Metronidazole-AKOS - Instructions For Use, Price, Solution, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Metronidazole-AKOS

Metronidazole-AKOS: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Metronidazole-AKOS

ATX code: J01XD01

Active ingredient: metronidazole (Metronidazole)

Producer: Sintez, JSC (Russia)

Description and photo updated: 30.11.2018

Prices in pharmacies: from 24 rubles.

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Metronidazole-AKOS is a drug with antiprotozoal, antimicrobial action.

Release form and composition

Dosage forms of Metronidazole-AKOS:

• concentrate for preparation of solution for infusion: transparent liquid with a greenish tint (100 ml in a vial / bottle, in a cardboard box of 1 or 35 vials / bottles; 20 ml in a bottle, in a cardboard box of 5 or 10 bottles);
• solution for infusion 0.5%: transparent, with a greenish tint (20 ml in dark glass vials, in a cardboard box 5 or 10 bottles; 100 ml in bottles / vials, in a cardboard box 1 bottle / bottle);
• tablets: white or white with a yellowish-greenish tinge, flat-cylindrical shape, with a chamfer and a score (10 tablets in a blister / cell-free package, in a cardboard box 1 or 2 packages).

Each pack also contains instructions for the use of Metronidazole-AKOS.

Composition of 1 ml of infusion solution:

• active substance: metronidazole - 5 mg;
• auxiliary components: disodium salt of ethylenediaminetetraacetic acid, water for injection.

Composition of 1 tablet:

• active substance: metronidazole - 250 mg;
• auxiliary components: potato starch, methylcellulose, milk sugar, stearic acid, low molecular weight polyvinylpyrrolidone.

Pharmacological properties

Pharmacodynamics

Metronidazole - the active substance of the drug, is a derivative of 5-nitroimidazole. Its mechanism of action is based on the biochemical reduction of the 5-nitro group by intracellular transport proteins of protozoa and anaerobic microorganisms. After reduction, the 5-nitro group interacts with the DNA of microbial cells against the background of inhibition of the synthesis of their nucleic acids, which leads to the death of bacteria.

Metronidazole is active against Entamoeba histolytica, Lamblia spp., Giardia lamblia intestinalis, Gardnerella vaginalis, Trichomonas vaginalis, as well as the obligate anaerobes Bacteroides spp. (including B. thetaiotaomicron, B. fragilis, B. ovatus, B. distasonis, B. vulgatus), Veillonella spp., Fusobacterium spp., Prevotella (P. buccae, P. bivia, P. disiens) and some gram-positive anaerobic microorganisms (Peptococcus spp., Clostridium spp., Eubacterium spp., Peptostreptococcus spp.). The MIC (minimum plasma concentration) for these strains is in the range from 0.125 to 6.25 μg / ml.

When used simultaneously with amoxicillin, metronidazole is active against Helicobacter pylori (due to the suppression of the development of resistance to metronidazole with amoxicillin).

Aerobic microorganisms and some anaerobes are insensitive to the action of metronidazole, but in a mixed flora (a combination of aerobes and anaerobes), metronidazole exhibits synergism with antibiotics, which are effective against conventional aerobes.

Due to the use of Metronidazole-AKOS, the sensitivity of tumors to radiation increases, sensitization to alcohol develops (disulfiram-like action), and reparative processes are stimulated.

Pharmacokinetics

Metronidazole has a high absorption, oral bioavailability ≥ 80%. The substance has a significant penetrating ability and reaches bactericidal concentrations in most body fluids and tissues, including in the lungs, liver, kidneys, skin, cerebrospinal fluid, brain, saliva, bile, abscess cavity, amniotic fluid, semen, vaginal secretions, breast milk.

Metronidazole crosses the blood-brain and placental barrier. Vd (volume of distribution) is: adults - approximately 0.55 l / kg, newborns - 0.54-0.81 l / kg. C _max (maximum concentration) when taken orally is reached in 1-3 hours and, depending on the dose received, is 6-40 μg / ml.

With intravenous administration of 500 mg of metronidazole (over 20 minutes), the following values of C _max in serum are achieved (after a specified time interval after administration): 60 minutes - 35.2 μg / ml; 4 hours - 33.9 μg / ml; 8 hours - 25.7 μg / ml. With subsequent injections, C _min (minimum concentration of the substance) is 18 μg / ml. The time to reach C _max is in the range from 30 to 60 minutes, the therapeutic concentration is maintained for 6-8 hours. After intravenous administration, the concentration of metronidazole in bile in the absence of bile formation disorders can significantly exceed the value of this indicator in plasma.

