dalteparin: profile and news

Proximal Deep Vein Thrombosis After Hip Replacement for Oncologic ... May 1, 2006
The use of prophylactic low-molecular-weight heparin (dalteparin) was associated with a 4% rate of proximal deep vein thrombosis (three of seventy-eight ... - Journal of Bone and Joint Surgery

Meta-Analysis: Low-Molecular-Weight Heparin and Bleeding in ... May 2, 2006
Data Synthesis: Eighteen studies using 3 preparations of LMWH (15 studies using enoxaparin, 2 using tinzaparin, and 1 using dalteparin) were included. ... - Annals of Internal Medicine

Momenta Pharmaceuticals Reports Financial Results for the First ... May 9, 2006
...progress in building our pipeline of complex drugs, including our next technology-enabled complex generic product, as well as M-Dalteparin and glycoproteins ... - Yahoo! News (press release)

Other information

Indication
For Anticoagulant therapy in prophylaxis and treatment of venous thrombosis and its extension, for prevention of post-operative deep venous thrombosis and pulmonary embolism , Prevention of clotting in arterial and cardiac surgery.

Pharmacology
Heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from six to twenty thousand. Heparin occurs in and is obtained from liver, lung, mast cells, etc., of vertebrates. Heparin is a well known and commonly used anticoagulant which has antithrombotic properties. Heparin is indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism, and also for the prophylaxis of ischemic complications of unstable angina and non-Q-wave myocardial infarction, when concurrently administered with aspirin. Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Heparin acts at multiple sites in the normal coagulation system. Small amounts of Heparin in combination with antithrombin III (Heparin cofactor) can inhibit thrombosis by inactivating activated Factor X and inhibiting the conversion of prothrombin to thrombin. Once active thrombosis has developed, larger amounts of Heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot by inhibiting the activation of the fibrin stabilizing factor.

Mechanism Of Action
The mechanism of action of Heparin is antithrombin-dependent. It acts mainly by accelerating the rate of the neutralization of certain activated coagulation factors by antithrombin, but other mechanisms may also be involved. The antithrombotic effect of Heparin is well correlated to the inhibition of factor Xa. Heparin interacts with Antithrombin III, Prothrombin and Factor X.

Drug Category
Fibrinolytic Agents; Anticoagulants; Heparins; ATC:B01AB01; ATC:C05BA01; ATC:C05BA03; ATC:S01XA09; ATC:S01XA14

Brand Names/Synonyms
000 Units in Sodium Chloride 0.45%; 000 Units in Sodium Chloride 0.9%; Alpha-Heparin; Ariven; Arteven; Bemiparin; CY 216; Calcilean; Calciparine; Certoparin; Clexane; Clivarin; Clivarine; Cy 222; Dalteparin; Depo-Heparin; Enoxaparin; Enoxaparin Sodium; Eparina [Dcit]; FR 860; Fluxum; Fragmin A; Fragmin B; Fraxiparin; HSDB 3094; Hed-Heparin; Hepalean; Heparin; Heparin Cy 216; Heparin Leo; Heparin Lock Flush; Heparin Sodium; Heparin Sodium Preservative Free; Heparin Sodium Salt; Heparin Sulfate; Heparinate; Heparinic Acid; Hepathrom; KB 101; Leparan; Lipo-Hepin; Liquaemin; Liquaemin Sodium; Liquemin; Low Molecular Weight Heparin Sodium; Multiparin; Novoheparin; OP 386; OP 622; Pabyrin; Parnaparin; Parvoparin; Pularin; Reviparin; Sandoparin; Sodium Heparin; Sublingula; Thromboliquine; Vetren; Vitrum Ab

Dosage Forms
Solution for subcutaneous injection, intravenous injection, or intravenous infusion

Absorption
Some oral absorption but lack of anticoagulant effect. Rapidly taken up by endothelial cells with remainder bound to plasma proteins.

Interactions
-->Interactions for Heparin:

Drug Interactions:

a. Drugs Enhancing Heparin Effect:
Oral anticoagulants: Heparin sodium may prolong the one-stage prothrombin time. Therefore, when heparin sodium is given with dicumarol or warfarin sodium, a period of at least 5 hours after the last intravenous dose or 24 hours after the last subcutaneous dose should elapse before blood is drawn if a valid prothrombin time is to be obtained.

Platelet inhibitors: Drugs such as acetylsalicylic acid, dextran, phenylbutazone, ibuprofen, indomethacin, dipyridamole, hydroxychloroquine and others that interfere with platelet-aggregation reactions (the main hemostatic defense of heparinized patients) may induce bleeding and should be used with caution in patients receiving heparin sodium.

The anticoagulant effect of heparin is enhanced by concurrent treatment with antithrombin III (human) in patients with hereditary antithrombin III deficiency. Thus in order to avoid bleeding, reduced dosage of heparin is recommended during treatment with antithrombin III (human).

b. Drugs Decreasing Heparin Effect:
Digitalis, tetracyclines, nicotine, or antihistamines may partially counteract the anticoagulant action of heparin sodium. Heparin Sodium Injection should not be mixed with doxorubicin, droperidol, ciprofloxacin, or mitoxantrone, since it has been reported that these drugs are incompatible with heparin and a precipitate may form.

Drug/ Laboratory Tests Interactions

Hyperaminotransferasemia: Significant elevations of aminotransferase (SGOT [S-AST] and SGPT [S-ALT]) levels have occurred in a high percentage of patients (and healthy subjects) who have received heparin sodium. Since aminotransferase determinations are important in the differential diagnosis of myocardial infarction, liver disease and pulmonary emboli, rises that might be caused by drugs (heparin sodium) should be interpreted with caution.

Chemical IUPAC Name
6-[5-acetylamino-4,6-dihydroxy-2-(sulfooxymethyl)tetrahydropyran-3-yl]oxy-3-[5-(6-carboxy-4,5-dihydroxy-3-sulfooxy-tetrahydropyran-2-yl)oxy-6-(hydroxymethyl)-3-sulfoamino-4-sulfooxy-tetrahydropyran-2-yl]oxy-4-hydroxy-5-sulfooxy-tetrahydropyran-2-carboxylicacid

Chemical Formula
(C26H40N2O36S5)n

Half Life
1.5 hours

Drug Type
Approved Drug

# Accession No
APRD00056

CAS Registry Number
9005-49-6