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Rifadin and Simvastatin Oral Suspension

Determining the interaction of Rifadin and Simvastatin Oral Suspension and the possibility of their joint administration.

Check result:

Rifadin <> Simvastatin Oral Suspension

Relevance: 22.08.2023 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:

RifAMPin may significantly reduce the blood levels of simvastatin, which may make the medication less effective in treating your cholesterol. Talk to your doctor if you have any questions or concerns. Your doctor may be able to prescribe alternatives that do not interact. 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:

GENERALLY AVOID: Coadministration with rifampin may significantly decrease the plasma concentrations of lovastatin and simvastatin and their pharmacologically active acid metabolites. The primary mechanism is rifampin induction of intestinal and hepatic CYP450 3A4 metabolism, resulting in reduced bioavailability of simvastatin and lovastatin and their metabolites. Induction of intestinal P-glycoprotein efflux transporters may also contribute. When a single 40 mg dose of simvastatin was administered to 10 healthy nonsmoking volunteers following pretreatment with rifampin 600 mg orally once daily for 5 days, mean simvastatin systemic exposure (AUC) decreased by 87% (range 56% to 94%) and mean simvastatin acid AUC decreased by 93% (range 82% to 97%) compared to pretreatment with placebo. Rifampin also decreased the mean peak plasma concentration (Cmax) of both by 90%. Although not studied, the interaction is expected to occur at a comparable level with lovastatin due to its similar metabolic profile to simvastatin.

MANAGEMENT: Given the magnitude of interaction, concomitant use of simvastatin, lovastatin, or red yeast rice (which contains lovastatin) with rifampin may result in significantly diminished hypolipidemic efficacy and should be avoided if possible. Pravastatin may be a suitable substitution, as it is not a substrate of CYP450 enzymes or P-glycoprotein. One study reported only a 31% decrease in the mean AUC of single-dose pravastatin following pretreatment with rifampin, and the interaction did not occur in all subjects.

References

Everett DW, Chando TJ, Didonato GC, Singhvi SM, Pan HY, Weinstein SH "Biotransformation of pravastatin sodium in humans." Drug Metab Dispos 19 (1991): 740-8
Kyrklund C, Backman JT, Kivisto KT, Neuvonen M, Laitila J, Neuvonen PJ "Rifampin greatly reduces plasma simvastatin and simvastatin acid concentrations." Clin Pharmacol Ther 68 (2000): 592-7
Bogman K, Peyer AK, Torok M, Kusters E, Drewe J "HMG-CoA reductase inhibitors and P-glycoprotein modulation." Br J Pharmacol 132 (2001): 1183-92
Kyrklund C, Backman JT, Neuvonen M, Neuvonen PJ "Effect of rifampicin on pravastatin pharmacokinetics in healthy subjects." Br J Clin Pharmacol 57 (2004): 181-7

Rifadin

Generic Name: rifampin

Brand name: Rifadin, Rifadin IV, Rimactane

Synonyms: n.a.

What is Rifadin?

Simvastatin Oral Suspension

Generic Name: simvastatin

Brand name: Zocor, Flolipid

Synonyms: Simvastatin

What is Simvastatin Oral Suspension?

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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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