Knowledge (XXG)

Linagliptin

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Linagliptin was approved for medical use in the United States, Japan, the European Union, Canada, and Australia in 2011. In 2020, it was the 293rd most commonly prescribed medication in the United States, with more than
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InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1
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Neumiller JJ (March 2012). "Pharmacology, efficacy, and safety of linagliptin for the treatment of type 2 diabetes mellitus".
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as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.
2185: 1831: 1718: 1604: 1260: 1225: 581: 275: 263: 112: 1130: 521: 2472: 1688: 1650: 1217: 870: 806:(but not type 1) in conjunction with exercise and diet. It is generally less preferred than 649: 436: 313: 48: 541: 2706: 1645: 1627: 803: 348: 321: 632: 2663: 2407: 2072: 2001: 1753: 1702: 1609: 1599: 1579: 1557: 2716: 2453: 2432: 2427: 2422: 2402: 2397: 2392: 2387: 2382: 2276: 2032: 1991: 1879: 1874: 1864: 1859: 1665: 1237: 1061: 842: 717: 461: 288: 154: 2286: 2281: 2261: 2163: 2153: 2148: 2037: 2011: 1979: 1939: 1917: 1912: 1907: 1894: 1884: 1869: 1849: 1835: 1561: 1369: 1178: 830: 811: 219: 214: 140: 1344: 2271: 2266: 2246: 2241: 2197: 2191: 2158: 2143: 2133: 2128: 2123: 2101: 2096: 2091: 2082: 2067: 2052: 2042: 2021: 1996: 1944: 1902: 1854: 1844: 1660: 822: 148: 1062:"Trajenta 5 mg film-coated tablets - Summary of Product Characteristics (SmPC)" 2448: 2335: 2325: 2320: 2315: 2231: 2226: 2221: 2062: 2047: 2016: 1821: 834: 826: 825:
include inflammation of the nose and throat. Serious side effects may include
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million prescriptions. From August 2021 linagliptin became available as a
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CC#CCN1C2=C(N=C1N3CCC(C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
705: 696: 572: 390: 386: 552: 297: 269: 1782: 1573: 1521: 282: 171: 954: 617: 245: 63: 84: 75: 69: 57: 1259:(76 ed.). Pharmaceutical Press. 2018. p. 680. 258: 781: 2690: 1095: 1093: 1091: 1089: 1087: 96: 87: 60: 51: 81: 78: 72: 54: 2471: 2441: 2372: 2344: 2306: 2299: 2211: 2172: 2114: 2081: 1978: 1966: 1957: 1926: 1893: 1830: 1802: 1793: 1716: 1679: 1636: 1618: 1590: 716: 694: 681: 648: 643: 611: 591: 571: 551: 531: 511: 491: 480: 471: 446: 426: 397: 380: 367: 357: 347: 337: 320: 312: 235: 230: 205: 191: 161: 147: 129: 121: 111: 66: 42: 37: 1185:. American Society of Health-System Pharmacists. 