fluconazole

medtigo

fluconazole

Brand Name :

diflucan

Synonyms :

fluconazole, fluconazol

Class :

Antifungal

Action and Spectrum

Mechanism of action

It is a triazole antifungal drug that inhibits the synthesis of ergosterol, a key component of fungal cell membranes. This leads to a reduction in fungal cell membrane permeability, causing fungal cell death.

Spectrum

It has a broad spectrum of activity against various fungal species, including Candida and Cryptococcus, making it effective against a wide range of fungal infections, including thrush, esophageal candidiasis, and systemic candidiasis.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined:

>10%

headache

1-10%

Abdominal pain

Rash

Nausea

Diarrhea

vomiting

Frequency undefined

Anaphylactic reaction

Cholestasis

Dyspnea

Hepatitis

Hypokalemia

Increased ALT/AST

Leukopenia

Seizures

Taste perversion

Toxic epidermal necrolysis

QT prolongation

Alopecia

Angioedema

Dizziness

Hepatic failure

Jaundice

Black Box Warning

Contraindication / Caution

Contraindications

Hypersensitivity to fluconazole or other azole antifungal drugs
Liver dysfunction
Pregnancy and breastfeeding
Concomitant use with certain medications, such as cisapride, terfenadine, astemizole, pimozide, and quinidine.
Age less than six months old
Known hereditary degenerative retinal disorders.

Caution

Use caution in patients with heart disease, kidney or liver disease, or compromised immune systems.
It may cause adverse effects such as nausea, vomiting, diarrhea, headache, rash, abdominal pain, and hepatic dysfunction.
It may interact with other medications, such as blood thinners, oral contraceptives, and anti-seizure medications.
It may cause an increased risk of abnormal heartbeats and a rare but potentially life-threatening skin reaction called Stevens-Johnson syndrome.
Long-term use may lead to the development of drug-resistant fungal strains.

Pregnancy / Lactation

Pregnancy consideration: It may be harmful to a developing fetus and should only be used during pregnancy if the potential benefits outweigh the potential risks to the fetus

Lactation: Excretion of the drug in human breast milk is known

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

It is a highly selective inhibitor of the fungal cytochrome P-450-dependent enzyme lanosterol 14-alpha-demethylase. This inhibition leads to the loss of normal sterols in fungi, which results in the accumulation of 14 alpha-methyl sterols. This accumulation is thought to be responsible for the fungistatic (stops fungal growth) activity of fluconazole. By blocking the growth of fungi, fluconazole helps treat various fungal infections, including yeast infections, thrush, and other fungal skin infections.

Pharmacodynamics

It specifically targets the cytochrome P-450-dependent enzyme lanosterol 14-alpha-demethylase, which is involved in the biosynthesis of ergosterol, a component of fungal cell membranes. By blocking the production of ergosterol, fluconazole disrupts the fungal cell membrane and leads to fungal cell death.

In addition to its fungistatic effect, fluconazole also has a long half-life, which allows for once-daily dosing and higher levels of drug exposure in the body. This increased exposure helps to achieve and maintain therapeutic levels of the drug in the bloodstream, which is essential for the effective treatment of fungal infections.

Pharmacokinetics

Absorption

It is well absorbed with oral bioavailability of over 90%. It reaches peak plasma levels in 1-2 hours after oral administration.

Distribution

It is widely distributed in the body with good penetration into various tissues and fluids, including cerebrospinal fluid (CSF), eye, peritoneal fluid, sputum, urine, and skin. It is only 11-12% protein bound in the blood.

Metabolism

It undergoes some liver metabolism, partially inhibited by CYP2C9 and CYP3A4

Elimination/excretion

The half-life of fluconazole is 30 hours, with a range of 20-50 hours, and it is slightly longer in the elderly. Excretion is mainly through the urine, with 80% excreted as an unchanged drug and 11% as metabolites.

Adminstartion

Administration

Intravenous administration

IV administration should be done as a 1–2-hour infusion.
The maximum infusion rate is 200 mg/hr.
The IV infusion should not be connected in series with other infusions to prevent air embolism.

Storage

The tablets should be stored at temperatures below 86°F (30°C).
The dry powder form should also be stored below 86°F (30°C), and reconstituted suspension should be stored between 41-86°F (5-30°C). The unused portion should be discarded after two weeks and protected from freezing.
The fluconazole injection in glass bottles should be stored between 41-86°F (5-30°C) and protected from freezing.
The fluconazole injection in Viaflex Plus plastic containers should be stored between 41-77°F (5-25°C) and protected from freezing.

Patient Information Leaflet

Patient information leaflet

Generic Name: fluconazole

Pronounced: [ floo-KOE-na-zole ]

Why do we use fluconazole?

It is a medication used to treat various fungal infections, including:

Yeast infections of the mouth, throat, esophagus, abdomen, lung, blood, and other organs.
Cryptococcal meningitis (an infection of the covering of the brain and spinal cord)
Fungal nail infections
Vaginal yeast infections
Peritonitis (inflammation of the lining of the abdomen)
Systemic candidiasis (a severe fungal infection that affects the blood and other parts of the body)

fluconazole

No data available for drug.

DRUG INTERACTION

fluconazole

&

fluconazole +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

fluconazole

No data available for drug.

DRUG INTERACTION

fluconazole

&

fluconazole +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

fluconazole

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet