Skip to main content

Drug Interactions between Corlanor and Targretin

This report displays the potential drug interactions for the following 2 drugs:

Edit list (add/remove drugs)

Interactions between your drugs

Moderate

bexarotene ivabradine

Applies to: Targretin (bexarotene) and Corlanor (ivabradine)

MONITOR: Coadministration with inducers of CYP450 3A4 may decrease the plasma concentrations of ivabradine and its active N-desmethylated metabolite, both of which are primarily metabolized by the isoenzyme. In 12 healthy volunteers, administration of a single 10 mg dose of ivabradine following pretreatment with the potent CYP450 3A4 inducer St. John's wort (300 mg three times daily for 14 days) decreased mean ivabradine peak plasma concentration (Cmax) and systemic exposure (AUC) by approximately 53% and 62%, respectively, compared to administration of ivabradine alone. Mean Cmax and AUC of the N-desmethylated metabolite, which is equipotent to ivabradine and circulates at concentrations approximately 40% that of ivabradine, decreased by 25% and 32%, respectively. The extent to which other, less potent inducers of CYP450 3A4 may interact with ivabradine is unknown.

MANAGEMENT: Caution is advised during concomitant use of ivabradine with CYP450 3A4 inducers. The potential for decreased efficacy of ivabradine should be considered.

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. (2015) "Product Information. Corlanor (ivabradine)." Amgen USA

Switch to consumer interaction data

Drug and food interactions

Major

ivabradine food

Applies to: Corlanor (ivabradine)

GENERALLY AVOID: Grapefruit juice may significantly increase the plasma concentrations of ivabradine. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. According to the product labeling, administration with grapefruit juice (quantity unknown) resulted in an approximately twofold increase in ivabradine systemic exposure (AUC). Elevated plasma levels of ivabradine may increase the risk of excessive bradycardia and conduction disturbances.

ADJUST DOSING INTERVAL: Food delays the absorption of ivabradine by approximately 1 hour and increases plasma exposure by 20% to 40% compared to fasting conditions.

MANAGEMENT: Patients treated with ivabradine should avoid or limit consumption of grapefruit or grapefruit juice. The manufacturer recommends taking ivabradine with meals to reduce variability in exposure.

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2015) "Product Information. Corlanor (ivabradine)." Amgen USA

Switch to consumer interaction data

Moderate

bexarotene food

Applies to: Targretin (bexarotene)

ADJUST DOSING INTERVAL: Food may enhance the oral bioavailability of bexarotene. In one clinical study, bexarotene peak plasma concentration (Cmax) and systemic exposure (AUC) resulting from a 75 to 300 mg dose were 35% and 48% higher, respectively, when administered after a fat-containing meal relative to a glucose solution. In all clinical trials, patients were instructed to take bexarotene with or immediately following a meal.

Coadministration with inhibitors of CYP450 3A4 such as grapefruit juice may theoretically increase the plasma concentrations of bexarotene. In vitro studies suggest that bexarotene is metabolized by CYP450 3A4. However, concomitant administration with multiple doses of ketoconazole, a potent CYP450 3A4 inhibitor, did not alter bexarotene plasma concentrations, which would imply that bexarotene elimination is not substantially dependent on CYP450 3A4 metabolism in vivo.

MANAGEMENT: Because safety and efficacy data are based upon administration with food, bexarotene should be administered once daily with a meal. Patients may want to avoid consuming large amounts of grapefruit or grapefruit juice.

References

  1. (2001) "Product Information. Targretin (bexarotene)." Ligand Pharmaceuticals
  2. Cerner Multum, Inc. "UK Summary of Product Characteristics."

Switch to consumer interaction data

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

See also

Report options

Loading...
QR code containing a link to this page

Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer