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Chemistry

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Also known as: 637-07-0, Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, Ethyl clofibrate, Atromid, Clofibratum, Atromid-s
Molecular Formula
C12H15ClO3
Molecular Weight
242.70  g/mol
InChI Key
KNHUKKLJHYUCFP-UHFFFAOYSA-N
FDA UNII
HPN91K7FU3

Clofibrate
A fibric acid derivative used in the treatment of HYPERLIPOPROTEINEMIA TYPE III and severe HYPERTRIGLYCERIDEMIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)
1 2D Structure

Clofibrate

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
ethyl 2-(4-chlorophenoxy)-2-methylpropanoate
2.1.2 InChI
InChI=1S/C12H15ClO3/c1-4-15-11(14)12(2,3)16-10-7-5-9(13)6-8-10/h5-8H,4H2,1-3H3
2.1.3 InChI Key
KNHUKKLJHYUCFP-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CCOC(=O)C(C)(C)OC1=CC=C(C=C1)Cl
2.2 Other Identifiers
2.2.1 UNII
HPN91K7FU3
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Athromidin

2. Atromid

3. Atromid S

4. Chlorophenoxyisobutyrate, Ethyl

5. Clofibric Acid, Ethyl Ester

6. Ethyl Chlorophenoxyisobutyrate

7. Miscleron

8. Miskleron

2.3.2 Depositor-Supplied Synonyms

1. 637-07-0

2. Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate

3. Ethyl Clofibrate

4. Atromid

5. Clofibratum

6. Atromid-s

7. Clofibrato

8. Liprin

9. Miscleron

10. Epib

11. Angiokapsul

12. Antilipid

13. Antilipide

14. Arterioflexin

15. Arterosol

16. Ateriosan

17. Athebrate

18. Atheromide

19. Atheropront

20. Chlorphenisate

21. Clofibate

22. Lipofacton

23. Ticlobran

24. Amotril

25. Anparton

26. Ateculon

27. Atrolen

28. Atromida

29. Lipavil

30. Lipavlon

31. Lipomid

32. Liprinal

33. Xyduril

34. Apolan

35. Amotril S

36. Ethyl Chlorophenoxyisobutyrate

37. Athranid-wirkstoff

38. Atromidin

39. Bioscleran

40. Cartagyl

41. Citiflus

42. Claripex

43. Clofibram

44. Clofibrat

45. Clofinit

46. Clofipront

47. Fibralem

48. Gerastop

49. Hyclorate

50. Klofibrat

51. Klofiran

52. Levatrom

53. Lipidsenker

54. Liponorm

55. Liporeduct

56. Lobetrin

57. Normalip

58. Persantinat

59. Regardin

60. Serotinex

61. Skleromexe

62. Atrovis

63. Azionyl

64. Bresit

65. Clobrat

66. Clofar

67. Delipid

68. Deliva

69. Lipamid

70. Liporil

71. Liposid

72. Normat

73. Regelan

74. Sklero

75. Dura Clofibrat

76. Sklero-tablinen

77. Neo-atomid

78. Neo-atromid

79. Atromid S

80. Claripex Cpib

81. Clobren-sf

82. Elpi

83. Cinnarizin

84. Cloberat

85. Misclerone

86. Normolipol

87. Robigram

88. Skerolip

89. Artevil

90. Negalip

91. Normet

92. Recolip

93. Scrobin

94. Yoclo

95. Sklero-tabuls

96. Regelan N

97. 2-(4-chlorophenoxy)-2-methylpropanoic Acid Ethyl Ester

98. Lipide 500

99. Chlorfenisate

100. Oxan 600

101. Propanoic Acid, 2-(4-chlorophenoxy)-2-methyl-, Ethyl Ester

102. Ethyl 2-(p-chlorophenoxy)isobutyrate

103. Ethyl P-chlorophenoxyisobutyrate

104. Nsc-79389

105. 2-(p-chlorophenoxy)-2-methylpropionic Acid Ethyl Ester

106. Ethyl Para-chlorophenoxyisobutyrate

107. Ethyl 2-(4-chlorophenoxy)-2-methylpropionate