The level of binding of metronidazole to plasma proteins is from 10 to 20%.

Approximately 30-60% of metronidazole is metabolized, the process is carried out by hydroxylation, oxidation and glucuronidation. 2-oxymetronidazole - the main metabolite of metronidazole, also has antimicrobial and antiprotozoal effects.

T _1/2 (half-life) in the absence of hepatic dysfunction is in the range of 6-12 hours (average 8 hours), in patients with alcoholic liver damage - 10-29 hours (average 18 hours). The value of this indicator in newborns (depending on the duration of pregnancy): 28-30 weeks: 75 hours; 32–35 weeks: 35 hours; Weeks 36-40: 25 hours.

60-80% of metronidazole is excreted by the kidneys (unchanged - 20%), through the intestines - from 6 to 15%. Renal clearance is 10.2 ml / min. In case of impaired renal function, after repeated administration of the substance, accumulation of metronidazole in the blood serum may occur. In this regard, in patients with severe renal failure, the frequency of use of Metronidazole-AKOS should be reduced.

During hemodialysis, metronidazole and its main metabolites are rapidly removed from the blood (T _1/2 decreases to 2.6 hours). During peritoneal dialysis, a small amount of the substance is excreted.

Indications for use

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

Contraindications

Absolute:

• hepatic failure (with the appointment of Metronidazole-AKOS in large doses);
• organic lesions of the central nervous system (including epilepsy);
• leukopenia (including a burdened history);
• I trimester of pregnancy and lactation;
• individual intolerance to the components of the drug.

Relative (Metronidazole-AKOS is prescribed under medical supervision):

• renal and / or hepatic impairment;
• II – III trimesters of pregnancy.

Metronidazole-AKOS, instructions for use: method and dosage

When administered intravenously for adults and children from 12 years old, the initial dose of Metronidazole-AKOS is 500-1000 mg, the drug is administered by drip (duration of infusion is from 30 to 40 minutes). In the future, therapy is continued with the introduction of 500 mg every 8 hours at a rate of 5 ml / min.

After the first 2-3 infusions, with good tolerance, the patient is transferred to jet injection. The duration of the course is 7 days, according to the indications, the treatment may be longer.

The maximum daily dose is 4000 mg. According to indications, it is possible to switch to a maintenance oral administration - 3 times a day, 400 mg. For children under 12 years old, Metronidazole-AKOS is prescribed according to the same scheme at the rate of a single dose of 7.5 mg / kg.

In the treatment of purulent-septic diseases, one course of therapy is performed.

For the purpose of prophylaxis, on the eve of the operation, adults and children from 12 years old are injected intravenously with 500–1000 mg, on the day of the operation and the next day, the drug is prescribed in a daily dose of 1500 mg (500 mg every 8 hours). After 1–2 days, the patient is transferred to oral maintenance therapy. Patients with hepatic impairment and / or chronic renal failure and creatinine clearance less than 30 ml / min Metronidazole-AKOS should be administered in a dose of not more than 1000 mg per day, the frequency of use is 2 times a day.

As a radiosensitizing agent, the drug is injected intravenously. The dose is calculated on the basis of 160 mg / kg or 4-6 g / m ² 30-60 minutes before the start of irradiation. Metronidazole-AKOS is applied before each radiation session for 7-14 days. During the remaining period of radiation therapy, metronidazole is not prescribed.

A single dose should not exceed 10,000 mg, course dose - 60,000 mg. To remove radiation-induced intoxication, a 5% dextrose solution, hemodez or 0.9% sodium chloride solution is injected drip.

Metronidazole-AKOS in the form of tablets is taken orally, without chewing, during meals or after meals (or with milk).

In the treatment of trichomoniasis, Metronidazole-AKOS is prescribed 2 times a day, 250 mg for 10 days or 400 mg for 5–8 days. Women should additionally use metronidazole in the form of vaginal tablets or suppositories. The course of treatment, if necessary, is repeated or the dose is increased to 750-1000 mg per day. Between courses take a break 3-4 weeks with repeated control laboratory tests. Alternatively, a single dose of 2000 mg is possible for both the patient and his sexual partner.

