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当前位置:药品说明书与价格首页 >> 骨科(骨, 肌肉药物) >> 类风湿关节炎 >> 吲哚美辛钠注射剂INDOCIN I.V.(INDOMETHACIN SODIUM TRIHYDRATE)

吲哚美辛钠注射剂INDOCIN I.V.(INDOMETHACIN SODIUM TRIHYDRATE)

2013-03-08 23:50:28  作者:新特药房  来源:互联网  浏览次数:108  文字大小:【】【】【
简介: 部分中文吲哚美辛处方资料(仅供参考)英文药名: Indocin (Indomethacin)中文药名: 消炎痛(吲哚美辛)药品名称吲哚美辛(Indometacin,Indomethacin)是一种非甾体抗炎药(NSAID),可消炎止痛、治疗发 ...

部分中文吲哚美辛处方资料(仅供参考)
英文药名: Indocin (Indomethacin)
中文药名: 消炎痛(吲哚美辛)
药品名称
吲哚美辛(Indometacin,Indomethacin)是一种非甾体抗炎药(NSAID),可消炎止痛、治疗发烧和缓解身体僵硬,作用机理是减少前列腺素的合成,减轻炎性反应。
英文商品名包括Indocin、Indocid、Indochron E-R 和 Indocin-SR.
中文商品名为消炎痛。
化学性质
吲哚美辛是一种甲基化的吲哚衍生物,与双氯芬酸(Diclofenac)同属NSAID中芳香基脂肪酸类。
作用机理
吲哚美辛是环氧酶(COX,可转化花生四烯酸为前列腺素)1和2的非选择性抑制剂。前列腺素是人体中常见的一类激素物质,有多种生理作用,其中部分可导致疼痛、发烧和炎症。
前列腺素可使妊娠中的妇女子宫收缩,因而吲哚美辛是一种有效的抑制分娩药,通过抑制子宫内前列腺素(PG)的合成,也可能是通过阻滞钙通道来减少子宫收缩,从而预防早产。
吲哚美辛还有另外2种具临床重要性的作用机理:
可抑制多形核白细胞(PMN)的的运动,类似秋水仙素的作用。
可在软骨和肝脏细胞中的线粒体中解偶联氧化磷酸化作用,类似水杨酸衍生物的作用。
这两种作用机理解释了吲哚美辛止痛和消炎的特性。
吲哚美辛可以穿过胎盘减少胎儿尿液,从而治疗羊水过多症。作用方式是减少肾血流(RBF)并增加肾脏血流阻力,可能是通过增强胎儿肾脏抗利尿激素的作用来实现的。
适应症
吲哚美辛的临床适应症包括:
动脉导管未闭(PDA)
强直性脊柱炎
类风湿性关节炎
痛风
骨关节炎
幼年特发性关节炎
银屑病关节炎
赖特综合征(Reiter's syndrome)
骨派杰氏病(Paget's disease of bone)
巴特综合征(Bartter syndrome)
用力性头痛
假痛风
痛经
心包炎
滑囊炎
腱鞘炎
肾性尿崩症(前列腺素抑制精氨酸加压素(AVP),导致肾脏集合管对抗利尿激素不起反应)
恶性疾病相关的发烧和疼痛(肿瘤、骨转移性癌、淋巴肉芽肿病)
慢性阵发性半侧颅痛、连续性半侧颅痛、偏头痛
肾绞痛(由肾结石引发)
冷球蛋白血症
临床上,吲哚美辛也用于预防早产、減少羊水以缓解羊水过多症和治愈动脉导管未闭。
吲哚美辛药性强烈,并伴有多种严重副作用,因此不应用于缓解轻微的疼痛和发烧。本药品的药性强于阿司匹林,但止痛效果并不会更好。轻度到中度疼痛所需的标准口服剂量,药效相当于600毫克阿司匹林。
不良反应
