Knowledge (XXG)

Leprostatic agent

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Sulfones, such as dapsone and sulfoxone (Diasone), are well absorbed orally and are widely distributed throughout body fluids and tissues. Peak concentrations of dapsone are reached within 1 to 3 hours of oral administration and have a half-life of 21 to 44 hours; about 50% of administered dapsone is
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and are used only in the treatment of leprosy. Dapsone (Avlosulfon) is the most widely used sulfone for the long-term therapy of leprosy. Although the sulfones are highly effective against most strains of M. leprae, a small number of organisms, especially those found in lepromatous leprosy patients,
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is characterized by depressed cell-mediated immunity, numerous bacilli within the tissues, no granulomas, and a negative skin test for lepromin. Within these two extremes are the patients with an intermediate or borderline form of leprosy who show a variable lepromin reaction and few bacilli; they
253:. The sulfones tend to remain in the skin, muscle, kidney, and liver up to 3 weeks after therapy is stopped. The concentration in inflamed skin is 10 to 15 times higher than that found in normal skin. The sulfones are retained in the circulation for a long time (12–35 days) because of 105:
cannot be grown on routine laboratory culture media, so drug sensitivity testing in vitro is not possible. Growth and drug susceptibility testing are done by injecting into animal models. One description of a clinical picture that results from
376:. The most disturbing adverse reaction to clofazimine is a red-brown discoloration of the skin, especially in light-skinned persons. A rare but serious adverse reaction is acute abdominal pain significant enough to warrant exploratory 99:. Host defenses are crucial in determining the patient's response to the disease, the clinical presentation, and the bacillary load. These factors also influence the length of therapy and the risk of adverse reactions to medication. 203:
because such a regimen has proven to be more effective, delays the emergence of resistance, prevents relapse, and shortens the duration of therapy. Established agents used in the treatment of leprosy are
288:. Acedapsone is a derivative of dapsone that has little activity against M. leprae but is converted to an active dapsone metabolite. It is a long-acting intramuscular repository form of dapsone with a 245:
are less susceptible and can persist for many years, resulting in relapse. Before the introduction of current multidrug regimens, resistance rates were as high as 20% with dapsone monotherapy.
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DNA binding. Its oral absorption is quite variable, with 9 to 70% of the drug eliminated in the feces. Clofazimine achieves significant concentrations in tissues, including the
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are weakly bacteriocidal against M. leprae and can be used as alternatives to clofazimine in the treatment of MDR leprosy. Both cause GI intolerance and are expensive.
216:. Treatment of tuberculoid leprosy is continued for at least 1 to 2 years, while patients with lepromatous leprosy are generally treated for 5 years. In addition to 1480: 364:
Clofazimine is given to treat sulfone-resistant leprosy or to patients who are intolerant to sulfones. It also exerts an antiinflammatory effect and prevents
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respond well to clofazimine. It also has some activity against M. tuberculosis and can be used as last resort therapy for the treatment of
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deficiency. Within a few weeks of therapy some patients may develop acute skin lesions described as sulfone syndrome or dapsone
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dye that has some activity against M. leprae. Its precise mechanism of action is unknown but may involve
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of 46 days. It may prove useful in leprosy patients who cannot tolerate long-term oral dapsone therapy.
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Current recommendations for the treatment of leprosy suggest multidrug regimens rather than
273:, is used in the treatment of both multibacillary and paucibacillary M. leprae infections. 1837: 1828: 1496: 1441: 1310: 1305: 1144: 1077: 1072: 958: 904: 745: 636: 589: 393: 354: 2054: 1979: 1723: 1573: 1475: 1375: 1370: 1224: 1214: 1164: 1149: 1139: 1040: 1035: 1025: 963: 935: 887: 882: 614: 569: 565: 331: 250: 241: 192: 2081: 1913: 1900: 1891: 1805: 1751: 1407: 1380: 1239: 1057: 968: 948: 944: 807: 735: 624: 539: 431: 412: 350: 254: 361:
of 70 days. It is primarily excreted in bile, with less than 1% excretion in urine.
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is a drug that interferes with proliferation of the bacterium that causes
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support, rehabilitation, and surgical repair of any disfiguration.
