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    Chemistry

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    Also known as: Glibenclamide, 10238-21-8, Glybenclamide, Glynase, Diabeta, Micronase
    Molecular Formula
    C23H28ClN3O5S
    Molecular Weight
    494.0  g/mol
    InChI Key
    ZNNLBTZKUZBEKO-UHFFFAOYSA-N
    FDA UNII
    SX6K58TVWC
    Glibenclamide
    An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide
    Glyburide is a Sulfonylurea.
    1 2D Structure

    Glibenclamide

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide
    2.1.2 InChI
    InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)
    2.1.3 InChI Key
    ZNNLBTZKUZBEKO-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3
    2.2 Other Identifiers
    2.2.1 UNII
    SX6K58TVWC
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Daonil

    2. Diabeta

    3. Euglucon 5

    4. Euglucon N

    5. Glibenclamide

    6. Glybenclamide

    7. Hb 419

    8. Hb 420

    9. Hb-419

    10. Hb-420

    11. Hb419

    12. Hb420

    13. Maninil

    14. Micronase

    15. Neogluconin

    2.3.2 Depositor-Supplied Synonyms

    1. Glibenclamide

    2. 10238-21-8

    3. Glybenclamide

    4. Glynase

    5. Diabeta

    6. Micronase

    7. Daonil

    8. Euglucon

    9. Maninil

    10. Glybenzcyclamide

    11. Semi-daonil

    12. Apo-glibenclamide

    13. Euglucon 5

    14. Azuglucon

    15. Bastiverit

    16. Benclamin

    17. Betanase

    18. Duraglucon

    19. Euglucan

    20. Euglykon

    21. Glibenil

    22. Glucolon

    23. Orabetic

    24. Prodiabet

    25. Renabetic

    26. Yuglucon

    27. Dibelet

    28. Gilemal

    29. Glibens

    30. Glibil

    31. Glimel

    32. Glimide

    33. Humedia

    34. Libanil

    35. Suraben

    36. Tiabet

    37. Adiab

    38. Melix

    39. Pira

    40. Med-glionil

    41. Glibenclamidum

    42. Glibenclamida

    43. Hb 419

    44. Glibenclamidum [inn-latin]

    45. Glibenclamida [inn-spanish]

    46. 5-chloro-n-(4-(n-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide

    47. Glyburide (glibenclamide)

    48. Hb-419

    49. Ur 606

    50. Cirara

    51. 1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexylurea

    52. 1-(p-(2-(5-chloro-2-methoxybenzamido)ethyl)benzenesulfonyl)-3-cyclohexylurea

    53. Neogluconin

    54. 5-chloro-n-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide

    55. 5-chloro-n-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-2-methoxybenzamide

    56. Glibenclamide [inn]

    57. U 26452

    58. Gewaglucon

    59. Glibenbeta

    60. Glidiabet

    61. Glucobene

    62. Glucohexal

    63. Glucoremed

    64. Hexaglucon

    65. Lederglib

    66. Lisaglucon

    67. Normoglucon

    68. Praeciglucon

    69. Calabren

    70. Cytagon

    71. Euclamin

    72. Glamide

    73. Glibesyn

    74. Glibetic

    75. Gliboral

    76. Glisulin

    77. Glitisol

    78. Glubate

    79. Glucomid

    80. Glucoven

    81. Glycomin

    82. Miglucan

    83. Debtan

    84. Gliban

    85. Gliben

    86. Glibet

    87. Glicem

    88. Gluben

    89. Glyben

    90. Nadib

    91. Sugril

    92. Sx6k58tvwc

    93. Chembl472

    94. Novo-glyburide

    95. Nsc-759618

    96. Glibenclamid Al

    97. 5-chloro-n-[4-(cyclohexylureidosulfonyl)phenethyl]-2-methoxybenzamide

    98. Gen-glybe

    99. Norglicem 5

    100. Betanese 5

    101. N-(4-(2-(5-chloro-2-methoxybenzamido)ethyl)phenylsulfonyl)-n'-cyclohexylurea

    102. Glibenclamid Fabra

    103. 5-chloro-n-[2-(4-{[(cyclohexylcarbamoyl)amino]sulfonyl}phenyl)ethyl]-2-methoxybenzamide

