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ID #1024

力比泰(ALIMTA)中文说明书

    力比泰现在主要看来是用在化疗失败、易瑞沙耐药后的药品,分为进口、国产、印度仿造三种,国产和进口的价格都非常昂贵,仿造的能拿到的价格在6000(两支的价格,单只3000元,因为一支不够用,两支富裕一点)。

  力比泰(注射用培美曲塞) [ 药品名称 ]

  力比泰(注射培美曲塞) 通 用 名: 注射用培美曲塞
  商 品 名: 英文: ALIMTA
  中文:力比泰
  英 文 名: Pemetrexed disodium for Injection
  汉语拼音: Zhu She Yong Pei Mei Qu Sai Er Na
  本品主要成分为培美曲塞二钠,其化学名称为: 谷氨酸, N -[4-[2-(2- 氨基 -4,7- 二氢 -4- 氧 -1H- 吡咯并 [2,3-d] 嘧啶 -5- 烷基 ) 乙基 ] 苯甲酰基 ]- , 二钠盐, 七水合物
  其结构式为:
  分子式: C 20H 19N 5Na 2O 6?7H 2O
  分子量: 597.49
  [ 性状 ]
  本品为白色至淡黄色或绿黄色的冷冻干燥固体。
  [ 药理毒理 ]
  药理作用: 培美曲塞是一种结构上含有核心为吡咯嘧啶基团的抗叶酸制剂, 通过破坏细胞内叶酸依赖性的正常代谢过程,抑制细胞复制,从而抑制肿瘤的生长 。体外研究显示,培美曲塞能够抑制 胸苷酸合成酶、二氢叶酸还原酶和甘氨酰胺核苷酸甲酰转移酶的活性,这些酶都是合成叶酸所必需的酶,参与胸腺嘧啶核苷酸和嘌呤核苷酸的生物再合成过程。培美曲塞通过运载叶酸的载体和细胞膜上的叶酸结合蛋白运输系统进入细胞内。一旦培美曲塞进入细胞内,它就在叶酰多谷氨酸合成酶的作用下转化为多谷氨酸的形式 。多谷氨酸存留于细胞内成为 胸苷酸合成酶和甘氨酰胺核苷酸甲酰转移酶的抑制剂。多谷氨酸化在肿瘤细胞内呈现时间 - 浓度依赖性过程,而在正常组织内浓度很低。多谷氨酸化代谢物在肿瘤细胞内的半衰期延长,从而也就延长了药物在肿瘤细胞内的作用时间。
  临床前研究显示培美曲塞体外可抑制间皮瘤细胞系 (MSTO?211H, NCI?H2052) 的生长。间皮瘤细胞系 MSTO?211H 的研究显示出培美曲塞与顺铂联合有协同作用。
  人群药效学分析采用的指标是绝对中性粒细胞计数,此时人群接受的为单药培美曲塞,未接受叶酸和维生素 B 12 的补充治疗。通过观察粒细胞最低值来判断血液学毒性发生的严重程度,结果发现其与本品全身给药剂量呈负相关关系。研究中也发现如果患者基线检查时胱硫醚或高半胱氨酸浓度高,那么其绝对粒细胞计数下降的会更为严重。叶酸和维生素 B 12 可以降低胱硫醚或高半胱氨酸这两种底物的浓度。经过培美曲塞多周期治疗,未见对中性粒细胞的累积毒性。
  培美曲塞全身给药后( AUC 38.3- 316.8 m g?hr/mL ),中性粒细胞下降至最低点的时间约为 8 - 9.6 天,经过最低点后,中性粒细胞计数恢复至基线水平的时间为 4.2 -7.5 天。
  毒理研究
  遗传毒性: 小鼠骨髓体内微核测定显示培美曲塞是断裂剂,但体外的多个实验研究( Ames 测定, CHO 细胞测定)均未显示致突变作用。
  生殖毒性: 培美曲塞按照 0.1 mg/kg/ 日或更大剂量(相当于人类推荐用量的 1/1666 )给予雄性小鼠,可导致生育能力下降、 精液过少和睾丸萎缩。
