Canesten, Vaginal (Clotrimazole)

CANESTEN® Vaginal

Bayer Consumer

Clotrimazole

Antifungal

Action And Clinical Pharmacology: Clotrimazole acts primarily by damaging the permeability barrier in the cell membrane of fungi. Clotrimazole brings about inhibition of ergosterol biosynthesis, an essential constituent of fungal cell membranes. If ergosterol synthesis is completely or partially inhibited, the cell is no longer able to construct an intact cell membrane. This leads to death of the fungus.

Exposure of C. albicans to clotrimazole causes leakage of intracellular phosphorus compounds into the ambient medium with a concomitant breakdown of cellular nucleic acids and potassium efflux. The onset of these events is rapid and extensive after exposure of the organism to the drug, and causes a time-dependent and concentration-dependent inhibition of fungal growth.

Pharmacokinetics: Metabolism studies performed after oral or i.v. administration have shown that in most species studied, levels of clotrimazole in tissue and serum are low. The majority of the drug is excreted as metabolites in the feces, with small amounts excreted in the urine. Human studies indicate slow excretion following oral administration of 4-labeled clotrimazole (greater than 6 days). After intraperitoneal and s.c. administration, very low levels have been observed in the urine. The absorption and organ distribution of the drug is very poor when administered parenterally.

The pharmacokinetics of topically applied clotrimazole in human subjects have been evaluated by Duhm et al. who reported on the penetration of radioactive clotrimazole 1% cream and 1% solution into intact and acutely inflamed skin. Six hours after application of the drug, the concentration of clotrimazole found in skin layers varied from 100 µg/cmin the stratum corneum to 0.5 to 1 g/cmin the stratum reticulare.

Intravaginal application of 4-labeled clotrimazole inserts containing 100 mg of active substance in human subjects has shown that the amount absorbed is less than 1/200 of that absorbed after the oral administration of 1.5 g of clotrimazole. The maximum serum concentration values were between 0.016 and 0.05 g/mL from 1 to 3 days after intravaginal application. Intravaginal application in human subjects of 5 mL 4-labeled clotrimazole vaginal cream containing 50 mg of active substance has shown that the systemic absorption of clotrimazole from the vaginal cream is quantitatively proportional to that from the vaginal inserts.

In animal experiments, clotrimazole exerts an in vitro and in vivo, dose-dependent, stimulating effect on certain microsomal enzyme systems which is approximately equal to that of phenobarbital in its inductive potential. However, this stimulating effect subsides rapidly when treatment is discontinued. The enzyme-inductive effect of clotrimazole has been found to be intact in adrenalectomized animals.

In 11 double-blind and 1 large multicentre open study, treatment of 814 patients with the 100 mg insert for 6 to 7 days resulted in an average mycological cure rate of 79% (range of 67 to 91%). In studies comparing the 3- and 7-day regimen, 168 patients were treated with one clotrimazole vaginal insert (100 mg) daily for 7 days. Overall and mycological cure rates were 67 and 70%, respectively.

In 8 double-blind studies and one single-blind study involving 432 patients using the 1% cream for 7 days, the average mycological cure rate was 72% with a range of 55 to 90%.

Oral contraceptives did not significantly alter mycological cure rates and overall success. In a limited number of pregnant women, both the 1% cream and the 100 mg insert appeared to be effective, although the cure rates seemed to be somewhat lower.

In clinical trials involving 200 mg clotrimazole vaginal inserts, 498/611 patients (82%) had a negative culture for Candida sp. 4 weeks following treatment.

In clinical trials with clotrimazole 2% vaginal cream, 266/303 patients (88%) had a negative culture for Candida sp. 4 weeks following treatment.

In clinical trials with clotrimazole 500 mg vaginal inserts, 158/231 patients (68%) had a negative culture for Candida sp. 4 weeks following treatment.

In clinical trials with clotrimazole 10% vaginal cream, 592/726 patients (82%) had a negative culture for Candida sp. 4 weeks following treatment.

Indications And Clinical Uses: Canesten 1% Vaginal Cream: For the 6-day treatment of vaginal candidiasis.

