Fluconazole

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Generic Name of Fluconazole - Learn More

Fluconazole

Fluconazole Precaution - What You Need to Know

Fluconazole is an antifungal medication used to treat a variety of fungal infections, including candidiasis, cryptococcal meningitis, and other systemic fungal infections. When prescribing fluconazole, special care should be taken in patients with a history of liver disease, as fluconazole is metabolized by the liver and may cause hepatic toxicity. Liver function should be monitored regularly, especially during long-term use or in patients with pre-existing liver conditions. The drug should be used with caution in patients with renal impairment as it is excreted unchanged by the kidneys, and dose adjustments may be necessary. Fluconazole may also cause QT interval prolongation, increasing the risk of serious arrhythmias, particularly in patients with existing heart conditions, electrolyte imbalances, or those on medications that also prolong the QT interval. Pregnant women, especially during the first trimester, should avoid fluconazole unless deemed absolutely necessary, as the drug can cause harm to the fetus, such as congenital abnormalities in higher doses. Fluconazole is generally considered safe for use in breastfeeding mothers, but it should still be used with caution as it passes into breast milk. Patients should also be informed about potential drug interactions, as fluconazole can interact with a wide range of medications, affecting their efficacy or increasing the risk of adverse effects. Regular follow-up and monitoring for side effects are essential, especially when used for prolonged periods.

Fluconazole Indication - Uses and Benefits

Fluconazole is primarily used to treat and prevent fungal infections caused by susceptible organisms. Its most common indications include the treatment of vaginal, esophageal, and systemic candidiasis, cryptococcal meningitis, and dermatophyte infections. It is particularly effective against Candida species and has a broad spectrum of activity against many types of fungi. Fluconazole is also used for the treatment of fungal infections in immunocompromised patients, such as those with HIV/AIDS or those undergoing chemotherapy, as it helps prevent opportunistic fungal infections. It is sometimes used as a prophylactic treatment in these high-risk populations to prevent fungal infections. Fluconazole is also indicated for onychomycosis (fungal nail infections) and for the treatment of tinea infections. In some cases, it may be prescribed off-label for fungal infections in non-immunocompromised patients or for less common fungal pathogens. The drug is particularly advantageous due to its high oral bioavailability, which makes it suitable for both oral and intravenous administration, and its long half-life, which allows for once-daily dosing in most cases.

Fluconazole Contraindications - Important Warnings

Fluconazole should be avoided in patients with a known hypersensitivity or allergy to fluconazole or other azole antifungal agents, as severe allergic reactions, including anaphylaxis, may occur. It is contraindicated in patients with a history of liver disease or severe hepatic impairment due to the potential for drug-induced liver toxicity. Fluconazole should also be avoided in patients who are taking certain medications that can lead to serious drug interactions. Specifically, it should not be used in combination with drugs that prolong the QT interval, such as terfenadine, astemizole, or cisapride, as this may increase the risk of fatal arrhythmias. In pregnant women, fluconazole is contraindicated in doses greater than 400 mg per day due to potential teratogenic effects. The drug should be used with caution during pregnancy, especially in the first trimester, and only when the benefits outweigh the potential risks. Additionally, fluconazole should not be used in combination with certain statins or anticoagulants due to the potential for dangerous drug interactions. In pediatric patients, fluconazole should be used cautiously, especially in those under 6 months of age, as the safety and efficacy in this population are not well-established for all indications.

Fluconazole Side Effects - What to Expect

Fluconazole is generally well-tolerated, but some side effects can occur. Common and mild side effects include headache, nausea, abdominal pain, and diarrhea. These symptoms usually resolve on their own and are more likely with oral administration. Liver enzyme elevations (such as ALT or AST) are a common side effect, especially in long-term use, and may indicate liver damage. In rare cases, more severe liver toxicity, including hepatitis and jaundice, can occur, particularly in patients with pre-existing liver conditions. Skin reactions, including rash and pruritus, are possible and usually mild; however, serious reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis, though rare, can occur. Fluconazole has been associated with QT interval prolongation, which can lead to arrhythmias, particularly in patients with existing heart conditions. Gastrointestinal side effects, such as nausea, vomiting, and flatulence, are more common with high doses of fluconazole, especially when taken for prolonged periods. In rare instances, fluconazole may cause a severe allergic reaction, including anaphylaxis, which requires immediate discontinuation of the drug and emergency medical care. Other side effects include dizziness, fatigue, and changes in taste. Long-term use can also increase the risk of fungal resistance, and there have been reports of patients developing secondary fungal infections, including invasive candidiasis, while on treatment.

