List of Suppliers' Film Formers Plasticizers Excipients Application used in Mebendazole on PharmaCompass.com

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ACTIVE PHARMA INGREDIENTS

27 API Suppliers, 10 USDMF, 4 CEP/COS, 4 EU WC, 9 NDC API, 16 Listed Suppliers, $ API Reference Price

27 API Suppliers
10 USDMF
4 CEP/COS
4 EU WC
9 NDC API
16 Listed Suppliers
$ API Reference Price

FINISHED DOSAGE FORMULATIONS

51 FDF Dossiers, 3 FDA Orange Book, 12 Europe, 1 Canada, 2 Australia, 15 South Africa, 18 Listed Dossiers

51 FDF Dossiers
3 FDA Orange Book
12 Europe
1 Canada
2 Australia
15 South Africa
18 Listed Dossiers

RELATED EXCIPIENT COMPANIES

2 Rochem International Inc, 4 SPI Pharma, 2 DKSH, 1 Pharm-RX Chemical, 1 Boai NKY Pharmaceuticals Ltd, 12 Gangwal Healthcare, 1 Actylis, 1 Aeon Procare, 6 Anhui Sunhere Pharmaceutical Excipients Co.,Ltd, 16 BASF, 1 Bioplus Life Sciences, 4 DFE Pharma, 6 Gangwal Chemicals, 1 Ideal Cures Pvt Ltd, 3 Ingredion Pharma Solutions, 10 Kerry, 11 Microlex e.U, 1 Novo Excipients, 3 Pharmatrans-Sanaq, 5 Pluviaendo, 3 Prachin Chemical, 19 Roquette, 1 Seppic, 3 Shanghai Shenmei Pharmaceutical Technology Co., Ltd, 10 Sigachi Industries, 1 Ulanqab Kema New Material, 3 Vasa Pharmachem

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47 Fillers, Diluents & Binders, 29 Direct Compression, 20 Disintegrants & Superdisintegrants, 19 Lubricants & Glidants, 17 Granulation, 15 Thickeners and Stabilizers, 13 Co-Processed Excipients, 11 Coating Systems & Additives, 11 Taste Masking, 10 Controlled & Modified Release, 7 Film Formers & Plasticizers, 7 Solubilizers, 5 Chewable & Orodispersible Aids, 3 Emulsifying Agents, 2 Parenteral, 2 Topical, 1 API Stability Enhancers, 1 Surfactant & Foaming Agents, 1 Rheology Modifiers

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1 US Medicaid Prescriptions, 4 Finished Drug Prices

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23 APIs, 2 FDF Dossiers

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23 APIs
2 FDF Dossiers

REF. STANDARDS & IMPURITIES

2 EDQM , 2 USP , 2 Others

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2 EDQM
2 USP
2 Others

ANALYTICAL

1 BioAnalytical Methods

otherMethods
1 BioAnalytical Methods

Atman Mebendazole

Synopsis

ACTIVE PHARMA INGREDIENTS

API Suppliers

USDMF

CEP/COS

JDMF

EU WC

KDMF

NDC API

VMF

Listed Suppliers

API REF. PRICE (USD/KG)

$ 28

MARKET PLACE

API

FDF

0INTERMEDIATES

FINISHED DOSAGE FORMULATIONS

FDF Dossiers

FDA Orange Book

Europe

Canada

Australia

South Africa

Listed Dossiers

0 DRUGS IN DEVELOPMENT

DRUG PRODUCT COMPOSITIONS

REF. STANDARDS OR IMPURITIES

EDQM

USP

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131 RELATED EXCIPIENT COMPANIES

221EXCIPIENTS BY APPLICATIONS

Chemistry

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Also known as: 31431-39-7, Vermox, Pantelmin, Telmin, Mebenvet, Ovitelmin

Molecular Formula

C₁₆H₁₃N₃O₃

Molecular Weight

295.29 g/mol

InChI Key

OPXLLQIJSORQAM-UHFFFAOYSA-N

FDA UNII

81G6I5V05I

A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.

Mebendazole is an Anthelmintic.