1491:"Linagliptin: medicine to treat type 2 diabetes" 460: 901:Linagliptin belongs to a class of drugs called 435: 414:8--7-(but-2-yn-1-yl)-3-methyl-1--3,7-dihydro-1 1533: 8: 1101:"Tradjenta- linagliptin tablet, film coated" 180: 21: 849:that works by increasing the production of 305:In general: ℞ (Prescription only) 2477: 2303: 2169: 1975: 1963: 1799: 1790: 1779: 1587: 1570: 1540: 1526: 1518: 1173: 1171: 1169: 1167: 1165: 1163: 1161: 1159: 631: 520: 1464:. World Health Organization. p. 66. 1179:"Linagliptin Monograph for Professionals" 917:(INN). Brand names: Trajenta, Tradjenta. 893:Linagliptin may cause severe joint pain. 540: 2738:Drugs developed by Eli Lilly and Company 1257:British national formulary : BNF 76 1251: 1249: 1247: 2728:Drugs developed by Boehringer Ingelheim 2697: 1433:U.S. Food and Drug Administration (FDA) 938: 755: 735: 627: 500: 411: 153: 1409:from the original on 25 September 2021 1042:from the original on 27 September 2021 1010:Therapeutic Goods Administration (TGA) 20: 1439:from the original on 13 December 2019 1370:"Linagliptin - Drug Usage Statistics" 1144:from the original on 29 December 2019 976:"Linagliptin, tablet, 5 mg, Trajenta" 845:is not recommended. Linagliptin is a 814:as an initial treatment. It is taken 600: 580: 139: 7: 1560:, and other drugs used in diabetes ( 1072:from the original on 19 January 2022 980:Pharmaceutical Benefits Scheme (PBS) 218: 2530:Glibenclamide (glyburide)/metformin 2510:Dapagliflozin/saxagliptin/metformin 1471:from the original on 3 October 2020 1325:from the original on 3 October 2022 1111:from the original on 15 August 2022 560: 451: 986:from the original on 31 March 2015 14: 2733:Dipeptidyl peptidase-4 inhibitors 1395:"Linagliptin: FDA-Approved Drugs" 1295:from the original on 3 April 2022 1189:from the original on 6 April 2019 915:international nonproprietary name 853:and decreasing the production of 2700: 847:dipeptidyl peptidase-4 inhibitor 666: 660: 343:75–99% (concentration-dependent) 47: 29: 763:Key:LTXREWYXXSTFRX-QGZVFWFLSA-N 1032:"Trajenta Product information" 672: 654: 1: 1210:The Annals of Pharmacotherapy 117:Tradjenta, Trajenta, Trazenta 2346:Alpha-glucosidase inhibitors 1401:Food and Drug Administration 1319:Boehringer Ingelheim Limited 1287:Food and Drug Administration 794:, sold under the brand name 2308:Aldose reductase inhibitors 2769: 2174:GLP1 poly-agonist peptides 644:Chemical and physical data 363:Pharmacologically inactive 353:Minimal (~10% metabolized) 2620:Sitagliptin/ertugliflozin 2615:Sitagliptin/dapagliflozin 2535:Glimepiride/rosiglitazone 2515:Empagliflozin/linagliptin 2505:Dapagliflozin/saxagliptin 2480: 2033:Glibenclamide (glyburide) 1789: 1778: 1586: 1569: 1136:European Medicines Agency 927:Empagliflozin/linagliptin 771: 746: 726: 722:202 °C (396 °F) 402: 28: 2600:Pioglitazone/sitagliptin 2590:Pioglitazone/glimepiride 2580:Phenformin/sulfonylureas 2525:Gemigliptin/rosuvastatin 2495:Cagrilintide/semaglutide 2630:Sitagliptin/simvastatin 2605:Rosiglitazone/metformin 2585:Pioglitazone/alogliptin 2575:Metformin/teneligliptin 2570:Metformin/sulfonylureas 2550:Metformin/ertugliflozin 2520:Empagliflozin/metformin 2500:Dapagliflozin/metformin 2490:Canagliflozin/metformin 2116:GLP-1 receptor agonists 2635:Vildagliptin/metformin 2595:Pioglitazone/metformin 2625:Sitagliptin/metformin 2610:Saxagliptin/metformin 2565:Metformin/repaglinide 2560:Metformin/gemigliptin 2540:Linagliptin/metformin 1345:"The Top 300 of 2020" 1140:. 