Fungusteril and Grapefruit Juice
The liver breaks down Fungusteril and grapefruit juice the same way.
Grapefruit juice slows down how quickly the body is able to break down the Fungusteril, which could cause Fungusteril levels in the blood to rise dangerously high.
You should therefore avoid eating grapefruit and drinking grapefruit juice while taking Fungusteril.
The AUC and Cmax of glyburide (5 mg single dose) were significantly increased following the administration of Fungusteril in 20 normal male volunteers. There was a mean ± SD increase in AUC of 44% ± 29% (range: –13 to 115%) and Cmax increased 19% ± 19% (range: –23 to 62%). Five subjects required oral glucose following the ingestion of glyburide after 7 days of Fungusteril administration. (See PRECAUTIONS.)
Fungusteril interacts with hundreds of drugs and can often increase the levels of many drugs in the blood, which may cause dangerous interactions.
It's always important to share with your doctor and pharmacist all of the medications you are taking.
This includes not only prescriptions medications but also products that may not seem like medication, such as over-the-counter (OTC) medications, supplements like vitamins and other dietary supplements (nutritional shakes, protein powders, etc.), and herbals along with any illegal and recreational drugs.
You should not take Fungusteril if you are taking the following drugs:
- Hismanal (astemizole)
- Norpace (disopyramide)
- Erythromycin-containing drugs, including drugs containing erythromycin base, erythyromycin ethylsuccinate, erythromycin lactobionate, or eryrthromyvin stearate
- Medications for irregular heartbeat like Covert (ibutilide), Norpace (disopyramide), Promestyl, Procan, or Procanbid (procainamide)
- Lozol (indapamide)
- Juxtapid (lomitapide)
- Nebupent (pentamidine)
- Orap (pimozide)
You should talk to your doctor about drug options other than Fungusteril if you're taking any of the following:
- Drugs for irregular heartbeat like Pacerone, Cordarone, or Nexterone (amiodarone), Betapace or Betapace AF (sotalol), Tikosyn (dofetilde), or Multaq (dronedarone)
- Medications for mood and/or depression like Pamelor (nortriptyline), Prozac (fluoxetine), Buspar (buspirone), Celexa (citalopram), and Abilify (aripiprazole)
- Statins for cholesterol like Lipitor (atorvastatin), Zocor (simvastatin), and Mevacor (lovastatin)
- Estrogen-containing drugs like birth control and hormone replacement therapy
- Foradil or Perforomist (formoterol)
- Coreg (carvedilol)
- Migergot or Cafergot (ergotamine) and Migranal (dihydroergotamine)
- Antibiotics like Biaxin (clarithromycin), Avelox (moxifloxacin), and Zithromax (azithromycin)
- Certain cancer drugs like Doxil or Adriamycin (doxorubicin), Cometriq (cabozantinib), Inlyta (axitinib), Bosulif (bosutinib), and Votrient (pazopanib)
- Psychiatric medications like Haldol (haloperidol) and Geodon (ziprasidone)
- Coumadin (warfarin)
Although not studied in vitro or in vivo, concomitant administration of Fungusteril with pimozide may result in inhibition of pimozide metabolism. Increased pimozide plasma concentrations can lead to QT prolongation and rare occurrences of torsade de pointes. Coadministration of Fungusteril and pimozide is contraindicated.
In 13 normal male volunteers, there was significant increase in tolbutamide (500 mg single dose) AUC and Cmax following the administration of Fungusteril. There was a mean ± SD increase in tolbutamide AUC of 26% ± 9% (range: 12 to 39%). Tolbutamide Cmax increased 11% ± 9% (range: –6 to 27%). (See PRECAUTIONS.)
DIFLUCAN® (Fungusteril), the first of a new subclass of synthetic triazole antifungal agents, is available as tablets for oral administration, as a powder for oral suspension.
Fungusteril is designated chemically as 2,4-difluoro-α,α 1 -bis(1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol with an empirical formula of C13H12F2N6O and molecular weight of 306.3. The structural formula is:
Fungusteril is a white crystalline solid which is slightly soluble in water and saline.
