- March 15, 2022
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Brand Name :
Tolsura , Onmel, Sporanox
Synonyms :
itraconazole
Class :
Antifungals, Systemic
Dosage Forms & Strengths
Capsule
65mg (Tolsura)
100mg (Sporanox, generic)
Oral solution
10mg/mL (Sporanox, generic)
Tablet
200mg (Onmel)
Safety and efficacy not established
Refer adult dosing
It may enhance the effect when combined with lonafarnib by affecting CYP3A4 metabolism
itraconazole: they may diminish the serum concentration of antacids
itraconazole: they may diminish the serum concentration of antacids
itraconazole: they may diminish the serum concentration of antacids
itraconazole: they may diminish the serum concentration of antacids
itraconazole: they may diminish the serum concentration of antacids
It may enhance the effect when combined with irinotecan liposomal by affecting CYP3A4 metabolism
when both drugs are combined, there may be an increased effect of nilotinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
may enhance the concentration of serum when combined with isavuconazonium sulfate
It may enhance the serum concentration when combined with clobetasone
when both drugs are combined, there may be a decreased metabolism of vinblastine
when both drugs are combined, there may be a reduced metabolism of erlotinib
QTc interval increases on taking itraconazole and lenvatinib together. Avoid or take an alternate drug
the effect of itraconazole is increased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
itraconazole increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of itraconazole
it will increase the impact or level of regorafenib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
may increase the level of effectiveness through P-glycoprotein MDR1 efflux transporter
may increase the serum concentration
may increase the serum concentration
may enhance the serum concentration when combined
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may increase the level of serum concentration of itraconazole
may decrease the level of serum concentrations of itraconazole
may decrease the level of serum concentrations of itraconazole
may decrease the level of serum concentrations of itraconazole
may decrease the level of serum concentrations of itraconazole
may decrease the level of serum concentrations of itraconazole
may increase the serum concentration of itraconazole
may increase the serum concentration of itraconazole
may increase the serum concentration of itraconazole
may increase the serum concentration of itraconazole
may increase the serum concentration of itraconazole
It may enhance the effect when combined with cannabidiol by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
itraconazole: they may enhance the serum concentration of rifabutin
when ajmaline is used together with itraconazole, the risk or seriousness of QTc prolongation is enhanced
increase the therapeutic effects of busulfan by inhibiting metabolism
when both drugs are combined, there may be a decreased metabolism of etoposide
has a synergistic effect over brentuximab vedotin by showing altered intestinal/hepatic CYP3A4 enzyme metabolism.
increase the therapeutic effect of daunorubicin by P-glycoprotein efflux transporter
increase the therapeutic effect of idarubicin by P-glycoprotein efflux transporter
may enhance the serum concentration
may diminish the amount of P-glycoprotein (MDR1) efflux transporter
it increases the effect of loperamide when used simultaneously
metronidazole enhances the effect of itraconazole by altering the intestinal or hepatic CYP3A4 enzyme metabolism
Actions and Spectrum:
itraconazole is an antifungal medication that is used to treat a variety of fungal infections.
itraconazole has a broad spectrum of activity against a variety of fungal organisms, including Aspergillus species, Candida species, Histoplasma capsulatum, Blastomyces dermatitidis, and Cryptococcus neoformans. It is also effective against some dermatophytes, such as Trichophyton rubrum and Microsporum canis.
Frequency Defined
1-10%
Edema (4%)
Vomiting (5%)
Headache (4%)
Diarrhea (3%)
Rash (9%)
Abnormal liver function test results (3%)
Fever (3%)
Hypertension (3%)
Fatigue (3%)
Pruritus (3%)
Dizziness (2%)
Abdominal pain (2%)
>10%
Nausea (11%)
Black Box Warning:
The black box warning of itraconazole is related to its potential to cause serious and sometimes fatal side effects, particularly in patients with underlying heart conditions.
Contraindication/Caution:
Pregnancy warnings:
Pregnancy category: N/A
Lactation: Excreted into human milk is known
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
Itraconazole is an antifungal medication that belongs to the triazole class of drugs. It is used to treat fungal infections caused by a variety of fungi, including Aspergillus, Candida, and Histoplasma.
Pharmacodynamics:
Mechanism of action
itraconazole works by inhibiting the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase. This enzyme is responsible for converting lanosterol to ergosterol, which is an essential component of fungal cell membranes. By inhibiting this enzyme, itraconazole prevents the formation of ergosterol, leading to membrane disruption and fungal cell death.
Pharmacokinetics:
Absorption
itraconazole is available in oral capsules, tablets, and oral solution forms. The absorption of itraconazole from the gastrointestinal tract is influenced by the formulation, food intake, and gastric pH
Distribution
After absorption, itraconazole is distributed to various tissues in the body, including the skin, nails, and organs. Itraconazole is highly lipophilic, and it can penetrate cell membranes and accumulate in tissues. The distribution of itraconazole in tissues is influenced by the tissue blood flow and protein binding
Metabolism
itraconazole undergoes extensive hepatic metabolism by cytochrome P450 enzymes, particularly CYP3A4
Elimination and Excretion
The elimination half-life of itraconazole is about 21 hours. About 3-18% of the drug is eliminated in the urine, while most of the drug and its metabolites are eliminated in the feces. Itraconazole is mainly eliminated by biliary excretion.
Administration:
itraconazole is an antifungal medication used to treat a variety of fungal infections. It is usually administered orally in the form of capsules, tablets, or oral solution.
The recommended dose of itraconazole varies depending on the condition being treated and the severity of the infection. It is important to follow the dosing instructions provided by your healthcare provider or pharmacist.
itraconazole capsules should be taken with a full meal or acidic beverage to increase absorption. The capsules should be swallowed whole and not chewed or crushed. The oral solution should be taken on an empty stomach at least one hour before or two hours after a meal.
Patient information leaflet
Generic Name: itraconazole
Why do we use itraconazole?
itraconazole is an antifungal medication used to treat a variety of fungal infections. It is effective against a wide range of fungal organisms, including Aspergillus species, Candida species, and some dermatophytes.
Some of the conditions that may be treated with itraconazole include:
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