| Fluconazole |
| Trade Name(s): |
Diflucan ·Tablets
50 mg
·Tablets
100 mg
·Tablets
150 mg
·Tablets
200 mg
·Powder for Oral Suspension
10 mg/mL when reconstituted
·Powder for Oral Suspension
40 mg/mL when reconstituted
·Injection
2 mg/mL
Apo-Fluconazole

Apo-Fluconazole-150

Diflucan-150

Gen-Fluconazole

PMS-Fluconazole

Indicates Canadian Trade Name.
|
|
| Class: |
Anti-infective
Antifungal
|
Action: |
Interferes with the formation of fungal cell membrane, causing leakage of cellular contents and cell death.
Absorption: Bioavailability is more than 90%. T
max
is 1 to 2 h.
|
|
Distribution: Apparent Vd is 0.65 L/kg, and it is 11% to 12% protein bound. Ratio of tissue (fluid) concentrations to concurrent plasma concentrations is as follows: CSF, 0.5 to 0.9; saliva, 1; sputum, 1; blister fluid, 1; urine, 10;
normal skin, 10; nails, 1; blister skin, 2; vaginal tissue, 1; and vaginal fluid, 0.4 to 0.7.
|
|
Excretion: Mean body Cl is 0.23
?
mL/min/kg; t
½
is 20 to 50 h. The drug is cleared primarily by renal excretion, about 80% in urine as unchanged drug and 11% excreted in urine as metabolites.
|
|
Hemodialysis
Hemodialysis -
A 3-h session decreases plasma concentrations about 50%.
|
|
Special Populations: Renal Function Impairment - Pharmacokinetics are markedly affected; there is an inverse relationship between t
½
and CrCl.
Children - |
|
9 mo to 15 yr of age
Mean Cl is 0.4 to 0.66 mL/min/kg; t
½
is 15.2 to 25 h. C
max
is 2.9 to 14.1 mcg/mL; Vd
ss
is 0.722 to 1.069.
|
|
Neonates (gestational age 26 to 29 wk)
Mean Cl is 0.18 to 0.333 mL/min/kg (increases with time after birth);
t
½
is 73.6 to 46.6 h (decreases with time after birth).
|
Indications: |
Oropharyngeal and esophageal candidiasis; vaginal candidiasis; prevention of candidiasis in bone marrow transplant;
Cryptococcal meningitis
.
|
Contraindications: |
Coadministration of cisapride; hypersensitivity to any component of the product.
|
Interactions: |
|
|
Alfentanil, benzodiazepines (eg, midazolam), buspirone, corticosteroids
(eg, prednisone), losartan, nisoldipine, sulfonylureas (eg, glyburide), tacrolimus, theophylline, tricyclic antidepressants, vinca alkaloids (eg, vincristine), zidovudine, zolpidem
Levels may be elevated by fluconazole, increasing the risk of adverse reactions and toxicity.
|
|
Anticoagulants (eg, warfarin)
Anticoagulant effect may be increased.
|
|
Cimetidine, rifamycins (eg, rifampin)
Fluconazole plasma levels may be reduced, decreasing therapeutic effects.
|
|
Cisapride
Contraindicated; increased cisapride plasma levels with cardiotoxicity may occur.
|
|
Cyclosporine
Increased cyclosporine concentrations.
|
|
Hydantoins (eg, phenytoin)
Increased hydantoin levels.
|
|
Hydrochlorothiazide
May increase fluconazole levels, increasing adverse reactions.
|
Lab Test Interferences: |
None well documented.
|
Adverse Reactions: |
|
|
cardiovascular:
QT prolongation (including torsades de pointes).
|
|
cns:
Headache (2%).
|
|
dermatologic:
Skin rash (2%); exfoliative skin disorders
(including Stevens-Johnson syndrome and toxic epidermal necrolysis).
|
|
gi:
Nausea (4%
[
children 2%
]
); vomiting
(2%
[
children 5%
]
); abdominal pain (2%
[
children 3%
]
);
diarrhea (2%).
|
|
hematologic:
Leukopenia (including neutropenia and agranulocytosis); thrombocytopenia.
|
|
hepatic:
Hepatitis; cholestasis; fulminant hepatitis.
|
Precautions: |
|
|
Pregnancy:
Category C
.
|
|
Lactation:
Excreted in breast milk.
|
|
Children:
An open-label, randomized, controlled trial has shown fluconazole to be effective in children 6 mo to 13 yr of age. Efficacy has not been established in infants younger than 6 mo of age.
|
|
Renal function impairment:
Dosage reduction based on CrCl may be necessary.
|
|
Anaphylaxis
Anaphylaxis occurred rarely.
|
|
Dermatologic changes
Exfoliative skin disorders reported.
|
|
Hepatic injury
Monitor patients with abnormal LFT results for development of more severe hepatic injury.
|
|
Immunocompromised patients
To prevent relapse, patients with AIDS and cryptococcal meningitis usually require maintenance therapy.
|
Overdosage: |
Signs & symptoms
Hallucinations, paranoid behavior.
|
Patient/Family Education: |
- Advise patient to read patient information leaflet before starting therapy and with each refill.
- Review dosing schedule and prescribed length of therapy with patient. Advise patient that treatment may be prolonged (eg, several weeks or months)
and to continue medication until advised to stop using by health care provider.
- Advise patient that tablets can be taken with a full glass of water without regard to meals but to take with food if GI upset occurs.
- Advise patient using suspension that the suspension can be taken without regard to meals but to take with food if GI upset occurs.
- Advise patient or caregiver to shake suspension well before measuring dose and to measure prescribed dose of suspension using dosing cup, spoon, or syringe.
- Advise patient that if a dose is missed, to take as soon as remembered. However, if it is nearing the time for the next dose, to skip the dose and take the next dose at the regularly scheduled time.
- Remind patient to complete entire course of therapy, even if symptoms of infection have disappeared.
- Advise patient to inform health care provider if infection does not improve or worsens.
- Advise patient to contact health care provider immediately if skin rash, persistent nausea or vomiting, dark urine, or yellowing of skin or eyes occur.
- Advise patient that medication will be prepared and administered by a health care professional in a health care setting when oral therapy is not feasible, but that the patient will be switched to oral therapy when health care provider believes it is appropriate.
|
 |
|