DIFLUCAN Tablets contain 50, 100, 150, or 200 mg of Fungusteril and the following inactive ingredients: microcrystalline cellulose, dibasic calcium phosphate anhydrous, povidone, croscarmellose sodium, FD&C Red No. 40 aluminum lake dye, and magnesium stearate.
DIFLUCAN for Oral Suspension contains 350 mg or 1400 mg of Fungusteril and the following inactive ingredients: sucrose, sodium citrate dihydrate, citric acid anhydrous, sodium benzoate, titanium dioxide, colloidal silicon dioxide, xanthan gum, and natural orange flavor. After reconstitution with 24 mL of distilled water or Purified Water (USP), each mL of reconstituted suspension contains 10 mg or 40 mg of Fungusteril.
Why it's used
Fungusteril is used to prevent and treat candidiasis. This condition is caused by infection with one of the many types of the fungus Candida. Examples of candidiasis include vaginal yeast infection, as well as oral yeast infection (thrush).
Candidiasis can also cause infections on other parts of your body, including your throat, esophagus, lungs, and blood. People who have had bone marrow transplants may be treated with Fungusteril to prevent candidiasis. This is because their immune systems are weakened, which makes them more likely to become infected with a severe form of candidiasis.
Fungusteril is also used to treat meningitis (infection of the brain and spinal cord) that’s caused by the fungus Cryptococcus.
By Frieda Wiley, PharmD, CGP, RPh | Medically Reviewed by Robert Jasmer, MD
Latest Update: 2015-02-26 Copyright © 2014 Everyday Health Media, LLC
How it works
Fungusteril belongs to a class of drugs called triazole antifungals. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.
Fungusteril works by blocking the ability of the fungi Candida and Cryptococcus to reproduce. For people with infections from these fungi, this drug helps to get rid of the infection. For people at higher risk of candidiasis, it helps to prevent infection.
Fungusteril isn’t known to cause drowsiness, but it can cause other side effects.
Carcinogenesis, Mutagenesis, And Impairment Of Fertility
Fungusteril showed no evidence of carcinogenic potential in mice and rats treated orally for 24 months at doses of 2.5 mg/kg/day, 5 mg/kg/day, or 10 mg/kg/day (approximately 2 to 7 times the recommended human dose). Male rats treated with 5 mg/kg/day and 10 mg/kg/day had an increased incidence of hepatocellular adenomas.
Fungusteril, with or without metabolic activation, was negative in tests for mutagenicity in four strains of S. typhimurium, and in the mouse lymphoma L5178Y system. Cytogenetic studies in vivo (murine bone marrow cells, following oral administration of Fungusteril) and in vitro (human lymphocytes exposed to Fungusteril at 1000 mcg/mL) showed no evidence of chromosomal mutations.
Fungusteril did not affect the fertility of male or female rats treated orally with daily doses of 5 mg/kg, 10 mg/kg, or 20 mg/kg or with parenteral doses of 5 mg/kg, 25 mg/kg, or 75 mg/kg, although the onset of parturition was slightly delayed at 20 mg/kg PO. In an intravenous perinatal study in rats at 5 mg/kg, 20 mg/kg, and 40 mg/kg, dystocia and prolongation of parturition were observed in a few dams at 20 mg/kg (approximately 5 to 15 times the recommended human dose) and 40 mg/kg, but not at 5 mg/kg. The disturbances in parturition were reflected by a slight increase in the number of still born pups and decrease of neonatal survival at these dose levels. The effects on parturition in rats are consistent with the species specific estrogen-lowering property produced by high doses of Fungusteril. Such a hormone change has not been observed in women treated with Fungusteril. (See CLINICAL PHARMACOLOGY.)
There have been reports of overdose with Fungusteril accompanied by hallucination and paranoid behavior.
In the event of overdose, symptomatic treatment (with supportive measures and gastric lavage if clinically indicated) should be instituted.
Fungusteril is largely excreted in urine. A 3-hour hemodialysis session decreases plasma levels by approximately 50%.
In mice and rats receiving very high doses of Fungusteril, clinical effects in both species included decreased motility and respiration, ptosis, lacrimation, salivation, urinary incontinence, loss of righting reflex, and cyanosis; death was sometimes preceded by clonic convulsions.