For children, Metronidazole-AKOS is prescribed depending on age (daily dose): 2–5 years - 250 mg; 5-10 years - 250-375 mg; from 10 years - 500 mg. The daily dose is divided into 2 doses. The duration of the course is 10 days.

Method of using the drug for other indications:

• giardiasis: adults: 2 times a day, 500 mg for 5-7 days; children (daily dose in 2 doses): up to 1 year old - 125 mg each, 2-4 years old - 250 mg each, 5-8 years old - 375 mg each, from 8 years old - 500 mg each; course of admission - 5 days;
• giardiasis (giardiasis): 5 mg / kg 3 times a day for 5 days;
• asymptomatic amebiasis (in adult patients with an identified cyst): 2–3 times a day, 500 mg for 5–7 days;
• chronic amebiasis: 3 times a day, 500 mg for 5-10 days;
• acute amoebic dysentery: 2250 mg in 3 divided doses, Metronidazole-AKOS is taken until symptoms stop;
• liver abscess: 2500 mg per day (maximum) in 1 or 2-3 doses for a course of 3-5 days, therapy is carried out in combination with antibiotics (tetracyclines) and other methods of treatment; children 1–3 years old are prescribed 1/4 of the adult dose, 3–7 and 7–10 years old - 1/3 and 1/2 of the adult dose, respectively;
• balantidiasis: 750 mg 3 times a day for 5–6 days;
• ulcerative stomatitis (adults, children are not prescribed the drug for this indication): 2 times a day, 500 mg for a course of 3-5 days;
• pseudomembranous colitis: 3-4 times a day, 500 mg;
• diseases associated with Helicobacter pylori: 3 times a day, 500 mg for a course of 7 days (simultaneously with other drugs, for example, with amoxicillin in a daily dose of 2250 mg);
• anaerobic infections: Metronidazole-AKOS is taken in a dose not exceeding 1500-2000 mg;
• chronic alcoholism: 500 mg per day, the duration of the course should not exceed 6 months;
• infectious complications (prevention): 3-4 days before the operation in a daily dose of 750-1500 mg in 3 divided doses or once on the first day after the operation in a dose of 1000 mg; 1-2 days after the intervention (when the patient is allowed oral administration) Metronidazole-AKOS is prescribed in a daily dose of 750 mg for 7 days.

Against the background of severe renal dysfunction (in patients with creatinine clearance less than 10 ml / min), the daily dose should be halved.

In the treatment of cervical and uterine body cancer, skin cancer, Metronidazole-AKOS can be applied topically in the form of applications before irradiation 1.5–2 hours before the procedure. In a 10% solution of dimethyl sulfoxide, 3000 mg of the drug should be dissolved, after which it will moisten the tampons in the prepared solution. In case of poor tumor regression, applications are prescribed for the entire course of radiation therapy. If there is a positive dynamics of cleansing the tumor from necrosis, Metronidazole-AKOS is used during the first 14 days of treatment.

Side effects

• digestive system: a feeling of a metallic taste in the mouth, constipation, diarrhea, anorexia, vomiting, nausea, intestinal colic, xerostomia, glossitis, stomatitis, pancreatitis;
• genitourinary system: urine staining red-brown, urinary incontinence, candidiasis, dysuria, polyuria, cystitis;
• nervous system: confusion, weakness, headache, insomnia, ataxia, peripheral neuropathy, dizziness, irritability, irritability, depression, impaired coordination of movements, convulsions, hallucinations;
• local reactions (with intravenous administration): thrombophlebitis in the form of pain, swelling or redness at the injection site;
• allergic reactions: nasal congestion, arthralgia, skin flushing, fever, urticaria, skin rash;
• others: leukopenia, neutropenia, flattening of the T wave on the electrocardiogram (ECG).

Overdose

There is no information on Metronidazole-AKOS overdose.

Therapy: metronidazole and its main metabolites can be quickly removed by hemodialysis (T _{1/2 is} reduced to 2.6 hours). With peritoneal dialysis, the drug is excreted in a small amount.

special instructions

During the treatment with Metronidazole-AKOS, ethanol intake is contraindicated, which is associated with a high probability of developing a disulfiram-like reaction, manifested in the form of spastic abdominal pain, vomiting, nausea, sudden flushes of blood to the face, and headache.

