Nadroparin
| Structural formula | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Mixture of glycosaminoglycans of different chain lengths | |||||||||
| General | |||||||||
| Surname | Nadroparin | ||||||||
| CAS number | none, as a mixture | ||||||||
| Monomers / partial structures | because heparin alternates between D - glucosamine and D - glucuronic acid or L - iduronic acid | ||||||||
| ATC code | |||||||||
| DrugBank | DB08813 | ||||||||
| Drug information | |||||||||
| Drug class |
Antithrombotic, low molecular weight heparin |
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| Mechanism of action |
Antithrombin-dependent inhibits the coagulation factors Xa and, to a lesser extent, factor IIa (thrombin) |
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| properties | |||||||||
| safety instructions | |||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||
Nadroparin ( non-proprietary name Nadroparin-Calcium , trade name Fraxiparin ® , manufacturer: GlaxoSmithKline ) is a drug from the group of low-molecular-weight heparins that is used to inhibit blood clotting . On September 30, 2013, GlaxoSmithKline announced the sale of the Fraxiparine and Arixtra brands to the South African pharmaceutical company Aspen Holdings for around EUR 835 million . The rights in China, India and Pakistan are excluded from the worldwide sales agreement. The official approval is still pending.
Clinical information
Application areas (indications)
Nadroparin is used to prevent vein thrombosis from surgery - including major orthopedic surgery (e.g. hip surgery) - and to treat deep vein thrombosis. Nadroparin is also used to inhibit coagulation during blood washing ( hemodialysis and hemofiltration ) in the extracorporeal circuit.
Dosis, kind and Time of the Use
Nadroparin is injected subcutaneously as a calcium salt in the form of an injection solution for the prevention and treatment of deep vein thrombosis . The dosage adjusted to body weight and the duration of treatment depend on the area of application. Depending on the situation, up to 19,000 IU of anti-Xa nadroparin calcium are injected daily in one to two daily doses over five or more days - as long as there is a risk of thrombosis.
Because of the risk of heparin-induced thrombocytopenia (HIT), the number of thrombocytes (blood platelets) must be monitored regularly during treatment. Occasionally, mild, transient thrombocytopenia (type I) may occur at the start of treatment with nadroparin. Since it generally does not lead to complications, treatment can be continued. If, however, severe thrombocytopenia (type II) occurs, treatment with nadroparin must be stopped immediately; other heparins cannot then be used to inhibit blood coagulation.
For anticoagulation during hemodialysis and hemofiltration, the dose must be set individually for each patient.
Contraindications (contraindications)
Like other low-molecular-weight heparins, nadroparin must not be used in the event of hypersensitivity to the active substance, in coagulation disorders such as the presence of a reduced number of blood platelets ( thrombocytopenia ) or a lack of coagulation factors, in the event of a tendency to bleed due to ulcers or other organ changes and injuries, as well as severe impairment of liver and kidney function. Nadroparin must also not be used in newborns, especially premature premature babies.
Side effects
The most common side effects are small bruising ( hematoma ) at the injection site, bleeding complications and an increase in potassium concentration and certain liver enzymes in the serum .
Mode of action
Low-molecular-weight heparins differ in their action from standard heparin mainly in that they predominantly inhibit factor Xa in the coagulation cascade . Their half-life is also longer than that of standard heparin. For nadroparin it is about 3.5 hours after subcutaneous injection. Nadroparin also inhibits thrombin to a small extent .
The potency of nadroparin is determined using the anti-factor Xa determination and expressed in anti-Xa international units (IU).
Effectiveness / tolerance
The once daily injection of 2,850 IU anti-Xa nadroparin prevented significantly more leg thromboses and pulmonary embolisms than the three times daily injection of standard heparin (5,000 IU) in general surgery in patients with medium or high risk. The twice daily administration of body weight-adapted nadroparin is at least as effective and safe as the continuous infusion of aPTT-controlled standard heparin and enables outpatient treatment. Thrombocytopenias occur significantly less frequently with nadroparin than with standard heparin.
Further information
Nadroparin is obtained from heparin from the intestinal lining of pigs . The long-chain molecules are depolymerized (= split) and fractionated by reaction with nitrous acid . The average relative molecular weight is 3600 to 5000, the degree of sulfation per disaccharide unit is approximately 2. The ratio of anti-factor Xa activity to anti-factor IIa activity is between 2.5 and 4.
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ a b c d e f Fraxiparin technical information (as of December 2006)
- ↑ European Fraxiparin Study et al. Br J Surg (1988) 75: 1058-1063
- ↑ Koopman et al. New Engl J Med (1996) 334: 682-687
- ↑ Hankowitz et al. Ann Hematology (1999) 78: P118
- ↑ Monograph “Nadroparin Calcium” 5.0 / 1134, European Pharmacopoeia 5.0
