CLOTRIMAZOLE
DESCRIPTION:
ACTIVE INGREDIENTS:
Inserts: Clotrimazole 200 mg per insert. Cream: Clotrimazole 1%.
INACTIVE INGREDIENTS:
Inserts: Corn starch, crospovidone, lactose, magnesium stearate, povidone.
Cream: Benzyl alcohol, cetearyl alcohol, cetyl esters wax, octyldodecanol,
polysorbate 60, purified water, sorbitan monostearate.
Gyne-Lotrimin3 antifungal vaginal inserts and external vulvar cream can kill the
yeast that may cause vaginal infection. They do not stain clothes.
INDICATIONS AND USAGE:
For the treatment of vaginal yeast (CANDIDA) infection and the relief of
external vulvar itching and irritation associated with a yeast infection. Starts
to relieve itching and other symptoms within 1-2 days.
IF THIS IS THE FIRST TIME YOU HAVE HAD VAGINAL OR VULVAR ITCH AND DISCOMFORT,
CONSULT YOUR DOCTOR. IF YOU HAVE HAD A DOCTOR DIAGNOSE A VAGINAL YEAST INFECTION
BEFORE AND HAVE THE SAME SYMPTOMS NOW, USE THESE INSERTS AND CREAM AS DIRECTED
FOR 3 CONSECUTIVE DAYS.
WARNINGS:
DO NOT USE IF YOU HAVE ABDOMINAL PAIN, FEVER, OR FOUL-SMELLING DISCHARGE.
CONTACT YOUR DOCTOR IMMEDIATELY. IF YOUR SYMPTOMS DO NOT IMPROVE IN 3 DAYS, YOU
MAY HAVE A CONDITION OTHER THAN A YEAST INFECTION. CONSULT YOUR DOCTOR. IF YOUR
SYMPTOMS RETURN WITHIN 2 MONTHS OR IF YOU HAVE INFECTIONS THAT DO NOT CLEAR UP
EASILY WITH PROPER TREATMENT, CONSULT YOUR DOCTOR. YOU COULD BE PREGNANT OR
THERE COULD BE A SERIOUS UNDERLYING MEDICAL CAUSE FOR YOUR INFECTIONS, INCLUDING
DIABETES, OR A DAMAGED IMMUNE SYSTEM (INCLUDING DAMAGE FROM INFECTION WITH HIV -
THE VIRUS THAT CAUSES AIDS). (PLEASE READ ENCLOSED EDUCATIONAL PAMPHLET). DO NOT
USE DURING PREGNANCY EXCEPT UNDER THE ADVICE AND SUPERVISION OF A DOCTOR. DO NOT
USE TAMPONS WHILE USING THIS MEDICATION. KEEP THESE AND ALL DRUGS OUT OF THE
REACH OF CHILDREN. IN CASE OF ACCIDENTAL INGESTION, SEEK PROFESSIONAL ASSISTANCE
OR CONTACT A POISON CONTROL CENTER IMMEDIATELY. NOT FOR USE IN CHILDREN LESS
THAN 12 YEARS OF AGE.
DOSAGE AND ADMINISTRATION:
Before using, read the enclosed pamphlet.
DIRECTIONS: (Inserts): Unwrap one insert, place it in the applicator, and use
the applicator to place the insert into the vagina, preferably at bedtime.
Repeat this procedure daily for 3 consecutive days to treat vaginal yeast
(CANDIDA) infection.
(Cream): Squeeze a small amount of cream onto your finger and gently spread the
cream into the irritated area of the vulva. Use once or twice a day for up to 7
days as needed to relieve external vulvar itching. THE CREAM SHOULD NOT BE USED
FOR VULVAR ITCHING DUE TO CAUSES OTHER THAN A YEAST INFECTION.
DESCRIPTION:
Each CANDID 500 mg Vaginal Tablet contains 500 mg clotrimazole (the active
ingredient) dispersed in lactose, microcrystalline cellulose, lactic acid, corn
starch, crospovidone, calcium lactate, magnesium stearate, silicon dioxide and
hydroxypropyl methylcellulose. Chemically, clotrimazole is (1-(o-Chloro-alpha,
alpha- diphenylbenzyl) imidazole), a synthetic antifungal agent having the
chemical formula C22H17ClN2 and a molecular weight of 344.84.
Clotrimazole is an odorless, white crystalline substance, practically insoluble
in water, sparingly soluble in ether, soluble in carbon tetrachloride, and very
soluble in ethanol and chloroform.
ACTIONS/CLINICAL PHARMACOLOGY:
Serum levels and levels in vaginal secretions of clotrimazole were measured in
six healthy volunteers who had one 500 mg vaginal tablet inserted. Although
serum levels of clotrimazole were higher than those in other volunteers given
100 mg and 200 mg vaginal tablets these levels did not exceed 10 nanograms/mL It
has been estimated that three to ten percent of a vaginal dose of clotrimazole
may be absorbed, but the drug rapidly and efficiently degrades to
microbiologically inactive metabolites. The clotrimazole concentrations
remaining in vaginal secretions were still in the mg/mL range for 48 hours and
in two of the six subjects at 72 hours.
