Detailed description page of ThPDB2

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Th1175 details
Primary information
ID10753
Therapeutic IDTh1175
Protein NameDesirudin
SequenceNA
Molecular Weight6963.52
Chemical FormulaC287H440N80O110 S6
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeMean terminal elimination half-life of 2 to 3 hours
DescriptionDesirudin 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/DiseasePreventing 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.
PharmacodynamicsThe 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 ActionDesirudin 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.
ToxicityNo data available.
MetabolismHuman 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%). There is no evidence for the presence of other metabolites. This indicates that desirudin is metabolized by stepwise degradation from the C-terminus probably catalyzed by carboxypeptidase(s) such as carboxypeptidase A.
AbsorptionAbsorption is complete after subcutaneous administration. Time to peak in plasma is 1 to 3 hours.
0.25 L/kg.
Clearance1.5 to 2.7 mL/min/kg.
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionAbciximab 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.
TargetNA
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA


Primary information
ID10754
Therapeutic IDTh1175
Protein NameDesirudin
SequenceNA
Molecular Weight6963.52
Chemical FormulaC287H440N80O110 S7
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeMean terminal elimination half-life of 2 to 3 hours
DescriptionDesirudin 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/DiseasePreventing 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.
PharmacodynamicsThe 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 ActionDesirudin 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.
ToxicityNo data available.
MetabolismHuman 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%). There is no evidence for the presence of other metabolites. This indicates that desirudin is metabolized by stepwise degradation from the C-terminus probably catalyzed by carboxypeptidase(s) such as carboxypeptidase A.
AbsorptionAbsorption is complete after subcutaneous administration. Time to peak in plasma is 1 to 3 hours.
0.25 L/kg.
Clearance1.5 to 2.7 mL/min/kg.
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionAbciximab 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.
TargetNA
Brand NameIprivask
CompanyValeant Pharmaceuticals North America LLC
Brand DescriptionValeant Pharmaceuticals North America LLC
Prescribed ForIprivask is indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism, in patients undergoing elective hip replacement surgery.
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationSubcutaneous
Recommended DosageInitial 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
ContraindicationIprivask 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 EffectsSpinal/Epidural Hematoma; Hemorrhagic Events; Increased Risk of Bleeding with Renal Impairment; Antibodies/Re-exposure.
Useful Link 1Link
Useful Link 2NA
RemarksNA


Primary information
ID10755
Therapeutic IDTh1175
Protein NameDesirudin
SequenceNA
Molecular Weight6963.52
Chemical FormulaC287H440N80O110 S8
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeMean terminal elimination half-life of 2 to 3 hours
DescriptionDesirudin 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/DiseasePreventing 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.
PharmacodynamicsThe 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 ActionDesirudin 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.
ToxicityNo data available.
MetabolismHuman 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%). There is no evidence for the presence of other metabolites. This indicates that desirudin is metabolized by stepwise degradation from the C-terminus probably catalyzed by carboxypeptidase(s) such as carboxypeptidase A.
AbsorptionAbsorption is complete after subcutaneous administration. Time to peak in plasma is 1 to 3 hours.
0.25 L/kg.
Clearance1.5 to 2.7 mL/min/kg.
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionAbciximab 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.
TargetNA
Brand NameIprivask
CompanyMarathon Pharmaceuticals, LLC
Brand DescriptionMarathon Pharmaceuticals, LLC
Prescribed ForIprivask is indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism, in patients undergoing elective hip replacement surgery.
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageInitial 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
ContraindicationIprivask 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 EffectsSpinal/Epidural Hematoma; Hemorrhagic Events; Increased Risk of Bleeding with Renal Impairment; Antibodies/Re-exposure.
Useful Link 1Link
Useful Link 2NA
RemarksNA