Itraconazole (Oral)

Overview

When patients develop fungal infections, they can affect almost any part of the body. As well as impacting on the eyes, nails, ears and oral cavities, fungal infections may occur in the lungs, gastrointestinal tract, brain and other organs.

When administered to the patient, Itraconazole inhibits lanosterol 14 alpha-demethylase. As a result, the structure of the fungal cell walls is weakened. As the cells can no longer replicate, they are unable to spread and the infection cannot worsen. Once the structure of the cell walls has been breached, the body is able to kill the cells and rid itself of the infection.

Although Itraconazole can be administered intravenously, it is more commonly used as an oral medication. When patients are prescribed Itraconazole, the type of medication they're given will depend on the nature of their infection.

For example, Itraconazole is prescribed as an oral solution when patients are being treated for esophageal or oropharyngeal candidiasis (thrush or oral thrush). Itraconazole may be prescribed as an oral capsule when treating blastomycosis, aspergillosis, onychomycosis or histoplasmosis. However, onychomycosis (fungal infection of the nails) may be treated with Itraconazole in tablet form, providing it is only the toenails which are affected.

Although Itraconazole is effective in treating fungal infections, it will not resolve viral or bacterial infections. If the cause of the patient's infection is unclear, a biopsy may be taken in order to confirm whether it is a fungal infection and, if so, which type of fungus has caused the condition.

Once this has been established, Itraconazole may be prescribed in order to reduce the patient's symptoms and treat the infection. Whilst Itraconazole can reduce the symptoms of an infection fairly quickly, patients may need to take this medication for a significant period of time in order for the infection to be fully resolved.

Conditions Treated

  • Esophageal or oropharyngeal candidiasis (Thrust or oral thrust)
  • Blastomycosis (e.g. Gilchrist's disease)
  • Aspergillosis (Often affecting the lungs)
  • Onychomycosis (Fungal infection of the nails)
  • Histoplasmosis (e.g. Darling's disease)
  • Type Of Medicine

  • Antifungal agent

Side Effects

When patients are taking Itraconazole, they may develop some side effects. Often, these occur when patients first starting the medicine but diminish over time. For example, when patients start using Itraconazole, they may experience the following:

  • Decreased interest in sexual intercourse
  • Trouble concentrating
  • Difficulty having a bowel movement (stool)
  • Trouble sleeping
  • Difficulty with moving
  • Tiredness
  • Discouragement
  • Swollen joints
  • Feeling of constant movement of surroundings or self
  • Runny or stuffy nose
  • Feeling empty or sad
  • Stomach discomfort
  • Inability to have or keep an erection
  • Soreness of the skin
  • Indigestion
  • Stomach fullness
  • Irritability
  • Unusual drowsiness or sleepiness
  • Loss of sexual drive, desire, performance or ability
  • Sensation of spinning
  • Loss of pleasure of interest
  • Increased sensitivity of the eyes to sunlight
  • Muscle stiffness or aching
  • Tenderness or pain in the cheekbones or eyes
  • Passing of gas
  • Sour or acid stomach
  • Passing urine more often
  • Belching
  • Menstrual changes
  • Change in taste
  • Thinning of the hair or hair loss
  • Heartburn
  • Loss of taste
  • Redness or other discoloration of the skin
  • Increased need to urinate
  • Severe sunburn
  • Loss of bladder control
  • Stomach upset, discomfort or fullness

If the above side-effects are fairly mild, patients may not need to seek medical treatment. However, if patients are suffering from serious side effects or are concerned about the presence of any adverse effects, they should always seek medical help.

If patients experience any of the following side effects whilst taking Itraconazole, they should notify their doctor immediately:

  • Convulsions
  • Blurred vision
  • Decreased urine
  • Stomach or abdominal pain or cramps
  • Dry mouth
  • Unusual weakness or tiredness
  • Fever
  • Trouble breathing
  • Increased thirst
  • Tingling or numbness in the lips, feet or hands
  • Irregular heartbeat
  • Nausea or vomiting
  • Loss of appetite
  • Mood changes
  • Dark urine
  • Muscle cramps or pain
  • Chest pain
  • Sneezing
  • Chills
  • Pounding, fast or slow pulse or heartbeat
  • Clay-colored stools
  • Shivering
  • Cloudy urine
  • Pounding in the ears
  • Cold sweats
  • Tingling or numbness in the fingertips or mouth
  • Confusion
  • Rattling, noisy breathing
  • Cough
  • Nervousness
  • Dark urine
  • Muscle twitching or spasms (tetany)
  • Decrease in urine output
  • Mental changes
  • Decrease in urine-concentrating ability
  • Light-colored stools
  • Diarrhea
  • Itching
  • Rash on the skin
  • Dizziness
  • Headache
  • Trembling
  • Lightheadedness, dizziness or faintness when getting up from a sitting or lying position suddenly
  • Sore throat
  • Drowsiness
  • Unpleasant breath odor
  • Sweating
  • Feeling unusually cold
  • Weight gain
  • Swelling of the lower legs, feet, hands or fingers
  • Vomiting of blood
  • Muscle cramps in the feet, legs, arms, face or hands
  • Tightness in the chest
  • Tarry, black stools
  • Yellowing of the skin or eyes
  • Stomach or abdominal tenderness
  • Bleeding gums
  • Loosening, peeling or blistering of the skin
  • Swelling or bloating of the hands, arms, feet, lower legs or face
  • Blood in the stools or urine
  • Welts or hives
  • Blue fingernails and lips
  • Itching, crawling, burning, prickling, pain, tingling, numbness or "pins and needles" feelings
  • Hearing loss
  • Continuing buzzing or ringing or other unexplained noise in the ears
  • Halos around lights
  • Coughing that sometimes produces a frothy pink sputum
  • General feeling of weakness or tiredness
  • Cracks in the skin
  • Irregular or fast breathing
  • Decreased appetite
  • Feeling of discomfort
  • Joint pain
  • Difficulty with swallowing
  • Loss of vision
  • Dilated neck veins
  • Loss of heat from the body
  • Disturbed color perception
  • Pain in side or lower back
  • Double vision
  • Night blindness
  • Extreme fatigue
  • Overbright appearance of lights
  • Large, hive-like swelling on the eyelids, tongue, lips, hands, throat, feet, legs, face or sex organs
  • Difficulty or painful urination
  • Irritated, red eyes
  • Pale skin
  • Swollen, red skin
  • Red pinpoint spots on the skin
  • Tunnel vision
  • Swelling or puffiness around the face, lips, tongue, eyes or of the eyelids
  • Rapid weight gain
  • Pain in stomach or upper right abdomen
  • Tingling in the feet or hands
  • Red skin lesions, sometimes with a purple center
  • Awkwardness or unsteadiness
  • Unusual weight loss or gain
  • Scaly skin
  • Ulcers, white spots or sores in the mouth or on the lips
  • Stomach pain, may be ongoing
  • Weakness in the hands, arms, feet or legs
  • Swollen lymph glands
  • Unusual bruising or bleeding

Patients should also obtain medical help if they experience any other side effects whilst taking this medication.

Dosage

When patients are prescribed Itraconazole, their dose will depend on the nature of their infection, their current presentation, their age, weight, medical history and the type of medication they're given.

If patients are prescribed Itraconazole capsules for the treatment of aspergillosis, for example, they are usually advised to take 200-400mg per day. Alternatively, Itraconazole capsules may be prescribed for histoplasmosis or blastomycosis and, in these cases, patients are usually prescribed 200mg per day as an initial dose. Following this, the patient's dose of Itraconazole may be increased but patients are not usually instructed to take more than 400mg per day.

Similarly, Itraconazole capsules may be prescribed to treat onychomycosis and when patients are being treated for an infection of the fingernails, they are usually advised to take two 200mg capsules per day. However, if the infection is affecting the toenails, patients are generally prescribed 200mg of Itraconazole, to be taken once per day.

Alternatively, onychomycosis of the toenails may be treated with Itraconazole tablets and, if so, patients are typically prescribed 200mg per day, to be taken for a period of twelve weeks.

Itraconazole can also be prescribed as an oral solution. When Itraconazole is administered in this form, it is usually to treat esophageal or oropharyngeal candidiasis. If patients have esophageal candidiasis, they are usually instructed to take 10mg or 10 milliliters of Itraconazole solution once per day, for a minimum of three weeks. However, if patients have oropharyngeal candidiasis, they are generally prescribed 20mg or 20 milliliters of Itraconazole solution once per day, for a period of one or two weeks.

Different forms of Itraconazole work in different ways so patients should only use the type of medication they are prescribed. If patients are given Itraconazole capsules, for example, they should not attempt to use Itraconazole solution instead.

Once Itraconazole starts to take effect, patients may begin to feel better and may notice a reduction in their symptoms. However, they should still continue to take their medication as directed and should finish the full course of treatment. If patients stop taking Itraconazole too early, their symptoms and infection may return and could be more difficult to treat.

