TERCONAZOLE suppository

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Cosette Pharmaceuticals, Inc.

INN (International Name):

Terconazole

Composition:

Terconazole 80 mg

Administration route:

VAGINAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Terconazole Vaginal Suppositories, 80 mg 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 suppositories.

Product summary:

Terconazole Vaginal Suppositories 80 mg are available as 2.5 g, elliptically-shaped white to off-white suppositories in packages of three with a vaginal applicator. NDC 0713-0552-73 Store at 20°- 25°C (68°- 77°F) [see USP Controlled Room Temperature].

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TERCONAZOLE- TERCONAZOLE SUPPOSITORY
COSETTE PHARMACEUTICALS, INC.
----------
TERCONAZOLE
VAGINAL SUPPOSITORIES 80 MG
RX ONLY
DESCRIPTION
Terconazole Vaginal Suppositories are white to off-white suppositories
for intravaginal
administration containing 80 mg 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, in triglycerides derived from coconut and/or palm
kernel oil (a base
of hydrogenated vegetable oils) and butylated hydroxyanisole.
The structural formula of terconazole is as follows:
TERCONAZOLE
C
H
Cl
N
O
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
ABSORPTION
Following a single intravaginal application of a suppository
containing 240 mg
C-
terconazole to healthy women, approximately 70% (range: 64 to 76%) of
terconazole
remains in the vaginal area during the suppository retention period
(16 hours);
approximately 10% (range: 5 to 16%) of the administered radioactivity
was absorbed
systemically over 7 days. Maximum plasma concentrations of terconazole
occur 5 to 10
hours after intravaginal application of the cream or suppository.
Systemic exposure to
terconazole is approximately proportional to the applied dose, whether
as the cream or
suppository. The rate and extent of absorption of terconazole are
similar in patients with
vulvovaginal candidiasis (pregnant or non-pregnant) and healthy
subjects.
26
31
2
5
3
14
DISTRIBUTION
Terconazole is highly protein bound (94.9%) in human plasma and the
degree of binding
is independent of drug concentration over the range of 0.01 to 5.0
mcg/mL.
METABOLISM
Systemically absorbed terconazole is extensively metabolized (>95%).
ELIMINATION
Across various studies in healthy women, after single or multiple
intravaginal
administration of terconazole as the cream or suppository/ovule, the
mean eliminati