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Bile acid sequestrant

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Because bile acid sequestrants are not well-absorbed from the gut, they are generally regarded as safe in pregnant women. However, by interfering with vitamin absorption (see below), they could cause vitamin deficiencies that may affect the fetus. So, vitamin supplementation may be considered, with
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ions for bile acids. By doing so, they bind bile acids and sequester them from the enterohepatic circulation. The liver then produces more bile acids to replace those that have been lost. Because the body uses cholesterol to make bile acids, this reduces the level of LDL cholesterol circulating in
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Bile acid sequestrants are large polymeric structures, and they are not significantly absorbed from the gut into the bloodstream. Thus, bile acid sequestrants, along with any bile acids bound to the drug, are excreted via the feces after passage through the gastrointestinal tract.
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In addition to bile acids, bile acid sequestrants may also bind drugs in the GI tract, preventing their absorption into the bloodstream. For this reason, it is generally advised that bile acid sequestrants be spaced several hours apart from other drugs.
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have all been used. Doses may not need to be as high as those previously used for hyperlipidemia. Many patients find them hard to tolerate, as although the diarrhea may improve, bloating and abdominal pain can worsen.
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Heel RC, Brogden RN, Pakes GE, Speight TM, Avery GS (March 1980). "Colestipol: a review of its pharmacological properties and therapeutic efficacy in patients with hypercholesterolaemia".
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As bile acid sequestrants are designed to stay in the gut; in general, they do not have systemic side effects. However, they may cause problems in the
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when used with statins. The bile-acid-binding resins can raise triglycerides modestly (about 5%) and cannot be used if the triglycerides are elevated.
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as an adjunct therapy. By inhibiting the enterohepatic circulation, more L-thyroxine will be lost through defecation, thus lowering body
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Chronic diarrhea may be caused by excess bile salts entering the colon rather than being absorbed at the end of the small intestine (the
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Hashim SA, Vanitallie TB (April 1965). "Cholestyramine resin therapy for hypercholesteremia: clinical and metabolic studies".
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by combining with bile constituents and preventing their reabsorption from the gut. In general, they are classified as
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Hofmann AF, Poley JR (August 1969). "Cholestyramine treatment of diarrhea associated with ileal resection".
156: 109: 59: 54:, although they may be used for purposes other than lowering cholesterol. They are used in the treatment of 2366: 2361: 1328: 1083: 244: 2148: 2457: 2371: 949: 794: 418: 167:, with a number of other gastrointestinal causes, or is commonly a primary, idiopathic condition. The 2412: 2138: 1997: 1088: 1068: 937: 113: 2540: 1784: 1697: 1433: 1219: 998: 825: 285: 124: 51: 1737: 2396: 1842: 1731: 1596: 1455: 909: 490: 390: 75: 164: 139:(another major group of cholesterol-lowering drugs), which are thought to increase the risk of 2391: 2060: 2017: 1915: 1692: 1475: 1465: 1368: 1198: 1154: 1138: 942: 932: 875: 865: 704: 655: 614: 560: 525: 482: 447: 382: 1702: 1525: 1450: 1438: 1363: 1229: 1108: 897: 694: 686: 645: 604: 596: 552: 517: 474: 439: 372: 55: 2276: 2092: 1742: 1687: 1556: 1551: 1390: 1323: 1318: 1204: 1150: 991: 882: 835: 219: 108:, disruption of bile acid reabsorption will decrease cholesterol levels, in particular, 2507: 2233: 2073: 1721: 1621: 1616: 1470: 1460: 1410: 1395: 1385: 1286: 1281: 1271: 1209: 1181: 1133: 1128: 860: 815: 811: 699: 674: 609: 584: 361:"Systematic review: the management of chronic diarrhoea due to bile acid malabsorption" 320: 179: 140: 17: 2534: 1880: 1870: 1653: 1626: 1485: 1303: 1214: 1194: 1190: 1053: 981: 870: 785: 521: 478: 443: 39: 494: 394: 2482: 2158: 2153: 2120: 2111: 2083: 2012: 1963: 1953: 1933: 1928: 1788: 1611: 1530: 1266: 1224: 1058: 1048: 964: 959: 248: 135:. They are occasionally used as an adjunct to the statins as an alternative to the 117: 1169: 650: 633: 267:
appropriate intervals between dosing of the vitamins and bile acid sequestrants.
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Bile acid sequestrants are the principal therapy for bile acid-induced diarrhea.
