Itraconazole

fungal infection in nails

Therapeutic indications

Itraconazole is atriazole antifungal agent. It is used in the management of infections caused by a fungus, both systematic and superficial. Itraconazole can be in form of tablets or syrup. It prevents the growth of fungus. Itraconazole is used in the treatment of broad spectrum infections caused by the fungus that include the following conditions:

  • Aspergillosis
  • Blastomycosis
  • Histoplasmosis fungal infection in nails
  • Vulvovaginal candidiasis
  • Oral candidiasis
  • Dermatophytoses
  • Pityriasis Versicolor
  • Superficial mycoses
  • Onychomycosis
  • Systemic candidiasis
  • Cryptococcal infections(cryptococcal meningitis)
  • In AIDS maintenance therapy
  • Esophageal candidiasis
  • Paracoccidioidomycosis
  • Pulmonary coccidiosis
  • Sporotrichosis
  • Chromomycosis
  • Zygomycosis
  • Ringworm
  • Tinea versicolor
  • Microsporidiosis
  • Penicilliosis marneffei

Do I need a prescription?

Itraconazole can be bought from online drug stores and pharmaceuticals near you. A doctor’s prescription is mandatory.

Dosage

The length of treatment and dosage of itraconazole is dependent on the medical condition and how one responds to the initial dose. The recommended dosage for a number of conditions is as follows:

  • Blastomycosis, histoplasmosis, and aspergillosis

In life-threatening situations, a loading dose of 200 mg taken orally three times a day for the first three days. A maintenance dose of 200 mg once or two times a day is then continued. The treatment should take at least a duration of three months. If no improvement is observed the dose is increased with 100 mg but not a maximum of 400 mg a day.

If immunosuppression is present, lifelong suppression therapy is needed in cases where the immunosuppression cannot be reversed.

  • Oropharyngeal candidiasis – 100 mg daily for fifteen days
  • Vulvovaginal candidiasis – 400 mg divided into two doses taken once a day
  • Resistant dermatophyte infections – 200 mg taken daily for a period of fifteen to thirty days. In infections of the nails, higher doses of 400 mg for seven days per month for three months.
  • Subcutaneous and systemic fungal infections – 200 to 400 mg once a day as long as lesions persist.

Chemical composition

The active ingredient is itraconazole. The amount varies with the tablet or syrup strength. Itraconazole can be found as 100 mg and 200 mg tablet and as a syrup 10 mg/ml.

Mechanism of Action (MOA)

Itraconazole is a selective inhibitor of cytochrome P-450 an enzyme involved in 14-α demethylation that catalyzes the conversion of lanosterol to ergosterol that is a component of the fungal cell membrane. When ergosterol is not produced, the permeability of cell membrane increases and the cell contents leak.

Itraconazole also functions by preventing yeast from being transformed to mycelial forms, prevention of endogenous respiration, preventing uptake of purine and biosynthesis of phospholipids and triglycerides.

Facts on itraconazole

  • Itraconazole is classified as a category B3 drug in pregnancy as it has been shown to have teratogenic effects in rat fetuses.
  • The bioavailability of itraconazole is reduced in some immunocompromised individuals.
  • Alternative therapy is advised in cases of cystic fibrosis as such individuals do not respond to itraconazole.
  • Itraconazole is one of the medications utilized to treat opportunistic infections in immunocompromised individuals like in HIV.
  • If the condition is life-threatening, a loading dose of 200 mg three times a day is recommended for the first three days.

