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Details

Stereochemistry ACHIRAL
Molecular Formula C13H12F2N6O
Molecular Weight 306.2713
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FLUCONAZOLE

SMILES

c1cc(c(cc1F)F)C(Cn2cncn2)(Cn3cncn3)O

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 306.2713
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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.127 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
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

6.334848E11
Curative
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

6.334848E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.54 μg/mL
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
2.61 μg/mL
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
6.72 μg/mL
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
11.4 μg/mL
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
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
2.9 μg/mL
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
5.5 μg/mL
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
9.8 μg/mL
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
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
76.4 μg × h/mL
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
156.1 ug*h/mL
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
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
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:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
46.2 h
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
30 h
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
15.2 h
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
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
25 h
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
17.4 h
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
19.5 h
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
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
88.5%
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:
unhealthy, 0 - 17 years
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
Sources:
Other AEs: Vomiting, Abdominal pain...
Other AEs:
Vomiting (5.4%)
Abdominal pain (2.8%)
Nausea (2.3%)
Diarrhea (2.1%)
Sources:
5.3 mg/kg 1 times / day steady, oral (mean)
Recommended
Dose: 5.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 5.3 mg/kg, 1 times / day
Sources:
unhealthy, 1 - 12 month
n = 40
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: unknown
Population Size: 40
Sources:
Other AEs: Anaemia, Transaminases increased...
Other AEs:
Anaemia (1 patient)
Transaminases increased (1 patient)
Sources:
6 mg/kg 1 times / day steady, oral (typical)
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
unhealthy, 1 - 12 month
n = 726
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: M+F
Population Size: 726
Sources:
Disc. AE: Nephrotoxicity, Hepatotoxicity...
AEs leading to
discontinuation/dose reduction:
Nephrotoxicity
Hepatotoxicity
Myelosuppression
Sources:
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:
unhealthy, 16 - 73 years
n = 31
Health Status: unhealthy
Condition: HIV-uninfected cryptococcal meningitis
Age Group: 16 - 73 years
Sex: M+F
Population Size: 31
Sources:
Disc. AE: Anemia, Transaminases increased...
AEs leading to
discontinuation/dose reduction:
Anemia (3 patients)
Transaminases increased (1 patient)
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
150 mg 1 times / day steady, oral (min)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult
n = 249
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 249
Sources:
Other AEs: Abortions spontaneous...
Other AEs:
Abortions spontaneous (249 patients)
Sources:
150 mg 1 times / day steady, oral (max)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult
n = 345
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 345
Sources:
Other AEs: Abortions spontaneous...
Other AEs:
Abortions spontaneous (345 patients)
Sources:
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
Other AEs: Headache, Nausea...
Other AEs:
Headache (13%)
Nausea (7%)
Abdominal pain (6%)
Diarrhea (3%)
Dyspepsia (1%)
Dizziness (1%)
Taste perversion (1%)
Sources:
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
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:
unhealthy, 0 - 17 years
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
Sources:
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:
unhealthy, 0 - 17 years
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
Sources:
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:
unhealthy, 0 - 17 years
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
Sources:
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:
unhealthy, 0 - 17 years
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
Sources:
Anaemia 1 patient
5.3 mg/kg 1 times / day steady, oral (mean)
Recommended
Dose: 5.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 5.3 mg/kg, 1 times / day
Sources:
unhealthy, 1 - 12 month
n = 40
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: unknown
Population Size: 40
Sources:
Transaminases increased 1 patient
5.3 mg/kg 1 times / day steady, oral (mean)
Recommended
Dose: 5.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 5.3 mg/kg, 1 times / day
Sources:
unhealthy, 1 - 12 month
n = 40
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: unknown
Population Size: 40
Sources:
Hepatotoxicity Disc. AE
6 mg/kg 1 times / day steady, oral (typical)
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
unhealthy, 1 - 12 month
n = 726
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: M+F
Population Size: 726
Sources:
Myelosuppression Disc. AE
6 mg/kg 1 times / day steady, oral (typical)
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
unhealthy, 1 - 12 month
n = 726
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: M+F
Population Size: 726
Sources:
Nephrotoxicity Disc. AE
6 mg/kg 1 times / day steady, oral (typical)
Dose: 6 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg/kg, 1 times / day
Sources:
unhealthy, 1 - 12 month
n = 726
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: M+F
Population Size: 726
Sources:
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:
unhealthy, 16 - 73 years
n = 31
Health Status: unhealthy
Condition: HIV-uninfected cryptococcal meningitis
Age Group: 16 - 73 years
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, 16 - 73 years
n = 31
Health Status: unhealthy
Condition: HIV-uninfected cryptococcal meningitis
Age Group: 16 - 73 years
Sex: M+F
Population Size: 31
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
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:
unhealthy, 46.1 years
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
Abortions spontaneous 249 patients
150 mg 1 times / day steady, oral (min)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult
n = 249
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 249
Sources:
Abortions spontaneous 345 patients
150 mg 1 times / day steady, oral (max)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult
n = 345
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 345
Sources:
Dizziness 1%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
Dyspepsia 1%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
Taste perversion 1%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
Headache 13%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
Diarrhea 3%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
Abdominal pain 6%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
Nausea 7%
150 mg single, oral
Dose: 150 mg
Route: oral
Route: single
Dose: 150 mg
Sources:
unhealthy, adult
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
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:
unhealthy
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
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
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
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
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
weak [Ki 529 uM]
weak
Drug as victimTox targets
PubMed

