Tekturna HCT
Generic name: Aliskiren and hydrochlorothiazide

What is Tekturna HCT?
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Tekturna HCT is used to lower blood pressure. It contains two medicines in one tablet: aliskiren and the diuretic hydrochlorothiazide. Tekturna HCT may be used alone or in combination with other blood pressure-lowering medications.

What is the most important information I should know about Tekturna HCT?
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Do not use Tekturna HCT during pregnancy. If you become pregnant while on this medication, stop taking Tekturna HCT and call your doctor right away. Tekturna HCT may harm an unborn baby, causing injury and even death.

Tekturna HCT does not cure high blood pressure; it works to keep it under control. It is important to take Tekturna HCT regularly for it to be effective. Since blood pressure declines gradually, it may take a few weeks before you see the full benefit of this medication; you must continue taking it even if you are feeling well.

Who should not take Tekturna HCT?
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You should not take this medication if you are pregnant, plan to become pregnant, or are breastfeeding. Also, you should not take Tekturna HCT if you are allergic to any of its ingredients or if you have urination problems due to kidney dysfunction.

What should I tell my doctor before I take the first dose of Tekturna HCT?
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Tell your doctor about all prescription, over-the-counter, and herbal medications you are taking before beginning treatment with Tekturna HCT. Also, talk to your doctor about your complete medical history, especially if you have any of the following: kidney or liver problems, systemic lupus erythematosus (SLE), allergies or asthma, or if you have ever had a reaction called angioedema to an ACE inhibitor medicine. Signs of angioedema include difficulty breathing and swelling of the face, lips, tongue, throat, arms and legs.

Alert your doctor immediately if you are pregnant, plan on becoming pregnant, or are breastfeeding.

What is the usual dosage?
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The information below is based on the dosage guidelines your doctor uses. Depending on your condition and medical history, your doctor may prescribe a different regimen. Do not change the dosage or stop taking your medication without your doctor's approval.

Adults: The usual starting dose is 150 milligrams (mg) of aliskiren/12.5 mg of hydrocholorothiazide taken once daily. Your doctor may increase the daily dose up to 300 mg of aliskiren/25 mg of hydrocholorothiazide if your blood pressure is not adequately controlled on a lower dose.

How should I take Tekturna HCT?
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Take Tekturna HCT once a day, at the same time each day. It can be taken with or without food.

What should I avoid while taking Tekturna HCT?
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Avoid becoming pregnant while on this medication. It is not known whether Tekturna HCT passes into breast milk; you may have to stop breastfeeding while on this medication or your doctor may want you to use another medication to lower your blood pressure instead. Speak to your doctor if you are breastfeeding.

What are possible food and drug interactions associated with Tekturna HCT?
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If Tekturna HCT is taken with certain other drugs, the effects of either could be increased, decreased, or altered. It is especially important to check with your doctor before combining Tekturna HCT with the following: other medicines for high blood pressure or a heart problem, diuretics, medicines for treating fungus or fungal infections, cyclosporine, potassium-containing medicines, potassium supplements, salt substitutes containing potassium, cholestyramine, colestipol, medicines to treat diabetes including insulin, nonsteroidal anti-inflammatory drugs (NSAIDs), blood thinners, barbiturates, and narcotic medicines.

Do not use Tekturna HCT if you are taking lithium.

What are the possible side effects of Tekturna HCT?
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Side effects cannot be anticipated. If any develop or change in intensity, tell your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking this drug.

Side effects may include: dizziness, flu-like symptoms, diarrhea, cough, tiredness, low blood pressure, active or worsened systemic lupus erythematosus (SLE).

Serious side effects that require immediate medical attention include difficulty breathing and swelling of the face, lips, tongue, throat, arms and legs.

Can I receive Tekturna HCT if I am pregnant or breastfeeding?
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You should not take this medication if you are pregnant. If you become pregnant while on this medication, inform your doctor as soon as possible. It is not known whether Tekturna HCT passes into breast milk; you may have to stop breastfeeding while on this medication or your doctor may want you to use another medication to lower your blood pressure instead. Tell your doctor immediately if you are breastfeeding.

What should I do if I miss a dose of Tekturna HCT?
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If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the one you missed and return to your regular schedule. Never double the dose.

