pharmachologic effect
A combined drug for intravaginal use, the effectiveness of which is due to the presence of two components in its composition: metronidazole and clotrimazole.
Metronidazole is active against protozoa
: Entamoeba histolytica, Giardia lamblia, Trichomonas vaginalis, as well as
gram-negative anaerobes
: Bacteroides fragilis, Fusobacterium spp., Prevotella spp.
(Prevotella bivia, Prevotella buccae, Prevotella disiens), Gardnerella vaginalis and some gram-positive microorganisms
: Clostridium perffringens, Clostridium difficile, Peptococcus spp., Peptostreptococcus spp. The MIC for these strains is 0.125-6.25 μg/ml.
Clotrimazole has a fungicidal and bactericidal effect. Inhibits the biosynthesis of ergosterol, which regulates the permeability of the cell wall of microorganisms. In small concentrations it acts fungistatically, and in large concentrations it is fungicidal. At fungicidal concentrations, it interacts with peroxidases and mitochondrial enzymes, resulting in an increase in the concentration of hydrogen peroxide to a toxic level, which also leads to the death of fungi. Has high activity
against fungi:
Blastomyces dermatitidis, Candida spp., Coccidioides immitis, Cryptococcus neoformans, dermatophytes (Trichophyton mentagrophytes, Microsporum canis, Epidermophyton foccosum), Histoplasma capsulatum, Paracoccidioides brasiliensis, Sporothrix schenckii;
protozoa:
Trichomonas vaginalis;
gram-positive bacteria
: Streptococcus spp., Staphylococcus spp., Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus mirabilis.
Compound
Metronidazole is used as an active component in the local medicine. This substance is capable of penetrating into the cell of a pathogenic bacterium and reacting with proteins, thereby inhibiting the synthesis of nucleic acids. This, in turn, leads to the death of the pathogenic microorganism.
The instructions for use of the Metrogyl vaginal gel indicate that in addition to the active component, the drug also contains excipients: propyl parahydroxybenzoate, sodium hydroxide, carbopol, methyl parahydroxybenzoate, disodium edetate, propylene glycol, distilled water.
Pharmacokinetics
Metronidazole
Suction
After intravaginal administration, metronidazole undergoes systemic absorption (about 56%). The relative bioavailability of metronidazole in the form of vaginal gel is 2 times higher than the bioavailability of metronidazole in the form of vaginal tablets with a single dose of 500 mg. After a single intravaginal administration of the gel at a dose of 5 g (50 mg of metronidazole), the average Cmax in the blood serum of healthy women is 237 ng/ml, which is 2% of the average Cmax of metronidazole when taken orally at a dose of 500 mg. Time to reach Cmax is 6-12 hours.
Distribution
Penetrates into most tissues, passes through the blood-brain barrier and the placental barrier. Excreted in breast milk. Plasma protein binding is less than 20%.
Metabolism and excretion
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. 60-80% is excreted by the kidneys (20% unchanged), through the intestines - 6-15%.
Clotrimazole
When using clotrimazole intravaginally, no more than 3-10% is absorbed. High concentrations in vaginal secretions and low concentrations in the blood persist for 48-72 hours. In the liver, clotrimazole is rapidly metabolized to inactive metabolites.
Release form
The manufacturer produces a drug with antibacterial and antiprotozoal effects in the form of tablets, solution for intravenous administration and vaginal gel. "Metrogyl" gel is most often used to treat dermatological pathologies and various sexually transmitted infections in women. The product for external use has a uniform consistency and a slightly yellowish tint. Sold in aluminum tubes of 30 g.
One cardboard package contains a tube of medication and an applicator for administering the gel.
Side effect
Local reactions:
burning sensation or increased urination; in the sexual partner - a burning sensation or irritation of the penis.
Systemic reactions:
possible dizziness, headache, nausea, cramping pain in the abdominal cavity.
Allergic reactions:
skin rash, urticaria.
The patient should be warned to stop using the drug and consult a doctor if any unwanted side effects occur.
Indications for use
Despite the fact that the medication in question is capable of inhibiting the vital activity of many pathogenic microorganisms, it does not belong to the category of antibacterial drugs. The active component contained in the drug is a bacteriostatic substance and is capable of providing anti-inflammatory, antioxidant and bactericidal effects. Such a wide range of effects allows the use of an external agent for the treatment of various pathologies caused by microbes sensitive to metronidazole.
Metrogyl vaginal gel will be effective in the treatment of the following ailments:
- vulvovaginitis;
- urogenital trichomoniasis;
- vaginal candidiasis;
- amoebiasis;
- vaginal dysbiosis;
- gardnerellosis.
Using the drug in gel form for the treatment of sexually transmitted infections in women, it is possible to achieve higher bioavailability and penetration of the active substance into the focus of the inflammatory process. Thanks to this, the necessary therapeutic effect is observed even when using a minimal amount of the drug.
special instructions
When using the drug, alcohol consumption 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.
