Tinzaparin sodium

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Tinzaparin sodium
Tinzaparin.svg
n = 1 to 25, R = H or SO3Na, R1 = H, SO3Na or COCH3, R2 = H and R3 = COONa or R2 = COONa and R3 = H
Clinical data
Trade names innohep(R)
AHFS/Drugs.com Monograph
Routes of
administration
subcutaneous (once daily)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 90% for Anti-Xa activity, 67% for Anti-IIa activity) [2]
Metabolism minor metabolisation in liver by desulfation and/or depolymerization; excretion via kidneys in almost unchanged form
Elimination half-life 200 min. for Anti-Xa activity, 257. min for Anti-IIa activity [3]
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
ChEMBL
ECHA InfoCard 100.110.590 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Molar mass 6500g/mol (average) [4]
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Tinzaparin is an antithrombotic drug in the heparin group. It is a low molecular weight heparin (LMWH) marketed as Innohep worldwide. It has been approved by the U.S. Food and Drug Administration (FDA) for once daily treatment and prophylaxis of deep vein thrombosis (DVT) and pulmonary embolism (PE). [5]

Contents

It can be given subcutaneously by syringe, or intravenously. [6] It was manufactured by Leo pharmaceutical company, who withdrew the product from the US in 2011 due to low sales and a contamination issue. [7]

Use in elderly

In July 2008, the company revised the prescribing information to restrict the use of tinzaparin in patients 90 years of age or older. FDA is concerned that the preliminary data from the IRIS study suggests that the increased risk of mortality is not limited only to patients 90 years of age or older.

According to the study Innohep increases the risk of death for elderly patients (i.e., 70 years of age and older) with chronic kidney disease. Healthcare professionals should consider the use of alternative treatments to Innohep when treating elderly patients over 70 years of age with chronic kidney disease and deep vein thrombosis, pulmonary embolism, or both.

Use in pregnancy

No LMWH, except tinzaparin, is licensed for use in gestational hypercoagulability. [8] Still, tinzaparin is often the LMWH of choice in pregnant women. [8]

Side effects

Bleeding in overdose. There is occasionally bruising at the site of injection.

Monitoring

Tinzaparin does not affect the international normalized ratio (INR), prothrombin time (PT).[ citation needed ] Anti-factor Xa levels can be measured, and are often used to monitor tinzaparin.

Reversal agent

Protamine sulfate will reverse tinzaparin by 85% per package insert.

Related Research Articles

<span class="mw-page-title-main">Anticoagulant</span> Class of drugs

An anticoagulant, commonly known as a blood thinner, is a chemical substance that prevents or reduces the coagulation of blood, prolonging the clotting time. Some occur naturally in blood-eating animals, such as leeches and mosquitoes, which help keep the bite area unclotted long enough for the animal to obtain blood.

<span class="mw-page-title-main">Thrombosis</span> Formation of blood clots inside the blood vessels

Thrombosis is the formation of a blood clot inside a blood vessel, obstructing the flow of blood through the circulatory system. When a blood vessel is injured, the body uses platelets (thrombocytes) and fibrin to form a blood clot to prevent blood loss. Even when a blood vessel is not injured, blood clots may form in the body under certain conditions. A clot, or a piece of the clot, that breaks free and begins to travel around the body is known as an embolus.

<span class="mw-page-title-main">Pulmonary embolism</span> Blockage of an artery in the lungs

Pulmonary embolism (PE) is a blockage of an artery in the lungs by a substance that has moved from elsewhere in the body through the bloodstream (embolism). Symptoms of a PE may include shortness of breath, chest pain particularly upon breathing in, and coughing up blood. Symptoms of a blood clot in the leg may also be present, such as a red, warm, swollen, and painful leg. Signs of a PE include low blood oxygen levels, rapid breathing, rapid heart rate, and sometimes a mild fever. Severe cases can lead to passing out, abnormally low blood pressure, obstructive shock, and sudden death.

<span class="mw-page-title-main">Venous thrombosis</span> Blood clot (thrombus) that forms within a vein

Venous thrombosis is the blockage of a vein caused by a thrombus. A common form of venous thrombosis is deep vein thrombosis (DVT), when a blood clot forms in the deep veins. If a thrombus breaks off (embolizes) and flows to the lungs to lodge there, it becomes a pulmonary embolism (PE), a blood clot in the lungs. The conditions of DVT only, DVT with PE, and PE only, are all captured by the term venous thromboembolism (VTE).

