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Budeprion SR and Sustiva

Determining the interaction of Budeprion SR and Sustiva and the possibility of their joint administration.

Check result:
Budeprion SR <> Sustiva
Relevance: 24.09.2022 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:

Efavirenz may reduce the blood levels and effects of buPROPion. Contact your doctor if your symptoms worsen or your condition changes during treatment with these medications. Your doctor may be able to prescribe alternatives that do not interact, or you may need a dose adjustment or more frequent monitoring to safely use both 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 inducers of CYP450 isoenzymes may decrease the plasma concentrations of bupropion, which undergoes extensive metabolism, particularly by CYP450 2B6. In 12 study patients with mood disorders, administration of a single 150 mg dose of bupropion during treatment with the potent CYP450 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% for erythrohydrobupropion; 81% and 86% for threohydrobupropion), while Cmax and AUC of the third, hydroxybupropion, increased by 71% and 50%, respectively. Although reduced therapeutic effects of bupropion may be anticipated from the interaction, 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. In another 13 study subjects administered a 150 mg dose of sustained-release bupropion during treatment with the 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.

MANAGEMENT: Pharmacologic response to bupropion should be monitored more closely whenever a known CYP450 inducer is added to or withdrawn from therapy, and the bupropion dosage adjusted as necessary. Increases in bupropion dosage should be guided by clinical response; however, the maximum recommended dosage of bupropion should not be exceeded.

References
  • Cerner Multum, Inc. "Australian Product Information." O 0
  • James WA, Lippmann S "Bupropion: overview and prescribing guidelines in depression." South Med J 84 (1991): 222-4
  • "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals, Wilmington, DE.
  • "Product Information. Wellbutrin (bupropion)." Glaxo Wellcome, Research Triangle Park, NC.
  • Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  • Ketter TA, Jenkins JB, Schroeder DH, Pazzaglia PJ, Marangell LB, George MS, Callahan AM, Hinton ML, Chao J, Post RM "Carbamazepine but not valproate induces bupropion metabolism." J Clin Psychopharmacol 15 (1995): 327-33
Budeprion SR

Generic Name: bupropion

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

Synonyms: Budeprion SR (Oral), Budeprion SR Tablets

Sustiva

Generic Name: efavirenz

Brand name: Sustiva

Synonyms: n.a.

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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