部份中文硫酸阿扎那韦处方资料（仅供参考） 药品英文名 Atazanavir 药品别名 硫酸阿扎那韦、锐艾妥、Atazanavir Sulfate、Reyataz、BMS-232632 药物剂型 胶囊：l00mg/粒，150mg/粒，200mg/粒，300mg/粒。 药理作用 本品是一新型氮杂肽类蛋白酶抑制剂(PI)，其体外活性与奈非那韦(Nelfinavir)等非肽类PI不伺，本品是根据酶-氮杂肽复合物的X射线衍射研究设计而成的，具有C-2对称的化学结构。它是HIV-1蛋白酶的高选择性和高效的抑制剂，通过阻断病毒gap和gap-pol前体多聚蛋白的裂解，从而抑制病毒结构蛋白、逆转录酶、整合酶和蛋白酶的生成，使HIV-1感染的细胞释放出非感染性的不成熟的病毒颗粒。本品对多株HIV-1病毒具有比其他PI更强的抑制活性，在体外培养基中半数有效浓度(EC50)为2.6～5.3nmol/L，90%有效浓度(EC90)为9～15nmol/L。 药动学 本品吸收迅速，达峰时间为2.5h，当每日剂量为200～800mg时，其药时曲线下面积(AUC)和血药峰浓度(Cmax)的增加呈剂量相关性，4～8天达稳态浓度。食物可增加其生物利用度，食用清淡饮食与禁食状态下，口服单剂量400mg，Cmax增加57%，AUC增加70%。健康志愿者口服400mg，每日1次，6～14天，血药谷浓度Cmin为149～219ng/ml，Cmax为2918～5867ng/ml，达峰时间(Tmax)为2～4h，达稳态时药时曲线下面积(AUCr)为18590～33500ng·h/ml。对慢吸收和快吸收类型两组患者，400mg或600mg，每日1次，中央室的表观容积分别为187L和109L，一级吸收速率常数分别为1.45/h和6.48/h。本品主要由肝脏微粒体细胞色素P450 CYP3A同工酶代谢，经胆汁消除。三种主要的代谢产物均无抗HIV活性。胶囊的生物利用度为口服溶液的60%～68%。 适应证 用于HIV感染患者。 禁忌证 1．对本品过敏者禁用。 2．严重肝损害患者禁用。 注意事项 1．具有轻、中度肝损害的患者慎用。 2．本品主要经肝脏代谢，具有轻、中度肝损害的患者应用时易发生药物蓄积，注意调整剂量。 3．当与一些可使心电图P-R间期延长的药物如阿托品合用时，应注意心脏监护。 4．15～30℃保存。 不良反应 1．常见的不良反应为恶心、呕吐、腹泻、胃痛、皮疹、发热、咳嗽、失眠、抑郁、手脚麻木等。 2．可出现皮肤及眼睛发黄、眩晕，可诱发糖尿病和血糖升高，对血液病患者可能会增加出血倾向，可使心电图显示P-R间期延长。 3．严重者可发生代谢性酸中毒，一般多发生于女性或肥胖者。 4．脂质代谢障碍很少出现，黄疸发生率与剂量相关。 用法用量 口服，推荐剂量为400mg，每日1次。并与食物同服。或本品300mg与利托那韦100mg合用，与食物同服。 药物相应作用 1．本品是中度CYP3A抑制剂，抑制常数为2．2～2．7nmol/L。与CYP3A强大的抑制剂利托那韦合用，本品的血药浓度增加数倍。 2．与CYP3A诱导剂艾法韦仑合用，本品的Cmax、AUC和Cmin分别减少了59%、74%和99%。 3．健康志愿者服用本品1h后再给予司他夫定和去羟肌苷未产生明显的相互作用，而当三药同时服用，本品的Cmax和AUC分别减少了89.3%和87%，原因可能是去羟肌苷导致抗酸的缓冲作用的形成所致。 4．本品与拉米夫定以及齐多夫定合用时剂量不需调整。 5．本品400mg，每日1次，与沙奎那韦软胶囊合用可使后者的AUC增加数倍，而自身的药代动力学参数不改变。 6．本品与抗生素利福布汀或克拉霉素合用，使二药的AUC分别增加2倍和1.9倍，与酮康唑合用药动学参数不变。 7．当与抗病毒药去羟肌苷合用时，应于服用去羟肌苷前2h或之后0.5h服用本品。 8．与依法韦仑合用时，必须同时合用利托那韦，一般为本品300mg＋利托那韦lOOmg＋依法韦仑600mg。 9．与替诺福韦合用时，必须同时合用利托那韦，一般为本品300mg＋利托那韦lOOmg＋替诺福韦30mg。 Medication name Generic name: Atazanavir - Oral Brand name(s): Reyataz Uses This drug is used with other HIV medications to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system can work better. This lowers your chance of getting HIV complications (such as new infections, cancer) and improves your quality of life.Atazanavir belongs to a class of drugs known as protease inhibitors. It may be given with ritonavir, another protease inhibitor, to increase ("boost") the levels of atazanavir. This helps atazanavir work better.Atazanavir is not a cure for HIV infection. To decrease your risk of spreading HIV disease to others, do all of the following: (1) continue to take all HIV medications exactly as prescribed by your doctor, (2) always use an effective barrier method (latex or polyurethane condoms/dental dams) during all sexual activity, and (3) do not share personal items (such as needles/syringes, toothbrushes, and razors) that may have contacted blood or other body fluids. Consult your doctor or pharmacist for more details. Other uses This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.This medication may also be used in combination with other HIV medications to reduce the risk of getting HIV infection after contact with the virus. Consult your doctor for more details. How to use Read the Patient Information Leaflet if available from your pharmacist before you start taking atazanavir and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, usually once daily with food. Do not open, crush, or chew the capsules. Swallow the capsules whole.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. For children, the dosage is also based on weight. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). If you are directed to take ritonavir with this medication, take them both at the same time.If you are taking antacids or buffered forms of drugs (such as didanosine solution, didanosine enteric-coated capsules), take atazanavir at least 2 hours before or 1 hour after these medications.This medication works best when the amount of drug in your body is kept at a constant level. Therefore, take this drug at evenly spaced intervals. To help you remember, take it at the same time each day.It is very important to continue taking this medication (and other HIV medications) exactly as prescribed by your doctor. Do not skip any doses. Do not take more or less of this drug than prescribed or stop taking it (or other HIV medicines) even for a short time unless directed to do so by your doctor. Doing so may cause the amount of virus to increase, make the infection more difficult to treat (resistant), or worsen side effects. Precautions Before taking atazanavir, tell your doctor or pharmacist if you are allergic to it; 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.