IKE 100 CAPSULES (Each hard gelatin capsule contains Hraconazole 100mg)

Indications

• Aspergillosis
• Blastomycosis
• Candidiasis (systemic and oral)
• Coccidioidomycosis
• Histoplasmosis
• Onychomycosis
• Tinea infections (dermatophyte infections)

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines based on the child's age and weight.

Adults: Dosage varies based on the specific infection and severity. Refer to specific guidelines for detailed dosing information.

Mechanism of action

Itraconazole works by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. This inhibition occurs through the blockade of the enzyme lanosterol 14-alpha-demethylase, which is crucial for converting lanosterol to ergosterol. The resultant disruption of the fungal cell membrane leads to increased permeability and ultimately, cell death.

Pharmacodynamics

Itraconazole exhibits fungistatic and fungicidal properties depending on the concentration relative to the minimum inhibitory concentration (MIC) of the target organism. It is effective against a broad spectrum of fungi, particularly in its ability to penetrate tissues and achieve therapeutic concentrations in various body fluids.

Pharmacokinetics

Itraconazole is well absorbed from the gastrointestinal tract, though its absorption is significantly enhanced when taken with food. It undergoes extensive hepatic metabolism, primarily via cytochrome P450 3A4, leading to the formation of active metabolites. The elimination half-life is approximately 24 hours, allowing for once-daily dosing in many cases. Itraconazole is primarily excreted in urine and feces.

Contra-indications

• Hypersensitivity to itraconazole or any component of the formulation
• Concurrent use with certain medications such as cisapride, dofetilide, or ergot alkaloids due to the risk of serious cardiac events

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Headache
• Dizziness
• Liver enzyme elevation
• Skin rash
• Anaphylaxis
• Heart failure in patients with pre-existing cardiac conditions

Interactions

• May increase plasma concentrations of certain drugs metabolized by CYP3A4, including statins, benzodiazepines, and calcium channel blockers
• Concomitant use with drugs that have a high potential for QT prolongation should be approached with caution

Precautions

• Use cautiously in patients with a history of liver disease, heart failure, or renal impairment
• Monitor liver function tests periodically during therapy
• Consider potential drug-drug interactions, especially in polypharmacy situations

Pregnancy

Category C. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether itraconazole is excreted in human milk. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Capsules
• Oral solution