Duration of Action of Heparin in the Body
Unfractionated heparin (UFH) has a short half-life of approximately 1.5 hours, while low molecular weight heparin (LMWH) has a longer half-life of 3-6 hours after subcutaneous injection. 1, 2
Unfractionated Heparin (UFH) Pharmacokinetics
- UFH is cleared through a combination of rapid saturable mechanisms (binding to endothelial cells and macrophages) and slower first-order mechanisms (primarily renal clearance) 2
- The half-life of UFH is approximately 1.5 hours when administered intravenously, but this is dose-dependent 1
- After entering the bloodstream, UFH binds to plasma proteins, endothelial cells, and macrophages, which affects its pharmacokinetics 2
- The anticoagulant effect of UFH is immediate when given intravenously but delayed by 1-2 hours when administered subcutaneously 2
- UFH's clearance is non-linear at therapeutic doses, with both intensity and duration of effect rising disproportionately with dose 2
Low Molecular Weight Heparin (LMWH) Pharmacokinetics
- LMWHs have a longer elimination half-life of 3-6 hours after subcutaneous injection 2
- The half-life of LMWH is dose-independent, unlike UFH 2
- Anti-Xa levels peak 3-5 hours after subcutaneous administration of LMWH 2
- LMWHs have higher bioavailability (approximately 90%) compared to UFH when administered subcutaneously 2
- LMWHs are predominantly cleared by the kidneys, which may prolong their biological half-life in patients with renal failure 2
Monitoring and Duration of Treatment
- For UFH, the activated partial thromboplastin time (aPTT) should be monitored approximately every 4 hours initially, then at appropriate intervals 3
- The therapeutic effect of UFH is considered adequate when the aPTT is 1.5 to 2 times normal 3
- For deep subcutaneous injections of UFH, tests for adequacy of dosage are best performed on samples drawn 4-6 hours after injection 3
- For LMWH, routine coagulation monitoring is generally not necessary except in specific populations (obese patients, renal insufficiency, pregnancy) 2
- When treating venous thromboembolism, a 5-day course of heparin has been shown to be as effective as a 10-day course 2
Clinical Implications
- When switching from heparin to oral anticoagulants like warfarin, full heparin therapy should be continued for several days until the INR reaches a stable therapeutic range 3
- For patients receiving intravenous heparin who are transitioning to non-warfarin oral anticoagulants, the IV infusion should be stopped immediately after administering the first dose of the oral agent 3
- Platelet counts should be monitored periodically during heparin therapy due to the risk of heparin-induced thrombocytopenia (HIT), which typically appears after 4-14 days of therapy 2
- Significant thrombocytopenia occurs in 1-5% of patients receiving heparin, while autoimmune HIT with thrombosis is a rare but dangerous complication (less than 0.2% incidence) 2
Understanding the duration of action of heparin is crucial for proper dosing, monitoring, and transitioning between anticoagulants to ensure optimal patient outcomes while minimizing bleeding risks.