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Griseofulvin

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12 API Suppliers, 7 USDMF, 2 CEP/COS, 4 NDC API, 5 Listed Suppliers, $ API Reference Price

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TABLET;ORAL - 125MG, TABLET;ORAL - 250MG

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TABLET;ORAL - 250MG

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Synopsis

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Chemistry

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Also known as: 126-07-8, (+)-griseofulvin, Amudane, Grisactin, Grisefuline, Griseofulvinum

Molecular Formula

C₁₇H₁₇ClO₆

Molecular Weight

352.8 g/mol

InChI Key

DDUHZTYCFQRHIY-RBHXEPJQSA-N

FDA UNII

32HRV3E3D5

An antifungal agent used in the treatment of TINEA infections.

Griseofulvin is a Tubulin Inhibiting Agent. The physiologic effect of griseofulvin is by means of Decreased Mitosis, and Microtubule Inhibition.

1 2D Structure

Griseofulvin

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(2S,5'R)-7-chloro-3',4,6-trimethoxy-5'-methylspiro[1-benzofuran-2,4'-cyclohex-2-ene]-1',3-dione

2.1.2 InChI

InChI=1S/C17H17ClO6/c1-8-5-9(19)6-12(23-4)17(8)16(20)13-10(21-2)7-11(22-3)14(18)15(13)24-17/h6-8H,5H2,1-4H3/t8-,17+/m1/s1

2.1.3 InChI Key

DDUHZTYCFQRHIY-RBHXEPJQSA-N

2.1.4 Canonical SMILES

CC1CC(=O)C=C(C12C(=O)C3=C(O2)C(=C(C=C3OC)OC)Cl)OC

2.1.5 Isomeric SMILES

C[C@@H]1CC(=O)C=C([C@]12C(=O)C3=C(O2)C(=C(C=C3OC)OC)Cl)OC

2.2 Other Identifiers

2.2.1 UNII

32HRV3E3D5

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Fulvicin U F

2. Fulvicin-u-f

3. Fulvicinuf

4. Grifulvin V

5. Gris Peg

6. Gris-peg

7. Grisactin

8. Grisefuline

9. Grispeg

2.3.2 Depositor-Supplied Synonyms

1. 126-07-8

2. (+)-griseofulvin

3. Amudane

4. Grisactin

5. Grisefuline

6. Griseofulvinum

7. Griseofulvina

8. Grizeofulvin

9. Grifulvin

10. Grisofulvin

11. Spirofulvin

12. Fulcin

13. Grysio

14. Lamoryl

15. Likuden

16. Fulvicin

17. Griseofulvine

18. Poncyl

19. Curling Factor

20. Grisovin

21. Grisactin V

22. Griseofulvine [inn-french]

23. Griseofulvinum [inn-latin]

24. Griseofulvina [inn-spanish]

25. Griseofulvin, Microcrystalline

26. Delmofulvina

27. Fulvistatin

28. Griscofulvin

29. Fulcine

30. Fulvina

31. Fulvinil

32. Fungivin

33. Greosin

34. Gresfeed

35. Grifulin

36. Grisetin

37. Guservin

38. Murfulvin

39. Neo-fulcin

40. Biogrisin-fp

41. Fulvican Grisactin

42. Griseofulvin-forte

43. Fulvicin-p/g

44. Fulvicin-u/f

45. Griseofulvin, Ultramicrocrystalline

46. Griseofulvin Microsize

47. Xuanjing

48. Mfcd00082343

49. Griseofulvin, Ultramicrosize

50. Usaf Sc-2

51. Griseomix

52. Grisactin Ultra

53. Nsc-755822

54. Griseofulvin Forte

55. Fulvicin P/g

56. 32hrv3e3d5

57. Chebi:27779

58. Griseofulvin Permeability Diameter

59. Nsc-34533

60. (2s,5'r)-7-chloro-3',4,6-trimethoxy-5'-methylspiro[1-benzofuran-2,4'-cyclohex-2-ene]-1',3-dione

61. Ncgc00091120-01

62. Dsstox_cid_674

63. Nsc 34533

64. Dsstox_rid_75725

65. Dsstox_gsid_20674

66. (1's,6'r)-7-chloro-2',4,6-trimethoxy-6'-methylspiro(benzofuran-2(3h),1'-(2)cyclohexene)-3,4'-dione

