Metrogil 5mg / ml solution for intravenous injection of 100ml No. 1 bottle
Metrogil 5mg / ml solution for intravenous injection of 100ml No. 1 bottle
Pharmacological action - antibacterial, antiprotozoal (trichomonacid), anti-ulcer.
The drug exhibits high activity against Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica, Lamblia intestinalis, as well as with respect to obligate anaerobes (spore-and non-sporogenous) - Bacteroides spp. (B.fragilis, B.ovatus, B.distasonis, B.thetaiotaomicron, B.vulgatus), Fusobacterium spp., Clostridium spp., Peptostreptococcus spp., Peptococcus spp., Sensitive Eubacterium strains.
Aerobic microorganisms and facultative anaerobes are not sensitive to metronidazole, but in the presence of mixed flora (aerobic and anaerobic) metronidazole acts synergistically with antibiotics that are effective against conventional aerobes.
Pharmacodynamics.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 recovered 5-nitro group of metronidazole interacts with the microbial cell DNA, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.
Pharmacokinetics.Absorption. After intravenous administration in a dose of 500 mg for 20 minutes, Cmax in serum after 1 hour is 35.2 μg / ml, after 4 hours - 33.9 μg / ml, after 8 hours - 25.7 μg / ml; Cmin with the subsequent introduction - 18 mcg / ml. With the on / in the introduction of Cmax is reached after 30-60 minutes, the therapeutic concentration lasts for 6-8 hours. With normal bile formation, the concentration of metronidazole in the bile after the / in the introduction can significantly exceed the concentration in plasma.
Distribution. Binding to plasma proteins - 10-20%. Vd in adults - 0.55 l / kg, in newborns - 0.54-0.81 l / kg. Metronidazole has a high penetrating ability. Reaches bactericidal concentrations in the lungs, kidneys, liver, brain, skin, cerebrospinal fluid, bile, saliva, amniotic fluid, abscess cavity, vaginal secretions, seminal fluid, breast milk. It penetrates the BBB, passes through the placental barrier.
Metabolism. Metabolized (about 30-60%) by hydroxylation, oxidation and glucuronidation. The main metabolite - 2 oxymetronidazole - has antiprotozoal and antimicrobial action.
Inference. Excreted by the kidneys (60-80%), 20% - unchanged; 6–15% is excreted through the intestines. T1 / 2 - 8 h (6-12 h).Renal clearance - 10.2 ml / min.
Pharmacokinetics in special clinical situations. With alcoholic liver damage T1 / 2 is 18 hours (10-29 hours), for newborns born with a gestation period of 28-30 weeks - 75 hours, with a period of 32-35 weeks - 35 hours, with a period of 36-40 weeks - 25 h
In patients with impaired renal function, after repeated administration, cumulation of metronidazole in serum may be observed.
Indications for use• Protozoal infections: extraintestinal amebiasis, including amebic liver abscess, intestinal amebiasis, trichomoniasis, giardiasis, balantidiasis, giardiasis, trichomonas vaginitis, trichomonas urethritis;
• Infections caused by Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus): infections of bones and joints, CNS infections (including meningitis, brain abscess), bacterial endocarditis, pneumonia, emp, inactivating heart disease, pneumonia, epic, endocarditis, pneumonia; ;
• 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 vault in the body of the vault in the body of the body of the vagina, endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, infections of the vault in the body of the body of the vagina, endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, infections of the vault in the body of the vault in the body of the body of the body of the abdominal cavity (endometritis, endomyometritis, abscess of the fallopian tubes and ovaries; after surgery), skin and soft tissue infections;
• Sepsis caused by Bacteroides spp. (including Bacteroides fragilis) and Clostridium spp .;
• Prevention of postoperative complications (especially interventions on the colon, near-rectal area, appendectomy, gynecological surgery);
• Combined therapy of severe mixed aerobic-anaerobic infections.
Mode of applicationThe solution is administered intravenously, drip, at a rate of 5 ml per minute.
