Sporanox

Oral Administration

Capsule: Take with food if possible

Oral solution: Swish in mouth 10 mL at a time for several seconds, then swallow; take without food if possible 

IV Preparation

Precise dilution (3.33 mg/mL) is required to maintain stability and avoid precipitate formation

Dilute with NS only; do not use dextrose or lactated Ringer solution

Add 25 mL (1 ampule = 250 mg) to 50 mL NS

Mix and withdraw 15 mL of solution before infusing

IV Administration

Using flow-control device, infuse 60 mL of diluted solution (200 mg itraconazole; pH 4.8) over 60 minutes, using extension line and infusion set provided

After administration, flush infusion set with 15-20 mL NS over 30 seconds to 15 minutes via 2-way stopcock; do not use bacteriostatic NS

Discard entire infusion set

GENERIC AVAILABLE: Yes

Itraconazole has not been adequately studied in pregnant women. Cases of congenital abnormalities have been reported. Itraconazole should not be used to treat nail fungal infections (onychomycosis) in pregnant patients. Women of child bearing age undergoing treatment for fungal infections of the nails must use adequate contraception measures while receiving itraconazole and for two months after treatment.

Itraconazole is excreted in human milk. Therefore, it should not be administered to nursing women or, alternatively, breastfeeding should be discontinued.

Tell your doctor if you are breastfeeding or plan to breastfeed. Sporanox is excreted in human breast milk and may harm your nursing baby.

If you think you took too much Sporanox, call your doctor or local poison control center, or go to the nearest hospital emergency room right away.

This medicine may cause blurred vision and may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Avoid taking antacids within 1 hour before or 2 hours after you take itraconazole. Some antacids can make it harder for your body to absorb itraconazole.

• Triazole-derivative azole antifungal.1 2 3 36 37 48

• Both itraconazole and its major metabolite, hydroxyitraconazole, have antifungal activity.1 48

• Usually fungistatic in action.1 48

• Presumably exerts its antifungal activity by altering cellular membranes resulting in increased membrane permeability, leakage of essential elements (e.g., amino acids, potassium), and impaired uptake of precursor molecules (e.g., purine and pyrimidine precursors to DNA).1 48 Inhibits cytochrome P-450 14-α-desmethylase in susceptible fungi, which leads to accumulation of C-14 methylated sterols (e.g., lanosterol) and decreased concentrations of ergosterol.1 48

• Spectrum of antifungal activity includes many fungi, including yeasts and dermatophytes.1 2 3 12 36

• Candida: Active in vitro and in vivo against C. albicans,1 C. guilliermondii,85 C. krusei,1 84 85 C. parapsilosis,82 84 85 and C. tropicalis.82 84 Some strains of C. lusitaniae are inhibited in vitro by itraconazole.80 81 85

• Dermatophytes: Active against Epidermophyton,133 Microsporum,133 Trichophyton mentagrophytes,1 and T. rubrum.1

• Other fungi: Active against Aspergillus (including A. flavus,1 122 A. fumigatus,1 122 A. niger,122 and A. terreus),122 Blastomyces dermatitidis,78 Coccidioides immitis,1 Cryptococcus neoformans,1 82 C. gattii,121 Histoplasma capsulatum,1 H. duboisii,1 Paracoccidioides brasiliensis,1 Penicillium marneffei,118 120 and Sporothrix schenckii.1 94 105 Some zygomycetes, including some strains of Rhizopus,127 Mucor,126 127 Absidia,126 127 Rhizomucor,126 127 Cunninghamella,126 and Apophysomyces elegans,126 are inhibited in vitro by itraconazole. The drug has some activity against Basidiobolus ranarum.104 123

• Itraconazole is not active against Fusarium,1 48 Scedosporium,1 48 or Scopulariopsis,1 48 including S. acremonium and S. brevicaulis.86

• Strains of fungi resistant to itraconazole have been isolated in vitro and from patients who received prolonged therapy with the drug.1 48 Itraconazole-resistant fungi may be cross-resistant to other azole antifungals (e.g., fluconazole, ketoconazole).5 48

Sporanox® is the brand name for itraconazole, an azole antifungal agent. Itraconazole is a 1:1:1:1 racemic mixture of four diastereomers (two enantiomeric pairs), each possessing three chiral centers. It may be represented by the following structural formula and nomenclature:

(±)-1-[(R*)-sec-butyl]-4-[p-[4-[p-[[(2R*,4S*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ2-1,2,4-triazolin-5-one mixture with (±)-1-[(R*)-sec-butyl]-4-[p-[4-[p-[[(2S*,4R*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ2-1,2,4-triazolin-5-one

or

(±)-1-[(RS)-sec-butyl]-4-[p-[4-[p-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ2-1,2,4-triazolin-5-one.