67. (1's-trans)- 7-chloro-2',4,6-trimethoxy-6'-methylspiro(benzofuran-2(3h),1'-cyclohex-2'-ene)-3,4'-dione

68. (2s,6'r)-7-chloro-2',4,6-trimethoxy-6'-methyl-3h,4'h-spiro[1-benzofuran-2,1'-cyclohex[2]ene]-3,4'-dione

69. (2s,6'r)-7-chloro-2',4,6-trimethoxy-6'-methyl-3h-spiro[benzofuran-2,1'-cyclohexan]-2'-ene-3,4'-dione

70. Ultragris-165

71. Ultragris-330

72. Fulvicin Bolus

73. Fulvicin-u/f (veterinary)

74. Fulvicin Bolus (veterinary)

75. Fulvicin P/g 165

76. Fulvicin P/g 330

77. Spiro(benzofuran-2(3h),1'-(2)cyclohexene)-3,4'-dione, 7-chloro-2',4,6-trimethoxy-6'-methyl-, (1's-trans)-

78. 7-chloro-4,6,2'-trimethoxy-6'-methylgris-2'-en-3,4'-dione

79. Caswell No. 471b

80. Fulvidex

81. (2s,6'r)-7-chloro-2',4,6-trimethoxy-6'-methyl-3h-spiro[1-benzofuran-2,1'-cyclohexan]-2'-ene-3,4'-dione

82. (1's,6'r)-7-chloro-2',4,6-trimethoxy-6'-methyl-3h-spiro[benzofuran-2,1'-cyclohex[2]ene]-3,4'-dione

83. Smr000718755

84. Ccris 320

85. Hsdb 1722

86. Sr-05000001535

87. Einecs 204-767-4

88. Epa Pesticide Chemical Code 471400

89. Griseofulvin And Alpha-ifn

90. Brn 0095226

91. Unii-32hrv3e3d5

92. Griseoflulvin

93. Griseofulvin, Microsize

94. Ai3-51015

95. Fulvicin Uf

96. Griseofulvin,(s)

97. Griseofulvin [usp:inn:ban:jan]

98. (2s,5'r)-7-chloro-3',4,6-trimethoxy-5'-methyl-spiro[benzofuran-2,4'-cyclohex-2-ene]-1',3-dione

99. Prestwick_247

100. Grisactin V (tn)

101. Gris-peg (tn)

102. Griseofulvin,microsize

103. Spectrum_000816

104. Cpd000718755

105. Specplus_000336

106. Prestwick3_000226

107. Spectrum2_000213

108. Spectrum3_000161

109. Spectrum4_000927

110. Spectrum5_000648

111. Griseofulvin [mi]

112. Griseofulvin [usp:inn]

113. Griseofulvin [inn]

114. Griseofulvin [jan]

115. Chembl562

116. Griseofulvin [hsdb]

117. Griseofulvin [iarc]

118. 7-chloro-2',4,6-trimethoxy-6'beta-methylspiro(benzofuran-2(3h),1'-(2)cyclohexene)-3,4'-dione

119. 7-chloro-4,6-dimethoxycoumaran-3-one-2-spiro-1'-(2'-methoxy-6'-methylcyclohex-2'-en-4'-one)

120. Griseofulvin [vandf]

121. Schembl21988

122. Bspbio_000271

123. Bspbio_001621

124. Griseofulvin [mart.]

125. Kbiogr_001454

126. Kbioss_001296

127. Spectrum200046

128. (2s-trans)-7-chloro-2',4,6-trimethoxy-6'-methylspiro(benzofuran-2(3h),1'-(2)cyclohexene)-3,4'-dione

129. 5-18-05-00150 (beilstein Handbook Reference)