The solution can be introduced undiluted or diluted with 300-400 ml of saline.
Adults and children over 12 years with anaerobic infections - 500 mg every 8 hours for 7-10 days, in severe cases - 2-3 weeks. The maximum daily dose - 4 g.
For the prevention of anaerobic infections before planned surgery on the pelvic organs and urinary tract in adults and children over 12 years old, metronidazole is administered as an infusion in the dose of 500-1000 mg, on the day of surgery and the next day in a dose of 1500 mg / day (500 mg every 8 hours ). After 1-2 days, they usually switch to maintenance therapy with oral forms of metronidazole.
Children up to 12 years: 7.5 mg / kg body weight (1.5 ml / kg) every 8 hours at a rate of 5 ml per minute.
For patients with severe impaired renal function (CC less than 30 ml / min) and / or liver, the daily dose of metronidazole is up to 1000 mg; (multiplicity of reception 2 times).
Side effect• On the part of the gastrointestinal tract: nausea, vomiting, diarrhea, lack of appetite, unpleasant metallic taste in the mouth, epigastric pain, pancreatitis;
• From the side of the central nervous system: headache, dizziness, irritability, depression, sleep disturbance, weakness; in some cases - confusion, hallucinations, convulsions, ataxia, incoordination;
• From the peripheral nervous system: peripheral neuropathy;
• On the part of the urogenital system: dysuria, cystitis, polyuria, urinary incontinence, urine staining in red-brown color, burning sensation in the urethra;
• Excessive development of the fungal flora of the vagina and oral cavity (candidosis);
• Allergic reactions: skin rash, itching, urticaria, skin flushing, nasal congestion, fever, arthralgia;
• From the side of the hematopoietic system: transient leukopenia and thrombocytopenia; described the case of bone marrow aplasia.
Contraindications• Hypersensitivity to metronidazole or other nitroimidazole derivatives;
• Organic lesions of the central nervous system;
• Blood diseases (leukopenia, thrombocytopenia, anemia);
• Hepatic failure (when using the drug in high doses);
• I trimester of pregnancy
• Lactation (breastfeeding)
Pregnancy and lactation
Metronidazole is contraindicated for use in the first trimester of pregnancy. In the II and III trimesters of pregnancy, the drug is used only for health reasons.
Metronidazole is excreted in breast milk. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.
OverdoseSymptoms: nausea, vomiting, ataxia, in severe cases - peripheral neuropathy and seizures.
Treatment: symptomatic; specific antidote is absent.
Application featuresBe wary prescribed for diseases of the kidneys, liver, central and peripheral nervous system.
While taking the drug should not be consumed alcohol, as metronidazole has the ability to cause aversion to alcohol. Long-term use of the drug should be under the control of peripheral blood
Interaction with other drugs
Metronidazol for intravenous infusion is not recommended to be mixed with other drugs.
When applying metronidazole, caution should be exercised while the appointment with some drugs:
Warfarin and other indirect anticoagulants. Metronidazole enhances the effect of indirect anticoagulants, which leads to an increase in the time of formation of prothrombin.
Disulfiram (esperal). Simultaneous use can lead to the development of various neurological symptoms, so metronidazole should not be prescribed to patients who have taken disulfiram in the last two weeks.
Cimetidine inhibits the metabolism of metronidazole, which can lead to an increase in its concentration in serum and an increase in the risk of side effects.
The simultaneous administration of drugs that stimulate the enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin) can accelerate the elimination of metronidazole, as a result of which its concentration in plasma decreases.
In patients receiving long-term treatment with lithium preparations in high doses, when taking metronidazole, it is possible to increase the concentration of lithium in the blood plasma and develop intoxication symptoms.
The antimicrobial effect of tetronidazole is enhanced in combination with sulfonamides and antibiotics.
Storage conditionsIn a dry, dark place at a temperature not higher than + 25 ° C.
It is a drug. Consultation with a doctor is required.