由于吲哚美辛抑制COX-1和COX-2,胃和肠脏中用于维持消化系统粘膜的前列腺素也受抑制。因此,吲哚美辛如其他非选择性COX抑制剂一样会导致消化性溃疡,严重时会导致出血及穿孔,部分病人甚至会死于并发症。
为减少罹患消化性溃疡的几率,应遵医嘱在达到治疗效果的最低剂量下使用,通常是50-200毫克/日,且应于饭后服用。同时服用抗消化性溃疡药,如大剂量抗酸剂雷尼替丁(就寝前150毫克)或奥美拉唑(就寝前20毫克)也可防治此病。其他普遍的胃肠并发症,包括消化不良、胃灼热和轻度腹泻并不算太严重,极少情况下才需要停用吲哚美辛。约10%服药者服用双氯芬酸也可能出现极为类似的症状。
很多NSAID都会抑制Li+从肾脏排出,而吲哚美辛的这种作用尤其明显,这就会提高本药品使用者锂中毒的风险。对于服用锂制剂(如治疗忧郁症或躁狂症的药物)的病人,最好服用低毒性的NSAID,如舒林酸(Sulindac)或阿司匹林。
吲哚美辛也会降低血浆肾素活性(PRA)及醛甾酮(Aldosterone)水平,同时会抑制Na+和K+离子排出,也会增强抗利尿激素的作用,这几种作用会共同导致以下后果:
水肿(体液过多引起)
高钾血症
高钠血症
高血压
药品也会引起血清肌氨酸酐上升和更严重的肾脏损害,如急性肾衰竭、慢性肾炎和肾病症候群,而这些病症的早期症状是水肿和高钾血症。
此外,吲哚美辛常会造成头痛(总用药人数的10-20%),有时伴有眩晕、眼花、听力损失、耳鸣、颈性视力障碍(视网膜感光与否均有可能),以及加重帕金森氏症、癫痫和精神病性障碍的病情。危及生命的休克(症状包括血管性水肿、出汗、重度低血压、心动过速和急性支气管痉挛)、重型肝炎和重度骨髓损伤也曾出现在医疗报告中。皮肤的光过敏反应也是可能存在的副作用。
吲哚美辛解热作用强,可能会使严重感染的临床病程变得不明确。
由于吲哚美辛有多种严重的副作用,并且现在有耐药性更好的药品可以使用,现在吲哚美辛一般不是治疗的首选药品。目前,吲哚美辛是治疗急性痛风和痛经的公认药物,因为治疗所需延续时间仅为几天,这样就不易产生严重的副作用。
药物过量
吲哚美辛对动物和人类都是急性高毒性的,大家鼠致死量为12毫克/千克,小鼠致死量为50毫克/千克,而准确的人类数据还不存在,不过目前已见到有关儿童和青少年的致命病例。
一般来说,过量服用吲哚美辛会引起瞌睡、眼花、重度头痛、精神错乱、感觉异常(Paresthesia)、肢体麻痹、反胃和呕吐,而严重的胃肠出血也有可能发生。脑水肿、心脏骤停(CA)这些致命后果也曾出现在儿童身上。而过量使用局部治疗剂型(如喷雾剂、凝胶)所带来的风险不算太大。
禁忌
下列情况禁忌使用吲哚美辛:
消化性溃疡及病史患者
对吲哚美辛、阿司匹林及其他NSAID过敏者
服用其他NSAID产生血管性水肿鼻息肉的患者
2岁以下儿童(患有动脉导管未闭的新生儿除外)
肝肾功能严重受损者
下列情况慎用吲哚美辛:
骨髓损伤者(血细胞数减少)
不明原因的出血倾向(抑制血小板聚集)
帕金森氏症、癫痫和精神病性障碍(有可能加重病情)
注意事项
病人应进行常规体检以检测水肿和中枢神经系统的副作用症状,而测量血压可以检测出病人血压是否过高。定期的血清电解质(Na+、K+、Cl−)测量、全血细胞计数(CBC)、肝功能评价以及肌氨酸酐测试(肾功能相关)也都是要进行的检查。如果吲哚美辛与血管紧张素转化酶抑制剂(ACEI)或保钾利尿剂(Potassium-sparing diuretics)类药物一同使用,这些检查就更是必不可少的了,这是由于合用这些药物能造成高钾血症甚至严重肾衰竭。不过,如果使用局部应用剂型,如喷雾剂或凝胶等,就无需这些检查了。