When carrying out long-term treatment, monitoring of the blood picture is required.

In case of development of leukopenia, the possibility of further treatment is determined by the degree of risk of an infectious process.

Cancellation of therapy is indicated when the following symptoms appear: ataxia, dizziness, and any other deterioration in neurological status.

It should be borne in mind that the use of Metronidazole-AKOS can immobilize treponemas and cause a false positive Nelson test result.

Metronidazole stains the urine dark.

During the treatment of Trichomonas vaginitis and Trichomonas urethritis (in women and men, respectively), one should refrain from sexual intercourse. Simultaneous treatment of sexual partners is mandatory. At the time of menstruation, therapy is not interrupted. After the end of the course of treatment for trichomoniasis, control tests are shown for three successive cycles before and after menstruation.

After completing the treatment of giardiasis, if the symptoms persist, the patient is prescribed three stool tests after 3-4 weeks at intervals of several days (in some cases, after successful treatment, patients notice symptoms resembling giardiasis for several weeks or months, although these signs are associated with intolerance caused by invasion lactose).

Application during pregnancy and lactation

• I trimester of pregnancy, breastfeeding period: Metronidazole-AKOS is not prescribed;
• II – III trimesters of pregnancy: therapy should be carried out under medical supervision.

Pediatric use

In pediatric practice, the drug is used according to indications in compliance with the dosage regimen prescribed by a specialist.

It is not recommended to use Metronidazole-AKOS in combination with amoxicillin in patients under 18 years of age.

With impaired renal function

In chronic renal failure and creatinine clearance less than 30 ml / min, Metronidazole-AKOS should be administered in a dose of not more than 1000 mg per day, the frequency of use is 2 times a day.

In patients with impaired renal function, therapy should be carried out with caution.

For violations of liver function

Metronidazole-AKOS is contraindicated in high doses for liver failure.

In patients with impaired liver function, therapy should be carried out with caution.

Drug interactions

The solution of Metronidazole-AKOS for intravenous administration is not recommended to be mixed with other drugs.

Possible interactions of metronidazole in case of joint use with other drugs / substances:

• indirect anticoagulants: their action is enhanced, as a result of which the time of prothrombin formation increases;
• disulfiram: the appearance of various neurological symptoms is possible, one should refrain from simultaneous use, maintaining a break between courses of at least 14 days;
• ethanol: as with the use of disulfiram, ethanol intolerance develops;
• cimetidine: inhibition of metronidazole metabolism occurs, which can cause an increase in its serum concentration in the blood and an increase in the likelihood of adverse reactions;
• lithium preparations: combined use leads to an increase in their plasma concentration and the development of signs of intoxication;
• drugs that stimulate enzymes of microsomal oxidation in the liver (phenytoin, phenobarbital): it is possible to accelerate the elimination of metronidazole and, as a result, to decrease its plasma concentration;
• sulfonamides: there is an increase in the antimicrobial effect of metronidazole;
• non-depolarizing muscle relaxants (vecuronium bromide): combination therapy is not recommended.

Analogs

Analogs of Metronidazole-AKOS are Batsimex, Metrogyl, Metronidazole, Metrovagin, Klion, Metroxan, Trichopol, Flagil, Deflamon, Rozex, Efloran, Rosamet, Orvagil.

Terms and conditions of storage

Store in a place protected from light and moisture at a temperature of 15-25 ° C. Keep out of the reach of children.

Shelf life: tablets - 2 years; infusion solution - 4 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Metronidazole-AKOS

The few reviews about Metronidazole-AKOS relate mainly to the drug in the form of an infusion solution, which is used mainly free of charge in a hospital setting. Most often, the high efficacy of the drug is noted, but at the same time its poor tolerance, which can vary from digestive disorders to mental disorders.

Price for Metronidazole-AKOS in pharmacies

The approximate price for Metronidazole-AKOS solution for infusion 5 mg / ml, 1 bottle (bottle) 100 ml is 25–30 rubles.

Metronidazole-AKOS: prices in online pharmacies

Drug name Price Pharmacy

Metronidazole-AKOS 5 mg / ml solution for infusion 100 ml 1 pc. RUB 24 Buy

Metronidazole-AKOS solution for inf. 5mg / ml 100ml fl. RUB 26 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!