The drug is intended for intravaginal use only. Avoid contact of the drug with the eyes.
During the course of therapy it is necessary to abstain from sexual activity.
Metrogyl for acne: instructions
The list of symptoms for which the drug is indicated is quite extensive:
- rosacea (rosacea);
- chronic inflammatory diseases of the sebaceous glands;
- seborrheic lesions;
- ulcers of the lower extremities;
- long-term non-healing wounds;
- soft tissue necrosis;
- haemorrhoids.
Metrogyl is equally effective against acne and hormonal rashes. It can be used to prevent infection of open wounds, chapping of the face and other serious injuries.
You can only buy acne gel at the pharmacy. The product is available without a prescription, but it is recommended to consult a doctor before use.
Drug interactions
When used simultaneously, the drug enhances the effect of indirect anticoagulants.
Concomitant use with non-depolarizing muscle relaxants (vecuronium) is not recommended.
When used simultaneously with lithium preparations, an increase in the concentration of lithium in the blood plasma is possible.
Phenobarbital accelerates the metabolism of metronidazole due to the induction of microsomal liver enzymes, while cimetidine reduces it.
Amphotericin B, nystatin, natamycin reduce the effectiveness of clotrimazole when used simultaneously.
When used simultaneously with ethanol, the drug can cause disulfiram-like reactions.
"Metrogil" in gynecology
Instructions for use of metronidazole-based gel are most often used in the fields of gynecology and dermatology. Due to the presence of an active antimicrobial substance in the composition, this medication can successfully combat pathologies caused by protozoa and anaerobic bacteria, as well as some types of gram-positive pathogens. In some cases, the drug is used for prophylactic purposes.
In gynecology, Metrogyl gel is often used in the treatment of candidiasis. Almost every woman is familiar with this disease. When infected with fungi of the genus Candida, unpleasant sensations occur in the form of burning and itching in the vaginal area, and a cheesy discharge appears.
With the help of a topical drug based on metronidazole, you can quickly get rid of these unpleasant symptoms. The active substance stops the inflammatory process at the local level, eliminates genital infections and prevents relapses of candidiasis.
Another common pathology in women is urogenital trichomoniasis. This infection can be sexually transmitted and may occur without obvious signs. The causative agent of the disease is the bacterium Trichomonas, which is highly sensitive to metronidazole. That is why doctors recommend using Metrogyl gel to treat this pathology.
Vaginal gel is prescribed only after confirmation of the diagnosis. Both sexual partners must undergo a therapeutic course, even if one of them has no symptoms of the disease. You should abstain from sexual activity for the entire period of therapy. In some cases, it is recommended to use not only an external drug, but also tablets based on the same active substance.
Contraindications
Vaginal gel "Metrogil" is prohibited from use in the following cases:
- with hypersensitivity to metronidazole or auxiliary components of the drug;
- if the patient has liver failure;
- for epilepsy and other severe disorders of the nervous system;
- for pathologies of the circulatory system.
It is strictly forbidden to use an antiprotozoal agent in the first trimester of pregnancy. Also, the drug is not prescribed during lactation. Breastfeeding should be interrupted during treatment with Metrogyl vaginal gel.
With extreme caution, the medication is used simultaneously with indirect anticoagulants. The active substance of the gel somewhat slows down the process of blood clotting.
Analogs
If Metrogyl gel cannot be used in the treatment of gynecological pathologies, then it is replaced with analogues. They have a gel or ointment consistency and are produced in the form of vaginal tablets and suppositories. The greatest therapeutic effectiveness is typical for Polygynax, Trichopolum, Mikozhinax, Efloran, Klion-D.
How else is the gel used?
According to numerous reviews, using Metrogyl vaginal gel you can successfully combat dermatological problems. The bactericidal properties of the drug help to quickly stop the inflammatory process and eliminate the cause of various skin rashes.
After applying the external product to the skin, a barrier is formed that prevents the proliferation of pathogenic bacteria. To treat acne, seborrheic dermatitis, rosacea and pimples, you can use not only gel, but also cream with metronidazole.
Instructions for use
The use of Metrogyl vaginal gel must be agreed with your doctor. The dosage and duration of treatment is determined only by a specialist in each individual case. Usually the course of therapy is 7-10 days. If necessary, it can be extended for a few more days.
Vaginal gel is intended for oral administration twice a day. The medicine must be administered using an applicator. It is placed against the neck of the tube with the drug and the gel is squeezed out until the applicator is completely filled.
It is best to perform the procedure for introducing the medicine into the vagina while lying down. An applicator filled with gel is inserted deep into the vagina and the plunger is slowly pressed. After the manipulation, it is recommended to lie down for several hours. After use, the applicator must be thoroughly washed with soap and treated with medical alcohol.
