(Clotrimazole 2%W/W+ Clindamycin 1%W/W Cream; Clotrimazole 200mg + Clindamycin 100mg Tablet)
COMPOSITION
Each Tablet Contains
Clotrimazole 200mg
Clindamycin 100mg
1g of Cream Contains
Clotrimazole 20mg
Clindamycin 10mg
CLINICAL PHARMACOLOGY
Pharmacodynamic Properties
Clotrimazole is an imidazole antifungal with antimicrobial activity similar to that of Ketoconazole.
Clotrimazole has a broad spectrum of activity (yeasts, dermatophytes and a number of other fungi). It is effective on yeast notably Candida albicans and Torulopsis glabrata as well as on Trichomonas vaginalis and some gram positive and gram negative bacteria (streptococci, staphylococci,Gardneralla vaginalis, Bacteroides).
Clindamycin is a lincosamide antibiotic with a primarily bacteriostatic action against Gram positive aerobes and a wide range of anaerobic bacteria.
Clindamycin is effective in the treatment of infection caused by susceptible anaerobic bacteria or susceptible strains of gram positive aerobic bacteria. It has been shown to have in-vitro activity against the following organisms which are associated with bacteria vaginosis Cardneralla vaginalis:-
Mobiluncus spp., Bacteroides spp.,Mycoplasma hominis.,Peptostreptococcus spp.
Pharmacokinetics properties
CREAM
The concentration of unchanged active substance in the plasma of volunteers following the application of 2% Clotrimazole vaginal cream was below the limit of detection (10mg/ml). Since only very small amounts of active substance are absorbed by the vaginal skin and it is metabolized very quickly (t1/2 = 1-2 hours), concentrations in the blood plasma are always below the limit of detection.
Following once a day dosing of 100mg of vaginally administered Clindamycin phosphate at a concentration equivalent to 20mg of clindamycin levels average 20 nanograms/ml (range 3 – 93 nanogram/ml in normal volunteers. Approximately 3% per gram of cream peak serum Clindamycin (range 0.1 – 7%) of the administered dose is absorbed systematically.
In women with bacterial vaginosis, the amount of Clindamycin absorbed following vaginal administration of 100mg of the cream (20mg/g) is 4% (range 0.8 – 8%) which is approximately the same as in normal women.
TABLET
When the tablet is inserted, Clotrimazole penetrates the epidermis but there is little if any systemic absorption. Absorption of 3 to 10% of a dose has been reported following vaginal administration. Clotrimazole is metabolized in the liver to inactive compounds and excreted in the faeces and urine. Small amounts of clindamycin may be absorbed after the application of the tablets: bioavailability from topical preparation of the hydrochloride and phosphate (the former in an extemporaneous, formulation) has been reported to be about 7.5% and 2% respectively. About 5% of an intravaginal dose may be absorbed systemically.
INDICATIONS
Mycoten®-Plus is indicated for treatment of infective leucorrhea (thick,whitish vaginal discharge) mixed infection and non-specific vaginitis, vaginal candidiasis, bacterial vaginosis and trichomoniasis.
CONTRAINDICATIONS
History of hypersensitivity to Clindamycin or Clotrimazole or any of the components of the preparation.
INTERACTIONS
Mycoten®-Plus vaginal cream contains oil base components. Some of these have been known to weaken rubber of condoms and diaphragms and make them less effective as a barrier method of Contraception or as a protection. Patients should be advised from sexually transmitted disease including AIDS patients should be advised to use alternative precautions of contraceptives at least five days after using the product. Cross resistance has been demonstrated between Clindamycin and Lincomycin, Erythromycin and Clindamycin. Antagonism has been demonstrated between clindamycin and erythromycin in-vitro. However, very little Clindamycin is absorbed into the blood stream when given vaginally so the likelihood of drug interactions is less. No information is available on concomitant use with other intravaginal products which is not recommended.
WARNINGS/PRECAUTIONS
If local irritation or allergic reaction should occur, the treatment should be discontinued.
Mycoten®-Plus Vaginal Cream/Tablet should not be used during the first trimester of pregnancy unless it is clearly needed because it has not been properly evaluated during the first trimester.
PREGNANCY AND LACTATION
Pregnancy
Clotrimazole has been used in pregnant patients for over a decade without attributable adverse effects.
It is therefore recommended that Clotrimazole should be used in pregnancy only when considered necessary by the clinician.
The frequency of congenital abnormalities was not increased when pregnant women used Clindamycin during the second and third trimesters and Clindamycin vaginal cream is approved for use during the second and third trimesters of pregnancy. However Clindamycin should not be used during the first trimester of pregnancy unless it is clearly needed because it has not been properly evaluated during the first trimester.
During pregnancy, extra care should be taken when using the applicator to prevent the possibility of mechanical trauma.
Lactation
It is not known if Clindamycin is excreted in breast milk following the use of vaginally administered Clindamycin. However, orally and parenterally administered Clindamycin has been reported to appear in breast milk. Therefore, a full assessment of benefit-risk should be made when consideration is given to using vaginal Clindamycin phosphate in a nursing mother.
KEEP OUT OF THE REACH OF CHILDREN!
SIDE EFFECTS/ADVERSE REACTIONS
Rarely, patients may experience local mild burning or irritation immediately after applying the cream. Hypersensitivity reactions may occur. There may be an increased need to urinate, low abdominal cramps may occur.
SYMPTOMS OF OVERDOSE AND ANTIDOTE
Intravaginal overdose is not possible. In the event of accidental oral ingestion, routine measures such as gastric lavage should be performed as soon as possible after ingestion.
DOSAGE AND ADMINISTRATION
Mycoten®-Plus Vaginal Cream
The recommended dose is one full applicator of the intravaginally, preferably at bed time for 3 or 7 days.
Mycoten®-Plus Vaginal Tablets should be inserted deep in the vaginal with patient lying on her back with the knee bent up once daily using the applicator supplied and preferably at bed time for 3 or 7days.
PRESENTATION
Mycoten®-plus Vaginal Cream is presented as 2% Clotrimazole plus 1% Clindamycin in 35g tube.
Mycoten®-plus Vaginal Tablets is presented as 2% Clotrimazole plus 1% Clindamycin in a blister of 1 x 7’s per pack.
STORAGE CONDITIONS
Store below 30OC. Protect from light and moisture.
