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Drug Interactions between Rexulti and Wellbutrin

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

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Interactions between your drugs

Major

buPROPion brexpiprazole

Applies to: Wellbutrin (bupropion) and Rexulti (brexpiprazole)

ADJUST DOSE: Coadministration with inhibitors of CYP450 3A4 and/or 2D6 may significantly increase the plasma concentrations of brexpiprazole, which is metabolized by these isoenzymes. According to product labeling, administration of brexpiprazole with a potent 3A4 inhibitor (ketoconazole) or a potent 2D6 inhibitor (quinidine) resulted in an approximately 2-fold increase in AUC.
The combination of brexpiprazole plus potent CYP450 3A4 inhibitors in poor 2D6 metabolizers is expected to result in a 4.8-fold increase in AUC. The combination of brexpiprazole plus potent CYP450 3A4 inhibitors plus potent CYP450 2D6 inhibitors in extensive 2D6 metabolizers is expected to result in a 5.1 increase in AUC.

MANAGEMENT: The manufacturer recommends that the brexpiprazole dosage be reduced as follows during concomitant administration of CYP450 inhibitors. The brexpiprazole dosage should be increased to the original level if these agents are discontinued. It is advisable to monitor patients for clinical response.

- Potent 3A4 inhibitor: One-half of the usual dose.
- Potent or moderate 3A4 inhibitor in known poor 2D6 metabolizers: One-fourth of the usual dose.
- Potent 2D6 inhibitor: One-half of the usual dose. No dosage adjustments are required for patients with major depressive disorder.
- Potent or moderate 3A4 inhibitor plus potent or moderate 2D6 inhibitor: One-fourth of the usual dose.

Potent CYP450 3A4 inhibitors: antiviral boosters, adagrasib, boceprevir, ceritinib, clarithromycin, conivaptan, delavirdine, idelalisib, indinavir, itraconazole, ketoconazole, lonafarnib, nefazodone, nelfinavir, posaconazole, saquinavir, telaprevir, telithromycin, voriconazole.

Moderate CYP450 3A4 inhibitors: aprepitant, atazanavir, ciprofloxacin, clotrimazole, crizotinib, dalfopristin, darunavir, diltiazem, dronedarone, erythromycin, fluconazole, fosamprenavir, fosaprepitant, imatinib, isavuconazonium, mifepristone, netupitant, nilotinib, ranolazine, stiripentol, verapamil.

Potent CYP450 2D6 inhibitors: bupropion, cinacalcet, fluoxetine, methotrimeprazine, paroxetine, quinidine, ritonavir.

Moderate CYP450 2D6 inhibitors: abiraterone, adagrasib, celecoxib, cimetidine, clobazam, darifenacin, diphenhydramine, duloxetine, eliglustat, givosiran, lorcaserin, mirabegron, panobinostat, ranolazine, sertraline, stiripentol.

References

  1. (2015) "Product Information. Rexulti (brexpiprazole)." Otsuka American Pharmaceuticals Inc

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Drug and food interactions

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

brexpiprazole food

Applies to: Rexulti (brexpiprazole)

GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents. Use in combination may result in additive central nervous system depression and/or impairment of judgment, thinking, and psychomotor skills.

MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol. Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

References

  1. Warrington SJ, Ankier SI, Turner P (1986) "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology, 15, p. 31-7
  2. Gilman AG, eds., Nies AS, Rall TW, Taylor P (1990) "Goodman and Gilman's the Pharmacological Basis of Therapeutics." New York, NY: Pergamon Press Inc.
  3. (2012) "Product Information. Fycompa (perampanel)." Eisai Inc
  4. (2015) "Product Information. Rexulti (brexpiprazole)." Otsuka American Pharmaceuticals Inc
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.


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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

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.