英文药名：Kaletra Combination Liquid for Internal(Lopinavir/Ritonavir)

中文药名：洛匹那韦/利托那韦组合液体

生产厂家：艾伯维 GK

カレトラ配合内用液

治疗类别名称
抗病毒化疗药物
欧文商標名
Kaletra
構造式

一般名
ロピナビル (Lopinavir) [JAN]
化学名
(-)-(2S )-N-{ (1S , 3S , 4S )-1-benzyl-4-[2-(2, 6-dimethylphenoxy) acetylamino]-3-hydroxy-5-phenylpentyl}-3-methyl-2-(2-oxotetrahydropyrimidin-1-yl) butyramide
分子式
C37H48N4O5
分子量
628.80
性状
白色到浅黄棕色粉末，有些还包括软质。
構造式

一般名
リトナビル (Ritonavir) [JAN]
化学名
(+)-5-thiazolylmethyl[(αS )-α-[(1S , 3S )-1-hydroxy-3-[(2S )-2-[3-[(2-isopropyl-4-thiazolyl) methyl]-3-methylureido]-3-methylbutyramido]-4-phenylbutyl] phenethyl] carbamate
分子式
C37H48N6O5S2
分子量
720.94
性状
白色到浅黄棕色粉末，有些还包括软质。
药效药理
1. 作用机序
本剂是洛匹那韦和利托那韦的制剂。洛匹那韦抑制HIV蛋白酶的活性，通过抑制由HIV蛋白酶多聚在gag-POL的裂解，抑制产生成熟的HIV感染性。利托竞争由CYP3A抑制洛匹那韦的代谢，导致增加洛匹那韦的血液水平。这种药物的抗病毒活性是洛匹那韦（见“药代动力学”）。
本剂对HIV蛋白酶的选择性亲和力，它显示了对人的天冬氨酸蛋白酶的小的抑制作用。
2. 抗病毒活性（体外）
洛匹那韦的抗病毒作用在淋巴母细胞系和感染的临床分离株艾滋病毒标准株后早期感染的外周血淋巴细胞。在人类中无血清的，洛匹那韦的EC50为5种HIV-1的标准菌株的平均为10〜27纳米（0.006〜0.017μg/ mL）的7），平均的六种类型的洛匹那韦的抗HIV-1临床分离株EC50为4〜11nM（0.003〜0.007μg/ mL）中。在50％人血清的平均洛匹那韦的存在下对HIV-1标准株的EC50是65〜289nM（0.04〜0.18μg/ mL）中，在效力下降7〜11倍，观察。
3. 耐药性
敏感具有降低的洛匹那韦，洛匹那韦分离的HIV-1变体单独或在洛匹那韦和利托那韦的血液浓度的存在下，在临床给药时的HIV-1的体外继代进行。了检查表型和传代分离株的基因型，利托那韦的存在有人提议对耐洛匹那韦株的出现没有影响（体外）。
交叉耐药：
HIV蛋白酶抑制剂（PI）之间观察到的交叉耐药性是变化的。关于病毒的交叉耐药性与由这种药物的治疗敏感性降低洛匹那韦信息尚未几乎获得。
此代理从四个患者PI使用历史，承认中洛匹那韦，茚地那韦，或交叉耐药性的表型电阻的增大获得了上届政府分离利托那韦已经保持了奈非那韦，交叉耐药这种药物的给药后收购。所有这是反弹或没有维持易感性安普那韦足够的病毒，仍然观察到（高达99倍，洛匹那韦，在安普那韦高达8.5倍）的弱灵敏度的降低。谁经历病毒反弹的科目，从科目沙奎没有经验得出两种菌株保持着易感性沙奎那韦。
在抗逆转录病毒治疗经验的患者抗病毒作用减少谁开始的联合治疗，包括洛匹那韦，利托那韦和基因型与相关：
在HIV蛋白酶的氨基酸替换（L10F/I/ R/V，K20M/N/R，L24I，L33F，M36I，I47V，G48V，I54L/T/V，V82A/C/F/S/T，I84V）3已经发现，影响这种药物的病毒学响应于存在或更多。在联合疗法中与HIV蛋白酶抑制剂（PI）抗性突变病毒学应答之间关系的速度在多个药物临床试验是如下的。（见药理学表）
HIV蛋白酶抑制剂（PI）中所使用的示例的抗病毒活性：
它是在体外对洛匹那韦的敏感性降低的临床意义，这种药物的施用，尽管在血液处理由多个PI的向谁超过病毒的1,000copies/毫升，在56例患者的HIV RNA的量它是评价基因型和表型。反对开始隔离56株洛匹那韦的EC50为0.5〜96倍的野生菌株的EC50。药物48周，依法韦仑和核苷逆转录酶抑制剂的给药后，患者血液中HIV RNA水平大于400copies等于或小于/毫升，开始洛匹那韦的敏感性的10倍或更小，10倍的超40折以下，和93％，分别在该基团的例（25/27），73％（11/15）的40倍以上，这是25％（2/8）。此外，患者血液中的HIV RNA水平大于在病人洛匹那敏组的开始在这些50copies/毫升等于或更小，分别为81％（22/27），60％（9/15），25％（2/8）。
本剂在管理的耐药病毒的选择：
在II期临床试验为227箱子抗逆转录病毒治疗经验的人，HIV蛋白酶抑制剂药物（PI）已经用一个例子来的主题，服用此药一段12-100周量化后的病毒载量（>400copies四例的患者中相比，在试验开始分离/毫升）分离物，易感性洛匹那韦已显著减少。这四个患者都在试验开始时的分离物，使用PI抗性相关的突变，观察至少四个位置。此外，病毒反弹后，在所有的菌株的突变数增加了，也包括带有PI抗性相关的突变。然而，在该药物的患者的施用，由于此时的数据不足的突变模式是不可能的，以确定是否由于洛匹那韦。
适应病症
HIV感染症
用法用量
成人：口服给药一次400毫克·饭后一天两次如洛匹那韦，利托那韦后100毫克一（5mL）中。
儿童：口服机身重量7kg高于每12毫克·3毫克1千克少多15千克，比40千克15千克更多每10毫克1公斤·在2.5mg的一餐，一天两次后，以下。最大剂量和管理为400mg·100毫克（5毫升），每日2次。
包装规格
组合口服液：160ML/瓶×1

