Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1492
| Predicate | Object |
|---|---|
| rdf:type | |
| rdfs:label |
Terazol 3 (Cream)
|
| dailymed-instance:dosage |
TERAZOL 7 (terconazole)
Vaginal Cream 0.4%: One full applicator (5 g) of TERAZOL 7 Vaginal Cream (20
mg terconazole) should be administered intravaginally once daily at bedtime
for seven consecutive days.<br/>TERAZOL 3 (terconazole)
Vaginal Cream 0.8%: One full applicator (5 g) of TERAZOL 3 Vaginal Cream (40
mg terconazole) should be administered intravaginally once daily at bedtime
for three consecutive days.<br/>TERAZOL 3 (terconazole)
Vaginal Suppositories 80 mg: One TERAZOL 3 Vaginal Suppository (80 mg terconazole) should
be administered intravaginally once daily at bedtime for three consecutive
days. Before prescribing another course of therapy,
the diagnosis should be reconfirmed by smears and/or cultures and other pathogens
commonly associated with vulvovaginitis ruled out. The therapeutic effect
of these products is not affected by menstruation.
|
| dailymed-instance:descripti... |
TERAZOL 7 (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-(1H-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. TERAZOL 3
(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-(1H-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. TERAZOL 3
(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-(1H-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 CHClNO 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.
|
| dailymed-instance:clinicalP... |
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��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
ofC-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 was eliminated
from the blood with a harmonic half-life of 52.2 hours (range 44���60).
Excretion of radioactivity was both by renal (32���56%) and fecal (47���52%)
routes. In vitro ,
terconazole is highly protein bound (94.9%) and the degree of binding is independent
of drug concentration. Photosensitivity reactions were
observed in some normal volunteers following repeated dermal application of
terconazole 2.0% and 0.8% creams under conditions of filtered artificial ultraviolet
light. Photosensitivity reactions have not been observed
in U.S. and foreign clinical trials in patients who were treated with terconazole
suppositories or vaginal cream (0.4% and 0.8%).<br/>Microbiology: Terconazole exhibits fungicidal activity in
vitro against Candida albicans.
Antifungal activity has also been demonstrated against other fungi. The MIC
values of terconazole against most Lactobacillus
spp. typically found in the human vagina were���128 mcg/mL;
therefore these beneficial bacteria are not affected by drug treatment. The
exact pharmacologic mode of action of terconazole is uncertain; however, it
may exert its antifungal activity by the disruption of normal fungal cell
membrane permeability. No resistance to terconazole has developed during successive
passages of C. albicans.
|
| dailymed-instance:activeIng... | |
| dailymed-instance:contraind... |
Patients known to be hypersensitive to terconazole or to
any of the components of the cream or suppositories.
|
| dailymed-instance:supply |
TERAZOL 7 (terconazole) Vaginal Cream 0.4%
is available in 45g (NDC 0062-5350-01) tubes with an ORTHO* Measured-Dose
Applicator. Store at Controlled Room Temperature 15���30��C (59���86��F). TERAZOL 3
(terconazole) Vaginal Cream 0.8% is available in 20g (NDC 0062-5356-01) tubes
with an ORTHO* Measured-Dose Applicator. Store at Controlled Room Temperature
15���30��C (59���86��F). TERAZOL 3
(terconazole) Vaginal Suppositories 80 mg are available as 2.5g, elliptically-shaped
white to off-white suppositories in packages of three (NDC 0062-5351-01) with
a vaginal applicator. Store at Controlled Room Temperature 15���30��C
(59���86��F).
|
| dailymed-instance:genericDr... | |
| dailymed-instance:activeMoi... | |
| dailymed-instance:inactiveI... | |
| dailymed-instance:precautio... |
General: Discontinue use and do not retreat with terconazole if sensitization,
irritation, fever, chills or flu-like symptoms are reported during use. The
base contained in the suppository formulation may interact with certain rubber
or latex products, such as those used in vaginal contraceptive diaphragms;
therefore concurrent use is not recommended.<br/>Laboratory Tests: If there is lack of response to terconazole, appropriate
microbiologic studies (standard KOH smear and/or cultures) should be repeated
to confirm the diagnosis and rule out other pathogens.<br/>Drug Interactions:<br/>TERAZOL 7 (terconazole)
Vaginal Cream 0.4% and TERAZOL 3 (terconazole) Vaginal Suppositories
80 mg: The therapeutic effect of these products is not affected
by oral contraceptive usage.<br/>TERAZOL 3 (terconazole)
Vaginal Cream 0.8%: The levels of estradiol (E2) and progesterone did not differ
significantly when 0.8% terconazole vaginal cream was administered to healthy
female volunteers established on a low dose oral contraceptive.<br/>Carcinogenesis, Mutagenesis, Impairment
of Fertility:<br/>Carcinogenesis: Studies to determine the carcinogenic potential of terconazole
have not been performed.<br/>Mutagenicity: Terconazole was not mutagenic when tested in
vitro for induction of microbial point mutations (Ames test), or
for inducing cellular transformation, or in vivo for chromosome breaks (micronucleus test) or dominant lethal mutations
in mouse germ cells.<br/>Impairment of Fertility: No impairment of fertility occurred when female rats were
administered terconazole orally up to 40 mg/kg/day for a three month period.<br/>Pregnancy:<br/>Teratogenic Effects:<br/>Nursing Mothers: It is not known whether this drug is excreted in human milk.
