Dalteparin

ATC CodeB01AB04
CAS number9005-49-6
PUB number772
Drugbank IDDB06779
Empirical formulaC26H42N2O37S5
Molar mass (g·mol−1)1134,9
Physical statesolid
Melting point (°C)228
PKS value-2,8
Solubility50 g/L

Basics

Dalteparin is an active ingredient for the prevention of thrombosis, heart attacks and unstable angina pectoris in high-risk patients. However, dalteparin is also used on medium- and long-haul flights to prevent deep vein thrombosis. It is a low molecular weight heparin, a "blood thinner" (anticoagulant).

The advantages of dalteparin are the increased availability (bioavailability) of the active ingredient in the body and its safe use in pregnant and breastfeeding women. It also has a longer half-life than heparin, so it stays in the body longer and can therefore act longer.

The disadvantage of dalteparin compared to heparin, however, is its slightly weakened effect. Due to its comparatively low side effect profile, it is nevertheless very popular. Dalteparin is obtained from the cleavage of high-molecular-weight heparin.

It prevents the formation of blood clots (thrombi) in blood vessels. In combination with aspirin, it is used in acute myocardial infarction as part of emergency medicine. Dalteparin is also used in hemodialysis for chronic renal failure. Dalteparin is usually present in medications as dalteparin sodium and is usually injected as an injection solution into fatty tissue (subcutaneously).

Effect

Dalteparin acts by binding to the protein antithrombin. This leads to the inhibition of coagulation factor Xa, which is responsible for the formation of the procoagulant enzyme thrombin. By inhibiting Xa, thrombin is no longer produced and the blood clots less. Because of the longer half-life, inhibition of clotting factor Xa is also sustained for longer and thus blood clotting is attenuated for longer.

Dalteparin has a bioavailability of 87%, which means that 87% of the active substance is available in the body after application (ingestion). The rest has already been broken down (metabolized).

Dalteparin is >90% bound to plasma proteins in the blood. Dalteparin is broken down in the liver and excreted in the urine. The half-life, i.e. the time required by the body to excrete half of the active substance, is 2 hours intravenously (application via the vein) and 3-5 hours subcutaneously (application into fatty tissue).

Dosage

Always take dalteparin exactly as described in the package leaflet or exactly as discussed with your doctor.

The usual recommended dose for the prevention of thrombotic events is 5,000 IU/day (international units) s.c . (injected subcutaneously into fatty tissue) in adults.

Dalteparin can be injected by the user after familiarization. It can be injected either in a U-shape around the belly button, or in the middle of the thigh. A different injection site should be chosen for each application. In areas where the skin is not completely intact (e.g., redness, swelling, scars, etc.), Dalteparin NEVER should be injected. Prior to use, the intended injection site should be disinfected with an alcohol swab and the contact time of the alcohol swab should be waited for. Before injection, a fold of skin should be raised with the fingers and then the needle should be injected at a 45°-90° angle. After removing the needle from the skin, there may be slight blood leakage from the puncture site. For this, you should apply light pressure to the puncture site with a cotton ball for approximately 10 seconds.

IMPORTANT:Always dispose of used syringes and needles in designated containers only, NEVER in the household waste!

Side effects

The following side effects may occur:

Organ systemSide effects
Diseases of the immune system, blood and lymphatic system

Reduction in platelet count (thrombocytopenia), hypersensitivity reactions, allergic shock, nausea and vomiting, headache, fever, pain in the limbs, rhinitis, lacrimation, hives (urticaria), pruritus, shortness of breath, drop in blood pressure, bronchial spasms

Metabolic and nutritional disorders

Adrenal hypofunction, increased serum potassium concentration, decreased serum sodium concentration, collapse, dehydration.

Nervous system disorders

Bleeding in the skull, bruising in the area of the spine or spinal cord

Vascular diseases

Bleeding, drop in blood pressure, slowed heartbeat (bradycardia), cerebral hemorrhage, numbness, constriction of blood vessels (vasoconstriction), painful permanent erection without sexual arousal (in men)

Gastrointestinal tract diseases

blood in stool, bleeding in the posterior peritoneum

liver and biliary diseases

increase in liver enzymes

Skin diseases

Death of skin areas (skin necrosis), hair loss, rash, bleeding

Skeletal muscle, connective tissue and bone disorders

Decrease in bone mass (osteoporosis)

Kidney and urinary tract diseases

Bleeding in the area of urinary and genital organs

Complaints at the site of administration (application site)

Bruising , pain at the injection site, skin reactions at the injection site (e.g., redness, discoloration, etc.), bleeding at the injection site

Dalteparin may increase thyroxine levels and potassium retention. It may also cause distortion of HDL cholesterol, blood glucose levels and bromosulphtalein test.

Interactions

Interactions may occur if the following medicines are taken at the same time:

An increase in the effect of dalteparin may occur with the following medicines:

Weakening of the effect of dalteparin may occur with the following medicines:

  • Anti-allergy agents (antihistamines).
  • nitroglycerin in heart disease (only if administered intravenously)
  • Digitalis drugs
  • tetracyclines (antibiotic group)
  • Vitamin C preparations
  • Nicotine abuse

In addition, dalteparin may weaken the effect of quinine and tricyclic antidepressants, used to treat depression.

Contraindications

Dalteparin must not be taken in the following cases:

  • in case of allergy to dalteparin or other heparins
  • low blood platelet count (thrombocytopenia), which is caused by heparin
  • in case of injuries or operations in the central nervous system, eyes and/or eye operations
  • in case of bleeding in the brain, the interior of the eye or bleeding in other organs
  • in case of active tuberculosis
  • severe blood coagulation disorders
  • diseases associated with an increased tendency to bleed
  • excessive menstrual bleeding
  • vascular dysfunction
  • high blood pressure (hypertension)
  • cerebral hemorrhage (hemorrhagic insult)
  • with bulges of the cerebral artery wall
  • in diseases of the ocular retina
  • in vitreous hemorrhages
  • inflammation of the inner lining of the heart
  • in case of threatened miscarriage
  • kidney and ureter stones
  • Chronic alcoholism

Age restriction

Dalteparin may be used from the completion of the first month of life.

Pregnancy & Lactation

In pregnancy, the use of dalteparin is permitted, since the active ingredient is not placenta-compatible and therefore there is no risk of fertility damage or malformation .

However, it should be noted that pregnant women who are treated with anticoagulant drugs must not receive anesthesia in the spinal cord (cross-stitch) during delivery under any circumstances.

The use of dalteparin is also permitted during breastfeeding. Although the active ingredient passes into breast milk in very small amounts, there are no reports that this has an effect on the infant. Breastfeeding can therefore continue.

The very high level of experience in pregnant and breastfeeding women should be emphasized.

Thomas Hofko

Thomas Hofko

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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