Itraconazole

Oral Candidiasis, Vulvovaginal Candidiasis ... show more

DRUG STATUS

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Approvals

US(FDA), UK(BNF)

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Essential Medicine

YES

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Teratogenicity

Unlisted

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Pharmaceutical Class

Azole Antifungal

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Drug Ingredient

Itraconazole

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Summary

  • Itraconazole is used to treat various fungal infections. These include Aspergillosis, Histoplasmosis, Blastomycosis, Onychomycosis, Candidiasis and Dermatophyte infections like athlete's foot and ringworm.

  • Itraconazole works by inhibiting the synthesis of a substance called ergosterol, which is a vital component of fungal cell membranes. Without ergosterol, the cell membrane becomes unstable, leading to the death of the fungal cell and preventing the spread of the infection.

  • The usual daily dosage for adults depends on the condition being treated. For fungal infections like Onychomycosis, the typical dose is 200 mg once daily or 100 mg twice daily. For systemic infections, higher doses may be prescribed. It should be taken with food to improve absorption.

  • Common side effects of Itraconazole include nausea, headache, abdominal pain, and diarrhea. Some people may also experience rash or dizziness. Rare but serious side effects include liver toxicity, heart failure, and severe allergic reactions.

  • Itraconazole should not be used in patients with a history of hypersensitivity to the drug or other azole antifungals. It is also contraindicated in people with active liver disease, heart failure, or severe cardiac conditions. Caution is advised for those with kidney disease or a history of arrhythmias.

Indications and Purpose

What is Itraconazole used for?

Itraconazole is used to treat various fungal infections, including:

  1. Aspergillosis (lung infections caused by Aspergillus fungi)
  2. Histoplasmosis (a fungal infection affecting the lungs)
  3. Blastomycosis (a fungal infection affecting the lungs and other organs)
  4. Onychomycosis (fungal nail infections)
  5. Candidiasis (yeast infections, including oral, esophageal, and vaginal)
  6. Dermatophyte infections (like athlete’s foot and ringworm)

How does Itraconazole work?

Itraconazole works by inhibiting the synthesis of ergosterol, a key component of the fungal cell membrane. Without ergosterol, the cell membrane becomes destabilized, leading to leakage of essential cellular components, which causes fungal cell death. This action helps eliminate fungal infections and prevents the fungi from spreading within the body. Itraconazole is effective against a wide range of fungi, including yeasts and molds.

Is Itraconazole effective?

Clinical studies and trials have shown that Itraconazole is highly effective in treating a wide variety of fungal infections, including systemic conditions like aspergillosis, histoplasmosis, and onychomycosis. Research supports its ability to reduce fungal load and symptoms, with significant improvement observed in patients with chronic or severe infections. Its efficacy is proven through its ability to target and disrupt fungal cell membranes, leading to the resolution of infections in many cases.

How does one know if Itraconazole is working?

The benefit of Itraconazole is evaluated by monitoring the improvement in symptoms, such as reduced inflammation, pain, or itching, depending on the infection. Laboratory tests, like fungal cultures or blood tests, are used to assess the reduction in fungal load and confirm the eradication of the infection. Clinical follow-up is essential to ensure complete resolution and prevent relapse of the infection.

Directions for Use

How do I take Itraconazole?

Itraconazole capsules should be taken with food to improve absorption, while the oral solution should be taken on an empty stomach for maximum effectiveness. Avoid grapefruit or grapefruit juice, as it can interfere with how the medication works. Follow your doctor’s instructions closely, and maintain a consistent schedule to ensure optimal results.

For how long do I take Itraconazole?

Treatment for fungal infections usually lasts at least three months, and until tests show the infection is gone. For toenail fungus, treatment typically lasts 12 weeks.

How long does it take for Itraconazole to start working?

Itraconazole typically starts working within a few days to weeks, depending on the type and severity of the fungal infection. For mild infections like nail fungus, it may take several weeks to see improvement, while for systemic infections, noticeable effects may take longer, often several weeks to months. Consistency in taking the medication as prescribed is important for full effectiveness.

How should I store Itraconazole?

