TERCONAZOLE VAGINAL CREAM 0.8%- terconazole cream

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

A-S Medication Solutions

Administration route:

VAGINAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Terconazole vaginal cream 0.8% is indicated for the local treatment of vulvovaginal candidiasis (moniliasis). As terconazole vaginal cream 0.8% 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:

Product: 50090-6299 NDC: 50090-6299-0 20 g in a TUBE, WITH APPLICATOR

Authorization status:

New Drug Application

Summary of Product characteristics

TERCONAZOLE VAGINAL CREAM 0.8%- TERCONAZOLE CREAM
A-S MEDICATION SOLUTIONS
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TERCONAZOLE VAGINAL CREAM 0.8%
DESCRIPTION
Terconazole vaginal cream 0.8% is a white to off-white, water washable
cream for
intravaginal administration containing 0.8% 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 0.8% terconazole 40 mg
(0.8% 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 0.8% 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 total radioactivity was 0.6%. Total radioactivity