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Details

Stereochemistry ACHIRAL
Molecular Formula C13H12F2N6O
Molecular Weight 306.2708
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FLUCONAZOLE

SMILES

OC(CN1C=NC=N1)(CN2C=NC=N2)C3=CC=C(F)C=C3F

InChI

InChIKey=RFHAOTPXVQNOHP-UHFFFAOYSA-N
InChI=1S/C13H12F2N6O/c14-10-1-2-11(12(15)3-10)13(22,4-20-8-16-6-18-20)5-21-9-17-7-19-21/h1-3,6-9,22H,4-5H2

HIDE SMILES / InChI
Molecular Formula C13H12F2N6O
Molecular Weight 306.2708
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf

Fluconazole, a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis. It inhibits the fungal lanosterol 14 alpha-demethylase which thereby prevents the formation of ergosterol which is an essential component in the fungal cell membrane. Indicated for the treatment of fungal infections.

CNS Activity

CNS Penetrant
2588
Curator's Comment: Fluconazole readily penetrated the blood-CSF/blood-brain barrier

Originator

Approval Year

1990
111
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
 0.127 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Approved
8583
Diflucan

Approved Use

DIFLUCAN (fluconazole) is indicated for the treatment of: 1. Vaginal candidiasis (vaginal yeast infections due to Candida). 2. Oropharyngeal and esophageal candidiasis. In open noncomparative studies of relatively small numbers of patients, DIFLUCAN was also effective for the treatment of Candida urinary tract infections, peritonitis, and systemic Candida infections including candidemia, disseminated candidiasis, and pneumonia. 3. Cryptococcal meningitis.

Launch Date

1990
Curative
Approved
8583
Diflucan

Approved Use

DIFLUCAN (fluconazole) is indicated for the treatment of: 1. Vaginal candidiasis (vaginal yeast infections due to Candida). 2. Oropharyngeal and esophageal candidiasis. In open noncomparative studies of relatively small numbers of patients, DIFLUCAN was also effective for the treatment of Candida urinary tract infections, peritonitis, and systemic Candida infections including candidemia, disseminated candidiasis, and pneumonia. 3. Cryptococcal meningitis.

