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Atosiban

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525: 31: 760:— showed a significant increase in the proportion of women undelivered by 48 hours in women receiving atosiban compared to placebo. When compared with β agonists, atosiban increased the proportion of women undelivered by 48 hours and was safer compared to β agonists. Therefore, oxytocin antagonists appear to be effective and safe for tocolysis in preterm labour. 2524: 943: 739:
Atosiban was approved in the European Union in January 2000 and launched in the European Union in April 2000. As of June 2007, atosiban was approved in 67 countries, excluding the United States and Japan. It was understood that Ferring did not expect to seek approval for atosiban in the US or Japan,
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Atosiban is used to delay birth in adult women who are 24 to 33 weeks pregnant, when they show signs that they may give birth pre-term (prematurely). These signs include regular contractions lasting at least 30 seconds at a rate of at least four every 30 minutes, and dilation of the cervix (the neck
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from the myometrial cell membrane. As a result, reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells and reduced influx of Ca from the extracellular space through voltage-gated channels occur. In addition, atosiban suppresses oxytocin-mediated release
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Multicentre, controlled trial of atosiban vs. ritodrine in 128 women shows a significantly better tocolytic efficacy after 7 days in the atosiban group than in the ritodrine group (60.3 versus 34.9%), but not at 48 hours (68.3 versus 58.7%). Maternal adverse events were reported less frequently in
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First- and second-trimester bleeding was more prevalent in ART than in spontaneous pregnancies. From 2004 to 2010, 33 first-trimester pregnancies with vaginal bleeding after ART with evident uterine contractions, when using atosiban and/or ritodrine, no preterm delivery occurred before 30 weeks.
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A 2012 clinical trial compared tocolytic efficacy and tolerability of atosiban with that of nifedipine. Forty-eight (68.6%) women allocated to atosiban and 39 (52%) to nifedipine did not deliver and did not require an alternate agent at 48 hours, respectively (p=.03). Atosiban has fewer failures
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for tocolysis in women with preterm labor (20–36 weeks), but it has been assigned to pregnancy category C by the U.S. Food and Drug Administration, so is not recommended before 20 weeks, or in the first trimester. A report from 2011 supports the use of atosiban, even at very early pregnancy, to
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in the suppression of preterm labour concluded that atosiban and nifedipine are effective in delaying delivery for seven days or more in women presenting with preterm labour. A total of 68.3% of women in the atosiban group remained undelivered at seven days or more, compared with 64.7% in the
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In human preterm labour, atosiban, at the recommended dosage, antagonises uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.
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A 2009 randomised controlled study demonstrated for the first time the direct effects of atosiban on fetal movement, heart rate, and blood flow. Tocolysis with either atosiban or nifedipine combined with betamethasone administration had no direct fetal adverse effects.
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Following the launch of atosiban in 2000, the calculated cumulative patient exposure to atosiban (January 2000 to December 2005) is estimated as 156,468 treatment cycles. To date, routine monitoring of drug safety has revealed no major safety issues.
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Shim JY, Park YW, Yoon BH, Cho YK, Yang JH, Lee Y, Kim A (November 2006). "Multicentre, parallel group, randomised, single-blind study of the safety and efficacy of atosiban versus ritodrine in the treatment of acute preterm labour in Korean women".
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focusing instead on development of new compounds for use in Spontaneous Preterm Labor (SPTL). The fact that atosiban only had a short duration before it was out of patent that the parent drug company decided not to pursue licensing in the US.
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and first reported in the literature in 1985. Originally marketed by Ferring Pharmaceuticals, it is licensed in proprietary and generic forms for the delay of imminent preterm birth in pregnant adult women.
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in the major outcomes i.e. pregnancy prolongation or neonatal outcomes. The finding of an increase in infant deaths in one placebo-controlled trial warrants caution. Further research is recommended.
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the atosiban group (7.9 vs 70.8%), resulting in fewer early drug terminations due to adverse events (0 versus 20%). Therefore, atosiban is superior to ritodrine in the treatment of preterm labour.