17 September 2018. 1068:. 27 September 2021. 1006:"AusPAR: Linagliptin" 2555:Metformin/evogliptin 2485:Alogliptin/metformin 1795:Insulin sensitizers 1550:diabetes medication 913:Linagliptin is the 897:Mechanism of action 798:among others, is a 278:(Prescription only) 254:(Prescription only) 25: 2723:Alkyne derivatives 2674:Never to phase III 2545:Metformin/acarbose 1895:Dual PPAR agonists 1764:Never to phase III 1671:Ultralente insulin 1435:. 28 August 2015. 2688: 2687: 2684: 2683: 2647: 2646: 2643: 2642: 2467: 2466: 2295: 2294: 2207: 2206: 2110: 2109: 1953: 1952: 1774: 1773: 1737: 1736: 1681:ultra-long-acting 1605:Insulin glulisine 1222:10.1345/aph.1Q522 1107:. 21 April 2022. 1038:. 25 April 2012. 789: 788: 707:Interactive image 613:CompTox Dashboard 418:-purine-2,6-dione 301: 286: 273: 261: 249: 174: 16:Chemical compound 2760: 2705: 2704: 2703: 2696: 2478: 2374:SGLT2 inhibitors 2304: 2213:DPP-4 inhibitors 2194:(GLP-1/GIP/GCGR) 2170: 1976: 1964: 1800: 1791: 1780: 1689:Insulin degludec 1651:Insulin glargine 1588: 1571: 1542: 1535: 1528: 1519: 1507: 1506: 1504: 1502: 1487: 1481: 1480: 1478: 1476: 1470: 1463: 1455: 1449: 1448: 1446: 1444: 1425: 1419: 1418: 1416: 1414: 1391: 1385: 1384: 1382: 1380: 1366: 1360: 1359: 1357: 1355: 1341: 1335: 1334: 1332: 1330: 1311: 1305: 1304: 1302: 1300: 1277: 1271: 1270: 1253: 1242: 1241: 1205: 1199: 1198: 1196: 1194: 1175: 1154: 1153: 1151: 1149: 1127: 1121: 1120: 1118: 1116: 1097: 1082: 1081: 1079: 1077: 1058: 1052: 1051: 1049: 1047: 1028: 1022: 1021: 1019: 1017: 1002: 996: 995: 993: 991: 972: 966: 965: 963: 961: 951:nctr-crs.fda.gov 943: 903:DPP-4 inhibitors 871:generic medicine 868: 785: 784: 777: 709: 689: 674: 668: 662: 656: 636: 635: 621: 619: 604: 584: 564: 544: 524: 504: 484: 464: 454: 453: 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1131:"Trajenta EPAR" 1129: 1128: 1124: 1114: 1112: 1099: 1098: 1085: 1075: 1073: 1060: 1059: 1055: 1045: 1043: 1030: 1029: 1025: 1015: 1013: 1004: 1003: 999: 989: 987: 974: 973: 969: 959: 957: 945: 944: 940: 935: 923: 911: 899: 891: 881:Linagliptin is 879: 866: 804:type 2 diabetes 780: 778: 775:(what is this?) 772: 767: 764: 759: 754: 753: 742: 739: 734: 733: 712: 687: 677: 671: 665: 659: 639: 629:DTXSID201021653 615: 607: 587: 567: 547: 527: 507: 487: 467: 450: 442: 422: 419: 410: 409: 370: 339:Protein binding 331: 322:Bioavailability 314:Pharmacokinetic 308: 289: 226: 194: 187: 101: 97: 50: 46: 17: 12: 11: 