英文药名: Agenerase(Amprenavir Capsules，Solution)

中文药名: 安普那韦口服液

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* 480 胶囊

口服液：15mg/ml*240ml  

Agenerase (amprenavir) 150mg. tabs

Agenerase Generic Name: Amprenavir (am-PREN-ah-veer)Brand Name: Agenerase
Agenerase is used for:
Treating HIV infection. Agenerase is used in combination with other medicines.

Agenerase is an HIV-protease inhibitor. It works by inhibiting the growth of HIV.

Do NOT use Agenerase if:
you are allergic to any ingredient in Agenerase
you are taking astemizole, cisapride, delavirdine, an ergot derivative (eg, ergotamine), eletriptan, erythromycin, certain HMG-CoA reductase inhibitors (lovastatin, simvastatin), midazolam, nevirapine, an oral contraceptive (birth control pills), pimozide, a quinazoline (eg, alfuzosin), rifampin, St. John's wort, sumatriptan, terfenadine, or triazolam
Contact your doctor or health care provider right away if any of these apply to you.

Before using Agenerase :
Some medical conditions may interact with Agenerase . Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

if you are pregnant, planning to become pregnant, or are breast-feeding
if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
if you have allergies to medicines, foods, or other substances
if you have had a severe allergic reaction (eg, severe rash, hives, difficulty breathing, dizziness) to any other sulfonamide medicine, such as acetazolamide, celecoxib, certain diuretics (eg, hydrochlorothiazide), glyburide, probenecid, sulfamethoxazole, valdecoxib, or zonisamide
if you have diabetes, hemophilia or other bleeding disorders, high cholesterol or triglyceride levels, high blood sugar, liver disease, a skin rash, or kidney problems
Some MEDICINES MAY INTERACT with Agenerase . Tell your health care provider if you are taking any other medicines, especially any of the following:

Carbamazepine, dexamethasone, methadone, non-nucleoside reverse transcriptase inhibitors (NNRTIs) (eg, efavirenz, nevirapine), oral contraceptives (birth control pills), phenobarbital, phenytoin, rifampin, saquinavir, or St. John's wort because the effectiveness of Agenerase may be decreased
HIV protease inhibitors (eg, indinavir, ritonavir) because the actions and side effects of Agenerase may be increased
Astemizole, certain HMG-CoA reductase inhibitors (eg, lovastatin, simvastatin), cisapride, eletriptan, ergot derivatives (eg, ergotamine), erythromycin, midazolam, pimozide, quinazolines (eg, alfuzosin), sumatriptan, terfenadine, or triazolam because the risk of side effects may be increased by Agenerase
Aldosterone blockers (eg, eplerenone), antiarrhythmics (eg, amiodarone, bepridil, flecainide, lidocaine, propafenone, quinidine), azole antifungals (eg, itraconazole, ketoconazole), benzodiazepines (eg, alprazolam), calcium channel blockers (eg, diltiazem, amlodipine), fluoxetine, fluticasone, immunosuppressants (eg, cyclosporine, tacrolimus), muscarinic receptor antagonists (eg, darifenacin), narcotic analgesics (eg, fentanyl), rifabutin, sildenafil, trazodone, or tricyclic antidepressants (eg, amitriptyline) because the risk of side effects may be increased by Agenerase
Delavirdine because effectiveness may be decreased by Agenerase
Anticoagulants (eg, warfarin) because actions and effectiveness may be altered by Agenerase
This may not be a complete list of all interactions that may occur. Ask your health care provider if Agenerase may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Agenerase :
Use Agenerase as directed by your doctor. Check the label on the medicine for exact dosing instructions.

Agenerase may be taken with or without food. If you take it with food, do not take it with a high fat meal.
Agenerase comes with an additional patient leaflet. Read it carefully and reread it each time you get Agenerase refilled.
Do not take antacids or a buffered form of didanosine within 1 hour before or 1 hour after taking Agenerase .
Continue to use Agenerase even if you feel well. Do not miss any doses.
Do not switch between the capsule and liquid forms of Agenerase . They are not equal milligram to milligram. Consult with your doctor or pharmacist.
If you miss a dose of Agenerase , take it as soon as possible. If you miss a dose by more than 4 hours, skip the missed dose and go back to your regular dosing schedule. It is important not to miss doses of Agenerase . Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use Agenerase .

Important safety information:
Agenerase is not a cure for HIV infection and patients may continue to acquire illnesses and infections associated with HIV. Remain under the care of your doctor.
Agenerase may not prevent other infections. If your health changes, check with your doctor.
When your medicine supply begins to run low, get more from your doctor or pharmacist as soon as possible. The virus may develop resistance to Agenerase and become more difficult to treat if you stop taking it, even for a short period of time.
Agenerase offers no protection from the transmission of HIV to others through sexual contact or blood contamination. Use barrier forms of contraception (eg, condoms) if you are infected with HIV. Do not share needles, other injection equipment, or personal items such as toothbrushes or razor blades.
Certain birth control pills may decrease the effectiveness of Agenerase . Women should not take birth control pills and should use additional or other birth control measures (eg, condoms, diaphragms) while taking Agenerase .
Do not take vitamin E supplements while you are taking Agenerase . Agenerase already contains vitamin E.
Agenerase may cause high blood sugar (eg, thirst, increased urination, confusion, drowsiness, flushing, rapid breathing, fruity breath odor). If these symptoms occur, tell your doctor immediately.
Changes in body fat may occur in some patients taking this type of medicine. These changes may include increased amount of fat in the upper back and neck, breast, and around the trunk, and loss of fat from the legs, arms, and face. The cause and long-term effects are unknown. Discuss any concerns with your doctor.
LAB TESTS, including liver function, blood cholesterol or triglyceride levels, and white blood cell counts, may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.
Use Agenerase with caution in the ELDERLY because they may be more sensitive to its effects.
Agenerase is not recommended for use in CHILDREN younger than 4 years of age. Safety and effectiveness in this age group have not been confirmed.
PREGNANCY and BREAST-FEEDING: If you become pregnant, discuss with your doctor the benefits and risks of using Agenerase during pregnancy. It is unknown if Agenerase is excreted in breast milk. Do not breast-feed while taking Agenerase . HIV-infected mothers should not breast-feed their infants because of the risk of transmitting the HIV infection or Agenerase .
Possible side effects of Agenerase :
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Diarrhea/loose stools; headache; nausea; numbness or tingling around the mouth and in the hands and feet; rash; shift of body fat to stomach and upper back; stomach pain; taste disorders; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); change in mood, emotions, or behavior; clumsiness; depression; excessive urination, thirst, or hunger; fever, chills, or sore throat; muscle pain or stiffness; red, swollen, or blistered skin; seizures; unusual tiredness or weakness; yellowing of the skin or eyes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. You may also report side effects at .

If OVERDOSE is suspected:
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center (http://www.aapcc.org), or emergency room immediately.

Proper storage of Agenerase :
Store Agenerase at 77 degrees F (25 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Agenerase out of the reach of children and away from pets.