GENERIC NAME: indomethacin
BRAND NAME: Indocin, Indocin-SR
DRUG CLASS AND MECHANISM: Indomethacin is a nonsteroidal anti-inflammatory drug (NSAID) that reduces fever, pain and inflammation. It is similar to ibuprofen (Motrin) and naproxen(Naprosyn, Aleve). Indomethacin works by reducing the production of prostaglandins.
Prostaglandins are chemicals that the body produces to cause fever and pain that are
associated with inflammation. Indomethacin blocks the enzymes that make prostaglandins (cyclooxygenase 1 and 2) and thereby reduces the levels of prostaglandins. As a result, fever, pain and inflammation are reduced. Indomethacin is available in a sustained (slow) release form (Indocin-SR). The FDA first approved indomethacin in January 1965.
PRESCRIPTION: Yes
GENERIC AVAILABLE: Yes
PREPARATIONS:
Capsules: 25 and 50 mg;
Capsules, sustained release: 75 mg;
Suspension: 25 mg/ml;
Suppositories: 50 mg.
STORAGE: Capsules should be kept at room temperature 15-30 C (59-86 F). Oral suspension and suppositories should be kept below 30 C (86 F). The oral suspension should not be frozen.
PRESCRIBED FOR: Indomethacin is used for the treatment of inflammation caused by rheumatoid arthritis, ankylosing spondylitis, gouty arthritis, osteoarthritis, and soft tissue injuries such as tendinitis and bursitis.
DOSING: The recommended dose for adults is 50-200 mg per day split into 2-3 doses. Indomethacin should be taken with food in order to reduce abdominal discomfort.
DRUG INTERACTIONS: Cholestyramine (Questran) and colestipol(Colestid) may decrease the absorption of indomethacin by binding to indomethacin in the intestine and preventing
absorption into the body.
Indomethacin and other NSAIDs may decrease the elimination of lithium (Eskalith, Lithobid) by the kidneys and, therefore, increase the blood level of lithium, which could lead to lithium toxicity.
Indomethacin may reduce the blood pressure-lowering effects of drugs that are given to reduce blood pressure.
This may occur because prostaglandins play a role in the regulation of blood pressure. When indomethacin is used in combination with aminoglycoside antibiotics (for example, gentamicin) the blood levels of the aminoglycoside may increase, presumably because
the elimination of aminoglycoside from the body is reduced.
This may lead to aminoglycoside-related side effects.
Individuals taking oral blood thinners or anticoagulants [for example, warfarin (Coumadin)] should avoid indomethacin because indomethacin also thins the blood, and excessive blood thinning may lead to bleeding.
PREGNANCY: Use during pregnancy has not been adequately studied. Indomethacin may have adverse effects on the fetus.
NURSING MOTHERS: Indomethacin is excreted in breast milk and therefore should be avoided by nursing mothers.
SIDE EFFECTS: The most common side effects are nausea, vomiting, diarrhea, stomach discomfort, heartburn, rash, headache, dizziness and drowsiness.
Indomethacin may cause or worsen stomach or intestinal bleeding or ulcers. It may lead to perforation of the intestine.
NSAIDs reduce the ability of blood to clot and therefore increase bleeding after an injury.
Indomethacin may cause ulceration of the stomach or intestine, and the ulcers may bleed. Sometimes, ulceration and bleeding can occur without abdominal pain, and black tarry stools, weakness, and dizziness upon standing (orthostatic hypotension) may be the only signs of a ulceration.
NSAIDs reduce the flow of blood to the kidneys and impair function of the kidneys. The impairment is most likely to occur in patients with preexisting impairment of kidney
function or congestive heart failure, and use of NSAIDs in these patients should be done cautiously.
Individuals who have nasal polyps or are allergic to aspirin or other NSAIDs should not use indomethacin because there is an increased risk of severe allergic reactions in these individuals.
Fluid retention, blood clots, heart attacks, hypertension (high blood pressure), and heart failure have also been associated with the use of NSAIDs.
附件:
201122418420239.pdf


---------------------------------------------------------------
产地国家: 美国
原产地英文商品名:
INDOCIN I.V. 1mg/vial 3vials/box
原产地英文药品名:
INDOMETHACIN SODIUM TRIHYDRATE
中文参考商品译名:
消炎痛I.V. 1毫克/瓶 3瓶/盒
中文参考药品译名:
吲哚美辛钠三水物
生产厂家中文参考译名:
LUNDBECK INC
生产厂家英文名:
LUNDBECK INC

该药品相关信息网址1:
http://www.rxlist.com/indocin-drug.htm
该药品相关信息网址2:
http://www.medicinenet.com/indomethacin/article.htm

责任编辑:admin


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