5: 2766: 2764: 2756: 2755: 2750: 2745: 2740: 2735: 2730: 2725: 2715: 2714: 2710: 2709: 2686: 2685: 2682: 2681: 2678: 2677: 2676: 2675: 2672: 2661: 2655: 2649: 2648: 2645: 2644: 2641: 2640: 2638: 2637: 2632: 2627: 2622: 2617: 2612: 2607: 2602: 2597: 2592: 2587: 2582: 2577: 2572: 2567: 2562: 2557: 2552: 2547: 2542: 2537: 2532: 2527: 2522: 2517: 2512: 2507: 2502: 2497: 2492: 2487: 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1853: 1851: 1848: 1846: 1843: 1842: 1840: 1837: 1833: 1829: 1823: 1820: 1818: 1815: 1813: 1810: 1809: 1807: 1805: 1801: 1798: 1796: 1792: 1788: 1781: 1777: 1763: 1761: 1758: 1757: 1755: 1752: 1749: 1746: 1744: 1741: 1740: 1729: 1726: 1725: 1723: 1721: 1720: 1715: 1708: 1704: 1701: 1698: 1694: 1690: 1687: 1686: 1684: 1682: 1678: 1672: 1669: 1667: 1666:Lente insulin 1664: 1662: 1659: 1656: 1655:+lixisenatide 1652: 1649: 1647: 1644: 1643: 1641: 1639: 1635: 1629: 1626: 1625: 1623: 1621: 1617: 1611: 1608: 1606: 1603: 1601: 1598: 1597: 1595: 1593: 1589: 1585: 1581: 1577: 1572: 1568: 1563: 1559: 1555: 1551: 1543: 1538: 1536: 1531: 1529: 1524: 1523: 1520: 1513: 1496: 1492: 1486: 1483: 1467: 1460: 1454: 1451: 1438: 1434: 1430: 1424: 1421: 1408: 1404: 1402: 1396: 1390: 1387: 1375: 1371: 1365: 1362: 1350: 1346: 1340: 1337: 1324: 1320: 1316: 1310: 1307: 1294: 1290: 1288: 1282: 1276: 1273: 1268: 1266:9780857113382 1262: 1258: 1252: 1250: 1248: 1244: 1239: 1235: 1231: 1227: 1223: 1219: 1216:(3): 358–67. 1215: 1211: 1204: 1201: 1188: 1184: 1180: 1174: 1172: 1170: 1168: 1166: 1164: 1162: 1160: 1156: 1143: 1139: 1137: 1132: 1126: 1123: 1110: 1106: 1102: 1096: 1094: 1092: 1090: 1088: 1084: 1071: 1067: 1063: 1057: 1054: 1041: 1037: 1036:Health Canada 1033: 1027: 1024: 1011: 1007: 1001: 998: 985: 982:. July 2012. 981: 977: 971: 968: 956: 952: 948: 942: 939: 932: 928: 925: 924: 920: 918: 916: 908: 906: 904: 896: 894: 888: 886: 884: 876: 874: 872: 862: 860: 856: 852: 848: 844: 843:breastfeeding 840: 836: 832: 828: 824: 819: 817: 813: 812:sulfonylureas 809: 805: 801: 797: 793: 783: 776: 770: 761: 756: 752: 745: 736: 732: 725: 721: 719: 718:Melting point 715: 708: 704: 703: 701: 698: 693: 686: 684: 680: 653: 651: 647: 642: 634: 630: 626: 625: 623: 614: 610: 603: 599: 598: 596: 594: 590: 583: 579: 578: 576: 574: 570: 563: 559: 558: 556: 554: 550: 543: 539: 538: 536: 534: 530: 523: 519: 518: 516: 514: 510: 503: 499: 498: 496: 494: 490: 483: 479: 478: 476: 474: 470: 463: 459: 458: 456: 449: 445: 438: 434: 433: 431: 429: 425: 417: 412: 408: 401: 396: 392: 388: 385: 383: 379: 375: 373: 366: 362: 360: 356: 352: 350: 346: 342: 340: 336: 332: 325: 323: 319: 315: 311: 304: 302: Rx-only 295: 292: 280: 277: 267: 265: 256: 253: 243: 242: 240: 238: 234: 229: 221: 216: 213: 212: 210: 208: 204: 201: 198: 196: 190: 183: 178: 169: 168: 166: 164: 160: 156: 152: 150: 146: 142: 138: 136: 132: 