Definition
Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.
Description
Fluconazole is only found in individuals that have used or taken this drug. It is a triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS. Fluconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Fluconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic Route of Elimination: 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)
- Uses/Sources: For the treatment of fungal infections.
- Symptoms: Symptoms of overdose include hallucinations and paranoid behavior.
- Treatment: In the event of overdose, symptomatic treatment (with supportive measures and gastric lavage if clinically indicated) should be instituted. (L1712)
- Route of Exposure: Intravenous, Oral
Mechanism of Action
| Target Name | Mechanism of Action | References |
|---|---|---|
|
Cytochrome P450 3A4 Cytochrome P450 2C19 Malate dehydrogenase, cytoplasmic |
14521410 23611293 19128860 |
|
| Lanosterol 14-alpha demethylase | Fluconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Fluconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis. |
17194716 17964172 11752352 19075057 16966400 16966178 15314102 12654649 |
Fluconazole Interacts with Diseases
| Disease | Inference Score | References/Inference Genes |
| Liver Cirrhosis, Experimental | 14.4 |
|
| Barrett's esophagus | 12.36 |
|
| Acute kidney injury | 9.96 |
|
| Drug-induced liver injury | 9.87 |
|
| Obesity | 9.32 |
|
| Chronobiology Disorders | 8.15 |
|
| Atherosclerosis | 7.84 |
|
| Diabetes Mellitus, Experimental | 7.77 |
|
| Diabetes Mellitus, Type 2 | 7.47 |
|
| Splenic Diseases | 7.15 |
|
| Metabolic Diseases | 6.96 |
|
| Urinary Bladder Neoplasms | 6.91 |
|
| Prostatic Neoplasms | 6.77 |
|
| Diabetes mellitus | 6.7 |
|
| Colorectal cancer | 6.47 |
|
| Endometriosis | 6.41 |
|
| Liver Neoplasms, Experimental | 6.17 |
|
| Metabolic Syndrome X | 5.68 |
|
| Adenoma, Liver Cell | 5.66 |
|
| Drug Metabolism, Poor, CYP2C19-Related | 5.62 |