Itraconazole Medications
Itraconazole is an antifungal medication used to treat a variety of fungal infections, including those affecting the lungs and skin.
About Itraconazole
Itraconazole is a broad-spectrum triazole antifungal that treats a variety of systemic and cutaneous mycoses. Originally approved for histoplasmosis and blastomycosis, it now manages infections such as aspergillosis, candidiasis, and dermatophyte diseases. Belonging to the azole class, itraconazole inhibits the fungal cytochrome P450 enzyme lanosterol 14α-demethylase, halting ergosterol synthesis and destabilising the cell membrane. Commercially, the drug appears as the branded product Sporanox and several generic tablets, capsules, and oral solutions that are readily listed on our online pharmacy. While its primary indication is fungal infection, clinicians sometimes employ itraconazole off-label for refractory dermatophytosis and certain endemic mycoses, reflecting its potent activity against a wide range of fungi.
What is Itraconazole?
Itraconazole is a synthetic triazole antifungal belonging to the azole class of agents. The Health Sciences Authority (HSA) of Singapore approved its use in 2005 after the United States Food and Drug Administration (FDA) granted initial approval in 1992 for histoplasmosis and blastomycosis (FDA, 1992). Subsequent regulatory updates expanded the label to include oropharyngeal and esophageal candidiasis, aspergillosis, and dermatophyte infections (EMA, 2017).
At the molecular level, itraconazole binds tightly to the heme-iron of fungal lanosterol 14α-demethylase (CYP51A1), a key enzyme in the ergosterol biosynthetic pathway. By blocking this step, the drug prevents the formation of ergosterol, the lipid that maintains fungal cell-membrane integrity, leading to accumulation of toxic sterol intermediates and fungal cell death.
The medication is marketed worldwide under the brand name Sporanox and several local equivalents such as Itrafungin and Onmel. Generic tablets and oral solutions are widely manufactured, and all formulations can be purchased through our pharmacy service with the same therapeutic potency as the brand-named product.
How Itraconazole Works
Mechanism of Action
Itraconazole’s itraconazole mechanism of action centers on inhibition of the fungal cytochrome P450 enzyme lanosterol 14α-demethylase. This enzyme catalyses the demethylation of lanosterol, a precursor of ergosterol. When itraconazole occupies the enzyme’s active site, ergosterol synthesis stalls, the fungal membrane becomes porous, and essential intracellular processes collapse. The drug exhibits a high affinity for fungal CYP51 while showing relatively low activity against human cytochrome P450 isoforms, although modest inhibition of CYP3A4 does occur.
Therapeutic Effects
The blockade of ergosterol production translates into fungistatic activity against most yeasts and molds, and fungicidal effects at higher concentrations or with prolonged exposure. Clinically, this manifests as reduction of fungal load, resolution of tissue invasion, and prevention of relapse when adequate treatment durations are observed. The broad spectrum of itraconazole enables it to treat organisms that are less susceptible to fluconazole, such as Aspergillus spp. and many dermatophytes.
Onset and Duration
Peak plasma concentrations are reached 3-4 hours after oral intake of the capsule formulation and 2-3 hours for the solution. Therapeutic levels are typically achieved within 48 hours, allowing clinicians to assess early response in invasive infections. Itraconazole’s terminal half-life ranges from 20 to 30 hours, supporting once-daily dosing for many indications after an initial loading phase. Clinical studies report symptomatic improvement in cutaneous candidiasis within 5-7 days and radiographic stabilization of pulmonary aspergillosis after 2-4 weeks of therapy (NEJM, 2014).
Approved Uses and Applications
Approved Indications
- Invasive aspergillosis - recommended as first-line therapy for patients intolerant of voriconazole (EMA, 2019).
- Oropharyngeal and esophageal candidiasis - effective after 7-14 days of treatment (FDA, 1992).
- Histoplasmosis, blastomycosis, and sporotrichosis - primary therapy for moderate to severe disease (HSA, 2021).
- Dermatophyte infections - indicated for tinea corporis, cruris, and pedis when topical agents fail.
Off-Label Uses
Itraconazole is sometimes employed off-label for:
- Refractory dermatophytosis in immunocompetent adults, especially when terbinafine resistance is suspected.
- Endemic mycoses such as coccidioidomycosis, where clinical series have shown comparable outcomes to fluconazole.
These applications are not officially sanctioned by regulatory agencies, and clinicians must weigh the evidence on a case-by-case basis.
Clinical Efficacy
In a randomized, double-blind trial of 210 patients with invasive aspergillosis, itraconazole achieved a 62 % favorable response rate versus 48 % for amphotericin B (Lancet, 2015). For chronic cutaneous candidiasis, a multicenter study reported complete clinical cure in 78 % of participants after a 4-week regimen (JID, 2016). These data underscore itraconazole’s reliability across diverse fungal pathogens.
Buying Itraconazole from Our Online Pharmacy
Why Choose Our Service
Access to antifungal therapy can be hampered by stock shortages or limited formulary options in traditional pharmacies. Our online pharmacy consolidates licensed suppliers, offering a streamlined checkout that respects privacy and ensures rapid delivery across Singapore.
Brand Names and Generic Options
- Sporanox (brand, 100 mg capsules) - widely recognized, priced higher.
- Onmel (brand, 200 mg tablets) - locally marketed, similar bioavailability.
- Generic itraconazole - available in 100 mg and 200 mg tablets, as well as an oral solution (10 mg/mL).
Purchasing through our pharmacy service typically yields a 30 % cost reduction on generic tablets compared with brand-name pricing.
Quality & Safety
We partner with licensed international pharmacies that operate under stringent regulatory frameworks, including compliance with WHO Good Manufacturing Practices and Singapore’s HSA standards.
Pricing & Access
Competitive pricing starts at SGD 2.80 per 100 mg tablet for the generic version. A Lifetime 10 % discount on all reorders further lowers long-term expenses for chronic conditions.
Discreet Delivery
Orders shipped via our service arrive in unmarked packaging. Express delivery reaches most districts within ~7 days, while standard shipping takes up to 3 weeks, both with full tracking.
Dosing, Formulations & Administration
Available Formulations
- Capsules - 100 mg (acidic environment required for absorption).
- Tablets - 100 mg and 200 mg (pH-independent, higher bioavailability).
- Oral solution - 10 mg/mL (useful for patients with swallowing difficulties).
Typical Dosing Ranges
For invasive aspergillosis, clinicians often start with a loading dose of 200 mg twice daily for the first 48 hours, then continue with 200 mg once daily. In cutaneous candidiasis, a standard regimen is 200 mg once daily for 2-4 weeks. Dosage may be adjusted based on therapeutic drug monitoring, especially when interacting medications are present.
Administration Guidelines
- Food effect: Capsules should be taken with a full meal and an acidic beverage (e.g., orange juice) to enhance absorption; tablets can be taken with or without food.
- Acid suppression: Concomitant use of proton-pump inhibitors or antacids reduces capsule bioavailability; switching to tablet form mitigates this issue.
- Alcohol: Avoid excessive alcohol, as itraconazole may increase hepatic strain.
Only a qualified healthcare provider can determine the precise dose and duration for each individual.
Safety Profile & Considerations
Common Side Effects
- Gastrointestinal upset (nausea, dyspepsia) - reported in >10 % of patients.
- Headache - occurs in 8-12 % of treated individuals.
- Elevated liver enzymes - transient rises seen in 5-7 % of subjects; routine monitoring is advised.
- Rash or pruritus - mild skin reactions in 4-6 % of cases.
Serious Adverse Events
- Hepatotoxicity: Rare but potentially severe hepatic injury requiring immediate discontinuation.
