Pharmacological properties
Pharmacodynamics.
Metronidazole is a derivative of 5-nitroimidazole, active against anaerobic protozoa and anaerobic bacteria. Metronidazole is effective against trichomonas vaginalis, giardia intestinalis, gardnerella vaginalis, entamoeba histolytica, lamblia spp., as well as obligate anaerobes: bacteroides spp. (b. fragilis, b. distasonis, b. thetaiotaomicron, b. vulgatus, b. ovatus), fusobacterium spp. and some gram-positive microorganisms: eubacterium spp., clostridium spp., peptostreptococcus spp., peptococcus spp. Metronidazole for external use has little antioxidant activity.
It has been established that metronidazole significantly reduces the production of active oxygen, hydroxyl radicals and hydrogen peroxide by neutrophils, which are potential oxidants and can harm tissues at the site of inflammation.
The mechanism of action of metronidazole is the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group of metronidazole interacts with the DNA of microorganisms, inhibiting its synthesis, which leads to the death of microorganisms.
When applied topically, the drug is effective against acne, but the mechanism of this action has not been fully studied.
Pharmacokinetics. When used externally, absorption of the drug is minimal and only a small amount of the drug is determined in the blood plasma. Absorbed metronidazole penetrates the placental barrier and the BBB. Cmax in the blood reaches 66 mg/ml (if 1 g of gel is applied, which is equivalent to 7.5 mg of metronidazole).
Metrogyl plus 50g vaginal gel with applicator 10 pcs.
pharmachologic effect
Antimicrobial and antiprotozoal agent + antifungal agent.
Composition and release form Metrogyl plus 50g vaginal gel with applicator 10 pcs.
Gel – 1 g.:
- Active ingredients: Metronidazole 10.0 mg; Clotrimazole 20.0 mg;
- Excipients: benzyl alcohol 40 mg, disodium edetate 0.50 mg, carbomer-940 10.0 mg, methyl parahydroxybenzoate 1.50 mg, sodium hydroxide 2.0 mg, propyl parahydroxybenzoate 0.50 mg, propylene glycol 50.0 mg, water . required, up to 1.0 g.
30 g in an aluminum tube or a plastic laminated tube, the neck of which is sealed with an aluminum membrane and a screw-on polyethylene cap with a protrusion for perforating the membrane. One lip along with an applicator and instructions for use in a cardboard box.
50 g in an aluminum lip or laminated plastic tube, the neck of which is sealed with aluminum foil laminated with polyethylene and with a polypropylene screw cap with a protrusion (or without a protrusion) for perforating the foil. One tube in a cardboard box along with an applicator and instructions for use.
50 g in an aluminum tube or laminated plastic tube, the neck of which is sealed with aluminum foil laminated with polyethylene and with a polypropylene screw cap with a protrusion (or without a protrusion) for perforating the foil. One tube in a cardboard box along with applicators, in the amount of 10 pieces, instructions for use.
Description of the dosage form
Homogeneous opalescent gel of white or almost white color.
Directions for use and doses
Intravaginally.
The recommended dose is 5 g (one full applicator) 2 times a day (morning and evening).
The course of treatment is 5 days. If necessary, the course of treatment can be repeated after 2 weeks.
Pharmacodynamics
A combined drug for intravaginal use, the effectiveness of which is due to the presence of two active components in its composition: metronidazole and clotrimazole.
The mechanism of action of metronidazole is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group of metronidazole interacts with the DNA of microbial cells, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria. Active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp., (including Bacteroides fragilis, Bacteroides thetaitaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp. ., Prevotella (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.) The minimum inhibitory concentration (MIC) for these strains is 0.125 - 6.25 μg/ml. Aerobic microorganisms and facultative anaerobes are insensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes), metronidazole acts synergistically with antibiotics effective against common aerobes. Clotrimazole is an imidazole derivative. Has a fungicidal effect. Reduces the synthesis of ergosterol, which is an integral part of the cell membrane of the microbial wall, and leads to a change in its structure and properties. In small concentrations it acts fungistatically, and in large concentrations (more than 20 μg/ml) it is fungicidal, and not only on proliferating cells. At fungicidal concentrations, it interacts with mitochondrial and peroxidase enzymes, resulting in an increase in the concentration of hydrogen peroxide to a toxic level, which also contributes to the destruction of fungal cells. It has high activity against pathogenic dermatophytes (Trichophyton mentagrophytes, Microsporum canis, Epidermophyton floccosum), yeast and mold fungi (genus Candida, Torulopsis glabrata, genus Rhodotorula, Pityrosporum orbiculare).
