Manufacturer:

Janssen Pharmaceuticals, Inc.

Pharmacological Class:

Opioid.

Active Ingredient(s):

Tapentadol 50mg, 100mg, 150mg, 200mg, 250mg; ext-rel tabs.

Indication(s):

Moderate-to-severe chronic pain when a continuous, around-the-clock opioid analgesic is needed for an extended period of time. Not for as-needed use.

Pharmacology:

Tapentadol is a centrally-acting synthetic analgesic. The exact mechanism of action is unknown. Although the clinical relevance is unclear, preclinical studies have shown that tapentadol is a mu-opioid receptor agonist and a norepinephrine reuptake inhibitor, and analgesia in animal models is derived from both of these properties.

Clinical Trials:

The efficacy of Nucynta ER was studied in four studies in patients with moderate-to-severe chronic pain. Efficacy was demonstrated in one randomized,double-blind, placebo- and active-controlled study in patients with chronic low back pain (LBP), and one randomized, double-blind, placebo-controlled study in patients with pain related to diabetic peripheral neuropathy (DPN).

In the LBP study, patients 18 years of age or older with chronic low back pain and a baseline pain score of ≥5 on an 11-point numerical rating scale, ranging from 0 to 10 were enrolled and randomized to 1 of 3 treatments: Nucynta ER, active-control (an extended-release CII opioid), or placebo. Patients randomized to Nucynta ER initiated therapy with a dose of 50mg twice daily for three days. After three days, the dose was increased to 100mg twice daily. Subsequent titration was allowed over a 3-week titration period to a dose up to 250mg twice daily, followed by a 12-week maintenance period. There were 981 patients randomized. The mean age of the study population was 50 (range 18 to 89) years; the mean baseline pain intensity score was 8 (SD 1). Approximately half of the patients were opioid-naïve. The number of patients completing the study was 51% in the placebo group, 54% in the Nucynta ER group and 43% in the active-control group. After 15 weeks of treatment, patients taking Nucynta ER had a significantly greater pain reduction compared to placebo.

In the DPN study, patients 18 years or older with pain due to diabetic peripheral neuropathy and a pain score of ≥5 on an 11-point numerical rating scale (NRS) ranging from 0 to 10 were enrolled. Following an open-label treatment period in which Nucynta ER was administered to all patients for three weeks, patients who had demonstrated at least a 1-point improvement in pain intensity on the NRS at the end of the open-label titration period were randomized to either the Nucynta ER dose (100mg to 250mg) reached during the open-label titration period, or placebo for 12 weeks of maintenance treatment. A total of 591 patients entered open-label treatment and 389 patients met the criteria for randomization into the double-blind treatment period. The mean age of the randomized population was 60 (range 29 to 87) years; approximately 2/3 of the patients were opioid-naïve. After 12 weeks of treatment, Nucynta ER provided a significantly greater reduction in pain intensity compared to placebo.

Legal Classification:

CII

Adults:

Individualize. Swallow whole; do not break, chew, dissolve or crush tabs. ≥18yrs: Usual dose: 100–250mg twice daily (approx. every 12 hours). Opioid-naïve: initially 50mg twice daily (approx. every 12 hours); then titrate to optimal dose within therapeutic range of 100–250mg twice daily. Converting from Nucynta to Nucynta ER: divide total daily dose of Nucynta into two equal doses of Nucynta ER separated by 12 hour intervals. Nucynta ER doses >500mg: not recommended. Converting from oxycodone CR and other opioids to Nucynta ER: see literature. Moderate hepatic impairment: initially 50mg once every 24 hours; max 100mg once daily.

Children:

<18yrs: not recommended.

Contraindication(s):

Significant respiratory depression, 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:

Not for management of acute or post-op pain. Severe renal or hepatic impairment: not recommended. Moderate hepatic impairment. Asthma. COPD. Cor pulmonale. Severe obesity. Sleep apnea syndrome. Myxedema. Kyphoscoliosis. CNS depression. Coma. Head injury. Increased intracranial pressure. Seizure disorders. Adrenocortical insufficiency (eg, Addison's disease). Delirium tremens. Toxic psychosis. Hypothyroidism. Hypovolemia. GI or GU obstruction. Biliary tract disease. Acute pancreatitis. Drug abusers. Avoid abrupt cessation. Elderly. Debilitated. Pregnancy (Cat.C). Monitor neonates, whose mothers have been taking Nucynta ER, for respiratory depression. Labor & delivery, nursing mothers: not recommended.

Interaction(s):

See Contraindications. Avoid concomitant alcohol or alcohol-containing medications; may cause fatal overdose. Additive CNS depression, hypotension with other CNS depressants (eg, general anesthetics, phenothiazines, other tranquilizers, sedatives, hypnotics, alcohol); consider reducing dose. Serotonin syndrome possible with concomitant SSRIs, SNRIs, tricyclics, MAOIs, triptans, other drugs that impair metabolism of serotonin. Concomitant mixed agonists/antagonists, (butorphanol, nalbuphine, pentazocine), partial agonists (eg, buprenorphine), and anticholinergics: not recommended.

Adverse Reaction(s):

Nausea, constipation, headache, dizziness, somnolence; respiratory, CNS depression, hypotension.

