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盐酸伊立替康注射液（开普拓Campto®）

2011-08-29 11:43:53 作者：新特药房来源：互联网浏览次数：232 文字大小：【大】【中】【小】

简介： 【药品名称】商品名：开普拓通用名：盐酸伊立替康注射液【成分】分子式成分：开普拓。赋形剂的组成：山梨醇，乳酸和注射用水。【性状】淡黄色澄明液体。赋形剂的组成：山梨醇，乳酸和注射用水。 ...

关键字：盐酸伊立替康注射液

【药品名称】
商品名：开普拓

通用名：盐酸伊立替康注射液
【成分】

分子式成分：开普拓。赋形剂的组成：山梨醇，乳酸和注射用水。

【性状】

淡黄色澄明液体。赋形剂的组成：山梨醇，乳酸和注射用水。溶液的pH值用氢氧化钠调到35。

【适应症】

晚期大肠癌患者的治疗。与5-氟尿嘧啶和亚叶酸联合治疗既往未接受化疗的晚期大肠癌患者，作为单一用药，治疗经含5-氟尿嘧啶化疗方案治疗失败的患者。

【药理作用】

药效学特性：抑制细胞生长的拓扑异构酶I抑制剂（L-抗肿瘤和免疫抑制剂）。实验资料：伊立替康是半合成喜树碱的衍生物，是能特异性抑制DNA拓扑异构酶 I的抗肿瘤药。它在大多数组织中被羧酸酯酶代谢为SN-38，而后者作用于提纯的拓扑异构酶I的活性比伊立替康更强，且对几种鼠和人肿瘤细胞系的细胞毒性也强于伊立替康。SN-38或伊立替康可诱导单链DNA损伤，从而阻断DNA复制叉，由此产生细胞毒性。这种细胞毒性是时间依赖性的，并特异性作用于S 期。在体外实验中，并未发现伊立替康和SN-38可被P-糖蛋白MDR有效识别，且显示出对阿霉素和长春花碱耐药的细胞系仍有细胞毒作用。另外，在体内实验中，伊立替康对鼠肿瘤模型显示了广谱的抗瘤活性（PPO3胰导管腺癌，MA -16/C乳腺癌，C38和C51结肠腺癌）并有抗人异种移植肿瘤的活性（CO03胰导管腺癌，MA-16 /C乳腺癌，C38和C51结肠腺癌）并有抗人异种移植肿瘤的活性（Co-4结肠腺癌，MX-1乳腺癌，St-15和SC-6胃腺癌），伊立替康对表达 P-糖蛋白MDR的肿瘤（长春新碱和阿霉素耐药的P3.88白血病）也有抗瘤活性。开普拓除具有抗肿瘤活性外，最相关的药理学作用为抑制乙酰胆碱酯酶。
【药学动力学】
主要毒副作用的强度（如白细胞减少症和腹泻）与母体药物和其代谢产物SN-38的曲线下面积相关。在单药治疗中，血液学毒性（白细胞及中性粒细胞下降至最低点）或腹泻的程度与伊立替康和其代谢产物SN-38的曲线下面积值显著相关。伊立替康和SN-38（其活性代谢产物）的药代动力学特性在I期临床试验中进行了研究，60例患者接受了推荐剂量方案的药物治疗，即30分钟静脉滴注开普拓100-750mg/m2。伊立替康的动力学曲线是非剂量依赖性的。在临床试验中登记的患者接受不同伊立替康给药方案，其药代动力学均相似。其血浆代谢既是二室的又是三室的。三室模型中第一阶段的平均血浆半衰期为12分钟，第二阶段为2.5小时，最终阶段为14.2小时。在使用推荐剂量350mg/m2静滴结束时伊立替康和SN-38达到血浆峰浓度，分别为7.7μg /ml，56ng/ml，其曲线下面积分别为34μgh/ml，451ngh/ml，其稳态分布容积很大，并保持相对稳定，为剂量的函数，平均为 157L/m2。机体总清除率平均值为15L/h/m2，且在同一患者的不同周期保持稳定。SN-38在不同个体其药物代谢参数变化很大。伊立替康和 SN-38.24小时平均尿排泄率分别为使用剂量的19.9%和0.25%。关于伊立替康药代动力学的II期临床试验在72例肿瘤患者中进行。限制采样模型计算出的药代动力学参数与I期研究的参数十分接近。体外实验中，伊立替康和SN-38的血浆蛋白结合率分别约为65%和95%。药代动力学资料表明5氟尿嘧啶/亚叶酸与伊立替康之间没有协同作用。
