Indomethacin 吲哚美辛
CAS 53-86-1 MFCD00057095
化学结构图
SMILES: COc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(Cl)cc1
化学属性
| Mol. Formula | C19H16ClNO4 |
|---|---|
| Mol. Weight | 357.79 |
| Melting Point | 155-162 °C |
| TSCA | Yes |
| Appearance | 白色或微黄色结晶性粉末。熔点158-162℃。溶于丙酮，略溶于乙醇、氯仿、乙醚，几乎不溶于水。无味，几乎无臭。 |
| Solubility | ethanol: 50 mg/mL, clear, yellow-green |
| Density | 1.32 |
别名和识别编码
| Chemical Name | Indomethacin |
|---|---|
| CAS Number | 53-86-1 |
| Synonym | (1-(4-chloro-benzoyl)-5-methoxy-2-methyl-indol-3-yl)-acetic acid (1-p-Chlorobenzoyl-5-methoxy-2-methylindol-3-yl)acetic acid (1-p-chlorobenzoyl-5-methoxy-2-methylindol-3-yl)aceticacid 1- 1-(4-CHLOROBENZOYL)-5-METHOXY-2-METHYL-1H-INDOLE-3-ACETIC ACID 1-(4-Chlorbenzoyl)-5-methoxy-2-methyl-1H-indol-3-essigsäure 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic Acid 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-3-indoleacetic acid 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indole-3-aceticaci 1-(4-氯苯甲酰基 1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1H-吲哚-3-乙酸 1-(P 1-(p-Chlorbenzoyl)-5-methoxy-2-methylindol-3-essigsaeure 1-(p-Chlorobenzoyl)-2-methyl-5-methoxy-3-indole-acetic acid 1-(p-Chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid Indom |
| MDL Number | MFCD00057095 |
| Beilstein Registry Number | 22(5)5,239 |
| EC Number | 200-186-5 |
| Merck Number | 4968 |
| PubChem Substance ID | 3715 |
| Reaxys-RN | 497341 |
| Chemical Name Translation | 吲哚美辛 |
| Wiswesser Line Notation | T56 BNJ BVR CG& C1 D1VQ GO1 |
| LabNetwork Molecule ID | LN00222621 |
| InChI | InChI=1S/C19H16ClNO4/c1-11-15(10-18(22)23)16-9-14(25-2)7-8-17(16)21(11)19(24)12-3-5-13(20)6-4-12/h3-9H,10H2,1-2H3,(H,22,23) |
| Canonical SMILES | COC1=CC=C(N(C(C2=CC=C(Cl)C=C2)=O)C(C)=C3CC(O)=O)C3=C1 |
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信息真实价格透明
资金保障
专业采购外包团队在线服务
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分类
- {SNA} Analytical Standards, Analytical/Chromatography, Chromatography, Pharmaceutical Standards, Pharmacopeia Standards, USP Standards, USP Standards I - K
- {SNA} Antibiotics, Antibiotics A to Z, Antibiotics G-M, Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology, Core Bioreagents, Enzyme Inhibitors, I, Inhibits an Enzyme, Mechanism of Action, Research Essentials
- {SNA} A to C, Antibiotics, Antibiotics A to Z, Antibiotics G-M, Antitumor Agents, Application Index, Approved Therapeutics/Dru
产品应用
- 环加氧酶(COX) 抑制剂,选择性地抑制COX-1；阻断前列腺索的生物合成。
- 医药上抗炎，解热作用明显，主要用于对水杨酸类药物不易耐受或疗效不显著的风湿性并节炎、强直性光脊椎炎、骨关节炎等。
相关文献及参考
- Merck:4968 Beilstein:22(5)5,239
- Salari, H., et al.: Prostagland. Leukotrienes Med., 13, 53 (1984),
- Short: IV/8A
- Merck:4968
- Short: EINECS
安全信息
GHS Symbol
- P201 Obtain special instructions before use. 使用前获取专门指示。
- P202 Do not handle until all safety precautions have been read and understood. 已阅读并理解所有的安全预防措施之前，切勿操作。
- P260 Do not breathe dust/fume/gas/mist/vapours/spray. 不要吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P261 Avoid breathing dust/fume/gas/mist/vapours/spray. 避免吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
- P270 Do not eat, drink or smoke when using this product. 使用本产品时不要吃东西，喝水或吸烟。
- P271 Use only outdoors or in a well-ventilated area.? 只能在室外或通风良好的地方使用。
- P272 Contaminated work clothing should not be allowed out of the workplace. 污染的工作服不得带出工作场所。
- P273 Avoid release to the environment. 避免释放到环境中。
- P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
- P281 Use personal protective equipment as required. 使用所需的个人防护装备。
- P301+P310
- P301+P310+P330
- P302+P352
- P304+P340
- P305+P351+P338
- P307+P311
- P308+P313
- P310 Immediately call a POISON CENTER or doctor/physician. 立即呼救解毒中心或医生/医师。
- P312 Call a POISON CENTER or doctor/physician if you feel unwell. 如果你感觉不适，呼叫解毒中心或医生/医师。
- P314 Get medical advice/attention if you feel unwell. 获取医疗咨询/就医，如果你觉得不舒服
- P321 Specific treatment (see … on this label). 具体治疗（见本标签上的）。
- P330 Rinse mouth. 漱口
- P333+P313
- P363 Wash contaminated clothing before reuse. 被污染的衣服洗净后方可重新使用。
- P403+P233
- P405 Store locked up. 上锁保管。
- P501 Dispose of contents/container to..… 处理内容物/容器.....