Itraconazole should be stored at room temperature, away from heat, moisture, and direct sunlight. Keep it in its original container with the lid tightly closed and out of reach of children. If you are using the oral solution, it should be stored in the refrigerator and used within 30 days. Always check the expiration date before use.

Warnings and Precautions

Who should avoid taking Itraconazole?

Itraconazole should not be used in patients with a history of hypersensitivity to the drug or other azole antifungals. It is contraindicated in people with active liver disease, heart failure, or severe cardiac conditions, as it can worsen these conditions. Caution is advised for those with kidney disease or a history of arrhythmias. Itraconazole can interact with other medications, so it’s important to inform your doctor about all medications being taken.

Can I take Itraconazole with other prescription drugs?

Itraconazole can interact with several prescription drugs, including:

  1. CYP3A4 inhibitors (e.g., ritonavir, clarithromycin), which can increase Itraconazole levels and risk of side effects.
  2. CYP3A4 inducers (e.g., rifampin, carbamazepine), which can reduce Itraconazole effectiveness.
  3. Benzodiazepines (e.g., midazolam, triazolam), which may have increased sedative effects when combined with Itraconazole.
  4. Statins (e.g., atorvastatin), increasing the risk of muscle toxicity.
  5. Antacids or proton pump inhibitors, which can decrease Itraconazole absorption.

Can I take Itraconazole with vitamins or supplements?

Itraconazole may interact with supplements that affect its absorption or metabolism. For example, calcium and magnesium supplements can reduce its effectiveness, especially in its capsule form. Taking it with antacids or proton pump inhibitors may lower its absorption, as the medication requires an acidic environment for proper absorption. Always consult a healthcare provider before combining Itraconazole with any vitamins or supplements.

Can Itraconazole be taken safely while pregnant?

Itraconazole is classified as a pregnancy category C drug, meaning there is limited evidence of harm to the fetus in animal studies, but its safety in humans has not been fully established. It should only be used during pregnancy if the potential benefits outweigh the risks. Pregnant women should consult their healthcare provider before using Itraconazole to assess the risk and need for treatment.

Can Itraconazole be taken safely while breastfeeding?

Itraconazole is excreted in breast milk in small amounts, and while it is generally considered safe for short-term use during breastfeeding, it is recommended to consult a healthcare provider before use. The infant should be monitored for any potential side effects, such as gastrointestinal upset or rash. Long-term or high-dose use may require caution to avoid any adverse effects on the infant.

Is Itraconazole safe for the elderly?

When using itraconazole for older adults, it's important to be cautious because it can affect their liver, kidneys, or heart. It should also be used carefully if they have other illnesses or are taking other medications. Some people, especially those also taking quinidine, have reported temporary or permanent hearing loss while using itraconazole. There's not enough information from clinical studies to know if itraconazole works differently in older adults compared to younger people.

Is it safe to exercise while taking Itraconazole?

Itraconazole is an antifungal medication that can affect your ability to exercise, especially if taken in higher doses. Some users report side effects like fluid retention and congestive heart failure, which can lead to decreased exercise tolerance—meaning you might feel more tired or short of breath during physical activity.

Additionally, itraconazole can have a negative effect on heart function, potentially reducing how well your heart pumps blood. This can make both moderate and strenuous exercise more challenging.

If you experience any unusual symptoms like swelling or difficulty breathing while on this medication, it's best to consult your healthcare provider before continuing your exercise routine

Is it safe to drink alcohol while taking Itraconazole?

Drinking alcohol occasionally or moderately while taking Itraconazole is not strictly prohibited, but it’s generally better to avoid it. Alcohol can put extra strain on your liver, and since Itraconazole is processed by the liver, combining the two may increase the risk of liver problems. Additionally, alcohol could worsen certain side effects like dizziness, nausea, or an upset stomach.

If you choose to drink, keep it minimal and watch for any unusual symptoms, such as tiredness, yellowing of the skin, dark urine, or abdominal pain—these could indicate liver issues. If you notice any of these, stop drinking and inform your doctor immediately. To stay on the safe side, discuss your drinking habits with your healthcare provider to ensure there’s no increased risk specific to your health condition. Prioritizing your health while on medication is always a smart choice!