Fondaparinux drug interactions: Difference between revisions
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In an in vitro study in human liver microsomes: | In an in vitro study in human liver microsomes: | ||
*Inhibition of [[CYP2A6 ]]hydroxylation of [[coumarin ]]by fondaparinux (200 micromolar i.e., 350 mg/L) was 17 to 28%. Inhibition of the other isozymes evaluated (CYPs 1A2, 2C9, 2C19, 2D6, 3A4, and 3E1) was 0 to 16%. | *Inhibition of [[CYP2A6 ]]hydroxylation of [[coumarin ]]by fondaparinux (200 micromolar i.e., 350 mg/L) was 17 to 28%. Inhibition of the other isozymes evaluated (CYPs 1A2, 2C9, 2C19, 2D6, 3A4, and 3E1) was 0 to 16%. | ||
*Since fondaparinux | *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.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = ARIXTRA (FONDAPARINUX SODIUM) INJECTION, SOLUTION [GLAXOSMITHKLINE LLC] | url =http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=05bb2dd4-5fb5-4ec9-29a8-d200e62d1a8f | publisher = | date = | accessdate = }}</ref> | Since fondaparinux sodium does not bind significantly to plasma proteins other than [[antithrombin|ATIII]], no drug interactions by protein-binding displacement are expected.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = ARIXTRA (FONDAPARINUX SODIUM) INJECTION, SOLUTION [GLAXOSMITHKLINE LLC] | url =http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=05bb2dd4-5fb5-4ec9-29a8-d200e62d1a8f | publisher = | date = | accessdate = }}</ref> | ||
==References== | ==References== | ||
Revision as of 21:49, 3 March 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]
Drug Interactions
In clinical studies performed with ARIXTRA:
- 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, ARIXTRA 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 therapy with ARIXTRA unless these agents are essential. If co-administration is necessary, monitor patients closely for hemorrhage. [See Warnings and Precautions (5.1).]
In an in vitro study in human liver microsomes:
- Inhibition of CYP2A6 hydroxylation of coumarin by fondaparinux (200 micromolar i.e., 350 mg/L) was 17 to 28%. Inhibition of the other isozymes evaluated (CYPs 1A2, 2C9, 2C19, 2D6, 3A4, and 3E1) was 0 to 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.[1]