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in the liver, and 70 to 80% of drug is excreted in the urine as
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may progress to either tuberculoid or lepromatous leprosy.
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Dapsone is also used in the treatment and prevention of
265:. Dapsone, combined with other antileprosy agents like 432:
Definition: leprostatic from Online Medical Dictionary
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Anatomical Therapeutic Chemical Classification System
2002: 1926: 1861: 1827: 1804: 1795: 1773: 1750: 1722: 1713: 1681: 1653: 1606: 1567: 1558: 1421: 1393: 1349: 1158: 1093: 1056: 1004: 917: 861: 821: 778: 662: 598: 510: 2025:Isoniazid/pyridoxine/sulfamethoxazole/trimethoprim 93:Leprosy is a chronic infectious disease caused by 284:patients who are allergic to or intolerant of 1523: 487: 38:The following agents are leprostatic agents: 8: 2015:Ethambutol/isoniazid/pyrazinamide/rifampicin 502:Major chemical drug groups – based upon the 1801: 1719: 1564: 1530: 1516: 1508: 494: 480: 472: 445:at the U.S. National Library of Medicine 232:The sulfones are structural analogues of 384:. Other infrequent side effects include 318:. Some rare side effects include fever, 424: 1481:Pharmacological classification systems 848:Selective estrogen receptor modulators 1128:Non-steroidal anti-inflammatory drugs 257:drug recirculation. The sulfones are 122:formation, and a relative paucity of 7: 741:Angiotensin II receptor antagonists 236:and are competitive inhibitors of 25: 2030:Rifampicin/isoniazid/pyrazinamide 312:glucose-6-phosphate dehydrogenase 1490: 1470: 1469: 2020:Ethambutol/isoniazid/rifampicin 878:Hypothalamic–pituitary hormones 278:Pneumocystis carinii pneumonia 1: 630:Thrombolytics / fibrinolytics 404:Ethionamide and Prothionamide 295:The sulfones can produce non- 286:trimethoprim–sulfamethoxazole 220:, patients with leprosy need 1341:Wakefulness-promoting agents 1914:Thioacetazone (amithiozone) 1715:Protein synthesis inhibitor 138:Kinds of antileprotic drugs 110:is characterized by intact 2109: 991:Intravenous immunoglobulin 2038: 1465: 366:erythema nodosum leprosum 1797:Cell envelope antibiotic 1683:Topoisomerase inhibitors 1046:Topoisomerase inhibitors 730:renin–angiotensin system 724:Calcium channel blockers 447:Medical Subject Headings 240:synthesis. Sulfones are 1775:Polypeptide antibiotics 1667:Calcium aminosalicylate 1672:Sodium aminosalicylate 1560:Nucleic acid inhibitor 1543:tuberculosis treatment 838:Hormonal contraception 768:Bile acid sequestrants 549:Proton-pump inhibitors 512:gastrointestinal tract 370:Mycobacterium ulcerans 306:, and sometimes acute 129:At the other extreme, 112:cell-mediated immunity 58:desoxyfructo-serotonin 1842:arabinosyltransferase 1662:4-Aminosalicylic acid 2010:Ethambutol/isoniazid 1447:Radiopharmaceuticals 1235:Antiparkinson agents 228:Dapsone and Sulfones 183:Other antibiotics - 96:Mycobacterium leprae 1878:synth. inhibition: 1230:Antimigraine agents 1220:Antidementia