制造商: 药理分类: 活性成分(补): 药理作用: 临床试验: 在bunionectomy研究中,患者18至80岁中度至重度疼痛的单侧,第一跖骨bunionectomy手术的患者给予了tapentadol 50毫克,75毫克,100毫克,或安慰剂,每4至6小时,72小时。患者的比例在48谁发现30%或更高,或50%或更高小时疼痛强度均显着减少了tapentadol在每个治疗剂量与安慰剂的病人高。 在最后阶段的退行性关节病的研究中,患者18至80岁的中度退化阶段,从结束的髋关节或膝关节疼痛是严重的疾病给予了tapentadol 50毫克,75毫克或安慰剂,每4至6小时10天。患者的比例在5谁发现30%或以上,或50%或更高天疼痛强度均显着降低了tapentadol在每个治疗剂量与安慰剂的病人高。 法律分类: 成人: 儿童: 禁忌(补):
互动(补): 不良反应(补): 如何提供: 最后更新: NUCYNTA Manufacturer:PriCara Pharmacological Class:Opioid Active Ingredient(s):Tapentadol 50mg, 75mg, 100mg; tabs. Indication(s):Moderate to severe acute pain in patients ≥18yrs of age. Pharmacology:Tapentadol is a centrally-acting synthetic analgesic. Although its mechanism of action is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake. Clinical Trials:Two randomized, double-blind, placebo- and active-controlled studies were conducted to evaluate the efficacy and safety of tapentadol in the treatment of moderate to severe acute pain from first metatarsal bunionectomy and end-stage degenerative joint disease. In the bunionectomy study, patients 18 to 80 years of age with moderate to severe pain following unilateral, first metatarsal bunionectomy surgery were given tapentadol 50mg, 75mg, 100mg, or placebo every 4 to 6 hours for 72 hours. The proportion of patients who showed reduction in pain intensity at 48 hours of 30% or greater, or 50% or greater were significantly higher in patients treated with tapentadol at each dose versus placebo. In the end-stage degenerative joint disease study, patients 18 to 80 years of age with moderate to severe pain from end stage degenerative joint disease of the hip or knee were given tapentadol 50mg, 75mg, or placebo every 4 to 6 hours for 10 days. The proportion of patients who showed reductions in pain intensity at 5 days of 30% or greater, or 50% or greater were significantly higher in patients treated with tapentadol at each dose versus placebo. Legal Classification:CII Adults:≥18yrs: 50–100mg every 4–6 hours depending upon pain intensity. First day of dosing: may give second dose one hour after first dose if adequate pain relief not attained with first dose; subsequent doses should be given every 4–6 hours. Max 700mg/day on the first day, 600mg/day on subsequent days. Moderate hepatic impairment: initially 50mg every 8 hours; max 3 doses/24 hours. Children:<18yrs: not recommended. Contraindication(s):Significant respiratory depression, acute or severe asthma or hypercapnia (in unmonitored settings or in the absence of resuscitative equipment). Paralytic ileus. During or within 14 days of MAOIs. Warnings/Precautions:Severe renal or hepatic impairment: not recommended. Asthma. COPD. Cor pulmonale. Severe obesity. Sleep apnea syndrome. Myxedema. Kyphoscoliosis. CNS depression. Coma. Head injury. Increased intracranial pressure. Seizure disorders. Biliary tract disease. Acute pancreatitis. Drug abusers. Avoid abrupt cessation. Elderly. Debilitated. Pregnancy (Cat.C). Labor & delivery, nursing mothers: not recommended. Interaction(s):See Contraindications. Additive CNS depression with other CNS depressants (eg, general anesthetics, phenothiazines, sedatives, hypnotics, alcohol); consider reducing dose. Serotonin syndrome possible with concomitant SSRIs, SNRIs, tricyclics, MAOIs, triptans, other drugs that impair metabolism of serotonin. Adverse Reaction(s):GI upset, dizziness, somnolence; respiratory, CNS depression. How Supplied:Tabs—100 美国FDA批准新药他喷他多NUCYNTA™(tapentadol)速释片上市 本品系一中枢作用的新口服镇痛药 ,通过激动μ型阿片受体和抑制去甲肾上腺素再摄取两种作用机制发挥疗效。批准的剂量规格:tapentadol 50 、75 和100 mg /片。 μ型阿片受体激动剂可结合于并可激活中枢神经系统的μ型阿片受体,改变疼痛的感觉、抑制疼痛在脊髓传递和控制脑疼痛接收区的活动。去甲肾上腺素再摄取抑制剂则是可通过抑制去甲肾上腺素被再吸收入神经细胞来增加脑内去甲肾上腺素浓度的中枢神经系统药物。这2种化合物均具有镇痛作用。 本品的药理作用与曲马多相似,但后者含左旋、右旋异构体的消旋体,激动μ型阿片类受体和抑制去甲肾上腺素再吸收作用分别获自曲马多不同构型的异构体及其代谢产物;而本品激动μ型阿片类受体和抑制去甲肾上腺素再吸收则是同一分子构型起作用不经过中间代谢途径。本品的镇痛作用强于曲马多。 本品获准上市是基于纳入2 100例患者的临床研究结果。此研究2008年初在27届美国疼痛协会科学年会上作了介绍,显示其较安慰剂可显著解除中度至严重急性疼痛。 本品最常见的不良反应是恶心、眩晕、呕吐、嗜眠和头痛。本品禁用于下列患者:呼吸明显抑制、急性或严重支气管哮喘或高碳血等禁用μ型阿片受体激动剂,麻痹性肠梗阻,目前正在使用或14日内使用过单胺氧化酶抑制剂的患者。 |