Diflucan

Di·flu·can (dflkn)

A trademark for the drug fluconazole.

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Diflucan,

trademark for a broad-spectrum antifungal agent (fluconazole).

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fluconazole

Canesten Oral (UK), Diflucan

Pharmacologic class: Synthetic azole

Therapeutic class: Systemic antifungal

Pregnancy risk category C

Action

Alters cellular membrane, increasing permeability and leakage of essential elements needed for fungal growth. At higher concentrations, may be fungicidal.

Availability

Injection: 2 mg/ml in 100- or 200-ml bottles or containers

Powder for oral suspension: 50 mg/5 ml in 35-ml bottle, 200 mg/5 ml in 35-ml bottle

Tablets: 50 mg, 100 mg, 150 mg, 200 mg

⊘Indications and dosages

➣ Oropharyngeal candidiasis

Adults: 200 mg P.O. or I.V. on first day, followed by 100 mg/day for at least 2 weeks

Children: 6 mg/kg P.O. or I.V. on first day, followed by 3 mg/kg/day for at least 2 weeks

➣ Esophageal candidiasis

Adults: 200 mg P.O. or I.V. on first day, followed by 100 mg/day for 3 weeks and then for 2 weeks after symptom resolution. Up to 400 mg/day may be used in severe cases.

Children: 6 mg/kg P.O. or I.V. on first day, followed by 3 mg/kg/day for 3 weeks and for at least 2 weeks after symptom resolution

➣ Systemic candidiasis

Adults: 400 mg P.O. or I.V. on first day, followed by 200 mg/day for 4 weeks and for at least 2 weeks after symptom resolution

Children: 6 to 12 mg/kg/day P.O. or I.V.

➣ Vaginal candidiasis

Adults: 150 mg P.O. as a single dose

➣ Cryptococcal meningitis

Adults: 400 mg P.O. or I.V. on first day, followed by 200 or 400 mg/day for 10 to 12 weeks after cerebrospinal fluid (CSF) is negative

Children: 12 mg/kg P.O. or I.V. on first day, followed by 6 mg/kg/day for 10 to 12 weeks after CSF is negative

➣ Suppression of cryptococcal meningitis in patients with AIDS

Adults: 200 mg/day P.O. or I.V.

➣ To prevent candidiasis after bone marrow transplantation

Adults: 400 mg/day P.O. or I.V. for several days before and 7 days after neutrophil count rises above 1,000 cells/mm³

Dosage adjustment

• Renal impairment
• Elderly patients

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:
• hypersensitivity to other azole antifungals
• renal impairment or hepatic disease
• pregnant or breastfeeding patients
• children younger than 6 months.

Administration

☞ Limit single I.V. infusion to 200 mg/hour or less, using infusion pump.
• Don't piggyback with other I.V. infusions.
• Keep overwrap on I.V. bag until just before use.
• Know that plastic container may be opaque (from moisture absorbed during sterilization). This doesn't affect drug and will decrease over time.

Route	Onset	Peak	Duration
P.O.	Slow	1-2 hr	2-4 days
I.V.	Rapid	1 hr	2-4 days

Adverse reactions

CNS: headache, dizziness

GI: nausea, vomiting, diarrhea, dyspepsia, abdominal discomfort

Hematologic: leukopenia, thrombocytopenia

Hepatic: hepatotoxicity

Skin: rash, pruritus, exfoliative skin disorders (including Stevens-Johnson syndrome )

Other: altered taste, anaphylaxis

Interactions

Drug-drug. Alfentanil, cyclosporine, phenytoin, rifabutin, tacrolimus, theophylline, zidovudine: increased blood levels of these drugs, greater risk of toxicity

Benzodiazepines, buspirone, losartan, nisoldipine, tricyclic antidepressants, zolpidem: increased blood levels and effects of these drugs

CYP3A4 inducers: inhibited CYP3A4 enzyme system, altered actions of CYP3A4 inducers (with fluconazole dosages above 200 mg/day)

Glipizide, glyburide, tolbutamide: increased hypoglycemic effect of these drugs

Rifampin: increased rifampin blood level, decreased fluconazole blood level

Thiazide diuretics: increased fluconazole blood level

Warfarin: increased warfarin activity

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, bilirubin, gamma-glutamyltransferase, hepatic enzymes: increased levels

Platelets, white blood cells: decreased counts

Patient monitoring

☞ Stay alert for signs and symptoms of anaphylaxis. Stop drug immediately if these occur.
• Monitor liver function test results and hematologic studies.
☞ Assess for rash; if lesions develop, monitor patient. Stop drug and notify prescriber if lesions progress (may signal Stevens-Johnson syndrome).
• Be aware that patients with human immunodeficiency virus have greater risk of adverse reactions.

Patient teaching

☞ Teach patient how to recognize and immediately report signs and symptoms of allergic response.
• Urge patient to contact prescriber if rash occurs, to determine whether Stevens-Johnson syndrome is developing.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Advise patient to minimize GI upset by eating frequent, small servings of food and drinking adequate fluids.
• Tell female patient to inform prescriber if she is pregnant or breastfeeding.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

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Diflucan®

Fluconazole, see there