RAPIVAB(PERAMIVIR)SOLUTION IV (INFUSION)是第一个神经氨酸酶抑制剂被批准为静脉(IV)给药 日前，美国食品药品管理局FDA批准抗病毒药物Rapivab用于治疗成年流感患者。Rapivab是BioCryst制药公司研制的一种神经氨酸苷酶抑制剂（NI）。 它是FDA批准的第三种治疗流感的NI。阿拉巴马大学Richard Whitley表示，Rapivab是第一种被证实安全有效的单剂量NI，也是15年来FDA批准的一种全新的流感抗病毒治疗方法。 批准日期： 2014年12月19日；公司： BioCryst 制药公司。 RAPIVAB(帕拉米韦peramivir)为静脉注射使用 Rapivab® (peramivir injection) is indicated for the treatment of acute uncomplicated influenza in patients 18 years and older who have been symptomatic for no more than 2 days. ■Efficacy of Rapivab was based on clinical trials in which the predominant influenza virus type was influenza A; a limited number of subjects infected with influenza B virus were enrolled. ■Influenza viruses change over time. Emergence of resistance substitutions could decrease drug effectiveness. Other factors (for example, changes in viral virulence) might also diminish clinical benefit of antiviral drugs. Prescribers should consider available information on influenza drug susceptibility patterns and treatment effects when deciding whether to use Rapivab. ■Efficacy could not be established in patients with serious influenza requiring hospitalization. RAPIVAB Rx Pharmacological Class: Neuraminidase inhibitor. Active Ingredient(s): Peramivir 10mg/mL; per vial; solution for IV injection after dilution; preservative-free. Company BioCryst Pharmaceuticals, Inc. Indication(s): Treatment of acute uncomplicated influenza in patients who have been symptomatic for ≤2 days. Limitations of use: Efficacy based on predominantly influenza A virus infections; limited number of influenza B virus subjects enrolled. Consider available information on influenza drug susceptibility patterns and treatment effects when deciding whether to use. Efficacy not established in serious influenza requiring hospitalization. Pharmacology: Peramivir inhibits influenza virus neuraminidase, an enzyme that releases viral particles from the plasma membrane of infected cells. The antiviral activity of peramivir against laboratory strains and clinical isolates of influenza virus was determined in cell culture. The concentrations of peramivir required for inhibition of influenza virus in cell culture varied depending on the assay method used and the virus tested. The relationship between the antiviral activity in cell culture, inhibitory activity in the neuraminidase assay, and the inhibition of influenza virus replication in humans has not been established. Clinical Trials: Study 621 was a randomized, multi-center, blinded trial conducted in Japan that evaluated a single IV administration of Rapivab 300mg, 600mg, or placebo given over 30 minutes in patients 18–65 years of age with acute uncomplicated influenza. Treatment was initiated within 48 hours of onset of symptoms. The primary endpoint, time to alleviation of symptoms, was defined as the number of hours from study drug initiation until the start of the 24-hour period in which all 7 symptoms of influenza (cough, sore throat, nasal congestion, headache, feverishness, myalgia, and fatigue) were either absent or present at a level no greater than mild for at least 21.5 