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It was for this reason and the fact that Tractocile (atosiban) only had a short duration before it was out of patent that the parent drug company decided not to pursue licensing in the USA.
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nifedipine group. They have the same efficacy and associated minor side effects. However, flushing, palpitation, and hypotension were significantly higher in the nifedipine group.
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Atosiban is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban inhibits the oxytocin-mediated release of
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Akerlund M, Carlsson AM, Melin P, Trojnar J (1985). "The effect on the human uterus of two newly developed competitive inhibitors of oxytocin and vasopressin".
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of the womb) of 1 to 3 cm and an effacement (a measure of the thinness of the cervix) of 50% or more. In addition, the baby must have a normal heart rate.
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de Heus R, Mulder EJ, Derks JB, Visser GH (June 2009). "The effects of the tocolytics atosiban and nifedipine on fetal movements, heart rate and blood flow".
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Lan VT, Khang VN, Nhu GH, Tuong HM (September 2012). "Atosiban improves implantation and pregnancy rates in patients with repeated implantation failure".
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Saleh SS, Al-Ramahi MQ, Al Kazaleh FA (January 2013). "Atosiban and nifedipine in the suppression of pre-term labour: a comparative study".
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Coomarasamy A, Knox EM, Gee H, Khan KS (November 2002). "Oxytocin antagonists for tocolysis in preterm labour -- a systematic review".
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Lamont CD, Jørgensen JS, Lamont RF (September 2016). "The safety of tocolytics used for the inhibition of preterm labour".
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Lamont RF, Kam KY (March 2008). "Atosiban as a tocolytic for the treatment of spontaneous preterm labor".
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of atosiban for tocolysis in preterm labour, six clinical studies — two compared atosiban to
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within 48 hours. Nifedipine may be associated with a longer postponement of delivery.
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showed that while atosiban had fewer side effects than alternative drugs (such as
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decrease the frequency of uterine contractions to enhance success of pregnancy.
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Flenady V, Reinebrant HE, Liley HG, Tambimuttu EG, Papatsonis DN (June 2014).
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A 2013 retrospective study comparing the efficacy and safety of atosiban and
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Salim R, Garmi G, Nachum Z, Zafran N, Baram S, Shalev E (December 2012).
