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Clotrimazole
1-(o-chloro- α, α - diphenylbenzyl) imidazole
C22H17ClN2
Molecular Weight 344.84
Clotrimazole is a colourless, crystalline, weakly alkaline substance, melting point 141°- 145°C, soluble in acetone, chloroform and ethanol and practically insoluble in water. It forms stable salts with both organic and inorganic acids. It is not photosensitive but is slightly hygroscopic, and may be hydrolysed in acid media.
Canesten Clotrimazole Thrush Treatment Once Cream contains 100 mg/g (10% w/w) of clotrimazole in a vanishing cream base. The cream also contains sorbitan monostearate, polysorbate 60, cetyl esters wax, cetostearyl alcohol, isopropyl myristate, benzyl alcohol (1% w/w) and purified water.
Canesten Clotrimazole Thrush Treatment 3 Day Cream contains 20 mg/g (2% w/w) of clotrimazole in a vanishing cream base. The cream also contains sorbitan monostearate, polysorbate 60, cetyl esters wax, cetostearyl alcohol, 2-octyldodecanol, benzyl alcohol (1% w/w) and purified water.
Canesten Clotrimazole Thrush Treatment 6 Day Cream contains 10 mg/g (1% w/w) of clotrimazole in a vanishing cream base. The cream also contains sorbitan monostearate, polysorbate 60, cetyl esters wax, cetostearyl alcohol, 2-octyldodecanol, benzyl alcohol (1% w/w) and purified water.
Canesten Clotrimazole Thrush Treatment Once Pessary contains 500 mg of clotrimazole in each pessary. The pessaries also contain lactose, microcrystalline cellulose, lactic acid, maize starch, crospovidone, calcium lactate; magnesium stearate, silicon dioxide, hypromellose.
Canesten Clotrimazole Thrush Treatment 6 Day Pessary contains 100 mg of clotrimazole in each pessary. The pessaries also contain lactose, maize starch, magnesium stearate, silica-colloidal anhydrous, calcium lactate pentahydrate, crospovidone, lactic acid, hypromellose, cellulose microcrystalline.
Canesten Clotrimazole Thrush Treatment Once Pessary + Cream contains 500 mg of clotrimazole in each pessary and 10 mg/g clotrimazole in the cream. The pessary also contains lactose, microcrystalline cellulose, lactic acid, maize starch, crospovidone, calcium lactate; magnesium stearate, silicon dioxide, hypromellose. The cream also contains sorbitan monostearate, polysorbate 60, cetyl esters wax, cetostearyl alcohol, 2-octyldodecanol, benzyl alcohol and purified water.
Canesten Topical Cream contains 10 mg/g (1%) of clotrimazole in a vanishing cream base. The cream also contains sorbitan monostearate, polysorbate 60, cetyl esters wax, cetostearyl alcohol, 2-octyldodecanol, benzyl alcohol (1% w/w) and purified water.
Canesten Topical Solution contains 10 mg/mL (1% w/v) of clotrimazole in a solution of propylene glycol, isopropyl alcohol and polyethylene glycol.
Studies using 14C-labelled clotrimazole have shown absorption of about 3% of the administered dose from normal or inflamed human vaginal mucosa (peak serum level of 0.03 µg/mL) 24 hours after insertion of a 100 mg tablet.
Studies in normal volunteers after vaginal insertion of one 500 mg pessary showed that plasma levels of clotrimazole up to 10 ng/mL were reached during the period of assay (up to 72 hours after insertion). Significant concentrations of clotrimazole were present in the vaginal secretion for up to 48 hours after insertion.
Canesten Clotrimazole cream containing 14C-labelled clotrimazole was administered intravaginally to five women (four without gynaecological disorder and one with Candida vaginitis). A maximum serum level of 0.01 µg/mL was found between 10 and 30 hours after administration.
Six hours after application of labelled topical Canesten Clotrimazole cream the concentrations of clotrimazole ranged from 100 µg/cm3 in the stratum corneum to 0.05 - 1.0 µg/cm3 in the stratum reticulare and 0.1 µg/cm3 in the subcutis.
No measurable radioactivity was found in the serum within 48 hours after application of 0.8 g of the cream.
Studies of urinary excretion have shown that less than 0.5% of dermally applied Canesten Clotrimazole cream appears in the urine over a five-day period of observation. Faecal excretion, the route by which most of the absorbed medicine is likely to be eliminated, has not been studied in man.
The primary mode of action of Canesten Clotrimazole cream appears to be on the cell membrane of the fungi, damaging the permeability barrier.
A single course of intravaginal Canesten Clotrimazole cream has produced mycological cure of vaginal candidiasis as follows:
One 100 mg pessary daily for six days 80%
Two 100 mg pessaries daily for three days 75%
One 500 mg pessary 84%
5 g of 1% cream daily for six days approx. 75%
When a first course proved unsuccessful, a second course produced success in 8 of 12 women treated.
Canesten Clotrimazole Thrush Treatment Once, 3 Day and 6 Day creams are indicated for the topical treatment of vulvovaginal candidiasis. Canesten Clotrimazole cream may also be used in conjunction with Canesten Clotrimazole vaginal pessaries in the management of Candida vulvovaginitis or infection of the peri-anal area while application of the cream to the glans penis of the partner may help prevent re-infection of the female.
Canesten Clotrimazole Thrush Treatment Once and 6 Day vaginal pessaries are indicated for the topical treatment of vaginal candidiasis.
Canesten Clotrimazole Thrush Treatment Once Pessary + Cream is indicated for the topical treatment of vulvovaginal candidiasis. The cream can also be used in the management of Candida vulvovaginitis or infection of the peri-anal area while application of the cream to the glans penis of the partner may help prevent re-infection of the female.
Canesten topical cream and topical solution are indicated for the topical treatment of the following dermal infections:
Known hypersensitivity to clotrimazole and/or to any of the excipients.
If evidence of local intolerance develops, consider withdrawal of the medicine and institution of appropriate therapy.
Canesten Clotrimazole vaginal pessaries are for intravaginal use only and are not to be taken orally.
Canesten creams and solution are not intended for ophthalmic use.
No carcinogenicity or mutagenicity has been observed in animal studies.
While controlled clinical studies in pregnant women do not exist, epidemiological investigations give no indications that harmful effects on the mother and child should be anticipated when Canesten Clotrimazole is used during pregnancy. However, as with all medicines in the first three months of pregnancy, Canesten Clotrimazole should only be used after first consulting a doctor.
Sanitation of the birth canal should be ensured particularly during the last 4 – 6 weeks of pregnancy.
During pregnancy, the treatment should be carried out with Canesten Clotrimazole vaginal pessaries since these can be inserted without using an applicator.
Because systemic absorption of clotrimazole following topical or vaginal application is marginal, there should be no risk for the infant during lactation.
Not reported with topical forms of Canesten Clotrimazole.
Not known.
Canesten Clotrimazole vaginal cream and vaginal pessaries may reduce the effectiveness and safety of latex products, such as condoms and diaphragms. This effect is temporary and occurs only during treatment.
Canesten Clotrimazole creams and solution are generally well tolerated after local application. The following have been reported infrequently: erythema, stinging, blistering, peeling, oedema, pruritus, urticaria and general irritation.
Eleven (1.6%) of 689 patients treated with Canesten Clotrimazole vaginal pessaries complained of possibly medicine-related effects. Mild burning occurred in four patients while other complaints such as skin rash and lower abdominal cramps were mentioned. Slight urinary frequency and burning or irritation in the sexual partner occurred rarely. In no case was it necessary to discontinue Canesten Clotrimazole vaginal pessaries.
Once daily, preferably in the evening for six successive days, one applicator should be filled with cream (approx. 5 g) and inserted as deeply as possible into the vagina with the patient lying on her back. The 35 g tube of cream for vaginal use provides for six such doses.
Once daily, preferably in the evening for three successive days, one applicator should be filled with cream (approx. 5 g) and inserted as deeply as possible into the vagina with the patient lying on her back. The 20 g tube of cream for vaginal use provides for three such doses.
Canesten Clotrimazole cream may also be used in conjunction with Canesten Clotrimazole vaginal pessaries in the management of Candida vulvovaginitis or infection of the peri-anal area while application of the cream to the glans penis of the partner may help prevent re-infection of the female.
The disposable applicator should be filled with Canesten cream, ensuring the entire contents of the tube are used (approx. 5 g). The cream is then inserted as gently and deeply as possible into the vagina with the patient lying on her back at bedtime as a single dose of treatment.
The pessaries should be inserted as deeply as possible into the vagina once daily, preferably in the evening. This is best achieved using the plastic applicator provided and following the directions on the patient instruction sheet. In pregnancy digital insertion may be preferable to use of the applicator.
A course of treatment normally consists of either a single 500 mg pessary (Canesten Clotrimazole Thrush Treatment Once Pessary) or of six 100 mg pessaries (Canesten Clotrimazole Thrush Treatment 6 Day Pessary). The latter may be given either as two pessaries, inserted one after the other, daily for three days or as one pessary daily for six days. Clinical investigations have shown comparable efficacy from either dosage scheme. Where a first course proved unsuccessful, a second course produced success in 8 of 12 women treated.
It is suggested that treatment be timed so as to avoid the menstrual period and to be complete before the onset of menstruation.
Apply sparingly to the affected areas and rub in gently, two or three times daily.
The following recommendations are made:
Cutaneous candidiasis 2 weeks
Dermatomycoses 2-4 weeks
Onychia and Paronychia
due to C. albicans 4-8 weeks or more
Regular application of Canesten topical cream or solution is essential for successful treatment and, whether or not a cure is confirmed mycologically, treatment should be continued for two weeks after all clinical signs have disappeared.
Attention to hygiene is important in the management of fungal diseases of the feet. After washing, the feet - especially between the toes - should be dried thoroughly. Canesten Clotrimazole cream may be useful in mycotic paronychia or onychia following removal of the nail.
Not applicable.
One tube containing 5 g of cream, 100 mg clotrimazole per gram (10% w/w) packed with a single-use applicator and patient instruction sheet.
One tube containing 20 g of cream, 20 mg clotrimazole per gram (2% w/w) packed with three single-use disposable applicators and patient instruction sheet.
One tube containing 35 g of cream, 10 mg clotrimazole per gram (1% w/w) packed with six single-use disposable applicators and patient instruction sheet.
One pessary sealed in a blister with plastic applicator and patient instruction sheet. Each pessary contains 500 mg clotrimazole.
Packs of six pessaries each sealed in a blister with plastic applicator and patient instruction sheet. Each pessary contains 100 mg clotrimazole per tablet.
Packs of one tube containing 20 g or 50 g of cream, 10 mg clotrimazole per gram (1% w/w).
Packs of one plastic dropper-type bottle containing 20 mL of solution, 10 mg of clotrimazole per mL (1% w/v).
Canesten Clotrimazole Thrush Treatment
Canesten
Bayer New Zealand Limited
Consumer Care Division
C. P. O. Box 2825
Auckland
Ph: (09) 443 3093 or 0800 847 874
Fax: (09) 443 3094
19 March 2007