agents 1123:Anti-inflammatories 813:Medicated dressings 753:Antihyperlipidemics 580:Diabetes medication 459:MeSH list of agents 131:lepromatous leprosy 108:tuberculoid leprosy 2093:Antileprotic drugs 2065:Never to phase III 1547:leprostatic agents 1539:Antimycobacterials 1083:Immunosuppressants 953:Antimycobacterials 909:Antithyroid agents 893:Mineralocorticoids 697:Cardiac stimulants 687:Cardiac glycosides 679:cardiac therapy / 575:Anti-obesity drugs 443:Leprostatic+agents 386:splenic infarction 310:in persons with a 18:Leprostatic agents 2075: 2074: 1922: 1921: 1912:Others/unsorted: 1791: 1790: 1709: 1708: 1505: 1504: 1408:Ophthalmologicals 1118:Anabolic steroids 1021:Anticancer agents 984:Ectoparasiticides 704:Antihypertensives 652:Antifibrinolytics 398:upper GI bleeding 390:bowel obstruction 304:methemoglobinemia 29:leprostatic agent 16:(Redirected from 2100: 1802: 1720: 1565: 1532: 1525: 1518: 1509: 1494: 1473: 1472: 1457:Senotherapeutics 1311:Neuroprotectives 1306:Mood stabilizers 1205:Anti-ADHD agents 1145:Muscle relaxants 1078:Immunostimulants 1073:Immunomodulators 905:Thyroid hormones 843:Fertility agents 746:Renin inhibitors 637:Antihemorrhagics 604:forming organs ( 590:Dietary minerals 496: 489: 482: 473: 466: 456: 450: 440: 434: 429: 374:MDR tuberculosis 359:plasma half-life 355:phagocytic cells 308:hemolytic anemia 21: 2108: 2107: 2103: 2102: 2101: 2099: 2098: 2097: 2078: 2077: 2076: 2071: 2070: 2055:Clinical trials 2034: 1998: 1918: 1857: 1838:Ethylenediamine 1829:Arabinogalactan 1823: 1787: 1769: 1746: 1724:Aminoglycosides 1705: 1686: 1677: 1649: 1602: 1572: 1554: 1536: 1506: 1501: 1497:Medicine portal 1461: 1417: 1389: 1384: 1376:Cough medicines 1371:Bronchodilators 1352: 1345: 1225:Antidepressants 1215:Anticonvulsants 1163: 1154: 1150:Bisphosphonates 1140:Corticosteroids 1102: 1089: 1061: 1052: 1036:Spindle poisons 1026:Antimetabolites 1009: 1000: 922: 913: 888:Glucocorticoids 883:Corticosteroids 864: 857: 824: 817: 774: 692:Antiarrhythmics 665: 658: 615:Antithrombotics 603: 594: 570:Antipropulsives 566:Antidiarrhoeals 543: 514: 506: 500: 470: 469: 457: 453: 441: 437: 430: 426: 421: 406: 394:paralytic ileus 340: 230: 140: 118:skin reaction, 23: 22: 15: 12: 11: 5: 2106: 2104: 2096: 2095: 2090: 2080: 2079: 2073: 2072: 2069: 2068: 2067: 2066: 2063: 2052: 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716: 711: 706: 701: 700: 699: 694: 689: 675: 673: 664:cardiovascular 660: 659: 657: 656: 655: 654: 649: 644: 634: 633: 632: 627: 625:Anticoagulants 622: 611: 609: 596: 595: 593: 592: 587: 582: 577: 572: 563: 558: 553: 552: 551: 546: 541: 537: 526: 524: 508: 507: 501: 499: 498: 491: 484: 476: 468: 467: 451: 435: 423: 422: 420: 417: 405: 402: 339: 336: 332:hepatotoxicity 251:serum proteins 242:bacteriostatic 229: 226: 197: 196: 193:Clarithromycin 181: 175: 164:Antitubercular 161: 151: 139: 136: 91: 90: 85: 80: 75: 70: 65: 60: 55: 50: 45: 24: 14: 13: 10: 9: 6: 4: 3: 2: 2105: 2094: 2091: 2089: 2086: 2085: 2083: 2064: 2062: 2059: 2058: 2056: 2053: 2050: 2047: 2045: 2042: 2041: 2037: 