中文药名: 安普那韦胶囊
英文药名: Agenerase (Amprenavir Capsules)
生产厂家: Glaxo Smith Kline 

药品说明

【通用名称】安瑞那韦，amprenavir
【商品名称】 Agenerase

【药理作用】安瑞那韦是一种新的（第五代）抗逆转病毒蛋白酶抑制剂，通过阻断从受感染的宿主细胞表面释放新的、成熟的病毒粒子的形成过程，抑制病毒的蛋白酶而起作用。当长期应用本品时，通常可降低血中的HIV病毒载体，增加CD4细胞的计数，降低感染爱滋病的机会，提高生活质量，延长生命。通过对抗急性及慢性受感染的成淋巴细胞以及外周系统血中的淋巴细胞可评价其体外抗病毒活性，其IC50对急性感染细胞是0.012～0.08mmol.L-13，对慢性感染细胞是0.4Immol.L-1。

【药代动力学】安瑞那韦吸收迅速，在 1～2h内达血药浓度峰值。口服1200mg，bid，3周后Cmax约为5.36μg.mL-1。表观分布容积约430L，体外蛋白结合率约90％。主要在肝中代谢，通过肝中P450酶CYP3A4的生物转化而清除。消除半衰期t1/2为7.l～10.6h。高脂肪食物可降低其吸收。其口服溶液剂的生物利用度比其胶囊剂约低14％，因此它们之间不能按等量换算。

【适应症】用于HIV感染的口服抗逆转病毒的治疗，须与其他抗逆转病毒制剂结合应用。

【用法用量】推荐剂量为1200mg，po，bid。服用了抗酸剂或地丹诺辛前后lh内不得服用本品。轻至中度肝功能不良的患者应降低剂量至450mg甚至300mg,bid。肾功能不良者勿需调整剂量。4～16岁的儿童推荐剂量为22.5mg.kg-1，bid（或17mg.kg-1,tid），直至最大剂量2800mg.d-1。

【不良反应】本品不良反应发生率约为15％～16％，最常见为胃肠道不良反应，如恶心、呕吐、胃痉挛、腹泻。潮红的发生率达28％，虽然大数都只是轻至中度带瘙痒的斑丘疹，但潜在并具危险性的Stevens－Johnson综合征的发生率在潮红中占4％（总的发生率为1％）。其他的不良反应尚有口周的麻刺感或麻木、抑郁、情绪紊乱、味觉紊乱。

【禁忌证】中至重度肝功能不良的患者不推荐使用本品。此前已证明对本品处方中任一组分过敏者禁用。由于本组中含有磺胺基团，因此对磺胺过敏者也不得应用。

【注意事项】
①服用本品或其他蛋白酶抑制剂时有下列倾向：自然出血、糖尿病或已有的糖尿病加重。还可出现三酸甘油、脂蛋白及肝酶水平的升高，因此有轻至中度肝功能不良的患者应降低剂量或慎用。
②本品并不能治愈HIV感染，患者有可能继续感染或出现与HIV疾病有关的其他并发症。没有证据表明本品能降低通过性接触或血液传染感染HIV的危险性。它仅作为抗HIV治疗整个方案的一部分。
③患者在服用本品时不要服用维生素E，因为本品中已含有维生素E。
④有糖尿病的患者需调整剂量。
⑤服药期间应避免怀孕或哺乳。采用激素避孕（节育丸）的应改用另一种避孕方式（如避孕套、子宫帽）。
*本品有增加体内脂肪的趋势，需注意脂肪的变化。
*严格按照处方服药，不能漏服。如果在4h之内发现漏服，应立即补上，且下次服药仍按常规时间服用。漏服时间超过4h则应等到下次常规时间时再服。任何时候都不能多服或少服，并在医生的严密监视下服药。
*食物对本品没有影响，但不能食用高脂肪食物，否则会降低疗效。

【药物相互作用】
①下列药物可能会与本品出现严重的相互作用，不得同时服用：阿司咪唑、苄普地尔、西沙必利、双氢麦角胺、麦角胺、咪达唑仑、三唑仑。利福平会显著降低本品的血药浓度和AUC，因此也应避免同服。
②本品可能会引起生物转化的严重抑制，增加心血管不良反应，可能会出现低血压、视力改变、阴茎动起时间超过4h。合用胺碘酮、利多卡因、抗抑郁药及奎宁也会出现类似严重的或威胁生命的相互作用。
③服用本品期间可能会导致高血糖或糖尿病。如果正在使用胰岛素或口服降糖药，则应适当增加其剂量。

