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Pharmacokinetics of Intrathecal Baclofen

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Book cover Local-spinal Therapy of Spasticity

Abstract

Due to its polarity and water solubility, GABA (γ-aminobutyric acid), an inhibitory transmitter within the central nervous system, does not cross the blood-brain barrier and, therefore, is ineffective after oral or parenteral application [2]. Baclofen (β-(p-chlorphenyl)-γ-aminobutyric acid) was synthesised in 1965 as a GABA derivative with lipophilic substitution in order to overcome this disadvantage [3]. Due to the assymmetric substitution, baclofen exists in two optical active isomers, D- and L-baclo-fen. The commercially available preparation contains the racemate, but central nervous activity (as well as toxicity) of the drug is only related to the L-isomer [11].

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References

  1. Anderson P, Noher H, Swahn CG (1984) Pharmacokinetics in baclofen overdose. J Toxicol Clin Toxicol 22: 11–20

    Article  PubMed  CAS  Google Scholar 

  2. Bencze WL (1977) GABA: Struktur-Aktivitäts-Beziehungen. Med Unserer Zeit 1: 173–179

    CAS  Google Scholar 

  3. CIBA Ltd. (1965) Amino acids. Patent, Netherlands Application 6, 407, 755, Jan 11, 1965. Chem Abstr 62: 14582d

    Google Scholar 

  4. Degen PH, Riess W (1976) The determination of Gamma-amino-beta-(p-chlorphenyl) butyric acid (baclofen) in biological material by gas-liquid chromatography. J Chromatogr 117: 399–405

    Article  PubMed  CAS  Google Scholar 

  5. Eriksson G, Swahn CG (1981) Concentrations of baclofen in serum and breast milk from a lactating woman. Scand J Clin Lab Invest 41: 185–187

    Article  PubMed  CAS  Google Scholar 

  6. Faigle JW, Keberle H (1972) Metabolismus und Pharmakokinetik von Lioresal. In: Birkmayer W (ed) Aspekte der Muskelspastik. Huber, Bern Stuttgart Wien, pp 94–100

    Google Scholar 

  7. Faigle JW, Keberle H (1972) The chemistry and kinetics of lioresal. Postgrad Med J 48 [Suppl]: 9–13

    PubMed  CAS  Google Scholar 

  8. Faigle JW, Keberle H, Degen PH (1980) Chemistry and pharmacokinetics of baclofen. In: Feldman RG, Young RR, Koalla WP (eds) Spasticity: Disordered motor control. Year Book, Chicago, pp 461–475

    Google Scholar 

  9. Faigle JW, Keberle H, Degen PH (1981) Pharmakokinetik von Baclofen. In: Bauer HJ, Koella WP, Struppler A (eds) Therapie der Spastik. Verlag fär angewandte Wissenschaften, München, pp 137–147

    Google Scholar 

  10. Harrison PM, Tonkin AM, McLean AJ (1985) Determination of 4-amino-3-(p-chlorphenyl) butyric acid (baclofen) in plasma by high-performance liquid chromatography. J Chromatogr 339: 424–428

    Article  PubMed  CAS  Google Scholar 

  11. Keberle H, Faigle JW (1972) Synthese sowie Beziehung zwischen Struktur und Wirkung der Gamma-Aminobuttersäurederivate. In: Birkmayer W (ed) Aspekte der Muskelspastik. Huber, Bern Stuttgart Wien, pp 90–93

    Google Scholar 

  12. Knuttson E, Lindblom U, Mårtensson A (1974) Plasma and cerebrospinal fluid levels of baclofen at optimal therapeutic responses in spastic paresis. J Neurol Sci 23: 473–478

    Article  Google Scholar 

  13. Krauß D (in preparation) Fluorimetric determination of baclofen after thin-layer chromatographic separation. Thesis, University of Frankfurt/ Main

    Google Scholar 

  14. Swahn CG, Beving H, Sedvall G (1979) Mass fragmentographic determination of 4-amino-3p-chlorphenyl-butyric acid (baclofen) in cerebrospinal fluid and serum. J Chromatogr Biomed Appl 162: 433–438

    Article  CAS  Google Scholar 

  15. Wuis EW, Dirks RJ, Vree TB, Van der Kleyn E (1985) High-performance liquid chromatographic analysis of baclofen in plasma and urine of man after precolumn extraction and derivatization with o-phthaldialdehyde. J Chromatogr 337: 341–350

    Article  PubMed  CAS  Google Scholar 

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© 1988 Springer-Verlag Berlin Heidelberg

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Müller, H., Zierski, J., Dralle, D., Krauß, D., Mutschler, E. (1988). Pharmacokinetics of Intrathecal Baclofen. In: Müller, H., Zierski, J., Penn, R.D. (eds) Local-spinal Therapy of Spasticity. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-72954-6_17

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  • DOI: https://doi.org/10.1007/978-3-642-72954-6_17

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-540-18295-5

  • Online ISBN: 978-3-642-72954-6

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