1 2D Structure

Mebendazole

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

methyl N-(6-benzoyl-1H-benzimidazol-2-yl)carbamate

2.1.2 InChI

InChI=1S/C16H13N3O3/c1-22-16(21)19-15-17-12-8-7-11(9-13(12)18-15)14(20)10-5-3-2-4-6-10/h2-9H,1H3,(H2,17,18,19,21)

2.1.3 InChI Key

OPXLLQIJSORQAM-UHFFFAOYSA-N

2.1.4 Canonical SMILES

COC(=O)NC1=NC2=C(N1)C=C(C=C2)C(=O)C3=CC=CC=C3

2.2 Other Identifiers

2.2.1 UNII

81G6I5V05I

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Anti Worm

2. Anti-worm

3. Bantenol

4. Banworm

5. Boots Threadworm Treatment

6. Lomper

7. Madicure

8. Mebendan

9. Mebenvet

10. Pripsen Mebendazole

11. R17635

12. Sqworm

13. Sufil

14. Surfont

15. Telmin

16. Vermicol

17. Vermidil

18. Vermox

19. Wormkuur

2.3.2 Depositor-Supplied Synonyms

1. 31431-39-7

2. Vermox

3. Pantelmin

4. Telmin

5. Mebenvet

6. Ovitelmin

7. Vermicidin

8. Vermirax

9. Mebenoazole

10. Bantenol

11. Mebutar

12. Lomper

13. Mbdz

14. Besantin

15. Verpanyl

16. Noverme

17. Mebendazolum

18. Methyl (5-benzoyl-1h-benzo[d]imidazol-2-yl)carbamate

19. 5-benzoyl-2-benzimidazolecarbamic Acid Methyl Ester

20. Methyl 5-benzoyl-2-benzimidazolecarbamate

21. Carbamic Acid, (5-benzoyl-1h-benzimidazol-2-yl)-, Methyl Ester

22. Methyl 5-benzoyl-2-benzimidazolylcarbamate

23. R 17,635

24. Methyl N-(6-benzoyl-1h-benzimidazol-2-yl)carbamate

25. R 17635

26. Methyl (5-benzoyl-1h-benzimidazol-2-yl)carbamate

27. Methyl 5-benzoyl Benzimidazole-2-carbamate

28. (5-benzoyl-1h-benzimidazol-2-yl)-carbamic Acid Methyl Ester

29. Mfcd00057872

30. Methyl N-(5-benzoyl-1h-benzimidazol-2-yl)carbamate

31. Zhihuanqing

32. Ccris 4479

33. Methyl N-(6-benzoyl-1h-1,3-benzodiazol-2-yl)carbamate

34. Nsc 184849

35. 2-benzimidazolecarbamic Acid, 5-benzoyl-, Methyl Ester

36. Mebendazole Polymorph C

37. Mebendazol

38. Sufil

39. Chembl685

40. Nsc-184849

41. N-2 (5-benzoyl-benzimidazole) Carbamate De Methyle

42. N-(benzoyl-5, Benzimidazolyl)-2, Carbamate De Methyle

43. Chebi:6704

44. Carbamic Acid, N-(5-benzoylbenzimidazol-2-yl)-, Methyl Ester

45. Versid

46. Methyl 6-benzoyl-1h-benzimidazol-2-ylcarbamate

47. 81g6i5v05i

48. R-17635

49. 5-benzoyl-2-benzimidazolecarbamic Acid, Methyl Ester

50. Nsc184849

51. Methyl [5-(phenylcarbonyl)-1h-benzimidazol-2-yl]carbamate

52. Ncgc00016806-01

53. (5-benzoyl-1h-benzimidazol-2-yl)carbamic Acid Methyl Ester

54. Mebex

55. Cas-31431-39-7

56. Equivurm Plus

57. Dsstox_cid_20682

58. Dsstox_rid_79538

59. Dsstox_gsid_40682

60. Mebendazol [inn-spanish]

61. Mebendazolum [inn-latin]

62. Vermox (tn)

63. Emverm

64. Smr000036734

65. Hsdb 3232

66. Sr-01000003109

67. Einecs 250-635-4

68. Methyl N-(5-benzoyl-2-benzimidazolyl)carbamate

69. Mebatreat

70. Mebendazole (jan/usp/inn)

71. Unii-81g6i5v05i

72. Equivurmp Plus

73. N-2 (5-benzoyl-benzimidazole) Carbamate De Methyle [french]

74. Mebendazole,(s)

75. N-(benzoyl-5, Benzimidazolyl)-2, Carbamate De Methyle [french]

76. V95

77. Prestwick_310

78. Mebendazole; 4030

79. Mebendazole [usan:usp:inn:ban:jan]

80. Spectrum_001298

81. Cpd000036734

82. Prestwick0_000217

83. Prestwick1_000217

84. Prestwick2_000217

