Metabolic interactions of central nervous system medications and selective serotonin reuptake inhibitors

Int Clin Psychopharmacol. 1999 May:14 Suppl 2:S35-47.

Abstract

Selective serotonin reuptake inhibitors (SSRIs) are prescribed alone and in combination with other psychotropic medications in the treatment of a variety of psychiatric disorders. Such combinations create the potential for pharmacokinetic interactions by affecting the activity of the cytochromes P450 (CYP450), drug metabolizing oxidative enzymes. SSRIs are not equivalent in their potential for interactions when combined with other central nervous system (CNS) medication. Generally citalopram and sertraline are characterized by weaker inhibition of CYP450 enzymes and, therefore, hold less potential for interaction than the other SSRIs. Paroxetine potently inhibits CYP2D6, which can result in increased neuroleptic serum concentrations, accompanied by increased CNS side-effects. Similarly, as a potent inhibitor of CYP2D6, fluoxetine can increase serum concentrations of neuroleptics and antidepressants and numerous case reports have documented concomitant adverse events. Fluoxetine also inhibits CYP3A and CYP2C19, increasing serum concentrations of some benzodiazepines. Fluvoxamine is a potent inhibitor of CYP1A2, a moderate inhibitor of CYP3A and a mild inhibitor of CYP2D6. Therefore, interactions with clozapine and benzodiazepines are evident.

Publication types

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

MeSH terms

  • Animals
  • Central Nervous System Agents / adverse effects*
  • Central Nervous System Agents / pharmacokinetics*
  • Central Nervous System Agents / therapeutic use
  • Depressive Disorder / complications
  • Depressive Disorder / drug therapy
  • Drug Interactions
  • Humans
  • Selective Serotonin Reuptake Inhibitors / adverse effects*
  • Selective Serotonin Reuptake Inhibitors / pharmacokinetics*
  • Selective Serotonin Reuptake Inhibitors / therapeutic use

Substances

  • Central Nervous System Agents
  • Serotonin Uptake Inhibitors