  致癌作用: 未进行培美曲塞致癌作用的研究。
  [ 药代动力学 ]
  培美曲塞药代动力学评价在 426 例多种肿瘤类型的患者中进行,采用单药治疗,剂量为0.2-838 mg/m 2 ,10 分钟静脉内给药。培美曲塞主要以原药形式从尿路排泄,在给药后的24 小时内,70%-90% 的培美曲塞还原成原药的形式从尿中排出。培美曲塞总体清除率为 91.8 mL/min( 肌酐清除率是90 mL/min) ,对于肾功能正常的患者,体内半衰期为 3.5 小时。随着肾功能降低,清除率会降低,但体内剂量会增加。随着培美曲塞剂量的增加,曲线下面积AUC 和最高血浆浓度(C max)
  会成比例增加。多周期治疗并未改变培美曲塞的药代动力学参数。培美曲塞呈现一稳态分布容积为 16.1 升。体外研究显示,培美曲塞的血浆蛋白结合率约为81% ,且不受肾功能影响。
  特殊人群
  培美曲塞 特殊人群中的药代动力学研究为在总计 400 例患者的单组研究。
  老年人 — 对于年龄为 26—80 岁的人群,培美曲塞药代动力学无明显变化。
  儿童 — 临床研究中未纳入儿童患者。
  性别 — 男性患者与女性患者相比,培美曲塞药代动力学无差别。
  种族 — 高加索裔和非洲裔患者,培美曲塞的药代动力学相似。曾有试验对日本患者的药代动力学进行研究,虽然没有日本患者和西方患者之间药代动力学参数规范的统计学对照报告,但仍可说明两者的绝对剂量参数值是基本相似的,而且没有显著的临床差异。
  肝脏功能不全 — 谷草转氨酶( AST 、 SGOT )、谷丙转氨酶( ALT 、 SGPT )和总胆红素升高,不影响培美曲塞的药代动力学。但是,未进行肝损害患者的药代动力学研究。 ( 参见 [ 注意事项 ] 项下 “肝功能不全的患者”部分 ) 。
  肾功能不全 — 总计 127 例肾功能不全患者进行了培美曲塞药代动力学研究。 如果同时合并有顺铂治疗,随着肾功能降低,培美曲塞的血浆清除率降低,而全身暴露剂量增加。将培美曲塞全身总暴露量( AUC )与 100 mL/min 的肌酐清除率比较,当肌酐清除率分别为 45 、 50 和 80 mL/min 时,全身总暴露量( AUC )增加 65% 、 54% 和 13% 。 ( 参见 [ 用法用量 ] 和 [ 注意事项 ] 项下“警告”部分 )
  [ 禁忌 ]
  本品 禁用于对培美曲塞或药品其他成分有严重过敏史的患者。
  [ 注意事项 ]
  警告
  肾功能减低的患者
  本品主要通过尿路以原药形式排除体外。如果患者肌酐清除率 3 45 mL/min ,本品 ò 无需剂量调整。对于肌酐清除率 <45 mL/min 的患者,无足够患者的研究资料来给予推荐剂量。因此,对于肌酐清除率 <45 mL/min 的患者,不应给予本品治疗。 ( 参见 [ 用法用量 ] 中的“推荐剂量调整方法” ) 。
  临床研究中,曾有一位严重肾功能不全(肌酐清除率 19 ml/min ) 的患者,未接受叶酸和维生素 B 12 补充治疗,接受单药本品治疗后,死于药物相关毒性。
  骨髓抑制
  本品可以引起骨髓抑制,包括中性粒细胞、 血小板减少、贫血(或各类血细胞减少)(参见 [ 不良反应 ] )。骨髓抑制是常见的剂量限制性毒性。应根据既往治疗周期中出现的最低中性粒细胞、血小板值和最严重非血液学毒性来进行剂量调整 。 ( 参见 [ 用法用量 ] 中的“推荐剂量调整方法” ) 。
  叶酸及维生素 B 12 的补充治疗
