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 详细处方信息以本药内容附件PDF文件（201431222240415.pdf）的“原文Priscribing Information”为准
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部分中文齐考诺肽处方资料（仅供参考）

分类名称
一级分类：神经系统药物 二级分类：镇痛药物 三级分类：其他 
 
药品英文名
Ziconotide
 
药品别名
Prialt
 
药物剂型
鞘内滴注剂：20ml (25mg/ml)；1ml (100mg/ml)；2ml (100mg/ml)；5ml(100mg/ml)。
 
药理作用
本品为含有3个二硫键和25个氨基酸的多肽。本品与位于脊髓背角浅层的初级伤害性传入神经上的N-型钙通道结合，抑制初级传人神经末梢兴奋性递质的释放，具有抗伤害感受作用。本品不与阿片受体结合，其药理作用也不被阿片受体拮抗剂所阻断。在动物模型中，本品可改变阿片引起的胃肠动力降低，但不能改善吗啡引起的呼吸抑制。给大鼠鞘内注射本品，同时给予吗啡、巴氯芬或可乐定，镇痛作用增强。本品与吗啡合用，不能防止大鼠对吗啡的耐受性。
 
药动学
慢性疼痛患者鞘内滴注本品1～10mg，1h后脑脊液中药代动力学显示，药时曲线下面积(AUC)和峰浓度(Cmax)呈剂量依赖性，表观分布容积为(155±263)ml，清除率(CL)为(0.38±0.56)ml/min，消除半衰期(t1/2)为(4.6±0.9)h。本品血浆蛋白结合率为50%，表观分布容积与脑脊液体积相近(140ml)。本品可被内肽酶和肽链端解酶切开，本品进如入体循环后可被存在于多种器官中的肽酶/蛋白酶溶蛋白性裂解，成为肽类片段或游离氨基酸。经尿液排出的原药不足1%。
 
适应证
本品用于适合鞘内注射并且对其他治疗(如全身镇痛药、辅助治疗或鞘内注射吗啡)不能耐受或无效的严重慢性疼痛患者。
 
禁忌证
1.对本品及其中成分过敏者禁用。
2.正在接受能增加鞘内给药危险的其他治疗的患者禁用。
3.有精神病史的患者应避免使用。
4.微量输液泵部位感染患者、未控制的出血患者及椎管阻塞影响脑脊液循环的患者禁用。
 
注意事项
1.本品生殖毒性分级为C，只有当可能的受益高于危险时方可用于孕妇。尚不知本品是否经乳汁分泌，哺乳期妇女使用本品应根据药物对母体的重要性确定停止哺乳或停止用药。
2.使用本品期间，从事危险活动、需要集中精力或运动协调性工作(如机械操作、驾车)应谨慎。
3.与其他中枢神经系统抑制剂合用应谨慎，由于可能的累加效应，本品剂量应进行调整。
4.儿童用药安全性尚未评价。
5.老年人用药应谨慎，从低剂量开始使用。
6.超过最高推荐剂量，临床表现为药理作用增强(如共济失调、眼球震颤、头晕、木僵、脊柱肌阵挛、混乱、镇静、低血压、言语困难、恶心、呕吐)。本品无特效解毒剂，出现药物过量应采取支持治疗直到症状缓解。本品不与阿片受体结合，因此其药理作用不能被阿片受体拮抗剂所阻断。出现低血压后，可采用卧位，必要时给予升压药。
7.原药2～8℃冷藏保存，稀释液2～8℃冷藏可保存24h，避免冷冻，避光。
 
不良反应
发生率5%以上的不良反应如下。
1.全身：无力、头痛、疼痛、发热。
2.消化系统：恶心、呕吐、腹泻、食欲减退。
3.神经系统：头晕、嗜睡、混乱、共济失调、异常步态、记忆缺陷、张力过高、焦虑、语言障碍、失语症、眼球震颤、感觉迟钝、幻觉、神经质、感觉异常、眩晕。
4.特异感觉：视觉异常。
5.泌尿生殖系统：尿潴留。
 
