Adenosine Diphosphate (ADP) Blockers

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Adenosine Diphosphate (ADP) Blockers
2013-07-30 12:13:07
ADP Blockers

Pharm- ADP blockers
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  1. drugs:
    • Ticlopidine- neutropenia
    • Clopidogrel- #1
    • Prasugrel
    • Ticagrelor
  2. Kinetics of Clopidogrel:
    • Slow peak onset of action·        
    • 5 days to achieve a plateau in platelet inhibition
  3. Biological half-life of Clopidogrel, prasugrel, and ticlopidine:
    • The biologic half-lives of these drugs are longer than their elimination half-lives
    • 5 to 7 days (the life span of a platelet)
  4. indication:
    • Prevention of ischemic stroke in patients intolerant to ASA
    • Acute MI
  5. dose for Clopidogrel:
    • 75 mg po qd    is the prophylactic dose (maintenance dose)
    • MI: 300 mg PO loading dose   STAT
  6. CI:
    • Active bleeding
    • Significant hepatic impairment
  7. which ones are prodrugs?
    • Clopidogrel and ticlopidine
    •      hence- hepatic impairment CI
  8. CI for Ticlopidine:
    • Hematopoietic disorders
    • Thrombotic thrombocytopenic purpura (TTP)
  9. why are polymorphisms imp?
    • They change the therapeutic dose for your pt- greater risk for stroke and events
    • CYP450mutations (BBW)· (CYP2C19*2 and/or CYP2C19*3 alleles)
    •     May have reduced conversion of clopidogrel to its active thiol metabolite
    • Alterations of the PGY12 receptor·     
    •    VerifyNow® P2Y12 assay
  10. SE:
    Serious SE:
    • Bleeding, rash, diarrhea
    • Severe neutropenia (rare)- c/ ticlopidine (not c/ Clopidogrel)