Pharmacokinetic drug interactions of new antidepressants

A review of the effects on the metabolism of other drugs

Elliott Richelson

Research output: Contribution to journalArticle

124 Citations (Scopus)

Abstract

Seven of the newest antidepressants are the serotonin-selective reuptake inhibitors (fluoxetine, sertraline, paroxetine, and fluvoxamine [currently approved in the United States only for obsessive-compulsive disorder]), a serotonin-norepinephrine reuptake inhibitor (venlafaxine), a postsynaptic serotonin antagonist-presynaptic serotonin reuptake inhibitor (nefazodone), and a presynaptic-postsynaptic noradrenergic-serotonergic receptor antagonist (mirtazapine). Many of these drugs are potent inhibitors of the cytochrome P- 450 enzymes (CYPs) of the liver. The isoforms of the CYPs most relevant to the use of antidepressants are CYP1A2. CYP2C9, CYP2C19, CYP2D6, and CYP3A4. CYP inhibition may affect the metabolism of numerous drugs in several classes that are substrates for these isoenzymes, with potentially serious consequences. To minimize the potential for an adverse event, the practitioner must remember the drug-drug interactions and possible consequences when one of these antidepressants is being prescribed. A 'primer' on drug metabolism is included herein, which serves as a basis for understanding these interactions. Each of the isoenzymes of the CYPs is discussed in relationship to the drugs they metabolize, and appropriate cautions are recommended for concurrent administration of these new antidepressants and other drugs most frequently prescribed to elderly patients.

Original languageEnglish (US)
Pages (from-to)835-847
Number of pages13
JournalMayo Clinic Proceedings
Volume72
Issue number9
StatePublished - 1997

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Drug Interactions
Antidepressive Agents
Pharmacokinetics
Pharmaceutical Preparations
Serotonin Uptake Inhibitors
Isoenzymes
Fluvoxamine
Sertraline
Cytochrome P-450 CYP3A
Cytochrome P-450 CYP1A2
Cytochrome P-450 CYP2D6
Paroxetine
Serotonin Antagonists
Fluoxetine
Obsessive-Compulsive Disorder
Protein Isoforms
Metabolic Side Effects of Drugs and Substances
Liver

ASJC Scopus subject areas

  • Medicine(all)

Cite this

Pharmacokinetic drug interactions of new antidepressants : A review of the effects on the metabolism of other drugs. / Richelson, Elliott.

In: Mayo Clinic Proceedings, Vol. 72, No. 9, 1997, p. 835-847.

Research output: Contribution to journalArticle

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