  接受本品治疗同时应接受叶酸和维生素 B 12 的补充治疗,可以预防或减少治疗相关的血液学或胃肠道不良反应。 ( 参加 [ 用法用量 ] 部分 ) 。临床研究显示, 给予叶酸和维生素 B 12 补充治疗的患者,接受本品治疗时总的不良反应发生率降低,包括 3/4 度的血液学毒性以及非血液学毒性,例如中性粒细胞减少、粒细胞减少性发热和 3/4 度粒细胞减少性感染。
  注意事项
  一般注意事项
  本品应在有抗肿瘤药物应用经验的合格医师指导下使用。应在有足够诊断与治疗技术的医疗机构进行本品治疗,这也可以保证并发症的及时处理。临床研究中看到的治疗相关不良反应均是可以恢复的。给药前未给予类皮质激素预处理的患者易出现皮疹。地塞米松(或相似药物)预处理可以降低皮肤反应的发生率及严重程度。 ( 参见 [ 用法用量 ] 部分 )
  本品是否导致体液储留例如胸水或腹水还不清楚。对于临床有明显症状的体液储留患者,可以考虑本品用药前进行体腔积液引流。
  实验室检查
  所有准备接受本品治疗的患者,用药前需完成包括血小板计数在内的血细胞检查和血生化检查,给药后需监测 血细胞最低点及恢复情况,临床研究时每周期的开始、第 8 天和第 15 天需检查上述项目。患者需在中性粒细胞 3 1500/mm 3 ,血小板 3 100,000 cells/mm 3 、肌酐清除率 3 45 ml/min. 时,才能开始本品治疗。
  肝功能不全的患者
  胆红素 > 1.5 倍正常上限的患者不纳入本品临床研究;无肝转移的患者,如果转氨酶 >3.0 倍正常上限,不纳入本品临床研究;有肝转移的患者,如果转氨酶在 3.0 和 5.0 倍正常上限之间,纳入本品临床研究。
  肝功能不全患者的剂量调整见表 2 。 ( 参见 [ 药代动力学 ] 项下 的“特殊人群”部分 ) 。
  肾功能不全患者
  本品主要通过肾脏排泄。与肾功能正常患者相比,肾功能不全患者的总体清除率下降, AUC 增加。 有中度肾功能不全患者,顺铂与本品联合用药的安全性尚未确定 ( 参见 [ 药代动力学 ] 项下 的“特殊人群”部分 ) 。
  药物与实验室检查的相互作用
  尚未确定。尚没有研究证明服用本品是否对患者驾驶和操作机器造成影响,然而研究证明本品可能导致疲劳,如果有这种情况发生,患者应被告知小心驾驶和操作机器。
  [ 孕妇及哺乳期妇女用药 ]
  妊娠: 妊娠妇女接受本品治疗可能对胎儿有害。妊娠 6 天 —15 天的小鼠,静脉予以 0.2 mg/kg (0.6 mg/m 2) 或 5 mg/kg (15 mg/m 2) 培美曲塞,有胎儿毒性并能致畸。给予小鼠 0.2 mg/kg 剂量 ( 大约为人类推荐剂量的 1/833) 培美曲塞即可引起胎儿畸形 ( 距骨和头颅骨的不完全骨化 ) , 5 mg/kg 时可导致腭裂 ( 相当于人类推荐剂量的 1/33) 。 胚胎毒性主要表现于胚胎死亡率增加,同时胚胎发育迟缓。没有有关妊娠妇女接受 本品治疗的研究,因为建议患者避孕。如果在妊娠期间使用了 本品或患者在使用本品期间怀孕,应告之可能对胎儿的潜在危险。
  哺乳: 本品或其代谢产物是否能从乳汁中分泌尚未确定。但是本品可能对吃奶的婴儿有潜在严重危害,接受本品治疗的母亲应停止哺乳。
  [ 儿童用药 ]
  儿童用药的安全性和有效性尚未确定。
  [ 老年患者用药 ]
  按照所有患者的剂量调整方法进行,无需特殊方案 ( 参见 [ 药代动力学 ] 中特殊人群部分 ) 。
  [ 药物相互作用 ]
