Diflucan (Fluconazole)

$ 127.03$ 320.73

Category: Antifungal
Commercial name: Diflucan
Active ingredient: Fluconazole
Production form: Pills
Available dosage: 50 mg, 200 mg

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Description

Diflucan (Fluсonazole). Dosage, Side Effects, Interactions

Diflucan (Fluсnazole) is an antifungal for systemic use and is used to treat and prevent fungal infections. The drug inhibits fungal 14-alpha-demethylase, stopping ergosterol synthesis and causing the fungus to die from the resulting membrane defects.

Diflucan (Fluсonazole) is used to treat the following fungal infections:

  • cryptococcal meningitis
  • coccidioidomycosis
  • Invasive candidiasis
  • Mucosal candidiasis, including oropharyngeal candidiasis, oesophageal candidiasis, candiduria and chronic mucocutaneous candidiasis
  • Chronic atropic oral candidiasis (denture stomatitis) when topical treatment and oral hygiene are inadequate.

For prophylaxis, fluconazole is used in:

  • Patients at high risk of recurrence of cryptococcal meningitis, oropharyngeal candidiasis, esophageal candidiasis, or candidiasis in HIV patients at high risk of recurrence.
  • Patients with prolonged neutropenia (e.g. patients with haematological tumors receiving chemotherapy or patients with haematopoietic stem cell transplantation to prevent Candida infections.

Application type

Fluconazole can be administered orally or by intravenous infusion.
The active ingredient is available on the market as a powder for suspension, hard capsules, solution for infusion and oral solution.

How Diflucan (Fluсonazole) works

Fluconazole inhibits cytochrome P450 -mediated 14-alpha-lanosterol demethylation of fungi, thereby blocking their ergosterol biosynthesis. Fluconazole is more selective for fungal cytochrome P450 enzymes than for the various mammalian cytochrome P450 enzyme systems.

Fluconazole exhibits antifungal activity in vitro against the following species:

  • C. albicans
  • C.parasilosis
  • C. tropicalis
  • C. glabrata
  • Cryptococcus neoformans
  • Cryptococcus
  • Blastomyces dermatitis
  • Coccidioides immitis
  • Histoplasma capsulatum
  • Paracoccidioides brasiliensis

Pharmacokinetics

The pharmacokinetic properties of fluconazole after intravenous or oral administration are comparable.

Absorption

Fluconazole is well absorbed after oral administration. The systemic bioavailability is more than 90 percent of the levels reached after intravenous administration. Simultaneous food intake does not affect oral absorption. Maximum plasma concentrations are reached 0.5 to 1.5 hours after dosing in the fasted state. Plasma concentrations are dose proportional.

Distribution

The volume of distribution of fluconazole corresponds to total body water. Plasma protein binding is low at 11 to 12 percent in plasma. Fluconazole is well distributed in all body fluids tested. CSF fluconazole levels are approximately 80 percent of the corresponding plasma levels.

Biotransformation

Fluconazole is a selective inhibitor of the isoenzymes CYP2C9 , CYP3A4 and CYP2C19 .

Elimination

The plasma elimination half-life of fluconazole is approximately 30 hours. The substance is mainly eliminated via the kidneys, with approximately 80 percent of the administered dose being excreted unchanged in the urine. Fluconazole clearance is proportional to creatinine clearance. Circulating metabolites have not been detected. Due to the long plasma elimination half-life, a single dose of fluconazole is sufficient for the treatment of Candida vaginosis. Once-daily or once-weekly administration for other indications is therefore also possible.

Pharmacokinetics in patients with renal impairment

In patients with severe renal insufficiency (GFR < 20 ml/min), the half-life increased from 30 to 98 hours, which is why the dose has to be reduced.

Dosage of Diflucan (Fluсonazole)

The dose depends on the type and severity of the fungal infection and can be found in the relevant product information.

Side effects of Diflucan (Fluсnazole)

The most common side effects (≥ 1/10) when taking fluconazole include:

  • headache
  • stomach pain
  • diarrhea
  • nausea
  • Vomit
  • Increase in alanine aminotransferase
  • Increase in aspartate aminotransferase
  • Increase in alkaline phosphatase
  • exanthema

Fluconazole should be used with caution in patients with hepatic impairment.

Fluconazole has been associated with rare cases of serious hepatic toxicity, including death, particularly in patients with serious underlying conditions.

Interactions

Fluconazole is a potent inhibitor of cytochrome P450 (CYP) isoenzyme 2C9 and a moderate inhibitor of CYP3A4. The isoenzyme CYP2C19 is also inhibited by fluconazole. This results in a series of interactions.

