伯尔定注射剂|PARAPLATIN（CARBOPLATIN INJECTION）

部份中文伯尔定处方资料（仅供参考）   n" x' Y$ N+ K' ]4 }药品英文名 Carboplatin 药品别名 铂尔定、卡波铂、顺羧酸铂、碳铂、顺二氨环丁烷羧酸铂、顺二氨环丁铂、Carboplatine、Carboplatinum、CBDCA、JM-8、Paraplatin、Platinum 8 n; C/ [' s, P+ F& U" c  S2 o药物剂型 注射剂(粉)：50mg，150mg  450mg。 : o9 N; K5 L/ D药理作用 卡铂为第二代铂类抗肿瘤药，具细胞周期非特异性，作用与烷化剂类似。卡铂细胞杀伤作用可能是由于其与DNA产生链间和链内交联，导致DNA损伤，以至DNA的复制和转录受损。单用时，卡铂的剂量4倍于顺铂，且细胞中出现DNA交联作用较顺铂缓慢。 药动学 ' i; c2 t9 X; F卡铂的分布与顺铂相似，在肝、肾、皮肤和肿瘤中浓度最高。但卡铂的血浆蛋白结合率很低，呈不可逆，结合后缓慢排出体外，半衰期γ相至少为5天。α相为1～2h，β相为2.6～5.9h。卡铂主要由肾排泄，当肌酐清除率为每分钟60ml时，24h内由肾脏清除71%，其中给药量的65%在头12h推出，6%在其次12h排出，仅有3%～5%在96h后排出。目前尚不清楚剩余药物是经胆汁还是经其他途径排出。24h尿中的铂都是有活性的卡铂，这说明仅有极少药物在体内发生代谢。肌酐清除率低的患者药物半衰期延长，因而剂量应相应调整。卡铂不经肾小管分泌，这可能是卡铂的肾毒性发生率较顺铂低的原因。 适应证 ( p/ S; s6 X% U. [与顺铂相似。主要用于卵巢癌、小细胞肺癌、头颈部癌、生殖细胞肿瘤，也可用于甲状腺癌、宫颈癌、膀胱癌及非小细胞肺癌。 禁忌证 8 e# |1 ]( C% k: r" w1.对顺铂或其他含铂化合物有过敏史者。 2.严重肾功能不全(肌酐清除率低于每分钟20ml)者。 3.孕妇及哺乳妇女。 4.老年患者。 注意事项 1.慎用：   c3 p# E  K. H3 Y$ H. p(1)感染水痘、带状疱疹等病毒者； 1 U9 B9 `9 V, `(2)肾功能不全者； (3)严重骨髓抑制者； (4)出血性肿瘤患者。 9 K, O* [) G5 `2.药物对妊娠的影响：本药有致畸作用，为FDA妊娠分类D类药物。3.用药前后及用药时应当检查或监测： (1)听力； (2)神经功能； (3)血尿素氮、肌酐清除率与血清肌酐； (4)血细胞比容、血红蛋白测定、白细胞分类与血小板计数，用药期间至少每周检查1次白细胞与血小板； (5)血清钙、镁、钾、钠含量。 ! I5 [5 |6 P: w( g4 r4.由于本药注射剂配方中含有甘露醇，故不能耐受甘露醇的患者可能也不能耐受卡铂的注射剂。 5.虽然本药对肾功能的影响低于顺铂，但用过顺铂者仍应谨慎，并注意肾功能变化。 1 v& V& Z. o9 U6.本药的骨髓毒性取决于剂量，并与药物的肾清除率成反比，患者肾功能受损时，毒性增加。 不良反应 & [$ b( L* l/ Z# ?1.骨髓抑制：为剂量限制性毒性。主要为血小板减少和白细胞降低。血小板最低点出现在用药后2～3周，第4周后恢复。白细胞最低点为2～4周，恢复较血小板慢，可延迟到6周左右。 2.消化道反应：常见但仅为轻度到中度，呕吐远较顺铂轻。 . i. I: Z  i% E; G2 G3.肾功能损害：很少引起肾功能损害，但与氨基苷类抗生素同时使用时能增加肾功能不全的发生率。用药期间应多饮水，使每天尿量在2000ml以上。 4.其他：肝功能损害(胆红素、转氨酶或碱性磷酸酶水平升高)、变态反应、口腔炎和“流感样”综合征。 . {* C& q8 I( U% ~6 z2 r7 O用法用量 $ |2 @. ]! R2 l0 O+ A1.静脉用药：1次给药，300～400mg/m2，静脉注射或静脉滴注，儿童可提高到560mg/m2，4周重复1次；或50～70mg/m2(一般1次100mg)，每天1次，连用5天，4周重复。近年来多主张根据AUC(血药浓度-时间曲线下面积)决定用药剂量。 2.腹腔内注射：300～400mg/m2，每4周1次。 7 |  }2 S+ i6 {4 N& P药物相应作用 1.本药与环孢素合用，可增加免疫抑制作用，在出现耐药性的一些肿瘤病例中可合用。 ! r5 {7 y3 E) C0 H2 z8 m8 F2.本药与活疫苗(如轮状病毒疫苗)合用时，可增加感染的危险性。故接受本药治疗的患者禁止注射活疫苗。处于缓解期的白血病患者，化疗结束后至少间隔3个月才能注射活疫苗。 6 s4 u# V# }2 j3.阿米卡星、庆大霉素、卡那霉素、奈替米星、链霉素、妥布霉素等氨基糖苷类抗生素与本药合用时耳毒性增加。 4.本药与苯妥英钠合用，可使苯妥英钠的胃肠道呼吸减少，作用降低。 临床研究 + W4 p* W+ u/ g! p卡铂为第二代铂类抗肿瘤药，其生化特性与DDP相似，但消化道反应、肾毒性及耳毒性均较低，而骨髓抑制明显。它与DDP有不完全交叉耐药，即既往使用DDP无效的患者，改用卡铂仍可能取得疗效。国外Ⅱ期临床单药试验表明，对DDP有效的肿瘤使用卡铂同样有效。另一组资料(n＞2000)采用DDP/卡铂单独或联合化疗治疗初期的卵巢癌患者，结果表明在存活期方面两者无明显差异。由于其非血液学毒性较DDP低，故更容易为患者所接受。由于作用机制与DDP相同，可代替DDP用于某些肿瘤的治疗。 $ J$ J7 \& I, c8 T( {1 [( G* U附：日本上市的使用资料：http://www.info.pmda.go.jp/go/pack/4291403A1088_1_09/ パラプラチン注射液50mg／パラプラチン注射液150mg／パラプラチン注射液450mg PARAPLATIN INJECTION（Carboplatin） PARAPLATIN INJECTION 150mg（パラプラチン注射液50mg） 4 f2 `3 K, V! P4 r8 b: MBrand name : PARAPLATIN INJECTION 50mg " Z- x' i4 s1 l& z　Active ingredient: Carboplatin 　Dosage form: injection - R1 a; \8 ?1 J7 w8 h8 ]　Print on wrapping: 1 r. ~5 ~: u+ P3 o6 m0 \! A* bPARAPLATIN INJECTION 150mg（パラプラチン注射液150mg）   : f: n* ~4 o/ x' m* z( ^0 f' |' J- oBrand name : PARAPLATIN