Launch Date

1990
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
6.72 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
2.61 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE
food status: UNKNOWN
2.9 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
2 mg/kg single, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
9.8 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
8 mg/kg single, oral
dose: 8 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
5.5 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
2 mg/kg 1 times / day multiple, intravenous
dose: 2 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
11.4 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
4 mg/kg 1 times / day multiple, intravenous
dose: 4 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
14.1 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
8 mg/kg 1 times / day multiple, intravenous
dose: 8 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
1.54 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
156.1 ug*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01806623
150 mg single, oral
dose: 150 mg
route of administration: oral
experiment type: single
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: unhealthy
age:
sex: F
food status:
79.5 ug*h/g
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01806623
150 mg single, oral
dose: 150 mg
route of administration: oral
experiment type: single
co-administered:
FLUCONAZOLE vaginal fluid
Homo sapiens
population: unhealthy
age:
sex: F
food status:
85.3 ug*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01806623
150 mg single, oral
dose: 150 mg
route of administration: oral
experiment type: single
co-administered:
FLUCONAZOLE vaginal fluid
Homo sapiens
population: unhealthy
age:
sex: F
food status:
76.4 μg × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
30 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
25 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
2 mg/kg single, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
19.5 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
8 mg/kg single, oral
dose: 8 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
17.4 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
2 mg/kg 1 times / day multiple, intravenous
dose: 2 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
15.2 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
4 mg/kg 1 times / day multiple, intravenous
dose: 4 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
17.6 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
8 mg/kg 1 times / day multiple, intravenous
dose: 8 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
46.2 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
88.5%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
FLUCONAZOLE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
15 mg/kg 1 times / day steady, oral
Dose: 15 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, 0 - 17 years
Health Status: unhealthy
Age Group: 0 - 17 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Other AEs: Vomiting, Abdominal pain...
Other AEs:
Vomiting (5.4%)
Abdominal pain (2.8%)
Nausea (2.3%)
Diarrhea (2.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
5.3 mg/kg 1 times / day steady, oral
Recommended
Dose: 5.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 5.3 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
unhealthy, 1 - 12 month
Health Status: unhealthy
Age Group: 1 - 12 month
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
Other AEs: Anaemia, Transaminases increased...
Other AEs:
Anaemia (1 patient)
Transaminases increased (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
6 mg/kg 1 times / day steady, oral
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
unhealthy, 1 - 12 month
Health Status: unhealthy
Age Group: 1 - 12 month
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
Disc. AE: Nephrotoxicity, Hepatotoxicity...
AEs leading to
discontinuation/dose reduction:
Nephrotoxicity
Hepatotoxicity
Myelosuppression
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30541454/
unhealthy, 16 - 73 years
Health Status: unhealthy
Age Group: 16 - 73 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30541454/
Disc. AE: Anemia, Transaminases increased...
AEs leading to
discontinuation/dose reduction:
Anemia (3 patients)
Transaminases increased (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/30541454/
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Other AEs: Xerosis, Alopecia...
Other AEs:
Xerosis (8 patients)
Alopecia (11 patient)
Fatigue (13 patients)
Nausea and vomiting (10 patients)
Anorexia (7 patients)
Headache (6 patients)
Arthralgia (5 patients)
Cheilitis (4 patients)
Xerostomia (2 patients)
Dizziness (3 patients)
Neuropathy (2 patients)
Abdominal discomfort (2 patients)
ALP increased (2 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
150 mg 1 times / day steady, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
Other AEs: Abortions spontaneous...
Other AEs:
Abortions spontaneous (345 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
150 mg 1 times / day steady, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
Other AEs: Abortions spontaneous...
Other AEs:
Abortions spontaneous (249 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Other AEs: Headache, Nausea...
Other AEs:
Headache (13%)
Nausea (7%)
Abdominal pain (6%)
Diarrhea (3%)
Dyspepsia (1%)
Dizziness (1%)
Taste perversion (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Other AEs: Glucose high, Acute depression...
Other AEs:
Glucose high (serious, 1 patient)
Acute depression (serious, 1 patient)
Agitation (below serious, 1 patient)
Aspartate aminotransferase increased (below serious, 1 patient)
Blood alkaline phosphatase high (below serious, 1 patient)
Taste altered (below serious, 1 patient)
Bilirubin total high (below serious, 3 patients)
Chlamydial infection (below serious, 1 patient)
Constipation (below serious, 1 patient)
Subcutaneous cyst (below serious, 1 patient)
Depressed mood (below serious, 2 patients)
Dry mouth (below serious, 2 patients)
Flank pain (below serious, 1 patient)
Blood glucose increased (below serious, 3 patients)
Headache NOS (below serious, 1 patient)
Insomnia (below serious, 1 patient)
Generalized joint pain (below serious, 1 patient)
Lightheadedness (below serious, 1 patient)
Lymphadenopathy cervical (below serious, 1 patient)
Nausea (below serious, 4 patients)
Nose bleed (below serious, 1 patient)
Prostatitis (below serious, 1 patient)
Sexual dysfunction (below serious, 1 patient)
Syphilis (below serious, 1 patient)
Tooth infection (below serious, 1 patient)
Upper respiratory infection (below serious, 1 patient)
Visual disturbance (below serious, 1 patient)
Vomiting (below serious, 1 patient)
Weight loss (below serious, 1 patient)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
AEs