Concomitant use of the following medicines is not recommended:

  • Halofantrine ► Possible increase in halofantrine plasma concentration (due to the inhibitory effect of fluconazole on CYP3A4) ► Increased risk of cardiotoxic effects
  • Rifampicin ► 25 percent decreased AUC and 20 percent decreased half-life of fluconazole
  • Alfentanil ► Possible increase in AUC of alfentanil
  • Amitriptyline , Nortriptyline ► Fluconazole increases the effects of amitriptyline and nortriptyline
  • Anticoagulants ► In clinical trials, concomitant treatment with fluconazole and warfarin increased the prothrombin time by a factor of two. This is probably due to inhibition of CYP2C9-mediated warfarin clearance
  • Short-acting benzodiazepines , e.g. B. midazolam , triazolam ► Considerable increase in the midazolam concentration and an increase in the psychomotor effect possible. With simultaneous oral administration of fluconazole and triazolam, the AUC and half-life of triazolam increased significantly
  • Carbamazepine ► Fluconazole inhibits the metabolism of carbamazepine, so that an increase in the serum level of carbamazepine by 30 percent is possible
  • Calcium channel blockers ( nifedipine , isradipine , amlodipine , verapamil , and felodipine ) ► Fluconazole may increase the systemic exposure of calcium channel blockers because they are metabolized by CYP3A4
  • Celecoxib ► Cmax and AUC of celecoxib increase sharply
  • Cyclophosphamide ► Increase in serum levels of bilirubin and creatinine
  • Fentanyl ► Fluconazole significantly slows the elimination of fentanyl (one fatality was reported)
  • HMG-CoA reductase inhibitors that are broken down by CYP3A4 (such as atorvastatin and simvastatin ) or by CYP2C9 (such as fluvastatin ) ► risk of myopathy and rhabdomyolysis is increased
  • Immunosuppressants ( ciclosporin , everolimus , sirolimus , tacrolimus ) ► Increase in the concentration and AUC of the immunosuppressants
  • Losartan ► Conversion of losartan to its active metabolite is inhibited by fluconazole
  • Methadone ► Serum concentration of methadone can be increased
  • Non- Steroidal Anti-Inflammatory Drugs ► Fluconazole has the potential to increase the systemic exposure of NSAIDs that are metabolised by CYP2C9, e.g. naproxen , lornoxicam , meloxicam , diclofenac _
  • Phenytoin ► Fluconazole inhibits the breakdown of phenytoin in the liver
  • Prednisone ► Patients receiving long-term fluconazole and prednisone therapy should be closely monitored for signs of adrenal insufficiency
  • Rifabutin ► Fluconazole increases the serum concentration of rifabutin
  • Saquinavir ► Increase in saquinavir AUC and Cmax by approximately 50 percent
  • Sulfonylureas ( chlorpropamide , glibenclamide , glipizide , tolbutamide ) ► Increased serum half-life
  • Theophylline ► Reduced plasma clearance rate of theophylline
  • Vinca alkaloids (e.g. vincristine and vinblastine ) ► Plasma levels of vinca alkaloids may be increased
  • Vitamin A ► CNS-related undesirable effects possible
  • Voriconazole (CYP2C9 and CYP3A4 inhibitor) ► Increase in Cmax and AUCτ of voriconazole
  • Zidovudine ► Increase in Cmax and AUC of zidovudine by 84 percent and 74 percent, respectively

Contraindications

The following contraindications exist for the use of fluconazole:

  • Hypersensitivity to the active substance and other azole derivatives
  • Terfenadine in patients repeatedly receiving fluconazole at doses of 400 mg per day or more
  • QT interval prolonging drugs
  • Cytochrome P450 isoenzyme (CYP) 3A4 substrates such as cisapride , astemizole , pimozide , quinidine and erythromycin , as fluconazole is a potent CYP2C9 inhibitor and a moderate CYP3A4 inhibitor

Pregnancy

Data from several hundred pregnant women treated with standard doses (less than 200 mg/day) of single or multiple doses of fluconazole during the first trimester have revealed no adverse effects on the fetus. However, there have been reports of multiple congenital anomalies (including brachycephaly, ear dysplasia, enlarged anterior fontanelle, femoral curvature, and humeroradial synostosis) in infants whose mothers have been treated with high doses (400-800 mg/day) of fluconazole for 3 months or more. were treated for coccidioidomycosis. The relationship between these findings and the use of fluconazole is unclear.

Animal studies have also shown reproductive toxicity.

Fluconazole in standard doses and as short-term treatment should not be used during pregnancy unless clearly necessary. Fluconazole in high doses and/or in long-term regimens should not be used during pregnancy unless life-threatening infections are present.

Lactation

Fluconazole is excreted in breast milk, where it reaches concentrations lower than those in plasma. Breastfeeding can continue with a single dose of fluconazole at a standard dose of 200 mg or less. Breast-feeding is not recommended after repeated use or after high doses of fluconazole.

driving ability

Patients must be advised of the possibility of dizziness and convulsions when using fluconazole. If these symptoms occur, do not drive or use machines.

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Additional information

Dosage

50 mg, 200 mg

Quantity

30, 60, 90, 120, 180

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