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Kaletra Oral Solution and Wellbutrin XL

Determining the interaction of Kaletra Oral Solution and Wellbutrin XL and the possibility of their joint administration.

Check result:

Kaletra Oral Solution <> Wellbutrin XL

Relevance: 05.01.2023 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Ritonavir may decrease the blood levels and effects of buPROPion. You may need a dose adjustment or more frequent monitoring by your doctor to safely use both medications. Contact your doctor if your symptoms worsen or your condition changes during treatment with these medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Professional:

MONITOR: Coadministration with ritonavir may decrease the plasma concentrations of bupropion and its pharmacologically active metabolites. The proposed mechanism is ritonavir induction of the CYP450 2B6-mediated metabolism of bupropion to hydroxybupropion and the further metabolism of the latter via glucuronidation. Additionally, ritonavir may inhibit the carbonyl reductase enzyme responsible for formation of two other metabolites. In healthy volunteers, administration of bupropion in combination with ritonavir 100 mg twice daily decreased bupropion peak plasma concentration (Cmax) by 21% and systemic exposure (AUC) by 22%. Likewise, the AUC of the metabolites hydroxybupropion, threohydrobupropion, and erythrohydrobupropion decreased by 23%, 38%, and 48%, respectively. When ritonavir was administered at a dose of 600 mg twice daily in healthy volunteers, the Cmax and AUC of bupropion decreased by 62% and 66%, respectively, while the AUC of hydroxybupropion, threohydrobupropion and erythrohydrobupropion decreased by 78%, 50% and 68%, respectively. The interaction has also been studied with lopinavir-ritonavir. When a single 100 mg dose of sustained-release bupropion was administered following lopinavir-ritonavir 400 mg-100 mg twice daily for two weeks in 12 healthy volunteers, bupropion Cmax and AUC decreased by 57% each, and hydroxybupropion Cmax and AUC decreased by 31% and 50%, respectively. The onset of interaction may be about three days after ritonavir initiation, as ritonavir does not appear to have significant acute effects on bupropion. A study in 7 healthy volunteers found that ritonavir 200 mg given for 2 days had minimal impact (less than 20% mean change) on the pharmacokinetics of a single 75 mg dose of bupropion.

MANAGEMENT: Patients should be monitored for altered efficacy of bupropion following the initiation or discontinuation of ritonavir. Dosage adjustments for bupropion may be required; however, the maximum recommended dosage should not be exceeded.

References

Faucette SR, Wang H, Hamilton GA, et al "Regulation of CYP2B6 in primary human hepatocytes by prototypical incucers." Drug Metab Dispos 32 (2004): 348-58
Hesse LM, Greenblatt DJ, von Moltke LL, Court MH "Ritonavir has minimal impact on the pharmacokinetic disposition of a single dose of bupropion administered to human volunteers." J Clin Pharmacol 46 (2006): 567-76
Kharasch ED, Mitchell D, Coles R, Blanco R "Rapid clinical induction of hepatic cytochrome P4502B6 (CYP2B6) activity by ritonavir." Antimicrob Agents Chemother 52 (2008): 1663-9
Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
"Product Information. Norvir (ritonavir)." Abbott Pharmaceutical, Abbott Park, IL.
Faucette SR, Hawke RL, Lecluyse EL, et al "Validation of bupropion hydroxylation as a selective marker of human cytochrome P450 2B6 catalytic activity." Drug Metab Dispos 28 (2000): 1222-30
Park-Wyllie LY, Antoniou T "Concurrent use of bupropion with CYP2B6 inhibitors, nelfinavir, ritonavir and efavirenz: a case series." AIDS 17 (2003): 638-40
Hesse LM, Venkatakrishnan K, Court MH, VonMoltke LL, Duan SX, Shader RI, Greenblatt DJ "CYP2B6 mediates the in vitro hydroxylation of bupropion: Potential drug interactions with other antidepressants." Drug Metab Disposition 28 (2000): 1176-83
Canadian Pharmacists Association "e-CPS. Available from: URL: http://www.pharmacists.ca/function/Subscriptions/ecps.cfm?link=eCPS_quikLink."
EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports. Available from: URL: http://www.ema.europa.eu/ema/index.jsp?curl=pages/includes/medicines/medicines_landingpage.jsp&mid."
Hogeland GW, Swindells S, McNabb JC, Kashuba AD, Yee GC, Lindley CM "Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects." Clin Pharmacol Ther 81 (2007): 69-75

Kaletra Oral Solution

Generic Name: lopinavir / ritonavir

Brand name: Kaletra

Synonyms: Kaletra

What is Kaletra Oral Solution?

Wellbutrin XL

Generic Name: bupropion

Brand name: Aplenzin, Buproban, Forfivo XL, Wellbutrin SR, Wellbutrin XL, Zyban, Zyban Advantage Pack, Budeprion XL

Synonyms: n.a.

What is Wellbutrin XL?

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In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

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