85. Prestwick3_000217

86. Spectrum2_001401

87. Spectrum3_001439

88. Spectrum4_000416

89. Spectrum5_001381

90. Mebendazole [inn]

91. Mebendazole [jan]

92. Mebendazole [hsdb]

93. Mebendazole [usan]

94. Probes1_000013

95. Probes2_000149

96. Mebendazole [vandf]

97. Cambridge Id 5250893

98. Methyl [5-(benzoyl)benzimidazol-2-yl]carbamate

99. Timtec1_000869

100. Mebendazole [mart.]

101. Oprea1_278237

102. Oprea1_768530

103. Schembl15860

104. Bspbio_000233

105. Bspbio_003178

106. Cbdive_010559

107. Kbiogr_000712

108. Kbioss_001778

109. Mebendazole [usp-rs]

110. Mebendazole [who-dd]

111. Mebendazole [who-ip]

112. Mls000028491

113. Mls006011879

114. Bidd:gt0087

115. Divk1c_000751

116. Mebendazolum [who-ip]

117. Spectrum1501110

118. Spbio_001442

119. Spbio_002154

120. Bpbio1_000257

121. Methyl N-[6-(benzoyl)-1h-benzimidazol-2-yl]carbamate

122. Dtxsid4040682

123. Mebendazole [green Book]

124. Hms502f13

125. Kbio1_000751

126. Kbio2_001778

127. Kbio2_004346

128. Kbio2_006914

129. Kbio3_002398

130. Mebendazole [orange Book]

131. Mebendazole For System Suitability

132. Ninds_000751

133. 2-benzimidazolecarbamic Acid, 5-benzoyl-, Methyl Ester (8ci)

134. Hms1536h11

135. Hms1568l15

136. Hms1921f03

137. Hms2090b03

138. Hms2092b15

139. Hms2095l15

140. Hms3259b11

141. Hms3604n11

142. Hms3712l15

143. Mebendazole [ep Monograph]

144. Mebendazole [usp Impurity]

145. Pharmakon1600-01501110

146. Zinc121541

147. Mebendazole [usp Monograph]

148. Tox21_110620

149. Bbl008298

150. Bdbm50180753

151. Ccg-39628

152. Mmv003152

153. Nsc757838

154. S4610

155. Stk093862

156. Akos000539066

157. Akos015896232

158. Carbamic Acid, (5-benzoyl-1h-benzimidazol-2-yl)-, Methyl Ester (9ci)

159. Tox21_110620_1

160. Cs-3974

161. Db00643

162. Mebendazole 100 Microg/ml In Methanol

163. Nc00639

164. Nsc-757838

165. Idi1_000751

166. Mebendazole Polymorph C [usp-rs]

167. Ncgc00016806-02

168. Ncgc00016806-03

169. Ncgc00016806-04

170. Ncgc00016806-05

171. Ncgc00016806-06

172. Ncgc00016806-07

173. Ncgc00016806-08

174. Ncgc00016806-09

175. Ncgc00016806-10

176. Ncgc00016806-12

177. Ncgc00016806-13

178. Ncgc00021698-03

179. Ncgc00021698-04

180. Ncgc00021698-05

181. Ncgc00021698-06

182. Ncgc00021698-07

183. Ac-12064

184. As-12272

185. Hy-17595

186. Sy051142

187. Sbi-0051641.p002

188. Ab00052203

189. Ft-0628179

190. Ft-0628180

191. M2273

192. En300-50844

193. D00368

194. D70118

195. 5-benzoyl-2-benzimidazolylcarbamicacidmethylester

196. Ab00052203-09

197. Ab00052203_10

198. Mebendazole, Vetranal(tm), Analytical Standard

199. 431m397

200. A820852

201. Ag-205/04588045

202. Mebendazole, Analytical Standard, >=98% (hplc)

203. Methyl (6-benzoyl-1h-benzimidazol-2-yl)carbamate

204. Q422194

205. Methyl 5-benzoyl-1h-benzo[d]imidazol-2-ylcarbamate

206. Sr-01000003109-2

207. Sr-01000003109-3

208. W-106901

209. Brd-k77987382-001-01-7

210. Brd-k77987382-001-06-6

211. Brd-k77987382-001-08-2

212. Sr-01000003109-10

213. Methyl N-(5-benzoyl-1h-1,3-benzimidazol-2-yl)carbamate

214. Z234895185

215. 5-benzoyl-1h-benzimidazol-2-yl Carbamic Acid Methyl Ester;

