英文药名: INVIRASE Tablet/Capsule(Saquinavir mesilate)

中文药名: 甲磺酸沙奎那韦片和胶囊

生产厂家: 中外制药
药品名称
沙奎那韦 Saquinavir
中文别名：沙奎那韦、甲磺酸沙喹那韦
英文别名：Invirase、Saquinavir Mesylate
药品类别：抗病毒类
药理药动
人免疫缺陷病毒(Human lmmunodeficiencyVirus，HIV)是获得性免疫缺陷综合征(艾滋病)的病原体，系RNA逆转录病毒，它的复制涉及多个重要酶系，其中包括蛋白酶，该酶系门冬氨酸蛋白酶(Aspartic Proteinase)，其特点之一是能水解断裂苯丙氨酸-脯氨酸和酪氨酸-脯氨酸的肽键。哺乳类动物的蛋白酶难以水解它们。
本品为一高效高选择性的HIV蛋白酶抑制剂。本品作用于HIV繁殖的后期，本品与HIV蛋白酶的激活点结合，使之失去结合和水解断裂多肽的功能。 本品抑制HIV蛋白酶与其它抗HIV病毒药如叠氮胸苷，抑制HIV逆转录酶的作用靶酶系不同，无交叉耐药病毒产生。
体外试验表明，本品的作用是竞争性和可逆性的，选择性较高，在高于对HIV-1和HIV-2产生抑制作用浓度近万倍的浓度下，对人体胃蛋白酶，组织蛋白酶D、E及人白细胞弹性硬蛋白酶等几无抑制作用，对二肽酶和脯肽酶无作用。
药动学
本品口服吸收不完全，生物利用度较低，食物能显著增加本品AUC，空腹服用本品血中药物浓度极低，须餐后2小时内服用。
本品主要由肝脏中细胞色素酶P-450的同工酶CYP3A4代谢。
大鼠口服本品10mg/kg，血浆峰浓度约70～90ng/ml，大于抗病毒IC50以上，并维持6小时。
适 应 症
与其它药物合用治疗严重的HIV感染(如CD4计数低于300个／立方厘米)，能增加CD4计数，降低血中HIV总量。
用法用量
口服，每日3次，每次600mg，饭后服用。
合用药物剂量：叠氮胸苷200mg，每日3次；扎西胞苷0.75mg，每日3次。
任何疑问,请遵医嘱!
不良反应
与本品有关的不良反应通常较轻，主要有腹泻(4％)、恶心(2％)和腹部不适(1％)，但本品不增强其它药物如叠氮胸苷和扎西胞苷(Zalcitabine)的不良反应。
禁忌症
16岁以下HIV感染青少年的安全性尚无资料。 肝功能不全者慎用。
药物相互作用
能增加酶CYP3A4代谢活性的药物如利福平可降低本品血浓度约20％，利福布丁可降低本品血浓度约40％，应避免合用。其它可诱导该同工酶的药物如苯巴比妥、苯妥因和卡马西平等均可降低本品的血药浓度。 可作为酶CYP3A4代谢底物的药物如Ca离子通道阻滞剂、奎尼丁、三唑仑可升高本品血药浓度，合用时须密切观察。据报道，酮康唑可升高本品AUC，但不必调整剂量。
包装规格
胶囊：200毫克*100粒（瓶）
片：500毫克*120粒（瓶）

