Canesten Clotrimazole Thrush Treatment. Product Information NAME OF THE MEDICINE DESCRIPTION. Vaginal Creams

Canesten® Clotrimazole Thrush Treatment Product Information NAME OF THE MEDICINE Active ingredient: Clotrimazole Chemical name: 1-(o-chloro-,-diphe...
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Canesten® Clotrimazole Thrush Treatment Product Information

NAME OF THE MEDICINE Active ingredient: Clotrimazole Chemical name: 1-(o-chloro-,-diphenylbenzyl) imidazole Structural formula:

CAS number: 23593-75-1 Molecular formula: C22H17ClN2 Molecular weight: 344.84

DESCRIPTION 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.

Vaginal Creams CANESTEN CLOTRIMAZOLE THRUSH TREATMENT 6 DAY CREAM This product contains 10 mg/g (1%) of clotrimazole in a vanishing cream base. It also contains sorbitan monostearate, polysorbate 60, cetyl palmitate, cetostearyl alcohol, octyldodecanol, benzyl alcohol and purified water.CANESTEN CLOTRIMAZOLE THRUSH TREATMENT 3 DAY CREAM This product contains 20 mg/g (2%) of clotrimazole in a vanishing cream base. It also contains sorbitan monostearate, polysorbate 60, cetyl palmitate, cetostearyl alcohol, octyldodecanol, benzyl alcohol and purified water. CANESTEN CLOTRIMAZOLE THRUSH TREATMENT ONCE CREAM This product contains 100 mg/g (10%) of clotrimazole in a vanishing cream base. It also contains sorbitan monostearate, polysorbate 60, cetylpalmitate, cetostearyl alcohol, isopropyl myristate, benzyl alcohol and purified water.

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Vaginal Tablets (Compressed Pessaries) CANESTEN CLOTRIMAZOLE THRUSH TREATMENT 6 DAY PESSARY This product contains 100 mg of clotrimazole in each compressed pessary. It also contains lactose, maize starch, magnesium stearate, silica-colloidal anhydrous, calcium lactate pentahydrate, crospovidone, lactic acid, hypromellose and cellulose-microcrystalline. CANESTEN CLOTRIMAZOLE THRUSH TREATMENT ONCE PESSARY This product contains 500 mg of clotrimazole in one compressed pessary. It also contains lactose, maize starch, magnesium stearate, silica-colloidal anhydrous, calcium lactate pentahydrate, crospovidone, lactic acid, hypromellose and cellulose-microcrystalline.

Composite Pack: ‘Once’ Compressed Pessary plus Antifungal Cream CANESTEN CLOTRIMAZOLE THRUSH TREATMENT ONCE PESSARY + CREAM This composite pack includes:  One CANESTEN compressed pessary containing 500 mg of clotrimazole. It also contains lactose, maize starch, magnesium stearate, silica-colloidal anhydrous, calcium lactate pentahydrate, crospovidone, lactic acid, hypromellose and cellulose-microcrystalline;  One tube of CANESTEN antifungal cream containing 10 mg/g (1%) of clotrimazole in a vanishing cream base. It also contains sorbitan monostearate, polysorbate 60, cetyl palmitate, cetostearyl alcohol, octyldodecanol, benzyl alcohol and purified water.

PHARMACOLOGY Pharmacotherapeutic group (ATC code): G01A F02 Clotrimazole is an imidazole derivative with a broad spectrum antimycotic activity. Mechanism of Action Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol synthesis leads to structural and functional impairment of the cytoplasmic membrane.

Pharmacodynamic Properties Clotrimazole has a broad antimycotic spectrum of action in vitro and in vivo, which includes dermatophytes, yeasts, moulds, etc. Under appropriate test conditions, the minimum inhibitory concentration (MIC) values for these types of fungi are in the region of less than 0.062-8.0 g/ml substrate. The mode of action of clotrimazole is primarily 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. In addition to its antimycotic action, clotrimazole also acts on Trichomonas vaginalis, grampositive microorganisms (Streptococci / Staphylococci), and gram-negative microorganisms (Bacteroides / Gardnerella vaginalis). In vitro clotrimazole inhibits the multiplication of Corynebacteria and gram-positive cocci - with the exception of Enterococci - in concentrations of 0.5-10 g/ml substrate and exerts a trichomonacidal action at 100 g/ml. 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.

-3Pharmacodynamic Effects 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 Two 100 mg pessary daily for three days One 500 mg pessary 5 g of 1% cream daily for six days

80% 75% 84% approx 75%

When a first course proved unsuccessful, a second course produced success in 8 of 12 women treated.

Pharmacokinetic Properties Absorption and distribution 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 ug/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 ug/mL was found between 10 and 30 hours after administration. Six hours after application of labeled 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. Pharmacokinetic investigations after dermal application have shown that only a small amount of clotrimazole (

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