制造厂商
艾伯维 GK（AVVI有限责任公司）
完整处方来源：http://www.info.pmda.go.jp/go/pack/6250101S1035_2_05/
Kaletra Combination Liquid for Internal Use（カレトラ配合内用液） 
Brand name : Kaletra Combination Liquid for Internal Use
　Active ingredient: Lopinavir/Ritonavir
　Dosage form: light yellow to orange clear solution
　Print on wrapping: 
Effects of this medicine
This medicine suppresses production/growth of human immunodeficiency virus (HIV) through inhibition of HIV protease activity by lopinavir and increase in the level of lopinavir in blood by ritonavir.
It is usually used to treat HIV infection.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
•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>>
•In general, for adults, take 5 mL at a time twice a day after meal.
In general, for children weighing 7 to 15 kg, take 0.15 mL per 1 kg of body weight, and for children weighing 15 to 40 kg, take 0.125 mL per 1 kg of body weight twice a day after meal. The maximum dose is 5 mL at a time twice a day. Strictly follow the instructions.
•If you miss a dose, take the missed dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose. You should never take two doses at one time.
•If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
•Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
•Avoid eating any food containing St. John's Wort with this medicine since it may increase metabolism of this medicine and diminish the effect of this medicine.
•This medicine contains ethanol. Be careful when operating dangerous machinery such as driving a car.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include diarrhea, nausea and abdominal pain. If any of these symptoms occur, consult with your doctor or pharmacist.
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.
•thirst, excessive drinking, polyuria [hyperglycemia, diabetes mellitus]
•vomiting, abdominal pain [pancreatitis]
•conditions that easily lead to bleeding, such as subcutaneous bleeding, nasal bleeding and bleeding gums [bleeding tendency (in patients with hemophilia)]
•general malaise, loss of appetite, yellowness of the skin or conjunctiva [hepatic dysfunction,hepatitis]
•shortness of breath, dizziness, chest discomfort [bradyarrhythmia]
•joint pain, conjunctival hyperemia of the eye [toxic epidermal necrolysis, erythema multiforme, mucocutaneous ocular syndrome]
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, and store this medicine in the refrigerator (at 2 to 8 degrees Celsius, and protect from light). In cases where this medicine is taken out of the refrigerator to be carried around, avoid temperatures of 25 degrees Celsius and above.
•Discard the remainder. Do not store them. Consult with your dispensing pharmacy or medical institution how to discard the medicine.
AbbVie GKInternal
Published: 3/2014
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.