    104. Benzamide, 5-chloro-n-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-2-methoxy-

    105. Mls000069721

    106. Chebi:5441

    107. Glibenclamid Basics

    108. Glibenclamid-cophar

    109. Glibenclamid Heumann

    110. Semi-euglucon

    111. Glibenclamid Genericon

    112. Hemi-daonil

    113. U-26452

    114. Glibenclamid-ratiopharm

    115. U-26,452

    116. 5-chloro-n-(2-{4-[(cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide

    117. Urea, 1-(p-(2-(5-chloro-2-methoxybenzamido)ethyl)benzenesulfonyl)-3-cyclohexyl-

    118. Benzamide, 5-chloro-n-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxy-

    119. Glyburide [usan]

    120. Ncgc00015467-11

    121. Abbenclamide

    122. Diabiphage

    123. Glibadone

    124. Smr000058229

    125. Semi-gliben-puren N

    126. Gbn 5

    127. Cas-10238-21-8

    128. Glibenclamid Riker M.

    129. Glyburide (micronized)

    130. Urea, 1-((p-(2-(chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexyl-

    131. Dsstox_cid_17237

    132. Dsstox_rid_79313

    133. Dsstox_gsid_37237

    134. U-26,45

    135. Micronized Glyburide

    136. Glycron

    137. 1-[[p-[2-(5-chloro-o-anisamido)ethyl]phenyl]sulfonyl]-3-cyclohexylurea

    138. 5-chloro-n-(2-{4-[n-(n-cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide

    139. 5-chloro-n-(4-(n-(cyclohexylcarbamoyl)sulfamoyl)-phenethyl)-2-methoxybenzamide

    140. Glyburide (usp)

    141. Micronase (tn)

    142. 1-{4-[2-(5-chloro-2-methoxybenzamido)ethyl]benzenesulfonyl}-3-cyclohexylurea;1-{4-[2-(5-chloro-2-methoxybenzamido)ethyl]benzenesulfonyl}-3-cyclohexylurea

    143. Diabeta (tn)

    144. Glynase (tn)

    145. Sr-01000000196

    146. Glyburide [usan:usp]

    147. Einecs 233-570-6

    148. Unii-sx6k58tvwc

    149. Brn 2230085

    150. Amglidia

    151. Delmide

    152. 5-chloro-n-(4-[n-(cyclohexylcarbamoyl)sulfamoyl]phenethyl)-2-methoxybenzamide