PubMed

TitleDatePubMed
Survival following fulminant hepatic failure from fluconazole induced hepatitis.
1999 Dec
Comparisons of the effects of fungicidal and fungistatic antifungal agents on the morphogenetic transformation of Candida albicans.
1999 Mar
In vitro antifungal activity of BMS-207147 and itraconazole against yeast strains that are non-susceptible to fluconazole.
1999 Oct
Optically active antifungal azoles. X. Synthesis and antifungal activity of N.
2000 Dec
Syncope associated with concurrent amitriptyline and fluconazole therapy.
2000 Dec
Synthesis and antimicrobial activity of new 3-(1-R-3(5)-methyl-4-nitroso-1H-5(3)-pyrazolyl)-5-methylisoxazoles.
2000 Dec
Comparison of the Etest and microdilution method for antifungal susceptibility testing of Cryptococcus neoformans to four antifungal agents.
2000 Dec
Prolonged QT interval and torsades de pointes caused by the combination of fluconazole and amitriptyline.
2000 Mar
Synergistic antifungal activities of bafilomycin A(1), fluconazole, and the pneumocandin MK-0991/caspofungin acetate (L-743,873) with calcineurin inhibitors FK506 and L-685,818 against Cryptococcus neoformans.
2000 Mar
In vitro susceptibility of Cryptococcus neoformans isolates to five antifungal drugs using a colorimetric system and the reference microbroth method.
2000 May
Activity of voriconazole against Candida albicans and Candida krusei isolated since 1984.
2000 Nov
Bactericidal and inhibitory effects of azole antifungal compounds on Mycobacterium smegmatis.
2000 Nov 15
In vitro antifungal activity of a novel lipopeptide antifungal agent, FK463, against various fungal pathogens.
2000 Oct
Fluconazole-induced convulsions at serum trough concentrations of approximately 80 microg/mL.
2000 Oct
Anti-Candida activity of a new platinum derivative.
2000 Oct
Lanoconazole, a new imidazole antimycotic compound, protects MAIDS mice against encephalitis caused by Cryptococcus neoformans.
2000 Sep
Efficacy of the echinocandin caspofungin against disseminated aspergillosis and candidiasis in cyclophosphamide-induced immunosuppressed mice.
2000 Sep
Muscular-skeletal cryptococcosis in a patient with idiopathic CD4+ lymphopenia.
2001
Fluconazole-induced torsade de pointes.
2001 Apr
Acute adrenal failure associated with fluconazole after administration of high-dose cyclophosphamide.
2001 Apr
Candida dubliniensis at a cancer center.
2001 Apr 1
Effect of ketoconazole, itraconazole and fluconazole on the gastrointestinal colonization of mice by Candida albicans.
2001 Feb
Determination of minumum inhibitory concentrations of Candida species isolated from vaginal swab specimens by using broth macrodilution and E-test.
2001 Feb
Cutaneous alternariosis in a cardiac transplant recipient.
2001 Feb
Penetration of topical fluconazole into human aqueous humor.
2001 Feb
Candida endophthalmitis: an unusual complication of prolonged intravenous access.
2001 Feb
Cromolyn cream for recalcitrant idiopathic vulvar vestibulitis: results of a placebo controlled study.
2001 Feb
Fluconazole prophylaxis in the very low birth weight infant: not ready for prime time.
2001 Feb
Fluconazole for prophylaxis against candidal rectal colonization in the very low birth weight infant.
2001 Feb
Reply to Dr. Chandrasekar (Clin Infect Dis 2001; 32:320-1) and Drs. Marr and Boeckh (Clin Infect Dis 2001; 32:321).
2001 Feb 1
Candida osteomyelitis and diskitis after spinal surgery: an outbreak that implicates artificial nail use.
2001 Feb 1
Interstitial lung disease induced by endogenous Candida albicans.
2001 Feb 28
Effect of fluconazole on agar invasion by Candida albicans.
2001 Jan
The combination of oral amphotericin B with azoles prevents the emergence of resistant Candida species in neutropenic patients.
2001 Jan
Microsphaeropsis olivacea keratitis and consecutive endophthalmitis.
2001 Jan
Endogenous amoebic endophthalmitis.
2001 Jan
Empirical antifungal therapy for persistent fever in patients with neutropenia.
2001 Jan 15
Candida lusitaniae: a cause of breakthrough fungemia in cancer patients.
2001 Jan 15
Candidiasis in a cured MB patient.
2001 Jan-Mar
Candida ciferrii, a new fluconazole-resistant yeast causing systemic mycosis in immunocompromised patients.
2001 Mar
Fluconazole dose recommendation in urinary tract infection.
2001 Mar
The influence of antifungal drugs on virulence properties of Candida albicans in patients with diabetes mellitus.
2001 Mar
Patents

Sample Use Guides

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
Fluconazole inhibited Candida albicans with MIC 0.125-16 ug/ml
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:04:58 UTC 2021
Edited
by admin
on Fri Jun 25 21:04:58 UTC 2021
Record UNII
8VZV102JFY
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
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
DIFLUCAN
Brand Name English
FLUCONAZOLI [WHO-IP LATIN]
Common Name English
BAYT006267
Code 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
FLUCONAZOLE [WHO-DD]
Common Name 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 Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
WHO-VATC QD01AC15
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
WHO-ATC J02AC01
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
NDF-RT N0000008217
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
WHO-ATC D01AC15
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
NCI_THESAURUS C514
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
WHO-VATC QJ02AC01
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
LIVERTOX 418
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
NDF-RT N0000175487
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
WHO-ESSENTIAL MEDICINES LIST 6.3
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C500
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL106
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
MERCK INDEX
M5423
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY Merck Index
INN
5851
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
DRUG CENTRAL
1187
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
EVMPD
SUB07674MIG
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
NDF-RT
N0000185504
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY Cytochrome P450 2C9 Inhibitors [MoA]
HSDB
7420
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
DRUG BANK
DB00196
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
LACTMED
Fluconazole
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
NDF-RT
N0000182141
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
WIKIPEDIA
FLUCONAZOLE
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
CAS
86386-73-4
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
NDF-RT
N0000182140
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY Cytochrome P450 2C19 Inhibitors [MoA]
RXCUI
4450
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY RxNorm
PUBCHEM
3365
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
WHO INTERNATIONAL PHARMACOPEIA
FLUCONAZOLE
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
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.
USP_CATALOG
1271700
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY USP-RS
EPA CompTox
86386-73-4
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
FDA UNII
8VZV102JFY
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
MESH
D015725
Created by admin on Fri Jun 25 21:04:59 UTC 2021 , Edited by admin on Fri Jun 25 21:04:59 UTC 2021
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> INHIBITOR
IC50
BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
EP
INHIBITOR -> METABOLIC ENZYME
METABOLIC ENZYME -> INHIBITOR
MAJOR
METABOLIC ENZYME -> INHIBITOR
IC50
BINDER->LIGAND
BINDING
Related Record Type Details
METABOLITE -> PARENT
MAJOR
URINE
Related Record Type Details
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 %).
IMPURITY -> PARENT
Fluconazole Impurity H Amount Not Specified.
IMPURITY -> PARENT
Fluconazole Impurity I Amount Not Specified.
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
Fluconazole Impurity G Amount Not Specified.
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
Fluconazole Impurity E Amount Not Specified.
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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 %).
IMPURITY -> PARENT
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
Fluconazole Impurity F Amount Not Specified.
IMPURITY -> PARENT
Amount not specified.
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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
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