Canesten 2% Vaginal Cream: For the 3-day treatment of vaginal candidiasis.

Canesten 10% Vaginal Cream: For the 1-day treatment of vaginal candidiasis.

Canesten Combi-Pak 3-Day Therapy: For the 3-day treatment of vaginal candidiasis.

Canesten Combi-Pak 1-Day Therapy: For the 1-day treatment of vaginal candidiasis.

Canesten 1 Day Cream Combi-Pak: For the 1-day treatment of vaginal candidiasis.

Contra-Indications: Hypersensitivity to clotrimazole.

Precautions: Clotrimazole vaginal inserts are not for oral use.

Not for ophthalmic use.

As with all topical agents, skin sensitization may result. Use of clotrimazole topical preparations should be discontinued should such reactions occur, and appropriate therapy instituted.

Pregnancy: Although intravaginal application of clotrimazole has shown negligible absorption from both normal and inflamed human vaginal mucosa, clotrimazole vaginal preparations should not be used in the first trimester of pregnancy unless the physician considers it essential to the welfare of the patient.

The use of applicators may be undesirable in some pregnant patients and digital insertion of the inserts may be considered.

Adverse Reactions: Experimental, therapeutic, and large scale clinical studies have shown clotrimazole to be well tolerated after topical application.

Erythema, stinging, blistering, peeling, edema, pruritus, urticaria and general irritation of the skin have been reported infrequently.

Two of 419 (0.5%) patients treated with the 1% vaginal cream experienced adverse reactions judged to be possibly drug related. These were intercurrent cystitis and vaginal burning. Neither necessitated discontinuation of treatment. None were of serious consequence and no complications occurred.

The 100 mg inserts were also well tolerated. Only a few cases consisting primarily of burning sensation and mild skin reactions were reported. In studies comparing the 3- and 7-day regimen, 4 of 212 patients (1.9%) in the 7-day group reported adverse reactions possibly related to treatment. These included: irritation, burning, cramping, itching, redness, abdominal bloating, bleeding and rash. In an additional 9 double-blind comparative studies, 5 out of 219 patients on the 7-day regimen with the 100 mg insert experienced similar types of adverse reactions, none of which necessitated discontinuation of treatment. In a large open multicentre and 2 double-blind studies employing the 100 mg insert in a 6-day regimen, 11 out of 595 (1.8%) patients complained of possible drug-related side effects. Mild burning occurred in 4 patients while other reactions such as skin rash, lower abdominal cramps, slight urinary frequency and burning or irritation in the sexual partner occurred rarely. In no case was it necessary to discontinue treatment.

In clinical trials involving 200 mg clotrimazole vaginal inserts, 24/832 patients (2.9%) experienced an adverse reaction. 2/217 patients (0.9%) who received 2% clotrimazole vaginal cream in clinical trials experienced an adverse reaction. In clinical trials involving 500 mg clotrimazole vaginal inserts, 12/515 patients (2.3%) experienced an adverse reaction. 26/796 (3.3%) of patients in clinical trials involving 10% clotrimazole vaginal cream experienced an adverse reaction. Most adverse reactions involved local itching and burning. Only rarely was it necessary to discontinue treatment.

Dosage And Administration: Canesten 1% Vaginal Cream: The recommended daily dose is 1 full applicator intravaginally for 6 consecutive days, preferably at bedtime.

Canesten 2% Vaginal Cream: The recommended daily dose is 1 full applicator intravaginally for 3 consecutive days preferably at bedtime.

Canesten 10% Vaginal Cream: The recommended dose is 1 full applicator intravaginally, (as a single dose therapy), preferably at bedtime.

Canesten Combi-Pak 3-Day Therapy: The recommended daily dose is 1 insert intravaginally for 3 consecutive days, preferably at bedtime. The cream should be spread onto the irritated area once or twice a day as needed, for up to 7 consecutive days.

Canesten Combi-Pak 1-Day Therapy: The recommended dose is 1 insert intravaginally for 1 day, preferably at bedtime. The cream should be spread onto the irritated area once or twice a day as needed, for up to 7 consecutive days.

