Fluconazole; Uses, Dosage, Side Effects, Interactions, Pragnancy

Fluconazole
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Fluconazole is a synthetic triazole with antifungal activity. Fluconazole preferentially inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols, the loss of normal fungal sterols, and fungistatic activity. Mammalian cell demethylation is much less sensitive to fluconazole inhibition.

Fluconazole is an Azole Antifungal. The mechanism of action of fluconazole is as a Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inhibitor. The chemical classification of fluconazole is Azoles.

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Fluconazole is a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis. It inhibits the fungal lanosterol 14 alpha-demethylase which thereby prevents the formation of ergosterol which is an essential component in the fungal cell membrane. It is used for a number of fungal infections.This includes candidiasis, blastomycosis, coccidiodomycosis, cryptococcosis, histoplasmosis, dermatophytosis, and pityriasis versicolor. It is also used to prevent candidiasis in those who are at high risk such as following organ transplantation, low birth weight babies, and those with low blood neutrophil counts.

Mechanism of action of Fluconazole 

Fluconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Fluconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Indications of Fluconazole 

  • Vaginal Yeast Infection
  • Candida Urinary Tract Infection
  • Bone Marrow Transplantation
  • Chronic Mucocutaneous Candidiasis
  • Fungal Infection, Internal and Disseminated
  • Blastomycosis
  • Candidemia
  • Coccidioidomycosis
  • Coccidioidomycosis, Meningitis
  • Cryptococcal Meningitis, Immunocompetent Host/Immunosuppressed Host
  • Cryptococcosis
  • Esophageal Candidiasis
  • Fungal Infection Prophylaxis
  • Fungal Peritonitis
  • Fungal Pneumonia
  • Histoplasmosis
  • Onychomycosis, Fingernail
  • Onychomycosis, Toenail
  • Oral Thrush
  • Sporotrichosis
  • Systemic Candidiasis
  • Tinea Corporis
  • Tinea Cruris
  • Tinea Versicolor
  • Candida intertrigo
  • Candida pneumonia
  • Candidemia
  • Esophageal Candidiasis
  • Infections, Fungal
  • Meningitis, Cryptococcal
  • Oropharyngeal Candidiasis
  • Peritoneal candidiasis
  • Pneumonia cryptococcal
  • Vaginal Candidiasis
  • Candidiasis infection
  • Disseminated Candidiasis
  • Urinary tract candidiasis
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Therapeutic Indications

  • For the treatment of fungal infections.
  • Diflucan is indicated in the following fungal infections in adults:
  • Acute vaginal candidiasis when local therapy is not appropriate.
  • Candidal balanitis when local therapy is not appropriate.

Contraindications of Fluconazole 

  • have known hypersensitivity to other azole medicines such as ketoconazole;
  • are taking terfenadine, if 400 mg per day multidose of fluconazole is administered;
  • concomitant administration of fluconazole and quinidine, especially when fluconazole is administered in high dosages;
  • take SSRIs such as fluoxetine or sertraline.

Dosage of Fluconazole 

Strengths

Injected solution

  • 2mg/mL

Oral suspension

  • 10mg/mL ,40mg/mL

Tablets

  • 50mg ,100mg ;150mg ;200mg

Vaginal Candidiasis

  • 150 mg orally as a single dose

Infectious Diseases Society of America (IDSA) Recommendations

  • Uncomplicated vaginitis: 150 mg orally as a single dose
  • Management of recurrent vulvovaginal candidiasis (after 10 to 14 days induction therapy): 150 mg orally once a week for 6 months
  • Complicated vulvovaginal candidiasis: 150 mg orally every 72 hours for 3 doses

US CDC Recommendations

  • Uncomplicated vulvovaginal candidiasis: 150 mg orally as a single dose
  • Initial therapy for recurrent vulvovaginal candidiasis: 100 to 200 mg orally every 72 hours for 3 doses
  • Maintenance therapy for recurrent vulvovaginal candidiasis: 100 to 200 mg orally once a week for 6 months
  • Severe vulvovaginal candidiasis: 150 mg orally every 72 hours for 2 doses

US CDC, National Institutes of Health (NIH), and IDSA Recommendations for HIV-infected Patients

  • Uncomplicated vulvovaginal candidiasis: 150 mg orally as a single dose
  • Severe or recurrent vulvovaginal candidiasis: 100 to 200 mg orally once a day for at least 7 days
  • Suppressive therapy for vulvovaginal candidiasis: 150 mg orally once a week

Oral Thrush

  • Oropharyngeal candidiasis: 200 mg IV or orally on the first day followed by 100 mg IV or orally once a day
  • Duration of therapy: At least 2 weeks, to reduce the risk of relapse

IDSA Recommendations

  • Moderate to severe oropharyngeal candidiasis: 100 to 200 mg IV or orally once a day for 7 to 14 days

US CDC, NIH, and IDSA Recommendations for HIV-infected Patients

  • Initial episodes of oropharyngeal candidiasis: 100 mg orally once a day for 7 to 14 days
  • Suppressive therapy for oropharyngeal candidiasis: 100 mg orally once a day or 3 times a week

Candidemia

  • Doses up to 400 mg/day have been used.

 Fungal Pneumonia

  • Doses up to 400 mg/day have been used.

Fungal Infection – Disseminated

  • Doses up to 400 mg/day have been used.
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Systemic Candidiasis

  • Doses up to 400 mg/day have been used.

Esophageal Candidiasis

  • 200 mg IV or orally on the first day followed by 100 mg IV or orally once a day
  • Duration of therapy: At least 3 weeks and for at least 2 weeks after symptoms resolve

Side Effects of Fluconazole 

The most common 

Common

Rare

Drug Interactions of Fluconazole 

Kitoconazole may interact with following drugs, supplements & may change the efficacy of drugs

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Pregnancy & Lactation of Fluconazole 

US FDA pregnancy category C

Pregnancy 

Most scientific studies suggest that a single 150mg dose of fluconazole during pregnancy will not harm a baby in the womb. Thrush is very common in pregnancy. If you think you have thrush it is best to consult your doctor or midwife who will advise you as to whether treatment is recommended.

Lactation

Fluconazole passes into breast milk and may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this drug. This medication shouldn’t be used in people younger than 6 months.

References

Fluconazole

 

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