Itraconazole is a triazole antifungal
agent prescribed to patients with fungal infections. The drug may be
given orally or intravenously. It is prescribed for systemic infections,
such as aspergillosis, candidiasis, and cryptococcosis, where other
antifungal drugs are inappropriate or ineffective. It has also recently
been explored as an anticancer agent for patients with basal cell
carcinoma, non-small cell lung cancer, and prostate cancer.
Mechanism of Action
It inhibits the fungal-mediated synthesis of ergosterol. Because of its ability to inhibit cytochrome P450 3A4 CC-3, caution should be used when considering interactions with other medications.
Dosing & Uses
1. Life-Threatening Infections
200 mg PO q8hr initially for 3-4 days, then 200-400 mg/day for at least 3 months
2. Blastomycosis
200 mg PO q8hr for 3 days, then 200 mg PO q12hr for 6-12 months
3. Aspergillosis
200-400 mg/day PO; may be used in combination with corticosteroids
4. Histoplasmosis
200 mg/day PO; may be increased by 100 mg/day increments; not to exceed 400 mg/day
5. Onychomycosis
Fingernails: 2 treatment pulses, each consisting of 200 mg q12hr for 1 week
Toenails, with or without fingernail involvement: 200 mg/day PO for 12 weeks
6. Oral Candidiasis
Oral solution: 100-200 mg/day for at least 3 weeks; continued for 2 weeks after symptom resolution
Refractory to fluconazole: 100 mg PO q12hr for 2-4 weeks
Swish in mouth 10 mL at a time for several seconds, then swallow; take without food if possible
7. Otomycosis
Suspension: Topical treatment of fungal otitis externa (otomycosis)
Before Taking Itraconazole
Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking itraconazole it is important that your doctor knows :
- If you are pregnant or breast-feeding.
- If you have liver or kidney problems.
- If you have any heart or lung problems.
- If you have porphyria (this is a rare inherited blood disorder).
- If you have ever had an allergic reaction to a medicine.
- If you are taking any other medicines. This includes any medicines you are taking which are available to buy without a prescription, such as herbal and complementary medicines.
Adverse Effects
Itraconazole is a relatively well-tolerated drug (although not as well tolerated as fluconazole or voriconazole) and the range of adverse effects it produces is similar to the other azole antifungals.
1. Elevated alanine aminotransferase levels are found in 4% of people taking itraconazole
2. "Small but real risk" of developing congestive heart failure
3. Liver failure, sometimes fatal
4. Others :
- Nausea
- Vomiting
- Abdominal pain
- Loss of appetite
- Itching
- Yellow skin (jaundice)
- Dark urine
- Pale stool
- Headache
Mechanism of Action
It inhibits the fungal-mediated synthesis of ergosterol. Because of its ability to inhibit cytochrome P450 3A4 CC-3, caution should be used when considering interactions with other medications.
Dosing & Uses
1. Life-Threatening Infections
200 mg PO q8hr initially for 3-4 days, then 200-400 mg/day for at least 3 months
2. Blastomycosis
200 mg PO q8hr for 3 days, then 200 mg PO q12hr for 6-12 months
3. Aspergillosis
200-400 mg/day PO; may be used in combination with corticosteroids
4. Histoplasmosis
200 mg/day PO; may be increased by 100 mg/day increments; not to exceed 400 mg/day
5. Onychomycosis
Fingernails: 2 treatment pulses, each consisting of 200 mg q12hr for 1 week
Toenails, with or without fingernail involvement: 200 mg/day PO for 12 weeks
6. Oral Candidiasis
Oral solution: 100-200 mg/day for at least 3 weeks; continued for 2 weeks after symptom resolution
Refractory to fluconazole: 100 mg PO q12hr for 2-4 weeks
Swish in mouth 10 mL at a time for several seconds, then swallow; take without food if possible
7. Otomycosis
Suspension: Topical treatment of fungal otitis externa (otomycosis)
Before Taking Itraconazole
Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking itraconazole it is important that your doctor knows :
- If you are pregnant or breast-feeding.
- If you have liver or kidney problems.
- If you have any heart or lung problems.
- If you have porphyria (this is a rare inherited blood disorder).
- If you have ever had an allergic reaction to a medicine.
- If you are taking any other medicines. This includes any medicines you are taking which are available to buy without a prescription, such as herbal and complementary medicines.
Adverse Effects
Itraconazole is a relatively well-tolerated drug (although not as well tolerated as fluconazole or voriconazole) and the range of adverse effects it produces is similar to the other azole antifungals.
1. Elevated alanine aminotransferase levels are found in 4% of people taking itraconazole
2. "Small but real risk" of developing congestive heart failure
3. Liver failure, sometimes fatal
4. Others :
- Nausea
- Vomiting
- Abdominal pain
- Loss of appetite
- Itching
- Yellow skin (jaundice)
- Dark urine
- Pale stool
- Headache
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