130. Mls001304062

131. Mls002152905

132. Mls002154239

133. Spiro(benzofuran-2(3h),1'-(2)cyclohexene)-3,4'-dione, 7-chloro-2',4,6-trimethoxy-6'-methyl-, (2s-trans)-

134. Bidd:gt0024

135. Divk1c_000154

136. Divk1c_006432

137. Griseofulvin [usp-rs]

138. Griseofulvin [who-dd]

139. Griseofulvin [who-ip]

140. Griseofulvin (jan/usp/inn)

141. Spbio_000225

142. Bpbio1_000299

143. Megxm0_000184

144. Dtxsid8020674

145. Acon0_000953

146. Acon1_001843

147. Bdbm31775

148. Fulvicin-u/f Powder And Tablets

149. Hms500h16

150. Kbio1_000154

151. Kbio1_001376

152. Kbio2_001296

153. Kbio2_003864

154. Kbio2_006432

155. Kbio3_001121

156. Griseofulvin [green Book]

157. Ninds_000154

158. Griseofulvin [orange Book]

159. Hms1923e09

160. Hms2091a03

161. Hms2095n13

162. Hms2235f13

163. Hms3259d05

164. Hms3712n13

165. Interacts With Polymerized Microtubules And Associated Proteins

166. Pharmakon1600-00200046

167. Zinc622123

168. Griseofulvin [ep Monograph]

169. 7-chloro-2',4,6-trimethoxy-6'.beta.-methylspiro(benzofuran-2(3h),1'-(2)cyclohexene)-3,4'-dione

170. Spiro(benzofuran-2(3h),1'-(2)cyclohexene)-3,4'-dione, 7-chloro-2',4,6-trimethoxy-6'-methyl-, (1's,6'r)-

171. Griseofulvin [usp Monograph]

172. Tox21_111087

173. Tox21_202235

174. Tox21_303005

175. Ccg-38416

176. Lmpk13060001

177. Nsc755822

178. S4071

179. Griseofulvinum [who-ip Latin]

180. Akos015896380

181. Tox21_111087_1

182. Cs-3426

183. Db00400

184. Nc00616

185. Sdccgmls-0066450.p001

186. Griseofulvin 100 Microg/ml In Methanol

187. Idi1_000154

188. Ncgc00091120-02

189. Ncgc00091120-03

190. Ncgc00091120-04

191. Ncgc00091120-05

192. Ncgc00091120-06

193. Ncgc00091120-07

194. Ncgc00091120-08

195. Ncgc00091120-09

196. Ncgc00091120-13

197. Ncgc00256353-01

198. Ncgc00259784-01

199. As-13736

200. Bt164513

201. Hy-17583

202. Griseofulvin 100 Microg/ml In Acetonitrile

203. G0384

204. En300-52615

205. Bim-0051396.0001

206. C06686

207. D00209

208. Ab00052005_07

209. Griseofulvin, Vetranal(tm), Analytical Standard

210. Griseofulvin Permeability Diameter [usp-rs]

211. Q416096

212. Sr-01000837512

213. Griseofulvin, Antibiotic For Culture Media Use Only

214. Q-201178

215. Sr-01000837512-2

216. Sr-05000001535-1

217. Sr-05000001535-3

218. Sr-05000001535-4

219. Brd-k08273968-001-05-9

220. Brd-k08273968-001-09-1

221. Brd-k08273968-001-19-0

222. Z1258578352

223. Griseofulvin, British Pharmacopoeia (bp) Reference Standard

224. Griseofulvin, From Penicillium Griseofulvum, 97.0-102.0%

225. Griseofulvin, European Pharmacopoeia (ep) Reference Standard

226. Griseofulvin, United States Pharmacopeia (usp) Reference Standard

227. Griseofulvin Permeability Diameter, United States Pharmacopeia (usp) Reference Standard

228. Griseofulvin, Pharmaceutical Secondary Standard; Certified Reference Material

229. 107912-37-8

230. 7-chloro-2',4,6-trimethoxy-6'-methylspiro[benzofuran-2(3h),1',- [2]cyclohexene]-3,4'-dione

2.4 Create Date

2005-06-24

3 Chemical and Physical Properties

Molecular Formula	C₁₇H₁₇ClO₆
Molecular Weight	352.8 g/mol
XLogP3	2.2
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	3
Exact Mass	352.0713660 g/mol
Monoisotopic Mass	352.0713660 g/mol
Topological Polar Surface Area	71.1 Å²
Heavy Atom Count	24
Formal Charge	0
Complexity	575
Isotope Atom Count	0
Defined Atom Stereocenter Count	2
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 8
Drug Name	Grifulvin v
Active Ingredient	Griseofulvin, microsize
Dosage Form	Tablet; Suspension
Route	Oral
Strength	500mg; 125mg/5ml
Market Status	Prescription
Company	Valeant Luxembourg

