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纳曲酮是什么?
关于纳曲酮治疗肺癌的相关是近几个月在国内才开始的,基本属于民间自己创的一些基本知识,有些只能是参考国外的一些资料,肺癌十万个为什么会在后边陆续介绍一些相关文章!
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【药理毒理】
药理学
纳曲酮是阿片受体桔抗剂,药效学与纳洛酮的作用相似,能明显的减弱或完全阻断阿片受体,甚至反转由静脉注射阿片类药物所产生的作用。能解除其对阿片的身体依赖性,使已戒断阿片瘾者保持正常生活。本品口服有效,而且作用维持时间较长。本品不产生躯体或精神依赖性。
毒理学
本品对大鼠2年的致癌研究证明,在雄鼠间皮瘤和两性中血管源性肿瘤的数目稍有增加。但除雌性血管瘤稍有增加外,肿瘤的发生都在对照组的范围内。
【适应症】
盐酸纳曲酮主要用于对已解除阿片类药物毒瘾者的康复期辅助治疗,使戒除阿片瘾者能维正常生活,防止或减少复吸。
【用法用量】
纳曲酮治疗必须在纳洛酮诱发呈阴性时才能实行。所以必须按下列原则用药:
(1)本品需在阿片瘾者戒断后7~10天后使用。戒断需经检查患者尿样证实。再以纳洛酮诱发,进一步确定不存在阿片依赖性。
(2)纳洛酮诱发试验:针筒内吸入盐酸纳洛酮0.8mg先静脉注射盐酸纳洛酮0.2mg,观察30秒钟看患者是否有阿片依赖性,若呈阴性反应,继续静注0.6mg,并观察20~30分钟,无症状者可给予治疗。
(3)纳洛酮治疗可有以下几种方案:每个工作日口服50mg,周六给100mg;隔日给100mg或每3天给150mg,疗程可持续半年。
【不良反应】
(1)纳曲酮的每日用量达到300mg时可引起肝细胞损害。
(2)除肝损害外,不良反应发生率在10%以上的反应有:睡眠困难、焦虑、易激动、腹痛/痉挛、恶心和/或呕吐、关节肌肉痛、头痛。
(3)不良反应发生率在10%以下的反应有:食欲不振、腹泻、便秘、口渴、头晕。
(4)在1%以下的不良反应有:
呼吸系统:鼻充血、发痒、流鼻涕、咽痛、粘液过多、声音嘶哑、咳嗽、呼吸短促。
心血管系统:鼻出血、静脉炎、浮肿、血压升高、非特异性心电改变、心悸、心动过速。
胃肠道:产气过多、便血、腹泻、溃疡。
肌肉骨路:肩、下肢和膝关节疼痛、震颤。
皮肤:油皮肤、瘙痒、痤疮、唇疱疹。
泌尿生殖系:排尿不适增多、性欲降低。
精神方面:抑郁、忘想狂、疲倦、不安、精神错乱、幻觉、恶梦。
【禁忌】
有下列情况者禁用纳曲酮:
(1)应用阿片类镇痛药者。
(2)有阿片瘾的病人未经戒除者。
(3)突然停用阿片的病人。
(4)纳曲酮诱发失败的病人。
(5)尿检阿片类物质阳性者。
(6)对纳洛酮有过敏史者,尚不清楚本品是否与纳洛酮或其他含有菲的阿片类物质是否有交叉过敏性。
(7)急性肝炎或肝功衰竭的个体。
【注意事项】
(1)本品有肝脏毒性可引起转氨酶升高。引起肝毒性的剂量只有临床常用量的5倍,故对肝功轻度障碍者也应当慎用。
(2)为避免发生戒断症状或戒断症状恶化,在应用纳曲酮之前病人至少应当有7~10天体内确无阿片类物质。
(3)应用本品之前或应用后应定期检查肝功,最好每月查1次。
【孕妇及哺乳期妇女用药】
本品属于妊娠危险性C级的药物。实验证明,临床用量140倍的剂量(约为100mg/kg),对家兔和大鼠可能有杀灭胚胎的作用,而且在大鼠能明显增加假妊的比例,并降低雌鼠的受孕率。但在人尚无对生育影响的报告。关于本品是否能从人乳计中排出尚不得知。对产程是否有影响也是未知数。所以对孕妇和哺乳期妇女使用本品应当慎重。
【儿童用药】
对18岁以下的个体使用本品的安全性问题尚未确定。
【老年患者用药】
【药物相互作用】
本品可能干扰含有阿片类药物的治疗作用,凡使用阿片类镇痛药应避免与这类药物同时使用。
【药物过量】
目前尚无人用过量的经验。只有1次研究说明,每日用纳曲酮800mg,连用1周而未发现毒性。在小鼠、大鼠和豚鼠口服本品的LD50分别为:1.100±96mg/kg,(1.450±265)mg/kg和1.490±102mg/kg 。小鼠、大鼠和犬急性致死的原因是阵挛性强直性惊厥和呼吸衰竭。
因为缺乏治疗纳曲酮过量的经验,故应做好对症治疗。
==== 汉译英 ====
Pharmacology
Naltrexone is a opioid receptor antagonistic agents, pharmacodynamics and the role of naloxone is similar significantly reduced or completely blocked by the opioid receptor, or even reversed by the intravenous injection of opiates on the impact of. Be able to lift its opioid physical dependence, so as to enable withdrawal of opioid addicts maintain a normal life. This product is orally effective, and the role of maintaining a long time. This product does not produce physical or psychological dependence.