108. Ici 28257

109. Ay-61123

110. Ay 61123

111. Alpha-p-chlorophenoxyisobutyryl Ethyl Ester

112. Ethyl 2-(4-chlorophenoxy)isobutyrate

113. Ethyl 2-(p-chlorophenoxy)-2-methylpropionate

114. Alpha-(p-chlorophenoxy)isobutyric Acid, Ethyl Ester

115. Ici-28257

116. 19 More Names Available

117. Propionic Acid, 2-(p-chlorophenoxy)-2-methyl-, Ethyl Ester

118. Chembl565

119. Hpn91k7fu3

120. Acetic Acid, (p-chlorophenoxy)dimethyl-, Ethyl Ester

121. Chebi:3750

122. Propanoic Acid, 2-(p-chlorophenoxy)-2-methyl-, Ethyl Ester

123. Propionic Acid, 2-(4-chlorophenoxy)-2-methyl-, Ethyl Ester

124. .alpha.-p-chlorophenoxyisobutyryl Ethyl Ester

125. 2-(4-chlorophenoxy)isobutyric Acid Ethyl Ester

126. Nsc79389

127. .alpha.-(p-chlorophenoxy)isobutyric Acid, Ethyl Ester

128. Ncgc00015257-08

129. Sklerepmexe

130. Serofinex

131. Sklerolip

132. Skleromex

133. Clofibrato [spanish]

134. Ethyl .alpha.-(4-chlorophenoxy)isobutyrate

135. Ethyl .alpha.-(p-chlorophenoxy)isobutyrate

136. Dsstox_cid_336

137. Sklero-tablinene

138. Clobren-5f

139. Dsstox_rid_75521

140. Vincamin Compositum

141. Clofibratum [inn-latin]

142. Dsstox_gsid_20336

143. Clofibrato [inn-spanish]

144. Ethyl 2-[(4-chlorophenyl)oxy]-2-methylpropanoate

145. Ethyl .alpha.-(p-chlorophenoxy)-.alpha.-methylpropionate

146. Ethyl .alpha.-(4-chlorophenoxy)-.alpha.-methylpropionate

147. Abitrate

148. Cas-637-07-0

149. Smr000058279

150. Ccris 177

151. Clofibrate (clof)

152. Ethyl-alpha-p-chlorophenoxy-isobutyrate

153. Ethyl Alpha-(4-chlorophenoxy)isobutyrate

154. Ethyl Alpha-(p-chlorophenoxy)isobutyrate

155. Hsdb 3038

156. Sr-01000075544

157. Einecs 211-277-4

158. Atromid-s (tn)

159. Nsc 79389

160. Unii-hpn91k7fu3

161. Brn 1913459

162. Bml2-f02

163. Clobren Sf

164. Clofibrate, Liquid

165. Ethyl Alpha-(4-chlorophenoxy)-alpha-methylpropionate

166. Ethyl Alpha-(p-chlorophenoxy)-alpha-methylpropionate

167. Mfcd00000615

168. Clofibrate [usan:usp:inn:ban:jan]

169. Isobutyric Acid, Alpha-(p-chlorophenoxy)-, Ethyl Ester

170. Ethyl 2-(para-chlorophenoxy)-2-methylpropionate (iupac)

171. Spectrum_001735

172. P-chlorophenoxyisobutyric Acid Ethyl Ester

173. Clofibrate [mi]

174. Clofibrate [inn]

175. Clofibrate [jan]

176. Spectrum2_001209

177. Spectrum4_000223

178. Spectrum5_001133

179. Clofibrate [hsdb]

180. Clofibrate [iarc]

181. Clofibrate [usan]

182. Lopac-c-6643

183. Clofibrate [vandf]

184. Upcmld-dp019

185. C 6643

186. Ethyl 2-(4-chlorophenoxy)-2-methyl-propanoate

187. Clofibrate [mart.]

188. Schembl2356

189. Clofibrate [who-dd]

190. Nciopen2_004739

191. Bidd:pxr0178

192. Cbiol_001860

193. Lopac0_000306

194. Bspbio_001577

195. Kbiogr_000297

196. Kbiogr_000885

197. Kbioss_000297

198. Kbioss_002215

199. Mls001336011

200. Mls001336012

201. Mls002153494

202. Bidd:gt0172

203. Divk1c_000822

204. Divk1c_000926

205. Spbio_000998

206. Clofibrate (jp17/usp/inn)

207. Gtpl2667

208. Clofibrate [orange Book]

209. Dtxsid3020336

210. Upcmld-dp019:001

211. Bcbcmap01_000104

212. Hms502j04

213. Hms502o08

214. Kbio1_000822

215. Kbio1_000926

