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Efavirenz Tablets and Nelfinavir Tablets

Determining the interaction of Efavirenz Tablets and Nelfinavir Tablets and the possibility of their joint administration.

Check result:
Efavirenz Tablets <> Nelfinavir Tablets
Relevance: 16.08.2022 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:

Consumer information for this minor interaction is not currently available. Some minor drug interactions may not be clinically relevant in all patients. Minor drug interactions do not usually cause harm or require a change in therapy. However, your healthcare provider can determine if adjustments to your medications are needed.

Professional:

Coadministration with efavirenz may modestly increase the plasma concentrations of nelfinavir. The proposed mechanism is efavirenz inhibition of nelfinavir metabolism via CYP450 2C19 to its active metabolite M8, which is a secondary pathway to CYP450 3A4 metabolism that yields inactive metabolites. In 10 study subjects, coadministration of nelfinavir (750 mg every 8 hours) and efavirenz (600 mg once a day) for 7 days resulted in an approximately 20% increase in nelfinavir peak plasma concentration (Cmax) and area under the concentration-time curve (AUC). Efavirenz Cmax and AUC decreased by 12%, while M8 Cmax and AUC decreased by 40% and 37%, respectively. The effect of efavirenz on the pharmacokinetics of nelfinavir boosted by ritonavir, and vice versa, have also been studied. In 24 healthy subjects, coadministration of efavirenz (600 mg) in combination with ritonavir (200 mg) and nelfinavir (1875 mg) once a day in the evening with a snack for 10 days resulted in an increase in nelfinavir Cmax, AUC and C24 (plasma concentration at 24 hours postdose) by 29%, 30% and 48%, respectively, compared to administration of nelfinavir and ritonavir alone. No changes were observed for efavirenz or M8, presumably due to inhibition of CYP450 3A4 metabolism by ritonavir. Although ritonavir Cmax, AUC and C24 were decreased by 24%, 20% and 12%, respectively, its boosting effects apparently remained. No dosage adjustment should be necessary when efavirenz is prescribed with nelfinavir, with or without ritonavir.

References
  • la Porte CJ, de Graaff-Teulen MJ, Colbers EP, et al. "Effect of efavirenz treatment on the pharmacokinetics of nelfinavir boosted by ritonavir in healthy volunteers." Br J Clin Pharmacol 58 (2004): 632-40
  • "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals, Wilmington, DE.
  • Fiske WD, Benedek IH, White SJ, Pepperess KA, Joseph JL, Kornhauser DM "Pharmacokinetic interaction between efavirenz (EFV) and nelfinavir mesylate (NFV) in healthy volunteers." 5th Conf Retrovir Oppor Infect (1998): 144(ab.no.349)
  • Carpenter CJ, Fischl MA, Hammer SM, et al. "Antiretroviral therapy for HIV infection in 1998: updated recommendations of the International AIDS Society--USA Panel." JAMA 280 (1998): 78-86
  • "Product Information. Viracept (nelfinavir)." Agouron Pharma Inc, La Jolla, CA.
Efavirenz Tablets

Generic Name: efavirenz

Brand name: Sustiva

Synonyms: Efavirenz

Nelfinavir Tablets

Generic Name: nelfinavir

Brand name: Viracept

Synonyms: Nelfinavir

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.

Interaction with food and lifestyle