216. Mebendazole, European Pharmacopoeia (ep) Reference Standard

217. Mebendazole, United States Pharmacopeia (usp) Reference Standard

218. Mebendazole For System Suitability, European Pharmacopoeia (ep) Reference Standard

219. Mebendazole Polymorph C, United States Pharmacopeia (usp) Reference Standard

2.4 Create Date

2005-03-25

3 Chemical and Physical Properties

Molecular Formula	C₁₆H₁₃N₃O₃
Molecular Weight	295.29 g/mol
XLogP3	2.8
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	4
Exact Mass	295.09569129 g/mol
Monoisotopic Mass	295.09569129 g/mol
Topological Polar Surface Area	84.1 Å²
Heavy Atom Count	22
Formal Charge	0
Complexity	423
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
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 2
Drug Name	Mebendazole
PubMed Health	Mebendazole (By mouth)
Drug Classes	Anthelmintic
Drug Label	Mebendazole is a (synthetic) broad-spectrum anthelmintic available as chewable tablets, each containing 100 mg of mebendazole. Inactive ingredients are: anhydrous lactose NF, corn starch, magnesium stearate, microcrystalline cellulose, sodium lauryl...
Active Ingredient	Mebendazole
Dosage Form	Tablet, chewable
Route	Oral
Strength	100mg
Market Status	Prescription
Company	Amedra Pharms

2 of 2
Drug Name	Mebendazole
PubMed Health	Mebendazole (By mouth)
Drug Classes	Anthelmintic
Drug Label	Mebendazole is a (synthetic) broad-spectrum anthelmintic available as chewable tablets, each containing 100 mg of mebendazole. Inactive ingredients are: anhydrous lactose NF, corn starch, magnesium stearate, microcrystalline cellulose, sodium lauryl...
Active Ingredient	Mebendazole
Dosage Form	Tablet, chewable
Route	Oral
Strength	100mg
Market Status	Prescription
Company	Amedra Pharms

4.2 Therapeutic Uses

Mesh Heading: Antinematodal agents

National Library of Medicine, SIS; ChemIDplus Record for Mebendazole (31431-39-7). Available from, as of April 17, 2006: https://chem.sis.nlm.nih.gov/chemidplus/chemidlite.jsp

Mebendazole is indicated as a primary agent for tichuriasis caused by Trichuris trichiura (whipworm). /Included in US product labeling/

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1992

Mebendazole is indicated in the treatment of multiple intestinal roundworm infections. /Included in US product labeling/

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1992

Mebendazole is indicated a a primary agent for enterobiasis caused by Enterobius vermicularis (pinworm). /Included in US product labeling/

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1992

For more Therapeutic Uses (Complete) data for MEBENDAZOLE (19 total), please visit the HSDB record page.

4.3 Drug Warning

Organ system function (including hematopoietic and hepatic) should be assessed periodically during prolonged mebendazole therapy.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

Other adverse effects reported rarely in patients receiving mebendazole include alopecia, rash, pruritus, urticaria, angioedema, flushing, hiccups, cough, weakness,drowsiness, chills, hypotension, seizures, transient abnormalities in liver function tests (e.g., increased serum concentrations of aminotransferases, alkaline phosphatase, and/or bilirubin), hepatitis, increased BUN, decreased hemoglobin concentration and/or hematocrit, leukopenia, thrombocytopenia, eosinophilia, hematuria, and cylindruria.Migration of roundworms through the mouth and nose also has been reported.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

Myelosuppression manifested as neutropenia (including agranulocytosis) and/or thrombocytopenia also has been reported in patients receiving high-dose (e.g., 30-50 mg/kg daily) mebendazole therapy for extraintestinal infections; while the myelosuppression usually was reversible following discontinuance of the drug, death has occurred rarely.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

At usual recommended dosages (i.e., 100-200 mg daily), mebendazole appears to cause minimal adverse effects. Adverse effects appear to occur more frequently when higher dosages (e.g., those used in the treatment of extraintestinal infections such as hydatid disease) are used, and may be related to effects resulting from drug-induced killing of the parasites in some cases. Transient diarrhea and abdominal pain have occurred occasionally during mebendazole treatment, but usually have been associated with massive infections and expulsion of the helminths. Nausea, vomiting, headache, tinnitus, numbness, and dizziness also have been reported occasionally during mebendazole therapy. Fever has occurred in some patients, particularly in those receiving high-dose therapy for extraintestinal infections.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

For more Drug Warnings (Complete) data for MEBENDAZOLE (9 total), please visit the HSDB record page.

