| Primary information |
|---|
| ThPP ID | Th1175 |
| Therapeutic Peptide/Protein Name | Desirudin |
| Sequence | NA view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 6963.52 |
| Chemical Formula | C287H440N80O110 S8 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | Mean terminal elimination half-life of 2 to 3 hours |
| Description | Desirudin is a direct, highly selective thrombin inhibitor. Reversibly binds to the active thrombin site of free and clot-associated thrombin. Inhibits fibrin formation, activation of coagulation factors V, VII, and XIII, and thrombin-induced platelet aggregation resulting in a dose-dependent prolongation of the activated partial thromboplastin time (aPTT). |
| Indication/Disease | Preventing blood clots in patients having hip replacement surgery. It may also be used for other conditions as determined by your doctor. Desirudin is a thrombin inhibitor. It works by blocking the activity of thrombin, which helps to prevent the formation of blood clots. |
| Pharmacodynamics | The pharmacodynamic effect of desirudin on proteolytic activity of thrombin was assessed as an increase in aPTT. A mean peak aPTT prolongation of about 1.38 times baseline value (range 0.58 to 3.41) was observed following subcutaneous b.i.d. injections of 15 mg desirudin. Thrombin time (TT) frequently exceeds 200 seconds even at low plasma concentrations of desirudin, which renders this test unsuitable for routine monitoring of Iprivask therapy. At therapeutic serum concentrations, desirudin has no effect on other enzymes of the hemostatic system such as factors IXa, Xa, kallikrein, plasmin, tissue plasminogen activator, or activated protein C. In addition, it does not display any effect on other serine proteases, such as the digestive enzymes trypsin, chymotrypsin, or on complement activation by the classical or alternative pathways. |
| Mechanism of Action | Desirudin is a direct inhibitor of free circulating and clot-bound thrombin. The anticoagulant properties of desirudin are demonstrated by its ability to prolong the clotting time of human plasma. One molecule of desirudin binds to one molecule of thrombin and thereby blocks the thrombogenic activity of thrombin. As a result, all thrombin-dependent coagulation assays are affected. Activated partial thromboplastin time (aPTT) is a measure of the anticoagulant activity of desirudin and increases in a dose-dependent fashion. |
| Toxicity | NA |
| Metabolism | Human and animal data suggest that desirudin is primarily eliminated and metabolized by the kidney. The total urinary excretion of unchanged desirudin amounts to 40 to 50% of the administered dose. Metabolites lacking one or two C-terminal amino acids constitute a minor proportion of the material recovered from urine ( < 7%). |
| Absorption | The absorption of desirudin is complete when subcutaneously administered at doses of 0.3 mg/kg or 0.5 mg/kg. Following subcutaneous administration of single doses of 0.1 to 0.75 mg/kg, plasma concentrations of desirudin increased to a maximum level (C max ) between 1 and 3 hours. Both C max and area-under-the-curve (AUC) values are dose proportional. |
| Volume of Distribution | Desirudin is distributed in the extracellular space with a volume of distribution at steady state of 0.25 L/kg, independent of the dose. |
| Clearance | Total clearance of desirudin is approximately 1.5 to 2.7 mL/min/kg following either subcutaneous or intravenous administration and is independent of dose. |
| Categories | NA |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Abciximab may increase the anticoagulant activities of Desirudin; Acenocoumarol may increase the anticoagulant activities of Desirudin; Acetylsalicylic acid may increase the anticoagulant activities of Desirudin; Alteplase may increase the anticoagulant activities of Desirudin; Anistreplase may increase the anticoagulant activities of Desirudin; Apixaban may increase the anticoagulant activities of Desirudin; Chlorotrianisene may decrease the anticoagulant activities of Desirudin; Citric Acid may increase the anticoagulant activities of Desirudin; The risk or severity of adverse effects can be increased when Desirudin is combined with Collagenase; Dabigatran etexilate may increase the anticoagulant activities of Desirudin. |
| Target | NA |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Iprivask |
| Company | Marathon Pharmaceuticals, LLC |
| Brand Discription | Iprivask 15 mg is supplied as a sterile, white, freeze dried powder for injection. Each vial contains 15.75 mg desirudin and the following inactive ingredients: 1.31 mg anhydrous magnesium chloride USP, sodium hydroxide for injection USP. Each prefilled syringe of diluent for Iprivask contains 0.6 mL sterile Mannitol USP (3%) in Water for Injection and is preservative free. The reconstituted solution has a pH of 7.4. |
| Prescribed for | Iprivask is indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism, in patients undergoing elective hip replacement surgery. |
| Chemical Name | NA |
| Formulation | NA |
| Physcial Appearnce | NA |
| Route of Administration | NA |
| Recommended Dosage | Initial Dosage: In patients undergoing hip replacement surgery, the recommended dose of Iprivask is 15 mg every 12 hours administered by subcutaneous injection with the initial dose given up to 5 to 15 minutes prior to surgery, but after induction of regional block anesthesia, if used |
| Contraindication | Iprivask is contraindicated in patients with known hypersensitivity to natural or recombinant hirudins due to risk of anaphylaxis, and in patients with active bleeding and/or irreversible coagulation disorders due to risk of hemorrhage. |
| Side Effects | Spinal/Epidural Hematoma; Hemorrhagic Events; Increased Risk of Bleeding with Renal Impairment; Antibodies/Re-exposure. |
| Useful Link | http://www.rxlist.com/iprivask-drug.htm; https://www.drugs.com/cdi/desirudin.html |
| PubMed ID | 25222191, 11980386, 11980386, 10972630, 9777138 |
| 3-D Structure | N.A. |