Klomegel

General characteristics. Structure:

Active ingredient:  1 g Clotrimazolum of 20 mg; metronidazole of 10 mg;

Excipients: benzyl alcohol - 2 g, carbomer (карбопол) - 1 g, methylparahydroxybenzoate - 0.15 mg, пропилпарагидроксибензоат - 0.05 g, a macrogoal - 45 g, propylene glycol - 30 g, dinatrium эдетат - 0.05 g, the water purified - to 100 g.

Description: gel vaginal colourless or with a yellowish shade.

Pharmacological properties:

The combined drug for intravaginalny use which efficiency is caused by existence in its structure of two components: Clotrimazolum and metronidazole.

Clotrimazolum - antifungal means from group of derivatives of an imidazole for external and topical (intravaginalny) use. Reduces synthesis of the ergosterol which is a component of a cellular membrane of a mushroom and leads to change of its structure and properties.

In small concentration affects fungistaticly, and in big (more than 20 mkg/ml) - fungitsidno, and not only proliferating cells. In fungicidal concentration interacts with mitochondrial enzymes and peroxidases therefore there is an increase in concentration of peroxide of hydrogen up to toxic value that also promotes destruction of fungal cells.

It is active concerning barmy and mold mushrooms (Candida spp., Torulopsis glabrata, sorts Rhodotorula, Pityrosporum orbiculare), pathogenic dermatophytes (Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis).

Metronidazole - antiprotozoan and antibacterial agent, derivative 5 nitroimidazoles. The mechanism of action consists in biochemical recovery 5 nitrogroups of metronidazole intracellular transport proteins of anaerobic microorganisms and protozoa. The recovered 5 nitrogroup of metronidazole interacts with DNA of a cell of microorganisms, inhibiting synthesis of their nucleic acids that leads to death of bacteria.

Entamoeba histolytica, and also gram-negative anaerobe bacterias of Bacteroides spp is active concerning Trichomonas vaginalis. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp. and some gram-positive anaerobe bacterias (sensitive strains of Eubacterium spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp.).

The minimum overwhelming concentration for these strains makes 0.125-6.25 mkg/ml.

 

Pharmacokinetics. Absorption

At use of Clotrimazolum no more than 3-10% of the entered dose are intravaginalno absorbed. High concentration in a vaginal secret and low concentration in blood remain during 48-72 h.

After intravaginalny introduction metronidazole is exposed to system absorption (about 56%). Relative bioavailability of vaginal gel is twice higher than bioavailability of a single dose (500 mg) of vulval tablets of metronidazole. After single intravaginalny introduction of 5 g of gel (50 mg of metronidazole) average Cmax is equal in blood serum of healthy women to 237 ng/ml that makes 2% of average Cmax of metronidazole at intake of a dose of 500 mg. Time of achievement of Cmax - 6-12 h.

Distribution

Metronidazole gets into breast milk and the majority of fabrics, passes through GEB and a placenta. Linkng with proteins of plasma makes less than 20%.

Metabolism

Clotrimazolum is quickly metabolized in a liver to inactive metabolites.

Metronidazole is metabolized in a liver by a hydroxylation, oxidation and a glyukuronirovaniye. Activity of the main metabolite (2 oxymetronidazole) makes 30% of activity of initial connection.

Removal

Metronidazole is removed by kidneys and through intestines.

Indications to use:

— the bacterial vaginoses caused by activators, sensitive to metronidazole, confirmed with clinical and microbiological data;

— candidosis vulvita and vulvovaginitis;

— urogenital trichomoniasis.

Route of administration and doses:

Intravaginalno. The recommended dose makes 5 g (1 full applicator) 2 (in the morning and in the evening). A course of treatment - 5 days. If necessary the course of treatment can be repeated in 2 weeks.

Features of use:

Only for intravaginalny use. To avoid hit of gel in eyes.

During a course of treatment it is necessary to abstain from sex life.

During treatment alcohol intake is contraindicated (possibly development of disulfiramopodobny reaction: spastic abdominal pains, nausea, vomiting, a headache, sudden rush of blood to the person).

Metronidazole can immobilize treponemas and lead to the false positive test of Nelson.

Influence on ability to driving of motor transport and to control of mechanisms

Use of drug does not exert impact on control of vehicles and on service of the cars and mechanisms demanding concentration of attention.

Side effects:

Local reactions: a burning sensation or the speeded-up urination; the sexual partner has a burning sensation or irritation of a penis.

Development of system effects is possible: dizziness, headache, nausea, spastic abdominal pains.

Allergic reactions: skin rash, small tortoiseshell.

In case of any undesirable side effects it is necessary to stop treatment and to see a doctor.

Interaction with other medicines:

Clotrimazolum

Amphotericinum In, nystatin, натамицин reduce efficiency of Clotrimazolum at simultaneous use.

Metronidazole

Strengthens effect of indirect anticoagulants that leads to increase in time of formation of a prothrombin.

Similar to Disulfiramum causes intolerance of ethanol.

Simultaneous use with Disulfiramum can lead to development of various neurologic symptoms.

Cimetidinum suppresses metronidazole metabolism that can lead to increase in its concentration in blood serum and to increase in risk of development of by-effects.

Co-administration of the medicines stimulating enzymes of a microsomal oxidation in a liver (phenobarbital, Phenytoinum) can accelerate metronidazole elimination therefore its concentration in plasma goes down.

At a concomitant use with drugs of lithium concentration of the last in plasma and development of symptoms of intoxication can increase.

It is not recommended to combine with not depolarizing muscle relaxants (a vekuroniya bromide).

Streptocides strengthen antimicrobic effect of metronidazole.

Contraindications:

— organic lesion of TsNS (including epilepsy);

— liver failure;

— a leukopenia (including in the anamnesis);

— pregnancy;

— hypersensitivity to drug components.

 

Use of the drug KLOMEGEL® at pregnancy and feeding by a breast
Use of drug at pregnancy is contraindicated. At purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

 

Use at abnormal liver functions
It is contraindicated at a liver failure.

Overdose:

At an intravaginalny way of introduction the overdose is not established.

Storage conditions:

Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature from 15 °C to 25 °C. Freezing is not allowed. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

30 g - aluminum (1) complete with the applicator for intravaginalny introduction with a capacity of 5 g (1) - packs cardboard.