EXPERIMENTAL PHARMACOLOGICAL
RESEARCHES EVALUATING THE ANALGESIC
ACTIVITY FOR NOVEL HYBRID PRODRUGS
OBTAINED BY ESTERIFICATION OF NSAIDs
COMPOUNDS WITH PROSTAGLANDINIC
COMPOUNDS.
SIMONA FIRULESCU1, SIMONA NEGREŞ2, DENISA MIHELE3
1Emergency Clinical Hospital Floreasca, Bucharest
2Department of Pharmacology and Clinical pharmacy, Faculty of
Pharmacy, UMF ”Carol Davila”, Bucharest
3Department of Clinical laboratory and Alimentation hygiene, Faculty of
Pharmacy, UMF ”Carol Davila”, Bucharest
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Abstract:

Safety reevaluation for non-selective cyclooxigenase (COX) inhibitor nonsteroidal antiinflamatory drugs (NSAIDs) demonstrated that the risk of inducing gastroduodenal ulcer is extremely high. Literature data show that the long term use of those drugs (piroxicam, naproxen, diclofenac) increases therapy costs by concomitant administration of antiulcer drugs: H2 antihistamines, proton pump inhibitors, whilst the risk of gastrointestinal hemorrhages is much reduced when non-selective COX inhibitor NSAIDs are administered in association with prostaglandinic derivatives which exhibit gastric cytoprotective effect.
Based on these observations, in the present non-clinical trial we aimed at determining the analgesic efficacy of newly synthesized derivatives noted: S4As, S6As, S8As, obtained by esterification of acetylsalicylic acid with prostaglandinic compounds [synthesized to Romanian National Institute of Chemical-Pharmaceutical Researches, Bucharest]. We have established for these derivatives the maximal tolerated dose of active substance orally administered in mouse without registering adverse reactions and we determined their analgesic efficacy in chemical and thermal stimulus tests

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