Aspirin

- mechanisms/target

- uses

Mechanism:

- inhibits platelet cyclooxygenase (COX) thus inhibiting synthesis of platelet thromboxane A₂ (TXA₂)

- inhibits plate let release reaction as well

Uses:

- reduces the risk of reinfarction

Dipyridamole

- type of drug

- mechanism/target

- uses

Type of drug:  antiplatelet drug

Mechanism of action:

- inhibits phosphodiesterase (PDE) activity thus increases intracellular cAMP

Uses:

- coronary vasodilator

- good only in combo with warfin for post-op primary prophylaxis of thromboemboli in patients with prosthetic heart valves

- combo with aspirin could reduce strokes in patients with history of strokes

Ticlopidine + Clopidogrel

- type of drug

- mechanism/target

- uses

Type of drug: antiplatelet drugs

Mechansism/target:

- increase intracellular cAMP through inhibition of P2Y₁₂ receptor

- P2Y₁₂ receptor binds ADP causing ↓ adenylate cyclase activity thus allowing platelet function to occur

Uses:

- good for patients that DO NOT tolerate aspirin or have failed aspirin therapy

- indicated for patients who have experienced stroke precursors

- good in combo with aspirin for patients undergoing angioplasty

Abciximab

- use

- type of drug

- combo therapy

Use:

- monoclonal antibody for percutaneous angioplasty for prophylaxis of coronary thromboses

Type of drug:

- glycoprotein IIb/IIIa (α_IIbβ₃) inhibitor

-antiplatelet drug

Combo:

- aspirin and heparin

Eptifibatide

Tirofiban

-type of drug

-use

-other

Type of drug:

- glycoprotein IIb/IIIa (α_IIbβ₃) inhibitor

- antiplatelet drug

Use:

- unstable angina 

- angioplastic coronary interventions

Other:

- duration 6-12 hours

- Tirofiban is non-peptide while eptifabtide is a cyclic peptide

Warfin

-mechanism

-adverse reactions

-pharmacokinetics

Mechanism:

- vitamin K antagonist

Adverse reactions:

- hemorrhage

- birth defects

- dermatitis

- small intestine necrosis

Pharmacokinetics:

- well absorbed orally

- >95% bound to plasma protein

- inactivated by hepatic microsomal enzymes

Factors 2, 7, 9, 10

C protein

S protein

Z protein

Heparin

- type of drug

- mechanism

- uses

- Side effects

Type of drug: anticoagulant

Mechanism:

- interacts with circulating antithrombin-3 and accelerates its action to inactivate factors 9, 10, and thrombin

- releases LPL to decrease platelet adhesiveness to endothelial cells

Uses:

- IV admin in hospital to initiate treatment of venous thromboses and pulmonary embolisms, unstable angina, acute MI, during and after angioplasty, cardiopulmonary bypass surgery

Side effects:

- hemorrhage

- thrombocytopenia

- fever

- osteoporosis

- hypersensitivity reactions

- does not cross placenta

- Protamine sulfate can reverse heparin-induced hemorrhage

Fondaparinux

- type of drug

- mechanism

- uses

- side effects

Type of drug: anticoagulant

Mechanism:

- synthetic heparin that has AT-3 binding site that inhibits only factor 10

- faster acting

Uses:

- for patients undergoing hip surgery, prophylaxis of PEs and DVTs

Side effects:

- contraindicated for patients with renal failure

Danaparoid

-type of drug

-mechanism

-uses

-side effects

Type of drug: anticoagulant

Mechanism:

- mixture of nonheparin GAGs

- promotes inhibition of factor 10 by antithrombin

Uses:

- prophylaxis of DVT in patients with heparin-induced thrombocytopenia

Side effects:

- not available in US

Hirudin

-type of drug

-mechanism

-uses

-side effects

Type of drug: anticoagulant

Mechanism: 

- antithrobmin 3 independent inhibitor of thrombin

- potent

Uses:

- naturally occuring in leaches

Lepirudin

-type of drug

-mechanism

-uses

-side effects

Type of drug: anticoagulant

Mechanism:

- inhibits thrombin independently

- derivative of hirudin

Uses:

- treatment of patients with heparin induced thrombocytopenia

- parenteral administration

- excreted by kidneys

Side effects:

- contraindicated in patients with renal failure

- needs daily monitoring with aPTT test

Bivalirudin

-type of drug

-mechanism

-uses

-side effects

Type of drug: anticoagulant

Mechanism: 

- synthetic heparin derivative binding directly to thrombin to block its access to substrates (fibrinogen)

Uses:

- can be given IV instead of heparin for coronary angioplasty

- good if AT-3 deficient

Argatroban

-type of drug

-mechanism

-uses

-side effects

Type of drug: anticoagulant

Mechanism:

- synthetic compound similar to L-arginine that acts as a competitive inhibitor of thrombin (binds catalytic site)

Uses:

- alternative to lepirudin for prophylaxis or treatment of patients with risk of developing heparin induced thrombocytopenia

Drotrecogin alfa

-type of drug

-mechanism

-uses

-side effects

Type of drug: anticoagulant

Mechanism: 

- recombinant form of human activated protein C which inhibits factors 5 & 8

Uses:

- given IV and reduces mortality in patients that are at risk for death from sepsis

Streptokinase

-type of drug

-mechanism

-uses

-side effects

Type of drug: 1G thrombolytic 

Mechanism:

- nonenzymatic protein from streptococci that forms 1:1 complex with plasminogen to promote conversion to plasmin

Uses:

- establishing blood flow post-MI

Side effects:

- hemorrhage

- allergic reactions

- systemic lytic state because 1st generation thrombolytics are not clot/fibrin selective

- not used clinically anymore

Urokinase

-type of drug

-mechanism

-uses

-side effects

Type of drug: 1G thrombolytic

Mechanism:

- serine protease; activates plasminogen directly

Uses:

- pulmonary embolism

- MI

- constant infusion for 12 hrs

Side effects:

- hemorrhage

- allergic reactions

- systemic lytic state because 1st generation thrombolytics are not clot/fibrin selective

tPAs (Alteplase, Reteplase, Tenecteplase)

-type of drug

-mechanism

-uses

-side effects

Type of drug: thrombolytic

Mechanism:

- binds selectively to fibrin and causes clot-selective fibrinolysis

Uses:

- re-establish tissue perfusion in stroke

- coronary thrombolysis (Alteplase)

- PE

- arterial occlusion

- venous thrombosis

*most important therapy in MI patients

*give in 100mg increments over 3 hr period

Side effects:

- all thrombolytics agents carry increased risk of bleeding and are contraindicated in vascular disease, recent surgery, serious trauma, patients with GI bleeds, hypertension, cancer and other bleeding risks

*aminocaproic acid & tranexamic acid inhibit plasminogen activators to control bleeding