【用法用量】
仅用于成人。推荐剂量：在单药治疗中（对既往接受过治疗的患者）：开普拓的推荐剂量为350mg/m2，静脉滴注30-90分钟，每3周用一次。在联合治疗中（对既往未接受过治疗的患者）：通过以下方案对与5-氟尿嘧啶（5-FU）和亚叶酸（FA）联合应用的安全性和有效性进行了评价。开普拓加5-氟尿嘧啶（5-FU）/亚叶酸（FA）的2周治疗方案。开普拓的治疗推荐剂量是180mg/m2，每2周给药一次，持续静脉滴注30到90分钟，随后滴注亚叶酸和5-氟尿嘧啶。
【不良反应】
对765例接受单药治疗，使用推荐剂量350mg/m2的患者，及145例接受联合治疗，使用开普拓推荐剂量180mg/m2，每2周给药一次，联合5- 氟尿嘧啶/亚叶酸治疗的患者进行的研究表明，有一些不良反应可能与使用开普拓有关。
胃肠道：迟发性腹泻：腹泻（用药24小时后发生）是开普拓的剂量限制性毒性反应。在单药治疗中：在所有听从腹泻处理措施忠告的患者中有20%发生严重腹泻。在可评估的周期内，14%出现严重腹泻。出现第一次稀便的中位时间为滴注开普拓后第5天。
在联合治疗中：在所有听从腹泻处理措施忠告的患者中有13.1%发生严重腹泻。在可评估的周期内，3.9%出现严重腹泻。个别病例出现伪膜性结肠炎，其中1例已被细菌学证实（难辨梭状芽胞杆菌）。
恶心与呕吐：在单药治疗中，使用止吐药后约10%患者发生严重的恶心及呕吐。在联合治疗中，严重的恶心和呕吐发生率较低（分别为患者的2.1%和2.8%）。
其他胃肠反应：腹泻及/或呕吐伴随与腹泻及/或呕吐相关的脱水症状已有报导。可发生与开普拓及/或氯苯哌酰胺治疗有关的便秘。在单药治疗中有少于10%的患者发生。在联合治疗中有3.4%的患者发生。少见发生肠梗阻或胃肠出血报导报道。罕见肠穿孔。
其他轻微反应如：厌食，腹痛及粘膜炎。血液学：中性粒细胞减少症是剂量限制性毒性。中性粒细胞减少症是可逆转和非蓄积的；无论在单药治疗或联合治疗中，到最低点的中位时间为8天。在单药治疗中：78.7%的患者均出现过中性粒细胞减少症，严重者（中性粒细胞计数<500/mm3）占 22.6%。在可评价的周期内，18%出现中性粒细胞计数<1，000/mm3，其中7.6%中性粒细胞计数<500/mm3。通常在第22 天完全恢复正常。62%的患者，按周期为17%，出现严重中性粒细胞减少症合并发热。10.3%的患者（按周期为2.5%）出现感染；5.3%的患者（按周期为1.1%）出现严重中性粒细胞减少症引起的感染，2例出现过中性粒细胞减少症，严重者（中性粒细胞计数<500/mm3）占22.6%。在可评价的周期内，18%出现中性粒细胞计数<1，000/mm3，其中7.6%中性粒细胞计数<500/mm3。通常在第22天完全恢复正常。 6.2%的患者，按周期为1.7%，出现严重中性粒细胞减少症合并发热。10.3%的患者（按周期为2.5%）出现感染；5.3%的患者（按周期为 1.1%）出现严重中性粒细胞减少症合并感染，2例导致死亡。贫血的发生率为58.7%（其中8%Hb<8g/dL，0.9%Hb<65g /dL）。7.4%的患者（按周期为1.8%）出现血小板减少症（<100，000/mm3），其中0.9%的患者血小板计数£50，000 /mm3，按周期为0.2%。几乎所有患者均在第22天恢复。
