Clinical Pharmacokinetics of Cerebrospinal Fluid

Overview

Journal Clin Pharmacokinet

Specialty Pharmacology

Date 1982 Jul 1

PMID 6749368

Citations 22

Authors

M Bonati

J Kanto

G Tognoni

Affiliations

Soon will be listed here.

Abstract

The distribution of drugs into the cerebrospinal fluid has long been considered a challenging field of investigation in 2 major respects: (a) understanding how the physicochemical properties (molecular weight, pKa, plasma protein binding) of various molecules influence their movements across such a specific structure as the blood-brain barrier; and (b) defining the relationship between cerebrospinal fluid concentrations of various drugs and their central (side) effects. An attempt has been made to review the very dispersed information presently available to offer a clinically orientated picture of this area of pharmacokinetics. Drugs acting on the central nervous system (benzodiazepines, tricyclic antidepressants, anticonvulsants, opioids), antibacterial agents, cardiovascular drugs (beta-adrenoceptor blockers and digoxin), antineoplastic drugs (mainly methotrexate), and other miscellaneous agents (corticosteroids, cimetidine, methylxanthines) are reviewed. The available evidence seems to support the conclusion that only for methotrexate and antibacterial agents does knowledge of cerebrospinal fluid pharmacokinetics have direct therapeutic implications, while the mosaic of information available for other drugs does little more than provide a partially satisfactory picture.

Citing Articles

Cerebrospinal fluid concentrations of fluoroquinolones and carbapenems in tuberculosis meningitis.

Maranchick N, Alshaer M, Smith A, Avaliani T, Gujabidze M, Bakuradze T Front Pharmacol. 2022; 13:1048653.

PMID: 36578553 PMC: 9791083. DOI: 10.3389/fphar.2022.1048653.

Utility of CSF in translational neuroscience.

de Lange E J Pharmacokinet Pharmacodyn. 2013; 40(3):315-26.

PMID: 23400635 PMC: 3663203. DOI: 10.1007/s10928-013-9301-9.

Doxepin concentrations in plasma and cerebrospinal fluid.

Schomburg R, Remane D, Fassbender K, Maurer H, Spiegel J J Neural Transm (Vienna). 2011; 118(4):641-5.

PMID: 21350940 DOI: 10.1007/s00702-011-0613-x.

Pharmacokinetic optimization of benzodiazepine therapy for acute seizures. Focus on delivery routes.

Rey E, Treluyer J, Pons G Clin Pharmacokinet. 1999; 36(6):409-24.

PMID: 10427466 DOI: 10.2165/00003088-199936060-00003.

Drugs and brain death.

Kennedy M, Kiloh N Drug Saf. 1996; 14(3):171-80.

PMID: 8934579 DOI: 10.2165/00002018-199614030-00004.

References

Norrby R . A review of the penetration of antibiotics into CSF and its clinical significance. Scand J Infect Dis Suppl. 1978; (14):296-309. View

Rieselbach R, MORSE E, Rall D, Frei 3rd E, Freireich E . Treatment of meningeal leukemia with intrathecal aminopterin. Cancer Chemother Rep. 1962; 16:191-6. View

Odar-Cederlof I, Borga O . Kinetics of diphenylhydantoin in uraemic patients: consequences of decreased plasma protein binding. Eur J Clin Pharmacol. 1974; 7(1):31-7. DOI: 10.1007/BF00614387. View

Sande M . Antibiotic therapy of bacterial meningitis: lessons we've learned. Am J Med. 1981; 71(4):507-10. DOI: 10.1016/0002-9343(81)90191-1. View

Samii K, FERET J, Harari A, VIARS P . Selective spinal analgesia. Lancet. 1979; 1(8126):1142. View

Kangas L, Kanto J, Erkkola R . Transfer of nitrazepam across the human placenta. Eur J Clin Pharmacol. 1977; 12(5):355-7. DOI: 10.1007/BF00562451. View

DE LOUVOIS J . The bacteriology and chemotherapy of brain abscess. J Antimicrob Chemother. 1978; 4(5):395-413. DOI: 10.1093/jac/4.5.395. View

Aaltonen L, Kanto J, Salo M . Cerebrospinal fluid concentrations and serum protein binding of lorazepam and its conjugate. Acta Pharmacol Toxicol (Copenh). 1980; 46(2):156-8. DOI: 10.1111/j.1600-0773.1980.tb02436.x. View

Neil-Dwyer G, Bartlett J, Mcainsh J, Cruickshank J . Beta-adrenoceptor blockers and the blood-brian barrier. Br J Clin Pharmacol. 1981; 11(6):549-53. PMC: 1402194. DOI: 10.1111/j.1365-2125.1981.tb01169.x. View

10.

Oyama T, Jin T, Yamaya R, Ling N, Guillemin R . Profound analgesic effects of beta-endorphin in man. Lancet. 1980; 1(8160):122-4. DOI: 10.1016/s0140-6736(80)90606-6. View

11.

Bond A, Lader M . Residual effects of hypnotics. Psychopharmacologia. 1972; 25(2):117-32. DOI: 10.1007/BF00423189. View

12.

Dobbing J . The development of the blood-brain barrier. Prog Brain Res. 1968; 29:417-27. DOI: 10.1016/S0079-6123(08)64172-2. View

13.

Price R . Histopathology of CNS leukemia and complications of therapy. Am J Pediatr Hematol Oncol. 1979; 1(1):21-30. View

14.

Lankelma J, Lippens R, Termond E, van der Kleijn E . Change in transfer rate of methotrexate from spinal fluid to plasma during intrathecal therapy in children and adults. Clin Pharmacokinet. 1980; 5(5):465-75. DOI: 10.2165/00003088-198005050-00004. View

15.

Somani S, Khanna N, Bada H . Caffeine and theophylline: serum/CSF correlation in premature infants. J Pediatr. 1980; 96(6):1091-3. DOI: 10.1016/s0022-3476(80)80652-4. View

16.

LITHANDER A, Lithander B . The passage of penicillin into the cerebrospinal fluid after parenteral administration in staphylococcic meningitis. 1. An experimental investigation on rabbits. Acta Pathol Microbiol Scand. 1962; 56:435-50. DOI: 10.1111/j.1699-0463.1962.tb04196.x. View

17.

Mirkin B . Developmental pharmacology. Annu Rev Pharmacol. 1970; 10:255-72. DOI: 10.1146/annurev.pa.10.040170.001351. View

18.

Engquist A, Chraemmer Jorgensen B, Andersen H . Epidural morphine-induced catatonia. Lancet. 1980; 2(8201):984. DOI: 10.1016/s0140-6736(80)92146-7. View

19.

Elwan O, Adam H . Relationship between blood and cerebrospinal levels of the antidepressant agent viloxazine. Eur J Clin Pharmacol. 1980; 17(3):179-82. DOI: 10.1007/BF00561897. View

20.

Jain R, Wei J, Gullino P . Pharmacokinetics of methotrexate in solid tumors. J Pharmacokinet Biopharm. 2010; 7(2):181-94. DOI: 10.1007/BF01059737. View