last updated 10/25/2013

Annotation of U.S. Food and Drug Administration (FDA) label information
for desipramine and CYP2D6

On FDA Biomarker List
Actionable PGx

Summary

The FDA-approved drug label for desipramine (NORPRAMIN) notes that CYP2D6 poor metabolizers have higher than expected plasma concentrations of tricyclic antidepressants (TCAs), such as desipramine, when given typical doses. Additionally, certain drugs inhibit the activity of this isozyme and make normal metabolizers resemble poor metabolizers. It is therefore desirable to monitor TCA plasma levels whenever a TCA is going to be co-administered with another drug known to be a CYP2D6 inhibitor.

Annotation

Desipramine (NORPRAMIN) is an antidepressant drug belonging to the tricyclic antidepressants class.The FDA-approved drug label for desipramine highlights information regarding CYP2D6 poor metabolizers, as well as information about usage of drugs that inhibit CYP2D6, one of the enzymes responsible for desipramine metabolism.

Excerpt from the desipramine (NORPRAMIN) label:

The biochemical activity of the drug metabolizing isozyme cytochrome P450 2D6...is reduced in a subset of the Caucasian population (about 7% to 10% of Caucasians are so called "poor metabolizers"); reliable estimates of the prevalence of reduced P450 2D6 isozyme activity among Asian, African and other populations are not yet available. Poor metabolizers have higher than expected plasma concentrations of tricyclic antidepressants (TCAs) when given usual doses. Depending on the fraction of drug metabolized by P450 2D6, the increase in plasma concentration may be small, or quite large (8 fold increase in plasma AUC of the TCA). In addition, certain drugs inhibit the activity of this isozyme and make normal metabolizers resemble poor metabolizers...It is desirable to monitor TCA plasma levels whenever a TCA including is going to be co-administered with another drug known to be an inhibitor of P450 2D6.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the desipramine drug label.

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Genes and/or phenotypes found in this label

  • Depression
    • appears in:
      • Indications & usage section
      • Warnings section
      • Adverse reactions section
      • Precautions section
    • source: PHONT
  • Depressive Disorder
    • appears in:
      • Indications & usage section
      • Warnings section
      • Adverse reactions section
      • Precautions section
    • source: PHONT
  • Depressive Disorder, Major
    • appears in:
      • Indications & usage section
      • Warnings section
      • Adverse reactions section
      • Precautions section
    • source: PHONT
  • CYP2D6
    • appears in:
      • Precautions section
    • category:
      • metabolism/PK
    • source: U.S. Food and Drug Administration

Label History