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Fluconazole Injection and Yosprala

Determining the interaction of Fluconazole Injection and Yosprala and the possibility of their joint administration.

Check result:
Fluconazole Injection <> Yosprala
Relevance: 12.07.2022 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:

Fluconazole can increase the blood levels of omeprazole. This may increase side effects such as diarrhea, abdominal pain, nausea, vomiting, and flatulence. During long-term treatment, you may also have an increased risk of developing osteoporosis, bone fractures, and a condition called hypomagnesemia (low blood magnesium), which in severe cases can lead to muscle spasm, irregular heart rhythm, and seizures. Talk to your doctor if you have any questions or concerns. Your doctor may be able to prescribe alternatives that do not interact, or you may need a dose adjustment or more frequent monitoring by your doctor 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:

ADJUST DOSE: Coadministration with fluconazole may significantly increase the plasma concentrations of omeprazole and other proton pump inhibitors (PPIs). The proposed mechanism is fluconazole inhibition of PPI metabolism via CYP450 2C19 and 3A4. In 18 healthy volunteers, administration of a single 20 mg oral dose of omeprazole on day 5 of multiple once daily dosing of fluconazole 100 mg resulted in approximately 2.4- and 6.3-fold increases in omeprazole peak plasma concentration (Cmax) and systemic exposure (AUC), respectively, compared to administration of omeprazole alone. Terminal half-life of omeprazole was increased from 0.85 hour to 2.59 hours by fluconazole. Since all PPIs are metabolized by CYP450 2C19 and 3A4, a similar interaction with fluconazole should be expected. Omeprazole does not appear to affect the gastrointestinal absorption of fluconazole like it does some other azole antifungal agents. In a study of 12 healthy volunteers, omeprazole 20 mg/day for 7 days increased median gastric pH from 1.1 to 4.7, but had no effect on the Cmax or AUC of a single 100 mg oral dose of fluconazole. The median bioavailability ratio of fluconazole before and after omeprazole treatment was 1.00.

MANAGEMENT: According to the manufacturers, dosage adjustment of omeprazole is not normally required when used with dual inhibitors of CYP450 2C19 and 3A4 such as fluconazole. However, it may be necessary in patients receiving higher dosages, such as those with Zollinger-Ellison syndrome. Patients should be monitored for potentially increased adverse effects of PPIs during coadministration with fluconazole. The same precaution may be applicable to other PPIs.

References
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  • "Product Information. Protonix (pantoprazole)" Wyeth-Ayerst Laboratories, Philadelphia, PA.
  • "Product Information. Dexilant (dexlansoprazole)." Takeda Pharmaceuticals America, Lincolnshire, IL.
  • "Product Information. Nexium (esomeprazole)" Astra-Zeneca Pharmaceuticals, Wilmington, DE.
  • "Product Information. Prilosec (omeprazole)." Merck & Co, Inc, West Point, PA.
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  • Lu C, Berg C, Prakash SR, Lee FW, Balani SK "Prediction of pharmacokinetic drug-drug interactions using human hepatocyte suspension in plasma and cytochrome P450 phenotypic data. III. In vitro-in vivo correlation with fluconazole." Drug Metab Dispos 36 (2008): 1261-6
  • Zimmermann T, Yeates RA, Riedel KD, Lach P, Laufen H "The influence of gastric ph on the pharmacokinetics of fluconazole: the effect of omeprazole." Int J Clin Pharmacol Ther 32 (1994): 491-6
  • Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  • "Product Information. Prevacid (lansoprazole)." TAP Pharmaceuticals Inc, Deerfield, IL.
Fluconazole Injection

Generic Name: fluconazole

Brand name: Diflucan

Synonyms: Fluconazole

Yosprala

Generic Name: aspirin / omeprazole

Brand name: Yosprala

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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