Metronidazole gel for external use. approx. 1% 18g tube No. 1

International nonproprietary name: Metronidazole/Metronidazole Synonyms: Metrogyl.

Pharmacotherapeutic group Antimicrobial drugs for local use

Composition Each tube contains: active substance metronidazole (in terms of 100% substance) 180.0 mg.

Pharmacological action When applied topically, it has an anti-acne effect, the mechanism of which is not precisely known (not related to the effect on the Demodex folliculorum mite, found in the hair follicles and the secretion of the sebaceous glands, and any effect on the production of this secretion) Metronidazole for external use, possibly has 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 ineffective against telangiectasias noted with rosacea.

Indications for use: rosacea (including post-steroid acne); — vulgar acne; - eczema, seborrheic eczema; oily seborrhea, seborrheic dermatitis; - trophic ulcers of the lower extremities (against the background of varicose veins, diabetes mellitus); - slow-healing wounds; - bedsores; - hemorrhoids, anal fissures

Method of application and dosage regimen The drug is intended for external and local use. Metronidazole gel is applied to previously cleansed affected areas of the skin or mucous membrane in a thin layer 2 times a day, morning and evening. A pronounced clinical effect occurs after 3 weeks of therapy. The duration of treatment is 1-4 months.

Special instructions It is important to apply the drug to the entire affected area. Metronidazole for external use in the form of a gel does not contain fats, is invisible on the face and does not leave stains on clothes. After applying the gel, you can use cosmetics.

Side effects When the gel is applied topically, the concentration of metronidazole in the blood is very low, so the risk of developing systemic side effects is very low. Rarely the following may be observed: allergic reactions (urticaria, skin rash); hyperemia, peeling, slight dryness and burning of the skin, lacrimation (if the gel is applied close to the eyes).

Contraindications Hypersensitivity to the components of the drug.

Precautions For external and local use only. Do not apply to the mucous membrane of the eyes or near the eyes (may cause lacrimation). If the gel gets into your eyes, rinse them immediately with plenty of water. When applied to large surfaces of the skin or with prolonged use, there is a possibility of resorption of metronidazole and the development of systemic side effects, so the drug should be prescribed with caution to patients with impaired hematopoietic function. If local reactions occur, the drug should be used less frequently or discontinued.

Interaction with other drugs When applied topically, metronidazole gel interacts with other drugs insignificantly, but caution should be exercised when administered concomitantly with warfarin and other indirect anticoagulants (increases prothrombin time).

Overdose When the gel is used externally in recommended doses, an overdose of the drug is unlikely.

Release form: gel for external use 1% in aluminum tubes 18 g.

Metronidazole solution for infusion 5 mg/ml bottle, 100 ml

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SYNTHESIS (Russia)

Dosage form

Medicine - Metronidazole-AKOS (Metronidazole-AKOS)

Description

Solution for infusion 0.5%

transparent, with a greenish tint.

1 ml

metronidazole 5 mg

Excipients

: disodium salt of ethylenediaminetetraacetic acid, water d/i.

20 ml - dark glass bottles (5) - cardboard packs. 100 ml - bottles (1) - cardboard packs. 20 ml - dark glass bottles (10) - cardboard packs. 100 ml - bottles (1) - cardboard packs.

Indications

protozoal infections (extraintestinal amebiasis /including liver abscess/, intestinal amebiasis, trichomoniasis, balantidiasis, giardiasis (giardiasis), cutaneous leishmaniasis, trichomonas vaginitis, trichomonas urethritis);
infections caused by Bacteroides spp., incl. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus (bone and joint infections, central nervous system infections (including meningitis, brain abscess/, bacterial endocarditis, pneumonia, empyema and lung abscess);
infections caused by Bacteroides spp. (including Bacteroides fragilis), Clostridium spp., Peptococcus spp., Peptostreptococcus spp. (infections of the abdominal cavity /peritonitis, liver abscess/, infections of the pelvic organs /endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, infections of the vaginal vault after surgery/, infections of the skin and soft tissues);
sepsis caused by Bacteroides spp. (including Bacteroides fragilis) and Clostridium spp.;
pseudomembranous colitis (associated with the use of antibiotics);
gastritis or duodenal ulcer associated with Helicobacter pylori;
alcoholism;
as a radiosensitizing agent during radiation therapy (in cases where tumor resistance is due to hypoxia in tumor cells);
prevention of postoperative infections (especially after operations on the colon, peri-rectal area, appendectomy, gynecological interventions).

Contraindications for use

leukopenia (including history);
organic lesions of the central nervous system;
epilepsy;
liver failure (when using the drug in high doses);
pregnancy (first trimester);
lactation (breastfeeding);
hypersensitivity to the drug.

pharmachologic effect

Antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with the DNA of the microbial cell, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

The drug is active against:

Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp.;
anaerobic bacteria:
Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella spp. (Prevotella bivia, Prevotella buccae, Prevotella disiens), Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp. The MIC for these strains is 0.125-6.25 μg/ml.

In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

Aerobic microorganisms and facultative anaerobes
are resistant to the drug

The drug increases the sensitivity of tumors to radiation, has a disulfiram-like effect, and stimulates reparative processes.

Drug interactions

With the simultaneous use of metronidazole with indirect anticoagulants, an increase in the time of prothrombin formation is observed.

With the simultaneous use of Metronidazole-AKOS with lithium salt preparations, it is possible to increase the concentration of lithium in the blood plasma and develop symptoms of intoxication.

When used simultaneously with cimetidine, inhibition of the metabolism of metronidazole is observed, which can lead to an increase in the concentration of metronidazole in the blood plasma and an increased risk of adverse reactions.

