Clinical pharmacokinetics of cerebrospinal fluid

Clin Pharmacokinet. Jul-Aug 1982;7(4):312-35. doi: 10.2165/00003088-198207040-00003.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Anti-Infective Agents / cerebrospinal fluid
  • Antidepressive Agents / cerebrospinal fluid
  • Antineoplastic Agents / cerebrospinal fluid
  • Blood-Brain Barrier
  • Cardiovascular Agents / cerebrospinal fluid
  • Cell Membrane Permeability
  • Central Nervous System Depressants / cerebrospinal fluid
  • Humans
  • Kinetics
  • Models, Biological
  • Pharmaceutical Preparations / cerebrospinal fluid*
  • Protein Binding


  • Anti-Infective Agents
  • Antidepressive Agents
  • Antineoplastic Agents
  • Cardiovascular Agents
  • Central Nervous System Depressants
  • Pharmaceutical Preparations