【临床评价】本品是一种新的用于爱滋病治疗的蛋白酶抑制剂，是目前6种蛋白酶抑制剂（沙奎那韦，利托那韦，茚地那韦，nelfinavir，安瑞那韦及ABT378／r）中生物利用度最高的药物之一，与其他蛋白酶抑制剂或核苷类转录酶抑制剂联用，可广泛用于爱滋病的治疗。据第4届爱滋病感染药物治疗国际年会的报告，本品与沙奎那韦、茚地那韦及nel－finavir 3种蛋白酶抑制剂任一种联用，63％（10／16）的患者在48周时血浆中RNA病毒降低到400copies.mLmpies·mL-1以下，42％（8／19）的患者在24周时血浆中RNA病毒降低到50copies.mL-1以下。通过48周的治疗，CD4细胞计数平均增加了100。与此同时，患者对药物的耐受性良好。在24周的治疗期间，96％的不良反应是轻到中度。在48周的治疗期间，没有1例严重的不良反应被认为是与药物有关。University of Central Florida 的Jeffrey Goodgame研究（内部资料未发表）表明，应用三联［安端那韦+拉米夫定（Epivir）+齐多夫定(Retrovir)]治疗后，80％的患者RNA病毒降到400copies.mL-1以下（标准法），67％的患者降到50copies.mL-1以下（超敏法），CD4细胞计数平均增加了113（24周）。

【规格包装】胶囊剂：50mg。

Amprenavir review

Amprenavir was developed by a U.S manufacturer GlaxoSmithKline. This drug was first approved by the U.S. Food and Drug Association (FDA) in 1999 to be used for treating HIV infections that is considered to be impossible with previous medical technology.

Amprenavir is defined as a protease inhibitor that was approved in 1999. It is an antiretroviral drug or ARV for treating people with HIV infection. Studies show that people with HIV over 4 years of age can make use of this drug. The medication is commonly used for people who have a high viral load with low levels of CD4 Cell Counts. This method is used to keep HIV patients healthy with every treatment.

The amprenavir capsule is orally ingested with a full glass of water. Adults are prescribed to take 1,200mg twice a day. This was first tested using the 150mg capsules that are no longer manufactured today. Considering that amprenavir capsule is no longer manufactured; people with HIV infection can take in the drug fosamprevanir as substitute.

Today, amprenavir is approved for use along with ritonavir -- another protease inhibitor drug. Dosage may include one of the following depending upon the advice of your doctor or physician:

1. 100mg of ritonavir along with 600mg or 4 capsules of amprenavir; twice a day; or
2. 200mg of ritonavir (2 caps) along with 1,200mg (8 caps) of amprenavir; once a day.

Common side effects associated with amprenavir include diarrhea, nausea, vomiting, numbness around the mouth, rashes, and stomach pains. A small population of the patients taking in amprenavir suffers from serious skin reactions, such as the Stevens-Johnson syndrome or other allergic reactions to the medication. Doctors prescribe over-the-counter medications to control some of these side effects.

People with allergic reaction to sulfa drugs might want to refrain from using amprenavir or seek the advice of a doctor or physician if you plan to proceed with the treatment. Considering that that amprenavir is a protease inhibitor, there were no records of it having problems with people suffering from high-cholesterol levels unlike other drugs in the same family.

Liquid-based amprevanir contains glycol that may cause some problems with infants under 4 years old, people suffering from kidney or liver problems, pregnant women, or those under specific medications.

There is a possibility for amprenavir to react with other medications or herbal supplements. Both drugs in the system might trigger an overdose that could prove fatal to the patient or an underdose that will render the treatment useless.

In most cases, other ARV drugs are said to interact adversely with amprenavir. Patients currently treated with tuberculosis drugs should avoid using the said medication. Drugs to treat headaches and migraines, as well as those used for erectile dysfunctions and control heart rhythms should be avoided when being treated with amprenavir or vice versa.

