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Chemistry

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Also known as: 54965-21-8, Albenza, Eskazole, Zentel, Valbazen, Proftril
Molecular Formula
C12H15N3O2S
Molecular Weight
265.33  g/mol
InChI Key
HXHWSAZORRCQMX-UHFFFAOYSA-N
FDA UNII
F4216019LN

Albendazole
A benzimidazole broad-spectrum anthelmintic structurally related to MEBENDAZOLE that is effective against many diseases. (From Martindale, The Extra Pharmacopoeia, 30th ed, p38)
Albendazole is an Anthelmintic. The mechanism of action of albendazole is as a Cytochrome P450 1A Inducer.
1 2D Structure

Albendazole

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
methyl N-(6-propylsulfanyl-1H-benzimidazol-2-yl)carbamate
2.1.2 InChI
InChI=1S/C12H15N3O2S/c1-3-6-18-8-4-5-9-10(7-8)14-11(13-9)15-12(16)17-2/h4-5,7H,3,6H2,1-2H3,(H2,13,14,15,16)
2.1.3 InChI Key
HXHWSAZORRCQMX-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CCCSC1=CC2=C(C=C1)N=C(N2)NC(=O)OC
2.2 Other Identifiers
2.2.1 UNII
F4216019LN
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Albendazole Monohydrochloride

2. Albendoral

3. Albenza

4. Andazol

5. Bendapar

6. Bilutac

7. Digezanol

8. Disthelm

9. Endoplus

10. Eskazole

11. Gascop

12. Lurdex

13. Mediamix V Disthelm

14. Metiazol

15. Monohydrochloride, Albendazole

16. Sk And F 62979

17. Sk And F-62979

18. Sk And F62979

19. Skf 62979

20. Skf-62979

21. Skf62979

22. Valbazen

23. Zentel

2.3.2 Depositor-Supplied Synonyms

1. 54965-21-8

2. Albenza

3. Eskazole

4. Zentel

5. Valbazen

6. Proftril

7. Albendazolum

8. Andazol

9. Sk&f 62979

10. Methyl 5-(propylthio)-2-benzimidazolecarbamate

11. Skf 62979

12. Sk&f-62979

13. 5-(propylthio)-2-carbomethoxyaminobenzimidazole

14. Skf-62979

15. Methyl N-[6-(propylsulfanyl)-1h-1,3-benzodiazol-2-yl]carbamate

16. Methyl N-(6-propylsulfanyl-1h-benzimidazol-2-yl)carbamate

17. (5-(propylthio)-1h-benzimidazol-2-yl)carbamic Acid Methyl Ester

18. O-methyl N-(5-(propylthio)-2-benzimidazolyl)carbamate

19. Nsc 220008

20. Carbamic Acid, [5-(propylthio)-1h-benzimidazol-2-yl]-, Methyl Ester

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

22. Albendazol

23. Bilutac

24. Nsc-220008

25. Chembl1483

26. Methyl [5-(propylsulfanyl)-1h-benzimidazol-2-yl]carbamate

27. Methyl [6-(propylsulfanyl)-1h-benzimidazol-2-yl]carbamate

28. ((propylthio)-5 1h-benzimidazolyl-2) Carbamate De Methyle

29. Chebi:16664

30. Zental

31. F4216019ln

32. Ncgc00016876-01

33. Cas-54965-21-8

34. Dsstox_cid_2563

35. Dsstox_rid_76632

36. Dsstox_gsid_22563

37. Albendazol [inn-spanish]

38. Albendazolum [inn-latin]

39. Methyl [5-(propylthio)-1h-benzimidazol-2-yl]carbamate

40. Methyl 5-(propylthio)-1h-benzo[d]imidazol-2-ylcarbamate

41. Methyl [5-(propylthio)benzimidazol-2-yl]carbamate

42. Methyl N-(5-propylsulfanyl-1h-benzimidazol-2-yl)carbamate

43. Methyl N-[5-(propylsulfanyl)-1h-1,3-benzodiazol-2-yl]carbamate

44. Methyl (nz)-n-(5-propylsulfanyl-1,3-dihydrobenzimidazol-2-ylidene)carbamate

45. Albenza (tn)

46. Hsdb 7444

47. Einecs 259-414-7

48. Mfcd00083232

49. Albendazole (jan/usp/inn)

50. Zenteltrade Mark

51. [5-(propylthio)benzimidazol-2-yl]carbamic Acid Methyl Ester

52. Albenzatrade Mark

53. Andazoltrade Mark

54. Unii-f4216019ln

55. Eskazoletrade Mark

56. Albendazole,(s)

57. ((propylthio)-5 1h-benzimidazolyl-2) Carbamate De Methyle [french]

