|
部分中文 VAPRISOL 处方信息（仅供参考）
盐酸考尼伐坦/葡萄糖5%-水-全球第一个获批治疗低钠血症的药物
VAPRISOL(conivaptan hydrochloride injection) is a nonpeptide, dual antagonist of arginine vasopressin (AVP) V1A and V2 receptors.
Conivaptan hydrochloride is chemically [1,1'-biphenyl]-2-carboxamide, N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-, monohydrochloride, having a molecular weight of 535.04 and molecular formula C32H26N4O2·HCl.
INDICATIONS
VAPRISOL is indicated for the treatment of euvolemic and hypervolemic hyponatremia in hospitalized patients.
Important Limitation
VAPRISOL is not indicated for the treatment of congestive heart failure. VAPRISOL should only be used for the treatment of hyponatremia in patients with underlying heart failure when the expected clinical benefit of raising serum sodium outweighs the increased risk of adverse events for heart failure patients.
DOSAGE AND ADMINISTRATION
VAPRISOL is for intravenous use only.
VAPRISOL is for use in hospitalized patients only.
Administration of VAPRISOL through large veins and change of the infusion site every 24 hours are recommended to minimize the risk of vascular irritation.
VAPRISOL therapy should begin with a loading dose of 20 mg IV administered over 30 minutes.
The loading dose should be followed by 20 mg of VAPRISOL administered in a continuous intravenous infusion over 24 hours.
Following the initial day of treatment, VAPRISOL is to be administered for an additional 1 to 3 days in a continuous infusion of 20 mg/day. If serum sodium is not rising at the desired rate, VAPRISOL may be titrated upward to a dose of 40 mg daily, again administered in a continuous intravenous infusion.
The total duration of infusion of VAPRISOL (after the loading dose) should not exceed four days.
The maximum daily dose of VAPRISOL (after the loading dose) is 40 mg/day.
SIDE EFFECTS
The most common adverse reactions reported with VAPRISOL administration were infusion site reactions. In studies in patients and healthy volunteers, infusion site reactions occurred in 73% and 63% of subjects treated with VAPRISOL 20 mg/day and 40 mg/day, respectively, compared to 4% in the placebo group.
Infusion site reactions were the most common type of adverse event leading to discontinuation of VAPRISOL.
Discontinuations from treatment due to infusion site reactions were more common among VAPRISOL-treated patients (3%) than among placebo-treated patients (0%). Some serious infusion site reactions did occur.
The adverse reactions presented in Table 5 are derived from 72 healthy volunteers and 243 patients with euvolemic or hypervolemic hyponatremia who received VAPRISOL 20 mg IV as a loading dose followed by 40 mg/day IV for 2 to 4 days, from 37 patients with euvolemic or hypervolemic hyponatremia who received VAPRISOL 20 mg IV as a loading dose followed by 20
mg/day IV for 2 to 4 days in an open-label study, and from 40healthy volunteers and 29 patients with euvolemic or hypervolemic hyponatremia who received placebo.
The adverse reactions occurred in at least 5% of patients treated with VAPRISOL and at a higher incidence for VAPRISOL-treated patients than for placebo-treated patients.
Storage
VAPRISOL in INTRAVIA Plastic Containers should be stored at 25°C (77°F); however, brief exposure up to 40°C (104°F) does not adversely affect the product. Avoid excessive heat.
Protect from freezing. Protect from light until ready to use.