The findings of high clotrimazole concentrations in vaginal secretions for up to
72 hours and low concentrations in the serum suggest that nearly all the
clotrimazole given in the 500 mg vaginal tablet remains in the vagina for 48
hours, and in some cases 72 hours, in fungicidal concentrations.
Clotrimazole is a broad-spectrum antifungal agent. It has been postulated that
the compound affects the permeability characteristics of the membrane allowing
the leakage of essential intracellular components with a consequent inhibition
of the synthesis of such macromolecules as protein, lipid, DNA, and
polysaccharides.
At concentrations as low as 2-5 mcgm/mL, clotrimazole exhibits fungicidal
activity In Vitro against Candida Albicans and other species of the genus
Candida.
No single-step or multiple-step resistance to clotrimazole has developed during
successive passages of Candida Albicans.
INDICATIONS AND USAGE:
CANDID-G 500 mg Vaginal Tablets are indicated for the local treatment of
vulvovaginal candidiasis when one day therapy is felt warranted. In the case of
severe vulvovaginitis due to candidiasis, longer antimycotic therapy is
recommended. The diagnosis should be confirmed by KOH smears and/or cultures.
Other pathogens commonly associated with vulvovaginitis, Trichomonas and
Gardnerella (Haemophilus) Vaginalis, should be ruled out by appropriate
laboratory methods.
CONTRAINDICATIONS:
CANDID-G 500 mg Vaginal Tablets are contraindicated in women who have shown
hypersensitivity to any components of the preparation.
WARNINGS:
None.
PRECAUTIONS:
If there is a lack of response to CANDID-G 500 mg Vaginal Tablets, appropriate
microbiological studies should be performed to confirm the diagnosis and rule
out other pathogens before instituting another course of antimycotic therapy.
CARCINOGENESIS
No long term studies in animals have been performed to evaluate the carcinogenic
potential of CANDID-G 500 mg Vaginal Tablets intravaginally. A long term study
in rats (Wistar strains) where clotrimazole was administered orally provided no
indication of carcinogenicity.
USAGE IN PREGNANCY
PREGNANCY CATEGORY B: The disposition of 14C- clotrimazole has been studied in
humans and animals. Clotrimazole is poorly absorbed following intravaginal
administration to humans, whereas it is rather well absorbed after oral
administration.
In clinical trials, use of vaginally applied clotrimazole in pregnant women in
their second and third trimesters has not been associated with ill effects.
There are, however, no adequate and well-controlled studies in pregnant women
during the first trimester of pregnancy.
Studies in pregnant rats given repeated intravaginal doses up to 100 mg/kg/day
have revealed no evidence of harm to the fetus due to clotrimazole.
Repeated high oral doses of clotrimazole in rats and mice ranging from 50 to 120
mg/kg resulted in embryotoxicity (possibly secondary to maternal toxicity),
impairment of mating, decreased litter size and number of viable young and
decreased pup survival to weaning. However, clotrimazole was not teratogenic in
mice, rabbits and rats at oral doses up to 200, 180 and 100 mg/kg, respectively.
Oral absorption in the rat amounts to approximately 90% of the administered
dose.
Because animal reproduction studies are not always predictive of human response,
this drug should be used only if clearly indicated during the first trimester of
pregnancy.
ADVERSE REACTIONS:
Of 297 patients in double-blind studies with the 500 mg vaginal tablet, 3 of 149
patients treated with active drug and 3 of 148 patients treated with placebo
reported complaints during therapy that were possibly drug related. In the
active drug group, vomiting occurred in one patient, vaginal soreness with
coitus in another, and complaints of vaginal irritation, itching, burning and
dyspareunia in the third patient. In the placebo group, clitoral irritation
occurred in one patient and dysuria, described as remotely related to drug, in
the other. A third patient in the placebo group developed bacterial vaginitis
which the investigator classed as possibly related to drug.
Eighteen (1.6%) of the 1116 patients treated with CANDID-G in other
formulations in double-blind studies reported complaints during therapy that
were possibly drug-related. Mild burning occurred in six patients while other
complaints such as skin rash, itching, vulval irritation, lower abdominal cramps
and bloating, slight cramping, slight urinary frequency, and burning or
irritation in the sexual partner, occurred rarely.
OVERDOSAGE:
No data available.
DOSAGE AND ADMINISTRATION:
The recommended dose is one tablet inserted intravaginally one time only,
preferably at bedtime. In the event of treatment failure, that is, persistence
of signs and symptoms of vaginitis after five days, other pathogens commonly
responsible for vaginitis should be ruled out before instituting another course
of antimycotic therapy.
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