    153. Glibenclamide,(s)

    154. Gbm

    155. Prestwick_569

    156. Glibenclamide B.p.

    157. Glyburide (diabeta)

    158. Mfcd00056625

    159. Rp-1127

    160. Spectrum_000250

    161. Tocris-0911

    162. Glibenclamide - Bio-x

    163. Glybenzcyclamide, 99%

    164. Glibenclamide; Glyburide

    165. Opera_id_801

    166. Glyburide [mi]

    167. Prestwick0_000316

    168. Prestwick1_000316

    169. Prestwick2_000316

    170. Prestwick3_000316

    171. Spectrum2_001816

    172. Spectrum3_001327

    173. Spectrum4_001199

    174. Spectrum5_001631

    175. Glyburide [vandf]

    176. Lopac-g-0639

    177. Probes1_000431

    178. Probes2_000378

    179. Upcmld-dp006

    180. G 0639

    181. Glibenclamide [jan]

    182. N-p-[2-(5-chloro-2-methoxybenzamido)ethyl]benzenesulfonyl-n'-cyclohexylurea

    183. Glyburide [usp-rs]

    184. Glyburide [who-ip]

    185. Glibenclamide (jp17/inn)

    186. N-(4-(beta-(2-methoxy-5-chlorbenzamido)-aethyl)-benzolsulfonyl)-n'-cyclohexyl-harnstoff

    187. Cbiol_001790

    188. Lopac0_000499

    189. Oprea1_764617

    190. Schembl22009

    191. Bspbio_000312

    192. Bspbio_001351

    193. Bspbio_003053

    194. Kbiogr_000071

    195. Kbiogr_001897

    196. Kbioss_000071

    197. Kbioss_000730

    198. Mls001077262

    199. Bidd:gt0239

    200. Divk1c_000481

    201. Glibenclamide [mart.]

    202. Spectrum2300229

    203. Spbio_001831

    204. Spbio_002531

    205. Glibenclamide [who-dd]

    206. Glibenclamide [who-ip]

    207. Bpbio1_000344

    208. Gtpl2414

    209. Glyburide [orange Book]

    210. Dtxsid0037237

    211. Upcmld-dp006:001

    212. Hms501i03

    213. Kbio1_000481

    214. Kbio2_000071

    215. Kbio2_000730

    216. Kbio2_002639

    217. Kbio2_003298

    218. Kbio2_005207

    219. Kbio2_005866

    220. Kbio3_000141

    221. Kbio3_000142

    222. Kbio3_002273

    223. Glyburide [usp Monograph]

    224. Glybenclamide, >=99% (hplc)

    225. Ninds_000481

    226. Bio1_000076

    227. Bio1_000565

    228. Bio1_001054

    229. Bio2_000071

    230. Bio2_000551

    231. Hms1361d13

    232. Hms1568p14

    233. Hms1791d13

    234. Hms1922l08

    235. Hms1989d13

    236. Hms2089l06

    237. Hms2093p04

    238. Hms2095p14

    239. Hms3259o12

    240. Hms3261d19

    241. Hms3267a15

    242. Hms3402d13

    243. Hms3411f16

    244. Hms3428d15

    245. Hms3651e17

    246. Hms3675f16

    247. Hms3712p14

    248. Pharmakon1600-02300229

    249. Zinc537805

    250. Bcp05327

    251. Glibenclamide [ep Monograph]

    252. Glibenclamide For Peak Identification

    253. Tox21_110158

    254. Tox21_300758

    255. Tox21_500499

    256. Bdbm50012957

    257. Ccg-39618

    258. Glucovance Component Glyburide

    259. Hd 419

    260. Nsc759618

    261. Nsc813214

    262. Stk362992

    263. Glibenclamidum [who-ip Latin]

    264. Glyburide - Cas 10238-21-8

    265. Akos001487495

    266. Tox21_110158_1

    267. Bcp9000729

    268. Cs-1075

    269. Db01016

    270. Ks-5326

    271. Lp00499

    272. Nc00566

    273. Nsc 759618

    274. Nsc-813214

    275. Sb17414

    276. Sdccgsbi-0050483.p004

    277. Glyburide Component Of Glucovance

    278. Idi1_000481

    279. Idi1_033821

    280. Glibenclamide 1.0 Mg/ml In Acetonitrile

    281. Ncgc00015467-01

    282. Ncgc00015467-02

    283. Ncgc00015467-03

    284. Ncgc00015467-04

    285. Ncgc00015467-05

    286. Ncgc00015467-06

    287. Ncgc00015467-07

    288. Ncgc00015467-08

    289. Ncgc00015467-09

    290. Ncgc00015467-10

    291. Ncgc00015467-12

    292. Ncgc00015467-13

