Interaction of Rifampin and Glyburide

Self, Timothy H.; Tsiu, Sandra J.; Fowler, John W.

doi:10.1378/chest.96.6.1443a

Cited by 13 publications

(11 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Many drugs are co‐substrates for CYP enzymes and P‐gp, exhibiting clinically relevant drug–drug interactions owing to the co‐induction of CYP3A4 and MDR1 genes by rifampin. In our study, we found that multiple doses of rifampin induced liver enzymes and possibly efflux transporters, leading to a significant decrease in glyburide exposure following oral dosing, consistent with previous studies and clinical observations 5 , 5 , 5 , 5 . However, when rifampin was present in the blood after enzyme induction, the AUC and C max were decreased by only 22 and 8%, respectively, in comparison to 63 and 81%, respectively, during the enzyme induction phase.…”

Section: Discussionsupporting

confidence: 91%

“…Clinical case reports showed that rifampin and ciprofloxacin exhibit interactions with glyburide, leading to decreased and increased glyburide effects, respectively. A study in patients and a case report indicated that multiple doses of rifampin decreased the effects of glyburide 16 , 17 . Further investigations showed that rifampin decreased the area under the concentration–time curve (AUC) of glyburide by 39% and maximal concentration ( C max ) by 22%.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Elucidating Rifampin's Inducing and Inhibiting Effects on Glyburide Pharmacokinetics and Blood Glucose in Healthy Volunteers: Unmasking the Differential Effects of Enzyme Induction and Transporter Inhibition for a Drug and Its Primary Metabolite

Zheng

Huang

Frassetto

et al. 2008

Clin Pharmacol Ther

118

View full text Add to dashboard Cite

The effects of single doses of intravenous ciprofloxacin and rifampin, multiple doses of rifampin, on glyburide exposure and effect on blood glucose levels in 9 healthy volunteers were investigated. The single intravenous dose of rifampin significantly increased the AUCs of glyburide and metabolite. Blood glucose levels dropped significantly in comparison to when glyburide was dosed alone. Multiple doses of rifampin induced liver enzymes leading to a marked decrease in glyburide exposure and in blood glucose measurements. When intravenous rifampin was given after multiple doses of rifampin, the inhibition of hepatic uptake transporters masked the induction effect, however, relative changes in AUC for glyburide and its hydroxyl metabolite were the same as that seen under non-induced conditions. The studies reported here demonstrate how measurements of both the parent drug and its primary metabolite are useful in unmasking simultaneous drug-drug induction and inhibition effects and characterizing enzymatic versus transporter mechanisms.

show abstract

Section: Discussionsupporting

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Elucidating Rifampin's Inducing and Inhibiting Effects on Glyburide Pharmacokinetics and Blood Glucose in Healthy Volunteers: Unmasking the Differential Effects of Enzyme Induction and Transporter Inhibition for a Drug and Its Primary Metabolite

Zheng

Huang

Frassetto

et al. 2008

Clin Pharmacol Ther

118

View full text Add to dashboard Cite

show abstract

“…15 A study in patients and a case report indicate that rifampin may decrease the effects of glyburide. 16,17 However, the effects of rifampin on the pharmacokinetics of glyburide or glipizide have not been studied previously. The aims of this study were to confirm the interaction of rifampin with glyburide and to determine whether it has a pharmacokinetic basis, as well as to investigate whether rifampin also interacts with glipizide.…”

Section: Results: In Study I Rifampin Decreased the Area Under The Pmentioning

confidence: 99%

Effects of rifampin on the pharmacokinetics and pharmacodynamics of glyburide and glipizide

Niemi

2001

Clin Pharma and Therapeutics

113

View full text Add to dashboard Cite

Rifampin moderately decreased the plasma concentrations and effects of glyburide but had only a slight effect on glipizide. The mechanism underlying the interaction between rifampin and glyburide is probably induction of either CYP2C9 or P-glycoprotein or both. Induction of CYP2C9 would explain the increased systemic elimination of glipizide. It is probable that the blood glucose--lowering effect of glyburide is reduced during concomitant treatment with rifampin. In some patients, the effects of glipizide may also be reduced by rifampin.

show abstract

“…Glyburide is reported to cause drug interactions with numerous drugs leading to an increase or decrease in the glyburide concentration, resulting in hypoglycemia or hyperglycemia (Asplund et al, 1983;Kubacka et al, 1987;Self et al, 1989;Ahmad, 1991). Conversely, several studies have shown that glyburide inhibited coadministered drugs (Jassel, 1991;Islam et al, 1996).…”

Section: Discussionmentioning

confidence: 99%

Inhibitory Effect of Glyburide on Human Cytochrome P450 Isoforms in Human Liver Microsomes

Kim

Park²

2003

Drug Metab Dispos

View full text Add to dashboard Cite

This article is available online at http://dmd.aspetjournals.org ABSTRACT:The However, glyburide showed no appreciable inhibitory effect on CYP1A2, CYP2C8, CYP2C19, CYP2E1, or CYP2D6. In summary, glyburide showed potent inhibition on CYP2C9 and weak inhibition on CYP3A4, whereas it had minimal or no inhibitory effect on the other cytochromes P450 examined. It is anticipated that clinically significant drug-drug interactions will ensue when glyburide is coadministered with agents that are cleared primarily by the CYP2C9-mediated pathway and those with narrow therapeutic ranges.

show abstract

Interaction of Rifampin and Glyburide

Cited by 13 publications

References 8 publications

Elucidating Rifampin's Inducing and Inhibiting Effects on Glyburide Pharmacokinetics and Blood Glucose in Healthy Volunteers: Unmasking the Differential Effects of Enzyme Induction and Transporter Inhibition for a Drug and Its Primary Metabolite

Elucidating Rifampin's Inducing and Inhibiting Effects on Glyburide Pharmacokinetics and Blood Glucose in Healthy Volunteers: Unmasking the Differential Effects of Enzyme Induction and Transporter Inhibition for a Drug and Its Primary Metabolite

Effects of rifampin on the pharmacokinetics and pharmacodynamics of glyburide and glipizide

Inhibitory Effect of Glyburide on Human Cytochrome P450 Isoforms in Human Liver Microsomes

Contact Info

Product

Resources

About