2 of 8
Drug Name	Griseofulvin
PubMed Health	Griseofulvin (By mouth)
Drug Classes	Antifungal
Drug Label	Griseofulvin microsize contains griseofulvin microsize for oral administration. The active ingredient, griseofulvin, is a fungistatic antibiotic, derived from a species of Penicillium. The chemical name of griseofulvin is 7-chloro-2', 4,6-trimethoxy-
Active Ingredient	Griseofulvin, microsize
Dosage Form	Tablet; Suspension
Route	Oral
Strength	250mg; 500mg; 125mg/5ml
Market Status	Prescription
Company	Vintage Pharms; Perrigo Co Tennessee; Sandoz; Ivax Sub Teva Pharms; Actavis Mid Atlantic; Sigmapharm Labs

3 of 8
Drug Name	Griseofulvin, ultramicrosize
Active Ingredient	Griseofulvin, ultramicrosize
Dosage Form	Tablet
Route	Oral
Strength	250mg; 125mg
Market Status	Prescription
Company	Riconpharma

4 of 8
Drug Name	Gris-peg
Drug Label	Gris-PEG Tablets contain ultramicrosize crystals of griseofulvin, an antibiotic derived from a species of Penicillium.Each Gris-PEG tablet contains:Active Ingredient: griseofulvin ultramicrosize .... 125 mgInactive Ingredients: colloidal silicon...
Active Ingredient	Griseofulvin, ultramicrosize
Dosage Form	Tablet
Route	Oral
Strength	250mg; 125mg
Market Status	Prescription
Company	Pedinol

5 of 8
Drug Name	Grifulvin v
Active Ingredient	Griseofulvin, microsize
Dosage Form	Tablet; Suspension
Route	Oral
Strength	500mg; 125mg/5ml
Market Status	Prescription
Company	Valeant Luxembourg

6 of 8
Drug Name	Griseofulvin
PubMed Health	Griseofulvin (By mouth)
Drug Classes	Antifungal
Drug Label	Griseofulvin microsize contains griseofulvin microsize for oral administration. The active ingredient, griseofulvin, is a fungistatic antibiotic, derived from a species of Penicillium. The chemical name of griseofulvin is 7-chloro-2', 4,6-trimethoxy-
Active Ingredient	Griseofulvin, microsize
Dosage Form	Tablet; Suspension
Route	Oral
Strength	250mg; 500mg; 125mg/5ml
Market Status	Prescription
Company	Vintage Pharms; Perrigo Co Tennessee; Sandoz; Ivax Sub Teva Pharms; Actavis Mid Atlantic; Sigmapharm Labs

7 of 8
Drug Name	Griseofulvin, ultramicrosize
Active Ingredient	Griseofulvin, ultramicrosize
Dosage Form	Tablet
Route	Oral
Strength	250mg; 125mg
Market Status	Prescription
Company	Riconpharma

8 of 8
Drug Name	Gris-peg
Drug Label	Gris-PEG Tablets contain ultramicrosize crystals of griseofulvin, an antibiotic derived from a species of Penicillium.Each Gris-PEG tablet contains:Active Ingredient: griseofulvin ultramicrosize .... 125 mgInactive Ingredients: colloidal silicon...
Active Ingredient	Griseofulvin, ultramicrosize
Dosage Form	Tablet
Route	Oral
Strength	250mg; 125mg
Market Status	Prescription
Company	Pedinol

4.2 Therapeutic Uses

Antibiotics, Antifungal

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

GRISEOFULVIN IS USED IN THE TREATMENT OF TINEAS (RINGWORM INFECTIONS) OF THE SKIN, HAIR & NAILS--TINEA CORPORIS, TINEA PEDIS, TINEA CRURIS, TINEA BARBAE, TINEA CAPITIS & TINEA UNGUIUM (ONYCHOMYCOSIS) CAUSED BY SUSCEPTIBLE SPECIES OF TRICHOPHYTON, MICROSPORUM, OR EPIDERMOPHYTON.

McEvoy, G.K. (ed.). American Hospital Formulary Service--Drug Information 94. Bethesda, MD: American Society of Hospital Pharmacists, Inc. 1994 (Plus Supplements)., p. 83

MEDICATION (VET): DRUG IS USEFUL IN TREATMENT OF SUPERFICIAL FUNGUS INFECTIONS CAUSED BY TRICHOPHYTON MENTAGROPHYTES, RUBRUM, INTERDIGITALE, SCHOENLEINI, SULPHUREUM AND VERRUCOSUM, AND MICROSPORUM AND OVINI, CANIS, AND GYPSEUM...

Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 1166

MEDICATION (VET): TO TREAT RINGWORM OF SKIN OR NAILS ESPECIALLY THOSE AREAS DIFFICULT TO TREAT LOCALLY (EYE, MOUTH, NAIL AREAS), OR THOSE REFRACTORY TO OTHER THERAPY.

Rossoff, I.S. Handbook of Veterinary Drugs. New York: Springer Publishing Company, 1974., p. 247

For more Therapeutic Uses (Complete) data for GRISEOFULVIN (14 total), please visit the HSDB record page.

4.3 Drug Warning

ORAL THRUSH DUE TO CANDIDAL OVERGROWTH HAS...OCCURRED.

McEvoy, G.K. (ed.). American Hospital Formulary Service--Drug Information 94. Bethesda, MD: American Society of Hospital Pharmacists, Inc. 1994 (Plus Supplements)., p. 84

GRISEOFULVIN...IS CONTRAINDICATED IN PATIENTS WITH ACUTE INTERMITTENT PORPHYRIA OR A HISTORY OF.../IT/, HEPATOCELLULAR FAILURE, AND HYPERSENSITIVITY TO THE DRUG. ... SAFE USE...DURING PREGNANCY HAS NOT BEEN ESTABLISHED.

American Medical Association, Council on Drugs. AMA Drug Evaluations Annual 1994. Chicago, IL: American Medical Association, 1994., p. 1593

RARELY, TRANSIENT DIMINUTION OF HEARING HAS OCCURRED...PARESTHESIAS OF HANDS AND FEET HAS FOLLOWED EXTENDED THERAPY... OCCASIONALLY, LARGE DOSES HAVE PRODUCED...PSYCHOTIC SYMPTOMS.

McEvoy, G.K. (ed.). American Hospital Formulary Service--Drug Information 94. Bethesda, MD: American Society of Hospital Pharmacists, Inc. 1994 (Plus Supplements)., p. 84

GRISEOFULVIN HAS BEEN REPORTED TO CAUSE TACHYCARDIA AND FLUSHING...

McEvoy, G.K. (ed.). American Hospital Formulary Service--Drug Information 94. Bethesda, MD: American Society of Hospital Pharmacists, Inc. 1994 (Plus Supplements)., p. 84

For more Drug Warnings (Complete) data for GRISEOFULVIN (17 total), please visit the HSDB record page.

4.4 Drug Indication

For the treatment of ringworm infections of the skin, hair, and nails, namely: tinea corporis, tinea pedis, tinea cruris, tinea barbae, cradle cap or other conditions caused by Trichophyton or Microsporum fungi.

FDA Label

5 Pharmacology and Biochemistry

5.1 Pharmacology

Griseofulvin is a mycotoxic metabolic product of Penicillium spp. It was the first available oral agent for the treatment of dermatophytoses and has now been used for more than forty years. Griseofulvin is fungistatic with in vitro activity against various species of Microsporum Epidermophyton, and Trichophyton. It has no effect on bacteria or on other genera of fungi. Following oral administration, griseofulvin is deposited in the keratin precursor cells and has a greater affinity for diseased tissue. The drug is tightly bound to the new keratin which becomes highly resistant to fungal invasions. Once the keratin-Griseofulvin complex reaches the skin site of action, it binds to fungal microtubules (tubulin) thus altering fungal mitosis.

5.2 MeSH Pharmacological Classification

Antifungal Agents

Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues. (See all compounds classified as Antifungal Agents.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

GRISEOFULVIN

5.3.2 FDA UNII

32HRV3E3D5

5.3.3 Pharmacological Classes

Microtubule Inhibition [PE]; Tubulin Inhibiting Agent [EPC]; Decreased Mitosis [PE]

5.4 ATC Code

D - Dermatologicals

D01 - Antifungals for dermatological use

D01A - Antifungals for topical use

D01AA - Antibiotics

D01AA08 - Griseofulvin

D - Dermatologicals

D01 - Antifungals for dermatological use

D01B - Antifungals for systemic use

D01BA - Antifungals for systemic use

D01BA01 - Griseofulvin

5.5 Absorption, Distribution and Excretion

Absorption

Poorly absorbed from GI ranging from 25 to 70% of an oral dose. Absorption is significantly enhanced by administration with or after a fatty meal.

