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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=C(F)C=C(F)C=C3

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
2554
Curator's Comment: Fluconazole readily penetrated the blood-CSF/blood-brain barrier

Originator

Approval Year

1990
108
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 0.127 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Approved
8429
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
8429
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
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
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
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
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
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
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
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
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
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
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:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
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
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
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
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
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
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
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
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
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 (mean)
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
n = 40
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: unknown
Population Size: 40
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 (typical)
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
n = 726
Health Status: unhealthy
Condition: systemic candidosis and candidaemia
Age Group: 1 - 12 month
Sex: M+F
Population Size: 726
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
n = 31
Health Status: unhealthy
Condition: HIV-uninfected cryptococcal meningitis
Age Group: 16 - 73 years
Sex: M+F
Population Size: 31
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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 (min)
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
n = 249
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 249
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 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:
https://pubmed.ncbi.nlm.nih.gov/30782643/
unhealthy, adult
n = 345
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 345
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 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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
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
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
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
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
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
n = 577
Health Status: unhealthy
Condition: candidosis
Age Group: 0 - 17 years
Sex: M+F
Population Size: 577
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019949s051lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
https://pubmed.ncbi.nlm.nih.gov/10394841/
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:
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
n = 31
Health Status: unhealthy
Condition: HIV-uninfected cryptococcal meningitis
Age Group: 16 - 73 years
Sex: M+F
Population Size: 31
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
n = 31
Health Status: unhealthy
Condition: HIV-uninfected cryptococcal meningitis
Age Group: 16 - 73 years
Sex: M+F
Population Size: 31
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
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
n = 124
Health Status: unhealthy
Condition: coccidioidomycosis
Age Group: 46.1 years
Sex: M+F
Population Size: 124
Sources:
https://pubmed.ncbi.nlm.nih.gov/30535104/
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:
https://pubmed.ncbi.nlm.nih.gov/30782643/
unhealthy, adult
n = 249
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 249
Sources:
https://pubmed.ncbi.nlm.nih.gov/30782643/
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:
https://pubmed.ncbi.nlm.nih.gov/30782643/
unhealthy, adult
n = 345
Health Status: unhealthy
Condition: fungal infections, pregnancies
Age Group: adult
Sex: F
Population Size: 345
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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 448
Health Status: unhealthy
Condition: Vaginal Candidiasis
Age Group: adult
Sex: F
Population Size: 448
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
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
n = 11
Health Status: unhealthy
Condition: HIV Associated Neurocognitive Disorder
Population Size: 11
Sources:
https://clinicaltrials.gov/ct2/show/NCT01354314
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587
inhibitor
1767
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C19
1478

P-gp
1461

UGT1A1
204

UGT1A3
84

UGT1A4
77

UGT1A6
108

UGT1A7
21

UGT1A8
36

UGT1A9
116

UGT1A10
32

UGT2B7
146

UGT2B15
64

MRP1
106

MRP2
383

MRP3
157

MRP4
204

MRP5
22

BCRP
699

BSEP
402

OATP1B1
788

OATP1B3
706
UGT1A1
418

UGT1A3
422

UGT1A4
347

UGT1A6
307

UGT1A7
236

UGT1A8
283

UGT1A9
380

UGT1A10
291

UGT2B4
249

UGT2B7
389

UGT2B15
203

UGT2B17
213
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1925
 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
1819
 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
773
 no
BSEP
403
 no
MRP1
172
 no
MRP2
475
 no
MRP3
207
 no
MRP4
238
 no
MRP5
48
 no
OATP1B3
715
 no
P-gp
1650
 no
UGT1A1
254
 no
UGT1A10
41
 no
UGT1A3
93
 no
UGT1A4
80
 no
UGT1A6
141
 no
UGT1A7
23
 no
UGT1A8
48
 no
UGT1A9
121
 no
UGT2B15
64
 no
CYP2C19
1553
 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
157
 weak [Ki 529 uM]
OATP1B1
803
 weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
UGT2B7
389
 major
UGT1A4
347
 minor
UGT1A1
418
 no
UGT1A10
291
 no
UGT1A3
422
 no
UGT1A6
307
 no
UGT1A7
236
 no
UGT1A8
283
 no
UGT1A9
380
 no
UGT2B15
203
 no
UGT2B17
213
 no
UGT2B4
249
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
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
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
eMolecules
877450
https://www.emolecules.com/cgi-bin/more?vid=877450
PubMed

