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Drug Interactions between nilotinib and Wellbutrin

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

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Interactions between your drugs

Moderate

buPROPion nilotinib

Applies to: Wellbutrin (bupropion) and nilotinib

MONITOR: Coadministration with inducers of CYP450 2B6 may decrease the plasma concentrations of bupropion. In vitro findings suggest that CYP450 2B6 is the principal isoenzyme involved in the formation of hydroxybupropion, one of three active metabolites of bupropion. In 12 study patients with mood disorders, administration of a single 150 mg dose of bupropion during treatment with the potent CYP450 2B6 inducer carbamazepine (mean dose 942 mg/day for at least 3 weeks) decreased mean bupropion peak plasma concentration (Cmax) and systemic exposure (AUC) by 87% and 90%, respectively, compared to administration with placebo. Mean Cmax and AUC of two active metabolites were also significantly reduced (86% and 96%, respectively, for erythrohydrobupropion; 81% and 86%, respectively, for threohydrobupropion), while Cmax and AUC of hydroxybupropion increased by 71% and 50%, respectively. In another 13 study subjects administered a 150 mg dose of sustained-release bupropion during treatment with the moderate CYP450 2B6 inducer efavirenz (600 mg once daily for 14 days), bupropion Cmax and AUC decreased by an average of 34% and 55%, respectively, while the Cmax of hydroxybupropion increased by 50% with no change in AUC. Although reduced therapeutic effects of bupropion may be anticipated from these interactions, the full clinical impact is uncertain, since metabolites are present in substantially higher plasma levels than the parent drug but have reduced potencies and possibly varied pharmacologic effects. The potency and toxicity of the metabolites relative to bupropion have not been fully characterized in humans. In an antidepressant screening test performed on mice, hydroxybupropion was found to be one-half as potent as bupropion and both erythrohydrobupropion and threohydrobupropion were 5-fold less potent than bupropion. Another CYP450 2B6 inducer, ritonavir, has also been studied but resulted in decreased plasma concentrations of bupropion and all three metabolites. When coadministered with ritonavir 100 mg twice daily for 17 days, bupropion Cmax and AUC decreased by 21% and 22%, respectively; erythrohydrobupropion Cmax and AUC decreased by 28% and 48%, respectively, threohydrobupropion Cmax and AUC decreased by 39% and 38%, respectively; and hydroxybupropion AUC decreased by 23% with no change in Cmax. When coadministered with ritonavir 600 mg twice daily for 8 days, bupropion Cmax and AUC decreased by 62% and 66%, respectively; erythrohydrobupropion Cmax and AUC decreased by 48% and 68%, respectively, threohydrobupropion Cmax and AUC decreased by 58% and 50%, respectively; and hydroxybupropion Cmax and AUC decreased by 42% and 78%, respectively. When coadministered with lopinavir-ritonavir 400 mg-100 mg twice daily for 14 days, bupropion Cmax and AUC decreased by 57% each, while hydroxybupropion Cmax and AUC decreased by 31% and 50%, respectively.

MANAGEMENT: Pharmacologic response to bupropion should be monitored more closely whenever a CYP450 2B6 inducer is added to or withdrawn from therapy, and the bupropion dosage adjusted as necessary. Concomitant use of potent and moderate CYP450 2B6 inducers such as carbamazepine, efavirenz, rifampin, ritonavir, and lopinavir-ritonavir should be avoided with fixed-dose combination products such as bupropion-naltrexone or bupropion-dextromethorphan. For other bupropion products, increases in bupropion dosage should be guided by clinical response; however, the maximum recommended dosage should not be exceeded.

References

  1. James WA, Lippmann S (1991) "Bupropion: overview and prescribing guidelines in depression." South Med J, 84, p. 222-4
  2. (2001) "Product Information. Wellbutrin (bupropion)." Glaxo Wellcome
  3. Ketter TA, Jenkins JB, Schroeder DH, Pazzaglia PJ, Marangell LB, George MS, Callahan AM, Hinton ML, Chao J, Post RM (1995) "Carbamazepine but not valproate induces bupropion metabolism." J Clin Psychopharmacol, 15, p. 327-33
  4. (2001) "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals
  5. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  6. Cerner Multum, Inc. "Australian Product Information."
  7. (2022) "Product Information. Forfivo XL (buPROPion)." Almatica Pharma Inc
  8. (2022) "Product Information. Auvelity (bupropion-dextromethorphan)." Axsome Therapeutics, Inc., 1
  9. (2022) "Product Information. Zyban (bupropion)." GlaxoSmithKline UK Ltd
  10. (2022) "Product Information. Wellbutrin XL (bupropion)." Bausch Health, Canada Inc.
  11. (2021) "Product Information. Contrave (bupropion-naltrexone)." Currax Pharmaceuticals LLC
View all 11 references

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Drug and food interactions

Major

nilotinib food

Applies to: nilotinib

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of nilotinib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. Because nilotinib is associated with concentration-dependent prolongation of the QT interval, increased levels may potentiate the risk of ventricular arrhythmias such as torsade de pointes and sudden death.

