Fluconazole


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Oropharyngeal candidiasis Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 7-21 days (until disease is in remission). Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week. Oesophageal candidiasis Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 14-30 days (until disease is in remission). Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week. Candiduria 200-400 mg once daily for 7-21 days. Chronic atrophic candidiasis 50 mg once daily for 14 days. Chronic mucocutaneous candidiasis 50-100 mg once daily for up to 28 days. Candidal balanitis; Vaginal candidiasis 150 mg given as a single dose. Treatment and prophylaxis of recurrent vaginal candidiasis (4 or more episodes a year): 150 mg every third day for a total of 3 doses (Day 1, 4, and 7), followed by a 150 mg once weekly maintenance dose (6 months). Dermatophytosis Tinea pedis, Tinea corporis, Tinea cruris, Candida infections: 150 mg once a week, or 50 mg once daily. Tinea versicolor: 300-400 mg once a week for 1-3 weeks, or 50 mg once daily for 2-4 weeks. Invasive candidiasis Initially, 800 mg on Day 1, followed by 400 mg once daily for 2 weeks. Cryptococcal meningitis Initially, 400 mg on Day 1, followed by 200-400 mg once daily, for at least 6-8 weeks. Prevention of relapse in patients with high risk of recurrence: 200 mg once daily. Coccidioidomycosis 200-400mg once daily for 11-24 months, or longer depending on severity of infection, clinical or mycologic response. Prophylaxis of fungal infections in immunocompromised patients In patients with prolonged neutropenia: 200-400 mg once daily. IV Oropharyngeal candidiasis Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 7-21 days (until disease is in remission). Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week. Oesophageal candidiasis Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 14-30 days (until disease is in remission). Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week. Candiduria 200-400 mg once daily for 7-21 days. Chronic atrophic candidiasis 50 mg once daily for 14 days. Chronic mucocutaneous candidiasis 50-100 mg once daily for up to 28 days. Invasive candidiasis Initially, 800 mg on Day 1, followed by 400 mg once daily for 2 weeks. Cryptococcal meningitis Initially, 400 mg on Day 1, followed by 200-400 mg once daily, for at least 6-8 weeks. Prevention of relapse of cryptococcal meningitis in patients with high risk of recurrence: 200 mg once daily. Coccidioidomycosis 200-400mg once daily for 11-24 months, or longer depending on severity of infection, clinical or mycologic response. Prophylaxis of fungal infections in immunocompromised patients 200-400 mg once daily.
Dosage Details
Intravenous
Oropharyngeal candidiasis
Adult: Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 7-21 days (until disease is in remission). Longer periods may be used in patients with severely compromised immune function. Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week. Infusion rate: 10 mL/min.
Child: 0-14 days Initially, 6 mg/kg, followed by 3 mg/kg every 72 hours. Max: 12 mg/kg 72 hourly. 15-27 days Initially, 6 mg/kg, followed by 3 mg/kg every 48 hours. Max: 12 mg/kg 48 hourly. 28 days-11 years Initially, 6 mg/kg, followed by 3 mg/kg once daily. Infusion rate: 10 mL/min.

Intravenous
Oesophageal candidiasis
Adult: Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 14-30 days (until disease is in remission). Longer periods may be used in patients with severely compromised immune function. Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week. Infusion rate: 10 mL/min.
Child: 0-14 days Initially, 6 mg/kg, followed by 3 mg/kg every 72 hours. Max: 12 mg/kg 72 hourly. 15-27 days Initially, 6 mg/kg, followed by 3 mg/kg every 48 hours. Max: 12 mg/kg 48 hourly. 28 days-11 years Initially, 6 mg/kg, followed by 3 mg/kg once daily. Infusion rate: 10 mL/min.

Intravenous
Coccidioidomycosis
Adult: 200-400mg once daily for 11-24 months, or longer depending on severity of infection, clinical or mycologic response. 800 mg may be considered for meningeal disease or some infections. Infusion rate: 10 mL/min.

Intravenous
Invasive candidiasis
Adult: Initially, 800 mg on Day 1, followed by 400 mg once daily for 2 weeks. Infusion rate: 10 mL/min.
Child: ≥4 weeks-11 years 6-12 mg/kg once daily. Infusion rate: 10 mL/min.

Intravenous
Cryptococcal meningitis
Adult: Initially, 400 mg on Day 1, followed by 200-400 mg once daily, for at least 6-8 weeks. Treatment durations are based on severity of infection, clinical and mycologic response. Prevention of relapse in patients with high risk of recurrence: 200 mg once daily. Infusion rate: 10 mL/min.
Child: ≥4 weeks-11 years Treatment: 6-12 mg/kg once daily. Prevention of relapse in patients with high risk of recurrence: As maintenance therapy, 6 mg/kg once daily. Infusion rate: 10 mL/min.

Intravenous
Chronic atrophic candidiasis
Adult: 50 mg once daily for 14 days. Infusion rate: 10 mL/min.