完整处方资料附件：http://www.haart-support.jp/information/sqvhgc_apndng.htm
INVIRASE Tablet 500mg（インビラーゼ錠500mg） 
Brand name : INVIRASE Tablet 500mg
　Active ingredient: Saquinavir mesilate
　Dosage form: pale to dusty orange, or faintly reddish-yellow tablet (major axis: approx. 19.0mm, minor axis: approx. 8.9mm, thickness: approx. 7.2mm)
　Print on wrapping: 
INVIRASE Capsule 200mg（インビラーゼカプセル200mg）
Brand name : INVIRASE Capsule 200mg
　Active ingredient: Saquinavir mesilate
　Dosage form: green/pale brown capsule (major axis: approx. 21.0mm)
　Print on wrapping:
Effects of this medicine
The medicine discourages reproduction of infectious viruses by inhibiting the function of HIV protease (enzyme which synthesizes protein). It is usually used to treat HIV infection in combination with ritonavir and other anti-HIV drugs.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you ever experienced any allergic reaction (itch, rash etc.) to any medicine.
If you are a patient with hepatic function disorder, QT prolonged, hypokalemia, hypomagnesemia, AV block complete without using pacemaker, hemophilia, bleeding tendency or renal function disorder.
•If you are pregnant or breastfeeding.
•If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
•Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>>
•General dosage regimen: For adults, take 2 tablets (1000mg of saquinavir) in combination with 100mg of ritonavir twice a day. They should be taken within 2 hours after meal concurrently. Strictly follow the instructions of your doctor/pharmacist.
•Each meal influences the absorption of the medicine. Eat meals on a regular schedule as much as possible, and make sure to take the medicine within 2 hours after meal.
•The medicine may lose effectiveness if you miss a dose. So it is important not to miss a dose. If you miss a dose by any chance and realize it, eat something and then take the missed dose as soon as possible. If it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. DO NOT take double doses to make up for the missed dose.
•If you took too much of the medicine (more than ordered), check with your doctor/pharmacist.
•Do not stop taking the medicine without the instructions of your doctor.
Precautions while taking this medicine
•Avoid taking hypericum perforatum (Saint John's wort)-containing food or garlic-constituent containing product (food,supplement,etc.), since they affect the medicine.
•Grape fruit juice may cause the medicine to act excessively. Do not take the medicine with it.
•Anti-HIV drugs may change distribution of fat in the body, which may lead to an increase of your waistline or loss of flesh on your face or limbs.
•After starting taking anti-HIV drug, your immunity will be improved, which may produce/worsen inflammatory reaction (such as fever and diarrhea) against opportunistic infection and so on.
Possible adverse reactions to this medicine
Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist: hepatic (function) disorder, anemia, diarrhea, nausea, fatigue, vomiting, abdominal pain, flatulence, etc.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
•suicide attempt [suicide attempt]
•confused/disturbed consciousness, impaired mind [confusion]
•convulsion [convulsion ]
•unable to perform intended/complicated movements [coordination disturbance]
•severe stomachache/abdominal pain, back pain, nausea, vomiting  [pancreatitis]
•severe lower abdominal pain, feeling sick at the stomach, vomiting, failure of passing stool [intestinal tract obstruction]
•enlarged feeling of abdomen [ascites]
•yellowness in the skin and/or the white of the eye, brown urine, rash, fever, lassitude, loss of appetite, nausea, vomiting, itch [severe hepatic function disorder , jaundice, hepatitis]
•enlarged feeling of abdomen, palpitation/shortness of breath when going upstairs or uphill, headache, shortness of breath, ear ringing, dizziness, lassitude  [portal hypertension]
•excess intake of water, thirst, increased urinary volume, lassitude, weight loss, feeling of weariness [hyperglycemia, diabetes]
•dizziness, palpitation, ear ringing, nose/gum bleeding, bleeding tendency, blue spot, shortness of breath [pancytopenia]
•lightheadedness, dizziness on standing up, easy fatigability, top-heavy feeling, dizziness, lassitude, palpitation/shortness of breath when moving, yellowness in the skin and/or the white of the eye, brown urine [hemolytic anemia]
•sore throat, fever [leukopenia, neutropenia]
•blue spot, gum bleeding, bleeding tendency [thrombocytopenia]
•skin, lips and nails turning bluish purple, swelling, fever, swollen legs [thrombophlebitis]
•bleeding [bleeding]
•lassitude, breathlessness, coldness of the limbs, facial pallor [peripheral vasoconstriction]
•shortness of breath, dizziness, fever, lassitude, bleeding tendency [acute myelogenous leukemia]
•high fever, pain in the genitalia, severe stomatitis, lip/intraoral sore, fever, red rash with dropsical swelling in the center, red rash, inflamed eye and eyelid, loss of appetite, lassitude, conjunctival sore [mucocutaneous ocular syndrome (Stevens-Johnson syndrome)]
•severe low-back/back pain, bloody urine [nephrolithiasis]
•falling upper eyelid, double vision, loss of strength, heavy feeling in the eyelids, muscle fatigue [asthenia]
•joint pain/enlargement [polyarthritis]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
•Keep out of the reach of children. Store at room temperature (1-30℃), away from direct sunlight and moisture.
•Discard the remainder. Do not store them. Ask the pharmacist how to discard.
Chugai Pharmaceutical Co., Ltd.Internal
Revised: 10/2011
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.