Anticoag & Lipid Drugs Flashcards
Aspirin
Irreversible COX Inhibitor
Prevents TXA2 from acting on its Gq receptor which would increase affinity of GP2b/3a receptor
Reduce risk of death and MI in pt with CAD or risk factors. Reduce risk of death and recurrent stroke in pt with hx of stroke or TIA.
Clopidogrel
Irreversible ADP Receptor Blocker
Binds P2Y12, increases cAMP, reduces platelet aggregation.
Prodrug converted to active form by CYP2C19. Avoid concomitant use with Omeprazole.
Given Orally. Treat acute coronary syndrome. Preventive treatment of pt with risk of thromboembolism, MI, stroke.
Prasugrel
Irreversible ADP receptor blocker
Binds P2Y12, increases cAMP, reduces platelet aggregation.
Prodrug converted to active form more efficiently than clopidogrel.
Given Orally. Treat acute coronary syndrome. Preventive treatment of pt with risk of thromboembolism, MI, stroke.
Ticagrelor
Reversible ADP receptor blocker
Binds P2Y12, increases cAMP, reduces platelet aggregation.
Given Orally. Treat acute coronary syndrome. Preventive treatment of pt with risk of thromboembolism, MI, stroke.
Cangrelor
Reversible ADP receptor blocker
Binds P2Y12, increases cAMP, reduces platelet aggregation.
Given IV. Treat acute coronary syndrome. Preventive treatment of pt with risk of thromboembolism, MI, stroke.
Dipyridamole
Phosphodiesterase Inhibitor
Raises platelet cAMP levels, prevents aggregation
Used for stroke prevention.
Cilostazol
Phosphodiesterase Inhibitor
Raises platelet cAMP levels, prevents aggregation
Used for intermittent claudication.
Abciximab
GP IIb/IIIa receptor blocker
Prevents platelet aggregation. Adjuncts to PCI for prevention of cardiac ischemic complications.
Eptifibatide
GP IIb/IIIa receptor blocker
Prevents platelet aggregation. Adjuncts to PCI for prevention of cardiac ischemic complications.
Tirofiban
GP IIb/IIIa receptor blocker
Prevents platelet aggregation. Adjuncts to PCI for prevention of cardiac ischemic complications.
Unfractionated Heparin
Co-factor for Anti-Thrombin 3
Forms complex with AT3 and inhibits Thrombin (2a) and 10a.
AE: Heparin Induced Thrombocytopenia due to Platelet Factor 4
Uses: DVT, Pulmonary embolism, MI, DOC in pregnancy
Low Molecular Weight Heparin
Co-factor for Anti-Thrombin 3
Forms complex with At3 and inhibits 10a. Inhibits 2a less efficiently, due to inability to form Ternary complex.
AE: Heparin Induced Thrombocytopenia due to Platelet Factor 4
Uses: DVT, Pulmonary Embolism, MI, DOC during pregnancy
Fondaparinux
Penta-saccharide that is a cofactor for Anti-Thrombin 3
Forms complex with AT3 and inhibits 10a. Negligible 2a activity.
Prevent and treat DVT
Warfarin
Vitamin K antagonist
Inhibits Vit K Epoxide Reductase- prevents regeneration of reduced (active) form of Vit K necessary for y-carboxylation (activation) of clotting factors.
Effects seen in 24h, peak effect in 72-96h, duration of action 2-5 days. Monitor effects via PT.
Used to prevent and treat DVT, PE and prevent thromboembolism in Afib.
AE: Warfarin induced skin necrosis in pt with deficiency of proteins C or S. Pregnancy category X. Interactions with CYP450 inhibitors and inducers.
Desirudin
Parenteral Direct Thrombin Inhibitor
Monitored by aPTT.
Used in patients undergoing PCI
Bivalirudin
Parenteral Direct Thrombin Inhibitor
Monitored by aPTT.
Used in patients undergoing PCI
Argatroban
Parenteral Direct Thrombin Inhibitor
Monitored by aPTT.
Used in patients undergoing PCI
Dabigatran Etexilate
Oral Direct Thrombin Inhibitor
Prodrug converted to dabigatran. Routine monitoring unnecessary.
Prevent stroke in non-valvular afib. Prevent & treat DVT & PE
Apixaban
Oral direct Factor 10a inhibitor
Doesn’t require monitoring. Doesn’t require heparin pre-treatment for DVT & PE.
Prevent stroke in non-valvular afib. Prevent & treat DVT & PE
Rivaroxaban
Oral direct Factor 10a inhibitor
Doesn’t require monitoring. Doesn’t require heparin pre-treatment for DVT & PE.
Prevent stroke in non-valvular afib. Prevent & treat DVT & PE
Streptokinase
Non-Fibrin-Specific Thrombolytic.
Produced by b-hemolytic streptococci
Activates plasminogen bound to fibrin and free plasminogen.
Urokinase
Non-Fibrin-Specific Thrombolytic
Human enzyme synthesized by kidney and found in the urine
Activates plasminogen bound to fibrin and free plasminogen
Alteplase
Fibrin-Specific Thrombolytic
Recombinant Tissue Plasminogen Activator. Activates plasminogen bound to thrombin in a thrombus.
Used for Acute STEMI, Acute Ischemic Stroke, Acute massive PE
Reteplase
Fibrin-Specific Thrombolytic
Recombinant Variant of Tissue Plasminogen Activator with a longer Half-Life. Activates plasminogen bound to thrombin in a thrombus.