VAPRISOL®盐酸考尼伐坦注射剂，静脉使用
美国首次批准：2005 公司：安斯泰来制药美国公司
适应症和用法
剂量和给药方法，制备，兼容性和稳定性。
禁忌症，无尿的患者。
警告和注意事项
低钠血症伴心力衰竭。
过于快速的校正血清钠。
合用的VAPRISOL及药物主要通过CYP3A介导的代谢。
合用VAPRISOL和地高辛。
肝功能不全。
肾功能不全。
注射部位反应。
适应症及用法
VAPRISOL®是一种血管加压素受体拮抗剂，在euvolemic和高容量性低钠血症住院的患者，提高血清钠。
重要的限制：
VAPRISOL还没有被证明是有效的治疗心脏衰竭的症状和体征。
它并没有被建立，提高血清钠与VAPRISOL提供了的病人的症状的好处。
【用法用量】
负荷剂量：20 mg静脉给药30分钟，其次是
连续输注：每天超过20毫克/ 24小时，2至最大4天。
继初始天的治疗，剂量可以增加至
40毫克/天持续静脉滴注，提高血清钠。
监听音量状态和血清钠经常和停止，如果病人出现低血容量，低血压或不合乎要求的快速血清钠上升。
剂型和优势
静脉注射溶液：考尼伐坦盐酸盐20毫克毫升5％葡萄糖中预混合。
禁忌
低血容量性低钠血症。
并用具有强效的CYP3A抑制剂。
无尿：没有任何好处，可以预期。
已知的过敏玉米或玉米产品。
警告和注意事项
高容量性低钠血症与心脏衰竭的安全性数据的量是有限的。 VAPRISOL应该使用这样的病人后，才考虑其他的治疗方案，提高血清中的钠。
过于迅速纠正血钠监测血清钠和神经系统的状态，严重的神经系统后遗症，可能会导致从快速校正的血清钠。
肝功能损害：减少剂量的VAPRISOL。
肾功能损害：减少的剂量VAPRISOL。在严重肾功能不全的患者，不建议。
注射部位反应：严重反应时有发生。管理通过大静脉和改变注射部位每24小时。
不良反应
最常见的不良反应（发生率≥10％），注射部位反应（包括静脉炎），发热，低血钾，头痛，体位性低血压。
药物相互作用
强效CYP3A抑制剂可能会增加曝光考尼伐坦和禁忌。
一般应避免CYP3A底物。
合用地高辛可能增加，应监测地高辛浓度。
特殊人群中使用
妊娠：根据动物数据，可能引起胎儿危害。
哺乳母亲：停止药物或考虑考虑药物对母亲的重要性的护理。
【儿童用药】：有没有研究。
盐酸考尼伐坦特点
盐酸考尼伐坦是Ｖ１ａ和Ｖ２受体的双重抑制剂，体外实验显示，盐酸考尼伐坦与上述两种受体之间的亲和力极强，可达到纳摩尔（ｎａｎｏｍｏｌａｒ）级。目前已知，精氨酸加压素效应是由肾脏集合管顶膜中水通道上的Ｖ２受体所介导的。
盐酸考尼伐坦在体内与血浆蛋白广泛结合，在１０～１０００ｎｇ／ｍｌ浓度范围中，盐酸考尼伐坦的血浆蛋白结合率达到９９％。盐酸考尼伐坦仅通过细胞色素Ｐ４５０同功酶ＣＹＰ３Ａ４代谢，其代谢产物目前已发现有４种。研究发现，在静脉（１０ｍｇ）或口服（２０ｍｇ）给药后，盐酸考尼伐坦的粪排泄率约为８３％，尿排泄率约为１２％。与肾功能正常患者相比，肾功能减退（ＣｒＣｌ＜６０ｍｌ／ｍｉｎ＝患者的药时曲线下面积（ＡＵＣ）要高８０％左右。
在一项随机、双盲、使用安慰剂的对照研究中，静脉注射Vaprisol，4天，40毫克/天，可有效校正轻度和中度住院患者体内的水钠平衡。
治疗的首日就可显著提高患者的血清钠浓度。Vaprisol最常见的不良反应是注射部位反应，通常是轻度的，不需要停止用药。
“目前使用的限制水分、使用利尿药、生理盐水等治疗手段，普遍存在疗效不佳的问题。”乔治敦大学医学中心（Georgetown University Medical Center）医疗部主席、医学博士Joseph Verbalis说，“Vaprisol能有效校正低钠血症患者的水钠平衡，更好的管理这种无明显症状但预后非常严重的疾病。”
Vaprisol (Conivaptan)
Vaprisol (conivaptan) is one of the few medications on the market that directly deals with the antidiuretic hormone. The hormone affects the quantity of salt and water in the organism. A dysfunctional disease or disorder may cause this hormone to act unnaturally. At that point, the patients encounter water conservation, while the reserves of salt are very poor. The first effect of this drug implies a better urination process, while the quantity of salt is balanced to ensure the proper quantity in the organism.
