1. PHARMACOGENOMIC TESTING FOR
PAIN MANAGEMENT
Research has demonstrated that genetic
factors may profoundly influence a person’s
response to medications‚ including possible
side effects.1
Physicians are increasingly
relying on pharmacogenomic testing to help
personalize treatment by predicting patient
response.
Exceltox’s advanced pharmacogenomic
testing technology analyzes structural
changes in a gene’s DNA sequence to
assess the influence of a drug in a
particular patient – allowing physicians
to understand if a patient could have a
toxic reaction to a drug despite a low
dosage, or if they will have any response
at all, even at a high dosage.
L A B O R A T O R I E S
Know the right drug and the right dosage
before they take the medication.
2. References
1. Cytochrome P450 Enzyme Genotyping: Optimizing Patient Care Through Pharmacogenetics. Communiqué Mayo Reference Services. 2005
Sep. Vol 30, No. 9.
DCO 010-003 8/27/14
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Knowing the right drug and the right dosage
for every patient in pain.
That’s personalized medicine,
powered by Exceltox Pharmacogenomics testing.
Characterizing Metabolic Types
There are four metabolic types associated
with CYP450 gene variants:
• Extensive Metabolizers (EM)
• Poor Metabolizers (PM)
• Intermediate Metabolizers (IM)
• Ultra-rapid Metabolizers (UM)
Table 1 explains the effects of CYP variants
when interacting with Active Drug and
Prodrug therapies.
CYP2D6 and CYP3A4/5
CYP2D6 and CYP3A4/5 are important
enzymes within the Cytochrome P450 family,
that are believed to metabolize ~30% of all
pharmaceuticals.1
Both are critical in
metabolizing many commonly prescribed
opioids such as codeine, dihydrocodeine,
oxycontin, and hydrocodone.
CYP phenotype and genotype
Increased efficacy
Active metabolite may
accumulate
Usually requires lower dose to
avoid toxic accumulation
Normal Normal
Normal Normal
Increased efficacy
Rapid onset of effect
May require lower dose to
prevent excessive accumulation
of active drug
•
•
•
Decreased efficacy
Prodrug may accumulate
May require lower dose to
avoid toxic accumulation or
may require atlernate drug.
Active Drug
(inactived by metabolism)
Drug Inactive
Drug
CYP2D6
CYP3A4/5
Prodrug
(needs metabolism to produce active drug)
Prodrug Active
Drug
CYP2D6
CYP3A4/5
Ultra-rapid
Normal Normal
NormalNormal
Extensive
Normal
Normal
Intermediate
Normal
Defective
Poor
Defective
Defective
Table 1: The Effects of CYP Variants on Therapeutic Efficacy
Decreased efficacy
Active drug rapidly inactivated
Usually requires higher dose
to offset inactivation
•
•
•
•
•
•
•
•
•
• May help physicians implement the appropriate
drug and dosage to minimize the risk of minor to
life threatening reactions and ensure optimal
response.
• May mitigate regulatory agency scrutiny by
providing clinical decision-making evidence for
several Schedule II narcotics.
• Cytochrome P450 genotyping tests can be
performed without taking patients off their
medications.1
• Testing information can be used as an adjunct to
other tools for clearer guidance in selecting among
various therapeutic choices each patient.
Benefits of Pharmacogenomic Testing for Opioids
Pharmacogenomic Testing for Response to Opioids
Cytochrome P450 Enzymes
CYP450 enzymes are a group of proteins that help the body metabolize a wide variety of medications.
Genetic variants shared by a large part of the human population of CYP450 alter the rate of drug metabolism
– causing increased or decreased drug efficacy or adverse drug reactions.
L A B O R A T O R I E S