How Supplied:

ER tabs—60

Last Updated:

10/28/2011

Nucynta ER（他喷他多缓释片）

制造商：
扬森制药公司

类药物：
阿片类药物。

活性成分（S）：
Tapentadol 50毫克，100毫克，150毫克，200毫克，250毫克; EXT - REL选项卡。

指示（S）：
中度至重度慢性疼痛时，连续的，昼夜阿片类镇痛药是需要长时间。不适合需要使用。

药理：
Tapentadol是中央行事合成镇痛。行动的确切机制不明。虽然临床相关性还不清楚，临床前研究表明，tapentadol是μ-阿片受体激动剂和去甲肾上腺素再摄取抑制剂，并在动物模型中的镇痛是派生的这两个属性。

临床试验：
四项研究在中度至重度慢性疼痛患者的疗效研究的Nucynta ER。在一项随机，双盲，安慰剂和积极控制慢性腰痛（LBP）的，和一个随机，双盲，安慰剂控制的研究与糖尿病周围神经病变患者疼痛患者的研究表明疗效（DPN）。

在枸杞多糖的研究，年满18岁或慢性腰痛和一个11点的数值评定量表，一个在5≥基线疼痛评分范围从0到10岁患者进行了登记和随机分配到治疗1 3：Nucynta ER，主动控制（CII的阿片类缓释），或安慰剂。 Nucynta急诊病人随机发起治疗剂量为50mg，每日两次，三天。三天后，剂量增加至100毫克，每天两次。随后的滴定不允许超过3周的滴定期间，以一个高达250毫克剂量，每日两次，由12周的维持期。有981例患者随机。研究人口的平均年龄为50（范围为18至89年）;基线平均疼痛强度评分为8（SD）。大约一半的患者阿片类药物初治。完成研究的患者人数分别为51％，在安慰剂组，在Nucynta ER组的54％和43％的主动对照组。 15周的治疗后，患者服用Nucynta ER了安慰剂相比，显着更大的痛苦减少。

在DPN的研究中，18岁或因糖尿病周围神经病变和一个11点的范围从0到10的数值评定量表（NRS）的疼痛评分≥5疼痛的患者进行了登记。开放标签Nucynta ER管理的三个星期，让所有有需要的病人治疗期间，曾表明至少在NRS的疼痛强度提高1点，在开放标签滴定期结束的患者被随机的Nucynta ER剂量（100毫克至250毫克），达到在开放标签滴定期间，或安慰剂12周的维持治疗。共有591例患者进入开放标签治疗，389例患者符合的随机双盲治疗期为标准。随机人口的平均年龄为60（范围从29至87年），约2 / 3的患者阿片类药物初治。 Nucynta急诊室治疗12周后，提供了一个与安慰剂相比，减少疼痛强度显着提高。

法律分类：
CII

成人：
个性化。整个燕子不破，咀嚼，溶解或粉碎标签。 ≥18yrs：常用剂量：100 - 250毫克，每天两次（约每12小时）。阿片类药物初治：最初50毫克，每天两次（约每12小时），然后滴定100 - 250毫克的治疗范围内的最佳剂量，每日两次。转换Nucynta Nucynta ER：分成两个相等的Nucynta ER相隔12个小时的间隔剂量Nucynta每日总剂量。 Nucynta ER剂量> 500毫克：不推荐使用。羟考酮的CR和Nucynta急诊室的其他阿片类药物转换：见文献。中度肝功能障碍：最初50毫克每24小时一次;最大100毫克，每日一次。

儿童：
<18yrs：不推荐。

禁忌（S）：
显着的呼吸抑制，严重哮喘或高碳酸血症（在不受监督的设置，或在复苏设备的情况下）。麻痹性肠梗阻。在14天的单胺氧化抑制剂期间内。

警告/注意事项：
不适用于急性或术后疼痛管理。严重肾功能或肝功能不全：不推荐。中度肝功能损害。哮喘。慢性阻塞性肺病。肺心病。重度肥胖。睡眠呼吸暂停综合征。粘液性水肿。脊柱后侧凸。中枢神经系统抑制。昏迷。头部受伤。颅内压增高。癫痫。肾上腺皮质功能不全（如阿狄森氏病）。震颤性谵妄。中毒性精神病。甲状腺功能减退。血容量。 GI或GU阻塞。胆道疾病。急性胰腺炎。吸毒者。避免突然停止。老人。虚弱。怀孕（Cat.C）。监视器的新生儿，其母亲已采取Nucynta急诊室，呼吸抑制。劳动和交付，哺乳期的母亲：不推荐。

相互作用（S）：
见禁忌。避免随之而来的酒精或含有酒精的药物，可能造成致命的过量。添加剂中枢神经系统抑制，低血压与其他中枢神经抑制剂（例如，全身麻醉药，吩噻嗪类，其他镇静剂，镇静剂，安眠药，酒精）;考虑减少剂量。伴随SSRIs的5 - 羟色胺综合征的可能，SNRIs，三环，单胺氧化抑制剂，曲坦类药物，其他药物损害羟色胺的代谢。伴随混合激动剂/拮抗剂，（喷他佐辛，纳布啡，布托啡诺），部分激动剂（如丁丙诺啡），以及抗胆碱药：不推荐。

不良反应（S）：
恶心，便秘，头痛，头晕，嗜睡，呼吸，中枢神经系统抑制，低血压。

如何提供：
急诊室制表符- 60

最后更新：
2011年10月28日