4. ECOSPRIN
Irreversible inhibitor of COX ( needeed for production of PG and
ThXA2).
Bioavailability- 80-100%.
Protein binding- 80-90%.
Metabolism – Liver (CYPC2C19, CYP3A).
Elimination half life-2-3 hr for low dose, 15-30 hr for large dose.
Excretion- urine (80-100%), sweat, saliva, faeces.
When to stop before surgery-7 days.
C/I- allergic to NSAIDs, NSAID induced bronchospasm, peptic ulcer.
Aspirin is known to cause hemolytic anaemia in G6PD Def patients.
Avoid in hyperuricemia/gout.
Associated with Rey’s Syndrome in children.
Major Trials: ISIS-2, CURRENT OASIS-7
5. CLOPIDOGREL
Thienopyridine group, Irreversible P2Y12 ADP
receptor antagonist
Bioavailability- >50%
Protein Binding- 94-98%
Metabolism- Liver
Onset of action- 2 hrs
Elimination Half life-7-8 hrs
Duration of action – 5 days
Excretion – 50% kidney, 46% biliary
When to stop before surgery- 5 days.
Major Trials: CURE, COMMIT, CLARITY TIMI28, PCI-CURE,
CREDO, PCI-CLARITY, CURRENT OASIS-7, GRAVITAS,
6. PRASUGREL
Thienopyridine group, Irreversible P2Y12 ADP receptor antagonist
Bioavailability- >79%
Protein binding -98%
Half life – 7 Hr
Peak plasma time - 30 min.
Absorption >79%
Metabolism via CYP3A4 and CYP2B6
Excretion –urine 68%, faeces 27%
When to stop before surgery- 7 days
C/I- active bleeding, H/o TIA, Stroke, Age > 75, weight <60 kg,TTP.
Major Trials: TRITON TIMI 38, TRIOLOGY-ACS, ACCOAST
7. TICAGRELOR
Chemical class- cyclopentyl-triazolo-pyrimidine(CPTP)
Reversible P2Y12 ADP receptor antagonist
Bioavailability-36%
Protein binding - >99%
peak plasma time- 1.5 hr, 2.5 hr (AM)
metabolized by CYP3A4
Half life- 7 hr, 9 hr(AM)
excretion- 58%faeces, 26% urine
When to stop before surgery- 3 days.
C/I- major bleeding, COPD/Asthma, Bradyarrhythmia, sick sinus
syndrome,severe hepatic impairment.
Major Trials: PLATO, ATLANTIC, PEGASUS – TIMI54.
8. CILASTOZOLE
Class- Phosphodiaesterase 3 inhibitor
Mechanism- inhibit platelet aggregation induced by collagen, 5’
ADP, epinephrine and Arachidonic acid.
Protein binding- 95-98%.
Metabolism- Liver ( CYP3A4, CYP249).
Elimination time half – 11-13 hr.
Excretion – kidney.