Pharmacology
Anticoagulants — warfarin, heparin, LMWH, DOACs
Pharmacology

Anticoagulants — warfarin, heparin, LMWH, DOACs

Mechanism, monitoring, reversal, and when to pick which agent.

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◆Mechanism & monitoring

  • •Unfractionated heparin (UFH): activates antithrombin → inhibits IIa + Xa; monitor aPTT (or anti-Xa); reversed by protamine
  • •Low molecular weight heparin (LMWH, enoxaparin): inhibits Xa >> IIa; monitor anti-Xa (only in renal failure, pregnancy, extremes of weight); partial reversal with protamine
  • •Warfarin: inhibits vitamin K epoxide reductase → ↓ factors II, VII, IX, X (and proteins C, S); monitor INR (target 2–3, or 2.5–3.5 for mechanical mitral valve)
  • •DOACs: apixaban, rivaroxaban, edoxaban (anti-Xa); dabigatran (anti-IIa); no routine monitoring; renal clearance matters

◆Reversal agents

  • •Warfarin: vitamin K (PO/IV) + 4-factor PCC (immediate) or FFP (slower)
  • •Heparin: protamine sulfate (1 mg per 100 units UFH)
  • •Dabigatran: idarucizumab
  • •Apixaban / rivaroxaban: andexanet alfa (or 4-factor PCC if not available)

◆When to pick which

  • •Acute DVT/PE, hemodynamically stable: DOAC (apixaban or rivaroxaban) → continue ≥3 mo (longer if unprovoked)
  • •Pregnancy: LMWH (preferred); NEVER warfarin (teratogen) or DOACs (no data, placenta-crossing)
  • •Mechanical heart valve: WARFARIN only (DOACs failed RE-ALIGN trial)
  • •Severe renal failure (CrCl <15–30): warfarin or UFH; DOACs/LMWH require dose adjustment or avoidance
  • •Active cancer-associated VTE: DOAC (apixaban) or LMWH
  • •AFib + valvular (moderate–severe MS): WARFARIN; DOACs in non-valvular only

◆Heparin-induced thrombocytopenia (HIT)

  • •Suspect: platelet drop >50% from baseline OR <100,000 between days 5–14 of heparin (sooner if prior exposure)
  • •Paradoxical thrombosis (arterial or venous) despite low platelets
  • •Stop ALL heparin (including LMWH and flushes); start argatroban or fondaparinux (no platelet effect)
  • •Do NOT give warfarin until platelets recover and on alternative anticoag (risk of skin necrosis)
  • •4Ts score for pretest probability; confirm with anti-PF4 ELISA → serotonin release assay if equivocal

◆Other key warnings

  • •Warfarin skin necrosis: paradoxical clotting in first 5 days (protein C deficiency unmasked) — bridge with heparin
  • •Warfarin teratogen: fetal warfarin syndrome (nasal hypoplasia, stippled epiphyses), CNS abnormalities
  • •Long-term warfarin: hair loss, purple toe syndrome (cholesterol embolization), osteoporosis
  • •DOACs: do not crush enteric-coated formulations; check for drug interactions (CYP3A4 inducers ↓ levels)

Anticoagulant comparison

DrugReversal / monitoring
UFHProtamine; aPTT
LMWH (enoxaparin)Partial protamine; anti-Xa (in special cases)
WarfarinVitamin K + 4F-PCC; INR
DabigatranIdarucizumab; no routine monitoring
Apixaban / rivaroxabanAndexanet alfa or 4F-PCC; no routine monitoring

High-yield pearls

  • ◆Pregnant + VTE → LMWH (NEVER warfarin in 1st trimester or DOACs ever)
  • ◆Mechanical mitral valve → warfarin only (target INR 2.5–3.5)
  • ◆HIT: stop heparin, start argatroban; do NOT give warfarin until platelet count recovers
  • ◆Warfarin + amiodarone, fluoroquinolones, TMP-SMX, metronidazole → ↑↑ INR (CYP inhibition)
  • ◆Rifampin, carbamazepine, phenytoin, St John's wort → ↓ warfarin/DOAC effect (CYP induction)
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