Anti-coagulants Flashcards by Chris Anderson | Brainscape

Q

Drug list?

A

Aspirin, Clopidogrel, Ticlopidine, Abciximab, Eptifibatide, Dipyridamole, Dabigatran etexilate, Hirudin, Argatroban, Bivalirudin, Rivaroxaban, HMW-Heparin, LMW-Heparin, Warfarin, Streptokinase, Alteplase, tPA, Activase, Reteplase, Tenecteplase

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Q

Aspirin (MoA)

A

Irreversibly acetylates Cox-1 and Cox-2&raquo_space; TxA2 formation is inhibited.

Inhibits PGI2 (prostacycline) at higher doses, which lessens the effect

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Q

Clopidogrel (MoA)

A

Prodrug (CYP2C19)

Irreversibly inhbits P2Y12 (ADP receptor)

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Q

Ticlopidine (MoA)

A

Prodrug (CYP2C19)

Irreversibly inhbits P2Y12 (ADP receptor)

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Q

Abciximab (MoA)

A

Fab frag against GPIIB/IIIA

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Q

Eptifibatide (MoA)

A

Peptide antagonist at fibrinogen binding site on GPIIB/IIIA

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Q

Dipyridamole (MoA)

A

Phosphodiesterase inhibitor (cAMP>AMP). cAMP levels rise > Ca decreases > platelet activation decreases.

Inhibits adenosine uptake

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Q

Dabigatran Etexilate (MoA)

A

Directly inhibits thrombin

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Q

Hirudin (MoA)

A

Irreversibly inhibits thrombin

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Q

Argatroban (MoA)

A

Reversibly inhibits thrombin

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Q

Bivalirudin (MoA)

A

Reversibly inhibits thrombin

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Q

Rivaroxaban (MoA)

A

Used for DVT pts

Inhibits factor 10

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Q

HMW-heparin (MoA)

A

Inhibits factors 9, 10, and thrombin by greatly increasing Anti-thrombin III activity

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Q

LMW-heparin (MoA)

A

Inhibits factor 10 via anti-thrombin, but not the others

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Q

Warfarin (MoA)

A

Blocks vit k epoxide reductase and prevents maturation of prothrombin, factors 7, 9, and 10

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Q

Streptokinase (MoA)

A

Combines with plasminogen to make an active complex for the conversion to plasmin

Q

Alteplase (MoA)

A

Directly converts plasminogen to plasmin

Q

tPA (MoA)

A

Directly converts plasminogen to plasmin

Q

Activase (MoA)

A

Directly converts plasminogen to plasmin

Q

Releplase (MoA)

A

Directly converts plasminogen to plasmin

Q

Tenecteplase (MoA)

A

Directly converts plasminogen to plasmin

Q

What are the anti-platelet drugs we need to know?

A

Prevent platelet activation/aggregation:

Aspirin, Clopidogrel/Ticlopidine, Abciximab/eptifibatide, and dipyridamole

Q

What are the anti-coagulants that we need to know?

A

Inhibit clotting cascade to prevent fibrin clot formation:

Dabigatran etexilate, HMW/LMW-heparin, Warfarin, Rivaroxaban

Q

What are the thrombolytics that we need to know?

A

Activate plasmin to break up clots:

Streptokinase, Alteplase (tPA), Reteplase, Tenecteplase

Q

Aspirin - adverse effects

A

1) 30% resistance in population
2) Bleeding (stroke, GI)
3) Tinnitus
4) Reye’s syndrome (multiorgan symptoms, but brain and liver get affected most. Hypoglycemia present)

Q

Clopidogrel/Ticlopidine - adverse effects

A

1) Prolonged bleeding
2) TTP
3) Poor metabolizers (Cyp2c19*2 or *3) cant convert the prodrug
4) Ticlo - nausea/vomiting, SEVERE neutropenia

Q

Abciximab/Eptifibatide - adverse effects

A

1) 10% major hemorrhagic event
2) Thrombocytopenia
3) Epti is renal metabolism, so use abciximab for renal disease

Q

Dipyridamole - adverse effects

A

1) Coronary steal
2) Hypotension
3) Bleeding

Q

Dabigatran etexilate - adverse effects

A

1) Hemorrhage
2) Heartburn, GI upset
3) MI risk

Q

Hirudin, Argatroban, Bivalirudin - adverse effects

A

Bleeding

Q

HMW/LMW-Heparin - adverse effects

A

1) thrombocytopenia

Overdose treated with protamine sulfate (not as effective for LMW)

Q

Rivaroxaban- adverse effects

A

Bleeding

Q

Warfarin - adverse effects

A

1) bleeding
2) crosses placenta and causes hemorrhage

Increased potency with cimetidine aspirin, vit k def, steroids, tamoxifen, oral hypoglycemics

Decreased potency with contraceptives, barbiturates

CYP2C9 induced with barbiturates, rifampicin
CYP2C9 inhibited with cimetidine

Q

Thrombolytics - adverse effects

A

1) hemorrhage

Do not use with prior hemorrhage of any kind