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Differential Brain Penetration of Cerebroprotective Drugs

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Frontiers in Cerebral Vascular Biology

Abstract

The use of cerebroprotective drugs has become a ubiquitous practice in neurosurgery, but our understanding of their pharmacokinetics and mode of action in the brain is limited. It has been speculated that beneficial therapeutic effects of cerebroprotective drugs may depend on their transport across the blood-brain barrier (BBB). To test this hypothesis, we studied two structurally different, but pharmacologically potent, cerebroprotective compounds, namely, a calcium-entry blocker, nimodipine, and a glucocorticoid, methyl-prednisolone. Clinical and experimental evidence suggests that nimodipine may act as a protective agent in ischemic brain damage secondary to cardiac arrest (1). Methyl-prednisolone is commonly used in the treatment of cerebral edema secondary to neoplasia (2, 3). In this study, an in situ vascular brain perfusion technique in guinea-pigs (4), and a capillary-depletion method (5) were used to determine pharmacokinetics of nimodipine and methyl-prednisolone at the BBB. The results described below are derived from our ongoing studies.

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© 1993 Springer Science+Business Media New York

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Zlokovic, B.V. et al. (1993). Differential Brain Penetration of Cerebroprotective Drugs. In: Drewes, L.R., Betz, A.L. (eds) Frontiers in Cerebral Vascular Biology. Advances in Experimental Medicine and Biology, vol 331. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-2920-0_19

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  • DOI: https://doi.org/10.1007/978-1-4615-2920-0_19

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-6267-8

  • Online ISBN: 978-1-4615-2920-0

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