INSTRUCTION
for Medicinal Usage of Preparation
Clomegel
Registration number
Trade name: Clomegel
Group name: Clotrimazole + Metronidazole&
Dosage form: vaginal gel
Formulation for preparation of 100 g of gel:
Active substances: clotrimazole - 2.0 g, metronidazole - 1.0 g
Adjuvants: propylene glycol, carbomer (carbopol), methyl parahydroxybenzoate (nipagin, methyl
paraben), propyl parahydroxybenzoate (nipazole, propylparaben), disodium edentate (dinatrii eathylendiamintetraacetas, trilon B), benzyl alcohol, macrohol (polyethylene glycol 400), purified water.
Appearance: Colorless or slightly yellowish gel.
Pharmacotherapeutic group: combination antimicrobial agent (antimicrobial and antiprotozoal
agent + antifungal agent)
ATX Code: [G01AF20]
Pharmacologic Properties
Pharmacodynamics. Combination preparation for intravaginal usage, the effectiveness of which is
conditioned by the presence of two components in its formulation: metronidazole and clotrimazole.
Metronidazole is an antiprotozoal and antibacterial preparation, a 5-nitroimidazole derivative. The
mechanism of action consists in biochemical reduction of metronidazole 5-nitrogroup by intracellular transport proteins of anaerobic microorganisms and protozoans. The reduced metronidazole 5nitrogroup interacts with the DNA of the microorganisms cells, inhibiting the synthesis of their nucleic acids, resulting in the bacteria death.
Active in relation to Trichomonas vaginalis, Entamoeba histolytica as well as to gram-negative anaerobes Bacteroides spp. (including В. Fragilis, В. distasonis, В. ovatus, В. thetaiotaomicron, В.
vulgatus), Fusobacterium spp., and some gram-positive anaerobes (sensitive strains Еubacterium
spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp.).
Minimal inhibitory concentration of these strains constitutes 0.125 to 6.25 mcg/ml.
Clotrimazole is an antifungal agent of the imidazole derivatives group for external and topical (intravaginal) use; it decreases the synthesis of ergosterine constituting a part of the fungus cellular
membrane, and brings about the change of its structure and properties.
It displays fungistatic activity in small concentrations and fungicidal activity in large concentrations
(of more than 20 mcg/ml), and not only in relation to proliferous cells at that. In fungicidal concentrations, it interacts with mitochondrial enzymes and peroxidases, resulting in an increase of the hydrogen peroxide concentration to the toxical value, that also contributing to the fungal cells destruction.
Active against pathogenic dermatophytes (Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis), yeast and mold fungi (Candida spp., Torulopsis glabrata, of genus Rhodotorula, Pityrosporum orbiculare).
Pharmacokinetics. At intravaginal introduction, metronidazole is subjected to systemic absorption
(about 56%). Relative bioavailability of vaginal gel is two times higher than that of a single dose
(500 mg) of vaginal metronidazole tablets. Penetrates breast milk and most of tissues, traverses
hematoencephalic barrier and placenta. After a single intravaginal introduction of 5 g gel (50 mg
metronidazole), mean maximal concentration in blood serum in healthy women amounts to 237
ng/ml, that constituting 2% of the mean maximal metronidazole concentration at a 500 mg dose ingestion. Time to achieving the maximal concentration is 6 to 12 hours. Binding with plasma proteins
constitutes less than 20%. Metabolized in liver by hydroxylation, oxidation and glucuronidation. Activity of the major metabolite (2-oxymetronidazole) constitutes 30% of the parent compound activity. Excreted by kidneys and via intestine.
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At intravaginal clotrimazole administration, not more than 3 to 10% of the introduced dose is absorbed. High concentrations in the vaginal secretion and low concentrations in blood persist for 48 to
72 hours. Clotrimazole is quickly metabolized to inactive metabolites in liver.
Indications for usage
Bacterial vaginosises caused by agents sensitive to metronidazole, proved by clinical and microbiological findings; candidous vulvitises and vulvovaginitises, urogenital trichomoniasis.
Contraindications
Increased sensitivity to the preparation components, leucopenia (also in the anamnesis), organic lesion of central nervous system (including epilepsy), liver impairment, pregnancy.
Pregnancy and lactation
The use of the preparation during pregnancy is contra-indicated. In case the drug is administered
during lactation, breast feeding is to be abandoned.
Method of application and doses
Intravaginally. Recommended dose constitutes 5 g (one completely filled applicator) 2 times a day
(in the morning and evening). Course of treatment: 5 days. If necessary, the course of treatment may
be repeated in 2 weeks.
Side Effects
Local reactions: burning sensation or more frequent urination; burning sensation or penis irritation
experienced by the sexual partner.
Systemic effects may develop: vertigo, headache, nausea, abdominal cramps.
Allergic reactions: skin eruption, nettle rush.
In case any adverse side effects occur, one must stop the treatment and consult a doctor!
Overdosage
Overdosage has not been detected at intravaginal administration method.
Interaction with other medicinal preparations
Metronidazole. Increases the action of indirect anticoagulants, that resulting in longer time of the
prothrombin formation.
Similar to disulfiram, causes intolerance to ethanol.
Simultaneous administration with disulfiram may bring about the development of various neurological symptoms.
Сimetidine suppresses the metabolism of metronidazole, that may cause an increase of its concentration in blood serum and an increased risk of the side effects development.
Simultaneous administration of medicinal agents stimulating the microsomal oxidation enzymes in
the liver (phenobarbital, phenytoin) may accelerate the metronidazole elimination, resulting in the
decrease of its concentration in plasma.
At simultaneous intake with preparations of Li+ the concentration of the latter in plasma may increase and signs of intoxication may develop.
Combination with nondepolarizing muscle relaxant (vecuronium bromide) is not recommended.
Sulfanilamides increase the metronidazole antimicrobial effect.
Clotrimazole.
Amphotericin В, nystatin, and natamycin decrease the clotrimazole effectiveness at simultaneous
use.
Specific Instructions
During the treatment, alcohol intake is contra-indicated (a disulfiram-like reaction may develop: abdominal cramps, nausea, vomiting, headache, sudden blood afflux to the face).
Metronidazole may immobilize treponemas and result in a false-positive result of Nelson’s test.
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For intravaginal usage only!
Do not let the gel get into your eyes!
During the course of treatment it is necessary to refrain from sexual intercourse.
Effect on the ability to drive a car or operate working mechanisms
Using the preparation does not affect the ability to drive transport vehicles and control machines and
mechanisms requiring a concentration of attention.
Form of issue
Vaginal gel 20 mg + 10 mg/g.
30 g in aluminum tubes. Each tube with an applicator for intravaginal introduction and an instruction
for usage is placed in a cardboard box.
Storage conditions
In a dry place protected from light, at a temperature of 15°С up to 25°С. Freezing is impermissible.
Keep out of reach of children.
Effective life
2 years. Do not use after the expiration of effective life specified on the package.
Dispensing Conditions
Prescription medicine.
Manufacturer/organization that accepts claims:
Open Joint Stock “Kurgan Joint Stock Company of Medical Preparations and Articles “Sintez” (Sintez Joint Stock Company);
#7, Prospect Konstitutsii, city of Kurgan, Russian Federation, 640008;
Tel. /fax: (3522)481689
Internet-site: http://www.kurgansintez.ru
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