Rx Product Guide

   
   
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Fluconazole (flew-KOE-nuh-zole)
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.


   
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