Canesten 1-Day Cream Combi-Pak: The recommended dose is 1 full applicator intravaginally, (as a single dose therapy), preferably at bedtime. The topical cream should be spread onto the irritated area once or twice a day as needed, for up to 7 consecutive days.

Vaginal candidiasis may be accompanied by irritation in the vaginal area. Therefore, concomitant local treatment with vaginal cream (or topical cream) applied to the irritated vaginal area and as far as the anal region twice a day is advisable. Topical cream (or vaginal cream) applied on the glans penis may prevent re-infection by the partner.

Note: The cream or insert should be inserted deep intravaginally by means of the applicator (see Precautions). The plunger should then be depressed slowly.

General hygienic measures such as twice daily tub baths and avoidance of tight underclothing are important in vaginal infections.

Availability And Storage: Canesten 1% Vaginal Cream: Each g contains: clotrimazole 10 mg in a vanishing cream base. Nonmedicinal ingredients: benzyl alcohol, cetostearyl alcohol, cetyl esters wax, 2-octyl dodecanol, polysorbate 60, purified water and sorbitan monostearate. Tubes of 50 g in a carton with 6 disposable plastic applicators and patient instructions. 50 g of vaginal cream is sufficient for 6 intravaginal applications with additional cream for extravaginal use if required.

Canesten 2% Vaginal Cream: Each g contains: clotrimazole 20 mg in a vanishing cream base. Nonmedicinal ingredients: benzyl alcohol, cetostearyl alcohol, cetyl esters wax, 2-octyl dodecanol, polysorbate 60, purified water and sorbitan monostearate. Tubes of 25 g in a carton with 3 disposable plastic applicators and patient instructions. 25 g of vaginal cream is sufficient for 3 intravaginal applications with additional cream for extravaginal use if required.

Canesten 10% Vaginal Cream: Each g contains: clotrimazole 100 mg in a vanishing cream base. Nonmedicinal ingredients: benzyl alcohol, cetostearyl alcohol, cetyl palmitate, isopropyl myristate, polysorbate, purified water and sorbitan monostearate. Boxes containing one 5 g pre-filled applicator with a plunger in a blister pack and patient instructions.

Canesten Combi-Pak 3-Day Therapy: Each insert contains: clotrimazole 200 mg and each g of topical cream contains: clotrimazole 10 mg. Nonmedicinal ingredients: adipic acid, benzyl alcohol, cetostearyl alcohol, cetyl esters wax, colloidal silicon dioxide, cornstarch, lactose, magnesium stearate, 2-octyl dodecanol, polysorbate 60, polysorbate 80, sodium bicarbonate, sorbitan monostearate and stearic acid. Boxes of 1 strip of 3 Canesten 200 mg Vaginal Inserts with one plastic applicator and one 10 g tube of Canesten 1% Topical Cream.

Canesten Combi-Pak 1-Day Therapy: Each insert contains: clotrimazole 500 mg and each g of topical cream contains: clotrimazole 10 mg. Nonmedicinal ingredients: benzyl alcohol, calcium lactate, cetostearyl alcohol, cetyl esters wax, cornstarch, hydroxypropyl methylcellulose, lactic acid, lactose, magnesium stearate, microcrystalline cellulose, 2-octyl dodecanol, polysorbate 60, polyvinyl pyrrolidone, silicon dioxide and sorbitan monostearate. Boxes of 1 strip of 1 Canesten 500 mg Vaginal Insert with one plastic applicator and one 10 g tube of Canesten 1% Topical Cream.

Canesten 1-Day Cream Combi-Pak: Each g of vaginal cream contains: clotrimazole 100 mg and each g of topical cream contains: clotrimazole 10 mg. Nonmedicinal ingredients: benzyl alcohol, cetostearyl alcohol, cetyl esters wax, cetyl palmitate, isopropyl myristate, 2-octyl dodecanol, polysorbate 60, purified water and sorbitan monostearate. Boxes containing one 5 g pre-filled applicator with plunger of Canesten 10% Vaginal Cream and one 10 g tube of Canesten 1% Topical Cream.

Store below 30°C. Avoid freezing. (Shown in Product Recognition Section)

CANESTEN® Vaginal Bayer Consumer Clotrimazole Antifungal

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