2031: 2028: 2026: 2023: 2021: 2018: 2016: 2013: 2011: 2008: 2007: 2005: 2001: 1994: 1993: 1988: 1987: 1982: 1981: 1977: 1975: 1972: 1969: 1965: 1964: 1960: 1957: 1953: 1949: 1948: 1944: 1941: 1937: 1936: 1932: 1931: 1929: 1927:Other/unknown 1925: 1915: 1911: 1910: 1907: 1904: 1902: 1901:Prothionamide 1899: 1897: 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1372: 1369: 1367: 1366:Decongestants 1364: 1363: 1361: 1358: 1354: 1348: 1342: 1339: 1337: 1334: 1332: 1329: 1327: 1324: 1322: 1319: 1317: 1314: 1312: 1309: 1307: 1304: 1302: 1298: 1295: 1291: 1288: 1286: 1285:Dissociatives 1283: 1281: 1278: 1277: 1276: 1275:Hallucinogens 1273: 1271: 1268: 1266: 1263: 1261: 1258: 1256: 1253: 1251: 1248: 1246: 1243: 1241: 1238: 1236: 1233: 1231: 1228: 1226: 1223: 1221: 1218: 1216: 1213: 1211: 1208: 1206: 1203: 1201: 1198: 1194: 1191: 1189: 1186: 1185: 1184: 1181: 1179: 1176: 1175: 1173: 1170: 1166: 1161: 1157: 1151: 1148: 1146: 1143: 1141: 1138: 1136: 1133: 1129: 1126: 1125: 1124: 1121: 1119: 1116: 1115: 1113: 1110: 1106: 1100: 1096: 1092: 1084: 1081: 1079: 1076: 1075: 1074: 1071: 1070: 1068: 1065: 1059: 1055: 1047: 1044: 1042: 1039: 1037: 1034: 1032: 1029: 1027: 1024: 1023: 1022: 1019: 1018: 1016: 1013: 1007: 1003: 997: 994: 992: 989: 985: 982: 980: 979:Anthelmintics 977: 975: 972: 971: 970: 967: 965: 962: 960: 957: 954: 950: 946: 943: 942: 940: 937: 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375: 371: 367: 362: 360: 356: 352: 351:mycobacterial 348: 344: 337: 335: 333: 329: 326:, reversible 325: 321: 317: 313: 309: 305: 301: 298: 293: 291: 287: 283: 279: 274: 272: 268: 264: 260: 256: 255:hepatobiliary 252: 246: 243: 239: 235: 227: 225: 223: 219: 215: 211: 207: 202: 194: 190: 186: 182: 179: 176: 173: 169: 165: 162: 159: 156:derivative - 155: 152: 149: 145: 142: 141: 137: 135: 132: 127: 125: 121: 117: 114:, a positive 113: 109: 104: 100: 98: 97: 89: 86: 84: 81: 79: 76: 74: 71: 69: 66: 64: 61: 59: 56: 54: 51: 49: 46: 44: 41: 40: 39: 36: 34: 30: 19: 2003:Combinations 1990: 1984: 1978: 1961: 1952:Pyrazinamide 1945: 1933: 1885:Methaniazide 1876:mycolic acid 1863:Mycolic acid 1742:Streptomycin 1701:Moxifloxacin 1696:Gatifloxacin 1660: 1546: 1541:, including 1280:Psychedelics 1250:Aphrodisiacs 924:infestations 900:Sex hormones 853:Sex hormones 798:Cicatrizants 728: 714:Vasodilators 681:antianginals 678: 530:stomach acid 529: 461: 454: 438: 427: 407: 363: 347:bactericidal 345:is a weakly 341: 294: 275: 247: 231: 222:psychosocial 218:chemotherapy 198: 128: 102: 101: 94: 92: 37: 28: 26: 2051:from market 1974:Bedaquiline 1940:Clofazimine 1906:Thiocarlide 1896:Ethionamide 1844:inhibitor: 1819:Cycloserine 1783:Capreomycin 1752:Oxazolidone 1640:Solasulfone 1608:Antifolates 1593:Rifapentine 1413:Otologicals 1385:antagonists 1351:respiratory 1326:Orexigenics 1321:Neurotoxins 1270:Euphoriants 1260:Entactogens 1255:Depressants 1245:Anxiolytics 1183:Anesthetics 959:Antifungals 556:Antiemetics 544:antagonists 409:Ethionamide 382:laparoscopy 357:; it has a 343:Clofazimine 338:Clofazimine 324:paresthesia 271:clofazimine 