Aminoleban Infusion Soln Mechanism of Action

Pharmacology: Amino Acids (AMINOLEBAN) normalized the Fischer's ratio in the plasma and brain, improved monoamine metabolism in the brain, and corrected a sleep-wakefulness pattern in portacaval-shunted rats (chronic hepatic insufficiency model).
When infused to portacaval-shunted rats loaded with ammonia, Amino Acids (AMINOLEBAN) normalized the Fischer's ratio in the plasma and brain, decreased blood ammonia levels, and improved EEG and monoamine metabolism in the brain.
Pharmacodynamics: No available information.
Clinical Studies: Amino Acids (AMINOLEBAN) was administered to patients with hepatic encephalopathy associated with chronic liver disease, and the clinical effect of Amino Acids (AMINOLEBAN) was evaluated. A prompt improvement in the coma scale (an index of disturbance of consciousness) and a prompt decrease in blood ammonia concentrations were observed. In addition, patients showed improvement in neuropsychological function as assessed by writing, drawing, flapping tremor, number connection test, and orientation and calculation tests as well as by EEG tracings. The efficacy of Amino Acids (AMINOLEBAN) in hepatic encephalopathy in clinical studies was summarized as follows: See Table 2.

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Pharmacokinetics: (Reference data in rats): ¹⁴C-labeled amino acids formulated in Amino Acids (AMINOLEBAN) were readily distributed to almost the entire body after intravenous infusion in rats. In 6 hours, 50 to 70% of the administered amino acids was taken up into protein fractions. The ratio of branched-chain amino acids to the total amino acids in the protein fractions was highest in the brain. Up to 72 hr, 41.7% of the administered dose was excreted in the expired air, 5.9% in the urine, and 2.6% in the feces.