英文药名: Lexiva(Fosamprenavir Tablets)

中文药名: 福沙那伟片

品牌药生产厂家: Glaxo Smith Kline

药品简介

福沙那韦钙是FDA批准用于抗人类免疫缺陷病毒(HIV)感染的新药,是用于控制HIV感染的蛋白酶抑制药类新药,可抑制HIV病毒蛋白酶,降低病毒载量,提高CD+4细胞计数。
2009年12月3日，美国食品药品管理局（FDA）和葛兰素史克公司(GSK)发布了一条有关成人人类免疫缺陷病毒(HIV)感染者应用Lexia(福沙那韦)与心肌梗死(MI)和血脂异常之间存在潜在相关性的通告。Lexiva适宜与其他抗逆转录病毒药物联用治疗HIV感染。
生产厂家对Lexiva处方信息中现有的警告和注意事项栏目进行了修改，指出应用该药治疗可导致胆固醇水平升高情况的发生。此外，还强调了控制血脂的重要性，而且说明书中还建议在开始Lexiva治疗前以及治疗期间进行定期甘油三酯和胆固醇检测。
GSK还在Lexiva片剂和口服悬液处方信息的不良反应中增加了MI和高胆固醇血症。2009年2月的国际HIV大会上公布了法国医院HIV数据库中的一项病例对照研究的数据。该研究由欧洲药品评审局(European Medicines Evaluation Agency)倡导，旨在分析应用特异性核苷酸反转录酶抑制剂及蛋白酶抑制剂对MI风险的影响。研究员报告指出，研究发现，福沙那韦/安普那韦累积用药与MI风险增加有关(风险比值比，1.52/增加1年用药；95%可信区间，1.19~1.95)。
GSK公司在向医护专业人员发布的这项最新通告中表示，MI已被确定为蛋白酶抑制剂类药物的常规信号。GSK宣称，所报告的相关性本身看似有据可循，可能与这类药物促进血脂水平升高的特性有关。生产厂家同时还提醒处方者，HIV感染本身就一直与血脂代谢异常和缺血性心脏病有关联。

 LEXIVA（福沙那伟钙）片剂，薄膜包衣

最初美国批准：2003年

适应症

LEXIVA是一种HIV蛋白酶抑制剂与其他抗逆转录病毒药物治疗HIV-1感染的组合表示。
 
剂量和用法

朴素治疗成人：LEXIVA 1,400毫克的两倍; LEXIVA 1400毫克后，每天加利托那韦200 mg，每天一次; LEXIVA 1400毫克后，每天加利托100毫克，每天一次; LEXIVA 700毫克，每天两次加利托100毫克每日两次。
蛋白酶抑制剂，经验丰富的成年人：LEXIVA 700毫克，每天两次加利托那韦100 mg，每天两次。
儿科患者（2至18岁）：剂量应根据体重（公斤）计算，不得超过成人剂量。
肝功能不全：轻度，中度或重度肝功能不全患者推荐的调整。
计量的思考

LEXIVA片可采取或没有食物。

LEXIVA悬架：成年人应采取无食品;儿童患者应采取与食物。
 
剂型和优势

700毫克片剂和50毫克/毫升口服混悬液

禁忌

过敏性到LEXIVA或安普那韦（例如，Stevens-Johnson综合征）。
药物高度依赖于CYP3A4的间隙和血浆水平升高，可能会导致严重的和/或危及生命的事件。

注意事项：

不应该被某些药物并用LEXIVA由于严重或危及生命的不良反应的风险。
LEXIVA应停止严重的皮肤反应，包括Stevens-Johnson综合征。 LEXIVA应采用与已知的磺胺类药物过敏患者慎用。
高于批准的剂量使用，可能会导致转氨酶升高。 B或C型肝炎患者在转氨酶升高的风险增加。
患者接受LEXIVA可能开发新的糖尿病发病或病情加重，高血糖，免疫重建综合征，体内脂肪的再分配/积累，升高的甘油三酯和胆固醇浓度。前治疗和其后定期监测胆固醇和甘油三脂。
安普那韦已报告急性溶血性贫血。
血友病：可能发生自发性出血，和额外的第八因子可能需要。
肾结石：肾结石病例已福沙那伟报道。

不良反应

在成人中最常见的不良反应（发生率大于或等于4％），腹泻，皮疹，恶心，呕吐，头痛。
呕吐是比成人更经常在儿科。

药物相互作用

可能会降低，诱导CYP3A4的药物合用LEXIVA安普那韦（活性代谢物）的浓度导致病毒学活动的潜在损失。
抑制CYP3A4的药物合用可能增加安普那韦的浓度。
LEXIVA和利托那韦合用，可能会导致由CYP2D6代谢的药物在临床上显着的相互作用。

日期：03/2012

Lexiva(Fosamprenavir Calcium) 700 mg 60 tablets

Lexiva is an HIV medication. It is in a category of HIV medicines called protease inhibitors (PIs). Lexiva prevents cells infected by HIV from producing new virus. This reduces the amount of virus in your body.

In some parts of the world, fosamprenavir is sold under the brand name Telzir.

Lexiva must be used in combination with other HIV drugs. Along with other medications, Lexiva is often combined with low doses of Norvir (ritonavir), another protease inhibitor used to boost the amount of Lexiva in the bloodstream (which makes Lexiva more effective against HIV, including drug-resistant HIV, and easier to take).