    293. Ncgc00015467-14

    294. Ncgc00015467-15

    295. Ncgc00015467-16

    296. Ncgc00015467-17

    297. Ncgc00015467-18

    298. Ncgc00015467-20

    299. Ncgc00015467-21

    300. Ncgc00015467-36

    301. Ncgc00015467-37

    302. Ncgc00016689-01

    303. Ncgc00023447-02

    304. Ncgc00023447-04

    305. Ncgc00023447-05

    306. Ncgc00023447-06

    307. Ncgc00023447-07

    308. Ncgc00023447-08

    309. Ncgc00023447-09

    310. Ncgc00023447-10

    311. Ncgc00023447-11

    312. Ncgc00023447-12

    313. Ncgc00254662-01

    314. Ncgc00261184-01

    315. Bg166164

    316. Hy-15206

    317. Sbi-0050483.p003

    318. Glyburide, Meets Usp Testing Specifications

    319. Ab00051949

    320. Eu-0100499

    321. Ft-0601608

    322. G-150

    323. G0382

    324. Glibenclamide 100 Microg/ml In Acetonitrile

    325. S1716

    326. Sw195828-5

    327. A19539

    328. C07022

    329. D00336

    330. D81733

    331. M01823

    332. Ab00051949-16

    333. Ab00051949-17

    334. Ab00051949_18

    335. Ab00051949_19

    336. Q420626

    337. Sr-01000000196-2

    338. Sr-01000000196-4

    339. Sr-01000000196-5

    340. Sr-01000000196-6

    341. Sr-01000000196-8

    342. W-108874

    343. Brd-k36927236-001-06-0

    344. Brd-k36927236-001-17-7

    345. Z277540138

    346. Glybenclamide, European Pharmacopoeia (ep) Reference Standard

    347. Glyburide, United States Pharmacopeia (usp) Reference Standard

    348. 1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexyl Urea

    349. 5-chloro-n-[4-(3-cyclohexylureidosulfonyl)phenethyl]-2-methoxybenzamide

    350. 5-chloro-n-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide.

    351. 5-chloro-n-[4-({[(cyclohexylamino)carbonyl]amino}sulfonyl)phenethyl]-2-methoxybenzamide

    352. Glibenclamide For Peak Identification, European Pharmacopoeia (ep) Reference Standard

    353. Glyburide (glibenclamide), Pharmaceutical Secondary Standard; Certified Reference Material

    354. N-(4-(.beta.-(2-methoxy-5-chlorbenzamido)-aethyl)-benzolsulfonyl)-n'-cyclohexyl-harnstoff

    355. N1-[4-({[(cyclohexylamino)carbonyl]amino}sulfonyl)phenethyl]-5-chloro-2-methoxybenzamide

    356. 5-chloro-n-(2-[4-(([(cyclohexylamino)carbonyl]amino)sulfonyl)phenyl]ethyl)-2-methoxybenzamide #

    357. 5-chloro-n-[2-[4-[[[(cyclohexylamino)carbonyl]-amino]sulfonyl]phenyl]-ethyl]-2-methoxybenzamide

    358. 5-chloro-n-[2-[4-[[[(cylcohexylamino)carbonyl]amino]sulphonyl]phenyl]ethyl]-2-methoxybenzamide

    2.4 Create Date
    2004-09-16
    3 Chemical and Physical Properties
    Molecular Weight 494.0 g/mol
    Molecular Formula C23H28ClN3O5S
    XLogP34.8
    Hydrogen Bond Donor Count3
    Hydrogen Bond Acceptor Count5
    Rotatable Bond Count8
    Exact Mass493.1438199 g/mol
    Monoisotopic Mass493.1438199 g/mol
    Topological Polar Surface Area122 Ų
    Heavy Atom Count33
    Formal Charge0
    Complexity746
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 8  
    Drug NameDiabeta
    PubMed HealthGlyburide (By mouth)
    Drug ClassesHypoglycemic
    Drug LabelDiaeta (glyburide) is an oral blood-glucose-lowering drug of the sulfonylurea class. It is a white, crystalline compound, formulated as tablets of 1.25 mg, 2.5 mg, and 5 mg strengths for oral administration. Diaeta tablets USP contain the activ...
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength2.5mg; 5mg; 1.25mg
    Market StatusPrescription
    CompanySanofi Aventis Us

    2 of 8  
    Drug NameGlyburide
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength1.5mg; 4.5mg; 6mg; 3mg
    Market StatusPrescription
    CompanyTeva; Hikma; Dava Pharms; Mylan