Animal studies have shown that rat offspring exposed via the milk of treated
(40 mg/kg/orally) dams showed decreased survival during the first few post-partum
days, but overall pup weight and weight gain were comparable to or greater
than controls throughout lactation. Because many drugs are excreted in human
milk, and because of the potential for adverse reaction in nursing infants
from terconazole, a decision should be made whether to discontinue nursing
or to discontinue the drug, taking into account the importance of the drug
to the mother.<br/>Pediatric Use: Safety and efficacy in children have not been established.<br/>Geriatric Use: Clinical studies of TERAZOL did not include
sufficient numbers of subjects aged 65 and over to determine whether they
respond differently from younger subjects. Other reported clinical experience
has not identified differences in responses between the elderly and younger
patients.
|
| dailymed-instance:overdosag... |
Overdose of terconazole in humans has not been reported to
date. In the rat, the oral LD 50 values were found to be 1741 and 849 mg/kg
for the male and female, respectively. The oral LD 50 values for the male
and female dog were���1280 and���640 mg/kg, respectively.
|
| dailymed-instance:genericMe... |
terconazole
|
| dailymed-instance:fullName |
Terazol 3 (Cream)
|
| dailymed-instance:adverseRe... |
TERAZOL 7 (terconazole)
Vaginal Cream 0.4%: During controlled clinical studies conducted in the United
States, 521 patients with vulvovaginal candidiasis were treated with terconazole
0.4% vaginal cream. Based on comparative analyses with placebo, the adverse
experiences considered most likely related to terconazole 0.4% vaginal cream
were headache (26% vs. 17% with placebo) and body pain (2.1% vs. 0% with placebo).
Vulvovaginal burning (5.2%), itching (2.3%) or irritation (3.1%) occurred
less frequently with terconazole 0.4% vaginal cream than with the vehicle
placebo. Fever (1.7% vs. 0.5% with placebo) and chills (0.4% vs. 0.0% with
placebo) have also been reported. The therapy-related dropout rate was 1.9%.
The adverse drug experience on terconazole most frequently causing discontinuation
was vulvovaginal itching (0.6%), which was lower than the incidence for placebo
(0.9%).<br/>TERAZOL 3 (terconazole)
Vaginal Cream 0.8%: During controlled clinical studies conducted in the United
States, patients with vulvovaginal candidiasis were treated with terconazole
0.8% vaginal cream for three days. Based on comparative analyses with placebo
and a standard agent, the adverse experiences considered most likely related
to terconazole 0.8% vaginal cream wereheadache (21% vs. 16% with placebo)
and dysmenorrhea (6% vs. 2% with placebo). Genital complaints in general,
and burning and itching in particular, occurred less frequently in the terconazole
0.8% vaginal cream 3 day regimen (5% vs. 6%���9% with placebo). Other
adverse experiences reported with terconazole 0.8% vaginal cream were abdominal
pain (3.4% vs. 1% with placebo) and fever (1% vs. 0.3% with placebo). The
therapy-related dropout rate was 2.0% for the terconazole 0.8% vaginal cream.
The adverse drug experience most frequently causing discontinuation of therapy
was vulvovaginal itching, 0.7% with the terconazole 0.8% vaginal cream group
and 0.3% with the placebo group.<br/>TERAZOL 3 (terconazole)
Vaginal Suppositories 80 mg: During controlled clinical studies conducted in the United
States, 284 patients with vulvovaginal candidiasis were treated with terconazole
80 mg vaginal suppositories. Based on comparative analyses with placebo (295
patients), the adverse experiences considered adverse reactions most likely
related to terconazole 80 mg vaginal suppositories were headache (30.3% vs.
20.7% with placebo) and pain of the female genitalia (4.2% vs. 0.7% with placebo).
Adverse reactions that were reported but were not statistically significantly
different from placebo were burning (15.2% vs. 11.2% with placebo) and body
pain (3.9% vs. 1.7% with placebo). Fever (2.8% vs. 1.4% with placebo) and
chills (1.8% vs. 0.7% with placebo) have also been reported. The therapy-related
dropout rate was 3.5% and the placebo therapy-related dropout rate was 2.7%.
The adverse drug experience on terconazole most frequently causing discontinuation
was burning (2.5% vs. 1.4% with placebo) and pruritus (1.8% vs. 1.4% withplacebo).
|
| dailymed-instance:warning |
None.
|
| dailymed-instance:indicatio... |
TERAZOL 7 (terconazole) Vaginal Cream 0.4%,
TERAZOL 3 (terconazole) Vaginal Cream 0.8% and TERAZOL 3
(terconazole) Vaginal Suppositories 80 mg are indicated for the local treatment
of vulvovaginal candidiasis (moniliasis). As these products are effective
only for vulvovaginitis caused by the genus Candida, the diagnosis should
be confirmed by KOH smears and/or cultures.
|
| dailymed-instance:represent... | |
| dailymed-instance:routeOfAd... | |
| dailymed-instance:name |
Terazol 3
|