XEOMIN
制造商：
梅尔茨制药
类药物：
神经肌肉阻滞剂。
活性成分（S）：
IncobotulinumtoxinA 50个单位，100个单位，每小瓶冻干PWD;重组和稀释后的IM注射含有人血清白蛋白;不含防腐剂。
指示（S）：
在成年人的颈部肌张力障碍，减少在这两个肉毒毒素的天真和先前治疗的患者头部位置异常和颈部疼痛的严重程度。在以前onabotulinumtoxinA治疗成年人的眼睑。
药理作用：
XEOMIN在肌张力障碍的管理发挥其作用，通过阻断神经肌肉接头处的胆碱能传递。这一行动是通过抑制乙酰胆碱的释放，从周边胆碱能神经末梢，按照下列顺序发生：XEOMIN结合和胆碱能神经末梢的内在分子的轻链的一部分，然后转运到神经末梢的细胞质，其次是酶裂解SNAP25，突触前的靶蛋白的乙酰胆碱的释放至关重要。脉冲传输是由形成新的神经末梢重新建立。
临床试验：
在第三阶段，随机，双盲，安慰剂对照研究涉及233例基线多伦多西方痉挛性斜颈量表，主要转动颈部肌张力障碍（TWSTRS）总分≥20，TWSTRS XEOMIN在颈部肌张力障碍的疗效评价严重程度评分≥10，TWSTRS残疾评分≥3，TWSTRS疼痛评分≥1。患者随机接受一个单一的管理研究剂（XEOMIN 240个单位，XEOMIN 120单位，或安慰剂）（4.8mL）。主要疗效终点是TWSTRS总评分从基线到4周注射后的变化。在意向性治疗（ITT）人群中，XEOMIN 240单位组和TWSTRS总分从基线到4周的变化，而安慰剂组之间的差异是-9分; XEOMIN 120单位组和之间的区别安慰剂组为-7.5点。每个XEOMIN组与安慰剂组比较统计学意义，P <0.001。谁是A型肉毒毒素的天真和那些曾收到此之前的研究A型肉毒毒素的患者XEOMIN的疗效相似。
在第三阶段，随机，双盲，安慰剂对照研究，涉及109个良性原发性眼睑痉挛患者与基线扬科维奇量表，考察了XEOMIN（JRS的）严重性子分数≥2，和稳定的理想的治疗反应onabotulinumtoxinA历届政府（肉毒杆菌）。患者随机接受单一XEOMIN治疗，是最近期的肉毒杆菌注射前研究，或安慰剂相似。在主要疗效终点，在ITT人群，JRS的严重性子分数从基线到6周的变化XEOMIN组和安慰剂组之间的差异是-1点。 XEOMIN组与安慰剂组比较统计学意义，P <0.001。
法律分类：
RX
成人：
应管理和管理由经验丰富的医师。 ≥0-18岁：个性化;见文献。颈部肌张力障碍：初始总剂量：每疗程120单位。 onabotulinumtoxinA以往治疗眼睑痉挛：（以前处理）：用相同剂量（前剂量不详）：最初1.25-2.5单位/注射部位。两只眼睛：总的初始剂量：最大70个单位（35单位/眼）。为两种：剂量，数量，注射地点的位置应根据参与肌肉的数量和位置，肌张力障碍或眼睑的严重性，和以往任何肉毒毒素INJ。可重复治疗，每12个星期，如果没有足够的反应。
儿童：
<18yrs：不推荐。
禁忌症（S）：
在拟议的注射部位的感染。
警告/注意事项：
不与其他A型肉毒毒素产品互换。预先存在吞咽困难或呼吸困难。较小的颈部肌肉质量或那些需要到胸锁乳突肌双边注射的病人：吞咽困难的风险增加。神经肌肉疾病（如兰伯特 - 伊顿综合征，重症肌无力，ALS）;密切监察。呼吸功能受损;显示器。窄角型青光眼。含有人血清白蛋白;可能的病毒传播疾病的监测。老人。怀孕（Cat.C）。哺乳的母亲。
互动（补）：
可能可以由氨基糖甙类抗生素或其他药物干扰神经肌肉传导（如筒箭毒型肌肉松弛剂）。伴抗胆碱能药物，会增强抗胆碱作用。伴随其他A型肉毒毒素产品或肌肉松弛剂，会增强肌肉无力。
不良反应（S）：
颈部肌张力障碍：吞咽困难（可能是严重的），颈部疼痛，肌肉无力，注射部位反应，肌肉骨骼疼痛;眼睑：眼睑下垂，眼干，口干，腹泻，头痛，视力障碍，呼吸困难，鼻咽炎，上呼吸道感染，角膜曝光/溃疡，眼睑外翻（避免注射下睑面积）;两种：呼吸衰竭，停止，如果发生过敏反应，传播毒素的作用（可能是致命的），可能形成抗体。
如何提供：
单次使用的小瓶-1
XEOMINFDA已批准Xeomin治疗颈部肌张力障碍和眼睑痉挛
2010年8月2日，麦氏制药( Merz PHarmaceuticals)宣布，美国食品药品管理局(FDA)已批准Xeomin一种A型肉毒杆菌毒素。该药品适用于治疗成人颈部肌张力障碍，降低异常头位和颈部疼痛的严重程度(无论患者之前是否接受过肉毒杆菌毒素治疗)，还适用于治疗有Botox(onabotulinumtoxinA)治疗史的成人眼睑痉挛。