58. Prestwick_675

59. Albendazole(albenza)

60. Albendazole (albenza)

61. Albendazole [usan:usp:inn:ban:jan]

62. Spectrum_001532

63. Cpd000036735

64. Albendazole [mi]

65. (5-propylsulfanyl-1h-benzoimidazol-2-yl)-carbamic Acid Methyl Ester

66. Prestwick0_000247

67. Prestwick1_000247

68. Prestwick2_000247

69. Prestwick3_000247

70. Spectrum4_000201

71. Spectrum5_001567

72. Albendazole [inn]

73. Albendazole [jan]

74. Chemdivam_000003

75. Chemdiv1_000190

76. Albendazole [hsdb]

77. Albendazole [usan]

78. Albendazole [vandf]

79. Albendazole [mart.]

80. Oprea1_429292

81. Oprea1_585016

82. Oprea1_640007

83. Schembl44682

84. Albendazole [usp-rs]

85. Albendazole [who-dd]

86. Albendazole [who-ip]

87. Bspbio_000034

88. Bspbio_002548

89. Kbiogr_000801

90. Kbioss_002012

91. Mls000069722

92. Albendazolum [who-ip]

93. Bidd:gt0615

94. Divk1c_000704

95. Spectrum1503903

96. Methoxy-n-(5-propylthiobenzimidazol-2-yl)carboxamide

97. Spbio_002253

98. Bpbio1_000038

99. Albendazole [green Book]

100. Dtxsid0022563

101. Hms502d06

102. Hms587i14

103. Hxhwsazorrcqmx-uhfffaoysa-

104. Kbio1_000704

105. Kbio2_002012

106. Kbio2_004580

107. Kbio2_007148

108. Albendazole [orange Book]

109. Ninds_000704

110. Albendazole [ep Monograph]

111. Hms1568b16

112. Hms1922k04

113. Hms2090g19

114. Hms2093k13

115. Hms2095b16

116. Hms2231o03

117. Hms3259b05

118. Hms3369c03

119. Hms3651c15

120. Hms3712b16

121. Pharmakon1600-01503903

122. Albendazole [usp Monograph]

123. [5-(propythio)-1h-benzimidazol-2-yl]carbamic Acid Methyl Ester

124. Bcp12108

125. Hy-b0223

126. Tox21_110659

127. Tox21_302300

128. Ac-015

129. Bbl005883

130. Bdbm50241293

131. Ccg-39620

132. Mfcd01220143

133. N-[6-(propylthio)-1h-benzimidazol-2-yl]carbamic Acid Methyl Ester

134. Nsc220008

135. Nsc758644

136. S1640

137. Stk387550

138. Stl046130

139. Zinc17146904

140. Akos000540882

141. Akos005431684

142. Akos005699352

143. Tox21_110659_1

144. Albendazole 100 Microg/ml In Methanol

145. Ccg-220247

146. Db00518

147. Ks-5159

148. Nc00615

149. Nsc-758644

150. Idi1_000704

151. Methyl [(2z)-5-(propylsulfanyl)-1,3-dihydro-2h-benzimidazol-2-ylidene]carbamate

152. Ncgc00016876-02

153. Ncgc00016876-03

154. Ncgc00016876-04

155. Ncgc00016876-05

156. Ncgc00016876-06

157. Ncgc00016876-07

158. Ncgc00016876-08

159. Ncgc00016876-09

160. Ncgc00016876-10

161. Ncgc00016876-12

162. Ncgc00022896-03

163. Ncgc00022896-04

164. Ncgc00022896-05

165. Ncgc00022896-06

166. Ncgc00022896-07

167. Ncgc00022896-08

168. Ncgc00255250-01

169. Albendazole, Analytical Standard, >=98%

170. Smr000036735

171. Albendazole 100 Microg/ml In Acetonitrile

172. Sbi-0051849.p002

173. Db-052669

174. Ab00052377

175. Ft-0621945

176. Sw196830-3

177. En300-49850

178. Methyl 5-propylthio-2-benzimidazole Carbamate

179. Vu0239747-6

180. Bim-0051849.0001

181. C01779

182. D00134

183. H10782

184. Ab00052377-13

185. Ab00052377-14

186. Ab00052377_15

187. Ab00052377_16

188. A830429

189. Albendazole, Antibiotic For Culture Media Use Only

190. Q411629

191. Sr-01000000171

192. Sr-05000001875

193. Methyl 5-(propylthio)-1h-benzimidazol-2-ylcarbamate

194. Q-200603

195. Q-200604

196. Sr-01000000171-2

197. Sr-05000001875-1

198. Brd-k79131256-001-04-7

199. Brd-k79131256-001-08-8

200. Methyl 5-(propylthio)benzimidazol-2-ylcarbamate

201. Methyl 6-(propylthio)-1h-benzo[d]imidazol-2-ylcarbamate

202. Z1245635850

203. 2-[(methoxycarbonyl)amino]-5-propylthio-1h-benzimidazole