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This article incorporates text from this source, which is in the
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Journal of the Formosan Medical Association = Taiwan Yi Zhi
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Conde-Agudelo A, Romero R, Kusanovic JP (February 2011).
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Atosiban is useful in improving the pregnancy outcome of
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fertilization-embryo transfer (IVF-ET) in patients with
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Chou PY, Wu MH, Pan HA, Hung KH, Chang FM (June 2011).
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The Journal of Maternal-Fetal & Neonatal Medicine
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The pregnancy rate improved from zero to 43.7%. 916: 914: 912: 910: 908: 906: 904: 1063:Taiwanese Journal of Obstetrics & Gynecology 274: 1492: 1490: 1440: 1438: 1436: 1434: 1390: 1388: 1386: 1384: 249: 1230: 1228: 1226: 1224: 1052: 1050: 607:among others, is an inhibitor of the hormones 1775: 1615: 1183:American Journal of Obstetrics and Gynecology 962:Acta Obstetricia et Gynecologica Scandinavica 8: 1237:Expert Review of Obstetrics & Gynecology 21: 1349:The Cochrane Database of Systematic Reviews 188:In general: ℞ (Prescription only) 2044: 1782: 1768: 1760: 1622: 1608: 1600: 448: 425: 334: 1462: 1364: 1204: 1194: 1153: 1136:Wu MY, Chen SU, Yang YS (December 2011). 1074: 1030: 1020: 1009:Therapeutics and Clinical Risk Management 354: 690:Atosiban use after assisted reproduction 2519: 819: 564: 544: 421: 314: 209: 439: 20: 1397:Journal of Obstetrics and Gynaecology 394: 62: 7: 1595:. U.S. National Library of Medicine. 1131: 1129: 127: 828:"Atosiban International Drug Names" 374: 265: 14: 677:of PGE and PGF from the decidua. 2560:Vasopressin receptor antagonists 2522: 1555:10.1111/j.1471-0528.2006.01053.x 1003:Sanu O, Lamont RF (April 2010). 941: 763:A 2014 systematic review by the 479: 473: 29: 1100:Reproductive Biomedicine Online 834:. 10 April 2020. Archived from 572:Key:VWXRQYYUEIYXCZ-OBIMUBPZSA-N 1357:10.1002/14651858.CD004452.pub3 491: 485: 467: 1: 2545:Oxytocin receptor antagonists 1284:10.1080/14740338.2016.1187128 1272:Expert Opinion on Drug Safety 700:repeated implantation failure 212:1-(3-Mercaptopropanoic acid)- 1464:10.1097/aog.0b013e3182755dff 1409:10.3109/01443615.2012.721822 715:adrenergic receptor agonists 603:, sold under the brand name 642:The most commonly reported 48:Tractocile, Antocin, others 2591: 1196:10.1016/j.ajog.2010.11.038 1155:10.1016/j.jfma.2011.11.016 1112:10.1016/j.rbmo.2012.05.014 1076:10.1016/j.tjog.2011.04.003 457:Chemical and physical data 2351:Vasotocin (argiprestocin) 2346:Vasopressin (argipressin) 2237:Vasotocin (argiprestocin) 2232:Vasopressin (argipressin) 2093:Vasotocin (argiprestocin) 2088:Vasopressin (argipressin) 1875:Vasotocin (argiprestocin) 1511:10.1080/14767050802702349 1451:Obstetrics and Gynecology 974:10.3109/00016348509156728 927:European Medicines Agency 580: 555: 535: 200: 28: 1723:Calcium channel blockers 1249:10.1586/17474108.3.2.163 1648:adrenoreceptor agonists 1593:Drug Information Portal 1318:Medical Science Monitor 784:Atosiban vs. nifedipine 756:and four atosiban to a 632:Ferring Pharmaceuticals 2267:ORG-52186 (SCH-740935) 1989:Catabolism inhibitors: 805:Atosiban vs. ritodrine 765:Cochrane Collaboration 674:inositol trisphosphate 630:. It was developed by 1795:vasopressin receptor 1633:/labor repressants ( 1189:(2): 134.e1–134.20. 626:(tocolytic) to halt 2575:Sec-Butyl compounds 1997:Bestatin (ubenimex) 1324:(11): RA268–RA273. 931:. 17 September 2018 838:on 27 December 2019 668:Mechanism of action 615:. It is used as an 232:-ornithine-oxytocin 176:(Prescription only) 163:(Prescription only) 64:UK Drug Information 25: 1022:10.2147/tcrm.s9378 744:Systematic reviews 735:Regulatory affairs 2510: 2509: 2490:Carrier proteins: 2478: 2477: 2469:lithium carbonate 2457:Other inhibitors: 2009: 1865:PF-06655075 (PF1) 1757: 1756: 1749:Magnesium sulfate 1741:Myosin inhibitors 1549:(11): 1228–1234. 922:"Tractocile EPAR" 750:systematic review 726:Pharmacovigilance 719:magnesium sulfate 624:labour repressant 598: 597: 526:Interactive image 407:CompTox Dashboard 231: 225: 221: 184: 171: 158: 83: 16:Chemical compound 2582: 2565:Ethoxy compounds 2527: 2526: 2525: 2518: 2045: 2020:o-Phenanthroline 2007: 1784: 1777: 1770: 1761: 1624: 1617: 1610: 1601: 1596: 1575: 1574: 1537: 1531: 1530: 1494: 1485: 1484: 1466: 1457:(6): 1323–1331. 1442: 1429: 1428: 1392: 1379: 1378: 1368: 1340: 1334: 1333: 1313: 1307: 1306: 1278:(9): 1163–1173. 1267: 1261: 1260: 1232: 1219: 1218: 1208: 1198: 1174: 1168: 1167: 1157: 1133: 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1536: 1533: 1528: 1524: 1520: 1516: 1512: 1508: 1504: 1500: 1493: 1491: 1487: 1482: 1478: 1474: 1470: 1465: 1460: 1456: 1452: 1448: 1441: 1439: 1437: 1435: 1431: 1426: 1422: 1418: 1414: 1410: 1406: 1402: 1398: 1391: 1389: 1387: 1385: 1381: 1376: 1372: 1367: 1362: 1358: 1354: 1350: 1346: 1339: 1336: 1331: 1327: 1323: 1319: 1312: 1309: 1305: 1301: 1297: 1293: 1289: 1285: 1281: 1277: 1273: 1266: 1263: 1258: 1254: 1250: 1246: 1242: 1238: 1231: 1229: 1227: 1225: 1221: 1216: 1212: 1207: 1202: 1197: 1192: 1188: 1184: 1180: 1173: 1170: 1165: 1161: 1156: 1151: 1147: 1143: 1139: 1132: 1130: 1126: 1121: 1117: 1113: 1109: 1105: 1101: 1094: 1091: 1086: 1082: 1077: 1072: 1068: 1064: 1060: 1053: 1051: 1047: 1042: 1038: 1033: 1028: 1023: 1018: 1014: 1010: 1006: 999: 996: 991: 987: 983: 979: 975: 971: 967: 963: 956: 953: 949: 948:public domain 930: 928: 923: 917: 915: 913: 911: 909: 907: 905: 901: 888: 884: 878: 875: 863: 859: 853: 850: 837: 833: 829: 823: 820: 813: 811: 804: 802: 798: 794: 791: 783: 778: 776: 774: 770: 766: 761: 759: 755: 751: 743: 741: 734: 732: 725: 723: 720: 716: 707: 703: 701: 697: 689: 684: 682: 678: 675: 667: 662: 660: 653: 651: 649: 645: 640: 637: 633: 629: 625: 621: 618: 614: 610: 606: 602: 592: 585: 579: 570: 565: 561: 554: 545: 541: 534: 527: 523: 522: 520: 517: 512: 505: 503: 499: 466: 464: 460: 455: 451: 447: 444: 442: 440:ECHA InfoCard 436: 428: 424: 423:DTXSID8048991 420: 419: 417: 408: 404: 397: 393: 392: 390: 388: 384: 377: 373: 372: 370: 368: 364: 357: 353: 352: 350: 348: 344: 337: 333: 332: 330: 