Factor V Leiden is a variant of human factor V, which causes an increase in blood clotting (hypercoagulability). Due to this mutation, protein C, an anticoagulant protein that normally inhibits the pro-clotting activity of factor V, is not able to bind normally to factor V, leading to a hypercoagulable state, i.e., an increased tendency for the patient to form abnormal and potentially harmful blood clots. Factor V Leiden is the most common hereditary hypercoagulability disorder amongst ethnic Europeans. It is named after the Dutch city of Leiden, where it was first identified in 1994 by Rogier Maria Bertina under the direction of Pieter Hendrik Reitsma. Despite the increased risk of venous thromboembolisms, people with one copy of this gene have not been found to have shorter lives than the general population. It is an autosomal dominant genetic disorder with incomplete penetrance.

<span class="mw-page-title-main">Deep vein thrombosis</span> Formation of a blood clot (thrombus) in a deep vein

Deep vein thrombosis (DVT) is a type of venous thrombosis involving the formation of a blood clot in a deep vein, most commonly in the legs or pelvis. A minority of DVTs occur in the arms. Symptoms can include pain, swelling, redness, and enlarged veins in the affected area, but some DVTs have no symptoms.

Low-molecular-weight heparin (LMWH) is a class of anticoagulant medications. They are used in the prevention of blood clots and, in the treatment of venous thromboembolism, and the treatment of myocardial infarction.

<span class="mw-page-title-main">Thromboembolism</span> Obstruction of a blood vessel by a clot

Thromboembolism is a condition in which a blood clot (thrombus) breaks off from its original site and travels through the bloodstream to obstruct a blood vessel, causing tissue ischemia and organ damage. Thromboembolism can affect both the venous and arterial systems, with different clinical manifestations and management strategies.

<span class="mw-page-title-main">Enoxaparin sodium</span> Anticoagulant medication (blood thinner)

Enoxaparin sodium, sold under the brand name Lovenox among others, is an anticoagulant medication. It is used to treat and prevent deep vein thrombosis (DVT) and pulmonary embolism (PE) including during pregnancy and following certain types of surgery. It is also used in those with acute coronary syndrome (ACS) and heart attacks. It is given by injection just under the skin or into a vein. It is also used during hemodialysis.

<span class="mw-page-title-main">Renal vein thrombosis</span> Medical condition

Renal vein thrombosis (RVT) is the formation of a clot in the vein that drains blood from the kidneys, ultimately leading to a reduction in the drainage of one or both kidneys and the possible migration of the clot to other parts of the body. First described by German pathologist Friedrich Daniel von Recklinghausen in 1861, RVT most commonly affects two subpopulations: newly born infants with blood clotting abnormalities or dehydration and adults with nephrotic syndrome.

<span class="mw-page-title-main">Rivaroxaban</span> Anticoagulant drug

Rivaroxaban, sold under the brand name Xarelto among others, is an anticoagulant medication used to treat and prevent blood clots. Specifically it is used to treat deep vein thrombosis and pulmonary emboli and prevent blood clots in atrial fibrillation and following hip or knee surgery. It is taken by mouth.

An embolus, is described as a free-floating mass, located inside blood vessels that can travel from one site in the blood stream to another. An embolus can be made up of solid, liquid, or gas. Once these masses get "stuck" in a different blood vessel, it is then known as an "embolism." An embolism can cause ischemia—damage to an organ from lack of oxygen. A paradoxical embolism is a specific type of embolism in which the embolus travels from the right side of the heart to the left side of the heart and lodges itself in a blood vessel known as an artery. It is termed "paradoxical" because venous emboli will usually be lodged in pulmonary artery in an event called pulmonary embolism, instead of systemic circulation.

<span class="mw-page-title-main">Dalteparin sodium</span> Pharmaceutical drug

Dalteparin is a low molecular weight heparin. It is marketed as Fragmin. Like other low molecular weight heparins, dalteparin is used for prophylaxis or treatment of deep vein thrombosis and pulmonary embolism to reduce the risk of a stroke or heart attack. Dalteparin acts by potentiating the activity of antithrombin III, inhibiting formation of both Factor Xa and thrombin. It is normally administered by self-injection.