Xeomin是目前惟一一种在配液前无需冷藏的肉毒杆菌毒素。FDA在审查两项关键性美国临床试验的结果后做出批准Xeomin的决定，这两项试验的受试者是确诊为颈部肌张力障碍或眼睑痉挛的成人患者。另外，在递交至FDA的审批材料中还包括在欧洲进行的有效性比较研究的数据，比较药物为Xeomin与Botox(onabotulinumtoxinA)。
接受Xeomin注射的颈部肌张力障碍患者最常见的不良反应为吞咽困难、颈部疼痛、肌无力、注射部位疼痛和肌肉骨骼疼痛。在眼睑痉挛的患者中最常见的不良反应包括眼睑下垂、眼干、口干、腹泻、头痛、视力损害、呼吸困难、鼻咽炎和呼吸道感染。
临床医生应知道，颈部肌张力障碍的患者、颈部肌肉量较少者以及需要胸锁乳突肌双侧注射者发生吞咽困难的风险增加。胸锁乳突肌内限量注射可减少吞咽困难的发生。
内科医生还应知道，眼睑痉挛的患者眼轮匝肌内注射Xeomin可导致眨眼动作减少和角膜暴露，且可能会发生溃疡或穿孔。若在先前注射肉毒杆菌毒素时出现复视，则不应反复行下眼睑注射。
生产厂家警告：Xeomin及所有的肉毒杆菌毒素制品的作用都可能会由注射区向远处扩散，产生肉毒杆菌毒素效应。目前有报告指出，这些症状可在注射后数小时至数周发生。因强直而接受治疗的儿童出现症状的风险可能最大，但成人亦可出现相关症状，尤其是存在易出现这些症状的基础疾病的患者。
Xeomin的效价单位与其他肉毒杆菌毒素制剂)不可互换使用。因此，不能将Xeomin的生物活性单位与其他任一肉毒杆菌毒素制品的单位相比较或转化。
据麦氏公司称，自2005年以来，全世界已有超过84,000例患者接受Xeomin治疗。美国是批准Xeomin治疗颈部肌张力障碍和眼睑痉挛的第20个国家
Manufacturer:
Merz Pharmaceuticals
Pharmacological Class:
Neuromuscular blocker.
Active Ingredient(s):
IncobotulinumtoxinA 50 Units, 100 Units; per vial; lyophilized pwd; for IM inj after reconstitution and dilution; contains human albumin; preservative-free.
Indication(s):
Cervical dystonia in adults, to reduce severity of abnormal head position and neck pain in both botulinum toxin-naïve and previously treated patients. Blepharospasm in adults previously treated with onabotulinumtoxinA.
Pharmacology:
Xeomin exerts its effect in the management of dystonias by blocking cholinergic transmission at the neuromuscular junction. This action is achieved through inhibition of acetylcholine release from peripheral cholinergic nerve endings that occurs in the following sequence: Xeomin binds to and is internalized into cholinergic nerve terminals, the light-chain part of the molecule is then translocated into the cytosol of the nerve terminal, and followed by enzymatic cleavage of SNAP25, a presynaptic target protein essential for the release of acetylcholine. Impulse transmission is re-established by the formation of new nerve endings.