PubMed

TitleDatePubMed
In-vitro activity of voriconazole (UK-109,496), LY303366 and other antifungal agents against oral Candida spp. isolates from HIV-infected patients.
1999 Nov
Prophylactic fluconazole in liver transplant recipients. A randomized, double-blind, placebo-controlled trial.
1999 Nov 16
Synergistic effects of low doses of histatin 5 and its analogues on amphotericin B anti-mycotic activity.
2000 Aug
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
Lanoconazole, a new imidazole antimycotic compound, protects MAIDS mice against encephalitis caused by Cryptococcus neoformans.
2000 Sep
Muscular-skeletal cryptococcosis in a patient with idiopathic CD4+ lymphopenia.
2001
Comparison of PCR to histology for the diagnosis of invasive candidiasis in a murine model.
2001
Effects of fluconazole and fluvoxamine on the pharmacokinetics and pharmacodynamics of glimepiride.
2001 Apr
Fluconazole-induced torsade de pointes.
2001 Apr
Increased resource use associated with catheter-related bloodstream infection in the surgical intensive care unit.
2001 Feb
In vitro activity of a new echinocandin, LY303366, and comparison with fluconazole, flucytosine and amphotericin B against Candida species.
2001 Jan
Aerobic bacterial and fungal infections in peripheral blood stem cell transplants.
2001 Jan
Coccidioidomycosis in adolescents with lupus nephritis.
2001 Jan
Impact of an intravenous fluconazole restriction policy on patient outcomes.
2001 Jan
Effect of fluconazole on agar invasion by Candida albicans.
2001 Jan
Successful treatment of Paecilomyces lilacinus endophthalmitis after foreign body trauma to the cornea.
2001 Jan
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 Jan 15
Empirical antifungal therapy for persistent fever in patients with neutropenia.
2001 Jan 15
Fluconazole-impregnated beads in the management of fungal infection of prosthetic joints.
2001 Mar
Susceptibility of fungal or yeast bloodstream isolates to antifungals: results from a national study.
2001 Mar-Apr
Therapy for fungal infections in leukemia.
2001 May
Patents

Patents

JP2006514917A
60
JP2011508747A
61
JP2011526302A
67
JP4728220B2
15
JP4787165B2
101
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 Sat Dec 16 17:48:37 GMT 2023
Edited
by admin
on Sat Dec 16 17:48:37 GMT 2023
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
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 Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
WHO-VATC QD01AC15
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
WHO-ATC J02AC01
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
NDF-RT N0000008217
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
WHO-ATC D01AC15
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
NCI_THESAURUS C514
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
WHO-VATC QJ02AC01
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
LIVERTOX NBK548300
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
NDF-RT N0000175487
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
WHO-ESSENTIAL MEDICINES LIST 6.3
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C500
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
ChEMBL
CHEMBL106
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
MERCK INDEX
m5423
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY Merck Index
INN
5851
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
DRUG CENTRAL
1187
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
EVMPD
SUB07674MIG
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
NDF-RT
N0000185504
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY Cytochrome P450 2C9 Inhibitors [MoA]
HSDB
7420
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
DRUG BANK
DB00196
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
LACTMED
Fluconazole
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
NDF-RT
N0000182141
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
RS_ITEM_NUM
1271700
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
DAILYMED
8VZV102JFY
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
NSC
758661
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
WIKIPEDIA
FLUCONAZOLE
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
CAS
86386-73-4
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
CHEBI
46081
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
NDF-RT
N0000182140
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY Cytochrome P450 2C19 Inhibitors [MoA]
RXCUI
4450
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY RxNorm
PUBCHEM
3365
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
SMS_ID
100000092657
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
WHO INTERNATIONAL PHARMACOPEIA
FLUCONAZOLE
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
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 Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
FDA UNII
8VZV102JFY
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
PRIMARY
MESH
D015725
Created by admin on Sat Dec 16 17:48:40 GMT 2023 , Edited by admin on Sat Dec 16 17:48:40 GMT 2023
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
MAJOR
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
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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