204. Albendazole, European Pharmacopoeia (ep) Reference Standard

205. Methyl (6-(propylthio)-1h-benzo[d]imidazol-2-yl)carbamate

206. Methyl 5-(propylsulfanyl)-1h-benzimidazol-2-ylcarbamate #

207. Albendazole, United States Pharmacopeia (usp) Reference Standard

208. Methyl N-(5-(propylthio)-1h-benzimidazol-2-yl)carbamate

209. Albendazole, Pharmaceutical Secondary Standard; Certified Reference Material

210. Carbamic Acid, N-[5-(propylthio)-1h-benzimidazol-2-yl]-,?methyl Ester

2.4 Create Date
2004-09-16
3 Chemical and Physical Properties
Molecular Weight 265.33 g/mol
Molecular Formula C12H15N3O2S
XLogP32.9
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count4
Rotatable Bond Count5
Exact Mass265.08849790 g/mol
Monoisotopic Mass265.08849790 g/mol
Topological Polar Surface Area92.3 Ų
Heavy Atom Count18
Formal Charge0
Complexity291
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 2  
Drug NameAlbenza
PubMed HealthAlbendazole (By mouth)
Drug ClassesAnthelmintic
Drug LabelALBENZA (albendazole) is an orally administered broad-spectrum anthelmintic. Chemically, it is methyl 5-(propylthio)-2-benzimidazolecarbamate. Its molecular formula is C12H15N3O2S. Its molecular weight is 265.34. It has the following chemical structu...
Active IngredientAlbendazole
Dosage FormTablet
RouteOral
Strength200mg
Market StatusPrescription
CompanyAmedra Pharms

2 of 2  
Drug NameAlbenza
PubMed HealthAlbendazole (By mouth)
Drug ClassesAnthelmintic
Drug LabelALBENZA (albendazole) is an orally administered broad-spectrum anthelmintic. Chemically, it is methyl 5-(propylthio)-2-benzimidazolecarbamate. Its molecular formula is C12H15N3O2S. Its molecular weight is 265.34. It has the following chemical structu...
Active IngredientAlbendazole
Dosage FormTablet
RouteOral
Strength200mg
Market StatusPrescription
CompanyAmedra Pharms

4.2 Therapeutic Uses

Mesh Headings: anthelmintics, anticestodalagents, antiprotozoal agents

National Library of Medicine, SIS; ChemIDplus Record for Albendazole (54965-21-8). Available from, as of April 13, 2006: https://chem.sis.nlm.nih.gov/chemidplus/chemidlite.jsp


Albendazole is a benzimidazole carbamate, used for the treatment of gastrointestinal infestations with roundworms, lungworms and tapeworms and adult flukes of Fasciola hepatica.

European Medicines Agency (EMEA), The European Agency for the Evaluation of Medicinal Products, Veterinary Medicines Evaluation Unit, Committee for Veterinary Medicinal Products; Albendazole, Summary Report(3). EMEA/MRL/865/03-Final (June 2004). Available from, as of July 25, 2006: https://www.ema.europa.eu/ema/index.jsp?curl=pages/document_library/landing/document_library_search.jsp&murl=menus/document_library/document_library.jsp&mid


Certain microsporidial species that cause intestinal infections in people with AIDS respond partially (Enterocytozoon bieneusi) or completely (Encephalitozoon intestintalis and related Encephalitozoon species) to albendazole; albendazole's sulfoxide metabolite appears to be especially effective against these parasites in vitro.

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


MEDICATION: ...Used against nematode infections: Ascaris, Necator, Ancylostoma, Trichuris, Enterobius, and systemic nematodes such as Trichinella spiralis, Gnathostoma spinigerum, and larval Angiostrongylus cantonensis. In addition it is used against the larval stages of the cestodes Echinococcus granulosus and E. multilocularis and for treatment of neurocysticercosis caused by Taenia solium.

