Bupropion with Nevirapine Interaction Details

Brand Names Associated with Bupropion

Brand Names Associated with Nevirapine

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Mar 06, 2024

Interaction Effect

Decreased buPROPion and hydroxybupropion exposure

Interaction Summary

Avoid coadministration of buPROPion and inducers of CYP2B6[1], as reductions in buPROPion plasma concentrations may lead to reduced efficacy [2][1]. In a series of studies in healthy volunteers, coadministration of buPROPion (CYP2B6 substrate) with different CYP2B6 inducers (efavirenz, lopinavir, and ritonavir) decreased buPROPion exposure by as much as 66% in a dose-dependent manner. If coadministration is necessary, consider increasing the buPROPion dose if necessary (avoiding exceeding the maximum recommended dose) [2].

Severity

Major

Onset

Delayed

Evidence

Theoretical

How To Manage Interaction

Avoid coadministration of buPROPion and inducers of CYP2B6[1], as reductions in buPROPion plasma concentrations may lead to reduced efficacy [2][1]. If coadministration is necessary, consider increasing the buPROPion dose if necessary (avoiding exceeding the maximum recommended dose) [2].

Mechanism Of Interaction

Induction of CYP2B6-mediated buPROPion metabolism

Literature Reports

A) Concomitant administration of buPROPion and ritonavir resulted in decreased buPROPion AUC and Cmax. When buPROPion was administered concurrently with ritonavir 600 mg twice daily for 8 days in healthy volunteers, decreases in AUC and Cmax were observed for both buPROPion (66% and 62%, respectively) and the hydroxybupropion metabolite (78% and 42%, respectively). In a second study, concomitant administration of buPROPion and ritonavir 100 mg twice daily in healthy volunteers reduced AUC and Cmax for both buPROPion (22% and 21%, respectively) and the hydroxybupropion metabolite Cmax by 44% [3][4].

B) Short-term ritonavir administration had minimal effect on buPROPion pharmacokinetics in healthy males in a randomized, crossover study (N=7, age 18 to 45 years). Subjects received either oral ritonavir 200 mg twice daily for 2 consecutive days or placebo. BuPROPion was given to all subjects as a single, oral 75-mg dose concurrently with the morning ritonavir or placebo dose on day 2. Following a 1-week washout period, subjects were crossed over to the opposite treatment arm and the procedure was repeated. Results showed a less than 20% change in pharmacokinetic parameters for buPROPion and its metabolites (hydroxybupropion, threohydrobupropion, and erythrohydrobupropion) when coadministered with ritonavir. Significant changes occurred in threohydrobupropion AUC, which decreased by 14%, and erythrohydrobupropion Tmax, which increased by 161%, from 2.6 to 5.2 hours [5].

C) In 13 healthy volunteers, the administration of a single dose of buPROPion 150 mg sustained-release before and after a 2-week regimen of efavirenz 600 mg once daily resulted in significant 34% and 55% decreases in buPROPion Cmax and AUC values, respectively, and a 50% increase in the Cmax of hydroxybupropion (active metabolite of buPROPion). While the ratio of hydroxybupropion to buPROPion increased significantly (2.3-fold) with the concomitant use of efavirenz, the AUC of hydroxybupropion was not affected [6].

D) In an open-label, sequential, 3-phase study in healthy participants, coadministration of buPROPion and lopinavir/ritonavir significantly decreased buPROPion and hydroxybupropion exposure. Subjects aged 20 to 44 years (N=12) were given a single 100-mg dose of sustained-release buPROPion (day 1) and following a 2-week washout period received lopinavir 400 mg/ritonavir 100 mg twice daily for 14 days. On day 30, a second 100-mg dose of sustained-release buPROPion was given simultaneously with lopinavir/ritonavir. Results showed that, when given in combination with lopinavir/ritonavir, both mean buPROPion Cmax and AUC significantly decreased by 57% compared to when buPROPion was given alone. The mean Cmax and AUC of buPROPion's active metabolite, hydroxybupropion, also significantly decreased by 31% and 50%, respectively. The AUC ratio of hydroxybupropion to buPROPion increased from 12.2 when buPROPion was given alone to 14.5 when given concurrently with lopinavir/ritonavir. No significant alterations occurred in lopinavir/ritonavir pharmacokinetic parameters [7].

References

1 ) Product Information: CONTRAVE(R) oral extended-release tablets, naltrexone HCl bupropion HCl oral extended-release tablets. Currax Pharmaceuticals LLC (per manufacturer), Morristown, NJ, 2021.

2 ) Product Information: WELLBUTRIN XL(R) oral extended-release tablets, bupropion HCl oral extended-release tablets. Bausch Health US, LLC (per FDA), Bridgewater, NJ, 2021.

3 ) Product Information: CONTRAVE(R) oral extended-release tablets, naltrexone HCl and bupropion HCl oral extended-release tablets. Orexigen Therapeutics, Inc. (per manufacturer), La Jolla, CA, 2014.

4 ) Product Information: WELLBUTRIN SR(R) oral sustained-release tablets, bupropion HCl oral sustained-release tablets. GlaxoSmithKline (per FDA), Research Triangle Park, NC, 2013.

5 ) Hesse LM, Greenblatt DJ, vonMoltke LL, et al: Ritonavir has minimal impact on the pharmacokinetic disposition of a single dose of bupropion administered to human volunteers. J Clin Pharmacol 2006; 46(5):567-576.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

6 ) Robertson SM, Maldarelli F, Natarajan V, et al: Efavirenz induces CYP2B6-mediated hydroxylation of bupropion in healthy subjects. J Acquir Immune Defic Syndr 2008; 49(5):513-519.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

7 ) Hogeland GW, Swindells S, McNabb JC, et al: Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Clin Pharmacol Ther 2007; 81(1):69-75.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

Bupropion Overview

• Bupropion (Aplenzin, Wellbutrin, Wellbutrin SR, Wellbutrin XL) is used to treat depression. Bupropion (Aplenzin, Wellbutrin XL) is also used to treat seasonal affective disorder (SAD; episodes of depression that occur at the same time each year [usually in the fall and winter but rarely may occur in the spring or summer months]). Bupropion (Zyban) is used to help people stop smoking. Bupropion is in a class of medications called antidepressants. It works by increasing certain types of activity in the brain.

Nevirapine Overview

• Nevirapine is used along with other medications to treat human immunodeficiency virus (HIV) infection in adults and children 15 days of age and older. Nevirapine should not be used to treat healthcare workers or other individuals exposed to HIV infection after contact with HIV-contaminated blood, tissues, or other body fluids. Nevirapine is in a class of medications called non-nucleoside reverse transcriptase inhibitors (NNRTIs). It works by decreasing the amount of HIV in the blood. Although nevirapine does not cure HIV, it may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses such as serious infections or cancer. Taking these medications along with practicing safer sex and making other life-style changes may decrease the risk of transmitting (spreading) the HIV virus to other people.

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Definitions

Severity Categories

Contraindicated

These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.

Major

This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.

Moderate

This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.

Minor

While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.

Onset

Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.

Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.

Evidence

Level of documentation of the interaction.

Established: The interaction is documented and substantiated in peer-reviewed medical literature.

Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.

How To Manage The Interaction

Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.

It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.

Mechanism Of Interaction

The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.

Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.

Where Does Our Information Come From?

Information for our drug interactions is compiled from several drug compendia, including:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

The prescribing information for each drug, as published on DailyMED, is also used. 

Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.

The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.