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欧盟批准Pegasys+Copegus为丙肝再治疗药物
罗氏表示，欧盟委员会已批准Pegasys+Copegus用作丙型肝炎患者的再治疗药物，这些患者通常在初期单用α干扰素或α干扰素+病毒唑（ribavirin）治疗后未达到预期目标。
这项批准拓宽了聚乙二醇干扰素α-2a类药物的应用范围，同时为接受过前期治疗但效果不佳的丙型肝炎患者的再治疗方案建立了最新标准，有望克服这种难以对付的病毒。
罗氏针对该药进行了一项名为REPEAT的临床实验，结果显示，那些起初采用PegIntron（聚乙二醇干扰素α-2b）和ribavirin治疗但无应答的患者转而使用聚乙二醇干扰素α-2a+病毒唑进行为期72周的再治疗之后基本痊愈，效果优于48周治疗期。此外，有57%的患者在用药12周之后即对药物产生应答，这部分患者在坚持治疗72周之后痊愈。
该公司制药部负责人表示，Pegasys+ Copegus的最新适应症表明了罗氏致力于开发慢性丙型肝炎治疗药的目标和决心。
药品英文名
Ribavirin
药品别名
奥得清、病毒唑、康立多、三氮唑核甙、三氮唑核苷、三唑核苷、威乐星、威利宁、酰胺三唑核苷、新博林、安替利、华东沙、Ribavirinum、RTC、Tribavirin、Virazole
药物剂型
1.片剂：20mg，50mg，100mg；
2.颗粒：50mg(复合膜袋装)，150mg(胶囊装)；
3.注射剂：100mg(1ml)，250mg(2ml)；
4.滴眼液：8mg(8ml)；
5.滴鼻液：50mg(10ml)。
药理作用
本药系广谱抗病毒药，作用机制尚未完全明确。为一种强的单磷酸次黄嘌呤核苷酸脱氢酶(IMP)抑制剂，抑制IMP，药物进入被病毒感染的细胞后迅速磷酸化，其产物作为病毒合成酶的竞争性抑制剂，抑制肌苷单磷酸脱氢酶、流感病毒RNA聚合酶和mRNA鸟苷转移酶，从而引起细胞内鸟苷三磷酸的减少，损害病毒RNA和蛋白合成，使病毒的复制与传播受抑。本药并不改变病毒的吸附、侵入和脱壳过程，也不诱导干扰素的产生。本药体外具抑制呼吸道合胞病毒、流感病毒、腺病毒等多种病毒生长的作用，进入体内对呼吸道合胞病毒也可能具免疫作用及中和抗体作用。
药动学
口服或吸入吸收迅速而完全，口服后1.5h血药浓度达峰值，约1～2mg/L。小儿每天以面罩吸药2.5h共3天，平均血药浓度峰值为0.2mg/L；每天吸药20h共5天，平均血药浓度峰值为1～7mg/L。本药生物利用度约45%，在呼吸道分泌物中的浓度大多高于血药浓度，与血浆蛋白几乎不结合。本药能进入红细胞内，积蓄量大且可积蓄数周。长期用药后脑脊液内药浓度可达同时期血药浓度的67%。药物可透过胎盘，也能进入乳汁。本药在肝内代谢。口服和静脉给药消除半衰期约为0.5～2h，吸入给药约为9.5h。主要经肾排泄。72～80h尿排泄率为30%～55%，72h粪便排泄率约15%。
适应证
1.主要用于腺病毒性肺炎的早期治疗及呼吸道合胞病毒(RSV)引起的病毒性肺炎与支气管炎。
2.用于流行性出血热和拉沙热的预防和治疗，发热早期应用本药能缩短发热期，减轻肾脏与血管损害及中毒症状。
3.本药滴眼液可治疗单纯疱疹病毒性角膜炎。
4.经静脉给药治疗由汉滩病毒(HANTAAN VIRUS)引起的出血热伴肾病综合征时，可有效地降低死亡率和减少少尿、出血发生的机率。
禁忌证
1.对本药过敏者。
2.孕妇。
3.自身免疫性肝炎患者。
4.肌酐清除率低于每分钟50ml的患者禁用本药口服制剂。
5.严重心脏病患者。
注意事项
1.慎用：
(1)血红蛋白病患者；
(2)心脏病患者。
2.药物对儿童的影响：
(1)由于药物可沉淀在呼吸器上，妨碍安全、有效地通气，因此施行辅助呼吸的婴儿不应采用本药气雾剂。
3.药物对老人的影响：老年人不宜使用本药。
4.药物对哺乳的影响：少量药物可由乳汁排泄，故乳母在用药期间需暂停哺乳。
5.口服或静脉给药引起血胆红素增高者可高达25%。大剂量可引起血红蛋白量下降。
不良反应
1.静脉或口服给药后较常见的不良反应有贫血、乏力等，停药后即消失。
2.较少见的不良反应有疲倦、头痛、失眠以及食欲减退、恶心等，多见于应用大剂量者。
3.少见的不良反应有结膜炎和低血压，表现为眼内异物感、怕光、瘙痒、红眼和水肿以及视力模糊、头晕、乏力等。
4.吸入用药时偶见皮疹，接触者可发生头痛、皮肤痒、皮肤发红、眼周水肿。
5.动物实验发现本药可诱发乳房、胰腺、垂体和肾上腺良性肿瘤，但对人体的致癌性并未肯定。
6.常见有口渴、思饮、腹泻、白细胞下降、血浆胆红素暂时性升高等，停药后恢复正常；剂量过大时可发生可逆性贫血；
7.偶见有AST、ALT升高。
用法用量
1.成人：
(1)口服给药：
①利巴韦林片：一般剂量：每天400～1000mg，分4次口服。疗程7～14天；
②利巴韦林颗粒：复合膜袋装或胶囊。病毒性上呼吸道感染：每次150mg，每天3次，连用7天。皮肤疱疹病毒感染：每次300mg，每天3～4次，连用7天。
(2)静脉滴注：每天500～1000mg，分2次给药。每次静脉滴注20min以上。疗程3～7天。治疗拉沙热、流行性出血热等严重病例时，首剂静脉滴注2000mg，继以每8小时500～1000mg，共10天。
(3)经眼给药：滴眼液浓度0.1%。
(4)经鼻给药：滴鼻液浓度0.5%。
(5)气雾吸入：每天吸入1000mg，此用法必须严格按照给药说明中所述气雾发生器的说明和给药方法进行。
2.儿童：
(1)口服给药：
①利巴韦林片：6岁及6岁以上小儿每天按体重10mg/kg，分4次服。疗程7～14天；6岁以下小儿口服剂量未定。
②利巴韦林颗粒：按体重计：每天10～15mg/kg，分3～4次服，连用7天。按年龄计：0.5～1岁，每次1袋(含利巴韦林50mg)；
③2～5岁，每次2袋(含利巴韦林100mg)；
④6～12岁，每次3袋(含利巴韦林150mg)。均为每天3次，用温开水溶解后服用，疗程7天。
(2)静脉滴注：每天按体重计为10～15mg/kg，分2次给药。每次静脉滴注20min以上。疗程3～7天。(3)气雾吸入：此用法必须严格按照给药说明中所述气雾发生器的说明和给药方法进行。给药浓度为20mg/ml，每天吸12～18h，疗程3～7天。对于呼吸道合胞病毒性肺炎和其他病毒感染，也可持续吸药3～6天；或每天3次，每次4h，疗程3天。
3.滴鼻：用于防治流感，用0.5%溶液(以等渗氯化钠溶液配制)，每小时1次。
4.滴眼：治疗疱疹感染，浓度0.1%，每天数次。
药物相应作用
1.与干扰素α-2b联用比两药单用能更好地降低丙型肝炎病毒RNA的浓度；而两药联用的安全性与两种药物单用的安全性相近。
2.与齐多夫定合用时可抑制后者转变成活性型的磷酸齐多夫定，从而降低后者药效。如果必须使用本药，可用其他抗反转录病毒制剂代替齐多夫定。
专家点评
本品为人工合成的广谱抗病毒药，是一种强力单磷酸次黄嘌呤核苷(IMP)脱氢酶抑制剂，可以抑制IMP，从而阻碍病毒核酸的合成。但对病毒无直接灭活作用。对流感病毒、腺病毒、麻疹病毒、疱疹病毒均有抑制作用。临床适用于病毒性上呼吸道感染、流感、副流感、乙脑、腮腺炎、水疱疹、带状疱疹、秋季腹泻、病毒性肺炎、生殖器疱疹、银屑病及小儿腺病毒性肺炎等均有特效，对出血热、乙型肝炎、甲型肝炎也有一定疗效。江西医学院对160例体温在38.5℃以上的急性上呼吸道病毒感染者采用随机、对照的方法，对其中100例应用利巴韦林葡萄糖注射剂静脉滴注，每次250ml含0.5g，每天2次，连续5天为1个疗程；对照组60例应用利巴韦林注射剂静脉滴注，每次5ml含0.5g，每天2次，疗程同上。结果两组的总有效率为97%和92%，病毒清除率为95%和96%，用药后两组患者体温降至正常。
国内报道，某医院应用利巴韦林与聚肌胞治疗带状疱疹的疗效进行比较，结果前者在缩短疼痛时间和总病程方面明显优于后者(P＜0.01)。某医院用利巴韦林及聚肌胞分别治疗流行性腮腺炎和水痘，利巴韦林组流行性腮腺炎78例，水痘28例。用药剂量5～7.5mg/kg，每天2次肌内注射，连续治疗3～6天。结果腮腺消肿时间为(4.3±1.9)天，水痘结痂时间为(3.6±1.6)天。聚肌胞组有流行性腮腺炎35例，水痘25例，用药剂量为1～2mg，肌内注射，隔日1次，治疗3～6天。结果腮腺消肿时间为(6±3)天，水痘结痂时间为(5.2±2.0)天。利巴韦林组显著优于聚肌胞组(P＜0.01及0.05)。江苏扬州市第一人民医院对120例婴幼儿轮状病毒肠炎患者在给予鞣酸铋合剂的基础上，其中90例加用口服利巴韦林，剂量依患儿年龄大小而增减。结果加服本品的总有效率为94.5%，不加服本品的30例组的总有效率为63.3%，两组差异显著(P＜0.01)。有报道对21例尖锐湿疣患者应用本品，肌内注射，每次0.3g，每天2次，连续7天，1周后应用激光CO2治疗，结果21例均治愈。
Copegus
Pronunciation: RYE-ba-VYE-rin
Generic Name: Ribavirin
Brand Name: Examples include Copegus and Ribasphere
Copegus is used for:
Treating chronic hepatitis C infection in certain patients when used in combination with peginterferon. It may also be used for other conditions as determined by your doctor.