As with other protease inhibitors, patients who are planning a treatment using amprenavir must consult their doctor for a thorough physical and medical examination to avoid risks, as well as following the prescribed dosage to avoid contraindications and fatal reactions.

Agenerase

What is Agenerase (amprenavir)?

Amprenavir is used to treat HIV, which causes acquired immunodeficiency syndrome (AIDS). Amprenavir is not a cure for HIV or AIDS.

Amprenavir may also be used for purposes other than those listed in this medication guide.

What is the most important information I should know about Agenerase (amprenavir)?

Do not take amprenavir with cisapride (Propulsid), pimozide (Orap), midazolam (Versed), triazolam (Halcion), or an ergot medicine such as Ergomar, Cafergot, Wigraine, D.H.E. 45, Migranal, Methergine, and others. These drugs can cause life-threatening side effects if you use them while you are taking amprenavir. Amprenavir oral liquid should also not be taken with disulfiram (Antabuse) or metronidazole (Flagyl).

There are many other medicines that can interact with amprenavir. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.

HIV/AIDS is usually treated with a combination of different drugs. To best treat your condition, use all of your medications as directed by your doctor. Do not change your doses or medication schedule without advice from your doctor. Every person with HIV or AIDS should remain under the care of a doctor.

Taking amprenavir will not prevent you from passing HIV to other people through unprotected sex or sharing of needles. Talk with your doctor about safe methods of preventing HIV transmission during sex, such as using a condom and spermicide. Sharing drug or medicine needles is never safe, even for a healthy person.

What should I discuss with my healthcare provider before taking Agenerase (amprenavir)?

Do not take this medication if you are allergic to amprenavir or a similar drug called fosamprenavir (Lexiva). Do not take amprenavir oral liquid if you are pregnant or if you have liver or kidney disease.

Do not take amprenavir with cisapride (Propulsid), pimozide (Orap), midazolam (Versed), triazolam (Halcion), or ergot medicines such as ergotamine (Ergomar, Cafergot), dihydroergotamine (D.H.E. 45, Migranal Nasal Spray), ergonovine (Ergotrate), or methylergonovine (Methergine). These drugs can cause life-threatening side effects if you use them while you are taking amprenavir. Amprenavir oral liquid should also not be taken with disulfiram (Antabuse), metronidazole (Flagyl).

Before taking amprenavir, tell your doctor if you are allergic to any drugs, or if you have:

• liver or kidney disease;

• diabetes;

• a bleeding disorder such as hemophilia; or

• high cholesterol or triglycerides.

If you have any of these conditions, you may not be able to use amprenavir, or you may need a dosage adjustment or special tests during treatment.

FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. HIV can be passed to the baby if the mother is not properly treated during pregnancy. Take all of your HIV medicines as directed to control your infection while you are pregnant. Taking amprenavir together with birth control pills can make the amprenavir less effective. Ask your doctor about using a non-hormone method of birth control (such as a condom, diaphragm, spermicide) to prevent pregnancy while taking amprenavir. You should not breast-feed while you are using amprenavir. Women with HIV or AIDS should not breast-feed at all. Even if your baby is born without HIV, you may still pass the virus to the baby in your breast milk. Do not give this medication to a child younger than 4 years old。

How should I take Agenerase (amprenavir)?

Take amprenavir exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.

Take amprenavir with a full glass (8 ounces) of water.

Amprenavir can be taken with or without food. Avoid taking with a high-fat meal, which can make it harder for your body to absorb the amprenavir.

Measure the liquid form of amprenavir with a special dose-measuring spoon or cup, not a regular tablespoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Do not switch from amprenavir capsules to oral liquid without your doctor's advice. Make sure you receive the right form of this medicine each time you get your prescription filled.

It is important to use amprenavir regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

HIV/AIDS is usually treated with a combination of different drugs. To best treat your condition, use all of your medications as directed by your doctor. Be sure to read the medication guide or patient instructions provided with each of your medications. Do not change your doses or medication schedule without advice from your doctor. Every person with HIV or AIDS should remain under the care of a doctor.

To be sure this medication is helping your condition, your blood will need to be tested on a regular basis. Your liver function may also need to be tested. Do not miss any scheduled visits to your doctor.

