Table 3 Pharmacological characteristics of unfractionated and low molecular weight heparins.
From: Being precise with anticoagulation to reduce adverse drug reactions: are we there yet?
Characteristic | Unfractionated heparin (UFH) | Tinzaparin | Dalteparin | Enoxaparin | Nadroparin |
---|---|---|---|---|---|
Trade name | Heparin | Innohep | Fragmin | Clexane | Fraxiparine |
Mean molecular mass (kDa) | 15 | 6.8 | 6.0 | 4.5 | 4.3 |
Dose-dependent pharmacokinetics | Yes | No | No | No | No |
Administration route | Intravenous & subcutaneous | Subcutaneous | Subcutaneous | Intravenous & subcutaneous | Intravenous & subcutaneous |
Bioavailability after SC injection (%) | Low doses: 10 High doses: 90 | 86.7 | 87 | 92 | 89 |
Protein/cell binding | Binds to macrophages, endothelial cells, platelets and many plasma proteins (e.g. lipoproteins, von Willebrand factor) | Reduced, but still occurs | Reduced, but still occurs | Reduced, but still occurs | Reduced, but still occurs |
Mean peak activity after SC injection | 2–4 | 4–6 | 4 | 3–5 | 3–6 |
Volume of distribution (L) | 4 | 4 | 3 | 5 | 3.6 |
Elimination t1/2 after SC injection | 1–2.5 | 3–4 | 3–4 | 4 | 3.5 |
Main elimination route | Low doses: cellular (liver) High doses: renal | Renal | Renal | Renal | Renal |
Monitoring | aPTT | Not routinely indicated (anti-Xa activity) | Not routinely indicated (anti-Xa activity) | Not routinely indicated (anti-Xa activity) | Not routinely indicated (anti-Xa activity) |
Pharmacodynamic anti-Xa/IIa ratio | 1 | 2.8 | 2.2 | >4.0 | 3.5 |
Intra- and interindividual variability | Extensive | Reduced, but still present | Reduced, but still present | Reduced, but still present | Reduced, but still present |
References |