Used for Acute STEMI
Tenecteplase
Fibrin-Specific Thrombolytic
Recombinant Variant of Tissue Plasminogen Activator with a longer Half-Life. Activates plasminogen bound to thrombin in a thrombus.
Used for Acute STEMI
Aminocaproic Acid
Inhibits Plasminogen Activation
Used in hemophilia treatment and counter bleeding from fibrinolytic therapy.
Tranexamic Acid
Inhibits Plasminogen Activation
Used in hemophilia treatment and counter bleeding from fibrinolytic therapy.
Protamine Sulfate
Chemical Heparin Antagonist
Rich in arginine, cationic. Forms a complex with anionic heparin which is inactive.
Vitamin K
Warfarin Effect Reversal
Takes 24 hours to show effects. If immediate hemostasis required, fresh frozen plasma needed.
Plasma Fractions
Treat bleeding due to deficiencies in plasma coagulation factors.
Atorvastatin
HMG-CoA Reductase Inhibitor
Effective at lowering LDL. Slightly lowers TG and slightly increases TG.
2nd most effective Statin.
AE: Pregnancy Category X, elevation of ALT/AST, Rhabdomyolysis
Rosuvastatin
HMG-CoA Reductase Inhibitor
Effective at lowering LDL. Slightly lowers TG and slightly increases TG.
Most effective Statin.
AE: Pregnancy Category X, elevation of ALT/AST, Rhabdomyolysis
Niacin
Hormone Sensitive Lipase Inhibitor
Gi receptor on adipocytes which inhibits HSL. Leads to reduction in liver TG, VLDL, and LDL production. Increases LPL activity, promoting clearance of TG from CM and VLDL.
Most pronounced effect- increase in HDL.
AE: Intense cutaneous flush, Acanthosis nigricans, hepatotoxicity, hyperglycemia, hyperuricemia, atrial arrhythmias, amblyopia, maculopathy.
Gemfibrozil
PPAR-a receptor activator
PPAR-a receptors in liver and brown adipose tissue lead to increased expression of LPL, apoC3, and b-oxidation of fatty acids.
Raises HDL, lowers TG. Can increase LDL.
DOC in severe hypertriglyceridemia, highest TG reduction.
AE: Mild GI disturbances, Myositis, Rhabdomyolysis, Lithiasis (gallstones). Particular to Gemfibrozil: Inhibits hepatic uptake of statins, increases risk of rhabdomyolysis.
Fenofibrate
PPAR-a receptor activator
PPAR-a receptors in liver and brown adipose tissue lead to increased expression of LPL, apoC3, and b-oxidation of fatty acids.
Raises HDL, lowers TG. Can increase LDL.
DOC in severe hypertriglyceridemia, highest TG reduction. Particular to Fenofibrate: Better choice if pt is taking a statin.
AE: Mild GI disturbances, Myositis, Rhabdomyolysis, Lithiasis (gallstones).
Cholestyramine
Bile Acid-Binding Resin
Prevents Bile Acid Reabsorption. Useful in pt with isolated increased LDL. If high TG, VLDL may increase.
Decreases LDL, increases HDL. DOC for pregnant women and children. Ineffective in pt with lack of functional LDL-receptors.
AE: bloating, nausea, cramping constipation. Colesevelam has fewest GI AEs. May increase TGs, CI in hypertriglyceridemia.
Colestipol
Bile Acid-Binding Resin
Prevents Bile Acid Reabsorption. Useful in pt with isolated increased LDL. If high TG, VLDL may increase.
Decreases LDL, increases HDL. DOC for pregnant women and children. Ineffective in pt with lack of functional LDL-receptors.
AE: bloating, nausea, cramping constipation. Colesevelam has fewest GI AEs. May increase TGs, CI in hypertriglyceridemia.
Colesevelam
Bile Acid-Binding Resin
Prevents Bile Acid Reabsorption. Useful in pt with isolated increased LDL. If high TG, VLDL may increase.
Decreases LDL, increases HDL. DOC for pregnant women and children. Ineffective in pt with lack of functional LDL-receptors.
AE: bloating, nausea, cramping constipation. Colesevelam has fewest GI AEs. May increase TGs, CI in hypertriglyceridemia.
Ezetimibe
Cholesterol Absorption Inhibitor
Inhibits NPC1L1, an intestinal transport protein. Prevents absorption of dietary and biliary cholesterol. Prodrug, conjugated to active glucuronide in liver and small intestine to be activated.
First non-statin drug that is considered to be given as a statin adjunct.
AE: reversible impaired hepatic function, myositis. Rare. Should not be given with bile-acid binding resins, will not be absorbed.
Omega-3 esters
Ester of EPA and DHA. Reduce liver TG synthesis, increase b-oxidation.
HDL may increase. EPA only products won’t increase LDL-C. Best at reducing TG levels in pt with hypertriglyceridemia.
Alirocumab
PCSK9 inhibitor, monoclonal antibody
Inhibits PCSK9, preventing degradation of LDL-receptors. Given as SC injections every 2-4 weeks. Usually given with statins.
Evolocumab
PCSK9 inhibitor, monoclonal antibody
Inhibits PCSK9, preventing degradation of LDL-receptors. Given as SC injections every 2-4 weeks. Usually given with statins.
