Information on VAPRISOL 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 40 healthy 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. 部分中文 VAPRISOL 处方信息（仅供参考） 通用名称VAPRISOL Conivaptan盐酸20mg/ampule;稀释后的静脉输液;含有酒精，丙二醇。 法律分类： 接收 药理班VAPRISOL 双精氨酸加压素（V1A和V2）受体拮抗剂。 制造商VAPRISOL 安斯泰来制药美国公司 适应症VAPRISOL Euvolemic和高容量性低钠血症患者在住院。 成人剂量VAPRISOL 通过大静脉管理，旋转输注部位每24小时。负荷剂量：20毫克静脉30分钟以上，由20毫克持续静脉输注24小时以上。初步治疗后的一天，给20mg/day连续1-3天为一个额外的静脉输注;可滴定到最大40mg/day如果血清钠是不想要的速度上升。最大负荷剂量后持续时间：4天。 儿童剂量为VAPRISOL 不推荐。 另外： VAPRISOL预混 禁忌的VAPRISOL 低血容量性低钠血症。伴随强大的CYP3A4抑制剂（如酮康唑，伊曲康唑，克拉霉素，利托那韦，茚地那韦）。预混：玉米或玉米产品过敏。 警告/注意事项的VAPRISOL 不适用于治疗瑞士法郎。肾或肝功能不全（包括腹水，肝硬化，门静脉高压症）。监测血清钠浓度，容量状态，神经功能状态。如果停止上涨过快血清钠（“12mEq / L时，每24小时）; 5月恢复，如果减少剂量持续或复发，低钠血症，也没有神经系统后遗症的证据。如果停止或低血压，低血容量的发展，愿继续在减少剂量，而不是如euvolemic低血压。劳动和交付。妊娠（Cat.C）。哺乳的母亲。 互作VAPRISOL 见禁忌。 Potentiated由CYP3A4抑制剂。 Potentiates CYP3A4的底物（如，咪唑安定，辛伐他汀，氨氯地平），密切监察或避免，如果中止合并治疗，这些药物前允许恢复后至少24小时的conivaptan政府任期结束。注意地高辛。 不良反应为VAPRISOL 输注部位反应（例如，静脉炎，红斑，疼痛），胃肠不适，头痛，低钾血症，低钠血症，体位性低血压，超或低血压，末梢水肿，口渴。 如何VAPRISOL提供？ 安培- 10 预混- 10 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。 FDA approves new formulation Vaprisol Posted by Kimberly O'Brien on October 24, 2008 The U.S. Food and Drug Administration has approved Astellas Pharma US, Inc.’s new Vaprisol (conivaptan hydrochloride injection) premixed in 5% Dextrose. An arginine vasopressin (AVP) receptor antagonist, Vaprisol is the only drug approved and indicated for use in the treatment of patients with either kind of hyponatremia – euvolemic or hypervolemic. Its single-use (100ml) premixed formulation is available in an INTRAVIA(R) Container. The latest formulation will simplify preparation as it requires no mixing or measuring. Its safe usage period is six months longer than the original ampule formulation. FDA Approval Tags: AVP receptor antagonist, FDA, hyponatremia, injection, Vaprisol VAPRISOL Generic Name for VAPRISOL Conivaptan HCl 20mg/ampule; for IV infusion after dilution; contains alcohol, propylene glycol. Legal Classification: Rx Pharmacological Class for VAPRISOL Dual arginine vasopressin (V1A and V2) receptors antagonist. Manufacturer of VAPRISOL Astellas Pharma US, Inc. Indications for VAPRISOL Euvolemic and hypervolemic hyponatremia in hospitalized patients. Adult dose for VAPRISOL Administer via large veins; rotate infusion site every 24hrs. Loading dose: 20mg IV over 30mins, followed by 20mg continuous IV infusion over 24hrs. After initial day of treatment, give 20mg/day continuous IV infusion for an additional 1–3 days; may titrate up to max 40mg/day if serum sodium is not rising at desired rate. Max duration after loading dose: 4 days. Children's dosing for VAPRISOL Not recommended. Also: VAPRISOL PREMIXED Contraindications for VAPRISOL Hypovolemic hyponatremia. Concomitant potent CYP3A4 inhibitors (eg, ketoconazole, itraconazole, clarithromycin, ritonavir, indinavir). Premixed: corn or corn product allergy. Warnings/Precautions for VAPRISOL Not for treating CHF. Renal or hepatic impairment (including ascites, cirrhosis, portal hypertension). Monitor serum sodium concentration, volume status, neurologic status. Discontinue if serum sodium rises too rapidly (>12mEq/L per 24hrs); may resume at reduced dose if hyponatremia persists or recurs and no evidence of neurologic sequelae. Discontinue if hypovolemia or hypotension develops; may resume at reduced dose if euvolemic and not hypotensive. Labor & delivery. Pregnancy (Cat.C). Nursing mothers. Interactions for VAPRISOL See Contraindications. Potentiated by CYP3A4 inhibitors. Potentiates CYP3A4 substrates (eg, midazolam, simvastatin, amlodipine); monitor closely or avoid; if discontinuing concomitant therapy, allow at least 24hrs after end of conivaptan administration before resuming these drugs. Caution with digoxin. Adverse Reactions for VAPRISOL Infusion site reactions (eg, phlebitis, erythema, pain), GI upset, headache, hypokalemia, hyponatremia, orthostatic hypotension, hyper- or hypotension, peripheral edema, thirst. How is VAPRISOL supplied? Amps—10 Premixed—10 Related Disease: Hyponatremia