216. Kbio2_000297

217. Kbio2_002215

218. Kbio2_002865

219. Kbio2_004783

220. Kbio2_005433

221. Kbio2_007351

222. Kbio3_000593

223. Kbio3_000594

224. Wln: Gr Dox1&1&vo2

225. Zinc56648

226. Clofibrate [ep Monograph]

227. Clofibrate [usp Impurity]

228. Clofibrate, >=98.0% (gc)

229. Ninds_000822

230. Ninds_000926

231. Bio1_000146

232. Bio1_000635

233. Bio1_001124

234. Bio2_000297

235. Bio2_000777

236. Hms1361o19

237. Hms1791o19

238. Hms1989o19

239. Hms2089p03

240. Hms2093g07

241. Hms2233c17

242. Hms3260n14

243. Hms3373c06

244. Hms3402o19

245. Hms3715j03

246. Pharmakon1600-01503429

247. Hy-b0287

248. Tox21_110116

249. Tox21_202414

250. Tox21_300277

251. Tox21_500306

252. Bdbm50085047

253. Ccg-40281

254. Nsc758474

255. Akos015889383

256. Tox21_110116_1

257. Db00636

258. Lp00306

259. Nsc-758474

260. Sdccgsbi-0050294.p004

261. Idi1_000822

262. Idi1_000926

263. Idi1_034047

264. Clofibrate, Analytical Reference Material

265. Ncgc00015257-01

266. Ncgc00015257-02

267. Ncgc00015257-03

268. Ncgc00015257-04

269. Ncgc00015257-05

270. Ncgc00015257-06

271. Ncgc00015257-07

272. Ncgc00015257-09

273. Ncgc00015257-10

274. Ncgc00015257-11

275. Ncgc00015257-12

276. Ncgc00015257-14

277. Ncgc00015257-22

278. Ncgc00093755-01

279. Ncgc00093755-03

280. Ncgc00093755-04

281. Ncgc00093755-05

282. Ncgc00093755-06

283. Ncgc00093755-07

284. Ncgc00093755-08

285. Ncgc00254073-01

286. Ncgc00259963-01

287. Ncgc00260991-01

288. Ac-33179

289. As-14127

290. Clofibrate 100 Microg/ml In Acetonitrile

291. Nci60_041748

292. Ethyl .alpha.-p-(chlorophenoxy)isobutyrate

293. Sbi-0050294.p003

294. Db-054528

295. Ethyl2-(4-chlorophenoxy)-2-methylpropanoate

296. Eu-0100306

297. Ft-0625865

298. Ft-0665112

299. S1820

300. 2-(p-chlorophenoxy)isobutyric Acid Ethyl Ester

301. C06916

302. D00279

303. F20382

304. Ab00052358-07

305. Ab00052358-08

306. Ab00052358_09

307. Ab00052358_10

308. Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate #

309. A834483

310. Ethyl 2-(4-chloranylphenoxy)-2-methyl-propanoate

311. Acetic Acid, (p-chlorophenoxy)dimethyl-, Ethyl Este

312. Ethyl 2-(4-chlorophenoxy)-2-methylpropionate, 99%

313. Q2701912

314. Sr-01000075544-1

315. Sr-01000075544-4

316. Sr-01000075544-5

317. Sr-01000075544-8

318. Z53835984

319. 2-(p-chlorophenoxy)-2-methylpropanoic Acid Ethyl Ester

320. 2-(4-chloro-phenoxy)-2-methyl-propionic Acid Ethyl Ester

321. Clofibrate, European Pharmacopoeia (ep) Reference Standard

322. Isobutyric Acid, .alpha.-(p-chlorophenoxy)-, Ethyl Ester

323. Clofibrate, United States Pharmacopeia (usp) Reference Standard

2.4 Create Date
2004-09-16
3 Chemical and Physical Properties
Molecular Weight 242.70 g/mol
Molecular Formula C12H15ClO3
XLogP33.3
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count3
Rotatable Bond Count5
Exact Mass242.0709720 g/mol
Monoisotopic Mass242.0709720 g/mol
Topological Polar Surface Area35.5 Ų
Heavy Atom Count16
Formal Charge0
Complexity232
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 Therapeutic Uses