ADJUST DOSING INTERVAL: Food increases the oral bioavailability of nilotinib. The mechanism of interaction is unknown. Compared to the fast state, nilotinib systemic exposure (AUC) increased by 82% when the dose was given 30 minutes after a high-fat meal. Because nilotinib is associated with concentration-dependent prolongation of the QT interval, increased levels may potentiate the risk of ventricular arrhythmias such as torsade de pointes and sudden death.

MANAGEMENT: Patients treated with nilotinib should avoid consumption of grapefruit, grapefruit juice, and any supplement containing grapefruit extract. In addition, no food should be consumed for at least 2 hours before and 1 hour after a nilotinib dose.

References

  1. (2007) "Product Information. Tasigna (nilotinib)." Novartis Pharmaceuticals

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Moderate

buPROPion food

Applies to: Wellbutrin (bupropion)

GENERALLY AVOID: Excessive use or abrupt discontinuation of alcohol after chronic ingestion may precipitate seizures in patients receiving bupropion. Additionally, there have been rare postmarketing reports of adverse neuropsychiatric events or reduced alcohol tolerance in patients who drank alcohol during treatment with bupropion. According to one forensic report, a patient died after taking large doses of both bupropion and alcohol. It is uncertain whether a drug interaction was involved. Single-dose studies in healthy volunteers given bupropion and alcohol failed to demonstrate either a significant pharmacokinetic or pharmacodynamic interaction.

MANAGEMENT: The manufacturer recommends that alcohol consumption be minimized or avoided during bupropion treatment. The use of bupropion is contraindicated in patients undergoing abrupt discontinuation of alcohol.

References

  1. Posner J, Bye A, Jeal S, Peck AW, Whiteman P (1984) "Alcohol and bupropion pharmacokinetics in healthy male volunteers." Eur J Clin Pharmacol, 26, p. 627-30
  2. Ramcharitar V, Levine BS, Goldberger BA, Caplan YH (1992) "Bupropion and alcohol fatal intoxication: case report." Forensic Sci Int, 56, p. 151-6
  3. Hamilton MJ, Bush MS, Peck AW (1984) "The effect of bupropion, a new antidepressant drug, and alcohol and their interaction in man." Eur J Clin Pharmacol, 27, p. 75-80
  4. (2001) "Product Information. Wellbutrin (bupropion)." Glaxo Wellcome
View all 4 references

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Moderate

buPROPion food

Applies to: Wellbutrin (bupropion)

MONITOR: Additive or synergistic effects on blood pressure may occur when bupropion is combined with sympathomimetic agents such as nasal decongestants, adrenergic bronchodilators, ophthalmic vasoconstrictors, and systemic vasopressors. Treatment with bupropion can result in elevated blood pressure and hypertension. In clinical practice, hypertension, in some cases severe and requiring acute treatment, has been observed in patients receiving bupropion alone and in combination with nicotine replacement therapy. These events have occurred in both patients with and without evidence of preexisting hypertension. Furthermore, postmarketing cases of hypertensive crisis have been reported during the initial titration phase with bupropion-naltrexone treatment.

MANAGEMENT: Caution is advised when bupropion is used with other drugs that increase dopaminergic or noradrenergic activity due to an increased risk of hypertension. Blood pressure and heart rate should be measured prior to initiating bupropion therapy and monitored at regular intervals consistent with usual clinical practice, particularly in patients with preexisting hypertension. Dose reduction or discontinuation of bupropion should be considered in patients who experience clinically significant and sustained increases in blood pressure or heart rate.

References

  1. (2022) "Product Information. Auvelity (bupropion-dextromethorphan)." Axsome Therapeutics, Inc., 1
  2. (2022) "Product Information. Zyban (bupropion)." GlaxoSmithKline UK Ltd
  3. (2022) "Product Information. Wellbutrin XL (bupropion)." Bausch Health, Canada Inc.
  4. (2021) "Product Information. Contrave (bupropion-naltrexone)." Currax Pharmaceuticals LLC
View all 4 references

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Moderate

buPROPion food

Applies to: Wellbutrin (bupropion)

MONITOR: The concomitant use of bupropion and nicotine replacement for smoking cessation may increase the risk of hypertension. In a clinical study (n=250), 6.1% of patients who used sustained-release bupropion with nicotine transdermal system developed treatment-emergent hypertension, compared to 2.5% of patients treated with bupropion alone, 1.6% treated with nicotine alone, and 3.1% treated with placebo. Three patients in the bupropion plus nicotine group and one patient in the nicotine-only group discontinued treatment due to hypertension. The majority had evidence of preexisting hypertension.

MANAGEMENT: Blood pressure monitoring is recommended for patients concomitantly using bupropion and nicotine replacement for smoking cessation.

References

  1. (2001) "Product Information. Zyban (bupropion)." Glaxo Wellcome

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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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