Low Molecular Weight Heparins (LMWH's) (Last Updated - 3/10/2005)
-act primarily as inhibitors of Factor Xa (via anti-thrombin) not inhibition of thrombin (IIa)
-have < 18 monosaccharide units --> cannot bind thrombin (IIa) & anti-thrombin simultaneously to catalyze thrombin's (IIa) inhibition
-simultaneous binding requires >= 18 units
-given sub-Q QD or BID in fixed or weight-adjusted doses
-minimal in vitro effex on coag labs --> no routine lab monitoring of PT's or aPTT's
-easier than heparin due to:
1) More predictable pharmacokinetics --> weight-adjusted dosing with no routine lab monitoring
2) Decreased side effex vs. heparin (Ex.) HIT, bleeding & osteoporosis)
-Cautions:
-ESRD --> may require lab monitoring (prolonged 1/2-life of drug in ESRD)
-Uses:
1) Venous Thromboembolism
2) Venous Thrombosis
3) Pulmonary Embolus (PE)
4) Unstable Angina
-Drugs:
1) Enoxaparin (Lovenox)
2) Dalteparin (Fragmin)
3) Ardeparin (Normiflo)
4) Tinzaparin (Innohep) --> not FDA-approved
5) Nadroparin (Fraxiparine) --> not FDA-approved
6) Reviparin (Clivarine) --> not FDA-approved
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References:
Goodman & Gilman's: The Pharmacologic Basis Of Therapeutics - 10th Edition - 2001. Chapter 55.