Capsule Presentation

Each hard gelatin capsule contains:
Itraconazole Pellets           100 mg
(eq. to Itraconazole)

Itraconazole is one of the triazole antifungal agents that inhibit cytochrome P-450-dependent enzymes resulting in impairment of ergosterol synthesis, a major component of fungal cell wall. It has been used in conditions like, blastomycosis, cryptococcal meningitis & aspergillosis. It is used for the treatment of the fungal infections in immunocompromised and non-immunocompromised patients.

Indications

• Coccidioidal meningitis
• Dermatomycoses
• Infections, Fungal
• Oropharyngeal Candidiasis
• Pulmonary coccidioides
• Vulvovaginal Candidiasis

Mechanism of action

Itraconazole is a selectively inhibits enzyme 14-α-demethylase and this enzyme is responsible to convert lanosterol to ergosterol, which is necessary for fungal cell wall synthesis. The free nitrogen atom located on the azole ring of fluconazole binds with a single iron atom located in the heme group of lanosterol 14-α-demethylase. This prevents oxygen activation and, as a result, inhibits the demethylation of lanosterol, halting the process of ergosterol biosynthesis. These accumulated sterols negatively affect the structure and function of the fungal cell plasma membrane.

It is absorbed from GIT with bioavailability of 55%. Volume of distribution is 796 L with 99.8% protein binding. Itraconazole is extensively metabolised in liver and about 40% of the inactive metabolites are excreted in urine. Only 3-18% of the drug is excreted in feces. The half-life of itraconazole is 21 hours.

Side Effects

• Headache
• Diarrhea
• Nausea or upset stomach
• Dizziness
• Stomach pain
• Vomiting
• Unusual or unpleasant taste
• Erection problems

Contraindication

• Chronic kidney disease
• Chronic heart failure
• Hearing loss
• Peripheral neuropathy