阿托喹酮在美国市场的商品名为Mepron，用于治疗卡氏肺孢子虫肺炎。它是葛兰素史克公司的用于治疗免疫系统受损的肺炎患者的抗原生动物药。Mepron（阿托伐醌）也用于治疗莱姆病。 MEPRON（阿托伐醌 atovaquone）口服混悬液 最初美国批准：1992年 作用机理 阿托伐醌是醌抗菌药物的[见临床药理]。 适应症和用法 MEPRON悬挂是表示醌抗菌药物的： •在成人和青少年年龄为13岁及以上谁不能耐受复方新诺明（TMP-SMX）肺囊虫肺炎（PCP）的预防。 •在成人和青少年年龄为13岁及以上谁不能耐受TMP-SMX轻度至中度PCP治疗。 使用限制（： •严重PCP治疗（肺泡动脉氧扩散梯度[（A-A）DO2]>45毫米汞柱）与MEPRON尚未研究。 •MEPRON在谁是失败与TMP-SMX治疗患者的疗效还没有研究。 用法用量 •预防PCP的：1500毫克（10毫升），每日一次食品 •PCP治疗：750毫克（5毫升），每日食物两次，持续21天 •在铝箔袋和瓶提供： •铝箔袋：对于一个5毫升的剂量，经口或者通过分配到勺子或杯子或直接放入口中采取全部内容。对于一个10毫升的剂量，需要两个袋。 •瓶：摇使用前轻轻瓶。 剂型和规格 口服混悬液：750每5ml。 禁忌症 已知严重过敏/过敏反应（例如，血管性水肿，支气管痉挛，喉密封性，荨麻疹），以阿托伐醌或任何MEPRON的组件。 警告和注意事项 •未能管理MEPRON悬浮液与食品可导致较低的血浆阿托伐醌的浓度，并可能限制对治疗的反应。患者胃肠道病症可具有导致次优的阿托伐醌的浓度有限的吸收。 •肝毒性：有报道肝升高化学测试和肝炎和致死性肝功能衰竭的病例。 不良反应 •PCP预防：最常见的不良反应为腹泻，皮疹，头痛，恶心，发热（即停药要求≥25％）。 •PCP治疗：最常见的不良反应（即停药要求≥14％），皮疹（包括斑丘疹），恶心，腹泻，头痛，呕吐和发热。 要报告疑似不良反应，请与葛兰素史克公司在1-888-825-5249或FDA电话1-800-FDA-1088或www.fda.gov/medwatch。 药物相互作用 •利福平或利福布丁同时服用阿托伐醌降低浓度;不建议用MEPRON悬挂同时使用。 •四环素同时服用阿托伐醌降低浓度;共同施用时要小心。监测患者MEPRON疗效的潜在损失，如果四环素合用是必要的。 •胃复安同时服用阿托伐醌降低浓度;伴随管理只有在其他止吐药不可用。 •茚地那韦同时服用茚地那韦降低谷浓度;共同施用时要小心。监测患者茚地那韦疗效的潜在损失，如果联合用药是必要的。 包装规格/储存与处理 MEPRON悬浮在5毫升（明亮的黄色，柑橘味）含有750毫克的阿托伐醌。 •210毫升防儿童帽（NDC0173-0665-18）瓶。商店在15°至25°C（59°至77°F）。不要冻结。分配在密封容器如USP定义。 •5毫升防止儿童开启的铝箔袋 - 42单位剂量包装（NDC0173-0547-00）。商店在15°至25°C（59°至77°F）。不要冻结。 Mepron(atovaquone)-Drug Summary GlaxoSmithKline LLC Mepron (atovaquone) THERAPEUTIC CLASS Naphthoquinone antiprotozoal DEA CLASS RX ADULT DOSAGE & INDICATIONS Pneumocystis Pneumonia Prevention of Pneumocystis jiroveci Pneumonia (PCP): 1500mg (10mL) qd Treatment of Mild to Moderate PCP: 750mg (5mL) bid for 21 days PEDIATRIC DOSAGE & INDICATIONS Pneumocystis Pneumonia ≥13 Years: Prevention of Pneumocystis jiroveci Pneumonia (PCP): 1500mg (10mL) qd Treatment of Mild to Moderate PCP: 750mg (5mL) bid for 21 days ADMINISTRATION Oral route Take w/ food Bottle Shake gently before administering the recommended dose Foil Pouch For 5mL, take entire contents PO either by placing directly into mouth or by dispensing into a dosing spoon (5mL) or cup prior to administration For 10mL, take entire contents of 2 pouches HOW SUPPLIED Sus: 750mg/5mL [5mL foil pouch, 42s; 210mL bottles] CONTRAINDICATIONS History of hypersensitivity reactions (eg, angioedema, bronchospasm, throat tightness, urticaria) to atovaquone or any of the components of this medication. WARNINGS/PRECAUTIONS Absorption is limited but can be significantly increased when taken w/ food; consider therapy w/ other agents in patients who have difficulty taking the drug w/ food or in patients who have GI disorders that may limit absorption of oral medications. Cases of cholestatic hepatitis, elevated liver enzymes, and fatal liver failure reported; closely monitor patients following administration if treating patients w/ severe hepatic impairment. ADVERSE REACTIONS Rash, N/V, diarrhea, cough, rhinitis, insomnia, fever, sweating, headache, sinusitis, pruritus, monilia (oral), depression, myalgia, flu syndrome. DRUG INTERACTIONS Decreased levels w/ rifampin or rifabutin; avoid concomitant use. Decreased levels w/ tetracycline; use w/ caution and monitor for potential loss of efficacy of atovaquone if coadministration of tetracycline is necessary. Decreased bioavailability w/ metoclopramide; use only if other antiemetics are not available. Decreased indinavir Ctrough; use w/ caution and monitor for potential loss of efficacy of indinavir if coadministration is necessary. PREGNANCY AND LACTATION Category C, caution in nursing. MECHANISM OF ACTION Naphthoquinone antiprotozoal; mechanism not fully understood. In Plasmodium species, the site of action appears to be cytochrome bc1 complex (Complex III). Inhibition of electron transport results in indirect inhibition of enzymes, which are linked to the mitochondrial electron transport chain, resulting in nucleic acid and adenosine triphosphate synthesis inhibition. PHARMACOKINETICS Absorption: Absolute bioavailability (47%); (500mg/day) AUC=280mcg•hr/mL (fed), 169mcg•hr/mL (fasting); (750mg bid) Cmax=24mcg/mL. Distribution: Vd=0.60L/kg (IV); plasma protein binding (99.9%). Elimination: Feces (>94%, unchanged), urine (<0.6%); T1/2=67-77.6 hrs. ASSESSMENT Assess for drug hypersensitivity, GI disorders, difficulty taking drug w/ food, severe hepatic impairment, pregnancy/nursing status, and possible drug interactions. MONITORING Monitor for cholestatic hepatitis, elevated liver enzymes, fatal liver failure, and other adverse reactions. PATIENT COUNSELING Instruct to take ud, to take daily doses w/ food, and to shake sus gently before use each time. STORAGE 15-25°C (59-77°F). Do not freeze. 原研药品的完整资料附件： 1）：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b426b6bf-f07e-4580-97ae-dfca1ddf5b8f 2）：https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=42750 --------------------------------------------------- 产地国家： 美国  原产地英文商品名: MEPRON oral suspension 210ML 750MG/5ML/bottle 原产地英文药品名: atovaquone 中文参考商品译名: MEPRON口服混悬液 210毫升 750毫克/5毫升/瓶 中文参考药品译名: 阿托喹酮 生产厂家中文参考译名: 葛兰素史克公司 生产厂家英文名: GlaxoSmithKline --------------------------------------------------- 产地国家： 美国  原产地英文商品名: MEPRON oral suspension 5ML/bag 42bag/box 原产地英文药品名: atovaquone 中文参考商品译名: MEPRON口服混悬液 5毫升/袋 42袋/盒 中文参考药品译名: 阿托喹酮 生产厂家中文参考译名: 葛兰素史克公司 生产厂家英文名: GlaxoSmithKline --------------------------------------------------- 产地国家： 美国  原产地英文商品名: atovaquone oral suspension 210mL 750mg/5mL/bottle 原产地英文药品名: atovaquone 中文参考商品译名: atovaquone口服混悬液 210毫升 750毫克/5毫升/瓶 中文参考药品译名: 阿托伐醌 生产厂家中文参考译名: Amneal 生产厂家英文名: Amneal Amneal was first-to-market with atovaquone oral suspension, USP, 750mg/5mL strength, an AB-rated therapeutic equivalent to GSK’s Mepron Oral Suspension. The product is used to treat Pneumocystis carinii pneumonia, common among patients with compromised immune systems.