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Drug Interactions between BuSpar and fluconazole

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Major

fluconazole busPIRone

Applies to: fluconazole and BuSpar (buspirone)

MONITOR CLOSELY: The combination of buspirone with azole agents may lead to significantly elevated buspirone plasma concentrations. In one study conducted in healthy volunteers, the average buspirone area under the plasma concentration-time curve (AUC) increased 19-fold and peak plasma concentrations increased 13-fold, after pretreatment with itraconazole. The probable mechanism is competitive inhibition of CYP450 3A4 first-pass metabolism by the azole.

MANAGEMENT: Close clinical observation is recommended if patients receiving buspirone are started on, stopped or receive a dose change of an azole agent. If buspirone is started in a patient currently receiving an azole, the clinician may wish to initiate buspirone doses conservatively. Patients should be cautioned about increased CNS side effects including dizziness, drowsiness, and impaired psychomotor performance.

References (2)
  1. Kivisto KT, Lamberg TS, Kantola T, Neuvonen PJ (1997) "Plasma buspirone concentrations are greatly increased by erythromycin and itraconazole." Clin Pharmacol Ther, 62, p. 348-54
  2. Kivisto KT, Lamberg TS, Neuvonen PJ (1999) "Interactions of buspirone with itraconazole and rifampicin: Effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of buspirone." Pharmacol Toxicol, 84, p. 94-7

Drug and food interactions

Moderate

busPIRone food

Applies to: BuSpar (buspirone)

GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of buspirone. Use in combination may result in additive central nervous system depression and/or impairment of judgment, thinking, and psychomotor skills.

ADJUST DOSING INTERVAL: In a small, randomized, crossover study, the consumption of large amounts of grapefruit juice (compared to water) was associated with significantly increased plasma buspirone concentrations, slightly prolonged elimination half-lives, and delayed times to reach peak drug concentration. The perceived pharmacodynamic effect of buspirone, as measured by subjective drowsiness and overall subjective drug effect, was also enhanced by grapefruit juice. These alterations may stem from the delay of gastric emptying as well as inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall induced by certain compounds present in grapefruits.

MANAGEMENT: Patients receiving buspirone should be advised to avoid consumption of alcohol. Patients also should preferably avoid the consumption of large amounts of grapefruits and grapefruit juice to prevent any undue fluctuations in plasma drug levels. If this is not possible, the buspirone dose should be taken at least 2 hours before or 8 hours after grapefruit or grapefruit juice. Monitoring for increased CNS depression is recommended.

References (3)
  1. (2002) "Product Information. Buspar (buspirone)." Bristol-Myers Squibb
  2. Lilja JJ, Kivisto KT, Backman JT, Lamberg TS, Neuvonen PJ (1998) "Grapefruit juice substantially increases plasma concentrations of buspirone." Clin Pharmacol Ther, 64, p. 655-60
  3. Bailey DG, Dresser GR, Kreeft JH, Munoz C, Freeman DJ, Bend JR (2000) "Grapefruit-felodipine interaction: Effect of unprocessed fruit and probable active ingredients." Clin Pharmacol Ther, 68, p. 468-77

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

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