How should I store Tekturna HCT?
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Store at room temperature in a dry place.

      第二代肾素抑制剂
　　阿利吉仑是新一代非肽类肾素阻滞药，能在第一环节阻断RAS系统，降低肾素活性，减少AngII和醛甾酮的生成，不影响缓激肽和前列腺素的代谢，起到降血压和治疗心血管疾病的作用。从目前研究来看阿利吉仑是强效的、高度选择性的、口服有效的、长效的新一代抗高血压药物。该药作用于肾素依赖性，因此加大剂量给药只会延长时间不会导致血压骤降，与ARB（氯沙坦、替米沙坦）相似，不良反应的发生率与安慰剂组相比无显著差异。aliskiren可以阻断噻嗪类利尿剂、血管紧张素转换酶抑制剂和血管紧张素受体拮抗剂导致的肾素反应性升高，小样本试验与氢氯噻嗪、雷米普利和厄贝沙坦联合时，血浆肾素活性并没有升高。
　　Stanton研究表明，阿利吉仑能有效减少正常志愿者AngII的水平，有效地降低轻、中度高血压患者的血压，其降压程度与剂量相关，而心率无明显改变，并可能对肾病、心力衰竭、动脉粥样硬化的治疗亦有效。Wood等研究了阿利吉仑对钠缺乏小猴的降压作用，发现在第1次给药后2h血压下降(13±2)mmHg，并于给药后约2Oh恢复到治疗前水平。在治疗8d中，血压最大下降(16±2)mmHg，停药后血压没有反跳性增高。
　　治疗依从性差是目前抗高血压治疗的主要问题之一。Stanton和Nussberger等的研究均表明，阿利吉仑37．5，75，150，300mg，每天1次，服药4周，坚持率>95％，受试者能很好地耐受。并在单次给药和多次给药研究中，口服剂量达到640mg，服药8d后，血压正常健康受试者亦能很好地耐受，且没有明显的毒性反应。实验中各项临床实验检查，如血液学、生化和尿液分析，以及体格检查、心电图记录，在整个服药过程中绝大多数保持正常。
　　目前的观察阿利吉仑不良反应很少，类似于安慰药。最常见的不良反应为乏力、胃肠道反应或头痛。增加阿利吉仑的剂量，不良反应的发生率没有增加。在226例高血压患者服用阿利吉仑300mg/d组中l例出现胸痛和心电图示局部缺血改变，另1例出现低血压休克，经治疗后均得到康复。另外，Dieterle等研究了健康人群中阿利吉仑与华法林钠之间的相互作用，结果显示阿利吉仑基本不影响华法林钠的抗凝作用，不会改变PT、INR、aPTT。
　　早在30年前，肾素-血管紧张素醛固酮（RAAS）系统在高血压及其并发症发生、发展过程中的重要作用已被认识。其中，肾素作为RAAS系统的起始步骤，可通过直接抑制其活性而阻断RAAS系统的病理作用。雷米吉仑（remikiren）、依那吉仑（enalkiren）等特异性肾素抗体以及肽类肾素拮抗药相继被开发出来，尽管这些制剂能够降低肾素水平，具有明显的降压作用，但因口服剂的生物利用度较低、作用维持时间短、合成费用高等缺点，最终未能成功应用于临床。
　　在这样的前提下，阿利吉仑的获准应用于临床具有了不寻常的意义。阿利吉仑是第二代肾素-血管紧张素受体抑制剂，虽然和血管紧张素转化酶抑制剂、血管紧张素Ⅱ受体拮抗剂和醛固酮受体阻断剂的作用机制一样，但所不同的是，阿利吉仑直接作用的部位是肾素。在爱尔兰进行的Ⅱ期临床试验证实，阿利吉仑能有效降低轻中度高血压患者的血压水平；在Ⅲ期临床试验中，受试者在开始治疗的2周内就出现了明显的降压效果。此外，阿利吉仑与厄贝沙坦的对比试验也证实了阿利吉仑对轻中度高血压患者的疗效。
　　尽管阿利吉仑显示出较好的降压作用，但Wright博士指出，降压治疗的主要目标是防止并发症，而现在还不能确切得知阿利吉仑能否防止产生心衰等并发症以及能否对肾起保护作用。