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Direct Thrombin InhibitorAka: Hirudin, Lepirudin, Refludan, Bivalirudin, Angiomax, Desirudin, Ipravask, Argatroban, Acova
- Indications
- Thrombus prophylaxis, treatment or Unstable Angina and
- Heparin-Induced Thrombocytopenia
- Dosing: Hirudins (peptide derivatives)
- Lepirudan (Refludan)
- See other references for dosing
- Bivalirudin (Angiomax)
- Used in Unstable Angina if Heparin contraindicated
- Coadminister with Aspirin
- Initial: 0.75 mg/kg IV bolus
- Later: 1.75 mg/kg/hour for 4 hours
- Maintenance: 0.2 mg/kg/hour for up to 20 hours
- Desirudin (Ipravask)
- DVT Prophylaxis: 15 mg SQ q12 hours after hip surgery
- Lepirudan (Refludan)
- Dosing: L-Arginine derivatives
- Argatroban (Acova)
- Initial: 2 mcg/kg/minute
- Maintenance: Adjusted per PTT
- Argatroban (Acova)
- Pharmacokinetics
- Clearance
- Renal clearance for Hirudins
- Hepatic clearance for L-Arginine derivatives
- Clearance
- Precautions
- Serious Allergic Reactions may occur to Hirudins
argatroban (C0048470) | |
|---|---|
| Definition (NCI) | A synthetic derivative of L-arginine with antithrombotic activity. Argatroban is a univalent and direct inhibitor of fibrin-bound thrombin. This agent reversibly binds to the thrombin active site thereby preventing the thrombin-dependent reactions, which include conversion of fibrinogen to fibrin; the activation of factors V, VIII and XI; the activation of protein C; and platelet aggregation. Argatroban is highly selective for thrombin and is able to inhibit the action of both free and clot-associated thrombin. As a result, stabilization of blood clots and coagulation is inhibited. |
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | C031942 |
| English | argatroban, ARGATROBAN PREPARATION, Argipidine, MMTQAP, MPQA |
| Spanish | argatroban, argatrobano |
| Parent Concepts | Anticoagulants (C0003280), Pipecolic Acids (C0031952), Drug allergen (C1320237), Direct thrombin inhibitor (C1532225) |
| Sources | MSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, VANDF Derived from the NIH UMLS (Unified Medical Language System) |
bivalirudin (C0168273) | |
|---|---|
| Definition (NCI) | A 20 amino acid long synthetic peptide with thrombin-specific anticoagulant properties. Bivalirudin reversibly binds thrombin, free as well as clot bound, at the catalytic site and the anion-binding exosite, thereby preventing the formation and activation of fibrin, factor XIIIa, and other coagulation factors. This drug is primarily used during coronary angioplasty procedures, in combination with aspirin, in patients with unstable angina. |
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | C074619 |
| English | bivalirudin, BIVALIRUDIN PREPARATION |
| Spanish | bivalirrudina, bivalirudina |
| Parent Concepts | Anticoagulants (C0003280), Unclassified Ingredients (C1372954), Hirudin and derivatives (C1320115), Direct thrombin inhibitor (C1532225) |
| Sources | MSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, VANDF Derived from the NIH UMLS (Unified Medical Language System) |
desirudin (C0378366) | |
|---|---|
| Definition (NCI) | A synthetic recombinant form of the naturally occurring hirudin, the anticoagulant substance found in leech. Desirudin is a selective and almost irreversible inhibitor of thrombin, both free and clot-bound, by blocking its active site. This anticoagulant agent has no effect on other components of the hemostatic system. Desirudin is particularly used to prevent deep vein thrombosis in patients undergoing hip and knee replacement surgery. |
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | C060225 |
| English | desirudin, Desirudine, Desulfatohirudin, desulphatohirudin, recombinant HV1 hirudin |
| Spanish | desirudin, desirudina |
| Parent Concepts | Anticoagulants (C0003280), Hirudin and derivatives (C1320115), Direct thrombin inhibitor (C1532225) |
| Sources | MSH, NCI, RXNORM, SCTSPA, SNOMEDCT Derived from the NIH UMLS (Unified Medical Language System) |
Refludan (C0661608) | |
|---|---|
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | C083544 |
| English | Aventis Behring Brand of Lepirudin, Aventis Brand Lepirudin, Aventis Pharma Brand of Lepirudin, Berlex Brand of Lepirudin, Hoechst Brand of Lepirudin, Pharmion Brand of Lepirudin, Refludan, Refludin, Schering Brand of Lepirudin |
| Sources | MSH, NCI, PDQ, RXNORM Derived from the NIH UMLS (Unified Medical Language System) |
lepirudin (C0772394) | |
|---|---|
| Definition (NCI) | A drug that inhibits blood clotting. It is being studied in cancer treatment. |
| Definition (PDQ) | A recombinant hirudin, a polypeptide naturally produced by the leech Hirudo medicinalis, derived from yeast cells and a highly specific inhibitor of thrombin. Lepirudin directly binds to thrombin, thereby inactivating the thrombogenic activity of thrombin. This anticoagulant produces dose-dependent increases in activated partial thromboplastin time (aPTT). Its action is independent of antithrombin III and it is not inhibited by platelet factor 4. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43356&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43356&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1839" NCI Thesaurus) |
| Definition (NCI) | A recombinant hirudin, a polypeptide naturally produced by the leech Hirudo medicinalis, derived from yeast cells and highly specific inhibitor of thrombin. Lepirudin directly binds to thrombin, thereby inactivating the thrombogenic activity of thrombin. This anticoagulant produces dose-dependent increases in activated partial thromboplastin time (aPTT). Its action is independent of antithrombin III and it is not inhibited by platelet factor 4. |
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | C083544 |
| English | 1-Leu-2-Thr-63-desulfohirudin, lepirudin, LEPIRUDIN PREPARATION, Recombinant Hirudin |
| Spanish | lepirudina |
| Parent Concepts | Anticoagulants (C0003280), HBW 023 (C0247502), Hirudin and derivatives (C1320115), Drug allergen (C1320237), Direct thrombin inhibitor (C1532225) |
| Sources | MSH, MTHSPL, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, VANDF Derived from the NIH UMLS (Unified Medical Language System) |
Acova (C0939245) | |
|---|---|
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | C031942 |
| English | Acova, SmithKline Beecham brand of argatroban |
| Sources | MSH, RXNORM Derived from the NIH UMLS (Unified Medical Language System) |
Angiomax (C0939677) | |
|---|---|
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | C074619 |
| English | Angiomax, The Medicines Company brand of bivalirudin |
| Sources | MSH, NCI, RXNORM Derived from the NIH UMLS (Unified Medical Language System) |
Hirudins (C1451270) | |
|---|---|
| Definition (CSP) | active principle in the buccal gland secretion (saliva) of leeches; it acts as an antithrombin and as an antithrombotic agent. |
| Definition (MSH) | Single-chain polypeptides of about 65 amino acids (7 kDa) from LEECHES that have a neutral hydrophobic N terminus, an acidic hydrophilic C terminus, and a compact, hydrophobic core region. Recombinant hirudins lack tyr-63 sulfation so are referred to as 'desulfato-hirudins'. They form a stable non-covalent complex with ALPHA-THROMBIN, thereby abolishing its ability to cleave FIBRINOGEN. |
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | D006629 |
| English | hirudin, Hirudins |
| Parent Concepts | Anticoagulants (C0003280), Antithrombins (C0003440) |
| Sources | CSP, MSH, MTH Derived from the NIH UMLS (Unified Medical Language System) |