Pharmacokinetics
After intravaginal administration, metronidazole undergoes systemic absorption (about 56%). The relative bioavailability of the vaginal gel is 2 times higher than the bioavailability of a single dose (500 mg) of metronidazole vaginal tablets. Penetrates into breast milk and most tissues, passes through the blood-brain barrier and placenta. After a single intravaginal administration of 5 g of gel (50 mg of metronidazole), the average maximum concentration in the blood serum of healthy women is 237 ng/ml, which is 2% of the average maximum concentration of metronidazole when taken orally at a dose of 500 mg. The time to reach maximum concentration is 6 - 12 hours. Communication with plasma proteins is less than 20%. Metabolized in the liver by hydroxylation, oxidation and glucuronidation. The activity of the main metabolite (2 - oxymetronidazole) is 30% of the activity of the parent compound. Excreted by the kidneys - 60 - 80% of the dose of the systemic drug (20% of this amount unchanged), by the intestines - 6 - 15% of the dose of the systemic drug.
When using clotrimazole intravaginally, no more than 3-10% of the administered dose is absorbed. High concentrations in vaginal secretions and low concentrations in blood persist for 48 to 72 hours. In the liver, clotrimazole is rapidly metabolized to inactive metabolites.
Indications for use Metrogyl plus 50g vaginal gel with applicator 10 pcs.
Bacterial vaginosis of various etiologies, confirmed by clinical and microbiological data; candidiasis vulvitis and vulvovaginitis, urogenital trichomoniasis.
Contraindications
Hypersensitivity to the components of the drug. Leukopenia (including history), organic lesions of the central nervous system (including epilepsy), liver failure, menstrual period. Pregnancy I trimester, lactation period.
Application Metrogyl plus 50g vaginal gel with applicator 10 pcs. during pregnancy and breastfeeding
The use of the drug in the second and third trimester of pregnancy is possible only for health reasons, if the potential benefit to the mother outweighs the risk to the fetus. When prescribing the drug during lactation, breastfeeding must be stopped.
special instructions
Simultaneous treatment of sexual partners is recommended.
During the course of treatment it is necessary to abstain from sexual activity.
For vaginitis caused by Trichomonas vaginalis, it is advisable to simultaneously treat the sexual partner with metronidazole for oral administration. If the drug is used together with metronidazole for oral administration, especially with a repeated course, monitoring of the peripheral blood picture is necessary (danger of leukopenia).
During the treatment period, alcohol intake is contraindicated (a disulfiram-like reaction may develop: cramping abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).
Metronidazole can immobilize treponemes and lead to a false-positive Nelson test.
Avoid contact with eyes!
Impact on the ability to drive vehicles and operate machinery
The drug does not affect the ability to drive vehicles or engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
There have been no cases of overdose when the drug is prescribed in recommended doses.
Side effects Metrogyl plus 50g vaginal gel with applicator 10 pcs.
Local reactions: Itching, burning and hyperemia of the mucous membrane of the external genitalia; in the sexual partner - a burning sensation or irritation of the penis, frequent urination.
Possible systemic effects: Dizziness, headache, dry mouth, changes in taste, including a “metallic” taste, nausea, vomiting, decreased appetite, abdominal cramps, constipation or diarrhea, dark urine, leukopenia or leukocytosis .
Allergic reactions: Skin rash, urticaria.
If any unwanted side effects occur, you must stop treatment and consult a doctor!
Drug interactions
For intravaginal use only!
Similar to disulfiram, it causes ethanol intolerance.
Enhances the effect of indirect anticoagulants; it is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).
When taken simultaneously with lithium preparations, the concentration of lithium in the blood plasma may increase.
Phenobarbital accelerates the metabolism of metronidazole due to the induction of microsomal liver enzymes, cimetidine reduces it, which can lead to an increase in its concentration in the blood serum and an increased risk of side effects.
Amphotericin B, nystatin, natamycin reduce the effectiveness of clotrimazole when used simultaneously.
special instructions
Avoid getting the drug into your eyes. If the gel gets into your eyes, you must immediately rinse them with plenty of water.
The gel should not be applied to areas close to the eyes. The affected area should be cleaned before applying Metrogyl gel. After applying the drug, you can use cosmetics.
For ordinary acne, the use of Metrogyl gel should be combined with oral antibiotics.
When applied to a large surface area of the skin or in case of prolonged use of Metrogyl gel, there is a possibility of developing systemic side effects.
The drug should be prescribed with caution to patients with impaired hematopoietic function.
Metronidazole for topical use is not effective for the treatment of telangiectasia, which occurs with erythematosus.
Propyl parahydroxybenzoate (E216) and methyl parahydroxybenzoate (E218), which are part of the drug, can cause an allergic reaction (possibly delayed).