Fluconazole Pregnancy Category ID - Safety Information

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Fluconazole Mode of Action - How It Works

Fluconazole is a triazole antifungal agent that works by inhibiting the synthesis of ergosterol, an essential component of the fungal cell membrane. Ergosterol is necessary for maintaining the integrity and function of the cell membrane, and by inhibiting its synthesis, fluconazole compromises the membrane’s structure, leading to cell death. The drug selectively inhibits fungal cytochrome P450 enzymes, particularly 14α-demethylase, which is involved in converting lanosterol to ergosterol. This inhibition results in the accumulation of toxic sterol precursors and a reduction in ergosterol, weakening the fungal cell membrane and making the fungus more susceptible to osmotic stress and other damaging factors. Fluconazole has a broad spectrum of activity against various fungal pathogens, including Candida species, Cryptococcus neoformans, and dermatophytes. Unlike other antifungal agents, fluconazole has high oral bioavailability and can be effectively used in both oral and intravenous forms, providing convenient treatment options. It also has a relatively long half-life, allowing for once-daily dosing in most cases, which improves patient compliance.

Fluconazole Drug Interactions - What to Avoid

Fluconazole is known to interact with a wide range of drugs, which can either increase the risk of side effects or reduce the effectiveness of either drug. One of the most significant interactions is with warfarin, an anticoagulant. Fluconazole can enhance the effects of warfarin, increasing the risk of bleeding, so monitoring of the international normalized ratio (INR) is essential during concurrent use. The drug also interacts with certain anticonvulsants like phenytoin and carbamazepine, as fluconazole can increase their serum levels, potentially leading to toxicity. Additionally, fluconazole can increase the blood concentration of certain statins (e.g., atorvastatin, simvastatin), raising the risk of muscle-related side effects, such as myopathy or rhabdomyolysis. When taken with drugs that also prolong the QT interval (e.g., quinine, certain antiarrhythmics), fluconazole may enhance this effect, increasing the risk of arrhythmias. Concomitant use with drugs that are metabolized by the liver, such as certain benzodiazepines (e.g., midazolam, triazolam), can increase their plasma concentrations, leading to sedation or respiratory depression. Fluconazole may also reduce the effectiveness of oral contraceptives, and additional contraceptive methods may be recommended during treatment. Alcohol should be avoided during treatment with fluconazole, as it can exacerbate the risk of liver toxicity and may also increase the occurrence of side effects such as gastrointestinal upset.

Fluconazole Adult Dose - Recommended Dosage

For adults, the typical dosage of fluconazole depends on the type and severity of the infection being treated. For vaginal candidiasis, a single 150 mg dose is usually sufficient. For oropharyngeal or esophageal candidiasis, the typical dose is 200 mg on the first day, followed by 100 mg daily for at least 2 weeks. In more severe systemic infections like cryptococcal meningitis, the recommended dose is 400 mg daily, with the dose typically reduced to 200 mg after the initial phase of treatment. For other fungal infections, such as onychomycosis or candidemia, the usual dose is 150-200 mg daily. Fluconazole is usually administered orally, but intravenous (IV) therapy is also an option for more severe cases or when the oral route is not possible. The duration of treatment varies depending on the infection being treated but can range from a few days to several months for chronic or recurrent infections. For fungal prophylaxis, particularly in immunocompromised patients, the typical dose is 200 mg daily.

Fluconazole Child Dose - Dosage for Children

The pediatric dose of fluconazole depends on the age, weight, and type of infection being treated. For infants and children, the typical dose for most fungal infections is 3 to 12 mg/kg per day, depending on the severity and type of infection. For systemic infections like cryptococcal meningitis, higher doses of up to 12 mg/kg per day may be used. For candidiasis, the usual dose is 6 mg/kg on the first day, followed by 3 mg/kg daily for the duration of treatment. For pediatric patients under 6 months of age, the dosing should be carefully adjusted, and the safety and efficacy of fluconazole in this age group should be considered. Fluconazole is available in liquid form, which makes it easier for children to take, and it should be dosed based on body weight to ensure appropriate drug levels.

Fluconazole Renal Dose - Dosage for Kidney Conditions

Fluconazole is primarily excreted unchanged in the urine, so dose adjustments are necessary in patients with renal impairment. For patients with mild to moderate renal impairment (creatinine clearance >50 mL/min), the standard dose can usually be maintained. In patients with severe renal impairment (creatinine clearance <50 mL/min), the dose of fluconazole should be reduced. The typical adjustment is to reduce the dose by 50% or increase the dosing interval to every 72 hours, depending on the severity of the renal impairment. For patients undergoing hemodialysis, an additional dose may be required after dialysis, as fluconazole is removed by the dialysis process. Renal function should be closely monitored during treatment, especially in patients with pre-existing renal conditions.