Four male subjects aged between 20 and 29 years were given intravenous injections of methanol at a dosage of 10 mg per kg body weight, once without prior administration of ethanol, and once after oral ingestion of 0.3 g ethanol per kg body weight. The serum methanol concentration was monitored over the next 5 h (after methanol administration alone) and 6-7 h (after methanol administration following ethanol ingestion). The elimination of methanol administered alone was found to follow first-order kinetics with a rate constant for the elimination phase of 0.475-0.259 h-1, corresponding to an elimination half-life of 1.8-3.0 h. When ethanol was also administered methanol oxidation was found to be completely blocked until the blood ethanol concentration had fallen to 0.2 g/kg. When the ethanol concentration had dropped to zero, methanol elimination followed exactly the same course as that observed in the experiment without prior administration of ethanol (k: 0.378-0.231 h-1; t1/2: 1.5-2.7 h).
After the enzyme systems responsible for methanol oxidation were blocked by ethanol, five test persons were given methanol at a dose of approximately 10 mg/kg weight, once orally and once parenterally. Taking into account the endogenous blood methanol levels detectable before the administration of methanol, C0 concentrations of 11.1-15.9 mg/kg were reached. This corresponds to a distribution volume of approximately 0.77 +/- 0.07 l/kg, which is comparable to the 0.78 +/- 0.09 l/kg obtained for ethanol. After parenterally administering methanol as a bolus, the distribution half-life was on average 8 min (range: 3.8-13.8 min). After oral administration of methanol diluted in 100 ml water on an empty stomach, invasion took place with a half-life of approximately 5 min (3.8-6.9 min). In one case, however, due to vegetative disturbances the invasion half-life was 23.1 min.
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