在联合治疗中：82.5%的患者出现中性粒细胞减少症，严重者（中性粒细胞计数<500/mm3）占9.8%。在可评价的周期内，67.3%出现中性粒细胞计数<1，000/mm3，其中2.7%中性粒细胞计数<500/mm3。通常在7-8天内完全恢复正常。3.4%的患者（按周期为0.9%）出现严重中性粒细胞减少症合并发热。2%的患者（按周期为 0.5%）出现感染；2.1%的患者（按周期为0.5%）出现严重中性粒细胞减少症引起的感染，1例合并感染，1例导致死亡。贫血的发生率为97.2% （2.1%Hb<8g/dL）。32.6%的患者（按周期为21.8%）出现血小板减少症（<100，000/mm3），无严重血小板减少症出现（<50，000/mm3）。
在上市后使用中，曾报道一例因抗血小板抗体导致外周血小板减少症的病例。急性胆碱能综合征：在单药治疗中9%的患者出现短暂严重的急性胆碱能综合征，而在联合治疗中仅为1.4%。
主要症状为：早发性腹泻及其他症状，例如：用药后第一个24小时内发生：腹痛、结膜炎、鼻炎、低血压、血管舒张、出汗、寒战、全身不适、头晕、视力障碍、瞳孔缩小、流泪及流涎增多。以上症状于阿托品治疗后消失。其他作用：早期的反应如呼吸困难，肌肉收缩、痉挛及感觉异常等均有报道。在单药治疗中少于10%的患者出现严重乏力，而在联合治疗中为6.2%。其与使用开普拓的确切关系尚未阐明。常见脱发，为可逆转的。在单药治疗中12%的患者在无感染及严重中性粒细胞减少症的情况下出现发热，而在联合治疗中为6.2%。轻度皮肤反应，变态反应及注射部位的反应尽管不常见，但也有报道。在与腹泻和/或呕吐有关的脱水患者或败血症患者中，少数病人出现肾功能不良、低血压或循环衰竭。实验室检查：单药治疗：在无进展性肝转移的患者中，血清中短暂、轻至中度转氨酶、碱性磷酸酶、胆红素水平升高的发生率分别为9.2%、8.1%和1.8%。7.3%的患者出现短暂的轻至中度血清肌酐水平升高。
联合治疗：在无进展性肝转移的患者中，血清中暂时性的SGPT、SGOT、碱性磷酸酶或胆红素水平升高（1度和2度）的发生率分别为15%、11%、11%和10%。暂时性的3度升高发生率分别为患者的0%、0%、0%和1%。未观察到4度升高。
【禁忌】
慢性肠炎和/或肠梗阻炎性肠病和/或肠梗阻，对盐酸伊立替康三水合物或开普拓中的赋型剂有严重过敏反应史。孕期和哺乳期。胆红素超过正常值上限的1.5 倍。严重骨髓功能衰竭。
【药物相互作用】
伊立替康与神经肌肉阻滞剂之间的相互作用不可忽视，开普拓具有抗胆碱酯酶活性，具有抗胆碱酯酶活性的药物可延长琥珀胆碱的神经肌肉阻滞作用，非去极化神经肌肉阻滞剂可延长琥珀胆碱的神经肌肉阻滞作用，而非去极化药物的神经肌肉阻滞作用可能被拮抗。配伍禁忌：尚不清楚。请勿与其他药物混合。
【规格】
2ml:40mg*1瓶 5ml:0.1g瓶/盒
【批准文号】
注册证号H20080574
【生产企业】
Aventis Pharma (Dagenham)