Intravenous
Candiduria
Adult: 200-400 mg once daily for 7-21 days. Longer periods may be used in patients with severely compromised immune function. Infusion rate: 10 mL/min.

Intravenous
Chronic mucocutaneous candidiasis
Adult: 50-100 mg once daily for up to 28 days. Longer periods depending on both the severity of infection or underlying compromised immune function and infection. Infusion rate: 10 mL/min.

Intravenous
Prophylaxis of fungal infections in immunocompromised patients
Adult: 200-400 mg once daily. Start treatment before anticipated onset of neutropenia and continue for 7 days after neutrophil count is within desirable range. Infusion rate: 10 mL/min.
Child: ≥4 weeks-11 years 3-12 mg/kg once daily. Infusion rate: 10 mL/min.

Oral
Oropharyngeal candidiasis
Adult: Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 7-21 days (until disease is in remission). Longer periods may be used in patients with severely compromised immune function. Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week.
Child: 0-14 days Initially, 6 mg/kg, followed by 3 mg/kg every 72 hours. Max: 12 mg/kg 72 hourly. 15-27 days Initially, 6 mg/kg, followed by 3 mg/kg every 48 hours. Max: 12 mg/kg 48 hourly. 28 days-11 years Initially, 6 mg/kg, followed by 3 mg/kg once daily.

Oral
Oesophageal candidiasis
Adult: Treatment: Initially, 200-400 mg on Day 1, followed by 100-200 mg once daily for 14-30 days (until disease is in remission). Longer periods may be used in patients with severely compromised immune function. Prevention of relapse in patients with HIV: 100-200 mg once daily, or 200 mg 3 times a week.
Child: 0-14 days Initially, 6 mg/kg, followed by 3 mg/kg every 72 hours. Max: 12 mg/kg 72 hourly. 15-27 days Initially, 6 mg/kg, followed by 3 mg/kg every 48 hours. Max: 12 mg/kg 48 hourly. 28 days-11 years Initially, 6 mg/kg, followed by 3 mg/kg once daily.

Oral
Candiduria
Adult: 200-400 mg once daily for 7-21 days. Longer periods may be used in patients with severely compromised immune function.

Oral
Chronic mucocutaneous candidiasis
Adult: 50-100 mg once daily for up to 28 days. Longer periods depending on both the severity of infection or underlying compromised immune function and infection.

Oral
Chronic atrophic candidiasis
Adult: 50 mg once daily for 14 days.

Oral
Dermatophytosis
Adult: Tinea pedis, Tinea corporis, Tinea cruris, Candida infections: 150 mg once a week, or 50 mg once daily. Tinea unguium (onychomycosis): 150 mg once weekly. Treatment durations are based on severity of infection, clinical or mycologic response. Tinea versicolor: 300-400 mg once a week for 1-3 weeks, or 50 mg once daily for 2-4 weeks.

Oral
Candidal balanitis, Vaginal candidiasis
Adult: 150 mg given as a single dose. Treatment and prophylaxis of recurrent vaginal candidiasis (4 or more episodes a year): 150 mg every third day for a total of 3 doses (Day 1, 4, and 7), followed by a 150 mg once weekly maintenance dose (6 months).

Oral
Coccidioidomycosis
Adult: 200-400 mg once daily for 11-24 months, or longer depending on severity of infection, clinical or mycologic response. 800 mg may be considered for meningeal disease or some infections.

Oral
Prophylaxis of fungal infections in immunocompromised patients
Adult: In patients with prolonged neutropenia: 200-400 mg once daily. Start treatment before anticipated onset of neutropenia and continue for 7 days after neutrophil count is within desirable range.
Child: ≥4 weeks-11 years 3-12 mg/kg once daily.

Oral
Cryptococcal meningitis
Adult: Initially, 400 mg on Day 1, followed by 200-400 mg once daily, for at least 6-8 weeks. Treatment durations are based on severity of infection, clinical and mycologic response. Prevention of relapse in patients with high risk of recurrence: 200 mg once daily.
Child: ≥4 weeks-11 years Treatment: 6-12 mg/kg once daily. Prevention of relapse in patients with high risk of recurrence: As maintenance therapy, 6 mg/kg once daily.

