fluconazole


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fluconazole

 [floo-kon´ah-zōl]
a triazoleantifungal agent used in the systemic treatment of candidiasis and cryptococcal meningitis.
Miller-Keane Encyclopedia and Dictionary of Medicine, Nursing, and Allied Health, Seventh Edition. © 2003 by Saunders, an imprint of Elsevier, Inc. All rights reserved.

fluconazole

Apo-Fluconazole (CA), Canesten Oral (UK), Co Fluconazole (CA), Diflucan, Dom-Fluconazole (CA), Gen-Fluconazole (CA), Novo-Fluconazole (CA), PHL-Fluconazole (CA), PMS-Fluconazole (CA), Riva-Fluconazole (CA)

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

Candidal urinary tract infection; peritonitis

Adults: 50 to 200 mg P.O. or I.V. daily

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

• Concurrent use of terfenadine (not available in U.S.) in patients receiving fluconazole at multiple doses of 400 mg or higher and other drugs known to prolong QT interval and that are metabolized via CYP3A4, such as cisapride, astemizole (not available in U.S.), pimozide, and quinidine

Precautions

Use cautiously in:

• hypersensitivity to other azole antifungals

• renal impairment or hepatic disease

• potentially proarrhythmic conditions

• concurrent use of erythromycin because of potential for increased risk of prolonged QT interval, torsades de pointes, and consequently sudden death (avoid use)

• 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.

• Be aware that powder for oral suspension contains sucrose and shouldn't be used in patients with hereditary fructose intolerance, glucose-galactose malabsorption, and sucrase-isomaltase deficiency.

Adverse reactions

CNS: headache, dizziness

CV: QT interval prolongation, torsades de pointes

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; discontinue drug if clinical signs and symptoms consistent with liver disease develop that may be attributable to fluconazole.

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.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved

fluconazole

(flo͞o-kŏn′ə-zōl′, -kō′nə-)
n.
A broad-spectrum antifungal agent, C13H12F2N6O, administered either orally or by injection and used especially to treat systemic candidiasis and cryptococcosis.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.

fluconazole

Diflucan® Infectious disease An antifungal used as a first-line therapy for mucocutaneous and systemic candidiasis, cryptococcal meningitis, and prophylaxis for BM recipients Adverse effects Hepatotoxicity, anaphylaxis, gastric pain, rashes especially in immunocompromised Pts.
McGraw-Hill Concise Dictionary of Modern Medicine. © 2002 by The McGraw-Hill Companies, Inc.

fluconazole

A triazole antifungal drug that can be taken by mouth and used to treat generalized fungus infections. Vaginal thrush can be cleared with a single dose. The drug is well tolerated, has few side effects and is highly effective but injudicious use may lead to the development of drug resistance. The drug is on the WHO official list. A brand name is Diflucan.
Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005

antifungal agent 

Any substance which destroys or prevents the growth of fungi. It is one of the antibiotic groups. There are several classes of antifungal drugs: Polyenes, which cause an increase in fungal cell wall permeability leading to its death. Examples: amphotericin B, natamycin, nystatin. Azoles, which act either by inhibiting the synthesis of ergosterol, a component of fungal cell wall or by causing direct wall damage. Examples: clotrimazole, econazole, fluconazole, itraconazole, ketoconazole, miconazole. Pyrimidines, which interfere with the normal function of fungal cells. Example: flucytosine. Syn antimycotic agent.
Millodot: Dictionary of Optometry and Visual Science, 7th edition. © 2009 Butterworth-Heinemann
References in periodicals archive ?
For all tested Candida strains [MIC.sub.50] and [MIC.sub.90] values for fluconazole were found to be 0.125 [micro]g/mL-0.25 [micro]g/mL while they were determined as 0.125 [micro]g/mL-64 [micro]g/mL and 0.125 [micro]g/mL-0.125 [micro]g/mL for green tea and quince leaves, respectively.
They found that taking oral fluconazole was linked to adverse outcomes.
Table 3 Susceptibility difference of ketoconazole, fluconazole, and miconazole.
guillermondii 2(1.5) Mixed infections 3 (8.3) 6 (4.5) Total 36 (27.4) 131 (100) Table 3--Susceptibility to fluconazole in monomicrobial isolates identified by E-test with the 2008 and 2012 breakpoints.
[8] Fluconazole is one of the most common drugs used in dermatological and gynecological practice.
Patients in Group A were put on 1% Clotrimazole ear drops and those in Group B were put on 0.3% Fluconazole ear drops in the dosage of 3 drops thrice daily.
The secondary endpoint of study was assessing the side effects of fluconazole and terbinafine.
The card of Vitek[R] 2--AST--YS01 (Lote 281223610), suitable for the realization of antifungal sensitivity tests are disposable and has four drugs at different concentrations (different dilutions): flucytosine (sensitivity [less than or equal to] 1 [micro]g/mL), voriconazole (sensitivity 0.125 [micro]g/mL, intermediate sensitivity 2 to 4 [micro]g/mL, resistant [greater than or equal to] 4 [micro]g/mL), amphotericin B (sensitivity [less than or equal to] 0.25 [micro]g/mL, intermediate sensitivity 4 to 8 [micro]g/mL, resistant [greater than or equal to] 16 [micro]g/mL) and fluconazole (sensitivity [less than or equal to] 2 [micro]g/mL, intermediate sensitivity 14 to [greater than or equal to] 32 [micro]g/mL, resistant [greater than or equal to] 64 [micro]g/mL).
Thus, quaternization of N-4 position of triazole ring in fluconazole produced the corresponding triazolium compounds, which demonstrated promising antibacterial potential [19].
Unlike bacterial and viral meningitis, adjunctive corticosteroid therapy is contraindicated for the management of CM and treatment is always long-term consisting of three phases: 2 weeks of induction therapy with amphotericin B plus flucytosine, and a further 8-10 weeks of consolidation with fluconazole 400-800mg daily followed by long-term fluconazole (200mg daily) therapy for maintenance phase, also known as secondary prophylaxis for at least 1 year [46].