- H300 Fatal if swallowed 吞食致命
- H301 Toxic if swallowed 吞食有毒
- H317 May cause an allergic skin reaction 可能导致皮肤过敏
- H318 Causes serious eye damage 严重伤害眼睛
- H335 May cause respiratory irritation 可能导致呼吸道刺激
- H336 May cause drowsiness or dizziness 肯能导致嗜睡或头晕
- H360 May damage fertility or the unborn child 可能对生育能力或未出生婴儿造成伤害
- H370 Causes damage to organs 导致器官损伤
- H373 May causes damage to organs through prolonged or repeated exposure 长期或频繁接触可能会损伤器官
- H413 Maycauselonglastingharmfuleffectstoaquaticlife 可能对水生生物造成长期持续有害影响。
- S28 After contact with skin, wash immediately with plenty of ... (to be specified by the manufacturer) 皮肤接触后，立即用大量…（由生产厂家指定）冲洗；
- S45 In case of accident or if you feel unwell seek medical advice immediately (show the label where possible) 发生事故时或感觉不适时，立即求医（可能时出示标签）；
- S20 When using do not eat or drink 使用时，不得进食，饮水；
- S36/37 Wear suitable protective clothing and gloves 穿戴适当的防护服和手套；
- R68 Possible risk of irreversible effects 可能有不可挽回的作用的危险
- R28 Very toxic if swallowed 吞咽极毒
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 644 mg/kg/92W-C TOXIC EFFECTS : Tumorigenic - neoplastic by RTECS criteria Skin and Appendages - tumors REFERENCE : CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 16,1493,1995
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 21 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,655,1981
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 18200 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1398,1980
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOS
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2420 ug/kg TOXIC EFFECTS : Gastrointestinal - ulceration or bleeding from stomach REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1526,1975
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 12 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,70,1968
TYPE OF TEST : LD50 -
TYPE OF TEST : Mutation in microorganisms
TEST SYSTEM : Bacteria - Salmonella typhimurium
DOSE/DURATION : 100 ug/disc
REFERENCE :
JNUDAT Journal of Nihon University School of Dentistry. (Nihon University
School of Dentistry, 1-8-13 Surugadai, Kanda, Chiyoda-ku, Tokyo, 101, Japan)
V.1- 1958- Volume(issue)/page/year: 34,183,1992TYPE OF TEST : Micronucleus test ROUTE OF EXPOSURE : Intraperitoneal TEST SYSTEM : Rodent - mouse DOSE/DURATION : 72 mg/kg/24H REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 188,343,1987
TYPE OF TEST : Mutation test systems - not otherwise specified TEST SYSTEM : Rodent - rat Cells - not otherwise specified DOSE/DURATION : 10 mg/L REFERENCE : REXMAS Research in Experimental Medicine. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.157- 1972- Volume(issue)/page/year: 189,173,1989
TYPE OF TEST : Dominant lethal test ROUTE OF EXPOSURE : Oral TEST SYSTEM : Rodent - ra
TYPE OF TEST : Sperm Morphology ROUTE OF EXPOSURE : Oral TEST SYSTEM : Rodent - mouse DOSE/DURATION : 60 mg/kg/5D (Continuous) REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 188,343,1987