Anticholesteremic Agents; Antilipemic Agents

National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)


Clofibrate is indicated only in subjects with increased concentrations of VLDL and IDL (such as patients with familial type-III hyperlipoproteinemia) who have failed to respond adequately to gemfibrozil or nicotinic acid. Because clofibrate has only a modest effect on LDL and more effective agents are available for lowering the concentration of LDL, the drug is of limited utility for patients with either familial hypercholesterolemia or polygenic hypercholesterolemia.

Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 889


In a ... trial of primary prevention involving asymptomatic men with hypercholesterolemia, clofibrate lowered the plasma cholesterol concentration by only 6 to 11%. This very modest effect in unselected patients can be contrasted with that seen in patients with familial type-III hyperlipoproteinemia, in whom concentrations of cholesterol and triglycerides were lowered by approximately 50% and by as much as 80%, respectively. In such patients, administration of clofibrate results in the mobilization of deposits of cholesterol in tissues, accompanied by regression and disappearance of xanthomas. Clofibrate has no effect on hyperchylomicronemia, nor does it affect concentrations of HDL. Thus, clofibrate appears to have specific efficacy only in patients with familial type-III hyperlipoproteinemia.

Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 886


The clinical evidence for the efficacy of clofibrate in preventing deaths from coronary artery disease is not encouraging. A number of clinical trials have been completed, and none has shown a clear-cut beneficial effect. A double blind study ... compared clofibrate with placebo in 10,000 men in the upper third of the distribution of plasma cholesterol concentrations. Patients treated with clofibrate had a decrease in nonfatal myocardial infarctions. ... Clofibrate treated patients had a higher noncardiac mortality rate than did control subjects, owing mainly to an increased incidence of malignant neoplasms and complications of cholecystectomy.

Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 886


For more Therapeutic Uses (Complete) data for CLOFIBRATE (9 total), please visit the HSDB record page.


4.2 Drug Warning

Impotence observed after clofibrate treatment was the fourth most frequently occurring side effect of more than 30 side effects recorded ... . Although the exact mechanism is not known ...

Thomas, J.A., K.S. Korach, J.A. McLachlan. Endocrine Toxicology. New York, NY: Raven Press, Ltd., 1985., p. 278


Response to clofibrate is variable, and serum cholesterol and triglyceride concn should be determined prior to and regularly during (eg, every 3-6 mo) clofibrate therapy. If possible, the LDL and HDL fractions should also be determined and the LDL fraction rechecked during the first few months of clofibrate therapy ...

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 1162


Liver function tests and complete blood cell counts should be performed periodically during clofibrate therapy ... some clinicians recommend serial determinations of plasma CK (CPK) concn during treatment with clofibrate ...

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 1162


...THE DRUG IS OF LIMITED UTILITY FOR PATIENTS WITH TYPE-II HYPERLIPOPROTEINEMIA. FURTHERMORE, SINCE CLOFIBRATE MAY INCREASE THE CONCN OF LOW DENSITY LIPOPROTEIN IN SOME PATIENTS WITH ELEVATIONS OF VERY LOW DENSITY LIPOPROTEIN /VLDL/, THE EFFECTS OF THE DRUG SHOULD BE MONITORED BY SEQUENTIAL MEASUREMENT OF PLASMA LIPOPROTEINS. A SHIFT FROM AN EXCESS OF VLDL TO ONE OF LDL /LOW DENSITY LIPOPROTEIN/ SUGGESTS THE NECESSITY TO DISCONTINUE THE DRUG.

Gilman, A. G., L. S. Goodman, and A. Gilman. (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 6th ed. New York: Macmillan Publishing Co., Inc. 1980., p. 841


For more Drug Warnings (Complete) data for CLOFIBRATE (10 total), please visit the HSDB record page.


