Itraconazole

For the treatment of dermatophytosis caused by Microsporum canis in cats.

Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Itrafungol®

ITRAFUNGOL oral solution is indicated for the treatment of dermatophytosis caused by Microsporum canis in cats.

Itrafungol®(itraconazole oral solution)

The mode of action of itraconazole is based on its highly selective binding ability to fungal cytochrome p-450 iso-enzymes. This inhibits the synthesis of ergosterol and affects membrane-bound enzyme function and membrane permeability. This effect is irreversible and causes structural degeneration of the fungal organism. Itraconazole was absorbed rapidly following oral administration of ITRAFUNGOL oral solution to laboratory cats. Compared to the fasted state, administration of ITRAFUNGOL oral solution with food results in slightly higher (1.3 fold) mean total itraconazole exposure (AUC), delay in median Tmax (Fed 4 hours vs. Fasted 2 hours) and significant decrease (approximately 0.55 fold) in maximum plasma concentration (Cmax). ITRAFUNGOL oral solution can be administered with or without food. Itraconazole oral solution binds extensively to plasma proteins (> 99%), and distributes well to tissues. More than 30 metabolites are formed. Hydroxy-itraconazole is the parent metabolite and has antifungal activity. Excretion is rapid and primarily via the feces. In cats, a single oral dose of 5 mg/kg results in a Cmax of 0.525 μg/mL post dose at 2 hours (Tmax). The AUC0-24h is 5.09 µg·h/mL and the half-life in plasma is 12.1 hours. After repeated daily administration for seven days at 5 mg/kg/day, the Cmax is doubled (1.05 μg/mL), the AUC0-24h is increased 3-fold (15.4 µg·h/ mL) and the plasma half-life is increased to 36 hours. In the therapeutic treatment schedule, itraconazole is almost completely cleared from plasma after each wash-out period. The hydroxy-itraconazole remains near or below the quantification limit in feline plasma after a single dose of itraconazole oral solution at 5 mg/kg. However, after repeated daily doses of itraconazole oral solution at 5 mg/kg for one week, the hydroxy-itraconazole Cmax of 0.059 µg/mL was reached at 2 hours (Tmax). Itraconazole concentrations in cat’s hair vary; an increase occurs during treatment to a median value of 3.0 μg/g (mean 5.2 μg/g) at the end of the third dosing week and concentrations drop slowly to 1.5 μg/g (mean 1.9 μg/g) at 14 days after final dosing. Concentrations of hydroxy-itraconazole in hair are insignificant

Itrafungol®(itraconazole oral solution)

Do not administer to cats with hypersensitivity to itraconazole.

Itrafungol®(itraconazole oral solution)

Not for use in humans. Keep this and all medications out of reach of children. Wash hands and exposed skin after use. In case of accidental contact with eyes, rinse thoroughly with water. In case of pain or irritation, seek medical advice. In case of accidental ingestion, rinse mouth with water and seek medical advice. Special precautions for person administering the veterinary product to the animal: Microsporum canis dermatophytosis is a zoonotic disease (a disease that can be transmitted from animals to humans); therefore consult a physician if a suspected lesion occurs on a human. Wear protective gloves when handling the animal during treatment or when cleaning the syringe. Wash hands and exposed skin after handling the animal. ITRAFUNGOL (itraconazole oral solution) has not been shown to be sporicidal; therefore in order to reduce zoonotic potential, environmental contamination, and to decrease course of the disease, topical and environmental treatment should also be utilized. Animal Safety Warnings ITRAFUNGOL oral solution has not been shown to be safe in pregnant cats (see Animal Safety). ITRAFUNGOL oral solution should only be used in pregnant or lactating cats when the benefits outweigh the potential risks. Keep ITRAFUNGOL oral solution in a secure location out of reach of dogs, cats, and other animals to prevent accidental ingestion or overdose.

Itrafungol®(itraconazole oral solution)

Post-Approval Experience (2021) The following adverse events are based on post-approval adverse drug experience reporting for ITRAFUNGOL (itraconazole oral solution). Not all adverse events are reported to FDA/CVM. It is not always possible to reliably estimate the adverse event frequency or establish a causal relationship to product exposure using these data. The following adverse events reported in cats are listed in decreasing order of reporting frequency: Anorexia, emesis, elevated liver enzymes, lethargy, weight loss, icterus, elevated total bilirubin, and diarrhea. Death (including euthanasia) has been reported. Some of these deaths were associated with the adverse events reported above.

Itrafungol®(itraconazole oral solution)

5 mg/kg (0.5 mL/kg) body weight administered once daily on alternating weeks for 3 treatment cycles.

Oral

Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Itrafungol®

The solution should be administered orally using the enclosed graduated dosing syringe. The daily dosage is 5 mg/kg (0.5 mL/kg) body weight administered once daily on alternating weeks for 3 treatment cycles. Cats are treated during weeks 1, 3, and 5, and left untreated during weeks 2 and 4. 7 days 7 days 7 days 7 days 7 days Daily treatment No treatment Daily treatment No treatment Daily treatment Each line on the dosing syringe represents 0.05 mL of oral solution. Table 1: Dose Table for ITRAFUNGOL Weight of Cat Volume of ITRAFUNGOL 0.5 lb 0.1 mL 1.0 lb 0.2 mL 1.5 lb 0.35 mL 2.0 lb 0.45 mL 2.5 lb 0.55 mL 3.0 lb 0.7 mL 3.5 lb 0.8 mL 4.0 lb 0.9 mL 4.5 lb 1.0 mL 5.0 lb 1.15 mL 6.0 lb 1.35 mL 7.0 lb 1.6 mL 8.0 lb 1.8 mL 9.0 lb 2.0 mL 10.0 lb 2.25 mL 11.0 lb 2.5 mL 12.0 lb 2.7 mL 13.0 lb 3.0 mL The solution should be administered orally using the enclosed graduated dosing syringe. Keep the bottle upright and insert the dosing syringe through the opening of the top of the bottle (Figure 1). Do not invert the bottle (Figure 2). Fill the syringe by pulling the plunger until it reaches the graduation corresponding to the correct mL dose as indicated at the top of the syringe ring (Figure 3). Treat the cat by slowly and gently administering the liquid into the mouth, allowing the cat to swallow the product (Figure 4). For cats weighing more than 13.0 lbs, the total dose will need to be calculated and given over two doses as the dosing syringe only holds 3.0 mL of solution. After dosing, do not replace syringe in the bottle. Rinse and dry the syringe. The bottle cap should be screwed back on tightly.

ORAL

Itrafungol®(itraconazole oral solution)