<span class="mw-page-title-main">Nadroparin calcium</span> Chemical compound

Nadroparin is an anticoagulant belonging to a class of drugs called low molecular weight heparins (LMWHs). Nadroparin was developed by Sanofi-Synthélabo.

<span class="mw-page-title-main">Dabigatran</span> Anticoagulant medication

Dabigatran, sold under the brand name Pradaxa among others, is an anticoagulant used to treat and prevent blood clots and to prevent stroke in people with atrial fibrillation. Specifically it is used to prevent blood clots following hip or knee replacement and in those with a history of prior clots. It is used as an alternative to warfarin and does not require monitoring by blood tests. In a meta analysis of 7 different studies, there was no benefit of dabigatran over warfarin in preventing ischemic stroke; however, dabigatran were associated with a lower hazard for intracranial bleeding compared with warfarin, but also had a higher risk of gastrointestinal bleeding relative to warfarin. It is taken by mouth.

Hypercoagulability in pregnancy is the propensity of pregnant women to develop thrombosis. Pregnancy itself is a factor of hypercoagulability, as a physiologically adaptive mechanism to prevent post partum bleeding. However, when combined with an additional underlying hypercoagulable states, the risk of thrombosis or embolism may become substantial.

<span class="mw-page-title-main">Reviparin sodium</span> Pharmaceutical drug

Reviparin is an antithrombotic and belongs to the group of low molecular weight heparins (LMWH).

<span class="mw-page-title-main">Apixaban</span> Anticoagulant medication

Apixaban, sold under the brand name Eliquis, is an anticoagulant medication used to treat and prevent blood clots and to prevent stroke in people with nonvalvular atrial fibrillation through directly inhibiting factor Xa. It is used as an alternative to warfarin to prevent blood clots following hip or knee replacement and in those with a history of prior clots. and does not require monitoring by blood tests or dietary restrictions. It is taken by mouth.

Direct thrombin inhibitors (DTIs) are a class of anticoagulant drugs that can be used to prevent and treat embolisms and blood clots caused by various diseases. They inhibit thrombin, a serine protease which affects the coagulation cascade in many ways. DTIs have undergone rapid development since the 90's. With technological advances in genetic engineering the production of recombinant hirudin was made possible which opened the door to this new group of drugs. Before the use of DTIs the therapy and prophylaxis for anticoagulation had stayed the same for over 50 years with the use of heparin derivatives and warfarin which have some well known disadvantages. DTIs are still under development, but the research focus has shifted towards factor Xa inhibitors, or even dual thrombin and fXa inhibitors that have a broader mechanism of action by both inhibiting factor IIa (thrombin) and Xa. A recent review of patents and literature on thrombin inhibitors has demonstrated that the development of allosteric and multi-mechanism inhibitors might lead the way to a safer anticoagulant.

<span class="mw-page-title-main">Ultrasonography of deep vein thrombosis</span> Medical diagnostic method

Ultrasonography in suspected deep vein thrombosis focuses primarily on the femoral vein and the popliteal vein, because thrombi in these veins are associated with the greatest risk of harmful pulmonary embolism.

References

  1. "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA . Retrieved 22 October 2023.
  2. Cheer S.M. et al. Drugs 2004; 64 (13): 1479–1502
  3. Pedersen P.C. et al. Thromb Res 1991; 61 (5-6): 477-487
  4. European Pharmacopoeia, 6th Edition, 2008
  5. Hull et al. NEJM 1992;326,15:975-982
  6. Farmaceutiska Specialiteter i Sverige - the Swedish official drug catalog. Fass.se Archived 21 January 2011 at the Wayback Machine > Innohep
  7. "Drug Shortages List". Archived from the original on 5 October 2016. Retrieved 4 October 2016.
  8. 1 2 "Archived copy". Archived from the original on 12 June 2010. Retrieved 15 May 2010.{{cite web}}: CS1 maint: archived copy as title (link)Therapeutic anticoagulation in pregnancy. Norfolk and Norwich University Hospital (NHS Trust). Reference number CA3017. 9 June 2006 [review June 2009]