128: 124: 120: 116: 114: 110: 106: 105: 92: 45: 43:Pronunciation 41: 38:Clinical data 36: 32: 27: 19: 2748:Quinazolines 2473:Combinations 2418:Sergliflozin 2287:Vildagliptin 2282:Trelagliptin 2262:Omarigliptin 2251: 2237:Garvagliptin 2164:Taspoglutide 2154:Orforglipron 2149:Lixisenatide 2083:Meglitinides 2038:Glibornuride 2028: 2012:Metahexamide 2007:Glycyclamide 1987: 1940:Cagrilintide 1930:analogs and 1918:Tesaglitazar 1913:Saroglitazar 1908:Muraglitazar 1885:Troglitazone 1870:Pioglitazone 1850:Darglitazone 1784:Non-insulins 1717: 1707:+semaglutide 1697:+liraglutide 1680: 1637: 1620:short-acting 1619: 1591: 1499:. Retrieved 1494: 1485: 1473:. Retrieved 1453: 1441:. Retrieved 1432: 1423: 1413:24 September 1411:. Retrieved 1398: 1389: 1377:. Retrieved 1373: 1364: 1352:. Retrieved 1348: 1339: 1327:. Retrieved 1318: 1309: 1297:. Retrieved 1284: 1275: 1256: 1213: 1209: 1203: 1191:. Retrieved 1182: 1146:. Retrieved 1134: 1125: 1113:. Retrieved 1104: 1074:. Retrieved 1065: 1056: 1044:. Retrieved 1035: 1026: 1014:. Retrieved 1009: 1000: 990:26 September 988:. Retrieved 979: 970: 958:. Retrieved 950: 941: 912: 900: 892: 889:Side effects 880: 877:Medical uses 863: 831:pancreatitis 823:side effects 820: 795: 791: 790: 779:   773:   602:ChEMBL237500 415: 369:Elimination 333:= 1.5 hours) 237:Legal status 231:Legal status 163:License data 18: 2743:Piperidines 2660:from market 2272:Sitagliptin 2267:Saxagliptin 2257:Melogliptin 2252:Linagliptin 2247:Gosogliptin 2242:Gemigliptin 2215:/"gliptins" 2200:(GLP-1/GIP) 2198:Tirzepatide 2192:Retatrutide 2159:Semaglutide 2144:Liraglutide 2134:Dulaglutide 2129:Danuglipron 2124:Albiglutide 2102:Repaglinide 2097:Nateglinide 2092:Mitiglinide 2085:/"glinides" 2068:Glisoxepide 2053:Glimepiride 2043:Glicaramide 2022:Tolbutamide 1997:Carbutamide 1945:Pramlintide 1903:Aleglitazar 1855:Englitazone 1845:Ciglitazone 1750:from market 1661:NPH insulin 1638:long-acting 1592:fast-acting 1501:21 November 1475:10 November 1443:1 September 1148:11 February 873:in the US. 792:Linagliptin 690: g·mol 582:CHEBI:68610 437:668270-12-0 398:Identifiers 359:Metabolites 182:Linagliptin 149:MedlinePlus 122:Other names 113:Trade names 23:Linagliptin 2717:Categories 2449:Benfluorex 2336:Zenarestat 2326:Ranirestat 2321:Fidarestat 2316:Epalrestat 2232:Evogliptin 2227:Anagliptin 2222:Alogliptin 2063:Gliquidone 2048:Gliclazide 2017:Tolazamide 1822:Phenformin 1804:Biguanides 1315:"10 years" 960:22 October 933:References 835:joint pain 827:angioedema 800:medication 695:3D model ( 683:Molar mass 542:3X29ZEJ4R2 513:ChemSpider 473:IUPHAR/BPS 428:CAS Number 407:IUPAC name 349:Metabolism 2753:Xanthines 2670:Phase III 2658:Withdrawn 2459:Imeglimin 2364:Voglibose 2331:Tolrestat 2182:Mazdutide 2139:Exenatide 2058:Glipizide 1817:Metformin 1760:Phase III 1748:Withdrawn 1719:inhalable 1379:7 October 