Argatroban pharmacokinetics

Tran JQ, Di Cicco RA, Sheth SB, et al. Assessment of the potential pharmacokinetic and pharmacodynamic interaction between erythromycin and argatroban. J Clin Pharmacol 1999 39 513-519. 

I Swan SK, Hursting MJ. The pharmacokinetics and pharmacodynamics of argatroban effects of age, gender, and hepatic or renal dysfunction. Pharmacotherapy 2000 20 318-329. 

Ahmad S, Ahsan A, Iqbal O, et al. Pharmacokinetics and pharmacodynamics of argatroban as studied by HPLC and functional methods implications in the monitoring and dosage-optimizations in cardiovascular patients. Clin Appl Thromb Hemost 1998 4 243-249. 

Cox, D.S. Kleiman, N.S. Boyle, D.A. Aluri, J. Parchman, 89. G. Holdbrook, F. Fossler, M.J. Pharmacokinetics and pharmacodynamics of argatroban in combination with a platelet glycoprotein IIB/IIIA receptor antagonist in patients undergoing percutaneous coronary intervention. 

The thrombin inhibitor argatroban had no effect on the steady-state pharmacokinetics of oral digoxin 0.375 mg/day in 12 healthy volunteers the argatroban was given as an intravenous infusion of 2 micrograms/kg/minute on days 11-15 (236). 

Argatroban is metabolized by CYP3A4/5, and its pharmacokinetics might therefore be expected to be altered by inhibitors of CYP3A. However, in 14 healthy men erythromycin 500 mg qds had no effects on the pharmacokinetics of argatroban 1 gg/kg/minute infused over 5 hours (18). 

Low-dose aspirin did not alter the pharmacokinetics or pharmacodynamic effects of ai atroban. Neither abciximab nor eptifibatide appeared to alter ai atroban pharmacokinetics. There is no pharmacodynamic interaction between bivalirudin and aspirin, ticlopidine, ciopidogrei, abciximab, eptifibatide or tirofiban. Nevertheless, the manufacturers warn of the increased bleeding risks if argatroban, bivalirudin or lepirudin are used with antiplatelet drugs or thrombolytics. 

Antiplatelet dru In a study in healthy subjects, pretreatment with oral aspirin 162.5 mg, given 26 and 2 hours prior to argatroban 1 microgram/kg per minute over 4 hours, caused no changes in the pharmacokinetics or pharmacodynamic effects of the argatroban. ... 

Use of argatroban with warfarin and related oral anticoagulants has an effect on the measurement of the BVR, and the manufacturer provides equations to adjust for this. Argatroban does not alter warfarin pharmacokinetics. The manufacturers warn of the increased bleeding risks if aigatroban, bivalirudin or lepirudin are used with other anticoagulants. 

Brown PM, Hursting MJ. Lack of pharmacokinetic interactions between argatroban and warfarin. Am JHealth-Syst Pharm (2002) 59, 2078-83. 

There was no pharmacokinetic interaction between argatroban and lidocaine, and no further change in coagulation parameters when both drugs were given together in a study. 

In 12 healthy subjects, lidocaine 2 mg/kg per hour was infused for 16 hours (after a loading dose of 1.5 mg/kg over 10 minutes) alone, then in combination with intravenous argatroban 1.5 micrograms/kg per minute for 16 hours. Concurrent use did not affect the pharmacokinetics of either drug. Lidocaine did not alter the effect of argatroban on aPTT. ... 

No significant pharmacokinetic interaction occurs between digoxin and argatroban. 

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