Carvedilol drug interactions: Difference between revisions
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==Drug-Drug Interactions== | ==Drug-Drug Interactions== | ||
Since carvedilol undergoes substantial oxidative metabolism, the metabolism and pharmacokinetics of carvedilol may be affected by induction or inhibition of cytochrome P450 enzymes. | Since carvedilol undergoes substantial oxidative metabolism, the metabolism and pharmacokinetics of carvedilol may be affected by induction or inhibition of [[cytochrome P450]] enzymes. | ||
====Amiodarone==== | ====Amiodarone==== | ||
In a pharmacokinetic trial conducted in 106 Japanese subjects with heart failure, coadministration of small loading and maintenance doses of amiodarone with carvedilol resulted in at least a 2-fold increase in the steady-state trough concentrations of S(-)-carvedilol[see Drug Interactions (7.6)]. | In a pharmacokinetic trial conducted in 106 Japanese subjects with heart failure, coadministration of small loading and maintenance doses of [[amiodarone]] with carvedilol resulted in at least a 2-fold increase in the steady-state trough concentrations of S(-)-carvedilol[see Drug Interactions (7.6)]. | ||
====Cimetidine==== | ====Cimetidine==== | ||
In a pharmacokinetic trial conducted in 10 healthy male subjects, cimetidine (1,000 mg/day) increased the steady-state AUC of carvedilol by 30% with no change in Cmax [see Drug Interactions (7.5)]. | In a pharmacokinetic trial conducted in 10 healthy male subjects, [[cimetidine ]](1,000 mg/day) increased the steady-state AUC of carvedilol by 30% with no change in Cmax [see Drug Interactions (7.5)]. | ||
====Digoxin==== | ====Digoxin==== | ||
Following concomitant administration of carvedilol (25 mg once daily) and digoxin (0.25 mg once daily) for 14 days, steady-state AUC and trough concentrations of digoxin were increased by 14% and 16%, respectively, in 12 hypertensive subjects [see Drug Interactions (7.4)]. | Following concomitant administration of carvedilol (25 mg once daily) and [[digoxin]] (0.25 mg once daily) for 14 days, steady-state AUC and trough concentrations of digoxin were increased by 14% and 16%, respectively, in 12 hypertensive subjects [see Drug Interactions (7.4)]. | ||
====Glyburide==== | ====Glyburide==== | ||
In 12 healthy subjects, combined administration of carvedilol (25 mg once daily) and a single dose of glyburide did not result in a clinically relevant pharmacokinetic interaction for either compound. | In 12 healthy subjects, combined administration of carvedilol (25 mg once daily) and a single dose of [[glyburide]] did not result in a clinically relevant pharmacokinetic interaction for either compound. | ||
====Hydrochlorothiazide==== | ====Hydrochlorothiazide==== | ||
A single oral dose of carvedilol 25 mg did not alter the pharmacokinetics of a single oral dose of hydrochlorothiazide 25 mg in 12 subjects with hypertension. Likewise, hydrochlorothiazide had no effect on the pharmacokinetics of carvedilol. | A single oral dose of carvedilol 25 mg did not alter the pharmacokinetics of a single oral dose of [[hydrochlorothiazide]] 25 mg in 12 subjects with hypertension. Likewise, hydrochlorothiazide had no effect on the pharmacokinetics of carvedilol. | ||
====Rifampin==== | ====Rifampin==== | ||
In a pharmacokinetic trial conducted in 8 healthy male subjects, rifampin (600 mg daily for 12 days) decreased the AUC and Cmax of carvedilol by about 70% [see Drug Interactions (7.5)]. | In a pharmacokinetic trial conducted in 8 healthy male subjects, [[rifampin]] (600 mg daily for 12 days) decreased the AUC and Cmax of carvedilol by about 70% [see Drug Interactions (7.5)]. | ||
====Torsemide==== | ====Torsemide==== | ||
In a trial of 12 healthy subjects, combined oral administration of carvedilol 25 mg once daily and torsemide 5 mg once daily for 5 days did not result in any significant differences in their pharmacokinetics compared with administration of the drugs alone. | In a trial of 12 healthy subjects, combined oral administration of carvedilol 25 mg once daily and [[torsemide]] 5 mg once daily for 5 days did not result in any significant differences in their pharmacokinetics compared with administration of the drugs alone. | ||
====Warfarin==== | ====Warfarin==== | ||
Carvedilol (12.5 mg twice daily) did not have an effect on the steady-state prothrombin time ratios and did not alter the pharmacokinetics of R(+)- and S(-)-warfarin following concomitant administration with warfarin in 9 healthy volunteers.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = COREG (CARVEDILOL) TABLET, FILM COATED [GLAXOSMITHKLINE LLC] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c57982f2-c7da-488a-7ea9-b9609439ac68#nlm34089-3 | publisher = | date = | accessdate = }}</ref> | Carvedilol (12.5 mg twice daily) did not have an effect on the steady-state [[prothrombin time]] ratios and did not alter the pharmacokinetics of R(+)- and S(-)-[[warfarin]] following concomitant administration with warfarin in 9 healthy volunteers.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = COREG (CARVEDILOL) TABLET, FILM COATED [GLAXOSMITHKLINE LLC] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c57982f2-c7da-488a-7ea9-b9609439ac68#nlm34089-3 | publisher = | date = | accessdate = }}</ref> | ||
==References== | ==References== | ||
Revision as of 20:56, 20 February 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]
Drug-Drug Interactions
Since carvedilol undergoes substantial oxidative metabolism, the metabolism and pharmacokinetics of carvedilol may be affected by induction or inhibition of cytochrome P450 enzymes.
Amiodarone
In a pharmacokinetic trial conducted in 106 Japanese subjects with heart failure, coadministration of small loading and maintenance doses of amiodarone with carvedilol resulted in at least a 2-fold increase in the steady-state trough concentrations of S(-)-carvedilol[see Drug Interactions (7.6)].
Cimetidine
In a pharmacokinetic trial conducted in 10 healthy male subjects, cimetidine (1,000 mg/day) increased the steady-state AUC of carvedilol by 30% with no change in Cmax [see Drug Interactions (7.5)].
Digoxin
Following concomitant administration of carvedilol (25 mg once daily) and digoxin (0.25 mg once daily) for 14 days, steady-state AUC and trough concentrations of digoxin were increased by 14% and 16%, respectively, in 12 hypertensive subjects [see Drug Interactions (7.4)].
Glyburide
In 12 healthy subjects, combined administration of carvedilol (25 mg once daily) and a single dose of glyburide did not result in a clinically relevant pharmacokinetic interaction for either compound.
Hydrochlorothiazide
A single oral dose of carvedilol 25 mg did not alter the pharmacokinetics of a single oral dose of hydrochlorothiazide 25 mg in 12 subjects with hypertension. Likewise, hydrochlorothiazide had no effect on the pharmacokinetics of carvedilol.
Rifampin
In a pharmacokinetic trial conducted in 8 healthy male subjects, rifampin (600 mg daily for 12 days) decreased the AUC and Cmax of carvedilol by about 70% [see Drug Interactions (7.5)].
Torsemide
In a trial of 12 healthy subjects, combined oral administration of carvedilol 25 mg once daily and torsemide 5 mg once daily for 5 days did not result in any significant differences in their pharmacokinetics compared with administration of the drugs alone.
Warfarin
Carvedilol (12.5 mg twice daily) did not have an effect on the steady-state prothrombin time ratios and did not alter the pharmacokinetics of R(+)- and S(-)-warfarin following concomitant administration with warfarin in 9 healthy volunteers.[1]
References
Adapted from the FDA Package Insert.