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Fluconazole information from DrugsUpdate  

See Available Brands of Fluconazole in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Fluconazole is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections. In a bulk powder form, it appears as a white crystalline powder, and it is very slightly soluble in water and soluble in alcohol. It is commonly marketed under the trade name Diflucan or Trican (Pfizer).

Pharmacodynamics

Pharmacokinetics

Fluconazole decreases ergosterol synthesis by interfering with cytochrome P450 activity, thus inhibiting cell membrane formation of susceptible fungi including B dermatitidis, Candida spp, C immitis, C neoformans, Epidermophyton spp, H capsulatum, Mycosporum spp, Trichophyton spp, thus leading to cell death.

Absorption
Well absorbed after oral admin; peak plasma concentrations after 1-2 hr (oral), may be increased with multiple dosing.

Distribution
Widely distributed. Protein-binding: 12%.

Excretion
Via urine (80% as unchanged, 11% as metabolites); 30 hr (elimination half-life); increased in renal impairment. Removed by dialysis.

Fluconazole Indications / Fluconazole Uses

Information Not Available

Fluconazole Adverse Reactions / Fluconazole Side Effects

Nausea, abdominal pain, vomiting, diarrhoea, flatulence; elevated liver function values; headache; rash, exfoliative dermatitis. Rarely, angioedema, anaphylactic reactions and thrombocytopenia.

Potentially Fatal: Hepatotoxicity; rarely anaphylaxis; Stevens-Johnson syndrome.

Precautions

Some azoles, including Fluconazole, have been associated with prolongation of the QT interval on the electrocardiogram. During postmarketing surveillance, there have been rare cases of QT prolongation and torsade de pointes in patients taking Fluconazole. Most of these reports involved seriously ill patients with multiple confounding risk factors, such as structural heart disease, electrolyte abnormalities and concomitant medications that may have been contributory.

Fluconazole should be administered with caution to patients with these potentially proarrhythmic conditions.

Special Precautions

Renal or hepatic impairment. May prolong QT interval. Pregnancy, lactation.

Other Drug Interactions

Rifampicin reduces fluconazole levels. Reduces theophylline clearance. Affects efficacy of oral contraceptives. May increase serum levels of alprazolam, triazolam, midazolam, diazepam. May raise serum concentrations and efficacy of oral sulphonylureas, phenytoin, ciclosporin, calcium channel blockers, tacrolimus, HMG-CoA reductase inhibitors (except pravastain and fluvastatin), warfarin and other anticoagulants. May reduce metabolism of caffeine. Avoid concurrent use with clopidogrel.

Potentially Fatal: Increased risk of cardiac arrhythmias with astemizole, cisapiride or terfenadine.

Other Interactions

Information Not Available

Dosage

Oral
Superficial Mucosal Candidiasis
Adult: (Except genital candidiasis) Usual dose: 50 mg daily, may increase to 100 mg daily if needed. Recommended treatment duration: 7-14 days (oropharyngeal candidiasis, except in severely immunocompromised patients), 14 days (atrophic oral candidiasis associated with dentures), 14-30 days (other mucosal candidiasis including oesophagitis).
Child: >4 weeks: Loading dose: 6 mg/kg followed by 3 mg/kg daily.



Renal impairment: Normal initial doses; adjust subsequent doses based on CrCl. Patients on dialysis: Single recommended dose after each session.


CrCl (ml/min)                                Dosage Recommendation
<50 and not receiving dialysis    Maintenance dose: 50% of the recommended doses.

Oral
Candidal balanitis
Adult: 150 mg as a single dose.

Oral
Vaginal candidiasis

Adult: 150 mg as a single dose.

Oral
Dermatophytosis

Adult: 50 mg daily for up to 6 weeks.


Renal impairment: Normal initial doses; adjust subsequent doses based on CrCl. Patients on dialysis: Single recommended dose after each session.



CrCl (ml/min)                               Dosage Recommendation
<50 and not receiving dialysis    Maintenance dose: 50% of the recommended doses.

Oral
Pityriasis Versicolor

Adult: 50 mg daily for up to 6 wk.


Renal impairment: Normal initial doses; adjust subsequent doses based on CrCl. Patients on dialysis: Single recommended dose after each session.


CrCl (ml/min)                               Dosage Recommendation
<50 and not receiving dialysis    Maintenance dose: 50% of the recommended doses.

Oral
Cutaneous Candidiasis

Adult: 50 mg daily for up to 6 weeks.


Renal impairment: Normal initial doses; adjust subsequent doses based on CrCl. Patients on dialysis: Single recommended dose after each session.


CrCl (ml/min)  Dosage Recommendation
<50 and not receiving dialysis    Maintenance dose: 50% of the recommended doses.

Oral
Systemic Candidiasis

Adult: Initially, 400 mg followed by 200-400 mg daily. Max: 800 mg daily in severe infections. Treatment duration is based on clinical and mycological response but is usually at least 6-8 wk in cryptococcal meningitis. May also be given via IV infusion. To prevent relapse after a primary course of treatment for acute cryptococcal meningitis in AIDS patients: 100-200 mg daily, may also be given via IV admin.


Child: >4 wk: 6-12 mg/kg daily; same doses may given every 72 hr in neonates up to 2 wk and every 48 hr in neonates 2-4 wk. Max: 400 mg daily.


Renal impairment: Normal initial doses; adjust subsequent doses based on CrCl. Patients on dialysis: Single recommended dose after each session.


CrCl (ml/min)                           Dosage Recommendation
<50 and not receiving dialysis    Maintenance dose: 50% of the recommended doses.

Oral
Cryptococcal Infections

Adult: Initially, 400 mg followed by 200-400 mg daily. Max: 800 mg daily in severe infections. Treatment duration is based on clinical and mycological response but is usually at least 6-8 weeks in cryptococcal meningitis. May also be given via IV infusion. To prevent relapse after a primary course of treatment for acute cryptococcal meningitis in AIDS patients: 100-200 mg daily, may also be given via IV admin.
Child: >4 wk: 6-12 mg/kg daily; same doses may given every 72 hr in neonates up to 2 wk and every 48 hr in neonates 2-4 wk. Max: 400 mg daily.


Renal impairment: Normal initial doses; adjust subsequent doses based on CrCl. Patients on dialysis: Single recommended dose after each session.


CrCl (ml/min)                           Dosage Recommendation
<50 and not receiving dialysis    Maintenance dose: 50% of the recommended doses.

Oral
Prophylaxis of fungal infections in immunocompromised patients

Adult: 50-400 mg daily. May also be given via IV infusion.
Child: 3-12 mg/kg daily; may also be given via IV infusion. For infants <2 wk, doses should be given every 72 hr; 2-4 wk, doses should be given every 48 hr. Max: 400 mg daily, or 12 mg/kg at recommended intervals in infants.


Renal impairment: Normal initial doses; adjust subsequent doses based on CrCl. Patients on dialysis: Single recommended dose after each session.


CrCl (ml/min)                               Dosage Recommendation
<50 and not receiving dialysis    Maintenance dose: 50% of the recommended doses.

Food(before/after)

May be taken with or without food.

List of Contraindications

Fluconazole and Pregnancy

Caution when used during pregnancy.


Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Fluconazole and Lactation

Caution when used during lactation

Fluconazole and Children

An open-label, randomized, controlled trial has shown fluconazole to be effective in children 6 mo to 13 years of age. Efficacy has not been established in infants younger than 6 months of age.

Fluconazole and Geriatic

Information Not Available

Fluconazole and Other Contraindications

Hypersensitivity

Storage

Oral
Store below 30°C.

Lab interference

Oral
Store below 30°C.

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