Store amprenavir at room temperature away from moisture and heat.

What happens if I miss a dose?

Take the missed dose as soon as you remember and take your next dose at the regularly scheduled time. If you are more than 4 hours late in taking your amprenavir, skip the missed dose and take the next regularly scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medication, or if a child has accidentally swallowed it. An overdose of amprenavir oral liquid could be fatal to a child.

What should I avoid while taking Agenerase (amprenavir)?

Avoid drinking alcohol while using amprenavir oral liquid, and do not take disulfiram (Antabuse) or you could have an alcohol reaction.

Taking amprenavir will not prevent you from passing HIV to other people through unprotected sex or sharing of needles. Talk with your doctor about safe methods of preventing HIV transmission during sex, such as using a condom and spermicide. Sharing drug or medicine needles is never safe, even for a healthy person.

Agenerase (amprenavir) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking amprenavir and call your doctor at once if you have any of these serious side effects:

• fever, sore throat, and headache with a severe blistering, peeling, and red skin rash;

• pale or yellowed skin, dark colored urine, fever, confusion or weakness;

• increased urination or extreme thirst;

• easy bruising or bleeding;

• signs of a new infection, such as fever or chills, cough, or flu symptoms; or

• seizures, muscle pain and weakness, fast heart rate, numbness or cold feeling in your arms or legs (while using amprenavir oral liquid).

Keep taking the medication and talk with your doctor if you have any of these less serious side effects:

• nausea, vomiting, diarrhea, stomach pain;

• numbness or tingling, especially around your mouth;

• headache, mood changes; or

• changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

What other drugs will affect Agenerase (amprenavir)?

Amprenavir should not be taken together with ritonavir (Norvir) if you are also using a steroid medicine called fluticasone (Advair, Flonase, Flovent). Ask your doctor about taking a different antiviral medication, or using another treatment for your allergic condition. Before taking amprenavir, tell your doctor if you are using:

• bepridil (Vascor);

• St. John's wort;

• vitamin E (tocopherol);

• antibiotics such as clarithromycin (Biaxin), itraconazole (Sporanox), ketoconazole (Nizoral), rifabutin (Mycobutin), or rifampin (Rifadin, Rimactane, Rifater);

• a blood thinner such as warfarin (Coumadin);

• antidepressants such as amitriptyline (Elavil, Etrafon), imipramine (Janimine, Tofranil), trazodone (Desyrel), and others;

• a calcium channel blocker such as amlodipine (Caduet, Lotrel, Norvasc), diltiazem (Tiazac, Cartia, Dilacor), felodipine (Plendil), nifedipine (Procardia, Adalat), or verapamil (Calan, Covera, Isoptin, Verelan);

• cholesterol-lowering medicine such as atorvastatin (Lipitor), lovastatin (Mevacor, Altocor), or simvastatin (Zocor);

• drugs that weaken the immune system, such as cyclosporine (Gengraf, Neoral, Sandimmune), sirolimus (Rapamune), or tacrolimus (Prograf);

• heart rhythm medications such as amiodarone (Cordarone) or quinidine (Quinaglute, Quinidex);

• other HIV /AIDS medicine such as delavirdine (Rescriptor), lopinavir/ritonavir (Kaletra), ritonavir (Norvir), or tipranavir (Aptivus);

• insulin or diabetes medication you take by mouth;

• medicines to treat erectile dysfunction, such as sildenafil (Viagra), tadalafil (Cialis), or vardenafil (Levitra); or

• seizure medications such as carbamazepine (Carbatrol, Tegretol), phenobarbital (Luminal, Solfoton), or phenytoin (Dilantin).

If you are using any of these drugs, you may not be able to take amprenavir, or you may need dosage adjustments or special tests during treatment.

There are many other medicines that can interact with amprenavir. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.

Where can I get more information?

• Your pharmacist has information about amprenavir written for health professionals that you may read.

What does my medication look like?

Amprenavir is available with a prescription under the brand name Agenerase. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you

• Agenerase 50 mg--off-white, opaque, oblong gelatin capsules

• Agenerase 150 mg--off-white, opaque, oblong capsules

• Agenerase Oral Solution 15 mg/mL-a clear, pale yellow, grape bubblegum peppermint-flavored liquid

• 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.