Antithrombotic drugs Flashcards
Heparin
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
Enoxaparin
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
Dalteparin
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
Warfarin
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.
Dabigatran
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
Rivaroxaban
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
Apixaban
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
Aspirin
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
Clopidogrel
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
Prasugrel
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
Ticagrelor
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
Dipyridamole
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
Abciximab
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
Eptifibatide
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
Tirofiban
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
Isosorbide Mononitrate
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)
Nitroglycerin
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)
Amlodipine
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
Nefedipine
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
Felodipine
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
