Metronidazole-Acos, bottles 500mg, 100ml

Product description

Minimum order quantity-5 pieces

Composition

Active ingredients:

metronidazole 5 mg;

Auxiliary substances:

sodium chloride,

citric acid monohydrate,

sodium hydrophosphate,

water for injection

Pharmacological action

Metronidazole-Akos – antimicrobial, antiprotozoal.

A derivative of 5-nitroimidazole. The mechanism of action consists in 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.

Active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotamicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (P. bivia, P. buccae, P. disiens) and some gram-positive anaerobic microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp. ). The MPC for these strains is 0.125-6.25 mcg / ml.

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

Aerobic microorganisms and some anaerobes are insensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes), metronidazole acts synergistically with antibiotics that are effective against conventional aerobes.

Increases the sensitivity of tumors to radiation, causes sensitization to alcohol (disulfiram-like effect), and stimulates reparative processes.

Pharmacokinetics

Absorption is high, and oral bioavailability is at least 80%. It has a high penetration capacity, reaching bactericidal concentrations in most body tissues and fluids, including lungs, kidneys, liver, skin, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretions, seminal fluid, breast milk; passes through the BBB and placental barrier. The volume of distribution in adults is approximately 0.55 l / kg, in newborns-0.54-0.81 l / kg. Cmax with oral use is reached after 1-3 hours and ranges from 6 to 40 mcg / ml, depending on the dose. Binding to plasma proteins is 10-20%. With intravenous use of 500 mg for 20 minutes, Cmax in serum after 1 hour is 35.2 mcg / ml, after 4 hours-33.9 mcg/ml, after 8 hours-25.7 mcg/ml; Cmin with subsequent use is 18 mcg/ml. The time to reach Cmax is 30-60 minutes, the therapeutic concentration is maintained for 6-8 hours. With normal bile formation, the concentration of metronidazole in the bile after intravenous use may significantly exceed the concentration in plasma.

Approximately 30-60% of metronidazole is metabolized in the body by hydroxylation, oxidation, and glucuronidation. Main metabolite (2-oxymetronidazole) it also has an antiprotozoal and antimicrobial effect.

T1 / 2 in normal liver function — 8 hours (from 6 to 12 hours), in alcoholic liver damage — 18 hours (from 10 to 29 hours); in newborns born at a gestation period of 28-30 weeks — approximately 75 hours,32-35 weeks — 35 hours and 36-40 weeks — 25 hours, respectively. Excreted by the kidneys 60-80% (20% unchanged), through the intestines-6-15%. Renal clearance is 10.2 ml/min.

In patients with impaired renal function, accumulation of metronidazole in the blood serum may occur after repeated use (therefore, patients with severe renal insufficiency should reduce the frequency of use). Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T1 / 2 is reduced to 2.6 hours). During peritoneal dialysis, it is excreted in small amounts.

Indications

• Protozoal infections: extra-intestinal amoebiasis, including amoebic liver abscess, intestinal amoebiasis (amoebic dysentery), trichomoniasis, giardiasis, balantidiasis, giardiasis, cutaneous leishmaniasis, trichomonas vaginitis, trichomonas urethritis.
• Infections caused by Bacteroides spp. B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. vulgatus): bone and joint infections, CNS infections, including meningitis, brain abscess, bacterial endocarditis, pneumonia, empyema, and lung abscess.
• Infections caused by Bacteroides species, including the B. fragilis group, Clostridium, Peptococcus and Peptostreptococcus species: abdominal infections (peritonitis, liver abscess), pelvic infections (endometritis, endomyometritis, fallopian tube and ovarian abscess, vaginal vault infections after surgery), skin and soft tissue infections.
• Infections caused by Bacteroides species, including the B. fragilis group, and Clostridium species.
• Pseudomembranous colitis (associated with the use of antibiotics).
• Gastritis or duodenal ulcer associated with Helicobacter pylori, alcoholism.
• Prevention of postoperative complications (especially interventions on the colon, peri-rectal area, appendectomy, gynecological operations).
• Radiation therapy of patients with tumors — as a radiosensitizing agent in cases where tumor resistance is caused by hypoxia in tumor cells.

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy; with caution — in the second and third trimesters of pregnancy.

During lactation, it is recommended to stop breastfeeding.