Ullmann's Encyclopedia of Industrial Chemistry. 6th ed.Vol 1: Federal Republic of Germany: Wiley-VCH Verlag GmbH & Co. 2003 to Present, p. V. 3 185 (2003)


For more Therapeutic Uses (Complete) data for ALBENDAZOLE (21 total), please visit the HSDB record page.


4.3 Drug Warning

Leukopenia has occurred in less than 1% of patients receiving albendazole, and rarely, granulocytopenia, pancytopenia, agranulocytosis, or thrombocytopenia have been reported. Therefore, blood counts should be performed at the start of, and every 2 weeks during, each 28-day treatment cycle. The manufacturer states that if decreases in the total leukocyte count occur, treatment with albendazole may be continued if the decreases are modest and do not progress.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 46


Because albendazole has been associated with mild to moderate increases of hepatic enzymes in about 16% of patients receiving the drug in clinical trials, and may cause hepatotoxicity, liver function tests should be performed prior to each course of albendazole therapy and at least every 2 weeks during treatment with the drug. If clinically important increases in liver function test results occur, albendazole should be discontinued. The drug can be reinstituted when liver enzymes return to pretreatment levels, but laboratory tests should be performed frequently during repeat therapy.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 46


Albendazole may cause harm to the fetus and should be used during pregnancy only if the benefits justify the risk to the fetus and only in clinical circumstances where no alternative management is appropriate. Women of childbearing age should begin treatment only after a negative pregnancy test, and should be cautioned against becoming pregnant while receiving albendazole or within 1 month of completing treatment with the drug.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 46


Teratogenic in animals (rats and rabbits) and is not recommended in pregnancy or in infants younger than 2 years.

Haddad, L.M. (Ed). Clinical Management of Poisoning and Drug Overdose 3rd Edition. Saunders, Philadelphia, PA. 1998., p. 714


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


4.4 Drug Indication

For the treatment of parenchymal neurocysticercosis due to active lesions caused by larval forms of the pork tapeworm, Taenia solium and for the treatment of cystic hydatid disease of the liver, lung, and peritoneum, caused by the larval form of the dog tapeworm, Echinococcus granulosus.


5 Pharmacology and Biochemistry
5.1 Pharmacology

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


5.2 MeSH Pharmacological Classification

Anthelmintics

Agents that kill parasitic worms. They are used therapeutically in the treatment of HELMINTHIASIS in man and animal. (See all compounds classified as Anthelmintics.)


Anticestodal Agents

Agents used to treat tapeworm infestations in man or animals. (See all compounds classified as Anticestodal Agents.)


Tubulin Modulators

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


Antiprotozoal Agents

Substances that are destructive to protozoans. (See all compounds classified as Antiprotozoal Agents.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
ALBENDAZOLE
5.3.2 FDA UNII
F4216019LN
5.3.3 Pharmacological Classes
Cytochrome P450 1A Inducers [MoA]; Anthelmintic [EPC]
5.4 ATC Code

P - Antiparasitic products, insecticides and repellents

P02 - Anthelmintics

P02C - Antinematodal agents

P02CA - Benzimidazole derivatives

P02CA03 - Albendazole


5.5 Absorption, Distribution and Excretion

Absorption

Poorly absorbed from the gastrointestinal tract due to its low aqueous solubility. Oral bioavailability appears to be enhanced when coadministered with a fatty meal (estimated fat content 40 g)


Route of Elimination

Albendazole is rapidly converted in the liver to the primary metabolite, albendazole sulfoxide, which is further metabolized to albendazole sulfone and other primary oxidative metabolites that have been identified in human urine. Urinary excretion of albendazole sulfoxide is a minor elimination pathway with less than 1% of the dose recovered in the urine. Biliary elimination presumably accounts for a portion of the elimination as evidenced by biliary concentrations of albendazole sulfoxide similar to those achieved in plasma.


