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NUCYNTA CR(TAPENTADOL HYDROCHLORIDE tabs)

2014-09-13 17:29:29 作者：新特药房来源：互联网浏览次数：110 文字大小：【大】【中】【小】

简介： 美国FDA批准新口服镇痛药他喷他多（tapentadol）速释片上市美国FDA批准强生药物研究与开发公司（J&JPRD）tapentadol速释片上市，用于解除成人中度至严重急性疼痛。本品系一中枢作用的新口服镇痛药，通过 ...

关键字：他喷他多速释片 TAPENTADOL HYDROCHLORIDE药品商标名NUCYNTA CR 镇痛药

美国FDA批准新口服镇痛药他喷他多（tapentadol）速释片上市
美国FDA批准强生药物研究与开发公司（J&JPRD）tapentadol速释片上市，用于解除成人中度至严重急性疼痛。
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100mg /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2100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。
Nucynta (他喷他多,tapentadol)速释片
批准日期：2008年11月20日；公司：Ortho-McNeil-Janssen Pharmaceuticals, Inc.
适应证：
NUCYNTA是一种阿片类镇痛药适用于在18岁或以上患者解除中度至严重急性疼痛。
剂量和用法：
如许多中枢作用镇痛药一样，NUCYNTA的给药方案应按照正在被治疗疼痛的严重程度个体化，用相似药物既往经验和监查患者的能力。
起始量NUCYNTA有或无食物剂量50mg、75mg、或100mg每4至6小时依赖于疼痛强度。在给药第1天，如首次给药未达到适当解除疼痛那末在首次给药后立即可给予第2剂量。随后给药是每4至6小时50mg，75mg，或100mg和应调整维持可接受耐受性适当镇痛。尚未研究在治疗第1天每天剂量大于700 mg和尚未研究随后天600mg和所以不推荐使用。
剂型和规格：
片：50mg、75mg、100mg。
禁忌证：
受损肺功能(显著呼吸压抑，急性或严重支气管哮喘或在非监查情况下的血碳酸过多症或缺乏复苏设备)。
麻痹性肠梗阻
与单胺氧化酶抑制剂(MAOI)同时使用或在14天内使用。
警告和注意事项：
呼吸压抑：在老年人、虚弱患者、患有缺氧、高碳酸血症、或上呼吸道阻塞伴随情况增加风险。
CNS效应：当与酒精、其它阿片类或非法药物联合使用增加CNS压抑作用。
颅内压升高：可能明显地加重存在的头损伤，其它颅内病变。
可能发生滥用。严密监查患者滥用和成瘾的征象。
受损的精神/身体能力：潜在危害性活动时必须慎用。
癫痫发作：有癫痫发作史患者慎用。
羟色胺综合征：同时给予血清素可能造成潜在危及生命情况。
不良反应：
最常见不良事件是恶心、眩晕、呕吐和嗜睡。
药物相互作用：
患者当前使用指定中枢作用药物或酒精时慎用NUCYNTA。
当前使用或14天内使用单胺氧化酶抑制剂(MAOI)患者不要使用NUCYNTA。
特殊人群中的使用：
分泌和生产：分娩和生产期间和前立即不要使用。母亲曾服用NUCYNTA监查新生儿呼吸压抑。
哺乳母亲：不要哺乳。
儿童使用：尚未确定在18岁以下患者的安全性和有效性。
肾或肝功能受损：在严重肾或肝功能受损患者中建议不使用。中度肝功能受损患者中慎用。
老年人：当选择初始剂量应谨慎。
友情提示：Nucynta为药师麻醉药品，2级管制。
Nucynta CR
Nucynta CR- Tablets- Extended Release
NUCYNTA® (tapentadol) is indicated for the management of moderate to severe acute pain in adults.
NUCYNTA® IMPORTANT SAFETY INFORMATION
Contraindications: Significant respiratory depression; acute or severe bronchial asthma or hypercarbia in an unmonitored setting or in the absence of resuscitative equipment; known or suspected paralytic ileus; hypersensitivity to tapentadol or to any other ingredients of the product; concurrent use of monoamine oxidase inhibitors (MAOIs) or use within the last 14 days.
