Antithrombotic drugs Flashcards

1
Q

Heparin

A

Binds ATIII –> inactivates IIa and Xa Parenteral (IV / SC)

Uses:
acute coronary syndrome
venous thromboembolism

Dose-dependent t1/2
aPTT used to monitor

Adverse reactions:
Bleeding
Thrombocytopenia

Drug-Drug interactions:
NSAID
Antiplatelet agents

Overdose treatment:
Protamine

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2
Q

Enoxaparin

A

Binds ATIII –> inactivates Xa
Parenteral (IV / SC)

Uses:
acute coronary syndrome
venous thromboembolism

renal clearance

Adverse reactions:
Bleeding
Thrombocytopenia

Drug-Drug interactions:
NSAID
Antiplatelet agents

Overdose treatment:
Protamine

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3
Q

Dalteparin

A

Binds ATIII –> inactivates Xa
Parenteral (IV / SC)

Uses:
acute coronary syndrome
venous thromboembolism

renal clearance

Adverse reactions:
Bleeding
Thrombocytopenia

Drug-Drug interactions:
NSAID
Antiplatelet agents

Overdose treatment:
Protamine

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4
Q

Warfarin

A

Inhibits liver synthesis of Vit K-dep factors (II, VII, IX, and X)

Uses:
Atrail fibrillation
Large Anterior Wall MI
Venous thromboembolism prophylaxis

Oral
Hepatic Metabolism (CYP2C9)

Monitored by INR

Adverse effects:
Bleeding
Skin Necrosis

Drug-Drug Interactions:
increase effect CYP450-inhibitors
decrease effect CYP450 inducers, dietary Vitamin K.

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5
Q

Dabigatran

A

Direct thrombin (IIa) inhibitor

Uses:
atrial fibrilation
venous thromboembolism (not approved)

Oral (prodrug)
renal clearance

Adverse effects:
Bleeding
gastritis symptoms

Drug-Drug interactions:
decrease effect with P-glycoprotein inducers
increase effect with P-glycoprotein inhibitors

Antidotes:
Fresh Frozen Plasma

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6
Q

Rivaroxaban

A

Direct factor Xa inhibitor

Uses:
atrial fibrilation
DVT-PE prevention after total hip or knee replacement

Oral
hepatic clearance CYP3A

Adverse effects:
Bleeding

Drug-Drug interactions:
decrease effect with P-glycoprotein inducers
increase effect with P-glycoprotein inhibitors, CYP3A inhibitors

Antidotes:
Fresh Frozen Plasma

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7
Q

Apixaban

A

Direct factor Xa inhibitor

Uses:
atrial fibrilation
DVT-PE prevention after total hip or knee replacement

Oral
hepatic clearance CYP3A

Adverse effects:
Bleeding

Drug-Drug interactions:
decrease effect with P-glycoprotein inducers
increase effect with P-glycoprotein inhibitors, CYP3A inhibitors

Antidotes:
Fresh Frozen Plasma

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8
Q

Aspirin

A

Low dose (81 mg) “selective” of platelet COX-1

Uses:
Acute-MI
Unstable Angina
Percutaneous Intervention

Hepatic clearance

Drug-Drug interaction:
increased bleeding risk with anticoagulants

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9
Q

Clopidogrel

A

irreversible inhibition of platelet ADP (P2Y12) receptor

Uses:
Acute-MI
Unstable Angina
Percutaneous Intervention

Oral (prodrug 1x daily)

activated by CYP2C19 —-> renal and fecal excretion

Adverse Effects:
Bleeding
Dyspepsia
Gastritis

Drug-Drug interactions:
PPI may block activation of prodrug

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10
Q

Prasugrel

A

irreversible inhibition of platelet ADP (P2Y12) receptor

Uses:
Acute-MI
Unstable Angina
Percutaneous Intervention

Oral (prodrug 1x daily)

activated by CYP3A4/2B6

Adverse Effects:
Bleeding

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11
Q

Ticagrelor

A

reversible inhibition of platelet ADP (P2Y12) receptor

Uses:
Acute-MI
Unstable Angina
Percutaneous Intervention

Oral (prodrug 2x daily)

activated by CYP3A4

Adverse Effects:
Bleeding
Dyspnea
Bradyarrhythmias

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12
Q

Dipyridamole

A

Inhibits phosphodiesterase in platelets –> increase cAMP —> increase PGI2 —-> anti-aggregation effect

Uses:
secondary prevention of MI/stroke

Oral

Hepatic phase II conjugation

Adverse effects:
Dizziness, 
HA,
nausea
GI upset
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13
Q

Abciximab

A

Blocks platelet GIIb/IIIa receptor preventing fibrinogen binding and platelet aggregation
monoclonal antibody

Uses:
percutaneous intervention

Parenteral infusion

renal clearance t1/2 = 30 min

Adverse effects:
bleeding

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14
Q

Eptifibatide

A

Blocks platelet GIIb/IIIa receptor preventing fibrinogen binding and platelet aggregation
cyclic peptide

Uses:
percutaneous intervention

Parenteral infusion

renal clearance t1/2 = 2.5 hours

Adverse effects:
bleeding

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15
Q

Tirofiban

A

Blocks platelet GIIb/IIIa receptor preventing fibrinogen binding and platelet aggregation
non-peptide(small molecule)

Uses:
percutaneous intervention

Parenteral infusion

renal clearance t1/2 = 2 hours

Adverse effects:
bleeding

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16
Q

Isosorbide Mononitrate

A

NO donor
venous dilator

Uses:
Acute Angina (sublingual tablet, translingual spray) 

Prophylaxis for chronic angina (long-acting oral, topical, transdermal)

Huge 1st bypass effect

Adverse effects:
orthostatic hypotension
reflex tachycardia

Drug-Drug interactions:
sildenafil, vardenatfil, tadlafil (phosphodiesterase 5 inhibitors –> prevent breakdown of cGMP)

17
Q

Nitroglycerin

A

NO donor
venous dilator

Uses:
Acute Angina (sublingual tablet, IV) 

Prophylaxis for chronic angina (transdermal)

Huge 1st bypass effect

Adverse effects:
orthostatic hypotension
reflex tachycardia

Drug-Drug interactions:
sildenafil, vardenatfil, tadlafil (phosphodiesterase 5 inhibitors –> prevent breakdown of cGMP)

18
Q

Amlodipine

A

Dihydropyridine (L-type Ca2+ channel blocker —> effect more on vessels)

Uses:
Angina:
long-lasting decrease in peripheral vascular resistance —> reduced oxygen requirements

reduced coronary arterial tone –> aid in vasospastic angina

hypertension

Adverse effects:
hypotension
headache, flushing
peripheral edema

19
Q

Nefedipine

A

Dihydropyridine (L-type Ca2+ channel blocker —> effect more on vessels)

Uses:
Angina:
long-lasting decrease in peripheral vascular resistance —> reduced oxygen requirements

reduced coronary arterial tone –> aid in vasospastic angina

hypertension

Adverse effects:
hypotension
headache, flushing
peripheral edema

20
Q

Felodipine

A

Dihydropyridine (L-type Ca2+ channel blocker —> effect more on vessels)

Uses:
Angina:
long-lasting decrease in peripheral vascular resistance —> reduced oxygen requirements

reduced coronary arterial tone –> aid in vasospastic angina

hypertension

Adverse effects:
hypotension
headache, flushing
peripheral edema