4.3 Drug Indication

For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. This helps control high cholesterol and high triglyceride levels.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Clofibrate is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction (Sf 20-400) rich in triglycerides. Serum cholesterol may be decreased, particularly in those patients whose cholesterol elevation is due to the presence of IDL as a result of Type III hyperlipoproteinemia. Several investigators have observed in their studies that clofibrate may produce a decrease in cholesterol linoleate but an increase in palmitoleate and oleate, the latter being considered atherogenic in experimental animals. The significance of this finding is unknown at this time. Reduction of triglycerides in some patients treated with clofibrate or certain of its chemically and clinically similar analogs may be associated with an increase in LDL cholesterol. Increase in LDL cholesterol has been observed in patients whose cholesterol is initially normal. Animal studies suggest that clofibrate interrupts cholesterol biosynthesis prior to mevalonate formation.


5.2 MeSH Pharmacological Classification

Anticholesteremic Agents

Substances used to lower plasma cholesterol levels. (See all compounds classified as Anticholesteremic Agents.)


Hypolipidemic Agents

Substances that lower the levels of certain LIPIDS in the BLOOD. They are used to treat HYPERLIPIDEMIAS. (See all compounds classified as Hypolipidemic Agents.)


5.3 ATC Code

C - Cardiovascular system

C10 - Lipid modifying agents

C10A - Lipid modifying agents, plain

C10AB - Fibrates

C10AB01 - Clofibrate


5.4 Absorption, Distribution and Excretion

Absorption

Completely but slowly absorbed from the intestine. Between 95% and 99% of an oral dose of clofibrate is excreted in the urine as free and conjugated clofibric acid; thus, the absorption of clofibrate is virtually complete.


IN MAN, CLOFIBRATE IS COMPLETELY ABSORBED FROM INTESTINE & APPEARS IN PLASMA AS DEESTERIFIED P-CHLOROPHENOXYISOBUTYRIC ACID (CPIB); PEAK PLASMA CONCN OF THE ACID OCCUR WITHIN 4 HR AFTER ORAL ADMIN ... MAJOR FRACTION OF CPIB ... BOUND TO PLASMA ALBUMIN. ELIMINATION OF CPIB PROCEEDS IN 2 KINETIC PHASES, WITH SLOWER EXPONENTIAL PHASE HAVING MEAN HALF-LIFE OF NEARLY 15 HR. ESSENTIALLY ALL ACID ... EXCRETED IN URINE, ABOUT 60% AS GLUCURONIDE.

Gilman, A. G., L. S. Goodman, and A. Gilman. (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 6th ed. New York: Macmillan Publishing Co., Inc. 1980., p. 841


TRANSFER ACROSS THE PLACENTA AND INTO THE MILK AND A POSTNATAL INCREASE IN LIVER ALPHA-GLYCEROPHOSPHATE DEHYDROGENASE HAS BEEN REPORTED IN NEWBORN RATS WHOSE MOTHERS WERE FED CLOFIBRATE.

IARC. Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Humans. Geneva: World Health Organization, International Agency for Research on Cancer, 1972-PRESENT. (Multivolume work). Available at: https://monographs.iarc.fr/ENG/Classification/index.php, p. V24 45 (1980)


CLOFIBRATE IS RAPIDLY AND COMPLETELY ABSORBED AFTER ORAL ADMINISTRATION. IN MAN, CLOFIBRIC ACID, A MAJOR METABOLITE OF CLOFIBRATE, IS EXCRETED IN THE URINE IN THE FORM OF THE GLUCURONIDE CONJUGATE; THE PLASMA ELIMINATION HALF-LIFE OF CLOFIBRIC ACID RANGES BETWEEN 12-25 HOURS.

IARC. Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Humans. Geneva: World Health Organization, International Agency for Research on Cancer, 1972-PRESENT. (Multivolume work). Available at: https://monographs.iarc.fr/ENG/Classification/index.php, p. V24 48 (1980)


Clofibrate is readily and reportedly almost completely absorbed from the GI tract; approx 95-99% of an orally admin dose ... is excreted in urine as free and conjugated clofibric acid. The drug is rapidly hydrolyzed by serum enzymes to the free acid, clofibric acid ... . Peak plasma clofibric acid concn 4-6 hr after oral admin of a single 500-mg, 1-g, or 2-g doses of clofibrate in healthy individuals average 49-53, 89, or 151 ug/ml, respectively.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 1160


For more Absorption, Distribution and Excretion (Complete) data for CLOFIBRATE (7 total), please visit the HSDB record page.


