Drug Interactions between eluxadoline and Roszet
This report displays the potential drug interactions for the following 2 drugs:
- eluxadoline
- Roszet (ezetimibe/rosuvastatin)
Interactions between your drugs
ezetimibe rosuvastatin
Applies to: Roszet (ezetimibe / rosuvastatin) and Roszet (ezetimibe / rosuvastatin)
MONITOR: Coadministration with ezetimibe may rarely increase the risk of myopathy and serum transaminase elevations associated with HMG-CoA reductase inhibitors (i.e., statins). The mechanism of interaction is unknown. A case report describes two patients whose serum creatine kinase increased after ezetimibe was added to their statin therapy (atorvastatin and fluvastatin, respectively). One of the patients also developed myalgia and tendinopathy, which resolved promptly after withdrawal of both drugs. Statin therapy was subsequently reintroduced at the previous dosage without incident. In the other patient, serum creatine kinase returned to normal within 4 weeks after discontinuation of ezetimibe while the statin was continued. On the contrary, no cases of myopathy or tendinopathy occurred in a study of 33 hypercholesterolemic patients treated with ezetimibe and atorvastatin or simvastatin. There were also no reports of myopathy or significant increases in serum creatine kinase in a study of 32 subjects treated with ezetimibe and fluvastatin. In controlled clinical studies, the incidence of consecutive elevations (greater than 3 times the upper limit of normal) in serum transaminases was 1.3% for patients treated with ezetimibe in combination with a statin versus 0.4% for patients treated with a statin alone. These elevations were generally asymptomatic, not associated with cholestasis, and returned to baseline after discontinuation of therapy or with continued treatment.
MANAGEMENT: Until further information is available, use of a statin in combination with ezetimibe should be approached with caution. Patients should be advised to promptly report to their physician any unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. The drugs should be discontinued if creatine kinase is markedly elevated in the absence of strenuous exercise or if myopathy is otherwise suspected or diagnosed. In addition, liver function tests should be performed at initiation of therapy and according to the recommendations of the HMG-CoA reductase inhibitor.
References
- Gagne C, Gaudet D, Bruckert E (2002) "Efficacy and safety of ezetimibe coadministered with atorvastatin or simvastatin in patients with homozygous familial hypercholesterolemia." Circulation, 105, p. 2469-75
- Fux R, Morike K, Gundel UF, Hartmann R, Gleiter CH (2004) "Ezetimibe and statin-associated myopathy." Ann Intern Med, 140, p. 671-2
ezetimibe eluxadoline
Applies to: Roszet (ezetimibe / rosuvastatin) and eluxadoline
MONITOR: Coadministration with eluxadoline may increase the plasma concentrations of drugs that are substrates of the organic anion transporting polypeptide (OATP) 1B1 and/or breast cancer resistance protein (BCRP) transporters. The mechanism is decreased clearance due to inhibition of OATP1B1-mediated hepatic uptake and BCRP-mediated intestinal and hepatobiliary efflux by eluxadoline. The interaction has been demonstrated for rosuvastatin, a known substrate of both OATP 1B1 and BCRP. When a single 20 mg dose of rosuvastatin was given during multiple dosing of eluxadoline 100 mg twice daily, rosuvastatin peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 18% and 40%, respectively, compared to administration of rosuvastatin alone. Similar results were reported for the active major metabolite, n-desmethyl rosuvastatin.
MANAGEMENT: Caution is advised when eluxadoline is used concomitantly with drugs that are substrates of the OATP1B1 and/or BCRP transporters, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever eluxadoline is added to or withdrawn from therapy.
References
- Cerner Multum, Inc. "UK Summary of Product Characteristics."
- (2015) "Product Information. Viberzi (eluxadoline)." Actavis Pharma, Inc.
rosuvastatin eluxadoline
Applies to: Roszet (ezetimibe / rosuvastatin) and eluxadoline
MONITOR: Coadministration with eluxadoline may increase the plasma concentrations of drugs that are substrates of the organic anion transporting polypeptide (OATP) 1B1 and/or breast cancer resistance protein (BCRP) transporters. The mechanism is decreased clearance due to inhibition of OATP1B1-mediated hepatic uptake and BCRP-mediated intestinal and hepatobiliary efflux by eluxadoline. The interaction has been demonstrated for rosuvastatin, a known substrate of both OATP 1B1 and BCRP. When a single 20 mg dose of rosuvastatin was given during multiple dosing of eluxadoline 100 mg twice daily, rosuvastatin peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 18% and 40%, respectively, compared to administration of rosuvastatin alone. Similar results were reported for the active major metabolite, n-desmethyl rosuvastatin.
MANAGEMENT: Caution is advised when eluxadoline is used concomitantly with drugs that are substrates of the OATP1B1 and/or BCRP transporters, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever eluxadoline is added to or withdrawn from therapy.
References
- Cerner Multum, Inc. "UK Summary of Product Characteristics."
- (2015) "Product Information. Viberzi (eluxadoline)." Actavis Pharma, Inc.
Drug and food interactions
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
- (2015) "Product Information. Viberzi (eluxadoline)." Actavis Pharma, 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
Drug Interaction Classification
| Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
| Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
| 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. | |
| No interaction information available. |
Further information
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