Fluconazole

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FLUCONAZOLE

Fluconazole 3

1.       TYPE OF DRUG- FLUCONAZOLE
Fluconazole, a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis.

 

2.       INDICATIONS (USE)- FLUCONAZOLE
Fluconazole is used to treat fungal infections, including yeast infections of the vagina, mouth, throat, esophagus (tube leading from the mouth to the stomach), abdomen (area between the chest and waist), lungs, blood, and other organs. Fluconazole is also used to treat meningitis (infection of the membranes covering the brain and spine) caused by fungus.

 

3.       MECHANISM OF ACTION (MOA) – 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.

 

4.       ROUTES OF ADMINISTRATION – FLUCONAZOLE
Fluconazole comes as a tablet and a suspension (liquid) to take by mouth.

 

5.       ONSET OF EFFECT OR ACTION – FLUCONAZOLE
It begins to work within a few hours, but full beneficial effects may tack several days up to 6-8 weeks.

 

6.       DOSAGE (DOSING INFORMATION) – FLUCONAZOLE
The recommended dosage of fluconazole for vaginal candidiasis is 150 mg as a single oral dose.

 

7.       HALF LIFE (DURATION OF ACTION) – FLUCONAZOLE
30 hours (range 20-50 hours)

 

8.       ADVERSE EFFECTS OR SIDE EFFECTS – FLUCONAZOLE
·         nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);

·         fever, chills, body aches, flu symptoms;

·         severe blistering, peeling, and red skin rash.

 

9.       CONTRAINDICATIONS – FLUCONAZOLE
Fluconazole is contraindicated in patients who have shown hypersensitivity to fluconazole or to any of its excipients. There is no information regarding cross-hypersensitivity between fluconazole and other azole antifungal agents.

 

10.   DRUG INTERACTIONS – FLUCONAZOLE
Fluconazole is a potent inhibitor of cytochrome P450 (CYP) isoenzyme 2C9 and 2C19, and a moderate inhibitor of CYP3A4. In addition to the observed/documented interactions mentioned below, there is a risk of increased plasma concentration of other compounds metabolized by CYP2C9, CYP2C19, and CYP3A4 co-administered with fluconazole.

 

11.    EXCRETION – FLUCONAZOLE
Excretion‎: ‎Renal 61–88%

 

 

Fluconazole 1

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