fluconazole (Diflucan)

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Introduction

Tradename: Diflucan.

Indications

Contraindications

Pregnancy category: D[6]

pregnancy category = c

safety in lactation = -

Dosage

100-400 mg IV/PO QD

Candidiasis: 200 mg IV/PO first day, then 100-200 mg QD.

Cryptococcal meningitis: 400 mg IV 1st day, then 200-400 mg QD.

Vaginal candidiasis: 150 mg single dose.

Tabs: 50, 100, 150, 200 mg.

Suspension: 10 & 40 mg/mL.

Injection: 2 mg/mL (100 mL, 200 mL) Maximum dose: > 2 g/day. Dose adjustment in renal failure:

Creatinine clearance dose
> 50 mL/min 100%
20-49 mL/min* 50%
10-19 mL/min 25%
post-dialysis 100%

* same dose for continuous arteriovenous hemofiltration

Pharmacokinetics

elimination via kidney

1/2life = 24-30 hours

protein binding = 11-12 %

Antimicrobial activity

Antifungal activity:

Adverse effects

Drug interactions

* may predispose to torsades de pointes; DO NOT administer concurrently

Laboratory

Mechanism of action

More general terms

Additional terms

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  5. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
  6. 6.0 6.1 FDA MedWatch: 08/03/2011 Diflucan (fluconazole): Drug Safety Communication - Long-term, High-dose Use During Pregnancy May Be Associated With Birth Defects http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm266468.htm
  7. 7.0 7.1 Molgaard-Nielsen D et al. Use of oral fluconazole during pregnancy and the risk of birth defects. N Engl J Med 2013 Aug 29; 369:830 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23984730 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1301066
  8. 8.0 8.1 8.2 8.3 8.4 8.5 Deprecated Reference
  9. 9.0 9.1 Molgaard-Nielsen D, Svanstrom H, Melbye M, Hviid A, Pasternak B. Association Between Use of Oral Fluconazole During Pregnancy and Risk of Spontaneous Abortion and Stillbirth. JAMA. 2016;315(1):58-67 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/26746458 <Internet> http://jama.jamanetwork.com/article.aspx?articleid=2480487
  10. 10.0 10.1 10.2 FDA Safety Alert. April 26, 2015 Fluconazole (Diflucan): Drug Safety Communication - FDA Evaluating Study Examining Use of Oral Fluconazole (Diflucan) in Pregnancy. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm497656.htm
  11. 11.0 11.1 11.2 Molgaard-Nielsen D, Svanstrom H, Melbye M et al Association Between Use of Oral Fluconazole During Pregnancy and Risk of Spontaneous Abortion and Stillbirth. JAMA. 2016;315(1):58-67. PMID: https://www.ncbi.nlm.nih.gov/pubmed/26746458 https://jamanetwork.com/journals/jama/fullarticle/2480487

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