ISENTRESS is an anti-HIV medicine used for the treatment of HIV. ISENTRESS must be used with other anti-HIV medicines, which may increase the likelihood of response to treatment. Isentress (Raltegravir, RAL) One 400 mg Isentress tablet should be taken, with or without food, twice a day (at the same time every morning and evening). Download Isentress 400 mg brochure. ** Attention ** This medication does not need to be taken with Norvir. Side effects The following minor side effects may often occur: •Nausea (headaches); •Vomiting. Important Information •Proper storage of the medication: ◦Do not store the medication in the bathroom; ◦Store the medication between 15 and 30 °C in a dark, dry area (away from light); ◦Never place the medication in a pillbox for longer than 24 hours, in order to prevent it from drying out; ◦Keep the medication out of reach of children. •If you miss a dose, avoid taking a double dose. Instead, wait until the next time you are supposed to take a pill and take a single dose of the medication, as prescribed by your physician. •The pill should be swallowed. Do not chew, crush or bite into it. •Avoid consuming alcohol at the same time as the medication, because this could cause liver damage. •Consult a health-care professional at a hospital, clinic, CLSC or pharmacy before consuming any natural health products (vitamins and minerals, medicinal plants, homeopathic remedies, probiotics, etc.); over-the-counter medications such as acetaminophen (Tylenol), ibuprofen (Advil, Motrin); or drops and syrups to treat coughs and sore throats (Benylin, Halls, Vicks, Cepacol, etc.) at the same time as the medication prescribed by your physician. •If you feel any discomfort or illness after taking your medication, immediately contact your physician. It is possible that the dosage or the medication itself is not suitable for you, in which case, your doctor will find an alternative.
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
适应证: 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%。
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