Acexazolamide is a new derivative of 1,3,4-thiadiazole and acexamic acid. In animal experiments, acute toxicity, pharmacological activity and bioavailability of acexazolamide were evaluate

Demidova, M. A.

Malygin, A. S.

Popova, N. S.

Popov, N. S.

DSpace at Belgorod State University

Assessment of pharmacological activity and bioavailability of the new derivative 1,3,4-thiadiazole

Introduction: Acexazolamide is a new derivative of 1,3,4-thiadiazole and acexamic acid.
        
          Materials and methods: In animal experiments, acute toxicity, pharmacological activity and bioavailability of acexazolamide were evaluated. Anti-inflammatory activity was assessed on the model of formalin edema of paw and cotton pellet granuloma in rats. Assessment of analgesic activity was carried out in a hot plate test in mice, chemical pain stimulation of the peritoneum and inflammatory hyperalgesia in rats. The antipyretic activity of acexazolamide was evaluated in a model of yeast-induced hyperthermia in rats. The anti-burn activity of acexazolamide was evaluated in a thermal skin burn model in rats. Bioavailability of acexazolamide with intragastric administration was determined in rabbits. The content of acetaxazolamide in blood plasma was determined by HPLC-MS/MS method.
        
          Results and discussion: DL50 of acexazolamide after intragastric administration to mice was 860.99 (95% CIs, 462.2 to 1259.8) mg/kg. The anti-inflammatory activity of acexazolamide (21.5 mg/kg) with formalin-induced paw edema and fetal granuloma in rats was higher than that of ketoprofen (23.0 mg/kg). ED50 value for analgesic activity with acetic acid induced cortex was 24.99 (95% CIs: 15.31–34.68) mg/kg. With thermal stimulation of the paw in mice, the ED50 value was 25.56 (95% CIs: 15.13 to 35.98) mg/kg. ED50 value for antipyretic activity was 31.85 (95% CIs: 19.22–44.47) mg/kg. Acexazolamide (21.5 mg/kg) had a stimulating effect on the regeneration of damaged tissues in case of thermal skin burns. Bioavailability of acexazolamide (1 mg/kg) with intragastric administration was 37%.
        
          Conclusion: Acexazolamide has the properties of a non-steroidal anti-inflammatory agent

Popov, Nikita S.

Demidova, Marina A.

Malygin, Alexandr S.

NEUROSURGERY ENTHUSIASTIC WOMEN SOCIETY

Popov,Nikita

Demidova,Marina

Malygin,Alexandr

ARPHA Preprints

ZENODO

http://dspace.bsu.edu.ru/bitstream/123456789/46410/1/Popov_Assessment_18.pdf

Assessment of pharmacological activity and bioavailability of the new derivative 1,3,4-thiadiazole

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DSpace at Belgorod State University

NEUROSURGERY ENTHUSIASTIC WOMEN SOCIETY

ARPHA Preprints

ZENODO

DSpace at Belgorod State University