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Drug Interactions between leflunomide and palbociclib

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

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Interactions between your drugs

Major

leflunomide palbociclib

Applies to: leflunomide and palbociclib

MONITOR CLOSELY: The use of leflunomide with other immunosuppressive or myelosuppressive agents may increase the risk of infections. The risk is thought to extend to teriflunomide, its principal active metabolite, because recommended dosages of both result in a similar range of plasma concentrations of teriflunomide. Serious infections including sepsis, as well as opportunistic infections like Pneumocystis jiroveci pneumonia, pulmonary and extrapulmonary tuberculosis, and aspergillosis have been reported with the use of leflunomide, particularly in patients on concomitant hematotoxic therapy. Agents that may be significantly immuno- or myelosuppressive include antineoplastic agents, radiation, zidovudine, linezolid, some antirheumatic agents, high dosages of corticosteroids or adrenocorticotropic agents (greater than 10 mg/day to 1 mg/kg/day, whichever is less, of prednisone or equivalent for more than 2 weeks), and long-term topical or inhaled corticosteroids. Rare cases of pancytopenia, agranulocytosis, and thrombocytopenia have also occurred with leflunomide alone, but were most frequent in the presence of concomitant or recent use of methotrexate or other myelotoxic agents. Due to the prolonged elimination half-life of leflunomide's active metabolite, an interaction may occur even when hematotoxic agents are initiated after the discontinuation of leflunomide. Administering a washout procedure with cholestyramine or activated charcoal helps to accelerate elimination of the active metabolite from plasma and reduce the overlap of systemic exposure to these agents.

MANAGEMENT: Close monitoring for the development of infection is recommended if leflunomide or teriflunomide is used in patients who are currently receiving or have recently received other immuno- or myelosuppressive agents, and vice versa. Platelet, white blood cell count, and hemoglobin or hematocrit should be evaluated at baseline and regularly during therapy. Patients should be advised to contact their physician if they develop signs and symptoms of infection such as fever, chills, diarrhea, sore throat, muscle aches, shortness of breath, blood in phlegm, weight loss, red or inflamed skin, body sores, and pain or burning during urination. If evidence of serious infection or bone marrow suppression occurs, treatment should be stopped, and cholestyramine or charcoal administered to accelerate elimination of leflunomide's active metabolite from plasma, which otherwise may take up to two years.

References (2)
  1. (2001) "Product Information. Arava (leflunomide)." Hoechst Marion Roussel
  2. (2012) "Product Information. Aubagio (teriflunomide)." Genzyme Corporation

Drug and food interactions

Moderate

leflunomide food

Applies to: leflunomide

GENERALLY AVOID: The consumption of alcohol during therapy with leflunomide may potentiate the risk of liver injury. Leflunomide has been associated with hepatotoxicity, including elevated liver transaminases, hepatitis, jaundice/cholestasis, hepatic failure, and acute hepatic necrosis,

MANAGEMENT: Patients should be advised to avoid excessive alcohol use during leflunomide treatment.

References (3)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Canadian Pharmacists Association (2006) e-CPS. http://www.pharmacists.ca/function/Subscriptions/ecps.cfm?link=eCPS_quikLink
  3. Cerner Multum, Inc. "Australian Product Information."
Moderate

palbociclib food

Applies to: palbociclib

GENERALLY AVOID: Grapefruit and/or grapefruit juice may increase the systemic exposure to palbociclib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Increased exposure to palbociclib may increase the risk of adverse effects such as infections, neutropenia, leukopenia, anemia, thrombocytopenia, anorexia, nausea, vomiting, diarrhea, stomatitis, alopecia, asthenia, peripheral neuropathy, and epistaxis.

ADJUST DOSING INTERVAL: Food may enhance the oral bioavailability of palbociclib capsules and reduce the intersubject variability of palbociclib exposure. According to the product labeling, absorption and exposure of palbociclib from its oral capsule formulation were very low in approximately 13% of the population when taken in the fasted state. Food intake increased the palbociclib exposure in this small subset of the population but did not alter exposure in the rest of the population to a clinically relevant extent. Compared to palbociclib capsules given under overnight fasted conditions, the population average palbociclib peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 38% and 21%, respectively, when given with high-fat, high-calorie food (approximately 800 to 1000 calories; 150, 250, and 500 to 600 calories from protein, carbohydrate and fat, respectively); by 27% and 12%, respectively, when given with low-fat, low-calorie food (approximately 400 to 500 calories; 120, 250, and 28 to 35 calories from protein, carbohydrate and fat, respectively); and by 24% and 13%, respectively, when given with moderate-fat, standard calorie food (approximately 500 to 700 calories; 75 to 105, 250 to 350 and 175 to 245 calories from protein, carbohydrate and fat, respectively) one hour before and two hours after palbociclib capsule dosing.

MANAGEMENT: Patients should avoid consumption of grapefruit or grapefruit juice while on treatment with palbociclib. To avoid variability in drug absorption between doses, palbociclib capsules should be taken with food. Palbociclib tablet formulations may be taken with or without food.

References (4)
  1. (2020) "Product Information. Ibrance (palbociclib)." Pfizer Australia Pty Ltd, pfpibrac10620
  2. (2021) "Product Information. Ibrance (palbociclib)." Pfizer Canada Inc
  3. (2023) "Product Information. Ibrance (palbociclib)." Pfizer Ltd
  4. (2022) "Product Information. Ibrance (palbociclib)." Pfizer U.S. Pharmaceuticals Group

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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