AEs

AESignificanceDosePopulation
Diarrhea 2.1%
15 mg/kg 1 times / day steady, oral
Dose: 15 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, 0 - 17 years
Health Status: unhealthy
Age Group: 0 - 17 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Nausea 2.3%
15 mg/kg 1 times / day steady, oral
Dose: 15 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, 0 - 17 years
Health Status: unhealthy
Age Group: 0 - 17 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Abdominal pain 2.8%
15 mg/kg 1 times / day steady, oral
Dose: 15 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, 0 - 17 years
Health Status: unhealthy
Age Group: 0 - 17 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Vomiting 5.4%
15 mg/kg 1 times / day steady, oral
Dose: 15 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, 0 - 17 years
Health Status: unhealthy
Age Group: 0 - 17 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Anaemia 1 patient
5.3 mg/kg 1 times / day steady, oral
Recommended
Dose: 5.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 5.3 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
unhealthy, 1 - 12 month
Health Status: unhealthy
Age Group: 1 - 12 month
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
Transaminases increased 1 patient
5.3 mg/kg 1 times / day steady, oral
Recommended
Dose: 5.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 5.3 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
unhealthy, 1 - 12 month
Health Status: unhealthy
Age Group: 1 - 12 month
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
Hepatotoxicity Disc. AE
6 mg/kg 1 times / day steady, oral
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
unhealthy, 1 - 12 month
Health Status: unhealthy
Age Group: 1 - 12 month
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
Myelosuppression Disc. AE
6 mg/kg 1 times / day steady, oral
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
unhealthy, 1 - 12 month
Health Status: unhealthy
Age Group: 1 - 12 month
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
Nephrotoxicity Disc. AE
6 mg/kg 1 times / day steady, oral
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
unhealthy, 1 - 12 month
Health Status: unhealthy
Age Group: 1 - 12 month
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/10394841/
Transaminases increased 1 patient
Disc. AE
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30541454/
unhealthy, 16 - 73 years
Health Status: unhealthy
Age Group: 16 - 73 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30541454/
Anemia 3 patients
Disc. AE
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30541454/
unhealthy, 16 - 73 years
Health Status: unhealthy
Age Group: 16 - 73 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30541454/
Nausea and vomiting 10 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Alopecia 11 patient
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Fatigue 13 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
ALP increased 2 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Abdominal discomfort 2 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Neuropathy 2 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Xerostomia 2 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Dizziness 3 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Cheilitis 4 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Arthralgia 5 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Headache 6 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Anorexia 7 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Xerosis 8 patients
400 mg 1 times / day steady, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
unhealthy, 46.1 years
Health Status: unhealthy
Age Group: 46.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
Abortions spontaneous 345 patients
150 mg 1 times / day steady, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
Abortions spontaneous 249 patients
150 mg 1 times / day steady, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
Dizziness 1%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Dyspepsia 1%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Taste perversion 1%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Headache 13%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Diarrhea 3%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Abdominal pain 6%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Nausea 7%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
Agitation below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Aspartate aminotransferase increased below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Blood alkaline phosphatase high below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Chlamydial infection below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Constipation below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Flank pain below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Generalized joint pain below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Headache NOS below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Insomnia below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Lightheadedness below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Lymphadenopathy cervical below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Nose bleed below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Prostatitis below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Sexual dysfunction below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Subcutaneous cyst below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Syphilis below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Taste altered below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Tooth infection below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Upper respiratory infection below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Visual disturbance below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Vomiting below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Weight loss below serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Depressed mood below serious, 2 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Dry mouth below serious, 2 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Bilirubin total high below serious, 3 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Blood glucose increased below serious, 3 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Nausea below serious, 4 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Acute depression serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Glucose high serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
2252
inhibitor
2438
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C19
2057