263:metabolites 210:clofazimine 201:monotherapy 189:Minocycline 172:Ethionamide 158:Clofazimine 88:thalidomide 78:rifapentine 68:ethionamide 48:clofazimine 2082:Categories 1992:Pretomanid 1968:Terizidone 1956:Morinamide 1872:Hydrazides 1846:Ethambutol 1817:analogue: 1688:quinolones 1625:Acedapsone 1583:Rifampicin 1569:Rifamycins 1336:Stimulants 1316:Nootropics 1290:Deliriants 1265:Entheogens 1200:Anorectics 1178:Analgesics 1031:Alkylating 964:Antivirals 919:infections 793:Emollients 647:Coagulants 517:metabolism 419:References 378:laparotomy 328:neuropathy 316:dermatitis 267:rifampicin 259:acetylated 238:folic acid 214:rifampicin 168:Rifampicin 83:sulfameter 73:rifampicin 43:acedapsone 2061:Phase III 2049:Withdrawn 1986:Delamanid 1963:Isoxazole 1935:Phenazine 1880:Isoniazid 1765:Sutezolid 1760:Linezolid 1737:Kanamycin 1645:Sulfoxone 1598:Rifalazil 1588:Rifabutin 1576:inhibitor 1486:ATC codes 1452:Dressings 1437:Antidotes 1301:Sedatives 1297:Hypnotics 1006:malignant 863:endocrine 709:Diuretics 642:Platelets 602:and blood 561:Laxatives 297:hemolytic 290:half-life 249:bound to 185:Ofloxacin 178:Solapsone 154:Phenazine 120:granuloma 103:M. leprae 1947:Pyrazine 1732:Amikacin 1630:Diucifon 1331:Serenics 996:Vaccines 763:Fibrates 585:Vitamins 535:Antacids 463:82007917 320:pruritus 166:drugs - 116:lepromin 63:diucifon 2088:Leprosy 1815:Alanine 1620:Dapsone 1188:General 1095:muscles 1064:L03–L04 1060:disease 1012:L01–L02 1008:disease 758:Statins 206:dapsone 148:Dapsone 144:Sulfone 124:bacilli 53:dapsone 33:leprosy 2044:WHO-EM 1635:Promin 1495:  1474:  1422:other 1353:system 1105:joints 1058:immune 865:system 825:system 666:system 449:(MeSH) 396:, and 330:, and 300:anemia 212:, and 150:(DDS), 1865:layer 1853:SQ109 1831:layer 1808:layer 1476:Drugs 1193:Local 1160:brain 1099:bones 600:blood 1545:and 1103:and 780:skin 411:and 282:AIDS 269:and 234:PABA 1654:ASA 1612:DSI 1551:J04 1424:ATC 1162:and 921:and 380:or 280:in 2084:: 2057:: 1989:, 1954:, 1894:: 1299:/ 1097:, 947:: 936:QI 934:, 930:, 907:/ 568:/ 515:/ 400:. 392:, 388:, 334:. 322:, 302:, 208:, 191:, 187:, 170:, 146:- 126:. 35:. 27:A 1995:) 1983:( 1970:) 1966:( 1958:) 1950:( 1942:) 1938:( 1874:/ 1840:/ 1685:/ 1674:) 1665:( 1610:/ 1571:/ 1553:) 1549:( 1531:e 1524:t 1517:v 1430:) 1428:V 1426:( 1401:) 1399:S 1397:( 1383:1 1381:H 1359:) 1357:R 1355:( 1171:) 1169:N 1167:( 1111:) 1109:M 1107:( 1101:, 1066:) 1062:( 1014:) 1010:( 955:) 951:( 938:) 932:P 928:J 926:( 871:) 869:H 867:( 831:) 829:G 827:( 786:) 784:D 782:( 672:) 670:C 668:( 608:) 606:B 542:2 540:H 523:) 521:A 519:( 495:e 488:t 481:v 195:, 180:, 174:, 160:, 20:)

Index

Leprostatic agents
leprosy
acedapsone
clofazimine
dapsone
desoxyfructo-serotonin
diucifon
ethionamide
rifampicin
rifapentine
sulfameter
thalidomide
Mycobacterium leprae
tuberculoid leprosy
cell-mediated immunity
lepromin
granuloma
bacilli
lepromatous leprosy
Sulfone
Dapsone
Phenazine
Clofazimine
Antitubercular
Rifampicin
Ethionamide
Solapsone
Ofloxacin
Minocycline
Clarithromycin

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