Albendazole is variably and erractically absorbed after oral admin; absorption is enhanced by the presence of fatty foods and possibly by bile salts as well. After a 400-mg oral dose, albendazole cannot be detected in plasma, because the drug is rapidly metabolized in the liver and possibly in the intestine as well, to albendazole sulfoxide, which has potent anthelmintic activity. Both the (+) and (-) enantiomers of albendazole sulfoxide are formed, but in human beings the (+) enantiomer reaches much higher peak concn in plasma and is cleared much more slowly than the (-) form. Total sulfoxide attains peak plasma concn of about 300 ng/mL, but with wide interindividual variation. Albendazole sulfoxide is about 70% bound to plasma proteins ... It is well distributed into various tissues, including hydatid cysts, where it reaches a concn of about one-fifth that in plasma ... Both sulfoxide derivatives are oxidized further to the nonchiral sulfone metabolite of albendazole, which is pharmacologically inactive; this reaction favors the (-) sulfoxide and probably becomes rate limiting in determining the clearance ... Albendazole metabolites are excreted mainly 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


Oral bioavailability of albendazole appears to be increased when the drug is administered with a fatty meal; when the drug is administered with meals containing about 40 g of fat, plasma concentrations of albendazole sulfoxide are up to 5 times higher than those observed when the drug is administered to fasting patients

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 46


Sheep bearing permanent ruminal and abomasal cannulae were given a single oral dose of 10 mg/kg bw albendazole as a 2.5% formulation. Albendazole was absorbed unchanged from the rumen. Once in the body it was rapidly degraded, and sulfone metabolites were detected in plasma, the former achieving the greater level. All 3 compounds were present in the abomasum. Presumably albendazole was passed through the stomachs while the metabolites were secreted or diffused into this organ. Non-detectable levels of all 3 compounds were reached in plasma and rumen at 96 hr and in abomasum at 120 hr.

Joint FAO/WHO Expert Committee on Food Additives; WHO Food Additive Series 25: Toxicological Evaluation of Ceratin Veterinary Drug Residues in Food: Albendazole (1990). Available from, as of July 17, 2006: https://www.inchem.org/documents/jecfa/jecmono/v25je01.htm


The parent compound was virtually undetectable in the plasma of Sprague Dawley males and females given a single gavage dose of 10.6 mg/kg bw albendazole in an aqueous suspension. Rapid metabolism let to the appearance of the sulfoxide and subsequently the sulfone derivatives in plasma. Both metabolites decreased to very low levels at 18 hr. Daily dosing at 10.6 mg/kg bw in males for a period of 10 days resulted in lower plasma levels of sulfoxide and higher levels of the sulfone. Albendazole induces certain hepatic drug-metabolising enzymes, which may be responsible for enhancing the degradation of sulfoxide to sulfone following repeated administration.

Joint FAO/WHO Expert Committee on Food Additives; WHO Food Additive Series 25: Toxicological Evaluation of Ceratin Veterinary Drug Residues in Food: Albendazole (1990). Available from, as of July 17, 2006: https://www.inchem.org/documents/jecfa/jecmono/v25je01.htm


For more Absorption, Distribution and Excretion (Complete) data for ALBENDAZOLE (9 total), please visit the HSDB record page.


5.6 Metabolism/Metabolites

Hepatic. Rapidly converted in the liver to the primary metabolite, albendazole sulfoxide, which is further metabolized to albendazole sulfone and other primary oxidative metabolites that have been identified in human urine.


Albendazole is converted first to a sulfoxide and then to a sulfone. All of these reactions are catalyzed by flavin monooxygenases (FMO) and/or cytochrome P450. Both enzymes are efficient catalysts of S-oxygenation ...

Klaassen, C.D. (ed). Casarett and Doull's Toxicology. The Basic Science of Poisons. 6th ed. New York, NY: McGraw-Hill, 2001., p. 176


Albendazole is metabolized in the liver to an active metabolite, albendazole sulfoxide, which accounts for detectable plasma concentrations of the drug; systemic anthelmintic activity of the drug has been attributed to this metabolite.

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 47


Albendazole ... is rapidly metabolized in the liver and possibly in the intestine as well, to albendazole sulfoxide, which has potent anthelmintic activity. Both the (+) and (-) enantiomers of albendazole sulfoxide are formed, but in human beings the (+) enantiomer reaches much higher peak concn in plasma and is cleared much more slowly than the (-) form. Total sulfoxide attains peak plasma concn of about 300 ng/mL, but with wide interindividual variation. Albendazole sulfoxide is about 70% bound to plasma proteins and has a highly variable plasma half-life ranging from about 4 to 15 hr. It is well distributed into various tissues, including hydatid cysts, where it reaches a concn of about one-fifth that in plasma. This probably explains why albendazole is more effective than mebendazole for treating hydatid cyst disease. Formation of albendazole sulfoxide is catalyzed by both microsomal flavin monooxygenase and isoforms of cytochrome P450 in the liver and possibly also in the intestine. Hepatic flavin monooxygenase activity appears associated with (+) albendazole sulfoxide formation, whereas cytochromes P450 preferentially produce the (-) sulfoxide metabolite. Both sulfoxide derivatives are oxidized further to the nonchiral sulfone metabolite of albendazole, which is pharmacologically inactive; this reaction favors the (-) sulfoxide and probably becomes rate limiting in determining the clearance and plasma half-life of the bioactive (+) sulfoxide metabolite. Induction of enzymes involved in sulfone formation from the (+) sulfoxide could account for some of the wide variation noted in plasma half-lives of albendazole sulfoxide. Indeed, in animal models, benzimidazoles can induce their own metabolism. Albendazole metabolites are excreted mainly 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