TYPE OF TEST : Micronucleus test ROUTE OF EXPOSURE : Oral TEST SYSTEM : Rodent - mouse DOSE/DURATION : 72 mg/kg/24H REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 188,343,1987
TYPE OF TEST
{haTYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE : 525 mg/kg SEX/DURATION : female 16-32 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Maternal Effects - other effects Reproductive - Specific Developmental Abnormalities - urogenital system REFERENCE : AJMGDA American Journal of Medical Genetics. (John Wiley & Sons Ltd., 605 Third Ave., New York, NY 10158) V.1- 1977- Volume(issue)/page/year: 39,252,1991
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE : 12 mg/kg SEX/DURATION : fema
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Primate - monkey DOSE : 6 mg/kg SEX/DURATION : female 2 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 27,505,1983
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Rodent - rat DOSE : 3 mg/kg SEX/DURATION : female 20 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system REFERENCE : TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 30(1),20A,1984
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Parenteral SPEC
其他信息
- TCI Shanghai:吲哚美辛 Indomethacin,>;98.0%(LC)(T)(53-86-1)
- 毒性分级:剧毒
- 消炎镇痛药:吲哚美辛又称消炎痛，是一种作用较强的非皮质激素类的消炎解热和镇痛药，通过抑制环氧酶减少前列腺素(PG)合成，制止炎症组织痛觉神经冲动的形成，抑制炎性反应，包括抑制白细胞的趋化性及溶酶体酶的释放等，从而产生解热、镇痛及消炎作用。吲哚美辛的消炎、解热作用很强，其抗炎作用比保泰松强84倍，比氢化可的松也强，与糖皮质激素、阿司匹林、保泰松联合使用，可减少它们的用量、毒性及副作用，提高疗效；其次是解热作用，为氨基比林的10倍；镇痛作用较弱，只对炎性疼痛有明显镇痛作用，但对炎性疼痛的效果好于保泰松、安乃近和水杨酸类。临床主要用于对水杨酸类药物不易耐受，或疗效不明显的急、慢性风湿性或类风湿性关节炎、强直性脊柱炎、滑囊炎、腱鞘炎、关节囊炎、骨关节炎、急性痛风及癌性疼痛等。近年来研究人员尝试将吲哚美辛用于胆绞痛、痛经、偏头痛、肾小球肾炎、多尿、沙门菌性胃肠炎、体位性低血压、巴特综合征等，均有较好疗效。还可用于治疗眼科色素膜炎、角膜炎、巩膜炎、青光眼以及癌症引起的发热或其他难以控制的发热。皮肤科用于红斑狼疮、白塞综合征、硬皮病、结节性红斑、带状疱疹、关节型银屑病等。外用治疗湿疹、过敏性皮炎、光感性皮炎、局部疼痛。
- 不良反应:吲
- 灭火剂:泡沫、雾状水、砂土、二氧化碳
- 可燃性危险特性:明火可燃; 高热分解有毒氯化物和氮氧化物气体
- MS
- 药动学:口服给药吸收迅速而完全，4h可吸收给药量的90%以上，食物或服用含铝及镁的制酸药可稍使吸收减慢，血浆蛋白结合率约为99%。口服25mg后达峰时间为1～4h，血药峰浓度(Cmax)为1.4μg/ml，50mg时Cmax为2.8μg/ml;半衰期(t1/2) 平均为4.5h，早产儿明显延长。少量吲哚美辛可透过血-脑屏障。并可透过胎盘。本品在肝脏代谢为去甲基化物和去氯苯甲酰化物，又可水解为吲哚美辛重新吸收再循环。60%从肾脏排泄，其中10%～20%以原形排出;部分随粪便排出。33% 从胆汁排泄，其中1.5%为原形;在乳汁中也有排出(每日可达0.5～2.0mg)。本品不能被透析清除。
- 图谱信息:吲哚美辛(53-86-1)核磁图( 1 HNMR) 吲哚美辛(53-86-1)核磁图( 13 CNMR) 吲哚美辛(53-86-1)质谱(MS) 吲哚美辛(53-86-1)红外图谱(IR1) 吲哚美辛(53-86-1)红外图谱(IR2)
- 用法与用量:1.抗风湿：成人用量：口服：初量每次25～50mg，每日2～4次，饭时饭后立即服。如耐受好，每日用量可每周递增25～50mg，1日最大量不应超过200mg。关节炎患者如有持续性夜间疼痛或晨僵现象，可将全天量100mg于睡前给予。 2.抗痛风：口服：初量1次100mg，继之50mg，每日3次，直至疼痛缓解，然后尽快逐渐减量，直至停药。 3.退热：成人用量：口服：每次25～50mg，每日3～4次;直肠给药：每次50mg，每日50～100mg。小儿用量：口服：每次0.5～1mg/kg，每日3次。
- 急性毒性:口服- 大鼠 LD50 2.42 毫克/ 公斤; 口服- 小鼠 LD50: 11.84 毫克/公斤
- 方法一:对氨基苯甲
- 上游原料:对甲氧基
- Alfa Aesar:吲哚美辛,98% Indomethacin, 98%(53-86-1)
- {Chemica
- 不良反应:吲哚美辛的不良反应的发生率相当高，常见的不良反应如下： ①恶心、呕吐、腹痛、腹泻、纳差，严重者可出现溃疡并引起出血和穿孔等。饭后即服可减少发生率。 ②常见有头痛、头晕、乏力，偶有惊厥、精神错乱、晕厥等。应注意适时停药。 ③皮肤瘙痒、红斑、荨麻疹以及少有的哮喘发作、呼吸困难甚至呼吸、循环的抑制。 ④造血系统的抑制如粒细胞减少、再生障碍性贫血、血小板减少等。虽
- 用途三:环加氧酶(COX) 抑制剂,选择性地抑制COX-1；阻断前列腺索的生物合成。医药上抗炎，解热作用明显，主要用于对水杨酸类药物不易耐受或疗效不显著的风湿性并节炎、强直性光脊椎炎、骨关节炎等。
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