Drug intelligence / Profile preview

itraconazole + terbinafine

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

The combination of itraconazole and terbinafine is an antifungal medication used to treat various fungal infections. This combination has shown enhanced efficacy compared to either drug used alone, particularly in resistant fungal infections. ## Mechanism of Action Itraconazole + terbinafine works through complementary mechanisms that target fungal cell membrane synthesis: - Itraconazole inhibits lanosterol 14α-demethylase, an enzyme crucial for ergosterol production in fungal cell membranes[7] - Terbinafine inhibits squalene epoxidase, another key enzyme in the ergosterol biosynthesis pathway[7] This dual inhibition of ergosterol production creates a synergistic antifungal effect that is more potent than either medication used individually[1][2]. ## Clinical Efficacy Clinical studies have demonstrated superior results with the combination therapy: - A randomized clinical trial showed that patients receiving the combination had significantly decreased symptom scores at 14 days compared to monotherapy groups[1] - At 28 days, the combination therapy eradicated fungal infections in 37 patients, compared to 26 in the terbinafine group and 19 in the itraconazole group[1] - The combination achieved a 100% cure rate with shorter treatment time compared to either drug alone[1][2] ## Indications This combination is primarily used for: - Resistant tinea infections (ringworm)[3] - Onychomycosis (fungal nail infections)[5] - Tinea corporis et cruris (fungal infections of the body and groin)[3][5] - Other difficult-to-treat fungal skin infections[1][5] ## Dosage Forms The combination is available as: - Oral tablets[4][5] - Topical creams[5] ## Side Effects Common side effects include: - Headache - Taste changes - Nausea - Vomiting - Diarrhea - Upset stomach - Loss of appetite - Itching - Rash - Elevated liver enzymes[4] ## Special Considerations - Should be taken with food, preferably at the same time each day - Full course of treatment should be completed even if symptoms improve - Reliable contraception should be used during treatment - Antacids should not be taken within two hours of this medication - Liver function may need monitoring during treatment - Caution is advised for patients with pre-existing liver or cardiac conditions[4][5] The combination of itraconazole and terbinafine represents an important therapeutic option for managing resistant fungal infections, with clinical evidence supporting its superior efficacy compared to monotherapy approaches.

Brand names
Darvican OTeriza ITTerbol ITTerbinid ITItorox TItrapro TTerbilan-PlusItrabampItra PlusItroflex
02

Targets

SQLE (Squalene monooxygenase)CYP51A1 (Sterol 14α-demethylase)

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