A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Naftin Gel Pharmacology, Pharmacokinetics, Studies, Metabolism - Naftifine
Naftin Gel Pharmacology, Pharmacokinetics, Studies, Metabolism - Naftifine
CLINICAL PHARMACOLOGY
Naftifine hydrochloride
is a synthetic, allylamine
derivative. The following in vitro data are available, but their
clinical significance
is unknown. Naftifine hydrochloride
has been shown to exhibit fungicidal activity
in vitro against a broad spectrum
of organisms including Trichophyton
rubrum, Trichophyton mentagrophytes, Trichophyton
tonsurans, Epidermophyton
floccosum, and Microsporum
canis, Microsporum
audouini, and Microsporum
gypseum; and fungistatic activity
against Candida species
including Candida albicans.
NAFTIN Gel 1% has only been shown to be clinically effective against
the disease entities listed in the INDICATIONS
AND USAGE section.
Although the exact mechanism
of action against fungi
is not known, naftifine hydrochloride appears to interfere with
sterol biosynthesis
by inhibiting the enzyme
squalene 2,3-epoxidase.
This inhibition of
enzyme activity
results in decreased amounts of sterols, especially ergosterol,
and a corresponding accumulation of squalene
in the cells.
Pharmacokinetics
In vitro and in vivo bioavailability
studies have demonstrated that naftifine penetrates the stratum
corneum in sufficient
concentration to inhibit the growth
of dermatophytes. Following single topical
applications of 3H-labeled naftifine gel
1% to the skin of healthy
subjects, up to 4.2% of the applied dose
was absorbed. Naftifine and/or its metabolites are excreted via
the urine and feces
with a half-life of
approximately two to three days.
top
