tinzaparin

Action and Spectrum

Actions and Spectrum: 

tinzaparin is a low molecular weight heparin (LMWH) that acts as an anticoagulant by binding to and potentiating the activity of antithrombin III (ATIII), a natural inhibitor of blood coagulation factors such as thrombin and factor Xa. tinzaparin, like other LMWHs, has a higher affinity for ATIII than unfractionated heparin (UFH), allowing for more predictable and reliable anticoagulation. The mechanism of action of tinzaparin is multifactorial and includes the following effects:  

Inhibition of thrombin: tinzaparin binds to and inhibits the activity of thrombin, a key enzyme in the blood coagulation cascade that converts fibrinogen to fibrin, which forms the backbone of blood clots.  

Inhibition of factor Xa: tinzaparin also binds to and inhibits the activity of factor Xa, another enzyme in the coagulation cascade that converts prothrombin to thrombin.  

Inhibition of platelet activation: tinzaparin can also bind to and activate platelet factor 4, a protein that inhibits platelet activation and aggregation, further preventing the formation of blood clots.  

tinzaparin has a broad spectrum of activity and is used to prevent and treat a range of thromboembolic conditions, including deep vein thrombosis (DVT), pulmonary embolism (PE), and unstable angina/non-ST-segment elevation myocardial infarction (UA/NSTEMI).

tinzaparin is also used as a prophylactic anticoagulant in patients undergoing surgery or immobilization to prevent the formation of blood cells 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Chest pain (2%) 

Constipation (1%), 

Skin rash (1%) 

Hematuria (1%), 

Vomiting (1%) 

Nausea (2%), 

Urinary tract infection (4%) 

Hematoma 

Dyspnea (1%) 

Pain (2%) 

Anemia 

Injection site reaction 

Irritation at the injection site 

Pain at the injection site 

Headache (2%) 

Back pain (2%) 

Epistaxis (2%) 

Fever (2%)  

<1% 

Abdominal pain 

Heparin-induced thrombocytopenia 

Diarrhea 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Active major bleeding: tinzaparin can increase the risk of bleeding, and its use is contraindicated in patients with active major bleeding. 
• Known hypersensitivity: tinzaparin is derived from heparin and may cause allergic reactions in patients with a known hypersensitivity to heparin. 
• Thrombocytopenia: tinzaparin can cause a decrease in platelet count, and its use is contraindicated in patients with a history of heparin-induced thrombocytopenia (HIT) or a baseline platelet count of less than 100,000/mm3. 
• Severe renal impairment: tinzaparin is eliminated by the kidneys, and its use is contraindicated in patients with severe renal impairment (creatinine clearance less than 30 mL/min). 
• Active ulcerative or angiodysplasia gastrointestinal disease: tinzaparin can increase the risk of gastrointestinal bleeding, and its use is contraindicated in patients with active ulcerative or angiodysplasia gastrointestinal disease. 
• Recent intracranial or spinal surgery: tinzaparin can increase the risk of bleeding at the site of recent intracranial or spinal surgery, and its use is contraindicated in these patients. 
• Acute bacterial endocarditis: tinzaparin can increase the risk of bleeding in patients with acute bacterial endocarditis and is generally contraindicated in these patients. 

Caution: 

• Liver impairment: tinzaparin is primarily metabolized in the liver, and its use should be closely monitored in patients with liver impairment. 
• Elderly patients: Elderly patients may have a higher risk of bleeding with tinzaparin due to age-related changes in kidney and liver function and an increased incidence of comorbidities. 
• Pregnancy and breast-feeding: The safety of tinzaparin during pregnancy and breast-feeding is not well established, and its use should be carefully considered in these populations. 
• Concurrent use of other anticoagulants: The concurrent use of tinzaparin with other anticoagulants, such as warfarin or aspirin, may increase the risk of bleeding and should be closely monitored. 
• Recent surgery or trauma: tinzaparin should be used with caution in patients who have recently undergone surgery or have experienced trauma, as these patients may have an increased risk of bleeding. 
• Thrombocytopenia: tinzaparin can cause a decrease in platelet count, and its use should be closely monitored in patients with a history of thrombocytopenia or other bleeding disorders. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

tinzaparin is a low-molecular-weight heparin (LMWH) that acts as an anticoagulant by binding to and enhancing the activity of antithrombin III (ATIII). ATIII is a natural anticoagulant that inhibits thrombin and other coagulation enzymes, and by enhancing its activity, tinzaparin can effectively prevent the formation of blood clots.  

tinzaparin has a molecular weight of approximately 6,000 daltons, smaller than unfractionated heparin (UFH). This smaller size allows tinzaparin to have a more predictable pharmacokinetic profile and a more consistent anticoagulant effect than UFH. 

