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Statement of Problem: One of the most important complications after tooth extraction and oral and maxillofacial surgery is transient bacteraemia and prescription of prophylactic antibiotic is necessary to prevent postoperative infections in immunocompromised patients. Purpose: The aim of this study was the evaluation of cephalexin and amoxicillin concentrations in dental alveolar sockets following tooth extraction. Materials and Methods: In this interventional study, 80 healthy patients subjected to tooth extraction were divided into two groups. Each group received 1 gr amoxicillin or cephalexin and teeth were extracted 30-60-90-120-180 minutes after antibiotic intake. Blood sampling was performed immediately after extraction and concentrations of two antibiotics were measured in microbiology laboratory. ANOVA test and Post-hoc (Duncan) test were used for statistical analysis with P<0.05 as the limit of significance. Results: The maximum serum concentration was 10.1006 μg/ml for amoxicillin at 120 minutes and 41.5467 μg/ml for cephalexin at 90 minutes after drug intake. The minimum inhibitory concentration (MIC) of cephalexin and amoxicillin for Streptococcus sanguis was 2 μg/ml and 1 μg/ml respectively. Conclusion: The mean concentration for amoxicillin was 10 times and for cephalexin was 20 times higher than MIC.