Abuse Potential: NUCYNTA® contains tapentadol, an opioid agonist and a Schedule II controlled substance that can be abused in a manner similar to other opioid agonists, legal or illicit. Misuse or abuse of NUCYNTA® by crushing, chewing, snorting, or injecting will pose a significant risk that could result in overdose and death. Assess risk for opioid abuse or addiction prior to prescribing NUCYNTA®. Routinely monitor for signs of misuse, abuse, and addiction because these drugs carry a risk for addiction even under appropriate medical use.
Life-threatening Respiratory Depression: Respiratory depression is the chief hazard of opioid agonists, including NUCYNTA® which, if not immediately recognized and treated, may lead to respiratory arrest and death. Management of respiratory depression may include close observation, supportive measures, and use of opioid antagonists, depending on the patient’s clinical status.
Accidental Exposure: Instruct patients against use by individuals other than the patient for whom NUCYNTA® was prescribed and to keep NUCYNTA® out of the reach of children, as such inappropriate use may result in fatal respiratory depression.
Elderly, Cachectic, or Debilitated Patients: Respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients as they may have altered pharmacokinetics or altered clearance compared to younger, healthier patients. Closely monitor these patients, particularly when NUCYNTA® is given concomitantly with other drugs that depress respiration.
Use in Patients With Chronic Pulmonary Disease: Patients with significant chronic obstructive pulmonary disease or cor pulmonale and patients having a substantially decreased respiratory reserve, hypoxia, hypercarbia, or pre-existing respiratory depression, should be monitored for respiratory depression. Consider the use of alternative nonopioid analgesics in these patients.
Interactions With CNS Depressants and Illicit Drugs: Concomitant use with other CNS depressants may result in hypotension and profound sedation, coma, or respiratory depression. If NUCYNTA® therapy is to be initiated in a patient taking a CNS depressant, start NUCYNTA® at 1/3 to 1/2 of the usual dosage and monitor patients for signs of sedation and respiratory depression; consider using a lower dose of the concomitant CNS depressant.
Hypotensive Effect: May cause severe hypotension; there is an increased risk in patients whose ability to maintain blood pressure has already been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (e.g., phenothiazines or general anesthetics). Monitor for signs of hypotension. Avoid the use in patients with circulatory shock; may cause vasodilation that can further reduce cardiac output and blood pressure.
Use in Patients With Head Injury or Increased Intracranial Pressure: Monitor patients who may be susceptible to the intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors) for signs of sedation and respiratory depression. NUCYNTA® may reduce respiratory drive, and the resultant CO2 retention can further increase intracranial pressure. Opioids may also obscure the clinical course in a patient with a head injury.
Seizures: NUCYNTA® may aggravate convulsions in patients with convulsive disorders, and may induce or aggravate seizures. Monitor patients with a history of seizure disorders for worsened seizure control during NUCYNTA® therapy.
Serotonin Syndrome Risk: Cases of life-threatening serotonin syndrome have been reported with the concurrent use of NUCYNTA® and serotonergic drugs. Serotonergic drugs comprise selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptans, drugs that affect the serotonergic neurotransmitter system, and drugs that impair metabolism of serotonin (including MAOIs). This may occur within the recommended dose. Serotonin syndrome may include mental-status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination), and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea) and can be fatal. If concomitant treatment with SSRIs, SNRIs, TCAs, or triptans is clinically warranted, careful observation of the patient is advised.
Use in Patients With Gastrointestinal (GI) Conditions: Contraindicated in patients with GI obstruction, including paralytic ileus; may cause spasm of the sphincter of Oddi. Monitor patients with biliary tract disease, including acute pancreatitis, for worsening symptoms.
Withdrawal: Withdrawal symptoms (e.g., anxiety, sweating, insomnia, rigors, pain, nausea, tremors, diarrhea, upper respiratory symptoms, piloerection, and rarely, hallucinations) may occur:
After abrupt discontinuation or a significant dose reduction of NUCYNTA® in physically dependent patients. When discontinuing NUCYNTA®, gradually taper the dose. If mixed agonists/antagonists (e.g., butorphanol, nalbuphine, pentazocine) and partial agonists (e.g., buprenorphine) are used in patients who have received or are receiving NUCYNTA®. Avoid the use of mixed agonists/antagonists and partial agonists with NUCYNTA®. If opioid antagonists (e.g., naloxone, nalmefene) are administered in physically dependent patients. Administration of the antagonist should be begun with care and by titration with smaller than usual doses of the antagonist.
