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PCM1 > Anticoag & Lipid Drugs > Flashcards

Anticoag & Lipid Drugs Flashcards

1
Q

Aspirin

A

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.

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2
Q

Clopidogrel

A

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.

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3
Q

Prasugrel

A

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.

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4
Q

Ticagrelor

A

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.

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5
Q

Cangrelor

A

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.

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6
Q

Dipyridamole

A

Phosphodiesterase Inhibitor

Raises platelet cAMP levels, prevents aggregation

Used for stroke prevention.

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7
Q

Cilostazol

A

Phosphodiesterase Inhibitor

Raises platelet cAMP levels, prevents aggregation

Used for intermittent claudication.

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8
Q

Abciximab

A

GP IIb/IIIa receptor blocker

Prevents platelet aggregation. Adjuncts to PCI for prevention of cardiac ischemic complications.

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9
Q

Eptifibatide

A

GP IIb/IIIa receptor blocker

Prevents platelet aggregation. Adjuncts to PCI for prevention of cardiac ischemic complications.

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10
Q

Tirofiban

A

GP IIb/IIIa receptor blocker

Prevents platelet aggregation. Adjuncts to PCI for prevention of cardiac ischemic complications.

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11
Q

Unfractionated Heparin

A

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

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12
Q

Low Molecular Weight Heparin

A

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

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13
Q

Fondaparinux

A

Penta-saccharide that is a cofactor for Anti-Thrombin 3

Forms complex with AT3 and inhibits 10a. Negligible 2a activity.

Prevent and treat DVT

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14
Q

Warfarin

A

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.

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15
Q

Desirudin

A

Parenteral Direct Thrombin Inhibitor

Monitored by aPTT.

Used in patients undergoing PCI

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16
Q

Bivalirudin

A

Parenteral Direct Thrombin Inhibitor

Monitored by aPTT.

Used in patients undergoing PCI

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17
Q

Argatroban

A

Parenteral Direct Thrombin Inhibitor

Monitored by aPTT.

Used in patients undergoing PCI

18
Q

Dabigatran Etexilate

A

Oral Direct Thrombin Inhibitor

Prodrug converted to dabigatran. Routine monitoring unnecessary.

Prevent stroke in non-valvular afib. Prevent & treat DVT & PE

19
Q

Apixaban

A

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

20
Q

Rivaroxaban

A

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

21
Q

Streptokinase

A

Non-Fibrin-Specific Thrombolytic.

Produced by b-hemolytic streptococci

Activates plasminogen bound to fibrin and free plasminogen.

22
Q

Urokinase

A

Non-Fibrin-Specific Thrombolytic

Human enzyme synthesized by kidney and found in the urine

Activates plasminogen bound to fibrin and free plasminogen

23
Q

Alteplase

A

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

24
Q

Reteplase

A

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

25
Q

Tenecteplase

A

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

26
Q

Aminocaproic Acid

A

Inhibits Plasminogen Activation

Used in hemophilia treatment and counter bleeding from fibrinolytic therapy.

27
Q

Tranexamic Acid

A

Inhibits Plasminogen Activation

Used in hemophilia treatment and counter bleeding from fibrinolytic therapy.

28
Q

Protamine Sulfate

A

Chemical Heparin Antagonist

Rich in arginine, cationic. Forms a complex with anionic heparin which is inactive.

29
Q

Vitamin K

A

Warfarin Effect Reversal

Takes 24 hours to show effects. If immediate hemostasis required, fresh frozen plasma needed.

30
Q

Plasma Fractions

A

Treat bleeding due to deficiencies in plasma coagulation factors.

31
Q

Atorvastatin

A

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

32
Q

Rosuvastatin

A

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

33
Q

Niacin

A

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.

34
Q

Gemfibrozil

A

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.

35
Q

Fenofibrate

A

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).

36
Q

Cholestyramine

A

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.

37
Q

Colestipol

A

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.

38
Q

Colesevelam

A

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.

39
Q

Ezetimibe

A

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.

40
Q

Omega-3 esters

A

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.

41
Q

Alirocumab

A

PCSK9 inhibitor, monoclonal antibody

Inhibits PCSK9, preventing degradation of LDL-receptors. Given as SC injections every 2-4 weeks. Usually given with statins.

42
Q

Evolocumab

A

PCSK9 inhibitor, monoclonal antibody

Inhibits PCSK9, preventing degradation of LDL-receptors. Given as SC injections every 2-4 weeks. Usually given with statins.

PCM1 (7 decks)

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