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ADP Receptor (P2Y12 Receptor) Inhibitors
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ADP Receptor (P2Y12 Receptor) Inhibitors
Examples:
Clopidogrel, prasugrel, ticagrelor and ticlopidine
are drugs in the ADP receptor (also known as P2Y12 receptor) inhibitor class.
Mechanism of action:
As discussed earlier,
ADP
is a substance released from platelets that activates other platelets and results in platelet aggregation. The drugs of this class irreversibly inhibit the ADP receptor on platelets, making them unresponsive to ADP. This results in decreased platelet aggregation.
Use:
Ticlopidine
is used for prevention of strokes in those who are unable to take
aspirin
, while
clopidogrel
is used to prevent thrombosis after a patient has coronary angioplasty to open an occluded coronary artery.
Laboratory measurement:
Like with
aspirin
, there are platelet aggregation tests that assess the ability of platelets to aggregate in vitro. A normal response to
clopidogrel
therapy (or therapy with the other drugs in this class) would be decreased platelet aggregation when a patient's platelets are exposed to platelet aggregation agonists. Genetic testing can be performed for CYP2C19, an enzyme involved in the metabolism of
clopidogrel
. This enzyme is needed to metabolize the ingested
clopidogrel
into its active form. This test may be ordered to determine if a patient who is not responding to
clopidogrel
testing has a genetic variant of the CYP2C19 enzyme.
Toxicity:
Ticlopidine
causes bone marrow suppression with neutropenia and thrombocytopenia and the values for those analytes must be monitored.
Clopidogrel
produces gastrointestinal symptoms similar to
aspirin
and doesn't have the bone marrow suppression of
ticlopidine
.
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