Toxicology
This product is on the 2-year carcinogenicity study in rats shows that in the male mesothelioma and gender in the number of vascular tumors increased slightly. However, a slight increase among females hemangioma, the tumor occurred in the control group range.
【Indications】
Naltrexone hydrochloride is mainly used for opiate addiction has been discharged from the rehabilitation period of adjuvant therapy, so that opiate addicts can kick-dimensional normal life, to prevent or reduce relapse.
【Usage consumption】
Naltrexone treatment must be found to be negative when induced by naloxone could be implemented. Medication according to the following principles must be:
(1) This product need to withdrawal of opioid addicts after 7 to 10 days to use. Withdrawal subject to examination in patients with urine proven. Longer naloxone-induced, and further establish the absence of opioid dependence.
(2) Naloxone-induced test: needle breathe the first intravenous injection of 0.8mg of naloxone hydrochloride, naloxone hydrochloride, 0.2mg, observe 30 seconds to see whether there are opioid-dependent patients, if the negative reaction to intravenous injection of 0.6 mg, and to observe the 20 to 30 minutes, those who are asymptomatic may be given treatment.
(3) Naloxone treatment can have the following programs: Each day oral administration of 50mg, Saturday to 100mg; every other day or every 3 days to 100mg to 150mg, sustainable treatment for six months.
Adverse reactions 【】
(1) The use of naltrexone to 300mg daily may cause liver cell damage.
(2) In addition to liver damage, the adverse reaction rate of over 10% of the responses include: sleep difficulties, anxiety, irritability, abdominal pain / cramps, nausea and / or vomiting, joint muscle pain, headache.
(3) The incidence of adverse reactions in 10% of the responses are: loss of appetite, diarrhea, constipation, thirst, dizziness.
(4) less than 1% of the adverse reactions are:
Respiratory: nasal congestion, itching, runny nose, sore throat, excessive mucus, hoarseness, coughing, shortness of breath.
Cardiovascular system: nose bleeding, phlebitis, edema, high blood pressure, non-specific ECG changes, palpitations, tachycardia.
Gastrointestinal: excessive gas production, blood in the stool, diarrhea, ulcers.
Musculoskeletal Road: shoulder, leg and knee pain, and tremor.
Skin: oil skin, itching, acne, cold sores.
Genito-urinary system: micturition does not increase sexual desire decrease.
Mental aspects: depression, forgotten like mad, fatigue, anxiety, mental confusion, hallucinations, nightmares.
【Taboo】
Any of the following are disabled naltrexone:
(1) The application of opioid analgesics are.
(2) patients with opioid addiction without the abstainers.
(3) suddenly out opioid patients.
(4), naltrexone-induced failure patients.
(5), opioid-positive urine test.
(6) naloxone has a history of allergies is not clear whether the product contains the Philippines with naloxone or other opioid substances whether there is cross-allergy.
(7) acute hepatitis or liver failure, individual.
【Note】
(1) This product has liver toxicity can cause elevated transaminase. Liver toxicity caused by the clinical dose of only 5 times the amount used, so mild impairment of liver function should also be used with caution.
(2) To avoid withdrawal symptoms or withdrawal symptoms worse, in the application of naltrexone prior to the patient should be at least 7 to 10 days the body is indeed non-opioid.
(3) should be applied before or after the FDA should regularly check the liver function, the best check one time per month.
【Pregnant and lactating women drug】
This product is part of the risk of pregnancy C class drug. Experiments show that the clinical dosage of 140 times the dose (approximately 100mg/kg), pairs of rabbits and rats may have a role to kill embryos, but also significantly increased in rats the proportion of false pregnancy and reduce the pregnancy rate of females . However, in the human there is no report on the impact on fertility. About This product is excreted from the human milk meter is not yet known. Whether the impact on the production process is also unknown. Therefore, pregnant women and lactating women to make the FDA should be cautious.
Pediatric Use
Individuals under the age of 18 so that the safety of the FDA issues yet to be determined.
【】 Medication in elderly patients
【Drug interactions】
It can be used to interfere with containing the therapeutic effect of opioids, where the use of opioid analgesics should be avoided with the use of these drugs at the same time.
Overdosage
There is no people use too much experience. Only 1 study shows that a daily naltrexone 800mg, used in conjunction 1 week but have not found toxicity. In mice, rats and guinea-pig oral LD50 of the goods, respectively: 1.100 ± 96mg/kg, (1.450 ± 265) mg / kg and 1.490 ± 102mg/kg. Mice, rats and dogs died because of acute tonic-clonic convulsions and respiratory failure.
Naltrexone treatment because of the lack of experience excessive, it should be prepared to symptomatic treatment.
Tags: 纳曲酮是什么?
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更新日期: 2009-11-11 03:38
作者: : mcyclub
修订: 1.0
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