P-gp
1741

UGT1A1
246

UGT1A3
89

UGT1A4
98

UGT1A6
136

UGT1A7
23

UGT1A8
37

UGT1A9
148

UGT1A10
37

UGT2B7
197

UGT2B15
84

MRP1
116

MRP2
499

MRP3
246

MRP4
290

MRP5
31

BCRP
910

BSEP
550

OATP1B1
1079

OATP1B3
961
UGT1A1
479

UGT1A3
470

UGT1A4
399

UGT1A6
343

UGT1A7
249

UGT1A8
323

UGT1A9
423

UGT1A10
331

UGT2B4
278

UGT2B7
456

UGT2B15
236

UGT2B17
237
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
2633
 moderate [IC50 13.1 uM]
yes (co-administration study)
Comment: see https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf#page=14 for DDIs
CYP2C9
2497
 moderate [IC50 30.3 uM]
yes (co-administration study)
Comment: see https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf#page=14 for DDIs
BCRP
985
 no
BSEP
554
 no
MRP1
232
 no
MRP2
625
 no
MRP3
326
 no
MRP4
345
 no
MRP5
80
 no
OATP1B3
970
 no
P-gp
1932
 no
UGT1A1
303
 no
UGT1A10
46
 no
UGT1A3
99
 no
UGT1A4
100
 no
UGT1A6
171
 no
UGT1A7
25
 no
UGT1A8
49
 no
UGT1A9
155
 no
UGT2B15
84
 no
CYP2C19
2141
 strong [IC50 12.3 uM]
yes (co-administration study)
Comment: see https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf#page=14 for DDIs
UGT2B7
210
 weak [Ki 529 uM]
OATP1B1
1095
 weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
UGT2B7
456
 major
UGT1A4
399
 minor
UGT1A1
479
 no
UGT1A10
331
 no
UGT1A3
470
 no
UGT1A6
343
 no
UGT1A7
249
 no
UGT1A8
323
 no
UGT1A9
423
 no
UGT2B15
236
 no
UGT2B17
237
 no
UGT2B4
278
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:46081
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:46081
ChemicalBook
CB3740293
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB3740293
ChemicalBook
CB4588407
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB4588407
eMolecules
877450
https://www.emolecules.com/cgi-bin/more?vid=877450
MolPort
MolPort-000-883-859
https://www.molport.com/shop/molecule-link/MolPort-000-883-859
Selleck Chemicals
Fluconazole
http://www.selleckchem.com/products/Fluconazole.html
ZINC
ZINC000000004009
http://zinc15.docking.org/substances/ZINC000000004009
PubMed

PubMed

TitleDatePubMed
Candidiasis in a cured MB patient.
2001-05-01
Therapy for fungal infections in leukemia.
2001-05
Candida dubliniensis at a cancer center.
2001-04-01
Effects of fluconazole and fluvoxamine on the pharmacokinetics and pharmacodynamics of glimepiride.
2001-04
Double-blind placebo-controlled trial of fluconazole to prevent candidal infections in critically ill surgical patients.
2001-04
Fluconazole-induced torsade de pointes.
2001-04
In vitro activity of propyl gallate-azole drug combination against fluconazole- and itraconazole-resistant Candida albicans strains.
2001-04
Susceptibility to fluconazole of Candida clinical isolates determined by FUN-1 staining with flow cytometry and epifluorescence microscopy.
2001-04
Acute adrenal failure associated with fluconazole after administration of high-dose cyclophosphamide.
2001-04
Access to fluconazole in less-developed countries.
2001-03-31
Candida ciferrii, a new fluconazole-resistant yeast causing systemic mycosis in immunocompromised patients.
2001-03
Impending rupture in an aortic arch aneurysm by Candida infection.
2001-03
Capecitabine (Xeloda) improves medical resource use compared with 5-fluorouracil plus leucovorin in a phase III trial conducted in patients with advanced colorectal carcinoma.
2001-03
Fluconazole-impregnated beads in the management of fungal infection of prosthetic joints.
2001-03
Laryngeal candidiasis.