Sheep bearing permanent ruminal and abomasal cannulae were given a single oral dose of 10 mg/kg bw albendazole as a 2.5% formulation. Albendazole was absorbed unchanged from the rumen. Once in the body it was rapidly degraded, and sulfone metabolites were detected in plasma, the former achieving the greater level. All 3 compounds were present in the abomasum. Presumably albendazole was passed through the stomachs while the metabolites were secreted or diffused into this organ. Non-detectable levels of all 3 compounds were reached in plasma and rumen at 96 hr and in abomasum at 120 hr.

Joint FAO/WHO Expert Committee on Food Additives; WHO Food Additive Series 25: Toxicological Evaluation of Ceratin Veterinary Drug Residues in Food: Albendazole (1990). Available from, as of July 17, 2006: https://www.inchem.org/documents/jecfa/jecmono/v25je01.htm


For more Metabolism/Metabolites (Complete) data for ALBENDAZOLE (12 total), please visit the HSDB record page.


Albendazole has known human metabolites that include Albendazole oxide.

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


5.7 Biological Half-Life

Terminal elimination half-life ranges from 8 to 12 hours (single dose, 400mg).


Albendazole ... is rapidly metabolized ... to albendazole sulfoxide, which ... has a highly variable plasma half-life ranging from about 4 to 15 hr ... Both /(+) and (-)/ sulfoxide derivatives are oxidized further to the nonchiral sulfone metabolite ... This reaction favors the (-) sulfoxide and probably becomes rate limiting in determining ... plasma half-life of the bioactive (+) sulfoxide metabolite. Induction of enzymes involved in sulfone formation from the (+) sulfoxide could account for some of the wide variation noted in plasma half-lives of albendazole sulfoxide.

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


5.8 Mechanism of Action

Albendazole causes degenerative alterations in the tegument and intestinal cells of the worm by diminishing its energy production, ultimately leading to immobilization and death of the parasite. It works by binding to the colchicine-sensitive site of tubulin, thus inhibiting its polymerization or assembly into microtubules. As cytoplasmic microtubules are critical in promoting glucose uptake in larval and adult stages of the susceptible parasites, the glycogen stores of the parasites are depleted. 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.


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


Although the exact mechanism of action of albendazole has not been fully elucidated, the principal anthelmintic effect of benzimidazoles, including albendazole, appears to be the specific, high-affinity binding of the drug to free beta-tubulin in parasite cells, resulting in selective inhibition of parasite microtubule polymerization, and inhibition of microtubule-dependent uptake of glucose. Benzimidazole drugs bind to the beta-tubulin of parasites at much lower concentrations than to mammalian beta-tubulin protein; the drugs do not inhibit glucose uptake in mammals, and do not appear to have any effect on blood glucose concentrations in humans

McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2006., p. 47


The mode of action of albendazole is by binding strongly with the tubulin in the cells of nematodes. The intestinal cells of the nematode are particularly affected, resulting in a loss of absorptive function which causes the nematodes to starve to death.

European Medicines Agency (EMEA), The European Agency for the Evaluation of Medicinal Products, Veterinary Medicines Evaluation Unit, Committee for Veterinary Medicinal Products; Albendazole, Summary Report(3). EMEA/MRL/865/03-Final (June 2004). Available from, as of July 25, 2006: https://www.ema.europa.eu/ema/index.jsp?curl=pages/document_library/landing/document_library_search.jsp&murl=menus/document_library/document_library.jsp&mid


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ZHANGJIAGANG CITY,JIANGSU, CHINA","customerAddress":"213, LAXMI PLAZA, LAXMI INDL."}]
02-Jan-2021
29-Aug-2024
KGS
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Quantity (KGS) & Unit rate (USD/KGS) over time

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