作者: Marc Sindou , George Georgoulis , Patrick Mertens
DOI: 10.1007/978-3-7091-1771-2_6
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摘要: Baclofen, a γ-aminobutyric acid-B (GABA-B) receptor agonist, has direct action on the receptors of dorsal horn gray matter, where density GABA-B is high. Baclofen activates presynaptic that inhibit release excitatory neurotransmitters horn, particularly aspartate and glutamate. The excitability monosynaptic polysynaptic reflexes spinal cord becomes thereby reduced. Given orally, baclofen weak capacity to penetrate blood–central nervous system barrier. After oral administration drug absorbed by more than 80 % through intestinal mucosa plasmatic concentration maximal within 90–120 min; most eliminated urinary excretion. Failure medication produce sufficient reduction spasticity due poor passage across In animal experiments, in cerebrospinal fluid (CSF) was less one-tenth plasma level. Systemic delivery would same concentrations along be distributed equally brain, consequences somnolence or even coma. To circumvent this problem, Penn Kroin introduced developed method delivering intrathecally subarachnoid lumbar infusion.