Possible Interaction: Ethanol and Tolbutamide

“Rats given both ethanol and tolbutamide showed decreased oxidative phosphorylation of the myocardial mitochondria as compared with rats given only ethanol.”

“The concentration of acetaldehyde tended to be higher in rats given both ethanol and tolbutamide than in rats given ethanol alone.”

“ Hydroxytolbutamide is oxidized further in vivo by alcohol and aldehyde dehydrogenases producing carboxytolbutamide.”

“Highly bound drugs with low intrinsic hepatic clearance are among the most commonly reported to have their kinetics altered by ethanol (e.g. benzodiazepines, phenytoin, tolbutamide and warfarin).”

“In addition alcohol apparently potentiates insulin secretion stimulated by glucose, arginine and tolbutamide [S] .”

“Pretreatment with tolbutamide, ethanol and tolbutamide plus ethanol resulted in protentiation of the acute phase insulin release and enhanced glucose disappearance with glucose doses of 10 gm.”

“Additional evidence is provided by the observed inhibition of tolbutamide metabolism by ethanol infusion.”

“Chronic addiction to alcohol produces an enhanced rate of tolbutamide metabolism; on the other hand, prolonged treatment with tolbutamide is able to increase the rate of ethanol oxidation.”

“Summary With a sensitive technic it is demonstrated that tolbutamide (100 mg/kg) injected intravenously inhibits the metabolism of ethanol in intact cats, average inhibition being 34%.”

“Acute po administration of varying doses of tolbutamide or chlorpropamide 2.5 hr before a 3.0 g/kg ip dose of ethanol to C57BL and DBA mice resulted in significant elevations of blood acetaldehyde when measured 2.5 hr after ethanol dosing.”

“Measurements of aldehyde dehydrogenase (ALDH) in hepatic subcellular fractions, obtained from both inbred strains treated with 100 mg/kg tolbutamide or chlorpropamide prior to a 3.0 g/kg dose of ethanol , revealed a 50 to 80% inhibition of the low-Km ALDH present in mitochondria.”

“The oral hypoglycemic agents, chlorpropamide (CP) and tolbutamide (TB) are known to elicit a clinical disulfiram-ethanol reaction (DER) when consumed with alcohol.”

“Beaser (1958) has recorded that prior administration of tolbutamide produces an intolerance to alcohol in the form of hot flushes.”