Pharmacodynamics: 

tinzaparin is a low-molecular-weight heparin (LMWH) that exerts its pharmacological effects by enhancing the activity of antithrombin III (ATIII). This natural anticoagulant inhibits thrombin and other coagulation enzymes. Tinzaparin binds to ATIII, which in turn inactivates factor Xa and, to a lesser extent, thrombin. This leads to a reduction in thrombin generation and clot formation, resulting in an anticoagulant effect.  

Unlike unfractionated heparin (UFH), which can bind to both factor Xa and thrombin, tinzaparin has a higher affinity for factor Xa and a lower affinity for thrombin. This selectivity allows tinzaparin to have a more predictable pharmacodynamic effect than UFH.  

tinzaparin has a dose-dependent anticoagulant effect, with higher doses leading to a more pronounced anticoagulant effect. However, the risk of bleeding also increases with higher doses, so careful monitoring of the patient’s clinical status and coagulation parameters is essential to ensure the optimal balance between anticoagulation and bleeding risk. 

Pharmacokinetics: 

Absorption 

tinzaparin is administered subcutaneously, and its absorption is rapid and predictable. The bioavailability of tinzaparin after subcutaneous administration is approximately 90%.  

Distribution 

tinzaparin is extensively distributed throughout the body, with a volume of distribution of approximately 0.1-0.2 L/kg. It binds extensively to plasma proteins, primarily to antithrombin III (ATIII), and has a plasma half-life of 2-4 hours.  

Metabolism 

tinzaparin is not metabolized by the liver or other organs, and its clearance is primarily through renal elimination. A small proportion of tinzaparin is metabolized by the endothelial cells in the liver and kidney.  

Elimination and Excretion 

tinzaparin is primarily eliminated through the kidneys, with approximately 40% of the administered dose excreted unchanged in the urine. The remainder of the dose is metabolized and excreted in the urine and faeces. 

Adminstartion

Administration: 

tinzaparin is administered subcutaneously (under the skin), typically in the abdomen, with a needle and syringe. The exact administration technique may vary based on the specific product and dose prescribed, so it is essential to follow the instructions provided by the healthcare provider or pharmacist.  

The injection site should be cleaned with an alcohol swab before injection, and the needle should be inserted at a 90-degree angle into the skin. The injection site should be rotated to avoid repeated injections in the same area, and the skin should be pinched gently to lift the tissue and create a space for the needle. The injection should be given slowly and steadily, and the needle should be withdrawn quickly after injection. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tinzaparin 

Why do we use tinzaparin? 

tinzaparin is a type of low molecular weight heparin (LMWH) used for several medical conditions related to blood clotting. Some of the common uses of tinzaparin include: 

• Prevention of deep vein thrombosis (DVT) and pulmonary embolism (PE) in patients at risk for these conditions, such as patients undergoing surgery, immobilized patients, or those with cancer. 
• Treatment of DVT and PE, alone or combined with other anticoagulant medications. 
• In combination with other medications, prevention of clotting in patients with unstable angina or non-ST-segment elevation myocardial infarction (NSTEMI). 
• In combination with other medications, prevention of clotting in patients with acute ST-segment elevation myocardial infarction (STEMI). 
• Treatment of disseminated intravascular coagulation (DIC) a rare condition that causes abnormal blood clotting throughout the body. 
• Prevent clotting in patients undergoing hemodialysis or other forms of renal replacement therapy. 
• Prevent miscarriage or recurrent fetal loss in women with antiphospholipid syndrome (APS), an autoimmune disorder that can cause blood clots and pregnancy complications.