英文药名: Isentress(Raltegravir Tablets)

中文药名: 整合酶抑制剂

生产厂家: Merck Frosst

药品简介

raltegravir片剂是FDA批准用于治疗艾滋病的新药。raltegravir片剂(Isentress)是默克公司生产的新型抗艾药物，获FDA批准与其它抗逆转录病毒药物联用于已接受过治疗但病毒仍在复制，且人免疫缺陷病毒-1(HIV-1)毒株对多种抗逆转录病毒药物耐药的成年患者治疗HIV-1感染。

商品名：整合酶抑制剂
英文名：Isentress(Raltegravir)
别名：L-900612，MK-051
研制公司：美国Merck公司

适应症：

与其他抗逆转录病毒药物联用，治疗那些经过其他药物治疗后仍发生病毒复制并且对多种抗逆转录病毒药物产生抗性的HIV感染者。

不良反应：

最常见的raltegravir相关性不良反应主要为恶心、头痛、腹泻、疲劳、瘙痒、便秘、出汗，较为温和，易于控制。

药理作用：

Raltegravir属于整合酶抑制剂，能通过阻止病毒DNA整合入宿主DNA而阻止病毒复制和感染新的细胞。整合酶抑制剂能更有效地阻止病毒的早期复制，从而阻止病毒库的产生。

药动学：
Raltegravir动物体内外的药动学研究显示，口服给药，最佳给药时间为每隔l2小时l次。对健康志愿者单剂量(100～1600mg)及多剂量(400～800mg)连续10d给与本品的药动学参数为：单剂量给药后，药物吸收迅速(tmax=0．5～1．3h)，体内二室模型分布，消除半衰期7～12h，生物利用度好，不受高脂饮食及性别的影响；多剂量给药两天后达到稳态血浆浓度。

临床研究：

临床试验表明，raltegravir对经过和未经高效抗逆转录病毒(HAART)治疗的患者均疗效显著。Ⅲ期临床试验结果显示，一天两次使用raltegravir和鸡尾酒疗法的病人中，未能检测到HIV的病人为60％；仅接受鸡尾酒疗法的病人中，未能检测到HIV的占35％。

ISENTRESS (raltegravir) tablet, film coated
ISENTRESS (raltegravir) tablet, chewable
[Merck Sharp & Dohme Corp.]
HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use ISENTRESS safely and effectively. See full prescribing information for ISENTRESS.
ISENTRESS® (raltegravir) Film-Coated Tablets, for oral use
ISENTRESS® (raltegravir) Chewable Tablets, for oral use
Initial U.S. Approval: 2007
RECENT MAJOR CHANGES
Indications And Usage
Dosage And Administration
Warnings And Precautions
Warnings And Precautions
INDICATIONS AND USAGE
ISENTRESS is a human immunodeficiency virus integrase strand transfer inhibitor (HIV-1 INSTI) indicated:
In combination with other antiretroviral agents for the treatment of HIV-1 infection
The safety and efficacy of ISENTRESS have not been established in children less than 2 years of age
DOSAGE AND ADMINISTRATION
ISENTRESS can be administered with or without food
ISENTRESS 400 mg film-coated tablets cannot be substituted with ISENTRESS 25 mg and 100 mg chewable tablets
Adults
400 mg film-coated tablet orally, twice daily
During coadministration with rifampin in adults, 800 mg twice daily
Children and Adolescents
12 years of age and older: One 400 mg film-coated tablet orally, twice daily 
6 to less than 12 years of age:
If at least 25 kg in weight:
One 400 mg film-coated tablet orally, twice daily OR
Chewable tablets: weight based to maximum dose 300 mg twice daily
If less than 25 kg in weight:
Chewable tablets: weight based to maximum dose 300 mg twice daily
2 to less than 6 years of age:
If at least 10 kg in weight:
Chewable tablets: weight based to maximum dose 300 mg twice daily 
DOSAGE FORMS AND STRENGTHS
Film-Coated Tablets: 400 mg .
Chewable Tablets: 100 mg scored and 25 mg .
CONTRAINDICATIONS None .
WARNINGS AND PRECAUTIONS
Severe, potentially life-threatening and fatal skin reactions have been reported. This includes cases of Stevens-Johnson syndrome, hypersensitivity reaction and toxic epidermal necrolysis. Immediately discontinue treatment with ISENTRESS and other suspect agents if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops and monitor clinical status, including liver aminotransferases closely .
Monitor for Immune Reconstitution Syndrome .
Inform patients with phenylketonuria that the 100 mg and 25 mg chewable tablets contain phenylalanine .
ADVERSE REACTIONS
The most common adverse reactions of moderate to severe intensity (≥2%) which occurred at a higher rate than the comparator are insomnia and headache  and.
Creatine kinase elevations were observed in subjects who received ISENTRESS. Myopathy and rhabdomyolysis have been reported. Use with caution in patients at increased risk of myopathy or rhabdomyolysis, such as patients receiving concomitant medications known to cause these conditions .
To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., at 1-877-888-4231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
DRUG INTERACTIONS
Coadministration of ISENTRESS with drugs that are strong inducers of UGT1A1 may result in reduced plasma concentrations of raltegravir
USE IN SPECIFIC POPULATIONS
Pregnancy:
ISENTRESS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus
Pregnancy registry available
Nursing Mothers:
Breastfeeding is not recommended while taking ISENTRESS
See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling 
Revised: 12/2011
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Isentress (Raltegravir)
Isentress (raltegravir) is a HIV medicine that keeps the infection under control and prevents it from spreading in your organism. It is very important to know that it cannot heal the HIV infection completely. As a matter of fact, the researchers are still working on finding the most appropriate treatment to cure it. So far, it can only be treated. Once infected, the patient will have to face the problematic symptoms for the rest of the life. The infection may also be detected in a severe case, when it is already evolved to AIDS. It doesn’t make any difference in the therapy.

The active substance is raltegravir and it is available on the market since 2007. Some tests are still ongoing and not conclusive enough. The drug can be used in monotherapy, as well as associated therapies with other HIV drugs.

Administration
The initial Isentress (raltegravir) dose for adults is 400mg. It is taken two times a day, with or without food. The effect of food over raltegravir is unknown yet, therefore don’t take any risks. Do not chew, crush or divide the tablets. Feel free to get a glass of water to help you in the process. When taken with rifampin, the dose is doubled up to 800mg.

Take the medicine exactly like your doctor prescribed. Do not adjust the dose if you find the effect too low or too powerful. Discuss with the doctor instead. Dose adjustments may be done on a regular basis, although such exceptions are quiet rare, mostly because the treatment is generalized.

Do not miss any of the consultations and appointments to your doctor. Your organism will be often checked for the doctor to determine whether the Isentress (raltegravir) tablets have a positive result or not. The effects of overdoses are unknown, so pay attention to your dose. Missing doses doesn’t cause life threatening symptoms, but call your doctor and ask for advice. They are quite risky though, since the HIV may have enough time to develop protection against the medication.

Contraindications
The simple fact that you are on a HIV treatment doesn’t mean that you or your partner are entirely protected. You will still need to protect yourself, as the infection is still transmitted.

Isentress (raltegravir) is not indicated in the people who present allergies to raltegravir or any other excipient.

Side effects
Some of the most frequent side effects to Isentress (raltegravir) include nausea, dizziness, drowsiness, diarrhea, vomiting or tiredness.