    3 of 8  
    Drug NameGlyburide
    PubMed HealthGlyburide (By mouth)
    Drug ClassesHypoglycemic
    Drug LabelGlyburide tablets USP contain glyburide, which is an oral blood-glucose-lowering drug of the sulfonylurea class. Glyburide is a white, crystalline compound. The chemical name for glyburide is 1-[[p-[2-(5-chloro-o-anisamido)ethyl]phenyl]-sulfonyl]-3-c...
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength2.5mg; 1.25mg; 5mg
    Market StatusPrescription
    CompanyCorepharma; Teva; Aurobindo Pharma; Heritage Pharms

    4 of 8  
    Drug NameGlynase
    Drug LabelGLYNASE PresTab Tablets contain micronized (smaller particle size) glyburide, which is an oral blood-glucose-lowering drug of the sulfonylurea class. Glyburide is a white, crystalline compound, formulated as GLYNASE PresTab Tablets of 1.5, 3, and 6 m...
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength1.5mg; 6mg; 3mg
    Market StatusPrescription
    CompanyPharmacia And Upjohn

    5 of 8  
    Drug NameGlyburide
    PubMed HealthGlyburide (By mouth)
    Drug ClassesHypoglycemic
    Drug LabelGlyburide tablets USP contain glyburide, which is an oral blood-glucose-lowering drug of the sulfonylurea class. Glyburide is a white, crystalline compound. The chemical name for glyburide is 1-[[p-[2-(5-chloro-o-anisamido)ethyl]phenyl]-sulfonyl]-3-c...
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength2.5mg; 1.25mg; 5mg
    Market StatusPrescription
    CompanyCorepharma; Teva; Aurobindo Pharma; Heritage Pharms

    6 of 8  
    Drug NameGlynase
    Drug LabelGLYNASE PresTab Tablets contain micronized (smaller particle size) glyburide, which is an oral blood-glucose-lowering drug of the sulfonylurea class. Glyburide is a white, crystalline compound, formulated as GLYNASE PresTab Tablets of 1.5, 3, and 6 m...
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength1.5mg; 6mg; 3mg
    Market StatusPrescription
    CompanyPharmacia And Upjohn

    7 of 8  
    Drug NameDiabeta
    PubMed HealthGlyburide (By mouth)
    Drug ClassesHypoglycemic
    Drug LabelDiaeta (glyburide) is an oral blood-glucose-lowering drug of the sulfonylurea class. It is a white, crystalline compound, formulated as tablets of 1.25 mg, 2.5 mg, and 5 mg strengths for oral administration. Diaeta tablets USP contain the activ...
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength2.5mg; 5mg; 1.25mg
    Market StatusPrescription
    CompanySanofi Aventis Us

    8 of 8  
    Drug NameGlyburide
    Active IngredientGlyburide
    Dosage FormTablet
    RouteOral
    Strength1.5mg; 4.5mg; 6mg; 3mg
    Market StatusPrescription
    CompanyTeva; Hikma; Dava Pharms; Mylan

    4.2 Drug Indication

    Glyburide is indicated alone or as part of combination product with metformin, as an adjunct to diet and exercise, to improve glycemic control in adults with type 2 diabetes mellitus.

    Amglidia is indicated for the treatment of neonatal diabetes mellitus, for use in newborns, infants and children.

    Sulphonylureas like Amglidia have been shown to be effective in patients with mutations in the genes coding for the -cell ATP-sensitive potassium channel and chromosome 6q24-related transient neonatal diabetes mellitus.

    Treatment of neonatal diabetes mellitus

    Treatment of large hemispheric infarction

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Glyburide is a second generation sulfonylurea that stimulates insulin secretion through the closure of ATP-sensitive potassium channels on beta cells, raising intracellular potassium and calcium ion concentrations. Glibenclamide has a long duration of action as it is given once daily, and a wide therapeutic index as patients are started at doses as low as 0.75mg but that can increase as high as 10mg or more. Patients taking glyburide should be cautioned regarding an increased risk of cardiovascular mortality as seen with tolbutamide, another sulfonylurea.