5.5 Metabolism/Metabolites

Hepatic and gastrointestinal: rapid de-esterification occurs in the gastrointestinal tract and/or on first-pass metabolism to produce the active form, clofibric acid (chlorophenoxy isobutyric acid [CPIB]).


IN MAN, CLOFIBRATE ... APPEARS IN PLASMA AS DEESTERIFIED PARA-CHLOROPHENOXYISOBUTYRIC ACID ... ESSENTIALLY ALL ACID ... EXCRETED IN URINE, ABOUT 60% AS GLUCURONIDE.

Gilman, A. G., L. S. Goodman, and A. Gilman. (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 6th ed. New York: Macmillan Publishing Co., Inc. 1980., p. 841


AN ACYL-LINKED ACID METABOLITE OF CLOFIBRATE HAS BEEN IDENTIFIED IN HUMAN URINE. THIS REPRESENTS THE FIRST ACYL-LINKED MERCAPTURATE FOUND IN MAN. AUTHORS PROPOSE THAT CLOFIBRATE ACYL GLUCURONIDE IS AN ELECTROPHILIC METABOLITE WHICH REACTS WITH SULFHYDRYL GROUPS & THEREFORE MAY BE RESPONSIBLE FOR THE HUMAN HEPATOTOXICITY OF CLOFIBRATE.

PMID:6130909 STOGNIEW W, FENSELAU C; DRUG METAB DISPOS 10 (6): 609-13 (1982)


5.6 Biological Half-Life

Half-life in normal volunteers averages 18 to 22 hours (range 14 to 35 hours) but can vary by up to 7 hours in the same subject at different times.


THE PLASMA ELIMINATION HALF-LIFE OF CLOFIBRIC ACID RANGES BETWEEN 12-25 HOURS.

IARC. Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Humans. Geneva: World Health Organization, International Agency for Research on Cancer, 1972-PRESENT. (Multivolume work). Available at: https://monographs.iarc.fr/ENG/Classification/index.php, p. V24 48 (1980)


Clofibric acid has an elimination half-life of 12-35 hr (mean 12-22 hr) in healthy adults and 29-88 hr in patients with renal failure. /Clofibric acid/

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 1160


5.7 Mechanism of Action

Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Clofibrate also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. Also, as a fibrate, Clofibrate is an agonist of the PPAR- receptor[4] in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, increased lipoprotein lipase activity.


Clofibrate decreases serum very low-density lipoprotein (VLDL) and low-density lipoprotein (LDL) concn in healthy individuals and abnormal lipoproteins in patients with type III hyperlipoproteinemia. Serum triglyceride concn are usually reduced more than cholesterol concn.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 1160


The exact mechanism by which clofibrate lowers serum concn of triglycerides and cholesterol is unknown. Apparently, the drug has several antilipemic actions, including increasing triglyceride and VLDL clearance, inhibition of the biosynthesis of cholesterol before mevalonate formation, mobilization of cholesterol from tissues, increasing fecal excretion of neutral sterols, decreasing hepatic lipoprotein synthesis and/or secretion (particularly VLDL), decreasing free fatty acid release, and decreasing triglyceride synthesis.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 1160


Clofibrate induces changes in blood coagulation which are independent of the lipid-lowering action of the drug. The drug decreases platelet adhesiveness. Plasma fibrinogen concn decrease during the first 6 wk to 4 mo of therapy after which the concn return toward normal. Plasma fibrinolysis is usually increased.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 1160


Their primary effect is to increase the activity of lipoprotein lipase, which in turn promotes the catabolism of the triglyceride rich lipoproteins, VLDL and IDL. The drugs may also decrease the hepatic synthesis and secretion of VLDL. Fibric acids are believed to raise HDL cholesterol indirectly as a result of the decrease in the concentration of VLDL triglyceride. VLDL normally exchanges lipids with HDL, the triglycerides of VLDL moving to HDL and the cholesteryl esters of HDL moving to VLDL. When VLDL concentrations are reduced, this exchange is slowed. Cholesteryl esters remain in HDL and thus the concentration of HDL cholesterol increases. /Fibric Acids/

Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 888


REF. STANDARDS & IMPURITIES

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