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test can be used for diagnosis. Bile salt diarrhea can also be a side-effect of
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Wong NN (2001). "Colesevelam: a new bile acid sequestrant".
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Three drugs are members of this class; all are synthetic
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are a group of resins used to bind certain components of
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Beigel F, Teich N, Howaldt S, et al. (June 2014).
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Anatomical Therapeutic Chemical Classification System
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has decreased markedly since the introduction of the
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Some patients complain of the bad taste. 2126: 2116: 1907: 1802: 1776: 1762: 1754: 740: 726: 718: 2443:Magnesium pyridoxal 5-phosphate glutamate 698: 649: 608: 376: 589:Therapeutic Advances in Gastroenterology 359:Wilcox C, Turner J, Green J (May 2014). 215:in patients with chronic liver disease. 344: 323:(generic and various proprietary names) 1727:Pharmacological classification systems 1094:Selective estrogen receptor modulators 104:As bile acids are biosynthesized from 1374:Non-steroidal anti-inflammatory drugs 673:Datta DV, Sherlock S (January 1963). 7: 987:Angiotensin II receptor antagonists 78:. Bile acid sequestrants exchange 25: 1807:Cholesterol absorption inhibitors 1736: 1716: 1715: 583:Walters, JR; Pattni, SS (2010). 522:10.1097/00132580-200101000-00009 479:10.2165/00003495-198019030-00001 444:10.1001/jama.1965.03080170017004 1124:Hypothalamic–pituitary hormones 510:Heart Disease (Hagerstown, Md.) 585:"Managing bile acid diarrhoea" 1: 876:Thrombolytics / fibrinolytics 1587:Wakefulness-promoting agents 651:10.1016/j.crohns.2014.05.009 159:occurs after surgery to the 557:10.1056/NEJM196908212810801 70:Bile acid sequestrants are 2562: 1237:Intravenous immunoglobulin 2491: 1711: 44:enterohepatic circulation 2357:Bempedoic acid/ezetimibe 1978:Niacin and derivatives ( 1292:Topoisomerase inhibitors 976:renin–angiotensin system 970:Calcium channel blockers 601:10.1177/1756283X10377126 365:Aliment. Pharmacol. Ther 232:Clostridioides difficile 74:compounds that serve as 2382:Fenofibrate/simvastatin 2377:Fenofibrate/pravastatin 2352:Amlodipine/atorvastatin 195:Use in other conditions 157:bile acid malabsorption 147:Bile acid malabsorption 123:Use of these agents as 110:low-density lipoprotein 60:bile acid malabsorption 2546:Bile acid sequestrants 2367:Ezetimibe/rosuvastatin 2362:Ezetimibe/atorvastatin 1839:Bile acid sequestrants 1084:Hormonal contraception 1014:Bile acid sequestrants 795:Proton-pump inhibitors 758:gastrointestinal tract 691:10.1136/bmj.1.5325.216 329:(Colestid, Colestipid) 245:gastrointestinal tract 40:gastrointestinal tract 32:bile acid sequestrants 18:Bile acid sequestrants 2458:Omega-3-triglycerides 2372:Ezetimibe/simvastatin 1785:Lipid-lowering agents 155:). This condition of 2413:Alipogene tiparvovec 2139:Aluminium clofibrate 1998:Aluminium nicotinate 1693:Radiopharmaceuticals 1481:Antiparkinson agents 286:fat-soluble vitamins 125:hypolipidemic