328: 324: 317: 313: 312: 310: 308: 304: 297: 293: 292: 290: 288: 284: 277: 273: 272: 270: 263: 259: 252: 248: 247: 245: 243: 239: 222:-tyrosine)-4- 217: 210: 206: 199: 194: 187: 185: Rx-only 178: 175: 165: 162: 152: 151: 149: 147: 143: 138: 130: 125: 122: 121: 119: 117: 113: 110: 107: 105: 99: 92: 87: 78: 77: 75: 73: 69: 65: 61: 59: 55: 51: 47: 45: 41: 38:Clinical data 36: 32: 27: 19: 2570:Nonapeptides 2489: 2456: 2417:Antagonists: 2416: 2366:JNJ-17079166 2358:Antagonists: 2357: 2341:Terlipressin 2311:Desmopressin 2307: 2283: 2277:TASP-0390325 2272:TASP-0233278 2244:Antagonists: 2243: 2227:Terlipressin 2207:Desmopressin 2203: 2128:JNJ-17308616 2123:JNJ-17079166 2102: 2100:Antagonists: 2099: 2083:Terlipressin 2059: 1988: 1924:Non-peptide: 1923: 1914: 1911: 1909:Antagonists: 1908: 1879:Non-peptide: 1878: 1816: 1813: 1694: 1592: 1546: 1542: 1535: 1502: 1498: 1454: 1450: 1403:(1): 43–45. 1400: 1396: 1348: 1338: 1321: 1317: 1311: 1303: 1275: 1271: 1265: 1240: 1236: 1186: 1182: 1172: 1145: 1141: 1103: 1099: 1093: 1066: 1062: 1012: 1008: 998: 965: 961: 955: 933:. Retrieved 925: 891:. Retrieved 886: 877: 865:. Retrieved 861: 852: 840:. Retrieved 836:the original 831: 822: 808: 799: 795: 787: 762: 747: 738: 729: 708: 704: 695: 693: 679: 671: 663:Pharmacology 657: 654:Medical uses 641: 604: 600: 599: 588:   582:   396:ChEMBL378642 215: 146:Legal status 140:Legal status 72:License data 18: 2493:Neurophysin 2331:Ornipressin 2316:Felypressin 2257:Brezivaptan 2222:Ornipressin 2212:Felypressin 2148:Relcovaptan 2078:Selepressin 2073:Ornipressin 2063:Felypressin 2040:Vasopressin 2010:-Methionine 1860:PF-06478939 1835:Demoxytocin 1713:Indometacin 1688:antagonists 1676:Terbutaline 1148:(12): 800. 1015:: 191–199. 644:side effect 617:intravenous 613:vasopressin 509: g·mol 446:100.234.128 226:-threonine- 196:Identifiers 109:Intravenous 44:Trade names 2555:Tocolytics 2539:Categories 2430:RWJ-339489 2425:Ribuvaptan 2420:Balovaptan 2386:Satavaptan 2381:RWJ-351647 2376:Mozavaptan 2371:Lixivaptan 2361:Conivaptan 2262:Nelivaptan 2168:WAY-267464 2113:Conivaptan 2108:Balovaptan 1982:WAY-162720 1977:SSR-126768 1932:Cligosiban 1897:WAY-267464 1850:Nacartocin 1830:Cargutocin 1825:Carbetocin 1820:Aspartocin 1798:modulators 1731:Nifedipine 1631:Tocolytics 1589:"Atosiban" 814:References 790:nifedipine 685:Other uses 620:medication 605:Tractocile 514:3D model ( 502:Molar mass 356:081D12SI0Z 327:ChemSpider 287:IUPHAR/BPS 251:90779-69-4 242:CAS Number 205:IUPAC name 2450:YM-222546 2391:Tolvaptan 2326:Lypressin 2308:Agonists: 2217:Lypressin 2204:Agonists: 2143:PF-184563 2138:LY-307174 2118:FR-218944 2068:Lypressin 2060:Agonists: 2030:Puromycin 2015:Leupeptin 1992:Amastatin 1972:Retosiban 1967:Nolasiban 1962:L-372,662 1957:L-371,257 1952:L-368,899 1942:Erlosiban 1937:Epelsiban 1927:Barusiban 1845:Merotocin 1814:Agonists: 1671:Ritodrine 1661:Fenoterol 1656:Buphenine 1257:1747-4108 832:Drugs.com 769:ritodrine 758:β agonist 102:Routes of 58:Drugs.com 2550:Peptides 2529:Medicine 2445:VMAX-382 2440:VMAX-372 2435:VMAX-367 2410:Unsorted 2401:YM-35471 2336:TC OT 39 2287:TASP-699 2284:Ligands: 2183:YM-35471 2163:TC OT 39 2103:Atosiban 1915:Atosiban 