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems (including hepatitis B or C infections), kidney problems (including kidney stones), heart problems (such as heart rhythm problems, irregular heartbeat, coronary artery disease, heart attack), diabetes, a certain bleeding problem (hemophilia).Atazanavir may increase the level of cholesterol and fats (triglycerides) in your blood. HIV infection can also cause this effect. This could increase your risk for heart problems such as a heart attack. Discuss the risks and benefits of treatment with your doctor and ways to lower your risk of heart disease. Tell your doctor if you have heart problems, if you smoke, or if you have other conditions that increase your risk of heart disease such as high blood pressure, diabetes, or high cholesterol/triglyceride levels.Before having surgery, tell your doctors or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Atazanavir should not be given to children younger than 3 months because of the risk of very serious side effects.During pregnancy, this medication should be used only when clearly needed. However, HIV medicines are now usually given to pregnant women with HIV. Treatment can decrease the risk of passing the HIV infection to your baby. Atazanavir may be part of that treatment. Discuss the risks and benefits with your doctor.It is unknown if atazanavir passes into breast milk. Because breast milk can transmit HIV, do not breast-feed. Drug interactions See also How to Use section.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.Atazanavir interacts with many medications. One product that may interact with this drug is: indinavir.Other medications can affect the removal of atazanavir from your body, which may affect how atazanavir works. Examples include boceprevir, carbamazepine, etravirine, phenobarbital, phenytoin, nevirapine, rifamycins (such as rifampin), St. John's wort, voriconazole, among others.Atazanavir can slow down the removal of other medications from your body, which may affect how they work. Examples of affected drugs include some alpha blockers (such as alfuzosin), certain benzodiazepines (midazolam, triazolam), cisapride, ergot alkaloids (such as dihydroergotamine, ergotamine), fluticasone, irinotecan, lurasidone, pimozide, drugs to treat erectile dysfunction-ED or pulmonary hypertension (such as sildenafil, vardenafil), certain "statin" cholesterol drugs (lovastatin, simvastatin), salmeterol, among others.Prescription and nonprescription drugs to treat heartburn, indigestion, or ulcers (including H2 blockers such as famotidine, proton pump inhibitors such as lansoprazole/omeprazole) reduce stomach acid and decrease the absorption of atazanavir. This may prevent atazanavir from working well. Ask your doctor or pharmacist how to use these medications safely.This medication may decrease the effectiveness of hormonal birth control such as pills, patch, or ring. This could cause pregnancy. Talk to your doctor about additional or alternative reliable forms of birth control, and always use an effective barrier method (latex or polyurethane condoms/dental dams) during all sexual activity to decrease the risk of spreading HIV to others. Tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your hormonal birth control is not working well. Side effects Headache or nausea may occur. If either of these effects persists or worsens, 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.Some people may experience worsening of a previous medical condition (such as an old infection) as their immune systems improve, or develop new conditions