Oral
Invasive candidiasis
Adult: Initially, 800 mg on Day 1, followed by 400 mg once daily for 2 weeks.
Child: ≥4 weeks-11 years 6-12 mg/kg once daily.
Renal Impairment
Haemodialysis patient: Usual daily dose given after each session.
CrCl (mL/min) Dosage
>50 Usual daily dose.
≤50 and not undergoing haemodialysis Reduce total daily dose by 50%.
Administration
May be taken with or without food.
Reconstitution
Powder for oral susp: Add 24 mL of distilled or purified water to a container labelled as 0.35 g or 1.4 g of fluconazole to make a suspension containing 50 mg/5 mL or 200 mg/5 mL respectively. Shake well before use.
Contraindications
Hypersensitivity. Concomitant use with astemizole, cisapride, quinidine, terfenadine, pimozide, erythromycin.
Special Precautions
Patient with potentially proarrhythmic conditions (e.g. hypokalaemia, electrolyte abnormality, advanced cardiac failure), serious underlying disease (e.g. AIDS, malignancy). Renal and hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: QT interval prolongation. Rarely, anaphylaxis.
Blood and lymphatic system disorders: Agranulocytosis, anaemia, leucopenia, thrombocytopenia, neutropenia.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, flatulence, dyspepsia, constipation, dry mouth.
General disorders and admin site conditions: Fatigue, malaise, asthenia, fever.
Immune system disorders: Angioedema, urticaria.
Metabolism and nutrition disorders: Hypercholesteremia, hypertriglyceridaemia, hyperlipidaemia, hypokalaemia, anorexia.
Musculoskeletal and connective tissue disorders: Myalgia.
Nervous system disorders: Headache, dizziness, dysgeusia, paraesthesia, tremor, vertigo.
Psychiatric disorders: Insomnia, somnolence.
Skin and subcutaneous tissue disorders: Rash, pruritus, increased sweating, alopecia.
Potentially Fatal: Hepatic toxicity (e.g. cholestasis, hepatocellular damage, hepatitis, fulminant hepatic failure), ventricular arrhythmia, torsade de pointes. Rarely, Stevens-Johnson syndrome, toxic epidermal necrolysis.
PO: C (For a single dose of 150 mg for vaginal candidiasis), D (for use in indications other than vag candidiasis); Parenteral: D
Patient Counseling Information
This drug may cause dizziness or seizures, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor LFTs, renal function tests and serum K levels periodically.
Overdosage
Symptoms: Hallucination and paranoid behaviour. Management: Symptomatic and supportive treatment. May consider performing gastric lavage if necessary. Haemodialysis may decrease plasma levels by approx 50%.
Drug Interactions
May increase prothrombin time with anticoagulants (e.g. warfarin). May increase serum concentrations of drugs metabolised by CYP3A4 and CYP2C9 isoenzymes (e.g. bosentan, ciclosporin, midazolam, nevirapine, amitriptyline, nortriptyline, phenytoin, rifabutin, sulfonylurea, nateglinide, celecoxib, parecoxib, tacrolimus, triazolam, zidovudine). May increase risk of myopathy and rhabdomyolysis with HMG-CoA reductase inhibitors (e.g. simvastatin, atorvastatin). May decrease plasma clearance of theophylline. May reduce plasma concentration with rifampicin.
Potentially Fatal: Increases the risk of cardiac arrhythmia with drugs known to prolong QT interval or induce torsade de pointes such as astemizole, cisapride, terfenadine, quinidine, pimozide, erythromycin. Increased risk of respiratory depression with fentanyl.
Action
Description: Fluconazole, a triazole derivative antifungal agent, inhibits the fungal CYP450 mediated 14 α-lanesterol demethylation, thereby decreasing ergosterol biosynthesis and inhibiting fungal cell membrane formation.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Bioavailability: ≥90% (oral). Time to peak plasma concentration: Approx 1-2 hours (oral).
Distribution: Widely distributed into body tissues and fluids. Enters breast milk. Volume of distribution: Approx 0.6 L/kg. Plasma protein binding: Approx 11-12%.
Metabolism: Metabolised only to a minor extent.
Excretion: Mainly via urine (approx 80% as unchanged drug, approx 11% as metabolites). Elimination half-life: Approx 30 hours.
Chemical Structure

Chemical Structure Image
Fluconazole

Source: National Center for Biotechnology Information. PubChem Database. Fluconazole, CID=3365, https://pubchem.ncbi.nlm.nih.gov/compound/Fluconazole (accessed on Jan. 21, 2020)

Storage
Tab, cap, powder for oral susp: Store below 30°C. IV, reconstituted powder for oral susp: Store between 5-30°C. Do not freeze.
MIMS Class
ATC Classification
J02AC01 - fluconazole ; Belongs to the class of triazole derivatives. Used in the systemic treatment of mycotic infections.
References
Anon. Fluconazole. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 10/05/2019.

Anon. Fluconazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/05/2019.

Buckingham R (ed). Fluconazole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/05/2019.

Diflucan 10 mg/mL Powder for Oral Suspension (Pfizer Limited). MHRA. https://products.mhra.gov.uk/. Accessed 10/05/2019.

Fluconazole 2 mg/mL Solution for Infusion (B. Braun Melsungen AG). MHRA. https://products.mhra.gov.uk/. Accessed 10/05/2019.

Fluconazole Powder for Suspension (Aurobindo Pharma Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/05/2019.

Fluconazole Tablet (Glenmark Pharmaceuticals Inc., USA). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/05/2019.

Joint Formulary Committee. Fluconazole. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/05/2019.

Disclaimer: This information is independently developed by MIMS based on Fluconazole from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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