Itraconazole Drug Information PDF

Overview of the Drug Class **Prototype: itraconazole (Sporanox) ** - **Category**: Azole Antifungal Agents  - **Primary Function**: Similar to amphotericin B, the azoles are broad-spectrum antifungal drugs.    - **Unique Features**: Azoles such as Itraconazole provide an alternativ...

Overview of the Drug Class **Prototype: itraconazole (Sporanox) ** - **Category**: Azole Antifungal Agents  - **Primary Function**: Similar to amphotericin B, the azoles are broad-spectrum antifungal drugs.    - **Unique Features**: Azoles such as Itraconazole provide an alternative to amphotericin B for treating systemic mycoses. Azoles have lower toxicity than amphotericin b and can be administered by mouth.   Mechanism of Action Itraconazole inhibits the synthesis of ergosterol (sterol), resulting in increased membrane permeability and leakage of cellular components.    **Title: Mechanism of antifungal drugs** - Cell wall - Cell membrane - DNA - Proteins - Echinocandins, triterpenoids - Azoles, polyenes, allylamines - 5-fluorocytosine - Sordarins   Indications and Therapeutic Uses - **Systemic Fungal Infections**: Itraconazole is active against a broad spectrum of fungal pathogens. It is considered first-line therapy for blastomycosis, histoplasmosis, paracoccidioidomycosis, and sporotrichosis and is an alternative to amphotericin b for aspergillosis, candidiasis and coccidioidomycosis.   - **Superficial Fungal Infections**: Itraconazole can also treat superficial mycoses. Side Effects and Adverse Reactions **Side Effect** **Description** --------------------- -------------------------------------------------------------------------------------------------------- GI Upset Nausea, vomiting, and diarrhea are common. Cardiac Suppression Itraconazole has a negative inotropic action that can cause a transient decrease in ejection fraction. Hepatic Injury Itraconazole has been associated with rare incidents of hepatic failure resulting in fatalities. Precautions and Contraindications **Precautions** - Use caution in clients with hepatic dysfunction.  - Use with caution in heart failure and only when the benefit outweighs the risk.  **Black Box Warning** - Itraconazole should not be used to treat superficial mycoses in clients with heart failure, a history of heart failure, or other indications of ventricular dysfunction.  Drug Interactions - Since **\[proton pump inhibitors\] **have a prolonged duration of action, clients using these agents may have insufficient stomach acid content for itraconazole absorption.  - Itraconazole is a **\[CYP3A4 Inhibitor\]** and can increase levels of many other drugs, including **\[cisapride, pimozide, dofetilide, and quinidine\]** which can increase the risk of **\[fatal ventricular dysrhythmias\]**. Other drugs influenced by CYP3A4 inhibition include **\[cyclosporine, digoxin, warfarin, and sulfonylureas\]**.  - Drugs that raise gastric pH, such as **\[antacids, H2 antagonists, and proton pump inhibitors\]** can reduce the absorption of oral Itraconazole. Administer these agents at least 1 hour before itraconazole or 2 hours after.  Dosing, Administration, & Client Teaching **Dosing** - Dosing varies based on the condition, severity, and client response.  - Check drug dosing guidelines for individualized dosing.  - Itraconazole is available for PO use in suspension (10mg/ml) and capsules (100 mg). Capsules should be taken with food or cola (cola enhances absorption).    - Recommended dose is 200 mg once daily and can be increased to 200 mg twice daily if needed.  **Administration** - Oral administration. **Client Teaching** - Educate clients about symptoms of hepatic insufficiency (persistent nausea, anorexia, fatigue, vomiting, RUQ pain, jaundice, dark urine, pale stools) and seek medical attention immediately if those symptoms occur.  Labs to Monitor **Basic Metabolic Panel** - Monitor the blood glucose levels of clients taking sulfonylureas with itraconazole as hypoglycemia can occur.  **Coagulation Studies** - Monitor PT/INR for clients taking warfarin with itraconazole, as excessive anticoagulation can occur.  **Serum Drug Levels** - Monitor drug levels of cyclosporine and digoxin for clients also taking itraconazole.