Instructions for use Metrogil gel for external use, tube 30 g
Composition
active ingredient: metronidazole;
1 g of gel contains 10 mg of metronidazole;
Excipients: propyl parahydroxybenzoate (E 216), propylene glycol, carbomer 940, disodium edetate, sodium hydroxide, methyl parahydroxybenzoate (E 218), purified water.
Dosage form
Gel for external use.
Main physicochemical properties: homogeneous gel from colorless to yellow.
Pharmacotherapeutic group
Chemotherapeutic agents for topical use. ATX code D06B X01.
Pharmacological properties
Pharmacodynamics
Metronidazole is a 5-nitroimidazole derivative, 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 topical use has minor antioxidant activity.
Metronidazole has been found to significantly reduce the production of reactive oxygen species, hydroxyl radicals, and hydrogen peroxide by neutrophils, which are potential oxidants and can cause tissue damage 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 understood.
Pharmacokinetics
When applied externally, the absorption of the drug is minimal and only a small amount of the drug is found in the blood plasma. Absorbed metronidazole penetrates the placental and blood-brain barriers. The maximum concentration in the blood reaches 66 mg/ml (if 1 g of gel is applied, which is equivalent to 7.5 mg of metronidazole).
Indication
For topical use in the treatment of inflammatory papules, pustules, and erythema in rosacea.
Contraindication
Hypersensitivity to metronidazole, as well as to nitroimidazole derivatives and to any components included in the drug.
Interaction with other medicinal products and other types of interactions
When applied topically at recommended doses, no systemic interactions of Metrogil® gel with other drugs have been identified. However, caution should be exercised when prescribing Metrogil® gel with certain drugs.
Warfarin and other coumarin anticoagulants. Metronidazole enhances the anticoagulant effect, leading to a prolongation of prothrombin time.
Phenobarbital. When used simultaneously with metronidazole, the antimicrobial activity of the latter decreases. The reason is the accelerated metabolism of metronidazole.
5-fluorouracil. Decreased clearance of 5-fluorouracil leads to increased toxicity of 5-fluorouracil.
Disulfiram. Concomitant use increases the toxicity of the drugs, which may lead to the development of neurological symptoms, therefore Metrogil® gel should not be prescribed to patients who have taken disulfiram within the last two weeks.
Cimetidine. Inhibits the metabolism of metronidazole, which may lead to increased serum metronidazole concentrations and an increased risk of adverse events.
Non-depolarizing muscle relaxants (vecuronium). Combination with metronidazole is not recommended.
Lithium Plasma lithium levels may increase when metronidazole is administered. Plasma lithium, creatinine and electrolyte concentrations should be monitored during concomitant use.
Cyclosporine: There is a risk of increased serum levels of cyclosporine. If concomitant use is necessary, cyclosporine and creatinine levels should be closely monitored.
Busulfan: Metronidazole may increase plasma levels of busulfan, which may lead to significant busulfan toxicity.
During systemic therapy with metronidazole, it is necessary to refrain from drinking alcohol, as a disulfiram-like reaction is possible.
Application features
Avoid contact with eyes. If the gel gets into your eyes, rinse them immediately with plenty of water.
Do not apply the gel to areas close to the eyes. The affected area should be cleaned before applying Metrogil® gel. Cosmetics may be used after application.
For common acne, the use of Metrogil® gel should be combined with the internal administration of antibiotics.
When applied to a large area of the skin surface or with prolonged use of Metrogil® gel, there is a possibility of developing systemic side effects.
Long-term use of the drug requires monitoring of blood counts. If leukopenia occurs, it is important to carefully compare the expected benefits of continued therapy with the possible risks.
Metrogil® gel should be prescribed with caution to patients with permanent or progressive nephropathies.
If ataxia, dizziness, hallucinations appear, or if the patient's neurological status deteriorates, treatment with the drug should be discontinued.
The drug should be administered with caution to patients with impaired hematopoietic function.
Topical metronidazole is ineffective for treating telangiectasia seen in acne vulgaris.
Propyl parahydroxybenzoate (E 216) and methyl parahydroxybenzoate (E 218), which are part of the preparation, may cause allergic reactions (possibly delayed). Propylene glycol, which is part of the preparation, may also cause skin reactions.
During treatment with metronidazole, alcohol consumption should be avoided (tachycardia, nausea, vomiting, feeling of heat, spastic pain in the epigastrium, headache may occur).
Use during pregnancy or breastfeeding
Despite the fact that the concentration of metronidazole in the blood is low when applied topically, Metrogil® gel is contraindicated in the first trimester of pregnancy, and in the second and third trimesters it can be used in case of extreme need.
Breastfeeding should be discontinued during treatment with the drug.
Ability to influence reaction speed when driving vehicles or other mechanisms
The use of the drug in the specified dose does not affect the ability to drive vehicles or operate potentially dangerous mechanisms.
Method of administration and doses
For external use only!
Apply a thin layer of the gel to the affected area of the skin after cleansing. Apply twice a day (morning and evening).
The duration of treatment is determined by the doctor individually. If necessary, apply an occlusive dressing. The therapeutic effect is observed after 3 weeks of treatment.
Children
Do not use on children.
Overdose
Cases of overdose of Metrogil® gel when applied topically are unknown. When applied topically, metronidazole is absorbed in small amounts. Leukopenia, neuropathy, ataxia, vomiting may occur. Since the specific antidote to metronidazole is unknown, symptomatic therapy is recommended.
Side effects
Adverse reactions associated with topical metronidazole are generally infrequent and mild. Adverse reactions have occurred in no more than 2% of patients.
Central nervous system: dizziness, headache, convulsions, peripheral sensory neuropathy; very rarely - encephalopathy (e.g., confusion) and subacute cerebellar syndrome (ataxia, dysarthria, gait disturbance, nystagmus, tremor), which may resolve after discontinuation of the drug.
Mental disorders, including confusion, hallucinations.
On the part of the organs of vision: tearing (if the gel is applied close to the eye area), temporary visual impairment (diplopia, myopia).
From the side of the hematopoietic system: leukopenia, leukocytosis, agranulocytosis, neutropenia, thrombocytopenia.
Allergic reactions: skin rash, mild dryness, urticaria, skin itching, skin hyperemia, fever, angioedema, rarely - anaphylactic shock. Isolated cases of pustular rash.
Propyl parahydroxybenzoate (E 216) and methyl parahydroxybenzoate (E 218), which are part of the preparation, may cause allergic reactions (possibly delayed). Propylene glycol, which is part of the preparation, may also cause skin reactions.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 ° C. Do not freeze. Keep out of the reach of children.
Packaging
30 g in an aluminum or laminated plastic tube. 1 tube in a cardboard box.
Vacation category
According to the recipe.
Producer
Unique Pharmaceutical Laboratories (a division of J.B. Chemicals and Pharmaceuticals Ltd.)
Address
Plot No. 304-308, G. I. D. C. Industrial Area, Panoli Town – 394 116, Bharuch District, India.
