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Drug Interactions between mycophenolic acid and rifampin

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

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Interactions between your drugs

Major

rifAMPin mycophenolic acid

Applies to: rifampin and mycophenolic acid

GENERALLY AVOID: Coadministration with rifampin may decrease the plasma concentrations of mycophenolic acid (MPA). The mechanism is thought to involve induction of MPA glucuronidation via gastrointestinal and hepatic uridine diphosphate glucuronosyltransferase (UGT) isozymes and reduction of enterohepatic recirculation of MPA metabolites secondary to competitive inhibition of multidrug resistance-associated protein 2 (MRP2)-mediated biliary excretion by rifampin. In one case report, a 67% decrease in dose-corrected MPA systemic exposure (AUC) was reported in a heart-lung transplant patient during concomitant treatment with mycophenolate mofetil and rifampin. Two weeks after discontinuation of rifampin therapy, the dose-corrected AUC of MPA increased by 221% and the 12-hour trough plasma concentration increased by approximately 7-fold. Another study in pediatric liver transplant patients also reported suboptimal levels of MPA in 2 patients who received concomitant treatment with rifampin, despite a 2-fold increase in the mycophenolate mofetil dosage. In a study with 8 kidney transplant recipients, coadministration of mycophenolate mofetil 750 mg to 1 g twice daily and rifampin 600 mg daily for 8 days decreased MPA systemic exposure (AUC) and trough plasma concentration by an average of 17.5% and 48.8%, respectively. In addition, the AUCs of the primary metabolites, MPA 7-O-glucuronide and MPA acyl-glucuronide, significantly increased by an average of 34.4% and 193%, respectively. Because MPA acyl-glucuronide is pharmacologically active and possesses proinflammatory properties, increased exposure may increase side effects such as diarrhea and anemia.

MANAGEMENT: Given the risk of organ rejection associated with inadequate immunosuppressant blood levels, mycophenolate mofetil and mycophenolic acid should not be administered with rifampin unless the potential benefit outweighs the risk.

References (7)
  1. (2001) "Product Information. CellCept (mycophenolate mofetil)." Roche Laboratories
  2. (2004) "Product Information. Myfortic (mycophenolic acid)." Novartis Pharmaceuticals
  3. Kuypers DR, Verleden G, Naesens M, Vanrenterghem Y (2005) "Drug interaction between mycophenolate mofetil and rifampin: Possible induction of uridine diphosphate-glucuronosyltransferase." Clin Pharmacol Ther, 78, p. 81-8
  4. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  5. Pharmaceutical Society of Australia (2006) APPGuide online. Australian prescription products guide online. http://www.appco.com.au/appguide/default.asp
  6. Naesens M, Kuypers DR, Streit F, et al. (2006) "Rifampin induces alterations in mycophenolic acid glucuronidation and elimination: Implications for drug exposure in renal allograft recipients." Clin Pharmacol Ther, 80, p. 509-21
  7. Barau C, Barrail-Tran A, et al. (2011) "Optimization of the dosing regimen of mycophenolate mofetil in pediatric liver transplant recipients." Liver Transpl, 17, p. 1152-8

Drug and food interactions

Moderate

rifAMPin food

Applies to: rifampin

GENERALLY AVOID: Concurrent use of rifampin in patients who ingest alcohol daily may result in an increased incidence of hepatotoxicity. The increase in hepatotoxicity may be due to an additive risk as both alcohol and rifampin are individually associated with this adverse reaction. However, the exact mechanism has not been established.

ADJUST DOSING INTERVAL: Administration with food may reduce oral rifampin absorption, increasing the risk of therapeutic failure or resistance. In a randomized, four-period crossover phase I study of 14 healthy male and female volunteers, the pharmacokinetics of single dose rifampin 600 mg were evaluated under fasting conditions and with a high-fat meal. Researchers observed that administration of rifampin with a high-fat meal reduced rifampin peak plasma concentration (Cmax) by 36%, nearly doubled the time to reach peak plasma concentration (Tmax) but reduced overall exposure (AUC) by only 6%.

MANAGEMENT: The manufacturer of oral forms of rifampin recommends administration on an empty stomach, 30 minutes before or 2 hours after meals. Patients should be encouraged to avoid alcohol or strictly limit their intake. Patients who use alcohol and rifampin concurrently or have a history of alcohol use disorder may require additional monitoring of their liver function during treatment with rifampin.

References (6)
  1. (2022) "Product Information. Rifampin (rifAMPin)." Akorn Inc
  2. (2022) "Product Information. Rifampicin (rifampicin)." Mylan Pharmaceuticals Inc
  3. (2023) "Product Information. Rifadin (rifampicin)." Sanofi
  4. (2024) "Product Information. Rifadin (rifaMPICin)." Sanofi-Aventis Australia Pty Ltd
  5. Peloquin CA, Namdar R, Singleton MD, Nix DE (2024) Pharmacokinetics of rifampin under fasting conditions, with food, and with antacids https://pubmed.ncbi.nlm.nih.gov/9925057/
  6. (2019) "Product Information. Rofact (rifampin)." Bausch Health, Canada Inc.
Moderate

mycophenolic acid food

Applies to: mycophenolic acid

ADJUST DOSING INTERVAL: Administration of enteric coated mycophenolic acid with meals may alter its pharmacokinetics relative to administration in the fasting state. When mycophenolic acid 720 mg was administered with a high-fat meal, there was a 33% decrease in the peak plasma concentration (Cmax); a 3.5-hour increase in delay time for the rise of plasma mycophenolic acid; and a 5-hour delay in the time to reach peak plasma concentration (Tmax). However, no effect was observed on the systemic exposure of mycophenolic acid.

MANAGEMENT: To avoid variability in drug absorption between doses, enteric coated formulations of mycophenolic acid should be taken on an empty stomach, one hour before or two hours after food intake. The tablets should be swallowed whole and not crushed, chewed or divided in order to maintain the integrity of the enteric coating.

References (1)
  1. (2004) "Product Information. Myfortic (mycophenolic acid)." Novartis Pharmaceuticals

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.

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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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