Recommendations
Vaprisol (conivaptan) can only be handled and dealt with by professionals. It cannot be purchased from a drugstore or a pharmacy, especially without a prescription. Other than that, no doctor will ever put it on a prescription. It is administrated intravenously by highly trained professionals and only in accredited medical institutions, such as clinics or hospitals. The medication is run through the big veins. The whole treatment should last between 2 and 4 days. One day is mandatory and 1 to 3 days are optional, according to the treatment and to how the organism supports it.
Warnings
In order to get a treatment with Vaprisol (conivaptan), every potential patient will have to go through a series of tests. One of them implies the allergy to corn. Other concomitant treatments with CYP3A stabilizers are forbidden. At the same time, Vaprisol (conivaptan) will increase the capacity to urinate, but it doesn’t mean it can be used with this purpose. The patients who are unable to naturally eliminate the fluids will never have to rely on this medication.
Side Effects
Vaprisol (conivaptan) is usually recommended for harsh cases. It is not a supplement or a common medication. The two major side effects it comes with are the central pontine myelinolysis and unexpected reactions at the injection site. The central pontine myelinolysis simply kills the activity of a particular range of cells in the brain, while the injection site reactions usually cause allergies. For the first reason particularly, this medication is often used as a last resort.
Usage
Vaprisol (conivaptan) is proven to have an impact on the fetus in pregnant women. It is only recommended in major emergencies, when the risk is worth taking. There is a 10% chance for the fetus to suffer from a malformation as a result of this medication. When it comes to nursing women, the effects are still unknown. The specialists haven’t determined yet whether the drug is transmitted through the milk. Pediatric uses also haven’t been studied yet.
2005年12月29日，日本安斯泰来制药株式会社美国子公司在美申报的低钠血症治疗药VAPRISOL（开发代码：YM087）对体液正常型的低钠血症的适应症获得批准。这是世界上第一个治疗低钠血症的药物。
低钠血症系相对于体内总钠量而言，总体液量过剩的疾病，从全身钠量和总体液量的关系来分，大致可分为体液正常型、体液贮留型和体液减少型。据报道，低钠血症是在住院患者电解质异常中出现最频繁的症状，在美国每年有3,000万人以上的患者，约占全部住院患者的4%。由于重度低钠血症甚至危及生命，故被作为需要紧急治疗的疾病，但迄今为止尚无有效的治疗药物。
VAPRISOL系安斯泰来制药创制的具有加压素（垂体后叶分泌的收缩血管的激素，vasopressin）V1a及V2受体拮抗作用的注射剂。通过对加压素受体的拮抗作用来减少体内贮留水份，从而改善患者血中钠浓度。
2007年，日本安斯泰来制药宣布，美国FDA批准其血钠/水失调药物Vaprisol增加适应症。
Vaprisol于2005年首次获得FDA批准，用于治疗euvolemic型低血钠症，即无水肿性低血钠。此次，FDA又批准该药用于治疗血容量过多型低血钠症，即水肿性低血钠。
附件：
20101509404630.pdf
-------------------------------------------------------
注：以下产品不同的规格和不同价格，购买时请以电话咨询为准！
-------------------------------------------------------
产地国家: 美国
原产地英文商品名:
VAPRISOL 20MG/100ML/BAG 10BAGS/BOX
原产地英文药品名:
CONIVAPTAN HCL/DEXTROSE 5%-WATER
原产地英文化合物名称:
N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]- [1,1'-Biphenyl]-2-carboxamide hydrochloride
中文参考商品译名:
VAPRISOL 20毫克/100毫升/袋 10袋/盒
中文参考药品译名:
盐酸考尼伐坦/葡萄糖5%-水
生产厂家中文参考译名:
ASTELLAS
生产厂家英文名:
ASTELLAS
-------------------------------------------------------
产地国家: 美国
原产地英文商品名:
VAPRISOL 20MG/100ML/BAG 5BAGS/BOX
原产地英文药品名:
CONIVAPTAN HCL/DEXTROSE 5%-WATER
原产地英文化合物名称:
N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]- [1,1'-Biphenyl]-2-carboxamide hydrochloride
中文参考商品译名:
VAPRISOL 20毫克/100毫升/袋 5袋/盒
中文参考药品译名:
盐酸考尼伐坦/葡萄糖5%-水
生产厂家中文参考译名:
ASTELLAS
生产厂家英文名:
ASTELLAS
| 