4.4 Drug Indication

For the treatment of Enterobius vermicularis (pinworm), Trichuris trichiura (whipworm), Ascaris lumbricoides (common roundworm), Ancylostoma duodenale (common hookworm), Necator americanus (American hookworm) in single or mixed infections.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Mebendazole is a (synthetic) broad-spectrum anthelmintic. The principal mode of action for Mebendazole is by its inhibitory effect on tubulin polymerization which results in the loss of cytoplasmic microtubules.

5.2 MeSH Pharmacological Classification

Antinematodal Agents

Substances used in the treatment or control of nematode infestations. They are used also in veterinary practice. (See all compounds classified as Antinematodal Agents.)

Tubulin Modulators

Agents that interact with TUBULIN to inhibit or promote polymerization of MICROTUBULES. (See all compounds classified as Tubulin Modulators.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

MEBENDAZOLE

5.3.2 FDA UNII

81G6I5V05I

5.3.3 Pharmacological Classes

Anthelmintic [EPC]

5.4 ATC Code

P02CA01

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

P - Antiparasitic products, insecticides and repellents

P02 - Anthelmintics

P02C - Antinematodal agents

P02CA - Benzimidazole derivatives

P02CA01 - Mebendazole

5.5 Absorption, Distribution and Excretion

Absorption

Poorly absorbed (approximately 5 to 10%) from gastrointestinal tract. Fatty food increases absorption.

Route of Elimination

In man, approximately 2% of administered mebendazole is excreted in urine and the remainder in the feces as unchanged drug or a primary metabolite.

Elimination: Fecal: Approximately 95% excreted unchanged or as the primary metabolite (2-amino derivative) in feces. Renal: Approximately 2 to 5% excreted unchanged or as the primary metabolite in urine.

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1993

Peak serum concentration: Following a dose of 100 mg twice a day for 3 days: Mebendazole: Not more than 0.03 ug/mL. 2-Amino metabolite: Not more than 0.09 ug/mL. Serum concentrations up to 0.5 ug/mL have been reported in chronic, high-dose therapy.

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1993

Time to peak serum concentration: 2 to 5 hours (range: 0.5 to 7 hours).

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1993

Mebendazole is highly bound to plasma proteins. It is not known if mebendazole is distributed into milk.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

For more Absorption, Distribution and Excretion (Complete) data for MEBENDAZOLE (11 total), please visit the HSDB record page.

5.6 Metabolism/Metabolites

Primarily hepatic. Primary metabolite is 2-amino-5-benzoylbenzimidazole, but also metabolized to inactive hydroxy and hydroxyamino metabolites. All metabolites are devoid of anthelmintic activity.

Primarily hepatic; metabolized in inactive amino, hydroxy, and hydroxyamino metabolites; primary metabolite is 2-amino-5-benzoylbenzimidazole.

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1993

Although the exact metabolic fate of mebendazole has not been fully determined, the drug is metabolized via decarboxylation to 2-amino-5(6)-benzimidazolyl phenylketone; this metabolite does not have anthelmintic activity.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

Mebendazole ... is extensively metabolized. Two major metabolites, methyl-5-(alpha-5-hydroxybenzyl)-2-benzimidazole carbamate and 2-amino-5-benzoylbenzimidazole, have lower rates of clearance than does mebendazole itself. Mebendazole, rather than its metabolites, appears to be the active drug form. Conjugates of mebendazole and its metabolites have been found in bile, but little unchanged mebendazole appears in the urine.

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 1126

5.7 Biological Half-Life

2.5 to 5.5 hours (range 2.5 to 9 hours) in patients with normal hepatic function. Approximately 35 hours in patients with impaired hepatic function (cholestasis).