because their immune systems have become overactive. This reaction may occur at any time (soon after starting HIV treatment or many months later). Tell your doctor right away if you have any serious side effects, including: unexplained weight loss, persistent muscle aches/weakness, joint pain, numbness/tingling of the hands/feet/arms/legs, severe tiredness, vision changes, severe/persistent headaches, signs of infection (such as fever, chills, trouble breathing, cough, non-healing skin sores), signs of an overactive thyroid (such as irritability, nervousness, heat intolerance, fast/pounding/irregular heartbeat, bulging eyes, unusual growth in the neck/thyroid known as a goiter), signs of a certain nerve problem known as Guillain-Barre Syndrome (such as difficulty breathing/swallowing/moving your eyes, drooping face, paralysis, slurred speech).Tell your doctor right away if you have any serious side effects, including: yellowing eyes/skin, increased thirst/urination, dizziness, lightheadedness, signs of a kidney stone (such as pain in side/back/abdomen, painful urination, blood in the urine).Changes in body fat may occur while you are taking this medication (such as increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Discuss the risks and benefits of treatment with your doctor, as well as the possible use of exercise to reduce this side effect.Get medical help right away if you have any very serious side effects, including: signs of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating).Atazanavir can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Therefore, get medical help right away if you develop any rash.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: 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. You may report side effects to FDA at 1-800-FDA-1088.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. Missed dose It is important not to miss doses of this drug. If you miss a dose, take it as soon as you remember, unless it is less than 6 hours until the next dose. In that case, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up. Overdose If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe dizziness, lightheadedness. Notes Do not share this medication with others.Laboratory and/or medical tests (such as viral load, T-cell counts, liver tests, cholesterol/triglyceride levels, blood sugar levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details. Storage Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications 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. Photos by medication strength Click the "Photos" link to see sample photographs for a specific medication strength. Common strengths Reyataz 100 mg capsule Reyataz 150 mg capsule Reyataz 200 mg capsule Reyataz 300 mg capsule *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. Information last revised March 2013. Copyright(c) 2013 First DataBank, Inc. Selected from NATIONAL DRUG DATA FILE (NDDF) data included with permission and copyrighted by First DataBank, Inc., 2012. This copyrighted material has been downloaded from a licensed data provider. The above information is intended to supplement, not substitute for, the expertise and judgment of your health care professional. You should consult your health care professional before taking any drug, changing your diet, or commencing or discontinuing any course of treatment. --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: REYATAZ 300mg 30caps 原产地英文药品名: ATAZANAVIR SULFATE 中文参考商品译名: 锐艾妥 300毫克/胶囊 30胶囊/盒 中文参考药品译名: 硫酸阿扎那韦 生产厂家中文参考译名: BRISTOL MYERS SQUIBB (US) 生产厂家英文名: BRISTOL MYERS SQUIBB (US) --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: REYATAZ 150mg 60caps 原产地英文药品名: ATAZANAVIR SULFATE 中文参考商品译名: 锐艾妥 150毫克/胶囊 60胶囊/盒 中文参考药品译名: 硫酸阿扎那韦 生产厂家中文参考译名: BRISTOL MYERS SQUIBB (US) 生产厂家英文名: BRISTOL MYERS SQUIBB (US) --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: REYATAZ 100mg 60caps 原产地英文药品名: ATAZANAVIR SULFATE 中文参考商品译名: 锐艾妥 100毫克/胶囊 60胶囊/盒 中文参考药品译名: 硫酸阿扎那韦 生产厂家中文参考译名: BRISTOL MYERS SQUIBB (US) 生产厂家英文名: BRISTOL MYERS SQUIBB (US)