Can the drug be used during pregnancy?
Pregnancy is accompanied by changes in hormonal levels in women, which often leads to bacterial vaginosis. The use of antibacterial drugs to eliminate this disease in the first trimester of pregnancy is prohibited. This is due to the fact that the active components of such medications can negatively affect the development of the fetus. Already from the second trimester, the doctor can prescribe Metrogyl vaginal gel.
During pregnancy, it is important to follow all the recommendations of the gynecologist and not self-medicate. The vaginal remedy in question is prescribed only for health reasons in a minimum dosage. It should also be borne in mind that the first trimester of pregnancy is not the only contraindication for the use of this drug.
What do patients say about the drug?
In the domestic pharmaceutical market, the drug for the treatment of sexually transmitted infections “Metrogil” (gel) is in great demand. This is due, first of all, to its relatively low cost (compared to similar medications), as well as its pronounced therapeutic effect. According to reviews from both specialists and women who have used this drug for medicinal purposes, with its help you can quickly get rid of a number of unpleasant symptoms: burning, itching, discharge, dryness.
The gel-like consistency of the drug makes it easy to put it into the applicator. The procedure for administering the medicine itself is very simple and does not cause any difficulties. After completing a course of treatment with an antimicrobial drug, it is recommended to restore the vaginal microflora. To do this, you should take medications that contain beneficial bacteria.
Is it possible to use Metrogyl vaginal gel without a doctor’s prescription? Reviews suggest that only a specialist can determine the need to use a specific drug in certain cases. The doctor makes a prescription only after the results of laboratory tests are known.
Description of the drug
Metrogyl vaginal gel is prescribed to patients only after laboratory testing of biological samples. Many pathogenic microorganisms can provoke inflammation of the vaginal mucosa.
Metrogyl gel is recommended for women by a doctor if the following colpitis pathogens are detected in the smear:
- Trichomonas;
- chlamydia;
- clostridia;
- gardenella;
- bacteroides.
Gynecologists prescribe the drug regardless of the stage of the disease, specific or nonspecific etiology. It effectively relieves inflammation, sanitizes infectious foci, eliminates swelling and redness.
Metrogyl vaginal gel is used for treatment in various ways. The drug is evenly distributed on the vaginal mucosa or administered intravaginally using an applicator.
Along with the gel, multivitamins with microelements, immunostimulants, and antiseptic solutions are often included in the therapeutic regimen.
A necessary condition for a quick recovery is proper nutrition. Foods high in sugar are completely excluded from the diet. After their breakdown, an environment favorable for the proliferation of bacteria and protozoa is created.
Clinical and pharmacological group
Metrogyl vaginal gel is part of a group of drugs with antiprotozoal and antibacterial activity used in gynecology.
pharmachologic effect
Vaginal gel is a broad-spectrum medicine.
Its active ingredient is metronidazole, which is chemically a derivative of nitroimidazole. It is active against bacteria, eukaryotes and certain gram-positive microbes. Metrogyl gel is not used for candidiasis (thrush), as it is not able to destroy pathogenic fungi.
The metronidazole molecule contains a nitro group. This electron acceptor is introduced into the respiratory chains of protozoa, anaerobes, in competition with flavoproteins. The result of this impact is:
- violation of respiratory processes;
- death of protozoa and pathogenic bacteria.
The principle of antimicrobial activity is based on the biochemical reduction reactions of the active ingredient. Metronidazole penetrates the cells of microorganisms, integrates into DNA chains, and inhibits polynucleotides. Protozoa and bacteria lose their ability to grow and reproduce and quickly die.
Release form and composition
The Indian manufacturer produces the drug in aluminum tubes. Each contains 30.0 g or 50.0 g of a transparent, odorless, yellowish gel. The secondary packaging, a cardboard box, also contains an applicator and instructions for use.
In addition to the active component metronidazole, the composition includes the following auxiliary ingredients:
- propyl parahydroxybenzoate;
- distilled water;
- sodium hydroxide;
- disodium edetate;
- carbopol;
- propylene glycol;
- methyl parahydroxybenzoate.
These chemical compounds promote the penetration of metronidazole into inflammatory lesions. They enhance and prolong the therapeutic effect of the main substance, moisturize the vaginal mucosa. Vaginal gel should be stored in a dark place at room temperature. The shelf life is 24 months, and after opening the aluminum tube it is reduced to 3 weeks.
The average cost of a topical product is 200 rubles.
The Metrogyl therapeutic line also includes other dosage forms:
- tablets for oral administration;
- dental gel;
- solution for oral administration;
- cream for the treatment of infectious skin diseases.
The instructions for use of Metrogyl vaginal gel recommend its use with tablets for severe infections. The combination of a systemic and local drug helps to quickly eliminate the symptoms of gynecological pathology and speed up recovery.