    5.2 MeSH Pharmacological Classification

    Hypoglycemic Agents

    Substances which lower blood glucose levels. (See all compounds classified as Hypoglycemic Agents.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    GLYBURIDE
    5.3.2 FDA UNII
    SX6K58TVWC
    5.3.3 Pharmacological Classes
    Sulfonylurea [EPC]; Sulfonylurea Compounds [CS]
    5.4 ATC Code

    A10BB01

    A10BB01

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    A - Alimentary tract and metabolism

    A10 - Drugs used in diabetes

    A10B - Blood glucose lowering drugs, excl. insulins

    A10BB - Sulfonylureas

    A10BB01 - Glibenclamide

    5.5 Absorption, Distribution and Excretion

    Absorption

    Elderly patients taking glyburide reached a Cmax of 211-315ng/mL with a Tmax of 0.9-1.0h, while younger patients reached a Cmax of 144-302ng/mL with a Tmax of 1.3-3.0h. Patients taking glyburide have and AUC of 348ng*h/mL.

    Route of Elimination

    Unlike other sulfonylureas, glyburide is 50% excreted in the urine and 50% in the feces. Glyburide is mainly excreted as the metabolite 4-trans-hydroxyglyburide.

    Volume of Distribution

    Elderly patients have a volume of distribution of 19.3-52.6L, while younger patients have a volume of distribution of 21.5-49.3L.

    Clearance

    Elderly patients have a clearance of 2.70-3.55L/h, while younger patients have a clearance of 2.47-4.11L/h.

    5.6 Metabolism/Metabolites

    Glyburide is metabolized mainly by CYP3A4, followed by CYP2C9, CYP2C19, CYP3A7, and CYP3A5. These enzymes metabolize glyburide to 4-trans-hydroxycyclohexyl glyburide (M1), 4-cis-hydroxycyclohexyl glyburide (M2a), 3-cis-hydroxycyclohexyl glyburide (M2b), 3-trans-hydroxycyclohexyl glyburide (M3), 2-trans-hydroxycyclohexyl glyburide (M4), and ethylhydroxycyclohexyl glyburide (M5). The M1 and M2b metabolites are considered active, along with the parent molecule.

    Glyburide has known human metabolites that include 2-trans-hydroxycyclohexyl glyburide, 3-cis-Hydroxycyclohexyl glyburide, 3-trans-Hydroxycyclohexyl glyburide, and 4-cis-hydroxycyclohexyl glyburide.

    S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560

    5.7 Biological Half-Life

    Elderly patients have a terminal elimination half life of 4.0-13.4h, while younger patients have a terminal elimination half life of 4.0-13.9h.

    5.8 Mechanism of Action

    Glyburide belongs to a class of drugs known as sulfonylureas. These drugs act by closing ATP-sensitive potassium channels on pancreatic beta cells. The ATP-sensitive potassium channels on beta cells are known as sulfonylurea receptor 1 (SUR1). Under low glucose concentrations, SUR1 remains open, allowing for potassium ion efflux to create a -70mV membrane potential. Normally SUR1 closes in response to high glucose concentrations, the membrane potential of the cells becomes less negative, the cell depolarizes, voltage gated calcium channels open, calcium ions enter the cell, and the increased intracellular calcium concentration stimulates the release of insulin containing granules. Glyburide bypasses this process by forcing SUR1 closed and stimulating increased insulin secretion.

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    20-Jan-2021
    30-Aug-2024
    KGS
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    DOSAGE - TABLET;ORAL - 1.25MG

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    DOSAGE - TABLET;ORAL - 1.25MG;250MG **Federal...DOSAGE - TABLET;ORAL - 1.25MG;250MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

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    DOSAGE - TABLET;ORAL - 2.5MG;500MG **Federal ...DOSAGE - TABLET;ORAL - 2.5MG;500MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

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    DOSAGE - TABLET;ORAL - 5MG;500MG **Federal Re...DOSAGE - TABLET;ORAL - 5MG;500MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

    USFDA APPLICATION NUMBER - 21178

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