Drug information of Fluconazole
Fluconazole is an antifungal medicine. Fluconazole is used to treat infections caused by fungus, which can invade any part of the body including the mouth, throat, esophagus, lungs, bladder, genital area, and the blood. Fluconazole is also used to prevent fungal infection in people who have a weak immune system caused by cancer treatment, bone marrow transplant, or diseases such as AIDS.
Mechanism of effect
Fluconazole is a highly selective inhibitor of fungal cytochrome P450 dependent enzyme lanosterol 14-α-demethylase. This enzyme functions to convert lanosterol to ergosterol. The subsequent loss of normal sterols correlates with the accumulation of 14-α-methyl sterols in fungi and may be responsible for the fungistatic activity of Fluconazole. Mammalian cell demethylation is much less sensitive to Fluconazole inhibition.
Fluconazole, a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis.
Absorption:90% Protein binding:11 to 12% Metabolism:Hepatic In normal volunteers, fluconazole is cleared primarily by renal excretion, with approximately 80% of the administered dose appearing in the urine as unchanged drug. Half life:30 hours (range 20-50 hours)
Drug indicationsfungal infections
Usual Adult Dose for Vaginal Candidiasis 150 mg orally as a single dose Usual Adult Dose for Oral Thrush Oropharyngeal candidiasis: 200 mg IV or orally on the first day followed by 100 mg IV or orally once a day Duration of therapy: At least 2 weeks, to reduce the risk of relapse
Drug contraindicationshypersensitivity to drug or its components.
Side effectsnausea , Headache , abdominal pain , Diarrhea , taste perversion
InteractionsEthosuximide , Adefovir , Ergotamine-C , Esomeprazole , Everolimus , Ipratropium bromide , Ifosfamide , Pantoprazole , Pimozide , Tamsulosin , Trazodone , Rabeprazole , Zolpidem , Cisapride , Cilostazol , Cyclosporine , Fluticasone propinate , Glibenclamide , Glimepiride , Lovastatin , Midazolam , Nitrazepam , Carbamazepine , Colchicine , Clobazam , Disulfiram , Bisoprolol , fentanyl , Ranolazine , fluvastatin , Ziprasidone , Ethinyl Estradiol , propoxyphene , Axitinib , nevirapine , Dolasetron , vandetanib , Droperidol , sparfloxacin , Indinavir , Mesoridazine , Procainamide , Indapamide , Dofetilide , Inotuzumab , chlorpropamide , Anagrelide , Ivacaftor , Parecoxib , Arsenic trioxide , Simeprevir , Halofantrine , Grepafloxacin , Acetohexamide , Terfenadine , Pazopanib , Ramelteon , Flibanserin , Avanafil , Entrectinib , Temsirolimus , Lorlatinib , Eliglustat , Bepridil , bedaquiline , Gefitinib , Gemtuzumab , Cannabidiol , vemurafenib , voxelotor , sitaxentan , Avapritinib , Florbetapir F18
1-Fluconazole should be administered with caution to patients with liver dysfunction. 2-Fluconazole should be discontinued in patients treated for superficial fungal infection who develop a rash that may be attributed to Fluconazole. 3-Fluconazole should be administered with caution to patients with these potentially proarrhythmic conditions. 4-Fluconazole should be administered with caution to patients with renal dysfunction
Points of recommendation
When driving vehicles or operating machines, it should be taken into account that occasionally dizziness or seizures may occur.
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