Usually, patients are advised to take Itraconazole tablets or capsules with a full meal. However, Itraconazole solution is normally administered when the patient has an empty stomach. Patients should take their medication at the same time each day so that their body has a stable dose of medication at all times.

If patients are prescribed Itraconazole for the treatment of oral thrush, they should place the appropriate dose in their mouth and swish it around for a few seconds before swallowing it. This allows the medication to work more effectively and may reduce their symptoms more quickly.

When patients are using Itraconazole in solution form, they should use a measuring cup, medical syringe or medicine spoon to measure out the appropriate dose of medication.

Patients who are also taking antacids should take the antacid at least one hour before their dose of Itraconazole or at least two hours after taking Itraconazole.

If patients forget to take a dose of Itraconazole, they should contact their physician or pharmacist for advice. Patients should not attempt to administer an extra dose of Itraconazole, even if an earlier dose of medication has been missed.

Potential Drug Interactions:

As Itraconazole interacts with a significant number of other medications, patients should tell their doctor if they are taking any other prescription medicines, over-the-counter medications, supplements and/or vitamins before they start using this medicine. If patients are taking any of the following, Itraconazole should not be prescribed due to the risk of an interaction occurring:

  • Alfuzosin
  • Eplerenone
  • Alprazolam
  • Irinotecan
  • Amifampridine
  • Irinotecan Liposome
  • Amisulpride
  • Isavuconazonium Sulfate
  • Astemizole
  • Ergotamine
  • Bepridil
  • Ergonovine
  • Cisapride
  • Felodipine
  • Colchicine
  • Eliglustat
  • Conivaptan
  • Flibanserin
  • Dabigatran Etexilate
  • Mesoridazine
  • Dihydroergotamine
  • Methadone
  • Disopyramide
  • Methylergonovine
  • Dofetilide
  • Methysergide
  • Dronedarone
  • Thioridazine
  • Eletriptan
  • Ticagrelor
  • Fesoterodine
  • Quinidine
  • Simvastatin
  • Ivabradine
  • Telithromycin
  • Levomethadyl
  • Tolvaptan
  • Lomitapide
  • Solifenacin
  • Lovastatin
  • Sparfloxacin
  • Lurasidone
  • Ranolazine
  • Maraviroc
  • Silodosin
  • Midazolam
  • Posaconazole
  • Naloxegol
  • Terfenadine
  • Nelfinavir
  • Triazolam
  • Nisoldipine
  • Venetoclax
  • Pimozide
  • Ziprasidone
  • Piperaquine

Similarly, it is not usually advisable to take Itraconazole alongside the following medicines:

  • Ado-Trastuzumab Emtansine
  • Goserelin
  • Afatinib
  • Hydroxychloroquine
  • Aliskiren
  • Halofantrine
  • Amiodarone
  • Hydrocodone
  • Anagrelide
  • Histrelin
  • Apixaban
  • Fosphenytoin
  • Aprepitant
  • Gonadorelin
  • Aripiprazole
  • Haloperidol
  • Arsenic Trioxide
  • Nevirapine
  • Atorvastatin
  • Avanafil
  • Nafarelin
  • Olaparib
  • Axitinib
  • Oxycodone
  • Bedaquiline
  • Palbociclib
  • Boceprevir
  • Nilotinib
  • Bosutinib
  • Ondansetron
  • Bretylium
  • Nifedipine
  • Brexpiprazole
  • Leuprolide
  • Bromocriptine
  • Levofloxacin
  • Buserelin
  • Levomilnacipran
  • Cabazitaxel
  • Macitentan
  • Cabozantinib
  • Lumacaftor
  • Calcifediol
  • Reboxetine
  • Carbamazepine
  • Repaglinide
  • Cariprazine
  • Rifampin
  • Ceritinib
  • Rivaroxaban
  • Cilostazol
  • Retapamulin
  • Citalopram
  • Risperidone
  • Clarithromycin
  • Romidepsin
  • Clozapine
  • Regorafenib
  • Cobicistat
  • Panobinostat
  • Cobimetinib
  • Pazopanib
  • Crizotinib
  • Cyclosporine
  • Pasireotide
  • Dabrafenib
  • Phenytoin
  • Daclatasvir
  • Pixantrone
  • Dasatinib
  • Pitolisant
  • Degarelix
  • Pimavanserin
  • Delamanid
  • Sulpiride
  • Deslorelin
  • Suvorexant
  • Digoxin
  • Tacrolimus
  • Docetaxel
  • Sunitinib
  • Domperidone
  • Tadalafil
  • Donepezil
  • Ivacaftor
  • Doxorubicin
  • Iloperidone
  • Doxorubicin Hydrochloride Liposome
  • Idelalisib
  • Efavirenz
  • Sildenafil
  • Elvitegravir
  • Salmeterol
  • Erlotinib
  • Simeprevir
  • Escitalopram
  • Sevoflurane
  • Eszopiclone
  • Sonidegib
  • Everolimus
  • Sirolimus
  • Fentanyl
  • Temsirolimus
  • Fluoxetine
  • Vilanterol
  • Fluticasone
  • Venlafaxine
  • Fosaprepitant
  • Vinflunine
  • Hydroxyzine
  • Topotecan
  • Ibrutinib
  • Triptorelin
  • Ibutilide
  • Toremifene
  • Ixabepilone
  • Vandetanib
  • Lapatinib
  • Vemurafenib
  • Manidipine
  • Trabectedin
  • Metronidazole
  • Ruxolitinib
  • Mifepristone
  • Vilazodone
  • Morphine
  • Vorapaxar
  • Morphine Sulfate Liposome
  • St John's Wort
  • Moxifloxacin
  • Vincristine
  • Ponatinib
  • Zolpidem
  • Vincristine Sulfate Liposome
  • Quetiapine
  • Zuclopenthixol
  • Sotalol
  • Warfarin
  • Tamsulosin

