Product Information
Registration Status: ActiveINNOHEP INJECTION 10,000 ANTI-XA IU/0.5ML (PRE-FILLED SYRINGES) is approved to be sold in Singapore with effective from 1999-02-18. It is marketed by LEO PHARMA ASIA PTE LTD, with the registration number of SIN10756P.
This product contains Tinzaparin 20000 axa iu/ml in the form of INJECTION. It is approved for SUBCUTANEOUS use.
This product is manufactured by LABORATOIRES LEO in FRANCE.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Tinzaparin is a low molecular weight heparin (LMWH), produced by enzymatic depolymerization of unfractionated heparin from porcine intestinal mucosa. It is a heterogeneous mixture of with an average molecular weight between 5500 and 7500 daltons. Tinzaparin is composed of molecules with and without a special site for high affinity binding to antithrombin III (ATIII). This complex greatly accelerates the inhibition of factor Xa. It is an anticoagulant and considered an antithrombotic. Tinzaparin must be given either subcutaneously or parenterally. LMWHs are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin.
Indication
Tinzaparin is used for the prevention of postoperative venous thromboembolism in patients undergoing orthopedic surgery and in patients undergoing general surgery who are at high risk of developing postoperative venous thromboembolism. It is also used for the treatment of deep vein thrombosis and/or pulmonary embolism. It is indicated for use in preventing clot formation in indwelling intravenous lines for hemodialysis.
Mechanism of Action
Tinzaparin binds to the plasma protein antithrombin III, forming a complex with then accelerates the inhibition of factor Xa. Its affinity for factor Xa is 2-4 times greater than that of unbound ATIII. The inactivation of factor Xa in turn will exponentially generation of thrombin (factor IIa) molecules, which is needed to activate fibrinogen to fibrin. The coagulation cascade is inhibited because fibrin cannot be formed in the presence of tinzaparin. Like all LMWH, it cannot be given intramuscularly due to increased risk of hematoma.
Pharmacokinetics
- Absorption
- Subcutaneous injection - about 90% when measured as anti-Xa activity versus 67% for anti-IIa activity.
- Distribution
- Anti-Xa activity is 4 L. Anti-IIa activity is 10.9 L
- Metabolism
- Sulfation and polymerization occurs in the liver.
- Elimination
Clearance
Clearance is dose-dependant. The clearance of tinzaparin based on anti-Xa activity ranged from 1.14 to 2.04 L/hr
Toxicity
Osteoporosis with increasing duration of use, bleeding, alopecia, heparin induced thrombocytopenia (HIT). All of these adverse drug reactions occur less with LMWH compared to unfractionated heparin. Tinzaparin showed no toxic effects at doses up to 5 mg/kg in mice, rats, or dogs in standard acute, subacute, and chronic toxicity studies.
Active Ingredient/Synonyms
Tinzaparin sodium | Tinzaparin |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.