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Flolipid and Sustiva

Determining the interaction of Flolipid and Sustiva and the possibility of their joint administration.

Check result:
Flolipid <> Sustiva
Relevance: 09.11.2022 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:

Using simvastatin together with efavirenz can decrease the effects of simvastatin. Contact your doctor if your condition worsens or if your cholesterol levels increase. You may need a dose adjustment or special test 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 efavirenz may decrease the plasma concentrations and pharmacologic effects of certain HMG-CoA reductase inhibitors (i.e., statins) and/or their active metabolites. The proposed mechanism is efavirenz induction of CYP450 3A4 metabolism. In 14 healthy, HIV-negative adult volunteers, coadministration of efavirenz (600 mg once daily for 15 days) and simvastatin (40 mg once daily on the last 4 days of efavirenz administration) resulted in a 58% median decrease in the systemic exposure (AUC) of simvastatin acid and a 60% median decrease in active HMG-CoA reductase inhibitory activity compared to administration of simvastatin alone. For atorvastatin (10 mg once daily in the same study), the systemic exposure was reduced by 43% and the total active atorvastatin exposure by 34% with efavirenz. Similarly, pravastatin (40 mg once daily in the same study) systemic exposure was reduced 40% by efavirenz. The median LDL cholesterol decrease associated with simvastatin was 11 mg/dL smaller with efavirenz coadministration than with simvastatin alone. For atorvastatin, the median LDL decrease was 6.5 mg/dL smaller with efavirenz, but the difference exhibited only a trend toward statistical significance. There was no significant difference in LDL decrease for pravastatin with or without efavirenz. Neither simvastatin, atorvastatin, nor pravastatin had any effect on the pharmacokinetics of efavirenz.

MANAGEMENT: Coadministration of simvastatin, atorvastatin, or other statins that are primarily metabolized by CYP450 3A4 (e.g., lovastatin) with efavirenz may result in diminished hypolipidemic efficacy. Although pravastatin is not significantly metabolized by CYP450 3A4, it has also been implicated. Dosage adjustment of these statins may be necessary if they are prescribed with efavirenz. The same precaution may be applicable during therapy with nevirapine, another nonnucleoside reverse transcriptase inhibitor that induces CYP450 3A4.

References
  • Gerber JG, Rosenkranz SL, Fichtenbaum CJ, et al. "Effect of efavirenz on the pharmacokinetics of simvastatin, atorvastatin, and pravastatin: results of AIDS Clinical Trials Group 5108 Study." J Acquir Immune Defic Syndr 39 (2005): 307-12
  • "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals, Wilmington, DE.
Flolipid

Generic Name: simvastatin

Brand name: Flolipid, Zocor

Synonyms: n.a.

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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