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本帖最后由 老马 于 2013-11-27 20:38 编辑
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o7 R7 r0 F& J依托泊苷 Etoposide VP-16口服胶囊的说明
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[中文别名]鬼臼乙叉甙,依托泊甙,表鬼臼毒吡喃葡萄糖。7 r) L% N) m# l- S
[商品名]胶囊剂:威克,拉司太特,泛必治。! z9 N% k! U( N
[英文名]Etoposide,Etopl,Vepeside.% @/ W. V- x. t) k- M4 {
[外文缩写]VP-16,VP16-213,EPEG。8 ?# N5 L T- }7 a4 P
[性 状]威克、泛必治、拉司太特软胶囊内含无色或淡黄色澄明粘性液体,易溶于甲醇和氯仿,难溶于水和乙醚。# b4 i# ?2 |6 Q7 M; F; q
[药理作用] 足叶乙甙是鬼臼脂(Podophyllin)中分离出的木脂体类有效成份。VP-16是细胞周期特异性抗肿瘤药物,作用于晚S期或G2期,其作用位点是拓扑异构酶Ⅱ,形成一种药物-酶-DNA三者之间稳定的可裂性复合物,干扰DNA拓朴异构酶Ⅱ(DNA topoisomeraseⅡ),致使受损的DNA不能修复。拓朴异构酶Ⅱ插入DNA中,产生一般细胞功能所需的断裂反应;VP-16似乎可通过稳定脱氧核糖核酸断裂复合物,引起DNA和拓扑异构酶Ⅱ的双线断裂。该品在体内激活某些内切酶,或通过其代谢物作用于DNA,其非糖苷同系物4-去甲基表鬼臼毒素则可抑制微管制组装。
: ~- a! K/ j& h& _1 k8 P) e, \[适应病症]小细胞肺癌,非小细胞肺癌(NCCN2013和2014年版的NSCLC治疗指南中均为一线药物)。' Q; A- j7 ]# G$ Z' A, @' T* J
2. 药代动力学! r3 [1 u/ b: J+ l4 X; `
依托泊苷口服0.44小时后吸收,约0.5-3小时后到达血药浓度峰值,平均半衰期为6.8小时。主要分布在胆汁、腹水、尿、胸水和肺组织中。依托泊苷主要经尿排出,72小时内排出45%,其中15%为代谢产物,仅有1.5%~16%从粪便排泄。脑脊液中药物浓试为血中的2%~10%。口服生物利用度为40-70%。$ P' I1 v! I/ @2 o' X! o/ H; [6 B' ^
3. 剂量方案
4 J0 {+ p) A9 X6 G方案:一天一次,一次50mg,空腹,连续服用二周,休息一周,每三周一个疗程。$ P/ C# Y2 Q1 o: |6 Y( B
注:如果是25mg的剂型,可以每天二次,一次25mg服用。1 F8 g; |, W' I3 A+ P8 C# Y* P9 p
对于50mg每天方案,如果头二个疗程无缓解,副作用微弱,可以加量到75mg每天(1天50mg,另一天100mg或者每天25mg*3),或者吃三周停一周,四周一个疗程
* ?% x1 W W: p2 c& j5 d5 s4 H2 F依托泊苷软胶囊(泊瑞)50mg*10粒 青岛海尔药业有限公司 232元一盒# E0 |3 e/ \# O
依托泊苷软胶囊(拉司太特)25mg*40粒 日本化药株式会社 862元一盒。* T! \3 f6 S0 t( V
依托泊苷软胶囊(威克) 50mg*10粒 江苏恒瑞医药 236一盒9 g7 z9 [" r) C: Z" S' ~
医保乙类药。8 Y; q$ b; F, c, A' S: N
注:此二方案为低剂量方案,比标准剂量依托泊苷的生物利用度更高,副作用更小。
0 s) H( y0 b J6 [9 R$ k# x0 V& o4.不良反应
$ C; c# ]0 t% k) C& L; Z(1)骨髓抑制:白细胞和血小板减少,贫血,此为剂量限制性毒性。白细胞减少最低点发生在7-14天后,血小板减少最低点发生在9-16天后,骨髓毒性完全恢复需要20天,骨髓毒性无蓄积。
, Z6 |7 [2 w& o+ Y; M: H(2)胃肠道反应:恶心,呕吐,食欲不振,口腔炎,腹泻。7 u- @. H, ]+ u5 e. X: n2 o. ?6 @
(3)脱发:脱发较明显,有时发展至全秃,但具可逆性。
3 Z$ Q+ `. s- k) J& |1 W/ y(4)小于1%概率的副作用:神经毒性,高尿酸血症,败血症,麻木和刺痛,头晕,抑郁症,指甲色素沉着和念珠菌病。罕见副作用:嗜睡,肝毒性,发热,皮疹,色素沉着,瘙痒,荨麻疹,腹痛,便秘,吞咽困难。$ W( D% ^& m: @, O
(5)心脏毒性:无心脏毒性和心电图改变,心肌缺血偶见。, r, q; X! G+ j7 N8 H/ p
可能发生的头痛等神经毒性可以服用弥可保(甲钴胺),或者VB1,VB6,VB12。 |
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个人公众号:treeofhope
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共68条精彩回复,最后回复于 2021-2-5 16:28
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本帖最后由 dgarden 于 2013-10-21 23:55 编辑 1 ]% c4 v1 _. R. v
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vp16联合bkm120,对于非小细胞肺癌的维持治疗,这个试验和想法都很好。/ e/ f- A; [! N
腺癌中 有很多 会发生 小细胞癌转化 发生了,使用vp16的有效率就高一些,毕竟vp16是小细胞癌的一线药物。& ?3 ^, ^$ t' c: c) v g* F4 Z% A
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本帖最后由 老马 于 2013-10-26 10:25 编辑 0 n! j$ T0 h0 z4 b# a& ^& s. A
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依托泊苷浙肿临床结果.pdf
(71.9 KB, 下载次数: 704)
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个人公众号:treeofhope