agents 114:hypercholesterolemia 52:hypolipidemic agents 2149:Choline fenofibrate 1476:Antimigraine agents 1466:Antidementia agents 1369:Anti-inflammatories 1059:Medicated dressings 999:Antihyperlipidemics 826:Diabetes medication 284:They can also bind 76:ion-exchange resins 42:. They disrupt the 2518:Never to phase III 2397:Niacin/simvastatin 2387:Niacin/laropiprant 1329:Immunosuppressants 1199:Antimycobacterials 1155:Antithyroid agents 1139:Mineralocorticoids 943:Cardiac stimulants 933:Cardiac glycosides 925:cardiac therapy / 821:Anti-obesity drugs 2528: 2527: 2392:Niacin/lovastatin 2340: 2339: 2228: 2227: 2106: 2105: 2061:ATP citrate lyase 2018:Nicotinyl alcohol 1916:HMG-CoA reductase 1897: 1896: 1751: 1750: 1654:Ophthalmologicals 1364:Anabolic steroids 1267:Anticancer agents 1230:Ectoparasiticides 950:Antihypertensives 898:Antifibrinolytics 378:10.1111/apt.12684 271:Drug interactions 203:diseases such as 16:(Redirected from 2553: 2277:PCSK9 inhibitors 2127: 2117: 1908: 1803: 1778: 1771: 1764: 1755: 1740: 1719: 1718: 1703:Senotherapeutics 1557:Neuroprotectives 1552:Mood stabilizers 1451:Anti-ADHD agents 1391:Muscle relaxants 1324:Immunostimulants 1319:Immunomodulators 1151:Thyroid hormones 1089:Fertility agents 992:Renin inhibitors 883:Antihemorrhagics 850:forming organs ( 836:Dietary minerals 742: 735: 728: 719: 713: 712: 702: 670: 664: 663: 653: 638:J Crohns Colitis 629: 623: 622: 612: 580: 569: 568: 540: 534: 533: 505: 499: 498: 462: 456: 455: 427: 421: 416: 410: 405: 399: 398: 380: 356: 56:chronic diarrhea 21: 2561: 2560: 2556: 2555: 2554: 2552: 2551: 2550: 2531: 2530: 2529: 2524: 2523: 2508:Clinical trials 2487: 2401: 2336: 2309: 2271: 2234:CETP inhibitors 2224: 2208: 2102: 2093:Dextrothyroxine 2078: 2055: 2022: 1973: 1893: 1833: 1792: 1782: 1752: 1747: 1743:Medicine portal 1707: 1663: 1635: 1630: 1622:Cough medicines 1617:Bronchodilators 1598: 1591: 1471:Antidepressants 1461:Anticonvulsants 1409: 1400: 1396:Bisphosphonates 1386:Corticosteroids 1348: 1335: 1307: 1298: 1282:Spindle poisons 1272:Antimetabolites 1255: 1246: 1168: 1159: 1134:Glucocorticoids 1129:Corticosteroids 1110: 1103: 1070: 1063: 1020: 938:Antiarrhythmics 911: 904: 861:Antithrombotics 849: 840: 816:Antipropulsives 812:Antidiarrhoeals 789: 760: 752: 746: 716: 685:(5325): 216–9. 672: 671: 667: 631: 630: 626: 582: 581: 572: 545:N. Engl. J. 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1269: 1268: 1265: 1264: 1262: 1259: 1253: 1249: 1243: 1240: 1238: 1235: 1231: 1228: 1226: 1225:Anthelmintics 1223: 1221: 1218: 1217: 1216: 1213: 1211: 1208: 1206: 1203: 1200: 1196: 1192: 1189: 1188: 1186: 1183: 1179: 1175: 1171: 1166: 1162: 1156: 1152: 1149: 1147: 1144: 1140: 1137: 1135: 1132: 1131: 1130: 1127: 1125: 1122: 1121: 1119: 1116: 1112: 1106: 1100: 1097: 1095: 1092: 1090: 1087: 1085: 1082: 1081: 1079: 1076: 1072: 1069:genitourinary 1066: 1060: 1057: 1055: 1052: 1050: 1049:Antipruritics 1047: 1045: 1042: 1040: 1037: 1036: 1034: 1031: 1027: 1023: 1015: 1012: 1010: 1007: 1005: 1002: 1001: 1000: 997: 993: 990: 988: 985: 983: 980: 979: 978: 977: 973: 971: 968: 966: 965:Beta blockers 963: 961: 958: 956: 953: 951: 948: 944: 941: 939: 936: 934: 931: 930: 929: 928: 923: 922: 920: 917: 913: 907: 899: 896: 894: 891: 889: 886: 885: 884: 881: 877: 874: 872: 869: 867: 866:Antiplatelets 864: 863: 862: 859: 858: 856: 853: 847: 843: 837: 834: 832: 829: 827: 824: 822: 819: 817: 813: 810: 808: 805: 803: 800: 796: 793: 791: 784: 782: 779: 778: 777: 774: 773: 771: 768: 764: 759: 755: 751: 743: 738: 736: 731: 729: 724: 723: 720: 710: 706: 701: 696: 692: 688: 684: 680: 676: 669: 666: 661: 657: 652: 647: 643: 639: 635: 628: 625: 620: 616: 611: 606: 602: 598: 595:(6): 349–57. 