Although the use of Itraconazole alongside the above medications is not normally recommended, it may be necessary for some situations. If so, the patient's dose may be altered or they may be advised to take their medications at different times.

Whilst Itraconazole may be prescribed in conjunction with the following medicines, patients may be more likely to experience side-effects if they take this medication at the same time as any of the following:

  • Acenocoumarol
  • Phenprocoumon
  • Anisindione
  • Ritonavir
  • Buspirone
  • Indinavir
  • Busulfan
  • Ciprofloxacin
  • Rosuvastatin
  • Dicumarol
  • Saquinavir
  • Micafungin
  • Didanosine
  • Tolterodine
  • Meloxicam

Patients should also be aware that Itraconazole can interact with certain foods and drinks. Due to this, patients should not consume the following when taking this medication:

  • Grapefruit, grapefruit juice or any items containing grapefruit

As well as informing their physician if they are taking any other medicines, vitamins or supplements before they start taking Itraconazole, patients should obtain medical advice before using any new medicines, vitamins or supplements once they have started receiving treatment with Itraconazole.

Warnings

If patients have any other existing health problems, their use of Itraconazole may be affected. Similarly, if patients have a history of certain conditions, they may be unable to take Itraconazole. It's important, therefore, that patients discuss their current health and medical history with their physician before they start taking Itraconazole. The following conditions may be particularly relevant:

  • Fluid retention or body swelling (Edema)
  • Chronic obstructive pulmonary disorder (COPD)
  • Elevated liver enzymes
  • Kidney disease
  • Heart rhythm problems
  • Heart attack
  • Congestive heart failure
  • Heart disease
  • Low levels of acid in the stomach (Hypochlorhydria)
  • Cystic fibrosis
  • Liver disease

When patients are treated with Itraconazole, they will need to have regular check-ups with their physician and may require regular blood tests in order to confirm that the medication isn't having any unwanted effects.

As the safety of Itraconazole has not been specifically tested on children and infants, this medication is not usually prescribed to pediatric patients.

Although Itraconazole can be prescribed to geriatric patients, these patients may be more likely to have age-related kidney, liver and/or heart problems. As a result, their dose of Itraconazole may need to be modified.

Patients may need to take Itraconazole for weeks or months before their infection is fully resolved. However, patients should notice an improvement in their symptoms within this time. If the patient's symptoms worsen or do not improve, they should contact their physician for further advice.

In some patients, congestive heart failure can be a side effects of using Itraconazole. Patients should obtain immediate medical help if they experience any of the following symptoms:

  • Decreased urine output
  • Irregular breathing
  • Chest pains
  • Extreme fatigue
  • Dilated neck veins
  • Irregular heartbeat
  • Tightness in the chest
  • Shortness of breath
  • Weight gain
  • Trouble breathing
  • Swelling of the fingers, lower legs, feet or face

In rare cases, patients may experience liver problems when taking Itraconazole. If patients develop the following symptoms, they should obtain urgent medical assistance:

  • Unusual weakness or tiredness
  • Stomach tenderness or pain
  • Dark-colored urine
  • Clay-colored stools
  • Fever
  • Itching
  • Headache
  • Decreased appetite
  • Yellowing of the eyes or skin
  • Nausea or vomiting
  • Loss of appetite
  • Swelling of the lower legs or feet
  • Rash on the skin

In some instances, Itraconazole may cause patients to develop nerve problems. Patients should contact their physician immediately if they experience the following symptoms:

  • Burning, itching or crawling feelings on the skin
  • Tingling, prickling, numbness or œpins and needles  feelings

When patients are taking Itraconazole, they may experience temporary or permanent hearing loss. If patients notice any changes to their hearing whilst taking this medicine, they should contact their physician straight away.