2001-03
Treatment for coccidioidomycosis in pregnancy?
2001-03
Fluconazole dose recommendation in urinary tract infection.
2001-03
The influence of antifungal drugs on virulence properties of Candida albicans in patients with diabetes mellitus.
2001-03
Candidal endophthalmitis after keratoplasty.
2001-03
Candidal endophthalmitis in a renal transplant patient.
2001-03
Interstitial lung disease induced by endogenous Candida albicans.
2001-02-28
Treating onychomycosis.
2001-02-15
South Africa cuts agreement for one AIDS drug but ignores another.
2001-02
Synergistic interaction of terbinafine with triazoles or amphotericin B against Aspergillus species.
2001-02
Identification and expression of multidrug resistance-related ABC transporter genes in Candida krusei.
2001-02
Fungal left ventricular assist device endocarditis.
2001-02
Antifungal and immunomodulating activities of 1,4-benzothiazine azole derivatives: review.
2001-02
Effect of ketoconazole, itraconazole and fluconazole on the gastrointestinal colonization of mice by Candida albicans.
2001-02
Determination of minumum inhibitory concentrations of Candida species isolated from vaginal swab specimens by using broth macrodilution and E-test.
2001-02
Cutaneous alternariosis in a cardiac transplant recipient.
2001-02
Effective fluconazole therapy for liver transplant recipients during continuous hemodiafiltration.
2001-02
Analytical validation for a series of marker compounds used to assess renal drug elimination processes.
2001-02
The evolution of Candida species and fluconazole susceptibility among oral and vaginal isolates recovered from human immunodeficiency virus (HIV)-seropositive and at-risk HIV-seronegative women.
2001-01-15
In vitro activity of a new echinocandin, LY303366, and comparison with fluconazole, flucytosine and amphotericin B against Candida species.
2001-01
Aerobic bacterial and fungal infections in peripheral blood stem cell transplants.
2001-01
Pharmacokinetics of sequential intravenous and enteral fluconazole in critically ill surgical patients with invasive mycoses and compromised gastro-intestinal function.
2001-01
Clinico-myocological profile of tinea capitis in North India and response to griseofulvin.
2001-01
Coccidioidomycosis in adolescents with lupus nephritis.
2001-01
Systemic Candida infection in University hospital 1997-1999: the distribution of Candida biotypes and antifungal susceptibility patterns.
2001
Muscular-skeletal cryptococcosis in a patient with idiopathic CD4+ lymphopenia.
2001
Electrophoretic karyotyping and antifungal susceptibility patterns of Candida parapsilosis clinical isolates causing deep and superficial fungal infections.
2001
Penicillium marneffei: types and drug susceptibility.
2001
In vitro susceptibility of 137 Candida sp. isolates from HIV positive patients to several antifungal drugs.
2001
Comparison of PCR to histology for the diagnosis of invasive candidiasis in a murine model.
2001
Candidemia before and during the fluconazole era: prevalence, type of species and approach to treatment in a tertiary care community hospital.
2001
[Current problems in etiotropic therapy of mycoses].
2001
The cost of treating systemic fungal infections.
2001
Clinical experience with itraconazole in systemic fungal infections.
2001
Current management of fungal infections.
2001
Synergistic effects of low doses of histatin 5 and its analogues on amphotericin B anti-mycotic activity.
2000-08
Patents