1912:Peptide: 1892:TC OT 39 1855:Oxytocin 1817:Peptide: 1806:Oxytocin 1791:Oxytocin 1695:Atosiban 1686:Oxytocin 1571:27031083 1563:16978233 1527:35810758 1519:19479644 1481:22487349 1473:23168756 1425:20753923 1417:23259877 1375:24903678 1366:11086629 1330:12444392 1292:27159501 1215:21284967 1164:22248840 1120:22818095 1085:21791296 1041:20463780 990:25799128 935:29 April 893:29 April 867:29 April 842:29 April 696:in vitro 609:oxytocin 601:Atosiban 591:(verify) 307:DrugBank 116:ATC code 23:Atosiban 2465:Lithium 2321:LIT-001 2252:ABT-558 2247:ABT-436 2133:LIT-001 1887:LIT-001 1300:4937942 1206:3437772 1032:2861440 982:4061066 773:placebo 754:placebo 463:Formula 336:4470550 316:DB09059 276:5311010 262:PubChem 218:-ethyl- 132:) 126: ( 124:G02CX01 88::  2515:Portal 2483:Others 2396:YM-471 2178:YM-471 2173:YM-218 2158:SRX251 2153:SRX246 1902:WJ0679 1705:NSAIDs 1569:  1561:  1525:  1517:  1479:  1471:  1423:  1415:  1373:  1363:  1328:  1298:  1290:  1255:  1213:  1203:  1162:  1118:  1083:  1039:  1029:  988:  980:  648:nausea 636:Sweden 540:SMILES 507:994.19 387:ChEMBL 376:D03008 172: 159: 91:by INN 84:  1947:IX-01 1635:G02CA 1567:S2CID 1523:S2CID 1477:S2CID 1421:S2CID 1296:S2CID 986:S2CID 929:(EMA) 887:(emc) 862:(emc) 748:In a 622:as a 560:InChI 516:JSmol 2002:EDTA 1870:TGOT 1793:and 1559:PMID 1543:BJOG 1515:PMID 1469:PMID 1413:PMID 1371:PMID 1326:PMID 1288:PMID 1253:ISSN 1211:PMID 1160:PMID 1116:PMID 1081:PMID 1037:PMID 978:PMID 937:2020 895:2020 869:2020 844:2020 717:and 611:and 367:KEGG 347:UNII 296:2213 54:AHFS 1882:CA7 1551:doi 1547:113 1507:doi 1459:doi 1455:120 1405:doi 1361:PMC 1353:doi 1280:doi 1245:doi 1201:PMC 1191:doi 1187:204 1150:doi 1146:110 1108:doi 1071:doi 1027:PMC 1017:doi 970:doi 646:is 634:in 412:EPA 266:CID 214:2-( 174:POM 129:WHO 86:EMA 2541:: 2501:II 2499:, 2195:1B 2051:1A 1922:; 1877:; 1591:. 1565:. 1557:. 1545:. 1521:. 1513:. 1503:22 1501:. 1489:^ 1475:. 1467:. 1453:. 1449:. 1433:^ 1419:. 1411:. 1401:33 1399:. 1383:^ 1369:. 1359:. 1347:. 1320:. 1302:. 1294:. 1286:. 1276:15 1274:. 1251:. 1239:. 1223:^ 1209:. 1199:. 1185:. 1181:. 1158:. 1144:. 1140:. 1128:^ 1114:. 1104:25 1102:. 1079:. 1067:50 1065:. 1061:. 1049:^ 1035:. 1025:. 1011:. 1007:. 984:. 976:. 966:64 964:. 924:. 903:^ 885:. 860:. 830:. 650:. 489:12 483:11 477:67 471:43 228:8- 181:EU 168:UK 161:S4 155:AU 81:EU 2517:: 2503:) 2497:I 2495:( 2471:) 2467:( 2299:2 2297:V 2193:V 2049:V 2008:L 1783:e 1776:t 1769:v 1646:2 1644:β 1637:) 1623:e 1616:t 1609:v 1573:. 1553:: 1529:. 1509:: 1483:. 1461:: 1427:. 1407:: 1377:. 1355:: 1332:. 1322:8 1282:: 1259:. 1247:: 1241:3 1217:. 1193:: 1166:. 1152:: 1122:. 1110:: 1087:. 1073:: 1043:. 1019:: 1013:6 992:. 972:: 950:. 939:. 897:. 871:. 846:. 713:2 711:β 518:) 495:2 492:S 486:O 480:N 474:H 468:C 414:) 410:( 230:L 224:L 220:D 216:O 183:: 170:: 157:: 56:/

Index


Trade names
AHFS
Drugs.com
UK Drug Information
License data
EMA
by INN
Routes of
administration

Intravenous
ATC code
G02CX01
WHO
Legal status
S4
POM
IUPAC name
CAS Number
90779-69-4
PubChem
5311010
IUPHAR/BPS
2213
DrugBank
DB09059
ChemSpider
4470550
UNII
081D12SI0Z
KEGG

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