用法用量
鞘内滴注，初始剂量根据患者情况而定，最高初始剂量为2.4mg/天(0.1mg/h)，以后剂量可提高但每周不超过2～3倍，直到第21天时达到最高推荐剂量19.2mg/天(0.8mg/h)。通过调整给药泵的滴速达到确定的给药剂量。剂量的调整应根据患者的疼痛程度及不良事件的发生情况而定，在临床试验中，21天时的平均药物剂量为6.9～19.2mg/天(0.29～0.8mg/h)。本品可采用剂量可调的植入式自动定时给药泵或外置式微量输液泵及导管鞘内滴注。可使用未稀释的原药液(25mg/ml，每支20ml)或稀释液(100mg/ml，每支1ml、2ml或5ml，用0.9%氯化钠注射液稀释)。
 
药物相应作用
本品与其他中枢神经系统抑制剂合用，可使中枢神经系统不良事件(如头晕、混乱)的发生率升高。

PRIALT is the only non-opioid intrathecal (IT) therapy approved for severe chronic pain.
Indication: PRIALT® (ziconotide intrathecal infusion) is indicated for the management of severe chronic pain in patients for whom intrathecal (IT) therapy is warranted, and who are intolerant of or refractory to other treatment, such as systemic analgesics, adjunctive therapies, or IT morphine.

Contraindications: PRIALT is contraindicated in patients with a known hypersensitivity to ziconotide or any of its formulation components and in patients with any other concomitant treatment or medical condition that would render IT administration hazardous. Patients with a pre-existing history of psychosis should not be treated with ziconotide. Contraindications to the use of IT analgesia include conditions such as the presence of infection at the microinfusion injection site, uncontrolled bleeding diathesis, and spinal canal obstruction that impairs circulation of CSF.

WARNINGS:
Severe psychiatric symptoms and neurological impairment may occur during treatment with PRIALT. Patients with a pre-existing history of psychosis should not be treated with PRIALT. All patients should be monitored frequently for evidence of cognitive impairment, hallucinations, or changes in mood or consciousness. PRIALT therapy can be interrupted or discontinued abruptly without evidence of withdrawal effects in the event of serious neurological or psychiatric signs or symptoms.

Precautions:
Meningitis and Other Infections
Meningitis can occur due to inadvertent contamination of the microinfusion device and other means. Patients, caregivers, and healthcare providers must be particularly vigilant for the signs and symptoms of meningitis.

Cognitive and Neuropsychiatric Adverse Events
Use of PRIALT has been associated with CNS-related adverse events, including psychiatric symptoms, cognitive impairment, and decreased alertness/unresponsiveness. The PRIALT dose should be reduced or discontinued if signs or symptoms of cognitive impairment develop, but other contributing causes should also be considered.

Reduced Level of Consciousness
Patients have become unresponsive or stuporous while receiving PRIALT. PRIALT should be discontinued until the event resolves, and other etiologies should be considered.

Elevation of Serum Creatine Kinase (CK-MM)
In clinical studies (mostly open label), 40% of patients had serum creatine kinase (CK) levels above the upper limit of normal (ULN), and 11% had CK levels that were =3 times the ULN. Most patients who experienced elevations in CK, even for prolonged periods of time, did not have limiting side effects. It is recommended that physicians monitor serum CK in patients undergoing treatment with PRIALT periodically.

Adverse Reactions:
The most frequently reported adverse events (25%) in the 1,254 patients (662 patient years) in  clinical trials were dizziness, nausea, confusional state, and nystagmus. Serious adverse events and discontinuation of PRIALT for adverse events are less frequent when the drug is slowly titrated over 21 days than with a faster titration schedule.

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 详细处方信息以本药内容附件PDF文件（201431222240415.pdf）的“原文Priscribing Information”为准
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