Contraindications

The use of itraconazole is not recommended in a number of conditions. Inform your doctor if you have any of the following conditions as it may affect the prescription dosage given:

  • Hypersensitive to the active ingredient in itraconazole.
  • Heart diseases such as Congestive Heart Failure(CHF) or a history of CHF, coronary artery disease, heart valve disease, heart rhythm disorder
  • Pregnancy or when one is expecting to get pregnant.
  • Should not be used in pediatric patients and in the elderly unless the benefits outweigh the risks.
  • Renal and hepatic impairment
  • Lung disease (chronic obstructive pulmonary disease-COPD)
  • Achlorhydria(reduced or no acid in the stomach)
  • Itraconazole should not be used together with CYP3A4 substrates as it leads to an increase in the level of the drugs in the bloodstream increasing its pharmacological effects and the chances of adverse effects occurring.

Side effects

Apart from the desired effects of itraconazole, it can also cause side effects in some individuals. The side effects caused may be common and less serious while others are rare but very serious. The side effects may depend on the dosage and the duration of using the drug. Report any side effects you experience to your doctor especially if they do not go away.

Less serious and common side effects include:

  • Vomiting
  • Bloating
  • Constipation
  • Bloating
  • Diarrhea
  • A headache
  • Itching
  • Dizziness
  • Skin rash
  • Stomach upset
  • Itching
  • Unpleasant taste in the mouth
  • Joint pain
  • Weakness
  • Pain in muscles
  • A runny nose
  • A decrease in urine output
  • Dry mouth
  • Increased thirst
  • Loss of appetite
  • Nausea
  • Tingling or numbness in lips, hands, and feet
  • Seizures

Serious and rare side effects include:

  • Breathing trouble
  • Swelling of feet and ankles
  • Hair loss
  • A fever and persistent sore throat
  • Feeling unusually tired
  • Frequent, burning or painful urination
  • Muscle cramps
  • A decrease in sexual ability
  • Irregular heartbeat
  • Mood changes
  • Ringing in ears
  • Hearing loss( permanent or temporary)
  • Blurred vision
  • Chest pain
  • Confusion
  • A cough
  • Cold sweats
  • Dark urine
  • Diarrhea
  • Dizziness
  • Lightheadedness when you get up abruptly
  • Unusual cold
  • Stool that is light colored
  • Stomach pain
  • Rattling breathing
  • Unpleasant breath odor
  • Gaining weight
  • Vomiting blood
  • Jaundice
  • Decrease output of urine
  • Nervousness
  • Trouble sleeping

If you accidentally take itraconazole tablets, inform your doctor and rush to the nearest emergency center with the package. An overdose of itraconazole is resolved with supportive measures. If appropriate, activated charcoal could be given. Dialysis cannot be used to remove itraconazole. Taking an overdose may result in any of the side effects listed above but might also cause seizures and collapse.

Drug interactions

Thrush fungal infectionInform your doctor if you are taking any medications, over the counter drugs, prescription drugs, vitamin supplements, and herbal products. This products may interact with itraconazole and may result in severe side effects occurring or may increase the concentrations of itraconazole or other medications prolonging their therapeutic effects. Drugs and products that interact with itraconazole include:

  • Warfarin
  • Erythromycin
  • Atorvastatin
  • Alprazolam
  • Rifampicin
  • Phenytoin
  • Rifabutin
  • Ritonavir
  • Clarithromycin
  • Indinavir
  • Quinidine
  • Mizolastine
  • Cisapride
  • Astemizole
  • Pimozide
  • Dofetilide
  • Bepridil
  • Levacetylmethadol
  • Sertindole
  • Terfenadine
  • Lovastatin
  • Atorvastatin
  • Simvastatin
  • Midazolam
  • Triazolam
  • Nisoldipine
  • Eletriptan
  • Ergot alkaloids that include ergotamine, dihydroergotamine, methylergometrine, and ergometrine.
  • Oral anticoagulants
  • HIV protease inhibitors
  • Antineoplastic agents such as busulfan, vinca , and trimetrexate
  • Digoxin
  • Glucosteroids (budesonide, dexamethasone, methylprednisolone

The above list does not give the complete list of products that interact with itraconazole thus other products may not be listed.

What to do if you skip a dose?

