Abstract
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.
Highlights
Acexazolamide is a new derivative of 1,3,4-thiadiazole and acexamic acid
DL50 value was determined by means of Litchfield and Wilcoxon probit analysis method modified by V.B
The hazard class of the studied compound was determined by the value of DL50 in accordance with GOST 12.1.007–76 and the classification of Hodge and Sterner
Summary
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. The anti-burn activity of acexazolamide was evaluated in a thermal skin burn model in rats. 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). The emergence of combined NSAIDs with components of other pharmacological groups (proton pump inhibitors, H2-histamine receptor blockers, prostaglandins, etc.) made it possible to reduce the damaging effect on the gastrointestinal mucosa. Such combination drugs had a number of side effects, non-specific for NSAIDs. The appearance of specific.
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