Zusammenfassung
Fast alle Neuroleptika sind basische amphiphile Substanzen, d. h. sie besitzen einen lipophilen und einen hydrophilen, nämlich geladenen Molekülanteil. Dies bestimmt ihr kinetisches Verhalten, das gekennzeichnet ist durch
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leichte Penetration durch Lipidmembranen, dadurch hohe Resorptionsquote aus dem Darm
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Anreicherung in Membranen, daher hohe Konzentration in parenchymatösen Organen, großes scheinbares Verteilungsvolumen
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hohe Plasmaproteinbindung
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geringe renale Ausscheidung in unveränderter Form
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Elimination durch Stoffwechsel, hauptsächlich in der Leber
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eingeschränkte orale Bioverfügbarkeit infolge Metabolismus beim ersten Durchgang durch Darmwand und Leber (“first-pass effect”).
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Breyer-Pfaff, U. (1987). Klinische Pharmakokinetik der Neuroleptika: Ergebnisse und Probleme. In: Pichot, P., Möller, HJ. (eds) Neuroleptika Rückschau 1952–1986, Künftige Entwicklungen. Tropon-Symposium, vol 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-83188-1_5
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