1354:7 October 1329:3 October 1299:3 October 1238:207264493 1183:Drugs.com 1115:3 October 1076:3 October 1046:3 October 883:indicated 839:pregnancy 837:. Use in 808:metformin 796:Tradjenta 382:Excretion 376:~24 hours 371:half-life 193:Routes of 141:Monograph 135:Drugs.com 2707:Medicine 2359:Miglitol 2354:Acarbose 1812:Buformin 1576:Insulins 1554:insulins 1466:Archived 1437:Archived 1407:Archived 1374:ClinCalc 1349:ClinCalc 1323:Archived 1293:Archived 1230:22318932 1187:Archived 1142:Archived 1109:Archived 1105:DailyMed 1070:Archived 1040:Archived 984:Archived 921:See also 859:pancreas 855:glucagon 816:by mouth 782:(verify) 493:DrugBank 462:10096344 207:ATC code 200:By mouth 177:DailyMed 2184:(GLP-1/ 1730:Afrezza 1727:Exubera 1193:6 April 1016:9 April 857:by the 851:insulin 821:Common 688:472.553 650:Formula 522:8271879 502:DB08882 448:PubChem 389:(80%), 293:Rx-only 290:WARNING 262:: 223:) 217: ( 215:A10BH05 179::  155:a611036 125:BI-1356 2693:Portal 2653:WHO-EM 1932:DACRAs 1928:Amylin 1743:WHO-EM 1495:NHS UK 1263:  1236:  1228:  867:  731:SMILES 593:ChEMBL 562:D09566 326:~30% ( 287: 274: 264:℞-only 250: 175:  107: 2442:Other 2300:Other 1548:Oral 1469:(PDF) 1462:(PDF) 1403:(FDA) 1399:U.S. 1289:(FDA) 1285:U.S. 1234:S2CID 1138:(EMA) 1066:(emc) 909:Names 751:InChI 697:JSmol 573:ChEBI 391:urine 387:Feces 2186:GCGR 1836:PPAR 1832:TZDs 1556:and 1503:2022 1477:2016 1445:2015 1415:2021 1381:2022 1356:2022 1331:2022 1301:2022 1261:ISBN 1226:PMID 1195:2019 1150:2020 1117:2022 1078:2022 1048:2022 1018:2023 992:2014 962:2023 841:and 810:and 553:KEGG 533:UNII 482:6318 393:(5%) 316:data 131:AHFS 104:-tin 102:GLIP 1970:ATP 1562:A10 1218:doi 955:FDA 618:EPA 452:CID 330:max 276:POM 220:WHO 100:-ə- 98:LIN 2719:: 2666:: 2031:: 1990:: 1756:: 1695:, 1552:, 1493:. 1431:. 1405:. 1397:. 1372:. 1347:. 1321:. 1317:. 1283:. 1246:^ 1232:. 1224:. 1214:46 1212:. 1181:. 1158:^ 1133:. 1103:. 1086:^ 1064:. 1034:. 1008:. 978:. 953:. 949:. 905:. 861:. 833:, 829:, 818:. 664:28 658:25 298:EU 283:US 270:UK 259:CA 252:S4 246:AU 172:US 2695:: 2188:) 1968:K 1838:) 1709:) 1705:( 1699:) 1691:( 1657:) 1653:( 1578:/ 1564:) 1541:e 1534:t 1527:v 1505:. 1479:. 1447:. 1417:. 1383:. 1358:. 1333:. 1303:. 1269:. 1240:. 1220:: 1197:. 1152:. 1119:. 1080:. 1050:. 1020:. 994:. 964:. 865:1 699:) 676:2 673:O 670:8 667:N 661:H 655:C 620:) 616:( 416:H 328:T 300:: 285:: 272:: 248:: 133:/ 91:/ 88:n 85:ɪ 82:t 79:p 76:ɪ 73:l 70:ɡ 67:ˈ 64:ə 61:n 58:ɪ 55:l 52:ˌ 49:/

Index


/ˌlɪnəˈɡlɪptɪn/
LIN-ə-GLIP-tin
Trade names
AHFS
Drugs.com
Monograph
MedlinePlus
a611036
License data
DailyMed
Linagliptin
Routes of
administration

By mouth
ATC code
A10BH05
WHO
Legal status
S4
℞-only
POM
WARNING
Pharmacokinetic
Bioavailability
Tmax
Protein binding
Metabolism
Metabolites
Elimination half-life
Excretion

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