ITRAZOL 100/MG CAP 15/CAP

Indications

Approved Uses

Approved uses (vary by local label) include: onychomycosis (fingernail/toenail), oropharyngeal and esophageal candidiasis, and systemic mycoses such as aspergillosis, blastomycosis, and histoplasmosis; superficial dermatophyte infections (e.g., tinea corporis/cruris/pedis/versicolor) and vulvovaginal candidiasis may be labeled in some jurisdictions but are not universally approved for every product.

Off-Label Uses

Common off-label uses include: coccidioidomycosis, cutaneous/lymphocutaneous sporotrichosis (where not labeled), chromoblastomycosis, paracoccidioidomycosis, and prophylaxis in selected immunocompromised patients (practice varies); note that tinea infections, pityriasis versicolor, and vulvovaginal candidiasis may be labeled in some regions and off-label in others-confirm against the SFDA leaflet for this product.

Dosage & Administration

Dosing by Condition

Typical adult dosing (capsules) per established labeling/guidelines: Oropharyngeal candidiasis 200 mg/day (either 200 mg once daily or 100 mg twice daily) for 1-2 weeks (may extend to 2 weeks); Esophageal candidiasis 200 mg/day for at least 3 weeks and for 2 weeks after symptom resolution (may increase to 400 mg/day if inadequate response); Onychomycosis-Toenail: 200 mg once daily for 12 weeks OR pulse 200 mg twice daily for 1 week per month × 3 pulses; Fingernail: pulse 200 mg twice daily for 1 week per month × 2 pulses; Histoplasmosis/Blastomycosis: often 200 mg three times daily for 3 days then 200 mg twice daily for months (duration depends on severity/site); Aspergillosis: commonly 200 mg twice daily with duration guided by response (often ≥3 months).

Maintenance Dose

100-200 mg once daily depending on indication

Maximum Dose

Typical maximum: 400 mg/day for capsules; higher doses (up to 600 mg/day) may be used short-term in selected severe systemic infections under specialist direction.

Children's Dosage

Not routinely approved for children; limited data available. When used in pediatric patients under specialist supervision: 5 mg/kg/day has been used. Safety and efficacy not established for most indications in children under 12 years

Dose Adjustment Notes

No routine renal dose adjustment is defined, but use caution in renal impairment (capsule absorption may be reduced and exposure can be variable); in hepatic impairment use caution and monitor LFTs closely and consider dose reduction/avoidance in significant liver disease; note formulation differences-capsules with food, oral solution on an empty stomach (if used).

How to Take

Swallow itraconazole 100 mg capsules whole (do not crush/chew/open) and take with a full meal to maximize absorption; if gastric acidity is reduced (e.g., achlorhydria or taking PPIs/H2-blockers/antacids), take with an acidic beverage (e.g., cola) and/or separate antacids by at least 2 hours.

Side Effects

Common Side Effects

Common adverse effects: nausea, vomiting, diarrhea, abdominal pain/dyspepsia, headache, dizziness, rash/pruritus, and elevated liver enzymes; peripheral edema can occur (and is clinically important given the heart failure warning).

Side Effect Frequency

Common (≥1%): GI upset (nausea, abdominal pain, diarrhea, vomiting), headache, rash; hepatic enzyme elevations/hepatitis can occur (frequency varies by dataset) and serious risks include hepatotoxicity and congestive heart failure (rare but clinically critical).

Safety & Warnings

Contraindications

Contraindications include: hypersensitivity to itraconazole; use for onychomycosis in patients with ventricular dysfunction/CHF history; pregnancy for onychomycosis; and coadministration with specific CYP3A4 substrates where increased levels can cause serious events (e.g., cisapride, pimozide, quinidine/dofetilide, oral midazolam/triazolam, ergot alkaloids, simvastatin/lovastatin).

Warnings & Precautions

Key warnings/precautions: CHF/negative inotropy risk (avoid in ventricular dysfunction for non-life-threatening indications); hepatotoxicity-check/monitor LFTs especially with prolonged therapy and stop if symptoms/significant elevations; extensive CYP3A4 interaction screening required; monitor for neuropathy and severe rash; consider electrolyte issues (e.g., hypokalemia) and rare adrenal insufficiency with prolonged use.

Age Restriction

Pediatric use: safety/efficacy not established; if used in children, it should be under specialist supervision (no fixed minimum age in labeling).

Driving Warning

May cause CNS depression, which may impair mental alertness and subsequently impair ability to operate heavy machinery or performing hazardous tasks.

Drug Interactions

Drug Interactions

Major interactions: strong CYP3A4/P-gp inhibition (↑ levels/toxicity of many drugs); contraindicated with cisapride, pimozide, quinidine/dofetilide, oral midazolam/triazolam, ergot alkaloids, simvastatin/lovastatin (and other high-risk CYP3A4 substrates per labeling). Also: ↑ warfarin effect, ↑ digoxin, ↑ calcineurin/mTOR inhibitors (cyclosporine/tacrolimus/sirolimus), ↑ some calcium-channel blockers (edema/CHF risk). Enzyme inducers (rifampin, phenytoin, carbamazepine, etc.) ↓ itraconazole exposure. Acid suppression (antacids/H2RA/PPIs) ↓ capsule absorption.

Interaction Severity

MAJOR/Contraindicated (examples): cisapride, pimozide, quinidine, dofetilide (serious QT/arrhythmia risk); simvastatin/lovastatin (rhabdomyolysis risk); oral midazolam/triazolam (profound sedation/respiratory depression); ergot alkaloids (ergotism). MODERATE/Significant: warfarin (↑INR), digoxin (↑levels), calcium channel blockers (↑edema/CHF risk), cyclosporine/tacrolimus/sirolimus (↑levels), and strong enzyme inducers like rifampin/carbamazepine/phenytoin (↓itraconazole-avoid). Acid suppressants (PPIs/H2 blockers/antacids) reduce capsule absorption (manage by timing/acidic beverage).

