Possible Interaction: Caffeine and Diazepam

“Diazepam DZ ) 0.3 mg/kg given at 60 min antagonized some effects of CAF but failed to antagonize YOH.”

“The coadministration of caffeine with diazepam resulted in a 22% reduction in diazepam plasma levels.”

“There were significant correlations between the caffeine and diazepam plasma levels and performance on several tasks and evidence for the development of acute tolerance to both drugs.”

“Other compounds including physostigmine, naloxone, bicuculline, picrotoxin, caffeine and theophylline, lack appreciable affinity for benzodiazepine binding sites but do antagonize at least some of the behavioral actions of diazepam.”

“ Caffeine antagonized the depression by diazepam , but not that by phenobarbitone, of the ventral root-evoked Renshaw cell discharge.”

“In the horizontal wire test in mice, caffeine was more potent in reversing the depression of performance induced by diazepam that that by phenobarbitone (ED50 1.8 mg·kg −1 and 139 mg·kg −1 p.o.,”

“The interaction between caffeine and diazepam is not due to a competition at the benzodiazepine receptors but may involve purinergic mechanisms.”

“The reduction of skeletal muscle tone in mice produced by diazepam was antagonized by low doses of caffeine (ED50 0.53 mg·kg −1 p.o.).”

“ DZ antagonized the CAF-induced staff-rated restlessness, and subject-ratings of tension, alertness, arousal and CAF symptoms.”

“The results generally support the hypothesis that DZ and CAF produce antagonistic effects through functionally opposing mechanisms, however, the observed effects of drug combinations are dependent on the specific doses being tested and on the measures of drug effect being examined.”

“Subjectively, diazepam exerted a calming effect which was counteracted by caffeine at either at either dose levels.”

“Finally, following the exciting discovery that the brain contained specific receptors for benzodiazepines, it was noted that caffeine was a competitive inhibitor of diazepam binding to these brain receptors.‘3,‘4 Conceivably, competitive interference”

“The serum half-life of caffeine was determined for the three healthy subjects when 25 mg diazepam was given one hour prior to the caffeine load.”

“The pretreatment with caffeine (10 micromol/L) inhibited I(GABA) which was potentiated by diazepam (1 micromol/L).”

“Furthermore, the benzodiazepine diazepam produced a dose-dependent inhibition of the caffeine rotation , but again, the apomorphine response, although qualitatively modified, was not significantly inhibited.”