Fluconazole Stella

Fluconazole

Treatment of coccidioidomycosis; mucosal candidiasis including oropharyngeal, oesophageal, candiduria; acute or recurrent vag candidiasis when local therapy is inappropriate; candidal balanitis when local therapy is inappropriate; dermatomycosis including tinea pedis, tinea corporis, tinea cruris, tinea versicolor & dermal candida infections when systemic therapy is indicated; tinea unguium (onychomycosis) when other agents are considered inappropriate. Prevent relapse of oropharyngeal or oesophageal candidiasis in HIV-infected patients who are at high risk of experiencing relapse. Reduce the incidence of recurrent vag candidiasis (≥4 episodes/yr). Prophylaxis of candidal infections in patients w/ prolonged neutropenia (eg, patients w/ haematological malignancies receiving chemotherapy or hematopoietic stem cell transplantation).

Adult Coccidioidomycosis 200-400 mg once daily for 11-24 mth or longer depending on the patient. Consider 800 mg daily for some infections & especially for meningeal disease. Oropharyngeal/oesophageal candidiasis Loading dose: 200-400 mg on day 1. Subsequent dose: 100-200 mg once daily. Duration of treatment until remission: 7-21 days (oropharyngeal); 14-30 days (oesophageal). Longer periods in patients w/ severely compromised immune function. Candiduria 200-400 mg once daily for 7-21 days. Longer periods in patients w/ severely compromised immune function. Candidal balanitis & acute vag candidiasis 150 mg as single dose. Treatment & prophylaxis of recurrent vag candidiasis (≥4 episodes/yr) 150 mg every 3rd day for a total of 3 doses (days 1, 4, 7) followed by 150 mg once wkly maintenance dose for 6 mth. Tinea pedis, tinea corporis, tinea cruris & dermal candida infections 150 mg once wkly for 2-4 wk (up to 6 wk for tinea pedis). Tinea versicolor 300-400 mg once wkly for 1-3 wk. Tinea unguium (onychomycosis) 150 mg once wkly. Continue until infected nail is replaced (uninfected nail grows in). Prevention of relapse of oropharyngeal/oesophageal candidiasis in HIV-infected patients 100-200 mg once daily. Indefinite duration of treatment for patients w/ chronic immune suppression. Prophylaxis of candidal infections in patients w/ prolonged neutropenia 200-400 mg once daily. Start treatment several days before the anticipated onset of neutropenia & continue for 7 days after recovery from neutropenia (neutrophil count >1,000 cells/mm³). Patient w/ renal impairment receiving multiple fluconazole doses Initially 50-400 mg based on the recommended daily dose for the indication. Daily dose according to indication: CrCl >50 mL/min 100% of recommended dose. CrCl ≤50 mL/min (no haemodialysis) 50% of recommended dose. Haemodialysis 100% of recommended dose after each haemodialysis. Administer reduced dose according to CrCl on non-dialysis days.

Hypersensitivity to fluconazole or related azole substances. Co-administration of terfenadine in patients receiving fluconazole at multiple ≥400 mg daily doses. Co-administration of QT-prolonging medicinal products metabolised by CYP3A4 eg, cisapride, astemizole, pimozide, quinidine & erythromycin.

Limited evidence for efficacy in the treatment of other forms of endemic mycoses eg, paracoccidioidomycosis, lymphocutaneous sporotrichosis & histoplasmosis. Potential to cause adrenal insufficiency. Associated w/ QT interval prolongation on ECG. Administer w/ caution to patients w/ potentially proarrhythmic conditions. Rare development of exfoliative cutaneous reactions (eg, SJS & TEN) during treatment. Discontinue if rash develops in a patient treated for superficial fungal infection. Rare cases of anaphylaxis. Not recommended w/ halofantrine. Monitor patients who are concomitantly treated w/ medicinal products w/ narrow therapeutic window metabolised through CYP2C9, CYP2C19 & CYP3A4. Monitor co-administration of fluconazole at doses <400 mg daily w/ terfenadine. Rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. May impair ability to drive or operate machinery. Patients w/ renal &/or hepatic impairment. Pregnancy. Breast-feeding is not recommended after repeated use or high doses.

Headache; abdominal pain, vomiting, diarrhoea, nausea; increased ALT, AST, blood alkaline phosphatase; rash.

Increased QT prolongation w/ amiodarone. Decreased AUC & shorter t_½ w/ rifampicin. Increased plasma conc w/ hydrochlorothiazide. Increased effect of amitriptyline & nortriptyline. Prolonged prothrombin time w/ warfarin. Interaction w/ short-acting benzodiazepines (eg, midazolam, triazolam). Increased serum bilirubin & serum creatinine w/ cyclophosphamide. Significantly delayed elimination of fentanyl. Increased risk of myopathy & rhabdomyolysis w/ HMG-CoA reductase inhibitors metabolised by CYP3A4 (eg, atorvastatin, simvastatin) or CYP2C9 (eg, fluvastatin). Risk of phenytoin toxicity. Risk of adrenal cortex insufficiency when fluconazole is discontinued in patients on long-term treatment w/ fluconazole & prednisone. Prolonged serum t_½ of oral sulfonylureas (eg, chlorpropamide, glibenclamide, glipizide, tolbutamide). Decreased mean plasma clearance rate of theophylline. May increase plasma levels of vinca alkaloids (eg, vincristine, vinblastine) & lead to neurotoxicity. Risk of CNS-related undesirable effects (pseudotumour cerebri) w/ all-trans-retinoid acid (acid form of vit A). Increased plasma conc of halofantrine; ibrutinib; olaparib; sirolimus. Increased serum conc of everolimus; orally administered tacrolimus. Enhanced serum conc of methadone. Increased serum conc & AUC of rifabutin. Significantly increased conc & AUC of ciclosporin. Increased AUC of alfentanil; ethinyl estradiol & levonorgestrel. Increased C_max & AUC of celecoxib; flurbiprofen; pharmacologically active isomer [S-(+)-ibuprofen]; saquinavir; voriconazole; zidovudine. Increased exposure of ivacaftor & hydroxymethyl-ivacaftor; tofacitinib. Potential to increase systemic exposure of Ca channel antagonists (eg, nifedipine, isradipine, amlodipine, verapamil, felodipine); NSAIDs metabolised by CYP2C9 (eg, naproxen, lornoxicam, meloxicam, diclofenac). Inhibited metabolism of carbamazepine; losartan.

Antifungals

J02AC01 - fluconazole ; Belongs to the class of triazole and tetrazole derivatives. Used in the systemic treatment of mycotic infections.

P₁S₁S₃