Itraconazole has a molecular formula of C35H38Cl2N8O4 and a molecular weight of 705.64. It is a white to slightly yellowish powder. It is insoluble in water, very slightly soluble in alcohols, and freely soluble in dichloromethane. It has a pKa of 3.70 (based on extrapolation of values obtained from methanolic solutions) and a log (n-octanol/water) partition coefficient of 5.66 at pH 8.1.

Sporanox® (itraconazole) Oral Solution contains 10 mg of itraconazole per mL, solubilized by hydroxypropyl-β-cyclodextrin (400 mg/mL) as a molecular inclusion complex. Sporanox® Oral Solution is clear and yellowish in color with a target pH of 2. Other ingredients are hydrochloric acid, propylene glycol, purified water, sodium hydroxide, sodium saccharin, sorbitol, cherry flavor 1, cherry flavor 2 and caramel flavor.

Sporanox (itraconazole) is an antifungal medicine that fights infections caused by fungus.

Sporanox is used to treat infections caused by fungus, which can invade any part of the body including the lungs, mouth or throat, toenails, or fingernails.

Sporanox may also be used for purposes not listed in this medication guide.

You should not take Sporanox if you have ever had congestive heart failure.

Before taking Sporanox, tell your doctor if you have heart disease, a history of stroke, a heart rhythm disorder, kidney or liver disease, a breathing disorder, cystic fibrosis, or a history of long QT syndrome.

Many drugs can interact with itraconazole, and some drugs should not be used together. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Sporanox.

Life-threatening side effects may occur if you take this medicine with cisapride, dihydroergotamine, disopyramide, dofetilide, dronedarone, eplerenone, ergonovine, ergotamine, felodipine, irinotecan, ivabradine, lurasidone, lovastatin, methadone, methylergonovine, oral midazolam, nisoldipine, pimozide, quinidine, ranolazine, simvastatin, ticagrelor, or triazolam.

If you have liver or kidney disease, you should not take itraconazole with colchicine, fesoterodine, solifenacin, or telithromycin.

You should not take Sporanox to treat a toenail or fingernail infection if you are pregnant or may become pregnant during treatment.

This medicine may cause blurred vision and may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Avoid taking antacids within 1 hour before or 2 hours after you take Sporanox. Some antacids can make it harder for your body to absorb itraconazole.

Get emergency medical help if you have signs of an allergic reaction to Sporanox: hives, severe skin rash, tingling in your arms or legs; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop taking Sporanox and call your doctor at once if you have:

• confusion, a light-headed feeling (like you might pass out);

• blurred vision, double vision, ringing in your ears, problems with hearing;

• fast heartbeats;

• numbness or tingly feeling, loss of bladder control;

• severe pain in your upper stomach spreading to your back, nausea and vomiting;

• little or no urinating, pain or burning when you urinate;

• signs of congestive heart failure - shortness of breath (even with mild exertion), cough with mucus, fast heartbeats, swelling, rapid weight gain, sleep problems; or

• liver problems - nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Common Sporanox side effects may include:

• headache, dizziness;

• nausea, vomiting, upset stomach, constipation;

• fever, muscle aches;

• impotence, erection problems; or

• changes in your menstrual periods.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Many drugs can interact with itraconazole, and some drugs should not be used together. Tell your doctor about all your current medicines and any you start or stop using, especially:

• an antibiotic;

• antipsychotic medicine or a sedative;

• an antiviral medicine to treat hepatitis C or HIV/AIDS;

• medicine to prevent blood clots;

• cancer medicine;

• drugs to treat urinary problems;

• heart or blood pressure medication;

• immunosuppressants, or medicine to prevent organ transplant rejection;

• medicine to treat high cholesterol;

• migraine headache medication;

• narcotic (opioid) pain medicine;

• seizure medicine; or

• steroid medication.

This list is not complete and many other drugs can interact with itraconazole. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed here. Give a list of all your medicines to any healthcare provider who treats you.