Contraindications

Hypersensitivity, leukopenia (including in the anamnesis), organic lesions of the central nervous system (including epilepsy), liver failure (in the case of high doses), I trimester of pregnancy, breast-feeding.

With caution — in the second and third trimesters of pregnancy, renal / hepatic insufficiency.

Side effects

From the digestive system:  diarrhea, anorexia, nausea, vomiting, intestinal colic, constipation, metallic taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.

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

Allergic reactions:  urticaria, skin rash, hyperemia of the skin, nasal congestion, fever, arthralgia.

From the genitourinary system:  dysuria, cystitis, polyuria, urinary incontinence, candidiasis, urine staining in red-brown color.

Local reactions:  thrombophlebitis (pain, redness, or swelling at the injection site).

Other services:  neutropenia, leukopenia, flattening of the T wave on the ECG.

Interaction

Metronidazole for intravenous use is not recommended to be mixed with other drugs.

Increases the effect of indirect anticoagulants, which leads to an increase in the time of prothrombin formation.

Similarly to disulfiram, it causes an intolerance to ethanol. Concomitant use with disulfiram may lead to the development of various neurological symptoms (the interval between use is at least 2 weeks).

Cimetidine inhibits the metabolism of metronidazole, which can lead to an increase in its concentration in the blood serum and increase the risk of side effects.

Concomitant use of drugs that stimulate microsomal oxidation enzymes in the liver (phenobarbital, phenytoin) may accelerate the elimination of metronidazole, resulting in a decrease in its concentration in plasma.

When taken concomitantly with lithium preparations, the concentration of the latter in plasma may increase and symptoms of intoxication may develop.

It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).

Sulfonamides enhance the antimicrobial effect of metronidazole.

How to take, course of use and dosage

Intravenous

Adults and children over 12 years of age at an initial dose of 0.5-1 g IV drip (duration of infusions-30-40 minutes), then every 8 hours 500 mg at a rate of 5 ml / min. With good tolerability, after the first 2-3 infusions, they switch to jet use. The course of treatment is 7 days. If necessary, intravenous use is continued for a longer time. The maximum daily dose is 4 g. According to indications, they switch to maintenance oral use at a dose of 400 mg 3 times a day. Children under 12 years of age are prescribed according to the same scheme in a single dose of 7.5 mg / kg.

When purulent-septic diseases are carried out 1 course of treatment.

For prophylactic purposes, adults and children over 12 years of age are given intravenous drops of 0.5-1 g on the eve of surgery, on the day of surgery and the next day — 1.5 g per day(500 mg every 8 hours). After 1-2 days, they switch to maintenance therapy inside. In patients with chronic renal failure and creatinine clearance less than 30 ml / min and / or hepatic insufficiency, the maximum daily dose is not more than 1 g, the frequency of use is 2 times a day.

As a radiosensitizing agent, it is administered intravenously at the rate of 160 mg / kg or 4-6 g / m%^%2 0.5-1 h before the start of irradiation, used before each irradiation session for 1-2 weeks. During the remaining period of radiation treatment, metronidazole is not used.The maximum single dose is no more than 10 g, the course dose is 60 g. To relieve intoxication caused by radiation, apply a drip of 5% dextrose solution, hemodesis or 0.9% sodium chloride solution.

Special instructions

During the treatment period, taking ethanol is contraindicated (a disulfiram-like reaction may develop: spastic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).

With long-term therapy, it is necessary to monitor the blood picture.

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

The appearance of ataxia, dizziness and any other deterioration in the neurological status of patients requires discontinuation of treatment.

May immobilize treponemes and result in a false positive Nelson test result.

Stains urine in a dark color.

When treating trichomonas vaginitis in women and trichomonas urethritis in men, it is necessary to refrain from sexual contact. Simultaneous treatment of sexual partners is mandatory. Treatment does not stop during menstruation. After trichomoniasis therapy, follow-up tests should be performed for three consecutive cycles before and after menstruation.

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

Product form

solution for injection

Storage conditions

Store in a dry place, protected from light, at a temperature of 15-25 °C

Shelf life

2 years

Active ingredient

Metronidazole

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Stomach and Duodenal Ulcers, Skin Infections, Osteomyelitis, Gastrointestinal Infections caused by Helicobacter Pylori, Amoebiasis and Giardiasis, Pneumonia, Female genital inflammation, Vaginitis, Urinary Tract Infections, Urethritis, Trichomoniasis, Alcoholism