Driving and Operating Heavy Machinery: May impair the mental or physical abilities needed to perform potentially hazardous activities such as driving a car or operating machinery. Warn patients not to drive or operate dangerous machinery unless they are tolerant to the effects of NUCYNTA® and know how they will react to the medication.
Renal and Hepatic Impairment:
Renal: Use of NUCYNTA® in patients with severe renal impairment (CLCR <30 mL/min) is not recommended due to accumulation of a metabolite formed by glucuronidation of tapentadol. The clinical relevance of the elevated metabolite is not known.Hepatic: Avoid use of NUCYNTA® in patients with severe hepatic impairment (Child-Pugh Score 10-15); reduce the dose in patients with moderate impairment (Child-Pugh Score 7-9).
Because elderly patients are more likely to have decreased renal and hepatic function, consideration should be given to starting elderly patients in the lower range of recommended doses.
Anticholinergics: Use with anticholinergic products may increase the risk of urinary retention and/or severe constipation, which may lead to paralytic ileus.
Pregnancy/Neonates/Nursing Mothers: Pregnancy Category C. NUCYNTA® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Neonates born to mothers physically dependent on opioids will also be physically dependent and may exhibit respiratory difficulties and withdrawal symptoms. Neonatal opioid withdrawal syndrome may be life-threatening and should be treated according to protocols developed by neonatology experts. Closely monitor infants of nursing mothers receiving NUCYNTA® because of the potential for adverse reactions (e.g., withdrawal symptoms).
Overdosage: Institute supportive measures to manage respiratory depression, circulatory shock, and pulmonary edema as required. The opioid antagonists, naloxone or nalmefene, are specific antidotes to respiratory depression.
Adverse Reactions in Clinical Trials: The most common (≥10%) adverse reactions were nausea, dizziness, vomiting, and somnolence.
Select Postmarketing Adverse Reactions: Anaphylaxis, angioedema, and anaphylatic shock have been reported very rarely with ingredients contained in NUCYNTA®. Advise patients how to recognize such reactions and when to seek medical attention. Panic attack has also been very rarely reported.
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产地国家: 加拿大
原产地英文商品名:
NUCYNTA CR 50mg 60 tabs
原产地英文药品名:
TAPENTADOL HYDROCHLORIDE
原产地英文化合物名称:
3-[(1R,2R)-3- (dimethylamino)-1-ethyl-2methylpropyl]phenol monohydrochloride
中文参考商品译名:
NUCYNTA CR 50毫克／片 60片／瓶
中文参考药品译名:
盐酸他喷他多
生产厂家中文参考译名:
JANSSEN
生产厂家英文名:
JANSSEN
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产地国家: 加拿大
原产地英文商品名:
NUCYNTA CR 100mg 60tabs
原产地英文药品名:
TAPENTADOL HYDROCHLORIDE
原产地英文化合物名称:
3-[(1R,2R)-3- (dimethylamino)-1-ethyl-2methylpropyl]phenol monohydrochloride
中文参考商品译名:
NUCYNTA CR 100毫克／片 60片／瓶
中文参考药品译名:
盐酸他喷他多
生产厂家中文参考译名:
JANSSEN
生产厂家英文名:
JANSSEN
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产地国家: 加拿大
原产地英文商品名:
NUCYNTA IR 75mg 100tabs
原产地英文药品名:
TAPENTADOL HYDROCHLORIDE
原产地英文化合物名称:
3-[(1R,2R)-3- (dimethylamino)-1-ethyl-2methylpropyl]phenol monohydrochloride
中文参考商品译名:
NUCYNTA IR 75毫克／片 100片／瓶
中文参考药品译名:
盐酸他喷他多
生产厂家中文参考译名:
JANSSEN
生产厂家英文名:
JANSSEN