Drug information of Fluconazole

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.

Pharmacodynamic

Fluconazole, a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis.

Pharmacokinetics

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 indications

fungal infections

Dosage

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 contraindications

hypersensitivity to drug or its components.

Side effects

nausea , Headache , abdominal pain , Diarrhea , taste perversion

Interactions

Ethosuximide , 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

Alerts

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.

Pregnancy level

C

Related drugs

Miconazole , Voriconazole , Ketoconazole , Climbazole , miconazol , Isavuconazonium