Hirudin Variant-1
Hirudin Variant-1 Uses, Dosage, Side Effects, Food Interaction and all others data.
Hirudin Variant-1 is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012.
Hirudin Variant-1 is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Hirudin Variant-1 requires no cofactor for its anticoagulant action. Hirudin Variant-1 is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
| Trade Name | Hirudin Variant-1 |
| Availability | Discontinued |
| Generic | Lepirudin |
| Lepirudin Other Names | Hirudin variant-1, Lepirudin, Lepirudin recombinant |
| Related Drugs | oprelvekin, Neumega, Refludan |
| Type | |
| Formula | C287H440N80O110S6 |
| Weight | 6963.425 Da |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Hirudin Variant-1 is a protein-based direct thrombin inhibitor used to reverse and prevent thrombus formation in heparin-induced thrombocytopenia.
For the treatment of heparin-induced thrombocytopenia
How Hirudin Variant-1 works
Hirudin Variant-1 forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
Toxicity
In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
Food Interaction
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Hirudin Variant-1 Hypertension interaction
[Moderate] Anticoagulants should be used with extreme caution in patients at increased risk for hemorrhage, including those patients with severe hypertension.
Hirudin Variant-1 Drug Interaction
Major: bivalirudin, bivalirudin, warfarin, warfarinUnknown: amoxicillin / clavulanate, amoxicillin / clavulanate, glucose, glucose, indium pentetate in-111, indium pentetate in-111, acetaminophen, acetaminophen, tiotropium, tiotropium
Hirudin Variant-1 Disease Interaction
Major: hemophilia, liver disease, peptic ulcer disease, retinopathy, subacute bacterial endocarditisModerate: hypertension, kidney disease
Volume of Distribution
- 12.2 L [Healthy young subjects (n = 18, age 18-60 years)]
- 18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)]
- 18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)]
- 32.1 L [HIT patients (n = 73)]
Elimination Route
Bioavailability is 100% following injection.
Half Life
Approximately 1.3 hours
Clearance
- 164 ml/min [Healthy 18-60 yrs]
- 139 ml/min [Healthy 65-80 yrs]
- 61 ml/min [renal impaired]
- 114 ml/min [HIT (Heparin-induced thrombocytopenia)]
Elimination Route
Hirudin Variant-1 is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
Innovators Monograph
You find simplified version here Hirudin Variant-1
