TERCONAZOLE cream

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

TERCONAZOLE (UNII: 0KJ2VE664U) (TERCONAZOLE - UNII:0KJ2VE664U)

Available from:

H.J. Harkins Company, Inc.

INN (International Name):

TERCONAZOLE

Composition:

TERCONAZOLE 4 mg in 1 g

Administration route:

VAGINAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Terconazole Vaginal Cream is indicated for the local treatment of vulvovaginal candidiasis (moniliasis). As this product is effective only for vulvovaginitis caused by the genus Candida, the diagnosis should be confirmed by KOH smears and/or cultures. Patients known to be hypersensitive to terconazole or to any of the components of the cream.

Product summary:

Terconazole Vaginal Cream 0.4% is available in 45 g (NDC 0591-3196-89) tubes with a measured-dose applicator. Store at Controlled Room Temperature 15° - 30° C (59° - 86° F). Terconazole Vaginal Cream 0.4% is available in 20 g (NDC 0591-3197-52) tubes with a measured-dose applicator. Store at Controlled Room Temperature 15° - 30° C (59° - 86° F).

Authorization status:

New Drug Application

Summary of Product characteristics

TERCONAZOLE - TERCONAZOLE CREAM
H.J. HARKINS COMPANY, INC.
----------
TERCONAZOLE VAGINAL CREAM 0.4%
7-DAY REGIMEN
TERCONAZOLE VAGINAL CREAM 0.4%
3-DAY REGIMEN
DES CRIPTION
Terconazole Vaginal Cream 0.4% is a white to off-white, water washable
cream for intravaginal
administration containing 0.4% of the antifungal agent terconazole,
_cis_-1-[_p_-[[2-(2,4-Dichlorophenyl)-2-
(1_H_-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-4-isopropylpiperazine,
compounded
in a cream base consisting of butylated hydroxyanisole, cetyl alcohol,
isopropyl myristate, polysorbate
60, polysorbate 80, propylene glycol, stearyl alcohol, and purified
water.
The structural formula of terconazole is as follows:
Terconazole, a triazole derivative, is a white to almost white powder
with a molecular weight of
532.47. It is insoluble in water; sparingly soluble in ethanol; and
soluble in butanol.
CLINICAL PHARMACOLOGY
Following intravaginal administration of terconazole in humans,
absorption ranged from 5–8% in three
hysterectomized subjects and 12–16% in two non-hysterectomized
subjects with tubal ligations.
Following daily intravaginal administration of 0.4% terconazole 40 mg
(0.4% cream x 5 g) for seven
days to normal humans, plasma concentrations were low and gradually
rose to a daily peak (mean of 5.9
ng/mL or 0.006 mcg/mL) at 6.6 hours.
Results from similar studies in patients with vulvovaginal candidiasis
indicate that the slow rate of
absorption, the lack of accumulation, and the mean peak plasma
concentration of terconazole was not
different from that observed in healthy women. The absorption
characteristics of terconazole 0.4% in
pregnant or non-pregnant patients with vulvovaginal candidiasis were
also similar to those found in
normal volunteers.
Following oral (30 mg) administration of
C-labelled terconazole, the harmonic half-life of elimination
from the blood for the parent terconazole was 6.9 hours (range
4.0–11.3). Terconazole is extensively
metabolized; the plasma AUC for terconazole compared to the AUC for