INJECTION 150mg 　Active ingredient: Carboplatin 8 L+ x" b. R' x) R- I) a  \/ U　Dosage form: injection - D9 I1 {+ Y6 x3 e　Print on wrapping:   7 n) M  G4 I3 J4 g1 F$ SPARAPLATIN INJECTION 150mg（パラプラチン注射液450mg） Brand name : PARAPLATIN INJECTION 450mg # e+ Y0 b/ Z3 R( Z　Active ingredient: Carboplatin 　Dosage form: injection 4 U+ `- ~% _, o2 R. c5 Z6 f　Print on wrapping: " {6 S' |% u# g% _Effects of this medicine This medicine inhibits growth of cancer cells at a cell division level and destroy the cells. It is usually used to treat head and neck cancer, small cell lung cancer, testicular tumor, ovarian tumor, uterine cervical cancer, malignant lymphoma, non-small cell lung cancer, breast cancer and pediatric malignant solid tumor (neuroblastoma, retinoblastoma, hepatoblastoma, central nervous system germ cell tumor, recurrent/refractory Ewing's sarcoma family of tumor, nephroblastoma). Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines. If you have impaired renal/hepatic function, low level of white blood cells or other blood components, fever or chicken pox. 8 ~: o/ q3 v: h3 P; k* x2 x7 U•If you are pregnant, possibly pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is ((to be written by a healthcare professional)) •In general, repeat the cycle of administering once a day or 2 days with a drug cessation period of 3 to 4 weeks. •It may be administered over a long period according to your response to the treatment. •In order to prevent nausea, medicines for nausea may be used in advance. ! k3 R! d$ X* m( \- K! `Precautions while taking this medicine ' j( P8 x3 C: D) r- Y+ |• Possible adverse reactions to this medicine The most commonly reported adverse reactions include nausea/vomiting, loss of appetite, hives, loss of hair, general malaise, fever, diarrhea, stomatitis, stomachache, constipation, rash, urine with blood, protein urea, edema, chill, dehydration, weight loss, respiratory distress, peripheral neuropathy and headache. If any of these symptoms occur, consult with your doctor or pharmacist. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •fever, chill, cough, nasal discharge, dizziness, bleeding tendency, continuous bleeding, bruise, dullness, easy fatigability, shortness of breath, sore throat [myelosuppression such as pancytopenic] . X( f0 v: R8 _. e: m2 t•lips/nails turning bluish-purple, breathing difficulty/chest tightness, suddenly feeling unwell, dizziness [shock, anaphylaxy] •fever, cough, breathing difficulty/chest tightness [interstitial pulmonary disease] & ^. `. a& y; {0 P( A: a•inability to pass urine, urine with blood [acute renal failure] •jaundice [hepatic failure, hepatic function disorder, jaundice] •severe stomachache, hematoma [gastrointestinal necrosis, gastrointestinal perforation, gastrointestinal bleeding, gastrointestinal ulceration] + t2 }; O8 D/ S' Z; u5 c0 