CAMPTO

Campto Information

The active component of Campto is a widely known substance called Irinotecan. This and the other ingredients of this medical remedy make it one of the most commonly employed chemotherapy medicines; in other words, a therapy course with this product can be prescribed in the therapy of patients who are suffering from bowel cancer.

Campto Indications

Numerous individuals from all over the world who have been diagnosed with a certain type of cancerous medical condition benefited from an intensive therapy course with Campto. Most patients who have been prescribed a treatment trial with this medication were suffering from bowel cancer.

Campto Warnings

All individuals who are to employ a therapy course with this medication should be aware of the fact that their therapy trial with Campto may increase their risk of developing thrombosis (blood clot). The symptoms of such a condition include redness, pain and swelling of one of the limbs (a leg, in general), chest pain, breathlessness, and so on. The presence of this condition is considered a medical emergency. As such, we strongly recommend all patients who develop any of these symptoms during their therapy trial with Campto to alert their main clinical prescriber or the health care professional who is bound to monitor their treatment.

All female patients should know that an intensive intake of this medical product may affect their ability of becoming pregnant. Furthermore, the use of Campto by male individuals may prevent them from being able to father a child. We recommend all patients who want to start using this medication to discuss all fertility-related issues with their physicians. All individuals with an active sexual life should employ an effective contraceptive method during their therapy with this product, and at least a couple of months after the end of their treatment, as if a pregnancy does arise during your use of Campto, the baby is to present severe, irreversible harm.

Campto Intake Guidelines

Most individuals are administered their prescribed doses of Campto as an infusion (a medical procedure also commonly referred to as a drip) through a special, fine tube (called by medical specialists a cannula). The IV administration of this product should be supervised by a well trained medical specialist. If you want to benefit to the full extent from your therapy’s beneficial results you should make sure that you obey all of your physician’s directions concerning your prescribed doses of this medication.

The average therapy span of one’s use of Campto involves several cycles (sessions) of treatment. For this reason, some individuals were administered this medication for several months. The length of one’s therapy course with this anti-cancer medication depends on the type of cancer that the patient is suffering from, on the severity of the patient’s condition, and so on. In most cases, the individual’s therapy with Campto is accompanied by the use of other chemotherapy medical remedies, as combination regimens are known to be the most effective therapeutic approach in such cases. You can discuss your therapy plan with your main medical prescriber.

Campto Dosage

All individuals are to be prescribed the correct Campto dosing schedule by their main health care prescriber. Depending on the patient’s response to his or her therapy course with this anti-cancer remedy, he or she may be prescribed a higher dose of this product. In other cases, the patient’s current dose of Campto may be diminished.

Campto Overdose

Over-dosage with this medication is uncommon, as the administration of a dose of Campto is generally supervised by a well trained medical provider. In such cases, the patient must be immediately hospitalized, and he or she should be administered the adequate symptomatic / supportive therapeutic approach.

Campto Missed Dose

As most prescribed doses of Campto should be administered under the strict supervision of the patient’s main clinical prescriber, missed doses of this product are unlikely to disrupt one’s therapy with this anti-cancer product (especially if the patient remains hospitalized during his or her therapy with this medication). For more information, study the drug’s label.

Campto Side Effects

Each individual is known to present a different reaction to their chemotherapy routine. While certain patients did not develop any severe symptoms (or developed only a few clinical manifestations), others have accused a wide variety of side effects due to their therapy course with Campto. The most common clinical manifestations that may affect an individual who is following a chemotherapy session with this anti-cancerous medication include the symptoms of the acute cholinergic syndrome (diarrhea, stomach cramps, increased production of saliva, increased sweating, and so on). These symptoms occur due to an increase of the body’s average increase of acetylcholine (a common chemical) and they develop during the administration of Campto or within a day after it.

Such clinical conditions can be prevented and also kept under control with the help of another medical product, atropine. This medication is generally administered as a subcutaneous injection. In some cases, certain patients had to be administered more than one dose of atropine in order to deal with the side effects of this drug.

Campto Drug Reactions

All individuals must be well aware of the fact that their therapy trial with Campto may be severely affected by the unauthorized use of other medical products as patients have suffered from a set of harmful consequences due to this matter. In some cases, even the use of herbal products, complementary therapies, and so on is not advised during one’s treatment course with Campto. The product’s medical guide-book should contain further information concerning this matter.