  化疗药物 — 顺铂不改变培美曲塞的药代动力学, 培美曲塞也对所有铂类药物的药代动力学无影响。
  维生素 — 同时给予口服叶酸和肌注维生素 B 12 不改变培美曲塞的药代动力学。
  细胞色素 P450 酶对药物代谢 — 体外肝脏微球蛋白预测研究结果显示,培美曲塞未导致通过 CYP3A 酶 , CYP2D6 酶 , CYP2C9 酶 和 CYP1A2 酶代谢的药物清除率降低。没有进行研究观察培美曲塞对细胞色素 P450 同工酶的影响。因为,如果按照推荐的给药日程(每 21 天 1 次), 本品对任何酶均无明显诱导作用。
  阿司匹林 — 给予低到中等剂量 ( 每 6 小时 325 mg ) 的阿司匹林,未影响培美曲塞的药代动力学。 高剂量的阿司匹林对培美曲塞药代动力学影响目前还不清楚。
  布洛芬 — 肾功能正常患者,布洛芬每日剂量为 400mg , 4 次 / 日时,可使培美曲塞的清除率降低 20% ( AUC 增加 20% )。更高剂量的布洛芬对 培美曲塞 药代动力学影响目前还不清楚。
  本品主要通过肾小球的过滤和肾小管的排泄作用,以原药形式从尿路排出体外。同时给予对肾脏有危害的药物会延迟本品的清除,同时给予增加肾小管负担的其他药物(例如丙磺舒)也可能延迟本品的清除。
  对于肾脏功能正常(肌酐清除率的患者 3 80 ml/min )的患者,本品可以和布洛芬同时用药 (400mg,4 次 / 日 ) ,但是对于有轻到中度肾功能不全(肌酐清除率在 45 到 79 ml/min 之间)的患者,本品与布洛芬同时使用要小心。有轻到中度肾功能不全的患者,在应用本品治疗前 2 天、用药当天和用药后 2 天,不要使用半衰期短的非甾体类抗炎药。
  长半衰期的非甾体类抗炎药与本品潜在相互作用,目前还不确定。但在应用本品治疗前 5 天、用药当天和用药后 2 天,也要中断非甾体类抗炎药的治疗。如果一定要应用非甾体类抗炎药,一定要密切监测毒性反应,特别是骨髓抑制、肾脏及胃肠道的毒性。
  [ 药物过量 ]
  仅有几例本品药物过量的报告。报告的主要不良反应为中性粒细胞减少、贫血、血小板减少、粘膜炎和皮疹。可预料到的药物过量并发症主要有骨髓抑制,表现为中性粒细胞减少、血小板减少和贫血。另外,也可能出现伴随或不伴随发热的感染、腹泻和粘膜炎。一旦发生药物过量,应立即在医生指导下采取合适医疗措施。
  临床研究中,如果出现 3 天以上 4 度白细胞减少或 3 天以上 4 度中    性粒细胞减少,可以使用甲酰四氢叶酸,如果出现 4 度血小板减少或 3 度血小板减少相关的出血或 3/4 度粘膜炎,应立即使用甲酰四氢叶酸。甲酰四氢叶酸的推荐使用剂量和方法是:静脉给药,第 1 次剂量 100 mg/m 2, 以后 50 mg/m 2, 每 6 小时 1 次,连用 8 天。
  通过透析解除本品过量的作用尚未确定。
  [ 规格 ]
  500 毫克/ 瓶
  [ 贮藏 ]
  本品应室温保存( 15-30 ° C ) 。
  按照上述方法配制的本品溶液,不含抗菌防腐剂,从微生物的角度应该立即使用,不用部分丢弃。如果没有一次用完,配好的本品溶液可置于冰箱冷藏( 2 - 8 ° C )或室温保存( 15-30 ° C ) ,无需避光,其物理、化学特性在 24 小时内保持稳定。
  本品没有光敏性。
  [ 包装 ] 玻璃瓶装, 1 瓶 / 盒
  [ 有效期 ] 24 个月。
  [ 进口药品注册证号 ] H20050441
  [ 生产企业 ]
  Lilly France S.A.S.
