproxen) because they may contain ingredients that could increase your blood pressure. Ask your pharmacist for more details.This product may interfere with certain laboratory tests (including parathyroid test, protein-bound iodide test), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
Side effects
Dizziness, lightheadedness, diarrhea, blurred vision, or cough may occur as your body adjusts to the medication. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: symptoms of a high potassium blood level (such as muscle weakness, slow/irregular heartbeat).This product may cause a loss of too much body water (dehydration) and salt/minerals. Tell your doctor right away if you have any symptoms of dehydration or mineral loss, including: very dry mouth, extreme thirst, muscle cramps/weakness, fast/slow/irregular heartbeat, confusion, decreased urination.Tell your doctor immediately if any of these unlikely but serious side effects occur: joint pain, increased thirst/urination, decrease in vision, eye pain.Tell your doctor immediately if any of these rare but very serious side effects occur: easy bruising/bleeding, signs of infection (e.g., fever, persistent sore throat), yellowing eyes/skin, persistent nausea/vomiting, severe stomach/abdominal pain, dark urine, unusual change in the amount of urine (not including the normal increase in urine when you first start this drug).A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects.
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.
Overdose
Notes
Do not share this medication with others.Talk with your doctor about making changes to your lifestyle that may increase the effectiveness of this medication (e.g., stress reduction programs, exercise, and dietary changes).Laboratory and/or medical tests (e.g., kidney function, blood mineral levels such as potassium) should be performed regularly to monitor your progress or check for side effects. Consult your doctor for more details.Have your blood pressure checked regularly while taking this medication. Learn how to monitor your own blood pressure at home, and share the results with your doctor.
Storage
Store at room temperature at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep all medicines away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.
Photos by medication strength
Tekturna HCT 150 mg-12.5 mg tablet
Tekturna HCT 150 mg-25 mg tablet
Tekturna HCT 300 mg-12.5 mg tablet
Tekturna HCT 300 mg-25 mg tablet
*The photos shown are samples only. Not all photos of the drug may be displayed. Your medication may look different. If you have questions, ask your pharmacist.
Important note
HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Information last revised July 2012. Copyright(c) 2012 First Databank, Inc.

完整处方资料附件：
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2D545C2F-29A4-432F-BEA9-2AEDA6592A62
美国食品和药物管理局（FDA）批准了阿利吉仑和氢氯噻嗪组合的复方制剂作为抗高血压的一线用药。
阿利吉仑（Tekturna）是一种肾素抑制剂是目前唯一的针对肾素的肾素血管紧张素醛固酮系统（RAAS）抑制剂。目前正在进行的一项包括14个试验、35000例患者的大规模心肾预后研究ASPIRE HIGHER表明，阿利吉仑的心肾保护作用可能与降低血压无关，具体作用还在进一步研究中。阿利吉仑于2007年3月在美国批准上市，2007年8月在欧洲上市，2009年7月，在日本也获得批准。阿利吉仑/氢氯噻嗪是第一个含有阿利吉仑的复方制剂，在2008年1月被批准用于高血压的二线治疗。
目前阿利吉仑/氢氯噻嗪复方制剂有4种组合：150mg/12.5mg；300mg/25mg；300mg/12.5mg；300mg/25mg。均为片剂。
FDA批准阿利吉仑/氢氯噻嗪用于高血压一线治疗，主要是根据一项为期8周的双盲、随机、安慰剂对照、平行临床试验作出的。研究共入选6200多例患者，其中2762例轻中度原发性高血压患者随机接受不同剂量的阿利吉仑（75～300mg）和氢氯噻嗪(6.25～25mg)联合治疗（均作为初次治疗）。与安慰剂组比较，单用150～300mg阿利吉仑，收缩压/舒张压下降（5～8）/（2～3）mmHg；单用12.5～25mg氢氯噻嗪，下降（6～7）/（2～3）mmHg；而（150～300）mg/（12.5～25）mg阿利吉仑/氢氯噻嗪联合治疗可以使收缩压/舒张压下降（10～14）/（5～7）mmHg。联合用药的效果明显优于单用。研究还评估了联合应用阿利吉仑和氢氯噻嗪作为一线治疗药物的安全性和有效性。阿利吉仑/氢氯噻嗪可以在治疗1周内显效，治疗4周时，可以达到最大疗效。
对于血压值高于目标值20/10mmHg的患者，目前的美国治疗指南主张一开始就使用两种药物，其中一种应为利尿剂。使用多种药物可使这类患者血压很快达标。目前，有高达85％的患者需要联合治疗，阿利吉仑/氢氯噻嗪复方制剂的获批，使医生有机会使用单一的复方制剂对患者实施积极的治疗。