Normal hepatic function: 2.5 to 5.5 hours (range: 2.5 to 9 hours). Impaired hepatic function (cholestasis): Approximately 35 hours.

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1993

The elimination half-life of mebendazole has been reported to be about 2.8-9 hours.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

5.8 Mechanism of Action

Mebendazole causes degenerative alterations in the tegument and intestinal cells of the worm by binding to the colchicine-sensitive site of tubulin, thus inhibiting its polymerization or assembly into microtubules. The loss of the cytoplasmic microtubules leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen stores. Degenerative changes in the endoplasmic reticulum, the mitochondria of the germinal layer, and the subsequent release of lysosomes result in decreased production of adenosine triphosphate (ATP), which is the energy required for the survival of the helminth. Due to diminished energy production, the parasite is immobilized and eventually dies.

Although the exact mechanism of anthelmintic activity of mebendazole has not been fully elucidated, the drug appears to cause selective and irreversible inhibition of the uptake of glucose and other low molecular weight nutrients in susceptible helminths; inhibition of glucose uptake appears to result in endogenous depletion of glycogen stores in the helminth. Mebendazole does not inhibit glucose uptake in mammals. Mebendazole appears to cause degenerative changes in the intestine of nematodes and in the absorptive cells of cestodes. The principal anthelmintic effect of the drug appears to be degeneration of cytoplasmic microtubules within these intestinal and absorptive cells. Microtubular deterioration results in inhibition of organelle movement and interferes with the absorptive and secretory function. As a result of excessive accumulation of intracellular transport secretory granules, hydrolytic and proteolytic enzymes are released and cause cellular autolysis. This irreversible damage leads to death of the parasite.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 53

Vermicidal; may also be ovicidal for ova or most helminths; mebendazole causes degeneration of parasite's cytoplasmic microtubules and thereby selectively and irreversibly blocks glucose uptake in susceptible adult intestine-dwelling helminths and their tissue-dwelling larvae; inhibition of glucose uptake apparently results in depletion of the parasite's glycogen stores; this, in turn, results in reduced formation of adenosine triphosphate (ATP) required for survival and reproduction of the helminth; corresponding energy levels are gradually reduced until death of the parasite ensues; mebendazole does not appear to affect serum glucose concentrations in humans, however.

Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2006., p. 1993

Benzimidazoles produce many biochemical changes in susceptible nematodes, eg, inhibition of mitochondrial fumarate reductase, reduced glucose transport, and uncoupling of oxidative phosphorylation ... /but/ the primary action ... /should be/ to inhibit microtubule polymerization by binding to beta-tubulin. The selective toxicity of these agents derives from the fact that specific, high-affinity binding to parasite beta-tubulin occurs at much lower concn than does binding to the mammalian protein ... Benzimidazole-resistant Haemonchus contortus display reduced high-affinity drug binding to beta-tubulin and alterations in beta-tubulin isotype gene expression that correlate with drug resistance ... Two identified mechanisms of drug resistance in nematodes involve both a progressive loss of "susceptible" beta-tubulin gene isotypes together with emergence of a "resistant" isotype with a conserved point mutation that encodes a tyrosine instead of phenylalanine at position 200 of beta-tubulin. While this mutation may not be required for benzimidazole resistance in all parasites, eg, Giardia lamblia, benzimidazole resistance in parasitic nematodes is unlikely to be overcome by novel benzimidazole analogs, because tyrosine also is present at position 200 of human beta-tubulin. /Benzimidazoles/

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 1126

API SUPPLIERS

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USDMF

01

Cadila Laboratories Pvt Ltd

India

Discovery on Target

Not Confirmed

Not Confirmed

05

Janssen Pharmaceutica Nv

U.S.A

Discovery on Target

Not Confirmed

06

Msn Life Sciences Private Ltd

India

Discovery on Target

Not Confirmed

07

Msn Life Sciences Private Ltd

India

Discovery on Target

Not Confirmed

08

Optimus Drugs Private Ltd

India

Discovery on Target

Not Confirmed

09

Shaanxi Hanjiang Pharmaceutical Grou...

China

Discovery on Target

Not Confirmed

10

Solara Active Pharma Sciences Ltd

India

Discovery on Target

Not Confirmed

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CEP/COS

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EU WC

01

Cipla

India

India

Discovery on Target

Not Confirmed

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NDC API

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Listed Suppliers

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API Reference Price

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