Itrasel 200mg (Itraconazole)

Itrasel 200 mg (Itraconazole): Detailed Overview

Generic Name: Itraconazole

Brand Name: Itrasel

Drug Class: Azole Antifungal

What is Itraconazole?

Itraconazole is an all-encompassing antifungal azole that is employed for treating a range of fungal illnesses. It’s powerful against dermatophytes and yeasts as well as mold. It does this by inhibiting the synthesis of fungal cell membranes and thus halting the growth of fungal cells.

Mechanism of Action

Itraconazole hinders the enzyme of fungal origin, the lanosterol 14α-demethylase, which is one of the cytochrome P450 processes. The enzyme is responsible for the conversion of lanosterol into Ergosterol, which is a vital part of the fungal cell membrane.

• The inhibition of ergosterol synthesis can result in:
  • Fungal cell membrane disruption Integrity
  • The permeability of the membrane is increased
  • Inhibited fungal cell growth and replication

Indications

Itraconazole is employed to treat many fungal diseases, such as:

• Onychomycosis (fungal nail infections)
• Dermatophytosis (ringworm, tinea infections)
• Candidiasis (oral thrush, esophageal candidiasis)
• Histoplasmosis
• Blastomycosis
• Aspergillosis (some cases)
• Fungal infections that are resistant to all other treatments

Dosage and Administration

• Standard dose: Most commonly, 200 mg is taken once each day. However, this dosage is able to be altered based on the type of infection and its severity.
• For onychomycosis: usually 200 mg at least every day for 6 to 12 weeks.
• Dosing and time of administration may vary. Sometimes, it’s best to start with an initial dose of.
• Taken in conjunction with food to improve absorption.
• Capsules/tablets must be swallowed completely by drinking a glass of water.
• Do not take an acid blocker, antacids, or proton pump inhibitors in the same order because they can reduce stomach acid and hinder absorption.

Pharmacokinetics

• Absorption: Variable. Enhanced when taken with food or in an acidic stomach atmosphere
• Bioavailability: Around 55% when combined with food
• Peak plasma concentration: 3 to 5 hours following oral dosage
• Protein binding: High (~99%)
• Half-life: ~24-42 hours (depending on dosing)
• Metabolism: Hepatic via CYP3A4
• Excretion: Mainly via feces

Side Effects

Common side effects:

• Gastrointestinal upset (nausea, vomiting, diarrhea)
• Headache
• Dizziness
• Rash or itching

Serious but rare side effects:

• Hepatotoxicity (Check for changes in liver function)
• Congestive heart failure (Exacerbation of predisposed patients)
• QT prolongation (Risk of arrhythmias)
• Allergic reactions (including Stevens-Johnson syndrome)

Contraindications

• Hypersensitivity to itraconazole as well as other antifungals containing azole
• Patients suffering from congestive heart failure or a history of heart failure (due to the negative effects of inotropics)
• The use of concurrently with certain drugs is not advised because of serious interactions (e.g., Cisapride, cisapride quinidine, etc).

Drug Interactions

Itraconazole is an effective inhibitor of the CYP3A4 enzyme that can cause a myriad of interactions between drugs:

• Statins (e.g., simvastatin) — increased risk of myopathy/rhabdomyolysis
• Benzodiazepines (e.g., midazolam) — increased sedation
• Calcium channel blockers — risk of hypotension and edema
• Warfarin — enhanced anticoagulant effects; track INR
• Digoxin — Higher levels, be sure to monitor them carefully
• Rifampin, carbamazepine, phenytoin — lower levels of itraconazole (avoid or check)
• Antacids, H2 blockers, PPIs — reduce itraconazole absorption

Precautions

• Take care when administering this medicine to patients with an impairment of the liver. Monitor your liver enzymes regularly.
• Be cautious when treating those with a heart condition.
• It is not recommended to use this method in the course of pregnancy unless the benefits outweigh the risks.
• Children are not extensively studied in this regard and are only used when clear indications are given.

Storage

• Keep in a dry, cool place far from direct sunlight.
• Make sure that the area is safe for young children.

Summary Table