Copegus is an antiviral medicine. Exactly how it works to treat hepatitis C is not known.
Do NOT use Copegus if:
you are allergic to any ingredient in Copegus or have had a severe allergic reaction (eg, red, swollen, blistered, or peeling skin) to ribavirin or any other ingredient in Copegus
you are pregnant or planning to become pregnant while you take Copegus or within 6 months after you stop taking it
you are a man with a female sexual partner who is pregnant or planning to become pregnant while you take Copegus or within 6 months after you stop taking it
you are breast-feeding
you have certain blood disorders (eg, hemolytic anemia, sickle cell anemia, thalassemia major), a history of serious or uncontrolled heart problems, or inflammation of the pancreas (acute pancreatitis)
you have autoimmune hepatitis (liver problems caused by your own body instead of a virus) or severely decreased liver function
you are taking didanosine
Contact your doctor or health care provider right away if any of these apply to you.
Before using Copegus:Some medical conditions may interact with Copegus.
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 have a female sexual partner who is of childbearing age
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 a history of cancer, heart problems or a heart attack, high blood pressure, kidney problems or if you are on dialysis, diabetes, pancreas problems, lung or breathing problems, sarcoidosis, blood problems (eg, anemia, spherocytosis), stomach or bowel bleeding, thyroid problems, psoriasis, HIV infection or other immune system problems, or eye or vision problems
if you have liver problems other than hepatitis C infection (eg, hepatitis B infection), cirrhosis of the liver, or decreased liver function
if you have a history of mood or mental disorders (eg, anxiety, depression, psychosis), thoughts of suicide, or suicidal behavior
if you have used interferon before to treat hepatitis C and it did not work
if you have a history of an organ transplant
if you have a history of drug or alcohol abuseSome MEDICINES MAY INTERACT with Copegus. Tell your health care provider if you are taking any other medicines, especially any of the following:
Didanosine or other nucleoside reverse transcriptase inhibitors (NRTIs) (eg, lamivudine), other antiretroviral medicines for HIV infection, or thiopurines (eg, azathioprine) because serious side effects, including risk of infection, nerve problems (peripheral neuropathy), pancreas problems, bone marrow suppression, lactic acidosis, and severe or fatal liver failure, may be increased by Copegus
Anticoagulants (eg, warfarin) or certain NRTIs (eg, lamivudine, stavudine, zidovudine) because their effectiveness may be decreased by Copegus
This may not be a complete list of all interactions that may occur. Ask your health care provider if Copegus 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 Copegus:
Use Copegus as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Copegus comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Copegus refilled.
Take Copegus by mouth with food.
Drinking extra fluids while you are taking Copegus is recommended. Check with your doctor for instructions.
Take Copegus on a regular schedule to get the most benefit from it. Taking Copegus at the same times each day will help you remember to take it.
Continue to take Copegus even if you feel well. Do not miss any doses.
If you miss a dose of Copegus and you remember the same day, take it as soon as possible.
If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once. Check with your doctor if you are unsure of what to do if you miss a dose.
Ask your health care provider any questions you may have about how to use Copegus.
Important safety information:
Copegus may cause drowsiness, dizziness, or blurred vision.
These effects may be worse if you take it with alcohol or certain medicines. Use Copegus with caution. Do not drive or perform other possibly unsafe tasks until you know how you
react to it.