  地址: 67640 ,Fegersheim ,France

==== 汉译英 ====

Alimta (pemetrexed for injection) [drug name]
Alimta (pemetrexed injection) generic name: pemetrexed for injection
Product Name: English: ALIMTA
Chinese: Alimta
English name: Pemetrexed disodium for Injection
Pinyin: Zhu She Yong Pei Mei Qu Sai Er Na
This product is the main component of pemetrexed disodium, its chemical name: glutamic acid, N - [4 - [2 - (2 - amino -4,7 - dihydro -4 - O-1H-pyrrolo [ 2,3-d] pyrimidine--5 - alkyl) ethyl] benzoyl] -, disodium salt, 7 hydrate
Its structural formula is:
Molecular formula: C 20H 19N 5Na 2O 6? 7H 2O
MW: 597.49
[Properties]
This product is white to pale yellow or green-yellow lyophilized solid.
[Pharmacology and toxicology]
Pharmacological effects: Pemetrexed is a structure that contains the core group for the pyrrole-pyrimidine anti-folic acid preparations, by destroying the cell's normal metabolism of folic acid-dependent process, inhibition of cell replication, thus inhibiting tumor growth. In vitro studies have shown that pemetrexed can inhibit thymidylate synthase, dihydrofolate reductase and GLYCINAMIDE nucleotide carbamoyl transferase activity, these enzymes are the enzymes necessary for synthesis of folic acid to participate in thymidylate and purine nucleotide bio-re-synthesis process. Pemetrexed by carrying folate carrier and membrane folate binding protein transport system into the cell. Once the pemetrexed into the cell, it more than in the leaf acyl glutamate synthesis under the action of the enzyme into a polyglutamate form. Polyglutamate to survive in the cell to become thymidylate synthase and GLYCINAMIDE nucleotide carbamoyl transferase inhibitors. Polyglutamate of presentation time in tumor cells - a concentration-dependent process, but the concentration is very low in normal tissues. Polyglutamate metabolites in tumor cells to extend the half-life, thereby also extending the drug in tumor cells and role within the time.
Pre-clinical studies have shown that pemetrexed can inhibit mesothelioma cell lines in vitro (MSTO? 211H, NCI? H2052) growth. Mesothelioma cell line MSTO? 211H studies have shown that out of pemetrexed and cisplatin have synergistic effect.
Population pharmacodynamic analysis of the indicators used is the absolute neutrophil count, this time for the groups receiving single-agent pemetrexed, did not receive folic acid and vitamin B 12 of the replacement therapy. By observing the value of granulocytes to determine the minimum severity of hematological toxicity occurred was found with the body of this product showed a negative correlation between dose. Studies have also found that patients with baseline inspection, cystathionine, or homocysteine at high concentrations, then the decline in the absolute granulocyte count would be more serious. Folic acid and vitamin B 12 can reduce homocysteine cystathionine or both the substrate concentration. After many cycles pemetrexed treatment, no accumulation of neutrophils toxicity.
Pemetrexed systemic after administration (AUC 38.3-316.8 mg? Hr / mL), under the nadir of neutrophils of time is about 8 - 9.6 days, after the lowest point, the neutrophil counts returned to baseline time for the level of 4.2 -7.5 days.
Toxicology
Genetic toxicity: in vivo mouse bone marrow micronucleus tests showed that pemetrexed is broken agent, but a number of in vitro experimental study (Ames measured, CHO cell assay) did not show mutagenic effect.
Reproductive Toxicity: Pemetrexed in accordance with 0.1 mg / kg / day or higher doses (equivalent to the human recommended dosage of 1 / 1666) give the male mice, can lead to fertility decline in semen is too small, and testicular atrophy.
Carcinogenic effects: the absence of carcinogenic effects of pemetrexed studies.
