Drug Class
Diphenylbutylpiperidine derivatives

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.


last updated 10/25/2013

1. FDA Label for pimozide and CYP2D6

Genetic testing required

Summary

CYP2D6 genotyping should be performed at doses above 0.05mg/kg/day in children or above 4 mg/day in adults. In poor CYP2D6 metabolizers, pimozide doses should not exceed 0.05mg/kg/day in children or 4 mg/day in adults and doses should not be increased earlier than 14 days.

Annotation

PGx information can be found in the Warnings, Precautions, Contraindications and Dosage and Administration label sections.

Excerpts from the pimozine (Orap) label:

Individuals with genetic variations resulting in poor CYP2D6 metabolism (approximately 5 to 10% of the population) exhibit higher pimozide concentrations than extensive CYP2D6 metabolizers. The concentrations observed in poor CYP 2D6 metabolizers are similar to those seen with strong CYP2D6 inhibitors such as paroxetine. The time to achieve steady state pimozide concentrations is expected to be longer (approximately 2 weeks) in poor CYP2D6 metabolizers because of the prolonged half-life. Alternative dosing strategies are recommended in patients who are genetically poor CYP2D6 metabolizers.

In children: At doses above 0.05mg/kg/day, CYP2D6 genotyping should be performed. In poor CYP2D6 metabolizers, ORAP doses should not exceed 0.05mg/kg/day, and doses should not be increased earlier than 14 days.
In adults: At doses above 4 mg/day, CYP2D6 genotyping should be performed. In poor CYP2D6 metabolizers, ORAP doses should not exceed 4 mg/day, and doses should not be increased earlier than 14 days.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the pimozine (Orap) drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • congenital long QT syndrome
    • Contraindications section
    • source: PHONT
  • Death, Sudden, Cardiac
    • Contraindications section, Warnings section
    • source: PHONT
  • Long QT Syndrome
    • Contraindications section
    • source: PHONT
  • Neutropenia
    • Precautions section
    • source: U.S. Food and Drug Administration
  • tardive dyskinesia
    • Warnings section, Adverse reactions section
    • source: U.S. Food and Drug Administration
  • CYP1A2
    • metabolism/PK, Drug interactions section, Clinical pharmacology section
    • source: U.S. Food and Drug Administration
  • CYP2D6
    • dosage, metabolism/PK, Dosage & administration section, Contraindications section, Drug interactions section, Clinical pharmacology section, Precautions section
    • source: U.S. Food and Drug Administration
  • CYP3A4
    • metabolism/PK, Contraindications section, Drug interactions section, Clinical pharmacology section, Precautions section
    • source: U.S. Food and Drug Administration

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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Overview

Generic Names
Trade Names
Brand Mixture Names

PharmGKB Accession Id

PA164712690

Other Vocabularies

Drugs And Small Molecules

The following have been classified under this therapeutic category:

Clinical Trials

These are trials that mention Diphenylbutylpiperidine derivatives and are related to either pharmacogenetics or pharmacogenomics.

No trials found.

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