Patents

JP2006514917A
62
JP2011508747A
62
JP2011526302A
67
JP4728220B2
15
JP4787165B2
104
JPH00338521A
6

Sample Use Guides

In Vivo Use Guide
Dosage and Administration in Adults: Single Dose Vaginal candidiasis: The recommended dosage of DIFLUCAN for vaginal candidiasis is 150 mg as a single oral dose. Multiple Dose SINCE ORAL ABSORPTION IS RAPID AND ALMOST COMPLETE, THE DAILY DOSE OF DIFLUCAN (FLUCONAZOLE) IS THE SAME FOR ORAL (TABLETS AND SUSPENSION) AND INTRAVENOUS ADMINISTRATION. In general, a loading dose of twice the daily dose is recommended on the first day of therapy to result in plasma concentrations close to steady-state by the second day of therapy. Oropharyngeal candidiasis: The recommended dosage of DIFLUCAN for oropharyngeal candidiasis is 200 mg on the first day, followed by 100 mg once daily. Esophageal candidiasis: The recommended dosage of DIFLUCAN for esophageal candidiasis is 200 mg on the first day, followed by 100 mg once daily. Doses up to 400 mg/day may be used.
Route of Administration: Oral
In Vitro Use Guide
Fluconazole inhibited Candida albicans with MIC 0.125-16 ug/ml
Substance Class Chemical
Created
by admin
on Wed Apr 02 09:33:53 GMT 2025
Edited
by admin
on Wed Apr 02 09:33:53 GMT 2025
Record UNII
8VZV102JFY
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DIFLUCAN
Preferred Name English
FLUCONAZOLE
EP   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD   WHO-IP  
USAN   INN  
Official Name English
1H-1,2,4-TRIAZOLE-1-ETHANOL, 1-(2,4-DIFLUOROPHENYL)-1-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-
Common Name English
FLUCONAZOLI [WHO-IP LATIN]
Common Name English
BAYT006267
Code English
Fluconazole [WHO-DD]
Common Name English
BAYT-006267
Code English
FLUCONAZOLE [MI]
Common Name English
FLUCONAZOLE [USP MONOGRAPH]
Common Name English
FLUCONAZOLE [ORANGE BOOK]
Common Name English
UK-49858
Code English
FLUCONAZOLE [WHO-IP]
Common Name English
NSC-758661
Code English
ZOLTEC
Common Name English
FLUCONAZOLE [USP-RS]
Common Name English
fluconazole [INN]
Common Name English
FLUCONAZOLE [EP MONOGRAPH]
Common Name English
FLUCONAZOLE [HSDB]
Common Name English
FLUCONAZOLE [MART.]
Common Name English
UK-49,858
Code English
DIFLUCONAZOLE
Common Name English
2,4-DIFLUORO-1',1'-BIS(1H-1,2,4-TRIAZOL-1-YLMETHYL)BENZYL ALCOHOL
Common Name English
ALKANAZOLE
Common Name English
FLUCONAZOLE [VANDF]
Common Name English
FLUCONAZOLE [JAN]
Common Name English
FLUCONAZOLE [USAN]
Common Name English
Classification Tree Code System Code
WHO-ATC J01RA07
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
WHO-VATC QD01AC15
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
WHO-ATC J02AC01
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
NDF-RT N0000008217
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
WHO-ATC D01AC15
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
NCI_THESAURUS C514
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
WHO-VATC QJ02AC01
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
LIVERTOX NBK548300
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
NDF-RT N0000175487
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
WHO-ESSENTIAL MEDICINES LIST 6.3
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
Code System Code Type Description
NCI_THESAURUS
C500
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
ChEMBL
CHEMBL106
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
MERCK INDEX
m5423
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY Merck Index
INN
5851
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
DRUG CENTRAL
1187
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
EVMPD
SUB07674MIG
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
NDF-RT
N0000185504
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY Cytochrome P450 2C9 Inhibitors [MoA]
HSDB
7420
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
DRUG BANK
DB00196
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
LACTMED
Fluconazole
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
NDF-RT
N0000182141
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
RS_ITEM_NUM
1271700
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
DAILYMED
8VZV102JFY
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
NSC
758661
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
WIKIPEDIA
FLUCONAZOLE
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
CAS
86386-73-4
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
CHEBI
46081
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
NDF-RT
N0000182140
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY Cytochrome P450 2C19 Inhibitors [MoA]
RXCUI
4450
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY RxNorm
PUBCHEM
3365
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
SMS_ID
100000092657
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
WHO INTERNATIONAL PHARMACOPEIA
FLUCONAZOLE