Avoid drinking alcohol, including beer, wine, and liquor, because it could worsen liver disease.
At least 2 reliable forms of effective birth control must be used during treatment by men and women who take Copegus and for 6 months after Copegus is stopped. Men who take Copegus should use a condom with spermicide as 1 of the 2 forms of birth control.
Women of childbearing potential who either take Copegus or are sexual partners of men who take Copegus must have a pregnancy test before therapy with Copegus is started, monthly during therapy, and monthly for 6 months after Copegus is stopped.
Patients who take Copegus may be at increased risk of suicidal thoughts or actions. The risk may be greater in children or teenagers who have had suicidal thoughts or actions in the past. Watch patients who take Copegus closely.
Contact the doctor at once if new, worsened, or sudden symptoms such as depressed mood; aggression, anger, anxiety, nervousness, or irritable behavior; or any unusual change in
mood or behavior occur. Contact the doctor right away if any signs of suicidal thoughts or actions occur.
Copegus may lower the ability of your body to fight infection. Avoid contact with people who have colds or infections. Tell your doctor if you notice signs of infection like fever, sore throat, rash, or chills.
Copegus may cause dry mouth and increase the risk of teeth and gum problems. Proper dental care is important while you are taking it. Brush and floss your teeth and visit the dentist regularly.
If vomiting occurs while you are taking Copegus, be sure to rinse your mouth and clean your teeth afterwards.
Do NOT take more than the recommended dose or use for longer than prescribed without checking with your doctor.
Diabetes patients - Copegus may affect your blood sugar.
Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.
Lab tests, including pregnancy; complete blood cell counts; hemoglobin or hematocrit levels; heart, liver, kidney, thyroid, and lung function; and eye exams, may be performed while you use Copegus. These tests may be used to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.
Use Copegus with caution in the ELDERLY; they may be more sensitive to its effects, especially anemia.
Copegus may affect growth rate in CHILDREN and teenagers in some cases. They may need regular growth checks while they take Copegus.
Copegus should be used with extreme caution in CHILDREN younger than 18 years old; safety and effectiveness in these children have not been confirmed.
PREGNANCY and BREAST-FEEDING: Do not use Copegus if you are pregnant. It has been shown to cause harm to the fetus. Avoid becoming pregnant while you are taking it.
If you think you may be pregnant, contact your doctor right away. It is not known if Copegus is found in breast milk. Do not breast-feed while taking Copegus.
Possible side effects of Copegus: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:Cough; diarrhea; dizziness; dry mouth; dry skin; hair loss; joint pain; loss of appetite; mild headache, nausea, or vomiting; mild stomach pain; sinus problems; tiredness; trouble sleeping; upset stomach; weakness or fatigue.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness; wheezing); bloating of the stomach; changes in hearing, taste, or vision; chest pain; confusion; dark, tarry, or bloody stools; dark urine; decrease in the amount of urine; fainting; fever, chills, or sore throat; hearing loss; irregular heartbeat; menstrual problems; mood or mental problems (eg, agitation, aggression, anger, anxiety, decreased concentration, depression, irritability, memory problems, nervousness); muscle pain or weakness; numbness of an arm or leg; pale stools; persistent loss of appetite; rapid breathing; rash with blisters or sores in your mouth, nose, or eyes; red, swollen, blistered, or peeling skin; severe or persistent diarrhea, nausea, or vomiting; severe or persistent headache or dizziness; severe stomach or back pain; shortness of breath; suicidal thoughts or actions; unusual bruising or bleeding; unusual or severe tiredness, weakness, or fatigue; vomit that looks like coffee grounds; weight loss; worsening psoriasis; yellowing of the eyes or skin.
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. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.If OVERDOSE is suspected:Contact 1-800-222-1222 (the American Association of Poison
Control Centers), your local poison control center, or emergency room immediately.
Proper storage of Copegus: Store Copegus between 59 and 86 degrees F (15 and 30 degrees
C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Copegus out of the reach of children and away from pets.
General information:
If you have any questions about Copegus, please talk with your doctor, pharmacist, or other health care provider.
Copegus is to be used only by the patient for whom it is prescribed. Do not share it with other people.
If your symptoms do not improve or if they become worse, check with your doctor.
Check with your pharmacist about how to dispose of unused medicine.
This information is a summary only. It does not contain all information about Copegus. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.
附件：
20121417405540.pdf
20121417405114.pdf
20121417404537.PDF
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产地国家: 美国
原产地英文商品名:
COPEGUS 200毫克/片 168片/瓶
原产地英文药品名:
RIBAVIRIN
中文参考商品译名:
COPEGUS 200MG/TAB 168TABS/BTL
中文参考药品译名:
利巴韦林
生产厂家中文参考译名:
罗氏
生产厂家英文名:
ROCHE
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