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Fondaparinux
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DRUG INFO
Fondaparinux
Drug Name:
Fondaparinux
Indication: For the treatment of prophylaxis of deep vein thrombosis.
Pharmacology: Fondaparinux is a synthetic and specific inhibitor of activated Factor X (Xa) indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism. Fondaparinux is also indicated for the treatment of acute deep vein thrombosis when administered in conjunction with warfarin, and the treatment of acute pulmonary embolism when administered in conjunction with warfarin. Fondaparinux does not inactivate thrombin (activated Factor II) and has no known effect on platelet function. At the recommended dose, Fondaparinux does not affect fibrinolytic activity or bleeding time.
Mechanism Of Action: The antithrombotic activity of Fondaparinux is the result of antithrombin III (ATIII)-mediated selective inhibition of Factor Xa. By selectively binding to ATIII, Fondaparinux potentiates (about 300 times) the innate neutralization of Factor Xa by ATIII. Neutralization of Factor Xa interrupts the blood coagulation cascade and thus inhibits thrombin formation and thrombus development.
Drug Category: Anticoagulants; Antithrombotics; ATC:B01AX05
Brand Names/Synonyms: Arixtra; Fondaparinux sodium
Dosage Forms: Solution
Absorption: 100%
Interactions: Interactions for Fondaparinux:
In clinical studies performed with Fondaparinux, the concomitant use of oral anticoagulants
(warfarin), platelet inhibitors (acetylsalicylic acid), NSAIDs (piroxicam), and digoxin did
not significantly affect the pharmacokinetics/pharmacodynamics of fondaparinux sodium. In
addition, Fondaparinux neither influenced the pharmacodynamics of warfarin, acetylsalicylic
acid, piroxicam, and digoxin, nor the pharmacokinetics of digoxin at steady state.
Agents that may enhance the risk of hemorrhage should be discontinued prior to initiation
of Fondaparinux therapy. If co-administration is essential, close monitoring may be appropriate.
In an in vitro study in human liver microsomes, inhibition of CYP2A6 hydroxylation of coumarin
by fondaparinux (200 m m M i.e., 350 mg/L) was 17-28%. Inhibition of the other isozymes evaluated
(CYPs 2A1, 2C9, 2C19, 2D6, 3A4, and 3E1) was 0-16%. Since fondaparinux does not markedly inhibit
CYP450s (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4) in vitro, fondaparinux
sodium is not expected to significantly interact with other drugs in vivo by inhibition of
metabolism mediated by these isozymes.
Since fondaparinux sodium does not bind significantly to plasma proteins other than ATIII, no
drug interactions by protein-binding displacement are expected.
Chemical IUPAC Name: decasodium 6-[6-[2-carboxylato-4-hydroxy-6-[4-hydroxy-6-methoxy-5-sulfonatoamino-2-(sulfonatooxymethyl)oxan-3-yl]oxy-5-sulfonatooxy-oxan-3-yl]oxy-5-sulfonatoamino-4-sulfonatooxy-2-(sulfonatooxymethyl)oxan-3-yl]oxy-3-[4,5-dihydroxy-3-sulfonatoamino-6-(sulfonatooxymethyl)oxan-2-yl]oxy-4,5-dihydroxy-oxane-2-carboxylate
Chemical Formula: C31H43N3Na10O49S8
Half Life: 17-21 hours
Drug Type: Approved Drug
# Accession No: APRD00500
CAS Registry Number: 114870-03-0
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Fondaparinux News
(When available)
Extremely Frustrating and Completely Unimportant: The Arcane Art ... Jan 10, 2006
MarketingProfs.com (subscription), In short, a world in which Tracinda and Fraxodi and Arixtra do business is a world in which there just are not enough letters to go around. ...
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