[Pharmacokinetics]
Pemetrexed pharmacokinetics evaluation of 426 cases of multiple tumor types of patients has been conducted, using a single drug treatment, a dose of 0.2-838 mg / m 2, 10 Fen Zhong intravenous administration. Pemetrexed mainly in the form of the original drug from the urinary excretion, in the 24 hours after administration, 70% -90% of the pemetrexed restored to the original form of the drug excreted from the urine. Pemetrexed overall clearance rate was 91.8 mL / min (creatinine clearance rate was 90 mL / min), for patients with normal renal function, in vivo half-life of 3.5 hours. As renal function decreased clearance rate would be reduced, but the dose will increase. With the pemetrexed dose increased, the area under the curve AUC and maximum plasma concentration (C max)
Will be proportional to the increase. Multi-cycle treatment did not change Pemetrexed pharmacokinetic parameters. Pemetrexed showed a steady-state volume of distribution of 16.1 liters. In vitro studies have shown that pemetrexed in plasma protein binding rate is about 81%, and renal function is not affected.
Special Populations
Pemetrexed in special populations pharmacokinetic study in patients with a total of 400 cases of single-group study.
The elderly - for the age group 26-80 years old, pemetrexed pharmacokinetics no significant changes.
Children - children are not included in clinical studies in patients.
Gender - male patients and female patients compared to pemetrexed pharmacokinetics of non-discrimination.
Race - Caucasian-American and African-American patients, pemetrexed pharmacokinetics similar. Japanese patients had tests to study the pharmacokinetics, although no Japanese patients and the West pharmacokinetic parameters between patients with standard statistical comparison report, but still shows that both the absolute dose of parameter values is a basic similarity of the and there is no significant clinical differences.
Liver dysfunction - aspartate aminotransferase (AST, SGOT), alanine aminotransferase (ALT, SGPT) and total bilirubin increased, does not affect pemetrexed pharmacokinetics. However, no damage to the liver of patients with pharmacokinetic study. (See [Note] under "liver dysfunction in patients with" section).
Renal insufficiency - a total of 127 cases of renal insufficiency in patients with pemetrexed pharmacokinetics. If there is concomitant cisplatin therapy, along with decreased kidney function, pemetrexed plasma clearance reduced, while systemic exposure to increased dosages. Be pemetrexed total systemic exposure (AUC) and 100 mL / min creatinine clearance rate of comparison, when the creatinine clearance rates were 45, 50 and 80 mL / min when the total systemic exposure (AUC) increased by 65%, 54% and 13%. (See [Usage dosage] and [Note] under the "warning" section)
[Taboo]
This product is banned from pairs of pemetrexed, or other components of drugs in patients with history of severe allergy.
[Notes]
Warning
In patients with reduced renal function
This product is mainly through the urinary tract to exclude the form of the original drug in vitro. If the creatinine clearance rate in patients with 3 45 mL / min, no dose adjustment of this product ò. For creatinine clearance <45 mL / min in patients without adequate study of patients with information to give the recommended dose. Therefore, creatinine clearance <45 mL / min in patients with treatment should not be given to this product. (See [Usage dosage] in the "Recommended dosage adjustment method").
Clinical studies, there was a severe renal insufficiency (creatinine clearance 19 ml / min) of the patients did not receive folic acid and vitamin B 12 replacement therapy, receive a single agent in this product after treatment, died of drug-related toxicity.
Myelosuppression
It can be used to cause bone marrow suppression, including neutropenia, thrombocytopenia, anemia (or pancytopenia) (see [adverse reactions]). Bone marrow suppression is a common dose-limiting toxicity. Should be based on past cycles appear in a minimum of neutrophil and platelet values and the most serious non-hematologic toxicity to dosage adjustment. (See [Usage dosage] in the "Recommended dosage adjustment method").