Use during pregnancy and lactation.
When taken orally, metronidazole crosses the placental barrier into breast milk in very significant concentrations.
Despite the fact that when applied topically, the concentration of metronidazole in the blood is low, Metrogyl gel is contraindicated in the first trimester of pregnancy, and in the second and third trimester it can be used if absolutely necessary.
Breastfeeding should be stopped during treatment.
Children. Do not use in children.
The ability to influence reaction speed when driving vehicles or operating machinery. The use of the drug at the indicated dose does not affect driving or working with potentially dangerous mechanisms.
Metrogyl gel for external application approx 10 mg/g aluminum tube 30 g
Registration Certificate Holder
UNIQUE PHARMACEUTICAL Laboratories (India)
Dosage form
Medicine - Metrogyl® (Metrogyl®)
Description
Gel for external use
homogeneous, colorless to yellow.
1 g
metronidazole 10 mg
Excipients
: methyl parahydroxybenzoate, propyl parahydroxybenzoate, carbomer 940, disodium edetate, sodium hydroxide, propylene glycol, purified water.
30 g - aluminum tubes (1) - cardboard packs.
Indications
- rosacea (including post-steroid acne);
- acne vulgaris;
- oily seborrhea, seborrheic dermatitis;
- trophic ulcers of the lower extremities (against the background of varicose veins, diabetes mellitus);
- poorly healing wounds;
- bedsores;
- hemorrhoids, anal fissures.
Contraindications for use
- hypersensitivity to the components of the drug.
pharmachologic effect
Metronidazole is a synthetic broad-spectrum antimicrobial and antiprotozoal agent from the group of imidazoles. Active against anaerobes
(Bacteroides spp., Fusobacterium spp., Mobiluncus spp., Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Eubacterium spp., Bacteroides fragilis, Prevotella spp.) and
protozoa
(Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica).
When applied topically, it has an anti-acne effect, the mechanism of which is precisely unknown (not related to the effect on the Demodex folliculorum mite, found in hair follicles and the secretion of the sebaceous glands, and any effect on the production of this secretion).
Metronidazole for external use may have antioxidant activity. It has been found that it significantly reduces the production of active oxygen, hydroxyl radicals and hydrogen peroxide by neutrophils, which are potential oxidants that can cause tissue damage at the site of inflammation. Metronidazole for external use is not effective against telangiectasias noted with rosacea.
Drug interactions
When the gel is applied topically, interaction with other drugs is negligible, but caution should be exercised when administered simultaneously with warfarin and other indirect anticoagulants (increases prothrombin time).
Dosage regimen
For external use. The gel is applied to previously cleansed affected areas of the skin in a thin layer 2 times a day, morning and evening, for 3-9 weeks.
The duration of treatment is 3-4 months, the therapeutic effect is usually observed after 3 weeks of treatment.
Overdose
There were no cases of drug overdose in recommended doses when using the drug externally.
Side effect
When the gel is applied topically, the concentration of metronidazole in the blood is very low, so the risk of systemic side effects is low.
Rarely
Allergic reactions may occur (urticaria, skin rash); hyperemia, peeling, slight dryness and burning of the skin, lacrimation (if the gel is applied close to the eyes).
special instructions
Avoid contact with eyes. If the gel gets into your eyes, rinse them immediately with plenty of water.
Storage conditions
Store at a temperature not exceeding 30°C, out of the reach of children. Do not freeze.
Best before date
Shelf life: 3 years. Do not use after the expiration date stated on the packaging.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - With caution. Restrictions when breastfeeding - With caution.
Carefully -
I trimester of pregnancy, lactation period.
Terms of sale
The drug is approved for use as a means of OTC.
Interactions
When applied topically in recommended doses, no systemic interaction of Metrogyl gel with other drugs was detected. however, caution should be exercised when prescribing Metrogyl gel with certain medications.
Warfarin and other coumarin anticoagulants. Metronidazole enhances the anticoagulant effect, which leads to an increase in the time of prothrombin formation.
Phenobarbital. When used simultaneously with metronidazole, the antimicrobial activity of the latter decreases. The reason is the accelerated metabolism of metronidazole.
Disulfiram. Concomitant use increases the toxicity of the drugs, which can lead to the development of neurological symptoms.
Cimetidine. Suppresses the metabolism of metronidazole, which may lead to increased concentrations of metronidazole in the blood serum.
During systemic therapy with metronidazole, it is necessary to refrain from drinking alcohol, since a disulfiram-like reaction is possible.
Note!
The description of the drug Metrogyl gel tube 30g on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
