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COMPOSITION:
Each ml contains:
Itraconazole IPĀ Ā 10 mg
Flavoured BaseĀ q.s.
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DESCRIPTION:
Felintra 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. Felintra oral solution is a yellow to slightly amber, clear solution containing the active ingredient, traconazole, at 10 mg/mL.
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CLINICAL PHARMACOLOGY:
Pharmacodynamics
The mode of action of FELINTRA (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.
Pharmacokinetics
Itraconazole wasĀ absorbed rapidly following oralĀ administration of FELINTRA (Itraconazole oral solution) to cats. Compared to the fasted state, administration of FELINTRA with food results in slightly higher (1.3 fold) meanĀ total itraconazole exposure. FELINTRA can be administered with or without food. Itraconazole oral solution binds extensively to plasma proteins (> 99%), and distributes throughout the tissues. 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 w/ml post dose at 2 hours (Tmax). The AUC0-24h isĀ 5.09 ug.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 pg/ml), the AUC0-24h is increased 3-fold (15.4 pg.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 pg/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 pg/g (mean 5.2 pg/g) at the end of the third dosing week and concentrations drop slowly to 1.5 pg/g (mean 1.9 pg/g) at 14 days after final dosing. Concentrations of hydroxy-traconazole in hair are insignificant.
INDICATIONS:
FELINTRA oral solution is indicated for the treatment of dermatophytosis caused by Microsporum canis in cats
DOSAGE AND ADMINISTRATION:
Cats: 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.
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CONTRAINDICATIONS:
Do not administer to itraconazole
catsĀ with hypersensitivity to
WARNINGS: FELINTRA (itraconazole oral solution) has not been shown to be safe in pregnant cats. FELINTRA should only be used in pregnant or lactating cats when the benefits outweigh the potential risks
ADVERSE EFFECTS:
Adverse effects related to gastrointestinal tract may occur.
Interactions:
The following drug interactions have been reported in animals receiving Itraconazole:
Amphotericin B: Lab animal studies have shown that itraconazole used concomitantly with amphotericin B may be antagonistic against Aspergillus or Candida.
Antacids: May reduce oral absorption of itraconazole: administer itraconazole at least 1 hour before or 2 hours after antacids
Benzodiazepines (alprazolam, diazepam, midazolam, triazolam): Itraconazole may increase levels Buspirone: Plasma concentrations may be elevated Busulfan: Itraconazole may increase levels Calcium-channel blocking agents (amlodipine,Ā verapamil): Itraconazole may increase levelsĀ Cisapride: Itraconazole may increase cisapride levels.
Corticosteroids: Itraconazole may inhibit the metabolism of corticosteroids; potential for increased adverse effects Cyclophosphamide: Itraconazole may inhibit the metabolism of cyclophosphamide and its metabolites; potential for increased toxicity
Cyclosporine: Increased cyclosporine levels.
Digoxin: traconazole may increase digoxin levels.
Fentanyl/Alfentanil: traconazole may increase fentanyl or alfentanil levels
H2-Blockers (ranitidine, famotidine, etc.): Increased gastric pH may reduce itraconazole absorption
Ivermectin: Itraconazole may increase risk for neurotoxicity
Indication:
- Broad spectrum of activity against pathogenic yeasts and fungi
- Enhanced tissue penetration & residual effect
- Higher safety margin
- Superior antifungal potency & fungicidal activity
Dose:
Pulse treatment in dermatophytosis at 5mg/kg daily for 3 alternating weeks as one week on, one week off
Presentation:
60ml Bottie