Taking Itraconazole can make patients feel drowsy, dizzy or less alert than normal. Patients should not operate machinery, drive or carry out any potentially dangerous tasks whilst they are affected by these side-effects.

Due to the risks to the unborn fetus, Itraconazole is not generally prescribed to patients who are pregnant. Itraconazole capsules, in particular, can be dangerous if taken by pregnant patients and may cause harm to the unborn fetus. Due to this, patients should use a reliable form of birth control whilst taking Itraconazole and for at least two months after they have finished their treatment.

If patients are pregnant or are planning to conceive, they should discuss this with their physician before they start taking Itraconazole. If patients become pregnant whilst taking Itraconazole or within two months of taking their last dose of medicine, they should notify their doctor immediately.

If patients who are breastfeeding take Itraconazole, it is likely that the medication will be present in their breast milk and may cause harm to an infant. Due to this, patients are usually advised not to breastfeed whilst taking Itraconazole or for some time after their last dose of medication. If patients are breastfeeding, they should discuss this with their physician before they start taking Itraconazole. Patients should obtain medical advice before breastfeeding if they are currently taking Itraconazole or if they have taken it in the past.

Before patients begin using Itraconazole, they should notify their doctor of any allergies they may have. This includes allergies to medicines, foods, dyes, preservatives and/or animals. In rare cases, patients may develop and allergic response when taking Itraconazole. If so, they will require emergency medical treatment. The symptoms of an allergy may include:

  • Wheezing
  • Trouble swallowing
  • Rash on the skin
  • Itching
  • Hives
  • Trouble breathing
  • Shortness of breath
  • Hoarseness
  • Swallowing of the face, lips, throat, mouth, tongue and/or hands

Storage

When patients are prescribed Itraconazole, they are usually advised to administer a dose of medication at least once per day. Due to this, patients will need to keep a supply of medication at home. When storing Itraconazole at home, patients must ensure that it is in a safe location and that children and/or pets cannot gain access to it.

In addition to this, patients should follow the manufacturer's instructions or medical guidelines when storing Itraconazole solution, capsules or tablets at home. In most cases, Itraconazole can be kept at room temperature but should be kept in a closed container. If capsules or tablets are supplied in a blister pack, for example, they should remain in their original packaging until the patient is ready to take their next dose of medicine.

Itraconazole also needs to be protected from heat, moisture and direct light so patients should keep their medication in a location which is not exposed to extremes of temperature, bright lights, water or condensation.

When patients are advised to stop taking Itraconazole, or if the medication reaches its expiry date, it will need to be disposed of carefully. Medication should not be discarded alongside regular household waste as it may pose a risk to other people. Instead, patients should contact their pharmacist or physician's office and use a designated medicine disposal service.

Summary

As an antifungal agent, Itraconazole can be used to treat numerous types of fungal infections. As these types of infections can affect almost any part of the patient's body, their treatment will depend on whether the infection is acute or systemic. Similarly, the patient's symptoms may indicate how advanced the infection is and what level of treatment is required.

Although Itraconazole can be used to successfully treat fungal infections, it can take some time for the infection to be fully resolved. Often, patients will need to take Itraconazole solution, capsules or tablets for a number of weeks or months in order for their infection to be completely treated.

Whilst the patient's symptoms should be reduced within this timeframe, it is essential that they keep taking their medication. In order for Itraconazole to work properly, the patient will need to take the medication for as long as their physician instructs them to or their infection is likely to return and may even be more severe.

Furthermore, patients should only take Itraconazole in the form they have been prescribed. As Itraconazole works in different ways depending on whether it's taken as a solution, capsule or tablet, patients must use the exact type of Itraconazole that has been prescribed for them.

Providing Itraconazole is taken appropriately and in accordance with a treatment schedule, it is effective in treating the vast majority of fungal infections and is well-tolerated by most patients. As a result, Itraconazole is the first-line treatment for both acute and systemic infections and is a much-used antifungal agent.