If a dose of itraconazole is skipped, it should be taken as soon as you realize it. If it is close to the next dose, it can be skipped and the next dose taken at the required time. The normal schedule should then be continued. Do not double the dose to compensate for the skipped dose as it might result in the adverse effects of the drug. Frequent skipping of the dose makes the drug to be less effective and may result in the re-occurrence of the condition which may be due to resistant species of the same causative micro-organism. To avoid frequent dose skipping, set a reminder or have a family member remind you when it is time to take the drug.

Precautions

A number of precautions should be considered while using itraconazole. The precautions include:

  • Itraconazole should not be used if you are hypersensitive the active ingredients of the drug.
  • Lactating mothers should not use itraconazole because it is secreted in milk and might harm the nursing child.
  • Pregnancy or planning to be pregnant. Itraconazole has may harm the growing fetus and thus should not be used unless the benefits outweigh the risks.
  • Itraconazole should be used with caution in individuals with renal and hepatic disorders. Its use should be discontinued if normal individuals have signs of hepatic impairment.
  • Itraconazole should not be used together with CYP3A4 substrates as it may result in cardiac dysrhythmias that are life-threatening or death.
  • Itraconazole should not be used in patients with cardiac diseases.
  • Itraconazole tablets should be taken after meals. Before a meal, the absorption of itraconazole is reduced because of reduced stomach acidity.
  • In cases neuropathy symptoms such as pain in the hands, weakness, and numbness, administration of itraconazole should be discontinued.
  • Itraconazole should not be administered with quinidine as it may result in either temporary or permanent loss of hearing. This may resolve when the treatment is stopped.
  • In case itraconazole causes dizziness or drowsiness do not handle heavy machinery or drive. Avoid alcoholic beverages.
  • Itraconazole should be stored at room temperature away from moisture and light.
  • Do not take itraconazole that is expired as it might cause undesirable effects. Always check the package for expiry date.
  • Itraconazole should be used with caution in the elderly, as they prone to the side effects.
  • Pediatric patients are not to use itraconazole unless the benefits outweigh the risks.
  • If you are taking antacids, itraconazole should be taken at least two hours before their administration as the absorption of itraconazole is reduced when the acid levels are reduced.
  • In patients that have systemic infections that are life-threatening, itraconazole is not recommended as the initiating treatment based on its pharmacokinetic properties.
  • Itraconazole tablets should not be chewed but swallowed whole.
  • Avoid the use of milk or products containing calcium and grapefruit juice while using itraconazole.

Different brands and manufacturing companies of the drug

Itraconazole is manufactured by different companies, with different strengths of either 100mg or 200 mg and an oral solution. It is sold under brand names that include:

  • Biospore – Biosciences Pharmakon
  • Candistat – Merck limited (India)
  • Canditral – Glenmark Pharmaceuticals
  • AFO – Mentis Pharma Ltd
  • Candiloss (100 mg) – Sarian Healthcare
  • Citroz – Cian Healthcare Pvt Ltd
  • Icoz – Raddiso Health Care Pvt Ltd
  • Intracan(100 mg) – Intra Labs Pvt Ltd
  • Fulcover – Saga Laboratories
  • Itaspor – Intas Pharmaceutical Ltd
  • IT-Mac – Macleods Pharmaceuticals Ltd
  • Itcona – Phoenix Pharmaceuticals
  • Itra – East West Pharma
  • Itra Good – Acinom Healthcare
  • Itrole – Chemo Biological
  • Itrafun – Total Healthcare
  • Itrasafe – Pax Healthcare
  • Itrasig – Signova Pharma Pvt Ltd
  • Itracross – Cross Berry Pharma
  • Sporanox – Johnson & Johnson
  • Onmel – Merz Pharmaceuticals Inc

Substitutes of the drug

Substitute drugs that have the same strength and work as itraconazole include:

  • Fluconazole
  • Isavuconazonium
  • Voriconazole

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