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Drug Interactions between elbasvir / grazoprevir and eluxadoline

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

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Interactions between your drugs

Major

eluxadoline grazoprevir

Applies to: eluxadoline and elbasvir / grazoprevir

CONTRAINDICATED: Coadministration with inhibitors of organic anion transporting polypeptides (OATP) 1B1 and/or 1B3 may significantly increase the plasma concentrations of grazoprevir, which is a substrate of the hepatic uptake transporters. In 12 study subjects, administration of a single 200 mg dose of grazoprevir with a single 600 mg intravenous dose of rifampin, a potent OATP1B1 inhibitor, resulted in greater than 10-fold increases in grazoprevir peak plasma concentration (Cmax) and systemic exposure (AUC) compared to administration of grazoprevir alone. A single 600 mg oral dose of rifampin administered during multiple-dosing of grazoprevir 200 mg once daily increased the Cmax and AUC of grazoprevir by 6.5- and 8.4-fold, respectively. Pharmacokinetic studies with other OATP1B1 inhibitors have reported similar results. In one study, administration of grazoprevir 200 mg once daily with atazanavir/ritonavir 300 mg/100 mg once daily increased grazoprevir Cmax, AUC and Cmin by 6.2-, 10.6- and 11.6-fold, respectively (n=12). Likewise, administration with darunavir/ritonavir 600 mg/100 mg twice daily increased grazoprevir Cmax, AUC and Cmin by 5.3-, 7.5- and 8.1-fold, respectively (n=13), while administration with lopinavir/ritonavir 400 mg/100 mg twice daily increased grazoprevir Cmax, AUC and Cmin by 7.3-, 12.9- and 21.7-fold, respectively (n=13). A single 400 mg dose of cyclosporine increased grazoprevir Cmax, AUC and Cmin by 17.0-, 15.2- and 3.4-fold, respectively (n=14). High plasma levels of grazoprevir may increase the risk of adverse effects such as alanine aminotransferase (ALT) elevations.

MANAGEMENT: Concomitant use of elbasvir-grazoprevir with OATP 1B1 or 1B3 inhibitors is considered contraindicated.

References (5)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2016) "Product Information. Zepatier (elbasvir-grazoprevir)." Merck & Co., Inc
  4. (2020) "Product Information. Nexlizet (bempedoic acid-ezetimibe)." Esperion Therapeutics
  5. (2020) "Product Information. Nexletol (bempedoic acid)." Esperion Therapeutics

Drug and food interactions

Major

eluxadoline food

Applies to: eluxadoline

CONTRAINDICATED: Consumption of more than 3 alcoholic beverages per day may increase the risk of acute pancreatitis during treatment with eluxadoline. Pancreatitis has been reported rarely during clinical trials of eluxadoline, and may or may not be related to sphincter of Oddi spasm.

ADJUST DOSING INTERVAL: High-fat meals may reduce the oral bioavailability of eluxadoline. In 28 healthy volunteers, administration of a single 100 mg dose of eluxadoline with a high-fat meal (approximately 800 to 1000 total calories, 50% from fat) decreased eluxadoline peak plasma concentration (Cmax) and systemic exposure (AUC) by 50% and 60%, respectively, compared to administration in the fasted state. There was no significant effect on the time to peak concentration (Tmax). The clinical relevance of this interaction is unknown. It should be noted that phase 3 clinical trials were conducted under fed conditions.

MANAGEMENT: Chronic or acute excessive use of alcohol should be avoided during treatment with eluxadoline. Alcoholism, alcohol abuse, alcohol addiction, and consumption of more than 3 alcoholic beverages per day are considered contraindications to the use of eluxadoline. The product labeling recommends taking eluxadoline with food. Patients should be advised to stop taking eluxadoline and seek medical attention if they experience potential symptoms of pancreatitis such as persistent nausea, vomiting, abdominal tenderness, and upper abdominal pain, especially that which is made worse after eating or radiates to the back or shoulders.

References (1)
  1. (2015) "Product Information. Viberzi (eluxadoline)." Actavis Pharma, Inc.
Minor

grazoprevir food

Applies to: elbasvir / grazoprevir

Food does not appear to have clinically significant effects on the pharmacokinetics of elbasvir and grazoprevir. When a single 50 mg-100 mg dose of elbasvir-grazoprevir was administered to healthy study subjects with a high-fat meal (900 kcal; 500 kcal from fat), elbasvir peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by 15% and 11%, respectively, while grazoprevir Cmax and AUC increased by 2.8- and 1.5-fold, respectively, compared to administration under fasting conditions. According to the product labeling, elbasvir-grazoprevir may be administered with or without food.

References (1)
  1. (2016) "Product Information. Zepatier (elbasvir-grazoprevir)." Merck & Co., Inc

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

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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

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