Folic acid and vitamin B 12 additional treatment
Acceptance of the goods should also be receiving treatment folic acid and vitamin B 12 additional treatment can prevent or reduce the treatment-related hematological or gastrointestinal adverse reactions. (Participation in [Usage dosage] section). Clinical studies have shown that giving folic acid and vitamin B 12 replacement therapy in patients receiving treatment of this product overall lower the incidence of adverse reactions, including 3 / 4 hematologic toxicity and the degree of non-hematologic toxicity, such as neutropenia , febrile neutropenia and 3 / 4 degree of neutropenia infection.
Notes
General Notes
This product should be applied where there anticancer drugs under the guidance of qualified and experienced doctors to use. Should be adequate diagnosis and therapy of medical institutions treating this product, which also guarantees the timely treatment of complications. Clinical studies, treatment-related adverse events seen both can be restored. The former administration not given corticoids in patients with pre-prone skin rash. With dexamethasone (or similar drugs) pretreatment can reduce the incidence of skin reactions and severity. (See [Usage dosage] section)
This product is causing the fluid retention such as pleural effusion or ascites is unclear. For obvious clinical symptoms in patients with fluid retention can be considered agents of this product prior to body cavity effusion drainage.
Laboratory
This product is all ready to accept patients, medication must be completed before the platelet count, including blood cells, including examination and blood biochemical tests, blood cells after administration need to monitor the recovery of the lowest points and the clinical study period of the beginning of each week, 8 days and the first 15 days of inspections of these items. Patients need to neutrophils 3 1500/mm 3, platelet-3 100,000 cells / mm 3, creatinine clearance rate of 3 45 ml / min. When you can begin treatment of this product.
In patients with liver dysfunction
Bilirubin "1.5 times the upper limit of normal in patients not included in clinical studies of the product; without liver metastasis in patients, if the transaminase" 3.0 times the upper limit of normal, non-clinical studies included in this product; a liver metastasis in patients, if the transaminase at 3.0 and 5.0 times the upper limit of normal between the clinical studies included in this product.
Liver dysfunction in patients with dose adjustments in table 2. (See [Pharmacokinetics] under the "special groups" section).
Patients with renal insufficiency
This product is primarily through renal excretion. Compared with patients with normal renal function, renal insufficiency in patients with an overall clearance rate has dropped, AUC increased. In patients with moderate renal insufficiency and cisplatin with the product safety of combination therapy has not been established (see [Pharmacokinetics] under the "special groups" section).
The interaction of drugs and laboratory tests
Yet been determined. Studies have shown that the FDA has not yet serving whether the patient affect the driving and operation of machinery, but studies have shown that product can lead to fatigue, if this happens, the patient should be told to drive and operate the machine.
[Pregnant and lactating women drug]
Pregnancy: pregnant women receiving treatment of this product may be harmful to the fetus. 6 days -15 days of pregnancy in mice, intravenous to be 0.2 mg / kg (0.6 mg / m 2) or 5 mg / kg (15 mg / m 2) pemetrexed, with fetal toxicity and can teratogenic. Mice given 0.2 mg / kg dose (about the human recommended dose of 1 / 833) pemetrexed can cause fetal malformations (talus and the incomplete ossification of skull), 5 mg / kg can result in cleft palate (the equivalent of recommended human dose of 1 / 33). Embryo toxicity mainly in the embryo increased mortality, while fetal growth retardation. Do not have the product in pregnant women receiving treatment in this study, as recommended in patients with contraception. If you use this product during pregnancy or the patient in making the FDA during the pregnancy, should be warned of the possible potential risk to the fetus.
Breast-feeding: This product or its metabolites is yet to be determined from the secretion of milk. But the product can be able to nurse the baby are potentially serious harm to receive treatment in this product should stop breast-feeding mothers.
[Children's medication]
Children's safety and effectiveness of drug use has not been established.
[Medication in elderly patients]
According to all methods of dosage adjustment in patients without the need for special programs (see [Pharmacokinetics] in special populations section).
[Drug Interactions]
Chemotherapy drugs - cisplatin does not change the pemetrexed pharmacokinetics, pemetrexed also for all platinum drugs had no effect on the pharmacokinetics.