When used simultaneously with metronidazole, drugs that stimulate microsomal oxidation enzymes in the liver (phenytoin, phenobarbital) may accelerate the elimination of metronidazole, resulting in a decrease in its concentration in the blood plasma.

Sulfonamides enhance the antimicrobial effect of metronidazole.

When used simultaneously with ethanol, the development of disulfiram-like reactions is observed.
Pharmaceutical interactions
Metronidazole for intravenous administration is not recommended to be mixed with other drugs.

Dosage regimen

IV drip for adults and children over 12 years old

the drug is prescribed in an initial dose of 0.5-1 g (infusion duration 30-40 minutes). Then every 8 hours, 500 mg at a rate of 5 ml/min. If well tolerated, after the first 2-3 infusions they switch to jet administration. The course of treatment is 7 days. If necessary, intravenous administration is continued for a longer time. The maximum daily dose is 4 g. According to indications, switch to maintenance oral administration at a dose of 400 mg 3 times a day.

Children under 12 years of age

prescribed according to the same regimen in a single dose of 7.5 mg/kg.

For purulent-septic diseases

usually carry out 1 course of treatment.

For preventive purposes
, adults and children over 12 years of age
are prescribed 0.5-1 g drips on the eve of surgery, on the day of surgery and the next day - 1.5 g / day (500 mg every 8 hours). After 1-2 days, they switch to maintenance therapy orally.

For patients with chronic renal failure (with CC less than 30 ml/min)

the maximum daily dose is 1 g.

As a radiosensitizing agent

the drug is administered intravenously at a rate of 160 mg/kg or 4-6 g/m2 of body surface 0.5-1 hour before the start of irradiation.
Apply before each irradiation session for 1-2 weeks. During the remaining period of radiotherapy, metronidazole is not used. The maximum single dose is 10 g, course dose is 60 g. To relieve intoxication caused by radiation, drip administration of glucose solutions, hemodez or isotonic sodium chloride solution is used.
For cervical and uterine cancer, skin cancer

the drug is used in the form of local applications (3 g dissolved in a 10% solution of dimethyl sulfoxide), swabs that are used topically are moistened 1.5-2 hours before irradiation). In case of poor tumor regression, applications are carried out throughout the entire course of radiation therapy. If the dynamics of tumor clearance from necrosis is positive - within the first 2 weeks.

Overdose

There are no data on drug overdose.

Treatment:

Metronidazole and its main metabolites are quickly removed by hemodialysis (T1/2 is reduced to 2.6 hours). During peritoneal dialysis, it is excreted in small quantities.

Side effect

From the digestive system:

nausea, vomiting, diarrhea, intestinal colic, constipation, metallic taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.

From the nervous system:

dizziness, impaired coordination of movements, ataxia, confusion, irritability, depression, increased excitability, weakness, insomnia, headache, convulsions, hallucinations, peripheral neuropathy.

From the urinary system:

dysuria, cystitis, polyuria, urinary incontinence, red-brown color of urine.

Allergic reactions:

skin rash, urticaria, skin hyperemia, nasal congestion, fever, arthralgia.
Local reactions:
with intravenous administration - thrombophlebitis (pain, redness, swelling).

Other:

candidiasis, neutropenia, leukopenia, flattening of the T wave on the ECG.

special instructions

It should be taken into account that during the period of use of the drug, ethanol is contraindicated, because a disulfiram-like reaction may develop (cramping abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).

During long-term therapy, blood counts should be monitored.

With leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process.

If neurological symptoms develop, you should stop using the drug.

When treating trichomonas vaginitis in women and trichomonas urethritis in men, it is necessary to abstain from sexual activity. Simultaneous treatment of sexual partners is mandatory. Treatment should be continued during menstruation. After completing treatment for trichomoniasis, control studies should be carried out during 3 consecutive cycles before and after menstruation.

After treatment for giardiasis is completed (if symptoms persist), 3 stool tests should be performed 3-4 weeks later at intervals of several days (in some successfully treated patients, lactose intolerance caused by infestation may persist for several weeks or months, resembling the symptoms of giardiasis).

The drug can immobilize treponemes and lead to a false-positive Nelson test.

It is not recommended to combine with non-depolarizing muscle relaxants (for example, vecuronium bromide).
Use in pediatrics
It is not recommended to use the drug in combination with amoxicillin in patients under 18 years of age

Storage conditions

List B. The drug should be stored in a place protected from light, out of reach of children at a temperature of 15° to 25°C.

Best before date

Shelf life – 2 years.
Conditions for dispensing from pharmacies
The drug is dispensed with a prescription.

Use during pregnancy and breastfeeding

Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.

The drug should be prescribed with caution in the second and third trimesters of pregnancy.

The drug is contraindicated for use in the first trimester of pregnancy and during breastfeeding.

Use for renal impairment

Restrictions for impaired renal function - With caution.

For patients with chronic renal failure (with CC less than 30 ml/min)

the maximum daily dose is 1 g.

Use for liver dysfunction

Restrictions for liver dysfunction - Contraindicated.

Contraindicated in case of liver failure (when using the drug in high doses);

Use in children

Restrictions for children - No restrictions.

IV drip for children over 12 years old

Children under 12 years of age

prescribed according to the same regimen in a single dose of 7.5 mg/kg.
For preventive purposes , children over 12 years of age
are prescribed 0.5-1 g drips on the eve of surgery, on the day of surgery and the next day - 1.5 g / day (500 mg every 8 hours). After 1-2 days, they switch to maintenance therapy orally.