For the use of a Registered Medical Practitioner or a Hospital or a Institution only.
GYNOSTAT (Clotrimazole) is a synthetic imidazole derivative, is an antifungal agent. Chemically, clotrimazole is 1-(o-Chloro-α, α–diphenylbenzyl)imidazole.The molecular formula is C22H17ClN2 and molecular weight is 344.84.
STRUCTURAL FORMULA :
Its structural formula is :
GYNOSTAT is off white to cream coloured elongated uncoated tablet, having one end flat & depressed and the other end circular.
Each uncoated tablet contains :
Clotrimazole USP 100 mg
(Lactose Monohydrate USP-NF, Corn Starch USP–NF, Methyl Paraben USP-NF, Propyl Paraben USP-NF, Povidone K-30 USP, Purified Water USP, Talc USP, Magnesium Stearate USP-NF, Sodium Starch Glycolate USP-NF, Colloidal Silicon Dioxide USP-NF, Adipic Acid USP-NF, Sodium Bicarbonate USP)
Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol synthesis leads to structural and functional impairment of the cytoplasmic membrane. It binds to phospholipids in the fungal cell membrane altering cell wall permeability resulting in loss of essential intracellular elements. The mode of action of clotrimazole is fungistatic or fungicidal depending on the concentration of clotrimazole at the site of infection. In-vitro activity is limited to proliferating fungal elements; fungal spores are only slightly sensitive.
Primarily resistant variants of sensitive fungal species are very rare; the development of secondary resistance by sensitive fungi has so far only been observed in very isolated cases under therapeutic conditions.
Pharmacokinetic investigations after vaginal application have shown that only a small amount of clotrimazole (3 – 10 % of the dose) is absorbed. Following intra-vaginal administration of 100 mg clotrimazole vaginal insert an average peak serum level, corresponding to only 0.03 µg equivalents/ml of clotrimazole, was reached 1-2 days after application.
For the treatment of vaginal yeast (candidiasis) infections.
Not for oral administration. FOR VAGINAL USE ONLY.
INSTRUCTIONS FOR USE OF INSERT :
Special directions for using applicator :
1. Prior to application, cut out one tablet from the aluminium foil.
2. Moisten the tablet by immersing it in water for 2 to 3 seconds before insertion.
3. Pull out plunger A until it stops. Place one vaginal tablet into the applicator B.
4. Insert applicator containing the tablet carefully as deep as possible into the vagina (This is done best by lying on the back).
5. Push plunger A until it stops, thereby depositing the tablet into the vagina. Withdraw the applicator.
6. After use, remove plunger A completely by pulling it out of the applicator B.
Thereafter wash both A & B in warm (not boiling) soapy water and dry completely. The applicator is ready for next use.
Antifungal (vaginal) :
Nonpregnant patients : 100 mg once a day, preferably at bedtime, for six or seven consecutive days.
Pregnant patients : Intravaginal, 100 mg once a day, preferably at bedtime, for seven consecutive days. In severe vulvovaginal candidiasis, longer treatment with the 100 mg or 200 mg vaginal tablets or vaginal cream is recommended.
The preparation is contraindicated during first trimester of pregnancy and for hypersensitivity to the drug.
i) Not for oral use.
ii) Use only if you have already had a vaginal yeast infection diagnosed by a medical practitioner and you have the same symptoms now, otherwise consult your doctor.These symptoms include itching and burning of the vagina and sometimes a white discharge.
iii) If there is no improvement in 3 days or if symptoms have not disappeared within 7 days, then consult a medical practitioner as not all vaginal infections are caused by yeasts.
iv) Consult a medical practitioner if you have abdominal pain, fever or a foul-smelling vaginal discharge before or during use of this medication.
v) If symptoms recur within 2 months, consult a medical practitioner.
vi) If you are pregnant or think you may be pregnant or are nursing, do not use this medication except on the advice of a medical practitioner.
vii) Do not use in girls under 12 years of age, except on the advice of a medical practitioner.
viii) If skin rash or new irritation occurs, discontinue use.
ix) GYNOSTAT may reduce the effectiveness and safety of latex products such as condoms and diaphragms. The effect is temporary and occurs only during treatment.
Pregnancy : Category B
Clotrimazole is very poorly absorbed following dermal application or intra-vaginal administration to humans.
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, this drug should be used only if clearly indicated during the first trimester of pregnancy.
Nursing mothers :
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when GYNOSTAT is used by a nursing woman.
INTERACTIONS AND INCOMPATIBILITIES :
Synergism or antagonism between clotrimazole and nystatin or amphotericin B or flucytosine against strains of C. albicans has not been reported. Antagonism with polyene antibiotics.
SIDE EFFECTS :
The following adverse reactions have been reported in connection with the use of Clotrimazole : erythema, stinging, blistering, peeling, oedema, pruritus, urticaria, burning and general irritation of the skin. “Inform your doctor in case of any adverse reactions related to drug use”.
Gastrointestinal disturbances and central nervous system depression may follow accidental oral ingestion.
TREATMENT OF OVERDOSAGE :
Treatment is symptomatic and supportive.
Store at room temperature below 300C, protected from moisture and light. Do not store in the bathroom, near the kitchen sink, or in other damp places. Heat or moisture may cause medicine to break down.
SHELF LIFE :
36 months from the date of manufacture.
Pack of 6 vaginal inserts packed in aluminium foil with an applicator.
Disclaimer : For the use of a Registered Medical Practitioner or a Hospital or a Institution only. Also it is not intended to be used by healthcare professionals or patients for the purpose of prescribing or administering these products. Questions regarding the complete and current content of product labeling / specification / presentation should be directed to SGPharma.