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Coagulation Drugs

This document summarizes different antiplatelet and anticoagulant medications, their mechanisms of action, uses, and side effects. It describes how aspirin, clopidogrel, ticlopidine, and abciximab/eptifibatide work as antiplatelet agents by inhibiting thromboxane A2, blocking the P2Y12 receptor, or inhibiting the GpIIb/IIIa receptor. It also outlines how unfractionated and low molecular weight heparins, warfarin, and direct thrombin inhibitors like hirudin and argatroban prevent thrombosis through inhibiting thrombin or various coagulation factors. The document provides a useful overview of each medication's pharmacokinetics

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222 views1 page

Coagulation Drugs

This document summarizes different antiplatelet and anticoagulant medications, their mechanisms of action, uses, and side effects. It describes how aspirin, clopidogrel, ticlopidine, and abciximab/eptifibatide work as antiplatelet agents by inhibiting thromboxane A2, blocking the P2Y12 receptor, or inhibiting the GpIIb/IIIa receptor. It also outlines how unfractionated and low molecular weight heparins, warfarin, and direct thrombin inhibitors like hirudin and argatroban prevent thrombosis through inhibiting thrombin or various coagulation factors. The document provides a useful overview of each medication's pharmacokinetics

Uploaded by

med test
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PDF, TXT or read online on Scribd
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ANTIPLATELETS = Thrombus Prevention

Low Dose Aspirin (325 mg) Dipyridamole Clopidogrel Ticlopidine Abciximab Eptifibatide
Site of Action GpIIb/IIIa Inhibitors
Irreversible acetylation PDEII, TXA2 synthase, Irreversible ADP (P2Y12) Inhibitors
of COX-1 & COX-2 Adenosine uptake Inhibitor The “Clop’s” - PROdrugs Fab fragment of
Cyclic peptide
monoclonal Ab
Downstream ↑cAMP ↓Ca2+ ↓Platelet
Effects ↓TXA2 ↓Platelet activation activation
↓GIIb/IIIa linkage with fibrinogen → ↓Platelet aggregation
(no vasodilation b/c also ↓PGI2) ↓TXA2 & ↑extracellular ADP
Vasodilation
Virtues Rapid absorption (20 min)
Anti-platelet DOC Vasodilator & Anti-platelet 7-10 day duration
7-10 day action (platelet’s life)
Vices Higher doses inhibit PGI2
Doesn’t work for
30% of population is allergic
CYP2C19 poor Max inhibition at
Cannot use in pediatrics – Short duration of action
metabolizers 8-11 days
Reye’s Syndrome
(14% of pts)
Uses Long-term clot prevention Combo with ASA to prevent w/ASA to prevent W/ASA or Heparin
Stroke prevention
stroke & TIAs stent thrombosis for coronary ACS
Anti-inflammatory, anti-pyretic, ACS
thrombosis/ Angioplasties
analgesic Angina (poor) PAD ASA intolerance angioplasties
Side effects Nausea, vomiting
Bleeding – stroke, GI bleed Vasodilation - Hypotension, Prolonged bleed
Neutropenia Major Hemorrhagic event (1-10%)
Other – Tinnitus, Renal toxicity flushing TTP
TTP

ANTICOAGULANTS – Thrombus prevention


HMW Heparin LMV Heparin / Warfarin Hirudin, Bivalirudin
Dalteparin Argatroban, Dabigatran
Site of Action ↑ATIII activity 1000x Vitamin K epoxide reductase inhibitor Thrombin Inhibitors
↓γ-carboxylation Vit. K dependent factors Bind active site
Factors Inhibited II, VII, IX, X, XI, XII (ser protease) X only II, VII, IX, X + Protein C & S V, VIII (cofactors)
Monitor with aPTT Monitor with aPTT Monitor with PT or INR (2-3) VII, FXI (serine proteases)
Administration/ Inpatient - IV or SC only Outpatient - 1 SC/day Slow onset of action (8-12 hrs) Dabigatran – oral 2/day
Drug properties Slower absorption Faster absorption Max effect (3-5 days) – keep on Heparin Hirudin – irreversible
Short duration (T½ = 1 hr) Long duration (T½ = 4 hr) ↓ by ↑CYP2P (barbiturates, rifampicin) Argatroban - reversible
↑ by ↓CYP2P (metronidazole (abx), cimetidine
Uses / Benefits Acute DVT, PE DVT, PE, Acute DVT, PE Alternatives to heparin in pts
Angina, acute MI Unstable angina, thrombosis Post-acute MI, prosthetic heart valves with heparin-induced
CAN use during pregnancy Less monitoring needed Chronic A-fib thrombocytopenia
Contraindications Hypocoagulable states/Bleeds CANNOT use during pregnancy
Bivalirudin – in angioplasties
Post-CNS surgery, HTN Drug rxns (below)
Side effects Bleeding, Lower risk of ↑Effects ↓Effects Dabigatran – ↓stroke in a-fib;
Heparin-induced thrombocytopenia & ASA, anabolic Chronic alcohol use no monitoring, rapid onset,
thrombocytopenia (aka HIT) osteoporosis steroids, Abx, loop OCP, corticosteroids no drug rxns
Osteoporosis/Fractures diuretics, fibrates Cholestyramine**
Tamoxifen ↑Vit K Essentially needs no monitoring
Hypoglycemia, ↓Vit. K
Antidote Protamine sulfate Incomplete -Protamine sulfate Vitamin K1 (phytonadione)

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