Food Interaction

Capsules: take with food (preferably a full meal) to increase absorption; reduced gastric acidity decreases absorption, so an acidic beverage (e.g., cola) can help when acidity is low and acid-suppressing agents should be avoided or separated (antacids by ≥2 hours).

Special Populations

Pregnancy

Use in pregnancy only if benefit outweighs potential risk

Children

Not routinely approved for children; limited data available. When used in pediatric patients under specialist supervision: 5 mg/kg/day has been used. Safety and efficacy not established for most indications in children under 12 years

Elderly

Standard adult dosing; use with caution due to increased risk of drug interactions, cardiac effects, and hepatic impairment. Monitor liver function and cardiac status more closely

Kidney Impairment

Capsules: no routine renal dose adjustment, but use caution in severe renal impairment; avoid oral solution in severe renal impairment due to cyclodextrin vehicle accumulation (not applicable to this capsule product).

Liver Impairment

No specific dose-adjustment algorithm; use with caution in hepatic impairment, avoid in active/significant liver disease when possible, and monitor LFTs-discontinue if hepatotoxicity develops.

Storage & Patient Advice

Missed Dose

Take the missed dose as soon as remembered; if it is close to the next scheduled dose, skip the missed dose and resume the regular schedule-do not double doses.

Stopping the Medicine

Do not stop early; complete the prescribed course and only discontinue early on prescriber advice or if serious adverse effects occur.

Overdose

Overdose: provide supportive care; consider gastric decontamination (activated charcoal ± gastric lavage if early); monitor ECG/electrolytes and liver function; itraconazole is not effectively removed by hemodialysis; seek urgent medical attention.

Patient Counseling

Take capsules with a full meal and swallow whole; complete the prescribed course; avoid/space antacids and discuss PPIs/H2-blockers (may need acidic beverage to aid absorption); report liver injury symptoms (fatigue, anorexia, nausea, dark urine, jaundice) and heart failure symptoms (shortness of breath, swelling, rapid weight gain); check for drug interactions before starting any new prescription/OTC/herbal (major CYP3A4 interactions); for nail infections, improvement is delayed until nail regrowth and may take months after finishing therapy.

Monitoring Requirements

Monitor liver function tests at baseline and periodically during therapy (especially if treatment >1 month or if symptoms occur); assess for signs/symptoms of heart failure (edema, dyspnea, weight gain) and avoid/use extreme caution in CHF; consider therapeutic drug monitoring (itraconazole trough) for severe infections, prolonged therapy, suspected malabsorption, or drug-interaction concerns; monitor electrolytes (e.g., potassium) if clinically indicated.

Pharmacology

Mechanism of Action

Inhibits fungal lanosterol 14-α-demethylase (CYP51), decreasing ergosterol synthesis and disrupting fungal cell membrane integrity (primarily fungistatic, sometimes fungicidal depending on organism/concentration).

Onset of Action

Pharmacokinetic onset: peak concentrations typically occur about 2-5 hours after a capsule dose; clinical response varies-superficial infections may improve within 1-2 weeks, while onychomycosis requires weeks to months with visible improvement as new nail grows.

Duration of Effect

Itraconazole persists in keratinized tissues: drug can remain detectable in nails for months after therapy (clinical effect continues as the nail grows out), while the terminal half-life increases with repeated dosing (approximately 24-42 hours at steady state; longer values have been reported).

Half-Life

Terminal half-life is ~16-28 hours after a single dose and increases with repeated dosing/steady state to roughly ~34-42 hours (can be longer in some sources).

Bioavailability

Itraconazole capsules have variable oral bioavailability (~55%) and absorption is increased when taken with a full meal (food increases exposure); they should be taken with food (unlike the oral solution, which is better fasting).

Metabolism

Extensively hepatically metabolized primarily by CYP3A4; major active metabolite is hydroxy-itraconazole with similar antifungal activity.

Excretion

Excreted mainly as inactive metabolites in feces (~54%) and urine (~35%); unchanged itraconazole in urine is negligible (<0.03%).

Protein Binding

Highly protein bound: ~99.8% (i.e., >99%).

Product Information

Available Dosage Forms

Capsule, Oral solution

Composition per Dose

Each capsule: 100 mg itraconazole (as coated pellets)

Generic Availability

Yes

OTC Alternatives

No OTC alternative for systemic antifungal therapy. Topical OTC antifungals (clotrimazole, miconazole) available for mild superficial skin infections only

Application

Oral

Legal Disclaimer - Al Mujtama Pharmacy

The product information provided is derived from verified pharmaceutical references and is intended for general health education only. It is not a substitute for professional medical advice, diagnosis, or treatment.

Al Mujtama Pharmacy assumes no legal or medical liability for:

• Any therapeutic decision made based on the information displayed without consulting a licensed physician or pharmacist
• Any discrepancy between the information provided and the product's package insert or SFDA guidelines
• Any misuse of medication resulting from personal interpretation of the content displayed

Important notice: Drug formulations and instructions may vary between production batches. Always rely on the leaflet included inside the product packaging you have, and consult your pharmacist or physician before starting, adjusting, or discontinuing any medication.

By using this content, you acknowledge that you have read this disclaimer and agree that Al Mujtama Pharmacy bears no liability arising from reliance on this information as a substitute for direct medical consultation.

Your health is a trust - always consult your doctor first.