IN RATS GIVEN ORAL DOSES OF 100 MG/KG BODY WT (36)CL-GRISEOFULVIN, 10% OF ACTIVITY WAS FOUND IN URINE AFTER 24 HR & 4% DURING 24-48 HR. ...IN ANOTHER STUDY, WITHIN 24-HR PERIOD ONLY 0.14% OF SIMILAR ORAL DOSES IN RATS WAS FOUND IN URINE, & 16% WAS RECOVERED IN FECES. FOLLOWING ITS IV INJECTION GRISEOFULVIN WAS DISTRIBUTED EVENLY THROUGHOUT TISSUES, ALTHOUGH HIGHER LEVELS WERE FOUND IN SKIN & LUNG.

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. V10 157 (1976)

Microsize - variable, ranging from 25 to 70% of an oral dose. Ultramicrosize - Almost completely absorbed. Absorption is significantly enhanced by administration with or after a fatty meal.

USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 1457

Griseofulvin is deposited in varying concentrations in the keratin layer of the skin, hair, and nails. It can be detected in the stratum corneum of the skin within a few hours following administration. Only a very small fraction of an oral dose is distributed in the body fluids and tissues.

USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 1457

Elimination: Renal. less than 1% of a dose is excreted as unchanged drug in the urine. Approximately 36% of griseofulvin is excreted unchanged in the feces.

USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 1457

GRISEOFULVIN IS PROBABLY DEPOSITED IN BASAL CELLS AND IS CARRIED OUTWARDS INTO EPIDERMIS AS NORMAL SKIN GROWTH PROCEEDS. THIS...MAKES FOR LONG LATENCY FROM TIME MEDICATION IS BEGUN UNTIL EVIDENCE OF IMPROVEMENT OCCURS.

Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 1166

5.6 Metabolism/Metabolites

Primarily hepatic with major metabolites being 6-methyl-griseofulvin and its glucuronide conjugate.

Griseofulvin is mainly metabolized to 6-dimethylgriseofulvin and its glucuronide.

Booth, N.H., L.E. McDonald (eds.). Veterinary Pharmacology and Therapeutics. 5th ed. Ames, Iowa: Iowa State University Press, 1982., p. 776

...IT HAS BEEN REPORTED THAT 6-DEMETHYLGRISEOFULVIN IS THE MAJOR URINARY METABOLITE...IN MAN, THE PREVIOUSLY REPORTED 4-DEMETHYL-GRISEOFULVIN WAS ABSENT. GRISEOFULVIC ACID (7-CHLORO-4,6-DIMETHOXY-6'-METHYLGRISAN-2',3,4'-TRIONE) WAS IDENTIFIED...

The Royal Society of Chemistry. Foreign Compound Metabolism in Mammals. Volume 6: A Review of the Literature Published during 1978 and 1979. London: The Royal Society of Chemistry, 1981., p. 275

5.7 Biological Half-Life

9-21 hours

DRUG HAS A HALF-LIFE IN PLASMA OF ABOUT 1 DAY, & APPROX 50% OF ORAL DOSE CAN BE DETECTED IN THE URINE WITHIN 5 DAYS, MOSTLY IN THE FORM OF METABOLITES /SRP: 36% IN THE FECES WITHIN 5 DAYS/.

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. 1173

The half-life of griseofulvin in canine plasma was found to be 47 minutes ... .

Booth, N.H., L.E. McDonald (eds.). Veterinary Pharmacology and Therapeutics. 5th ed. Ames, Iowa: Iowa State University Press, 1982., p. 775

5.8 Mechanism of Action

Griseofulvin is fungistatic, however the exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin. It binds to keratin in human cells, then once it reaches the fungal site of action, it binds to fungal microtubes thus altering the fungal process of mitosis.

Fungistatic; griseofulvin inhibits fungal cell mitosis by causing disruption of the mitotic spindle structure, thereby arresting the metaphase of cell division. It is deposited in varying concentrations in the keratin precursor cells of skin, hair, and nails, rendering the keratin resistant to fungal invasion. As the infected keratin is shed, it is replaced with healthy tissue.

