Fluconazole
Also known as: diflucan, triflucan,
Fluconazole is antifungal agent. Fluconazole is a substituted triazole derivetive. The requirement for intravenous administration and the toxicity of the older antifungal agents created a need for antifungal agents with a better therapeutic profile. The relatively non-toxic oral azole medications represent the first major advance in this direction. Since their introduction in the 1980s, these medications have played an increasingly important role in the systemic therapy of fungal disease.
Primary Characteristics
Fluconazole is also known as diflucan, triflucan, .
It is of Synthetic origin and belongs to Triazol.
It is classified in Antifungal Agent, Parental pharmacological group.
Molecular Weight: 306.3 · pKa: 2.03 · Solubility in Water: Slightly Soluble · Solubility in Alcohol: sparingly soluble · Non-proprietary name: Fluconazole.

Pharmacokinetics
Absorption: Fluconazole has an oral bioavailability is 45% (±45%), pre-systemic (first-pass) metabolism accounts for 2.5% (±2.5%).
Distribution: Fluconazole has a volume of distribution is 0.55-0.651 l/kg. plasma protein binding is 11 - 12 %.
Elimination: it is metabolised via 11%, plasma half-life is 25 - 30 hr, renal excretion is 80 %.
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Indications
Fluconazole is primarily indicated in conditions like Adjunctive therapy without valproate, Candidiasis, Cryptcoccal meningitis, Fungal infection, Neurogenic bladder, Oropharangeal candidiasis, Parkinsonism, Pityriasis versicolor, Vaginal infections.
Fluconazole is also indicated for secondary conditions like Bone marrow transplantation, Cryptococcal infections including meningitis, Esophagitis, Urinary tract infection.
Contraindications
None recorded.
Dosage
Fluconazole's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 450 mg /day | 450 mg /day | Every 24h | IV | for Mucocutaneous candidiasis |
| 350 mg | 350 mg | Every 24h | PO,IV | Maintenance, As Required |
| 400 mg | 400 mg | — | PO,IV | Initially for Once |
| Paediatric Dosage (20kg) | ||||
| 1.5 mg/kg | 1.5 mg/kg | Every 24h | Slow IV | - |
| Neonatal Dosage (3kg) | ||||
| 1.5 mg/kg | 1.5 mg/kg | Every 24h | Slow IV | - |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Fluconazole in overdosage may give rise to further complications which include Alopecia , Thrombocytopenia , Elevated alkaline phosphatase concentration, Eelvated hepatic enzymes , Hyperlipidemia, Elevated alkaline phosphatase concentration.
Fluconazole produces potentially life-threatening effects which include Hepatic necrosis, Death, Severe skin reactions in AIDS. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Fluconazole are Hallucinations , Paranoid psychosis.
Fluconazole is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Anaphylaxis, Diarrhea, Dizziness, Headache, Hypokalemia , Leucopenia, Nausea, Pallor, Rashes , Vomiting .
Warnings / Precautions
Interference in Pathology
Fluconazole may interfere in the diagnosis of Increased Alkaline Phosphatase , Bilirubin (increased level).
Available Brands
Storage Conditions
Drug Classification
- 1.6.3 — Antifungal drugs
Manufacturers
Manufacturers of Fluconazole in Pakistan: