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Drugs of hemostasis

Terms in this set (17)

Glycoprotein IIb/IIIa Inhibitors
Effective therapy for the acute inhibition of platelet aggregation via blockade of platelet membrane fibrinogen receptors. Used of prevention of thrombosis following Percutaneous Coronary Interventions (PCA-angioplasty and stents) and may be of value in Acute Coronary Syndromes (ACS - Unstable Angina, and MI)
Abciximab
Action?
Therapy?
Indication?
Glycoprotein IIb:IIIa inhibitor

Monoclonal antibody, binds to IIb/IIIa, inhibits binding of fibrinogen

Acute inhibition of platelet aggregation; arterial side

PCI (percutaneous Coronary Artery
Interventions), ACS (acute coronary syndrome)
Eptifibatide
Action?
Therapy?
Indication?
Glycoprotein IIb:IIIa inhibitor

Peptide, binds to fibrinogen binding pocket on IIb/IIIa; competitive inhibitor

Acute inhibition of platelet aggregation; arterial side

PCI, ACS
Acetylsalicylic acid
Action?
Therapy?
Indication?
COX inhibitor

Irreversible COX inhibitor; blocks platelet production of TXA2, no real effect on endothelial production of PGI2

Chronic inhibition of platelet aggregation; arterial side

CAD, risk of MI; risk of TIA, CVA; arterial prosthesis, damaged endothel
Clopidogrel
Action?
Therapy?
Indication?
Platelet aggregation inhibitor

Inhibits ADP-induced expression of GpIIb:IIIa receptors, inhibits platelet aggregation

Chronic inhibition of platelet aggregation; arterial side

thrombosis prophylaxis during PCI; stroke prophylaxis, MI, ACS, PVD
Tissue Plasminogen Activator (TPA)
Action?
Therapy?
Indication?
Fibrinolytic

Protease, binds to fibrin, selectively activates bound plasminogen; lyses clot

Acute thrombolytic therapy; often with anti-platelet and -coagulant

Acute MI and stroke: benefits decrease 6-12h after event

Blocked by aminocaproic acid, inhibits plasminogen binding to fibrin
Streptokinase
Action?
Therapy?
Indication?
Fibrinolytic

Bacterial protein, binds to any plasminogen, activates to plasmin

Acute thrombolytic therapy; often with anti-platelet and -coagulant

Acute MI and stroke: benefits decrease 6-12h after event

Blocked by aminocaproic acid, inhibits plasminogen binding to fibrin
Heparin
Action?
Therapy?
Indication?
Anti-coagulant

Natural sulfated proteoglycan; binds to anti-thrombin, inactivates coag. factors kallikrein, XIIa, XIa, IXa, Xa, & IIa

Rapid anti-coagulation in hospital: WATCH PTT (1.5-2.5X norm)

Risk of thrombosis & embolism; safe in pregnancy

IV infusion or subQ injection (low MW only)

Greater effect on PTT than PT; neutralized by PF4
Warfarin
Action?
Therapy?
Indication?
Anti-coagulant (Dicoumarol)

Competitively inhibits Vitamin K Epoxide Reductase (VKOR); factors VII, IX, X, and II cannot be activated

Chronic anti-coagulation; WATCH PT/INR (2-3X normal)

Risk of thrombosis & embolism; A fib; prosthetic valves, stents & grafts; teratogenic!
Abciximab
Complications?
Bleeding 1-10%
Eptifibatide
Complications?
Bleeding
Acetylsalicylic acid
Complications?
Rare
Clopidogrel
Complications?
Bleeding when w/ ASA; Rare: thrombotic thrombocytopenic purpura (TTP)
Tissue Plasminogen Activator (TPA)
Complications?
Bleeding 2-4%; intracranial bleed 1%
Streptokinase
Complications?
Bleeding
Heparin
Complications?
Bleeding, immune thrombocytopenia (1.5%); T1/2 increased with cirrhosis & chronic renal failure
Warfarin
Complications?
Bleeding, necrotic skin ulcers, birth defects; Antibiotics, sulfinpyrazone, cimetitidine, & allopurinol will increase action; barbiturates, phenytoin & Vit K will decrease action
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