Class antiplatelet
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This document discusses various antiplatelet and antithrombotic drugs used to prevent thrombosis. It describes the mechanisms and indications for aspirin, clopidogrel, ticlopidine, cilostazol, abciximab, eptifibatide, tirofiban, terutroban, and dipyridamole. It also briefly mentions prasugrel and ticagrelor, newer P2Y12 receptor antagonists with more rapid onset of action than clopidogrel. The document lists common indications for antiplatelet therapy as myocardial infarction, unstable angina, coronary artery bypass grafts, prosthetic heart valves, venous thromboembolism, and transient ischemic
Class antiplatelet
- 1. Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC. 1
- 6. ADP receptor blocker CLOPIDOGREL TICLOPIDINE COX inhibitor (Aspirin) Phosphodiesterase inhibitor- DIPYRIDAMOLE, CILOSTAZOLE Gb IIb/IIIa receptor blockers ABCIXIMAB EPTIFIBATIDE TIROFIBAN TXA2 receptor TERUTROBAN
- 7. Aspirin N.B.Aspirin inhibitsThromboxane A2 & prostacyclin too, but the former is more affected because platelets don’t have nuclei can’t synthesize new enzymes for next 7 daysplatelets life span
- 8. Most authorities recommend initial therapy with a dose of 160 mg (one half-tablet) to 325 mg (one adult tablet) Aspirin should be crushed/chewed (to facilitate faster absorption by breaking the enteric-coated delayed release tablet
- 9. Prophylaxis against unstable angina Post MI Post stroke Adverse effects GI –ulceration Prolonged bleeding time ↑ risk of hemorrhage
- 10. It is an inhibitor of phosphodiesterase III (PDE III) enzyme Vasodilator and inhibitor of platelet aggregation Initially approved for Intermittent claudication Indicated for the reduction of events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent MI or established peripheral arterial disease.
- 11. ABCIXIMAB is composed of 7E3 Fab fragments. derived from murine (mouse) Humanized monoclonal antibody. directed against glycoprotein receptor type GPIIb/IIIa. Mechanism: The m7E3 Fab binds selectively to the glycoprotein GPIIb/IIIa receptors inhibiting platelet aggregation Plasma T1/2- 30min Bolus –followed by slow IV Angioplasty, recurrent MI Major side effect- bleeding, thrombocytopenia, bleeding
- 12. TIROFIBAN -non-peptic Synthetic arginine-glycine- aspartic acid (R-G-D) sequence mimetics. Hence, it blocks the binding of fibrinogen to glycoprotein GPIIb/IIIa receptors They are given intravenously for the reduction of thrombotic complications during coronary angioplasty (if they are given orally they are toxic) Clinical trials showed reductions in the incidence of death and non-fatal MI in response to the use of tirofiban.
- 13. Synthetic cyclic Peptide inhibitor of fibrinogen binding site on Gp IIb/ 3a receptors on platelets It does not bind to receptors for vWF Duration of action : 30 – 45 mins Should be continued for 18-24 hours Superior to Abciximab for upstream use S/E-bleeding
- 14. TICLOPIDINE & CLOPIDOGREL They inhibit irreversibly ADP binding to receptors inhibit platelet aggregation No effect on PG synthesis Used in aspirin intolerant patients
- 15. Acts by in inhibiting phoshodiesterase enzyme Incompletely absorbed from the gastrointestinal tract with peak plasma concentration occurring about 75 minutes after oral administration More than 90% bound to plasma proteins A terminal half-life of 10 to 12 hours Metabolised in the liver Mainly excreted as glucuronides in the bile; a small amount is excreted in the urine
- 16. It is an inhibitor of phosphodiesterase III (PDE III) enzyme Vasodilator and inhibitor of platelet aggregation Intermittent claudication Indicated for the reduction of events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent MI or established peripheral arterial disease C/I- CHF patients
- 17. Prasugrel Thienopyridine More rapid onset of action than clopidogrel Irreversible inhibitor of the P2Y12 receptor Beneficial in the treatment and prevention of ACS and the prevention of thromboembolic events Adenosine Diphosphate-Receptor Antagonists
- 18. Ticagrelor Cyclo-pentyl-triazo-pyrimidine (CPTP) More rapid onset of action than clopidogrel Reversible inhibitor of the P2Y12 receptor
- 19. Myocardial infarction Unstable angina Coronary bypass implants Prosthetic heart valves and arteriovenous shunts Venous thromboembolism and PVD Cerebrovascular transient ischemic attacks