594: 590: 586: 579: 577: 575: 571: 566: 562: 558: 554: 550: 546: 539: 536: 531: 527: 523: 519: 515: 511: 504: 501: 496: 492: 488: 484: 480: 476: 473:(3): 161–80. 472: 468: 461: 458: 453: 449: 445: 441: 437: 433: 426: 423: 420: 415: 412: 409: 404: 401: 396: 392: 388: 384: 379: 374: 371:(9): 923–39. 370: 366: 362: 355: 353: 351: 349: 345: 339: 334: 331: 328: 325: 322: 319: 318: 317: 315: 307: 305: 303: 299: 295: 291: 287: 279: 277: 270: 268: 264: 262: 258: 254: 250: 246: 238: 236: 234: 233: 227: 225: 221: 216: 214: 210: 206: 202: 194: 192: 189: 185: 181: 176: 174: 170: 166: 162: 158: 154: 146: 144: 142: 138: 134: 130: 126: 121: 119: 115: 111: 107: 99: 94: 92: 88: 85: 81: 77: 73: 65: 63: 61: 57: 53: 49: 45: 41: 37: 33: 27:Class of drug 19: 2483:Volanesorsen 2345:Combinations 2317:inhibitors ( 2159:Clinofibrate 2154:Ciprofibrate 2063:inhibitors ( 2030:inhibitors ( 2013:Nicofuranose 1964:Rosuvastatin 1954:Pitavastatin 1934:Cerivastatin 1929:Atorvastatin 1838: 1526:Psychedelics 1496:Aphrodisiacs 1170:infestations 1146:Sex hormones 1099:Sex hormones 1044:Cicatrizants 1013: 974: 960:Vasodilators 927:antianginals 924: 776:stomach acid 775: 682: 678: 668: 641: 637: 627: 592: 588: 548: 544: 538: 516:(1): 63–70. 513: 509: 503: 470: 466: 460: 435: 431: 425: 414: 403: 368: 364: 311: 283: 274: 265: 249:constipation 242: 239:Side effects 230: 228: 217: 198: 177: 150: 122: 118:dyslipidemia 103: 95:Medical uses 89: 69: 31: 29: 2504:from market 2463:Policosanol 2438:Lapaquistat 2418:Azacosterol 2295:Bococizumab 2267:Torcetrapib 2262:Obicetrapib 2257:Evacetrapib 2252:Dalcetrapib 2247:Anacetrapib 2199:Ronifibrate 2194:Pemafibrate 2184:Gemfibrozil 2179:Fenofibrate 2144:Bezafibrate 2051:Mitratapide 2041:Dirlotapide 1969:Simvastatin 1959:Pravastatin 1939:Fluvastatin 1889:glucomannan 1856:Colesevelam 1659:Otologicals 1631:antagonists 1597:respiratory 1572:Orexigenics 1567:Neurotoxins 1516:Euphoriants 1506:Entactogens 1501:Depressants 1491:Anxiolytics 1429:Anesthetics 1205:Antifungals 802:Antiemetics 790:antagonists 333:Colesevelam 199:In chronic 188:colesevelam 173:gallbladder 106:cholesterol 87:the blood. 2541:Hepatology 2535:Categories 2478:Triparanol 2453:Mipomersen 2433:Darapladib 2428:Benfluorex 2423:Azalanstat 2332:Evinacumab 2305:Inclisiran 2300:Evolocumab 2290:Alirocumab 2204:Simfibrate 2174:Etofibrate 2169:Clofibride 2164:Clofibrate 2098:Resmetirom 2046:Lomitapide 2008:Niceritrol 1949:Mevastatin 1944:Lovastatin 1866:Colestipol 1861:Colestilan 1824:Hyzetimibe 1582:Stimulants 1562:Nootropics 1536:Deliriants 1511:Entheogens 1446:Anorectics 1424:Analgesics 1277:Alkylating 1210:Antivirals 1165:infections 1039:Emollients 893:Coagulants 763:metabolism 438:: 289–93. 