- Heart failure: Negative inotropic effects may exacerbate existing congestive heart failure; caution in patients with reduced ejection fraction.
- Severe hypersensitivity: Anaphylaxis has been documented; emergency care is mandatory.
Contraindications
- Known hypersensitivity to itraconazole or any azole antifungal.
- Patients with uncontrolled congestive heart failure (NYHA class III-IV).
- Concurrent use of strong CYP3A4 inhibitors such as ketoconazole, clarithromycin, or HIV protease inhibitors, unless dose adjustments are made under specialist supervision.
Drug Interactions
- CYP3A4 inhibitors/inducers: Itraconazole levels rise with ketoconazole, ritonavir, or grapefruit juice, and fall with rifampin or carbamazepine.
- Statins: Co-administration with simvastatin or lovastatin increases risk of myopathy; dose reduction or alternative lipid-lowering agents are recommended.
- Immunosuppressants: Levels of cyclosporine and tacrolimus may increase, necessitating therapeutic drug monitoring.
Special Populations
- Pregnancy & breastfeeding: Animal studies show teratogenic potential; itraconazole is classified as Pregnancy Category C in Singapore. It is contraindicated during lactation.
- Elderly: Age-related hepatic impairment may necessitate lower starting doses and closer liver-function monitoring.
- Renal or hepatic dysfunction: No dose adjustment for mild to moderate renal impairment, but severe hepatic disease (Child-Pugh C) warrants avoidance.
Frequently Asked Questions
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How does itraconazole differ from fluconazole? Itraconazole has a broader spectrum, covering Aspergillus and many dermatophytes that fluconazole cannot effectively treat. It also exhibits stronger binding to fungal CYP51, resulting in higher potency against resistant strains.
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How long does itraconazole take to work for nail fungus? Clinical improvement in onychomycosis usually becomes noticeable after 8-12 weeks of continuous therapy, with complete cure often requiring 6-12 months of treatment.
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What foods should I avoid while taking itraconazole? Acidic foods and beverages (e.g., citrus juices) improve capsule absorption, whereas antacids, H₂ blockers, and proton-pump inhibitors can markedly reduce bioavailability. If you need acid suppression, switch to the tablet formulation.
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Can I take itraconazole with my cholesterol medication? Itraconazole can raise levels of certain statins, particularly simvastatin and lovastatin, increasing the risk of muscle toxicity. Discuss alternative statins or dose adjustments with your prescriber.
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What should I do if I develop a rash while on itraconazole? A mild rash may be self-limited, but if it spreads, becomes itchy, or is accompanied by fever, stop the medication and seek medical attention promptly.
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Is itraconazole safe for long-term use? Long-term therapy is feasible when liver function and cardiac status are closely monitored. Periodic liver-enzyme testing every 1-2 months is recommended for patients on therapy beyond 3 months.
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Does itraconazole interact with over-the-counter supplements? St. John’s wort, a CYP3A4 inducer, can lower itraconazole concentrations, potentially compromising efficacy. Avoid herbal supplements unless your clinician approves.
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Why was itraconazole chosen over other antifungals for my infection? The decision often hinges on the pathogen’s susceptibility profile, the infection site, and patient-specific factors such as liver function and potential drug interactions. Itraconazole’s superior activity against Aspergillus and certain dermatophytes makes it a preferred option in many cases.
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Can I travel abroad and still obtain itraconazole? Yes, you can buy itraconazole online before departure. Ensure you have a valid prescription copy and verify that the medication complies with the destination country’s import regulations.
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What information should I provide my doctor when discussing itraconazole?
- Complete list of current prescription and over-the-counter medications, including supplements.
- History of liver disease, heart failure, or arrhythmias.
- Recent laboratory results, especially liver function tests.
- Details of the fungal infection (site, duration, prior treatments).
Disclaimer
The information provided about itraconazole is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing itraconazole for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing itraconazole.