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追风剑客家吃VP-16(50mg每天,一天一次)联合BKM120(100mg每天,一天一次)二周,
9 t2 A- {9 I0 F+ l1 T& |; Vcea从871下到715。 |
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个人公众号:treeofhope
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VP-16+BKM120, 十分关注。
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对鳞癌效果如何?? |
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本帖最后由 老马 于 2013-11-25 02:31 编辑 $ `# h; ?, d+ x {+ [6 L* l, w
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WCLC 2013年0 B0 u) `; k `9 l
SINGLE AGENT ORAL ETOPOSIDE FOR ELDERLY AND INFIRM ADVANCED NON SMALL CELL LUNG CANCER : A REASONABLE THERAPEUTIC OPTION
5 F; o. ?) C/ D* e, nBackground: The use of chemotherapy has been shown to increase the effectiveness of best supportive care (BSC) in elderly patients with non-small cell lung cancer (NSCLC). The use of Intra venous chemotherapy ( IV ) has many times been diffcult in elderly patients or patients with poor performance status owing to fear of toxicity.We studied the effectiveness of a non toxic regimen with single agent oral chemotherapy with etoposide plus best supportive care versus best supportive care alone in subjects with advanced non small cell lung cancer unft for IV chemotherapy.
2 \3 `, t8 X4 t; r; OMethods: Eighty fve cases of advanced non small cell lung cancer and ECOG performance status of 2 to 3 , unft for IV chemotherapy as per treating physician‘s discretion were included in the study.
$ H) x( D D! K! G' {; xForty three patients received chemotherapy with Tablet Etoposide 50 mg once daily for 14 days along with best supportive care ( BSC )every 21 days for a maximum of 8 cycles in responding patients. Regimen was re challenged on progression. The remaining received BSC only.) R1 m& n5 h5 A0 L
Results: We measured at least 1 of the following outcomes: Overall survival ( OS ) or treatment-related mortality. Overall, patients that received chemotherapy plus BSC had signifcant longer OS 7 W! S8 n9 V. p9 _9 B" h
than those that received BSC alone (HR 0.75; 95%CI, 0.68–0.82; P,0.001). Additionally, 5 F3 r6 k1 \% ^/ ]/ {
motherapy plus BSC as compared to BSC alone resulted in a 24% RR reduction (95%CI: 10–38; P = 0.001) in 6-month mortality, 10% RR reduction (95%CI: 8–15; P,0.001) in 12-month mortality and 6% RR reduction (95%CI: 2–9; P = 0.02) in 2-year mortality. Toxicity was not signifcantly greater in patients who received chemotherapy plus BSC.
( t; e8 U& g- h0 g, s( `Conclusion: Chemotherapy with single agent oral etoposide plus BSC is a non toxic therapeutic option in infrm and elderly NSCLC patients unft to receive intravenous chemotherapy.
7 _5 Z' ]% K1 y" `; c/ V2 `本临床方案:VP-16口服50mg每天,吃二周停一周,三周一个疗程。 |
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个人公众号:treeofhope
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