通用名称为AFINITOR
依维莫司2.5mg，5毫克，10毫克。
法律分类：
接收
类药物为AFINITOR
mTOR激酶抑制剂。
制造商的AFINITOR
诺华制药公司
主治为AFINITOR
进神经内分泌肿瘤起源于不能手术切除的局部晚期或转移性疾病患者的胰腺癌（PNET）。舒尼替尼或索拉非尼治疗失败后晚期肾细胞癌（RCC）。室管膜下巨细胞星形细胞瘤（SEGA）与结节性硬化症的患者需要干预治疗，但不用于治疗手术切除候选人。
成人剂量为AFINITOR
燕子整个水或分散于水30ml片剂，并立即饮用。在每天同一时间采取要么始终没有食物。 PNET或RCC：10毫克，每日一次。中度肝功能不全（Child - Pugh分级B级），或不良反应：减少至5mg，每日一次。伴随中度CYP3A4或P -糖蛋白抑制剂：降低到2.5mg，每日一次，可考虑增加至5mg，如果容忍。如果中度抑制剂停产，允许前2-3天洗脱期增加everolimus的剂量;返回剂量使用开始前的中度抑制剂。伴随强CYP3A4诱导剂：从10 - 20毫克可能会增加增量为5mg，每日一次。如果强有力的诱导剂是停产了，应该返回到发起强烈的诱导之前使用的剂量。世嘉：牛血清白蛋白<0.58平方米：不推荐。最初：牛血清白蛋白：0.5 -1.2平方米：2.5mg，每日一次; 1.32.1平方米：5毫克，每日一次;≥2.2平方米：7.5mg，每日一次。评估SEGA体积约。 3个月后开始治疗并在此后定期调整剂量，可能会在2周的时间间隔。谷浓度应评估每2周，剂量应逐步达到的5-10ng/mL浓度（见文献）。严重不良反应：暂时减少剂量或中断治疗;考虑为患者接受2.5mg每日隔日给药。伴随强CYP3A4抑制剂：避免，中度CYP3A4和/或PGP抑制剂：减少50％的剂量，如果CYP3A4和/或PGP抑制剂停产，返回到之前使用启动中度抑制剂的剂量。伴随强CYP3A4诱导剂：避免，如果需要的话，然后依维莫司的剂量加倍;如果停止，然后返回到发起强烈的诱导前使用的剂量。对于所有的继续，只要有利于观察或直到出现不可接受的毒性。
儿童剂量为AFINITOR
PNET或RCC：不推荐。世嘉：<3岁：不推荐。
禁忌症为AFINITOR
temsirolimus的，西罗莫司，雷帕霉素过敏。
为AFINITOR警告/注意事项
严重肝功能不全（Child - Pugh分级C类）：不推荐。中度肝功能损害：减少剂量。感染的风险增加，有的可能是严重的或致命的。预先存在的侵入性真菌感染：治疗开始之前。 CBCS：监视器，肾功能，血脂，血糖，肺炎和感染治疗及时出现。生育能力的妇女，应使用期间和多达8个星期治疗后有效的避孕方法。 （Cat.D）怀孕，哺乳期的母亲：不建议。
为AFINITOR的相互作用
避免使用活疫苗。 Potentiated强CYP3A4抑制剂，或P -糖蛋白抑制剂;避免（如酮康唑，伊曲康唑，克拉霉素，阿扎那韦，奈法唑酮，沙奎那韦，泰利霉素，利托那韦，茚地那韦，奈非那韦，伏立康唑，西柚汁）。中度CYP3A4抑制剂（如安普那韦，fosamprenavir，阿瑞吡坦，红霉素，氟康唑，维拉帕米，地尔硫卓）或P -糖蛋白抑制剂的注意事项;减少everolimus的剂量，如果使用。拮抗强CYP3A4诱导剂;避免（如苯妥英钠，卡马西平，利福平，利福布丁，利福喷丁，苯巴比妥，圣约翰草）;增加everolimus的剂量，如果使用。
AFINITOR的不良反应
性肺炎（减少剂量和/或管理与皮质类固醇），感染（中止如果侵入全身性真菌感染的发展），口腔炎（治疗非酒精，非双氧水漱口水），胃肠不适，皮疹，乏力，发热，头痛，乏力，咳嗽;增加血清肌酐，血糖，血脂，血红蛋白下降，血小板，中性粒细胞，血清磷酸盐;肾功能衰竭，其他人（见文献）。
AFINITOR是如何提供的？
标签- 28（4吸塑卡× 7制表符）
Generic Name for AFINITOR
Everolimus 2.5mg, 5mg, 10mg; tabs.