Vitamin - while giving oral administration of folic acid and intramuscular vitamin B 12 does not change the pemetrexed pharmacokinetics.
Cytochrome P450 enzymes in drug metabolism - in vitro liver-microglobulin predicted results show that pemetrexed has not led to the adoption CYP3A enzyme, CYP2D6 enzyme, CYP2C9 enzyme and drug metabolism enzyme CYP1A2 clearance rate. No concept of Cha Pei Mei Qu Cypriot research on cytochrome P450 isozymes. Because, according to the recommended dose schedule (every 21 days one time), the product of any enzyme were not significantly induced.
Aspirin - for low to moderate doses (every 6 hours 325 mg) of aspirin, did not affect pemetrexed pharmacokinetics. High-dose aspirin on pemetrexed pharmacokinetics is still unclear.
Ibuprofen - in patients with normal renal function, ibuprofen daily dose of 400mg, 4 times / day, the can pemetrexed to reduce the clearance rate of 20% (AUC increase of 20%). Higher doses of ibuprofen on pemetrexed pharmacokinetics is still unclear.
This product is primarily through glomerular filtration and tubular excretion of the role of the form of the original drug excreted from the urinary tract. While giving the right kidney against drug will delay the clearance of the goods, while providing additional renal burden of other drugs (such as probenecid) also may delay the clearance of the goods.
For the normal renal function (creatinine clearance rate in patients with 3 80 ml / min) of the patients, It can be used to, and ibuprofen at the same time medication (400mg, 4 times / day), but for a mild to moderate renal insufficiency (creatinine clearance the rate of 45 to 79 ml / min between) patients, the goods to be careful with the use of ibuprofen at the same time. Have mild to moderate renal insufficiency patients in the 2 days before treatment should be the FDA, medication that day and 2 days after treatment, do not use a short half-life of non-steroidal anti-inflammatory drugs.
A long half-life of non-steroidal anti-inflammatory drugs interact with the product potential, at present uncertain. However, the FDA should be 5 days before treatment, medication that day and 2 days after treatment, but also interrupt non-steroidal anti-inflammatory drug treatment. If you must use non-steroidal anti-inflammatory drugs, we must closely monitor the toxicity, especially myelosuppression, renal and gastrointestinal toxicity.
[Overdose]
This product is only a few cases of overdose reported. The major adverse reactions were neutropenia, anemia, thrombocytopenia, mucositis and rash. Might be expected, the main complication of drug overdose are bone marrow suppression, manifested as neutropenia, thrombocytopenia and anemia. In addition, it may be accompanied or not accompanied by fever infections, diarrhea and mucositis. The event of overdose, doctors should immediately take appropriate under the guidance of medical interventions.
Clinical studies, if there is more than 3 days 4 leucopenia or 3 days over the 4 degrees neutropenia, you can use folinic acid, if there is 4 degrees or 3 degrees thrombocytopenia thrombocytopenia-related bleeding or 3 / 4 degree of mucositis should be immediately citrovorum. Folinic acid dose and the recommended methods are: intravenous administration, the first one dose of 100 mg / m 2, after 50 mg / m 2, every 6 hours 1 qd for 8 days.
Analyzing the role of excessive lifting of the goods has not been established.
[Specifications]
500 mg / bottle
[Storage]
This product should be stored at room temperature (15-30 ° C).
Prepared in accordance with the above-mentioned method of solution of this product, does not contain antimicrobial preservatives, from the microbiological point of view should be used immediately, without some discarded. If there is no time running out, with a good solution of this product may be placed in the refrigerator (2 - 8 ° C) or kept at room temperature (15-30 ° C), no dark, its physical and chemical properties remain stable within 24 hours .
This product is not photosensitive.
[Packaging] glass containers, 1 bottle / box
[Valid] 24 months.
[Imported drug registration证号] H20050441
[Manufacturer]
Lilly France S.A.S.
Address: 67640, Fegersheim, France
 
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更新日期: 2014-06-27 08:43
作者: : mcyclub
修订: 1.6

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