USP Convention. USPDI-Drug Information for the Health Care Professional. 14th ed. Volume I. Rockville, MD: United States Pharmacopeial Convention, Inc., 1994. (Plus Updates)., p. 1457

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LIMITED","customerCountry":"INDIA","quantity":"1000.00","actualQuantity":"1000","unit":"KGS","unitRateFc":"70","totalValueFC":"70769.3","currency":"USD","unitRateINR":"5946.5","date":"29-Oct-2024","totalValueINR":"5946500","totalValueInUsd":"70769.3","indian_port":"JNPT","hs_no":"29419090","bill_no":"6390189","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"OFFICE,F,32\/F, PLAZA 88NO.88 YEUNG UK ROAD, TSUEN WAN,NT, HONG KONG SDNF CHINA","customerAddress":"501-502,AMBA SADAN,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q4","strtotime":1730226600,"product":"GRISEOFULVIN IP\/BP","address":"42,MAHANT ROAD,3,VILE PARLE","city":"MUMBAI,MAHARASHTRA","supplier":"SINOBRIGHT PHARMACEUTICAL COMPANY LTD","supplierCountry":"CHINA","foreign_port":"SHANGHAI","customer":"PRATISTHA PHARMA","customerCountry":"INDIA","quantity":"1000.00","actualQuantity":"1000","unit":"KGS","unitRateFc":"70","totalValueFC":"70797.5","currency":"USD","unitRateINR":"5948.9","date":"30-Oct-2024","totalValueINR":"5948868.41","totalValueInUsd":"70797.5","indian_port":"JNPT","hs_no":"29419090","bill_no":"6421366","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"SHANGHAI","supplierAddress":"OFFICE F,32\/F,PLAZA 88 NO.88 YEUNG UK ROAD,TSUEN WAN,NT,HONG KONG,CHIN A ., , CHINA CHINA","customerAddress":"42,MAHANT ROAD,3,VILE PARLE"}]

Number of Transactions

Total Quantity (KGS)

Total Value (USD)

Quantity (KGS) & Unit rate (USD/KGS) over time

API Imports and Exports

Importing Country	Total Quantity (KGS)	Average Price (USD/KGS)	Number of Transactions

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Drugs in Development

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DRUG PRODUCT COMPOSITIONS

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DOSAGE - TABLET;ORAL - 125MG

USFDA APPLICATION NUMBER - 50475

DOSAGE - TABLET;ORAL - 250MG

USFDA APPLICATION NUMBER - 50475

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Fillers, Diluents & Binders

Direct Compression

Coating Systems & Additives

Thickeners and Stabilizers

Lubricants & Glidants

Disintegrants & Superdisintegrants

Granulation

Controlled & Modified Release

Co-Processed Excipients

Solubilizers

Parenteral

Film Formers & Plasticizers

Taste Masking

Topical

Emulsifying Agents

Chewable & Orodispersible Aids

Rheology Modifiers

API Stability Enhancers

Surfactant & Foaming Agents

Coloring Agents

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CHEMISTRY

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ACTIVE PHARMA INGREDIENTS

12 API Suppliers

7 USDMF

2 CEP/COS

4 NDC API

5 Listed Suppliers

$ API Reference Price

DEVELOPMENTS

1 Drugs in Development

FINISHED DOSAGE FORMULATIONS

68 FDF Dossiers

38 FDA Orange Book

3 Europe

2 Australia

3 South Africa

22 Listed Dossiers

DRUG PRODUCT COMPOSITIONS

TABLET;ORAL - 125MG

TABLET;ORAL - 250MG

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5 Actylis

2 Aeon Procare

6 Anhui Sunhere Pharmaceutical Excipients Co.,Ltd

17 BASF

1 Clariant

5 Corel Pharma Chem

6 DFE Pharma

1 Finar

10 Gangwal Chemicals

4 Ideal Cures Pvt Ltd

3 Ingredion Pharma Solutions

28 Kerry

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16 Microlex e.U

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2 Novo Excipients

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1 Seppic

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11 Sigachi Industries

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4 Vasa Pharmachem

EXCIPIENTS BY APPLICATIONS

68 Fillers, Diluents & Binders

36 Direct Compression

30 Coating Systems & Additives

25 Thickeners and Stabilizers

23 Lubricants & Glidants

22 Disintegrants & Superdisintegrants

20 Granulation

16 Controlled & Modified Release

15 Co-Processed Excipients

15 Solubilizers

13 Parenteral

13 Film Formers & Plasticizers

11 Taste Masking

11 Topical

5 Emulsifying Agents

5 Chewable & Orodispersible Aids

5 Rheology Modifiers

3 API Stability Enhancers