Human Pharmacokinetics of Aniracetam
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- Roncari, G. Drug Invest (1993) 5(Suppl 1): 68. doi:10.1007/BF03258428
Aniracetam is very rapidly and completely absorbed from the gastrointestinal tract. However, absolute systemic bioavailability is only about 0.2%. Aniracetam has a high volume of distribution (2.5 L/kg, which implies extensive extravascular distribution) and is very rapidly eliminated from the body. Indeed, total body clearance from blood (10 L/min) exceeds cardiac output (implying that the lung is a major clearance organ) and plasma elimination half-life is very short (≈ 0.5 hours). Aniracetam is completely metabolised and the principal metabolites, N-anisoyl-γ-aminobutyric acid (N-anisoyl-GABA), 2-pyrrolidinone, succinimide and anisic acid, are excreted via the urine (84%), the faeces (2%) or as CO2 in expired air. After multiple dose administration, there is no indication of accumulation of drug or principal metabolites, with the exception of succinimide. Measurable concentrations of 2 main metabolites, N-anisoyl-GABA and 2-pyrrolidinone, were found in the cerebrospinal fluid of patients treated with aniracetam for 12 weeks.
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