Based on what we know about the drug interactions with Lexiva, it is likely that other HIV drugs can interact with Lexiva. HIV protease inhibitors can interact with Lexiva. Norvir (ritonavir), Kaletra (lopinavir/ritonavir), Reyataz (atazanavir), Crixivan (indinavir), and Viracept (nelfinavir) may all increase Lexiva levels in the bloodstream. An increased rate of side effects have been seen when people combine Lexiva with Kaletra, and the two should not be used together. Invirase (saquinavir) may decrease the amount of Lexiva in the bloodstream, and studies have not established a safe way to combine Invirase and Lexiva.

HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs) can also interact with Lexiva. Sustiva (efavirenz) and Viramune (nevirapine) may decrease the amount of Lexiva in the bloodstream. Rescriptor (delavirdine), can increase levels of Lexiva in the bloodstream. No dosing recommendations have been made, although low-dose Norvir may be necessary if Viramune is combined with Lexiva. An additional 100mg (total 300mg) of Norvir may be needed if Lexiva is used once-daily with Sustiva. No additional Norvir is recommended if Lexiva is dosed twice-daily. Using Lexiva with either Rescriptor or Intelence is not recommended.

Short-term side effects include rash, appetite loss, headaches, feeling crummy (malaise), diarrhea, nausea, and vomiting. While these are the same side effects caused by Agenerase, many are less common with Lexiva. Very often, these side effects improve within a few months/weeks of starting Lexiva.

Severe, life-threatening rashes have been documented with Lexiva. People with a moderate rash and other allergic symptoms, and people with severe rashes should stop taking Lexiva.

HIV drug regimens containing protease inhibitors, including Lexiva, can cause increased fat levels (cholesterol and triglycerides) in the blood, abnormal body-shape changes (lipodystrophy; including increased fat around the abdomen, breasts, and back of the neck, as well as decreased fat in the face, arms, and legs), and diabetes.

Generic Name for LEXIVA
Fosamprenavir (as calcium) 700mg; tabs; (prodrug of amprenavir).

Legal Classification:
Rx

Pharmacological Class for LEXIVA
HIV-1 protease inhibitor.

Manufacturer of LEXIVA
GlaxoSmithKline Pharmaceuticals

Indications for LEXIVA
HIV-1 infection.

Adult dose for LEXIVA
Oral susp: take without food; if emesis occurs within 30 minutes after dosing, re-dose. Therapy-naive: 1.4g twice daily; or fosamprenavir 1.4g + ritonavir 200mg once daily; or fosamprenavir 1.4g + ritonavir 100mg once daily; or fosamprenavir 700mg + ritonavir 100mg twice daily. Protease-inhibitor-experienced: fosamprenavir 700mg + ritonavir 100mg twice daily. Hepatic dysfunction: see literature for dose adjustments.

Children's dosing for LEXIVA
<2yrs: not recommended. Oral susp: take with food; if emesis occurs within 30 minutes after dosing, re-dose. Therapy-naive: 2–5yrs: 30mg/kg twice daily. ≥6yrs: fosamprenavir 30mg/kg twice daily; or fosamprenavir 18mg/kg + ritonavir 3mg/kg twice daily. Therapy-experienced: ≥6yrs: fosamprenavir 18mg/kg + ritonavir 3mg/kg twice daily. For all: do not exceed the adult dosage (see literature). Alternative oral tabs regimen: see literature.

Also:
LEXIVA ORAL SUSPENSION

Contraindications for LEXIVA
Concomitant cisapride, pimozide, ergots, midazolam, triazolam, possibly others; see literature. Concomitant flecainide, propafenone, or oral contraceptives with ritonavir-boosted fosamprenavir. St. John's wort, rifampin, lovastatin, simvastatin, delavirdine: not recommended.

Warnings/Precautions for LEXIVA
Sulfonamide allergy. Hepatic impairment: see literature. Do not exceed recommended dose. Discontinue if severe rash occurs. Monitor lipids, liver function, and for fat redistribution and hyperglycemia. Hemophilia: monitor for spontaneous bleeding. Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interactions for LEXIVA
See Contraindications. Life-threatening arrhythmias possible with bepridil. Concomitant nevirapine without ritonavir: not recommended. Reduce rifabutin dose by at least ½ (or by 75% if with ritonavir) and monitor for neutropenia (do weekly CBCs). Potentiates sildenafil, tadalafil, vardenafil; reduce doses of these. May potentiate fluticasone (consider alternative therapy), trazodone (reduce trazodone dose). Monitor amiodarone, anticonvulsants (eg, phenytoin), H2 blockers, immunosuppressants, lidocaine (systemic), quinidine, tricyclics, warfarin, drugs that affect or are affected by CYP3A4 (eg, azole antifungals, benzodiazepines, calcium channel blockers, macrolides, NNRTIs, protease inhibitors, statins, steroids). May antagonize, or be antagonized by antacids, hormonal contraceptives (use non-hormonal methods), methadone.

Adverse Reactions for LEXIVA
GI upset, headache, rash (may be serious, eg, Stevens-Johnson), fat redistribution, depression, fatigue, hypertriglyceridemia, elevated liver enzymes, immune reconstitution syndrome, vomiting (esp. children).

Notes for LEXIVA
Register pregnant patients exposed to fosamprenavir by calling (800) 258-4263.

How is LEXIVA supplied?
Tabs—60; Susp—225mL

Related Disease:
HIV~antivirals
规格：700mg *60 片