Legal Classification:
Rx
Pharmacological Class for AFINITOR
mTOR kinase inhibitor.
Manufacturer of AFINITOR
Novartis Pharmaceuticals Corp
Indications for AFINITOR
Progressive neuroendocrine tumors of pancreatic origin (PNET) in patients with unresectable, locally advanced or metastatic disease. Advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis in patients who require therapeutic intervention but are not candidates for curative surgical resection.
Adult dose for AFINITOR
Swallow whole with water or disperse tablet in 30mL of water and drink immediately. Take at the same time each day either consistently with or without food. PNET or RCC: 10mg once daily. Moderate hepatic dysfunction (Child-Pugh class B), or adverse reactions: reduce to 5mg once daily. Concomitant moderate CYP3A4 or P-glycoprotein inhibitors: reduce to 2.5mg once daily; may consider increasing to 5mg if tolerated. If moderate inhibitor is discontinued, allow 2–3 days washout period before increasing everolimus dose; return to dose used prior to initiating the moderate inhibitor. Concomitant strong CYP3A4 inducers: may increase from 10–20mg once daily by increments of 5mg. If strong inducer is discontinued, should return to dose used prior to initiating the strong inducer. SEGA: BSA< 0.58m2: not recommended. Initially: BSA: 0.5–1.2m2: 2.5mg once daily; 1.3–2.1m2: 5mg once daily; ≥2.2m2: 7.5mg once daily. Evaluate SEGA volume approx. 3 months after starting therapy and periodically thereafter; dose adjustments may be made at 2 week intervals. Trough concentrations should be assessed every 2 weeks, dosing should be titrated to attain a concentration of 5–10ng/mL (see literature). Severe adverse reactions: temporarily reduce dose or interrupt therapy; consider alternate day dosing for patients receiving 2.5mg daily. Concomitant strong CYP3A4 inhibitors: avoid; moderate CYP3A4 and/or PgP inhibitors: reduce dose by 50%, if CYP3A4 and/or PgP inhibitor discontinued, return to dose used prior to initiating moderate inhibitor. Concomitant strong CYP3A4 inducers: avoid, if required, then double dose of everolimus; if discontinued, then return to dose used prior to initiating strong inducer. For all: continue as long as benefit observed or until unacceptable toxicity occurs.
Children's dosing for AFINITOR
PNET or RCC: not recommended. SEGA: <3yrs: not recommended.
Contraindications for AFINITOR
Sirolimus, temsirolimus, rapamycin allergy.
Warnings/Precautions for AFINITOR
Severe hepatic impairment (Child-Pugh class C): not recommended. Moderate hepatic impairment: reduce dose. Increased risk of infections; some may be severe or fatal. Pre-existing invasive fungal infections: treat before starting. Monitor CBCs, renal function, lipids, blood glucose, and for pneumonitis and infections: treat promptly if occur. Women of childbearing potential should use effective method of contraception during and up to 8 weeks after treatment. Pregnancy (Cat.D), nursing mothers: not recommended.
Interactions for AFINITOR
Avoid live vaccines. Potentiated by strong CYP3A4 inhibitors, or P-glycoprotein inhibitors; avoid (eg, ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole, grapefruit juice). Caution with moderate CYP3A4 inhibitors (eg, amprenavir, fosamprenavir, aprepitant, erythromycin, fluconazole, verapamil, diltiazem) or P-glycoprotein inhibitors; reduce everolimus dose if used. Antagonized by strong CYP3A4 inducers; avoid (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital, St. John's wort); increase everolimus dose if used.
Adverse Reactions for AFINITOR
Pneumonitis (reduce dose and/or manage with corticosteroids), infections (discontinue if invasive systemic fungal infection develops), stomatitis (treat with non-alcoholic, non-peroxide mouthwash), GI upset, rash, fatigue, fever, headache, asthenia, cough; increased serum creatinine, blood glucose, lipids; decreased hemoglobin, platelets, neutrophils, serum phosphate; renal failure, others (see literature).
How is AFINITOR supplied?
Tabs—28 (4 blister cards x 7 tabs)