hours. Overall, patients receiving Rapivab 600mg experienced alleviation of their combined influenza symptoms a median of 21 hours earlier than those receiving placebo. The median time to recovery to normal temperature (<37°C) in the Rapivab 600mg group was about 12 hours earlier as compared with placebo. Study 301 was a randomized, double-blind, multi-center, placebo-controlled trial in patients with serious influenza requiring hospitalization (n=398). Patients were randomized to receive Rapivab 600mg daily for 5 days plus standard of care (which could include other neuraminidase inhibitors [eg, oseltamivir]) vs. placebo plus standard of care within 72 hours of symptom onset. The primary endpoint was time to clinical resolution defined as the time in hours from initiation of study treatment until resolution of at least 4 of 5 signs (temperature, oxygen saturation, respiration rate, heart rate, or systolic blood pressure), maintained for at least 24 hours. Rapivab plus standard of care did not improve median time to clinical resolution compared with standard of care alone. For more clinical trial data, see full labeling. Legal Classification: Rx Adults: Start within 2 days of symptom onset. Give as IV infusion over 15–30 minutes. ≥18 years: 600mg as a single dose. Renal impairment (CrCl 30–49mL/min): 200mg; (CrCl 10–29mL/min): 100mg; (on hemodialysis): administer after dialysis. Children: <18 years: not established. Warnings/Precautions: Serious skin/hypersensitivity reactions (eg, erythema multiforme, Stevens-Johnson syndrome): treat as appropriate if occur or is suspected. Monitor closely for signs of abnormal behavior. Risk of secondary bacterial infections; treat as appropriate. Pregnancy (Category C). Nursing mothers. Interaction(s) Do not administer live attenuated influenza vaccine within 2 weeks prior or 48 hours after treatment. Adverse Reaction(s) Diarrhea; neuropsychiatric events (eg, hallucinations, delirium, abnormal behavior); serious skin reactions. How Supplied: Single-use vials (20mL)—3 LAST UPDATED: 3/19/2015 完整治疗资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7fdedaec-9e53-4a37-a4e4-a301c8a251b8 12月19日，美国FDA批准BioCryst制药帕拉米韦(商品名：Rapivab)用于治疗成人患者流感。流感是由流感病毒引起的一种传染性呼吸道疾病。流感的病情可由轻到重，有时会导致住院甚至死亡。据美国疾病控制与预防中心(CDC)称，每年5-20%的美国人群会得流感，超过20万人会因季节性流感并发症而住院。 帕拉米韦是属于流感病毒神经氨酸酶抑制剂，神经氨酸酶是一种可从感染细胞释放病毒粒子的酶。神经氨酸酶抑制剂通常用来治疗流感。帕拉米韦是首款获批的静脉注射用神经氨酸酶抑制剂，作为单次静脉注射使用。这款药物适用于18岁及以上年龄患有急性无并发症流感并仅有两天流感症状的患者。 “帕拉米韦是FDA批准用于治疗流感的第三款神经氨酸酶抑制剂，但是首款以静脉注射剂型获批的该类药物，”FDA药物评价与研究中心抗微生物产品办公室主任、医学博士、公共卫生学硕士Cox称。“急性无并发症流感的单一剂量静脉注射治疗药物可以允许卫生保健专业人员及患者根据个体患者需求而拥有一个选择。” FDA批准治疗流感的其它神经氨酸酶抑制剂有奥司他韦（口服）和扎那米韦（吸入）。用于流感的抗病毒老药金刚烷胺与金刚乙胺不再被CDC推荐，因为正在传播的流感病毒株对这些药物耐药。 帕拉米韦的有效性基于297名确诊患有流感的受试者，他们被随机配给帕拉米韦300mg、帕拉米韦600mg或安慰剂。总之，以帕拉米韦治疗的受试者与安慰剂治疗患者相比，其合并流感症状得到缓解平均快了21小时，这与同类药物中的其它药物一致。 以帕拉米韦600mg剂量治疗的受试者与安慰剂治疗受试者相比，其体温恢复到正常快了大约12个小时。支持性试验证实了这些结果。但对需要住院的严重流感患者的疗效不能确定。 在帕拉米韦治疗受试者中观察到的最常见副作用是腹泻。罕见但严重副作用有严重皮肤或过敏反应，如史蒂文斯—约翰逊综合征和多形性红斑。 患有流感的患者在疾病早期可能处于幻觉升高、谵妄和行为异常的风险中。这些事件已在神经氨酸酶抑制剂使用中有报道，但尚不清楚这款药物引起的异常行为。 帕拉米韦及其它用于治疗流感的抗病毒药物不是每年流感疫苗的替代品，如CDC免疫实践顾问委员会所建议的那样。CDC建议所有6个月及以上年龄的人每年注射流感疫苗。帕拉米韦由位于北卡罗来纳州达勒姆的BioCryst制药生产。