340:References 327:Colestipol 288:, such as 261:flatulence 247:, such as 184:colestipol 48:bile acids 2514:Phase III 2502:Withdrawn 2189:Nafenopin 1876:Colextran 1829:SCH-48461 1819:Ezetimibe 1732:ATC codes 1698:Dressings 1683:Antidotes 1547:Sedatives 1543:Hypnotics 1252:malignant 1109:endocrine 955:Diuretics 888:Platelets 848:and blood 807:Laxatives 314:polymeric 302:vitamin K 298:vitamin E 294:vitamin D 290:vitamin A 224:thyroxine 205:cirrhosis 175:removal. 72:polymeric 66:Mechanism 2473:Tiadenol 2468:Probucol 2448:Meglutol 2220:GW501516 2131:Fibrates 1993:Acipimox 1885:psyllium 1883:such as 1798:GI tract 1577:Serenics 1242:Vaccines 1009:Fibrates 831:Vitamins 781:Antacids 709:14025214 679:Br Med J 660:24953836 619:21180614 530:11975771 495:27745975 452:14271976 395:12016216 387:24602022 316:resins: 308:Examples 280:Vitamins 257:bloating 253:diarrhea 226:levels. 213:pruritus 209:pruritus 137:fibrates 84:chloride 82:such as 2315:ANGPTL3 1912:Statins 1434:General 1341:muscles 1310:L03–L04 1306:disease 1258:L01–L02 1254:disease 1004:Statins 700:2123703 610:3002596 565:4894463 487:6988203 129:statins 58:due to 38:in the 2497:WHO-EM 2213:Others 2086:(VLDL) 2003:Niacin 1843:resins 1811:NPC1L1 1741:  1720:  1668:other 1599:system 1351:joints 1304:immune 1111:system 1071:system 912:system 707:  697:  658:  617:  607:  563:  528:  493:  485:  450:  393:  385:  300:, and 259:, and 169:SeHCAT 80:anions 2406:Other 2123:(LDL) 1903:Liver 1722:Drugs 1439:Local 1406:brain 1345:bones 846:blood 491:S2CID 467:Drugs 391:S2CID 201:liver 163:, in 161:ileum 153:ileum 2032:VLDL 2028:MTTP 1982:and 1887:and 1349:and 1026:skin 705:PMID 656:PMID 615:PMID 561:PMID 526:PMID 483:PMID 448:PMID 432:JAMA 383:PMID 186:and 116:and 36:bile 30:The 2323:HDL 2319:LDL 2281:LDL 2238:HDL 2065:LDL 1984:LDL 1980:HDL 1920:LDL 1847:LDL 1789:C10 1670:ATC 1408:and 1167:and 695:PMC 687:doi 646:doi 605:PMC 597:doi 553:doi 549:281 518:doi 475:doi 440:doi 436:192 373:doi 133:LDL 46:of 2537:: 2510:: 1918:, 1809:, 1545:/ 1343:, 1193:: 1182:QI 1180:, 1176:, 1153:/ 814:/ 761:/ 703:. 693:. 681:. 677:. 654:. 640:. 636:. 613:. 603:. 591:. 587:. 573:^ 559:. 547:. 524:. 512:. 489:. 481:. 471:19 469:. 446:. 434:. 389:. 381:. 369:39 367:. 363:. 347:^ 296:, 292:, 255:, 251:, 182:, 120:. 62:. 2325:) 2321:/ 2283:) 2279:( 2240:) 2236:( 2067:) 2034:) 1986:) 1922:) 1914:( 1849:) 1845:( 1841:/ 1791:) 1787:( 1777:e 1770:t 1763:v 1676:) 1674:V 1672:( 1647:) 1645:S 1643:( 1629:1 1627:H 1605:) 1603:R 1601:( 1417:) 1415:N 1413:( 1357:) 1355:M 1353:( 1347:, 1312:) 1308:( 1260:) 1256:( 1201:) 1197:( 1184:) 1178:P 1174:J 1172:( 1117:) 1115:H 1113:( 1077:) 1075:G 1073:( 1032:) 1030:D 1028:( 918:) 916:C 914:( 854:) 852:B 788:2 786:H 769:) 767:A 765:( 741:e 734:t 727:v 711:. 689:: 683:1 662:. 648:: 642:8 621:. 599:: 593:3 567:. 555:: 532:. 520:: 514:3 497:. 477:: 454:. 442:: 397:. 375:: 20:)

Index

Bile acid sequestrants
bile
gastrointestinal tract
enterohepatic circulation
bile acids
hypolipidemic agents
chronic diarrhea
bile acid malabsorption
polymeric
ion-exchange resins
anions
chloride
cholesterol
low-density lipoprotein
hypercholesterolemia
dyslipidemia
hypolipidemic agents
statins
LDL
fibrates
rhabdomyolysis
ileum
bile acid malabsorption
ileum
Crohn's disease
SeHCAT
gallbladder
Cholestyramine
colestipol
colesevelam

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