d! I7 C•severe stomachache, diarrhea [hemorrhagic enteritis, pseudomembranous colitis] •loss of appetite, nausea/vomiting, severe constipation, stomachache, abdominal distention, retention of bowel contents [paralytic ileus] •decreased consciousness, numbness of limbs, breathing difficulty [cerebral infraction, lung infraction] ' U2 ?1 g: t: z2 i# F  x- t: R•numbness of limbs, breathing difficulty [thrombosis/embolism] % @! B  z0 t% K2 f+ g* X•palpitation, shortness of breath, chest pain, breathing difficulty [myocardial infarction, congestive heart failure] •bleeding tendency, continuous bleeding, failure of urinating, yellowness in the skin or whites of the eyes, dizziness, purple spots in the skin [hemolytic-uremic syndrome] % \" \, D% ]2 i3 A) j•sudden respiratory distress [acute respiratory distress syndrome] 7 Q7 ~, M2 [( b•bleeding tendency, continuous bleeding [disseminated intravascular coagulation] •severe upper abdominal pain [acute pancreatitis] : ~: M; t% C6 }. [•hearing loss [hearing impairment] •unstableness while walking, speech disorder, memory loss, slow movement [leukoencephalopathy (reversible posterior leukoencephalopathy)] ) v" R* f) M2 \! B' H* WThe above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. * b  g) w( X! ~# ]& @0 A, z8 x$ hBristol-Myers SquibbInjection ( ^6 \  F+ F. @* X8 [" A( ~! a8 vRevised: 8/2014 , _$ n" E* F' h  l; HThe information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment. ---------------------------------------------------------------- 产地国家: 日本 0 S( A8 |* {3 ^+ E, S; _9 \& Q原产地英文商品名: - D2 R* w8 Z  iPARAPLATIN INJECTION（パラプラチン注射液）50mg/5ml/Vial ! `* |; y9 S% z: f原产地英文药品名: CARBOPLATIN 中文参考商品译名: 8 C2 e; }- T) |3 |% R  e. h' Y伯尔定注射用输液（パラプラチン注射液）50毫克/5毫升/瓶   6 F8 F2 g* F  R+ S, K7 [7 Q: ^5 d中文参考药品译名: 卡铂 9 H* g1 i) D6 _3 P' h生产厂家英文名: . n: j* L2 ]3 O/ N0 e! A% M0 b% EBRISTOL-MYERS SQUIBB 0 b% L- R5 X9 b+ S# J3 a                                登录/注册后可看大图 , c! G$ l% U. A- G" i---------------------------------------------------------------- 产地国家: 日本 - f# |0 |3 ^7 e8 b) w+ s' m原产地英文商品名: ) E1 ?0 q, M9 [5 `! p. bPARAPLATIN INJECTION（パラプラチン注射液）150mg/15ml/Vial 原产地英文药品名: CARBOPLATIN 中文参考商品译名: $ b3 _, e& L7 Y伯尔定注射用输液（パラプラチン注射液）150毫克/15毫升/瓶   ) P6 x7 T  D5 u, o- m1 E% ~中文参考药品译名: 卡铂 生产厂家英文名: 8 e0 U- s' {; D7 y, \( R* fBRISTOL-MYERS SQUIBB & t. O* g$ N6 L$ e& N2 {" U                                登录/注册后可看大图 : h% n) j! u) z3 u5 J3 B* O3 T---------------------------------------------------------------- 产地国家: 日本 ( I" h  C( @" p/ u  ^. U原产地英文商品名: PARAPLATIN INJECTION （パラプラチン注射液）450mg/45ml/Vial 原产地英文药品名: 8 B* d& X9 {) L' u7 A, |CARBOPLATIN 中文参考商品译名: 7 j( _+ y5 E( m# i) m3 A! q伯尔定注射用输液（パラプラチン注射液）450毫克/45毫升/瓶 中文参考药品译名: 卡铂 生产厂家英文名: 9 [# l( S1 a6 e3 [( IBRISTOL-MYERS SQUIBB                                 登录/注册后可看大图

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