Itraconazole: Difference between revisions
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* Azole antifungal |
* Azole antifungal |
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* Indications include {{#ask: [[Is treated by::itraconazole]]}} |
* Indications include {{#ask: [[Is treated by::itraconazole]]}} |
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| + | |||
| + | === Pharmacokinetics === |
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| + | |||
| + | * Blood concentrations are about 30% higher with oral solution compared to oral capsules |
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| + | * Wide intersubject variability in levels |
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| + | * Serum half-life is long |
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| + | * Metabolized by [[Metabolized by::CYP3A4]] and inhibits [[Inhibits:CYP3A4]] |
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| + | * Excreted in urine and feces |
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== Dosing == |
== Dosing == |
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| + | * Preference for oral solution rather than capsules in severe infections (see PK section above) |
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| + | * Can consider initial loading doses with IV or p.o |
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* Typical dose: 200 mg p.o. twice daily |
* Typical dose: 200 mg p.o. twice daily |
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* May be used once daily for the treatment of some [[Candida|candidal]] or [[dermatophytes|dermatophytic]] infections |
* May be used once daily for the treatment of some [[Candida|candidal]] or [[dermatophytes|dermatophytic]] infections |
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=== Therapeutic Drug Monitoring === |
=== Therapeutic Drug Monitoring === |
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| + | * Recommended in more serious or severe infections |
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* Should be measured 5 to 7 days after starting or changing the dose, or when interacting medications are changed |
* Should be measured 5 to 7 days after starting or changing the dose, or when interacting medications are changed |
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| + | ** Can likely be collected at any time after steady-state is reached, due to long halflife |
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| − | * Target in prophylaxis is a trough ot 0.5 mg/L |
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| − | * Target in |
+ | * Target in prophylaxis is a trough level of 0.5 µg/mL |
| + | * Target in treatment is a trough level greater than 0.5 µg/mL, or greater than 0.5 to 1 µg/mL for [[blastomycosis]] |
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| + | * Toxicity likely increased at trough levels greated than 10 µg/mL |
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=== Adverse Drug Reactions === |
=== Adverse Drug Reactions === |
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* [[Adverse drug reaction::Hepatotoxicity]] |
* [[Adverse drug reaction::Hepatotoxicity]] |
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* [[Adverse drug reaction::QTc prolongation]] |
* [[Adverse drug reaction::QTc prolongation]] |
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| + | |||
| + | == Further Reading == |
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| + | |||
| + | * Therapeutic drug monitoring (TDM) of antifungal agents: guidelines from the British Society for Medical Mycology. ''J Antimicrob Chemother.'' 2014;69(5):1162-1176. doi: [https://doi.org/10.1093/jac/dkt508 10.1093/jac/dkt508] |
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[[Category:Triazoles]] |
[[Category:Triazoles]] |
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Revision as of 10:06, 23 September 2024
Background
- Azole antifungal
- Indications include Alternaria, Blastomyces dermatitidis, Chromoblastomycosis, Coccidioides immitis, Cryptococcus, Entomophthoromycotina, Exophiala, Exserohilum, Fonsecaea, Histoplasma capsulatum, Mycetoma, Paracoccidioides brasiliensis, Sappinia diploidea, Sporothrix schenckii
Pharmacokinetics
- Blood concentrations are about 30% higher with oral solution compared to oral capsules
- Wide intersubject variability in levels
- Serum half-life is long
- Metabolized by CYP3A4 and inhibits Inhibits:CYP3A4
- Excreted in urine and feces
Dosing
- Preference for oral solution rather than capsules in severe infections (see PK section above)
- Can consider initial loading doses with IV or p.o
- Typical dose: 200 mg p.o. twice daily
- May be used once daily for the treatment of some candidal or dermatophytic infections
Safety
Therapeutic Drug Monitoring
- Recommended in more serious or severe infections
- Should be measured 5 to 7 days after starting or changing the dose, or when interacting medications are changed
- Can likely be collected at any time after steady-state is reached, due to long halflife
- Target in prophylaxis is a trough level of 0.5 µg/mL
- Target in treatment is a trough level greater than 0.5 µg/mL, or greater than 0.5 to 1 µg/mL for blastomycosis
- Toxicity likely increased at trough levels greated than 10 µg/mL
Adverse Drug Reactions
Further Reading
- Therapeutic drug monitoring (TDM) of antifungal agents: guidelines from the British Society for Medical Mycology. J Antimicrob Chemother. 2014;69(5):1162-1176. doi: 10.1093/jac/dkt508