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY Description: A white or almost white, crystalline powder.Solubility: Slightly soluble in water, freely soluble in methanol, soluble in acetone.Category: Antifungal.Storage: Fluconazole should be kept in a tightly closed container.Additional information: Fluconazole is hygroscopic and exhibits polymorphism.Definition: Fluconazole contains not less than 99.0% and not more than 101.0% of C13H12F2N6O, calculated with reference to the dried substance.
EPA CompTox
DTXSID3020627
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
FDA UNII
8VZV102JFY
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
MESH
D015725
Created by admin on Wed Apr 02 09:33:53 GMT 2025 , Edited by admin on Wed Apr 02 09:33:53 GMT 2025
PRIMARY
Related Record Type Details
Structure of FLUCONAZOLE
EXCRETED UNCHANGED
URINE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INHIBITOR
IC50
Structure of FLUCONAZOLE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
EP
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 2B7
INHIBITOR -> METABOLIC ENZYME
CYTOCHROME P450 2C9
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 2C19
METABOLIC ENZYME -> INHIBITOR
IC50
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Related Record Type Details
Structure of FLUCONAZOLE GLUCURONIDE
METABOLITE -> PARENT
MAJOR
URINE
Structure of FOSFLUCONAZOLE
PRODRUG -> METABOLITE ACTIVE
Related Record Type Details
Structure of ISO FLUCONAZOLE
IMPURITY -> PARENT
In the chromatogram obtained with solution (1): ? the area of any peak corresponding to impurity A is not is not greater than 0.8 times the area of the principal peak in the chromatogram obtained with solution (2) (0.4 %).
Structure of 1-BROMO-2-(2,4-DIFLUOROPHENYL)-3-(1H-1,2,4-TRIAZOL-1-YL)PROPAN-2-OL
IMPURITY -> PARENT
Fluconazole Impurity H Amount Not Specified.
Structure of 4-AMINO-1-2-(2,4-DIFLUOROPHENYL)-2-HYDROXY-3(1H-1,2,4-TRIAZOL-1-YL)PROPYL)-4H-1,2,4-TRIAZOLIUM ION
IMPURITY -> PARENT
Fluconazole Impurity I Amount Not Specified.
Structure of 1,1'-(1,3-PHENYLENE)DI-1H-1,2,4-TRIAZOLE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 1-(((2RS)-2-(2,4-DIFLUOROPHENYL)OXIRAN-2-YL)METHYL)-1H-1,2,4-TRIAZOLE
IMPURITY -> PARENT
Fluconazole Impurity G Amount Not Specified.
Structure of 1,1'-(1,3-PHENYLENE)DI-1H-1,2,4-TRIAZOLE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 1-((6RS)-4,6-DIFLUORO-6-(1H-1,2,4-TRIAZOL-1-YL)CYCLOHEXA-1,4-DIEN-1-YL)ETHANONE
IMPURITY -> PARENT
Fluconazole Impurity E Amount Not Specified.
Structure of 2-(4-FLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPAN-2-OL
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of ISO FLUCONAZOLE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 4-DEFLUORO-4-(1H-1,2,4-TRIAZOL-1-YL) FLUCONAZOLE
IMPURITY -> PARENT
In the chromatogram obtained with solution (1):? the area of any peak corresponding to impurity B, when multiplied by a correction factor of 1.5, is not greater than 0.3 times the area of the principal peak in the chromatogram obtained with solution (3) (0.3 %).
Structure of 2,4-DIFLUORO-.ALPHA.-(1H-1,2,4-TRIAZOLYL)ACETOPHENONE
IMPURITY -> PARENT
Structure of 4-DEFLUORO-4-(1H-1,2,4-TRIAZOL-1-YL) FLUCONAZOLE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 2-(2,4-DIFLUOROPHENYL)-3-(1H-1,2,4-TRIAZOL-1-YL)PROPANE-1,2-DIOL
IMPURITY -> PARENT
Fluconazole Impurity F Amount Not Specified.
Structure of 2-(4-FLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPAN-2-OL
IMPURITY -> PARENT
Amount not specified.
Structure of 4-DEFLUORO-4-(1H-1,2,4-TRIAZOL-1-YL) FLUCONAZOLE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 1,1'-(1,3-PHENYLENE)DI-1H-1,2,4-TRIAZOLE
IMPURITY -> PARENT
The test is not valid, unless in the chromatogram obtained with solution (4), the resolution between the peaks due to impurity C and fluconazole is at least 3.0. In the chromatogram obtained with solution (1):? the area of any peak corresponding to impurity C is not is not greater than 0.1 times the area of the principal peak in the chromatogram obtained with solution (3) (0.1 %).
Related Record Type Details
Structure of FLUCONAZOLE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
MAXIMUM TOLERATED DOSE TOXICITY
Route of Elimination PHARMACOKINETIC ELDERLY: 22% UNCHANGED

EXCRETED AS METABOLITE: 11%

Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC CHILDREN, AGE 9 MONTHS TO 15 YEARS: 15.2 - 25 HOURS

ELDERLY: 46.2 HOURS

PREMATURE NEWBORNS, GESTATIONAL AGE 26 - 29 WEEKS: 73.6 HOURS (WITHIN 36 HOURS OF BIRTH), MEAN OF 53.2 HOURS (6 DAYS LATER) AND 46.6 HOURS (12 DAYS LATER)

Biological Half-life PHARMACOKINETIC
Cmax PHARMACOKINETIC Route

Dose
PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC ROUTE OF ADMINISTRATION: ORAL

Tmax PHARMACOKINETIC EFFECT OF FOOD: NONE

Volume of Distribution PHARMACOKINETIC ROUTE OF AMINISTRATION: IV

ORAL BIOAVAILABILITY PHARMACOKINETIC EFFECT OF FOOD: NONE

PROTEIN BINDING PHARMACOKINETIC
Cmax PHARMACOKINETIC ROUTE
PHARMACOKINETIC
DOSE
PHARMACOKINETIC
NIH
NCATS
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ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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