Rapid steady-state analysis of blood-brain transfer of l-Trp in rat, with special reference to the plasma protein binding

1993 ◽  
Vol 23 (4) ◽  
pp. 351-359 ◽  
Author(s):  
A. Takada ◽  
M. Grdiša ◽  
M. Diksic ◽  
A. Gjedde ◽  
Y.L. Yamamoto
1987 ◽  
Vol 36 (16) ◽  
pp. 2641-2645 ◽  
Author(s):  
C. Hamberger ◽  
S. Urien ◽  
D. Essassi ◽  
B. Grimaldi ◽  
J. Barre ◽  
...  

1995 ◽  
Vol 3 (3) ◽  
pp. 133-138 ◽  
Author(s):  
José-Esteban Peris ◽  
María Pascual-Arce ◽  
Luis Granero ◽  
Jesús Chesa-Jiménez ◽  
Mercedes Almela

2016 ◽  
Vol 250-251 ◽  
pp. 21-28 ◽  
Author(s):  
Manoj Amaraneni ◽  
Anshika Sharma ◽  
Jing Pang ◽  
Srinivasa Muralidhara ◽  
Brian S. Cummings ◽  
...  

2010 ◽  
Vol 23 (4) ◽  
pp. 858-883 ◽  
Author(s):  
Roland Nau ◽  
Fritz Sörgel ◽  
Helmut Eiffert

SUMMARY The entry of anti-infectives into the central nervous system (CNS) depends on the compartment studied, molecular size, electric charge, lipophilicity, plasma protein binding, affinity to active transport systems at the blood-brain/blood-cerebrospinal fluid (CSF) barrier, and host factors such as meningeal inflammation and CSF flow. Since concentrations in microdialysates and abscesses are not frequently available for humans, this review focuses on drug CSF concentrations. The ideal compound to treat CNS infections is of small molecular size, is moderately lipophilic, has a low level of plasma protein binding, has a volume of distribution of around 1 liter/kg, and is not a strong ligand of an efflux pump at the blood-brain or blood-CSF barrier. When several equally active compounds are available, a drug which comes close to these physicochemical and pharmacokinetic properties should be preferred. Several anti-infectives (e.g., isoniazid, pyrazinamide, linezolid, metronidazole, fluconazole, and some fluoroquinolones) reach a CSF-to-serum ratio of the areas under the curves close to 1.0 and, therefore, are extremely valuable for the treatment of CNS infections. In many cases, however, pharmacokinetics have to be balanced against in vitro activity. Direct injection of drugs, which do not readily penetrate into the CNS, into the ventricular or lumbar CSF is indicated when other effective therapeutic options are unavailable.


2017 ◽  
Vol 62 ◽  
pp. 24-29 ◽  
Author(s):  
Manoj Amaraneni ◽  
Jing Pang ◽  
Tanzir B. Mortuza ◽  
Srinivasa Muralidhara ◽  
Brian S. Cummings ◽  
...  

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