Clinical Trials:
The efficacy of Xeomin in cervical dystonia was evaluated in a Phase 3, randomized, double-blind, placebo-controlled study involving 233 patients with predominantly rotational cervical dystonia, with baseline Toronto Western Spasmodic Torticollis Rating Scale (TWSTRS) total score ≥20, TWSTRS severity score ≥10, TWSTRS disability score ≥3, and TWSTRS pain score ≥1. Patients were randomized to receive a single administration (4.8mL) of the study agent (Xeomin 240 Units, Xeomin 120 Units, or placebo). The primary efficacy endpoint was the change in the TWSTRS total score from baseline to Week 4 post-injection. In the intent-to-treat (ITT) population, the difference between the Xeomin 240 Unit group and the placebo group in the change of TWSTRS total score from baseline to Week 4 was -9 points; the difference between the Xeomin 120 Unit group and the placebo group was -7.5 points. Comparison of each Xeomin group to the placebo group was statistically significant at p<0.001. Efficacy of Xeomin was similar in patients who were botulinum toxin naïve and those who had received botulinum toxin prior to this study.
Xeomin was investigated in a Phase 3, randomized, double-blind, placebo-controlled study involving 109 patients with benign essential blepharospasm, with baseline Jankovic Rating Scale (JRS) Severity subscore ≥2, and a stable satisfactory therapeutic response to previous administrations of onabotulinumtoxinA (Botox). Patients were randomized to receive a single Xeomin treatment that was similar to the most recent Botox injection prior to study, or placebo. At primary efficacy endpoint, in the ITT population, the difference between the Xeomin group and the placebo group in the change of JRS Severity subscore from baseline to Week 6 was -1 point. Comparison of the Xeomin group to the placebo group was statistically significant at p<0.001.
Legal Classification:
Rx
Adults:
Should be administered and managed by experienced physicians. ≥18yrs: Individualize; see literature. Cervical dystonia: initial total dose: 120 Units per treatment session. Blepharospasm: (previously-treated): use same dose as previous treatment of onabotulinumtoxinA; (previous-dose unknown): initially 1.25–2.5 Units/injection site. Both eyes: total initial dose: max 70 Units (35 Units/eye). For both: dose, number, and location of inj sites should be based on the number and location of muscles involved, dystonia or blepharospasm severity, and response to any previous botulinum toxin inj. May repeat treatments every 12 weeks if insufficient response.
Children:
<18yrs: not recommended.
Contraindication(s):
Infection at proposed injection site.
Warnings/Precautions:
Not interchangeable with other botulinum toxin products. Pre-existing dysphagia or breathing difficulties. Patients with smaller neck muscle mass or those who require bilateral inj into the sternocleidomastoid muscles: increased risk of dysphagia. Neuromuscular disorders (eg, myasthenia gravis, ALS, Lambert-Eaton syndrome); monitor closely. Compromised respiratory function; monitor. Narrow angle glaucoma. Contains human albumin; monitor for possible viral disease transmission. Elderly. Pregnancy (Cat.C). Nursing mothers.
Interaction(s):
May be potentiated by aminoglycosides or other agents interfering with neuromuscular transmission (eg, tubocurarine-type muscle relaxants). May potentiate anticholinergic effects with concomitant anticholinergic drugs. Concomitant other botulinum toxin products or muscle relaxants may potentiate neuromuscular weakness.
Adverse Reaction(s):
Cervical dystonia: dysphagia (may be severe), neck pain, muscle weakness, inj site reactions, musculoskeletal pain; blepharospasm: eyelid ptosis, dry eye, dry mouth, diarrhea, headache, visual impairment, dyspnea, nasopharyngitis, respiratory tract infection; corneal exposure/ulceration, ectropion (avoid injection of lower lid area); both: respiratory failure, allergic reactions (discontinue if occurs), spread of toxin effect (may be fatal), possible antibody formation.
How Supplied:
Single-use vial—1
Last Updated:
8/12/2011