Metrogil

General characteristics. Structure:

Active agent: metronidazole (5 mg / 1мл);

excipients: sodium chloride, citric acid, sodium phosphate double-base anhydrous, water for injections.

Pharmacological properties:

Metrogil is effective anti-protozoan and antibacterial agent of a broad spectrum of activity. Drug shows high activity concerning Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica, Lamblia intestinalis, and also concerning strict anaerobes (sporo-and asporous) - Bacteroides spp. (B.fragilis, B.ovatus, B.distasonis, B.thetaiotaomicron, B.vulgatus), Fusobacterium spp., Clostridium spp., Peptostreptococcus spp., Peptococcus spp., sensitive strains of Eubacterium. 

  Aerobic microorganisms and facultative anaerobes, but in the presence of the mixed flora are not sensitive to Metrogil (aerobes and anaerobe bacterias) metronidazole works synergy with antibiotics, effective against usual aerobes. 

Pharmacodynamics. The mechanism of action of Metrogil consists in biochemical recovery 5 nitrogroups of metronidazole intracellular transport proteins of anaerobic microorganisms and protozoa. The recovered 5 nitrogroup of metronidazole interacts with DNA of a cell of microorganisms, inhibiting synthesis of their nucleic acids that leads to death of bacteria. 

Pharmacokinetics. At intravenous administration of 500 mg Metrogila within 20 minutes by the patient with a mephitic gangrene concentration of drug in blood serum made in an hour 35,2 mkg/ml, in 4 hours - 33,9 mkg/ml, in 8 hours – 25,7 mkg/ml. Drug has high penetration, reaching bactericidal concentration in the majority of fabrics and liquids of an organism, including lungs, kidneys, a liver, skin, cerebrospinal fluid, a brain, bile, saliva, amniotic liquid, cavities of abscesses, a vaginal secret, semen, breast milk. Linkng with blood proteins weak also does not exceed 10 - 20%. At a normal bile production concentration of metronidazole in bile after intravenous administration can exceed considerably concentration of metronidazole in a blood plasma. 

Metrogil's removal is carried out by kidneys - 63% of a dose, 20% of drug are removed in not changed look. The elimination half-life of metronidazole makes 6-7 hours. The renal clearance makes 10,2 ml/min. 

At patients with a renal failure after repeated administration of drug accumulation of metronidazole in blood serum can be observed. Therefore at patients with a heavy renal failure the frequency of reception of metronidazole should be reduced. 

Indications to use:

Metrogil for injections is recommended for treatment of the infections caused by microorganisms, sensitive to drug: 

- prevention and treatment of mephitic gangrenes at surgical interventions, mainly on  abdominal organs and urinary tract; 

- a combination therapy of the heavy mixed aerobic-anaerobic infections; 

- severe form of an intestinal and hepatic amebiasis; 

- sepsis; 

- peritonitis; 

- osteomyelitis; 

- gynecologic infections; 

- abscesses of a small pelvis and brain; 

- the abscessing pneumonia; 

- gas gangrene; 

- infections of skin and soft tissues; bones and joints. 

Route of administration and doses:

Intravenous administration of Metrogil is shown at the heavy course of infections, and also in the absence of a possibility of administration of drug inside. 

For adults and children 12 years a single dose are more senior makes 500 mg, the speed of intravenous continuous (jet) or drop administration – 5 ml a minute. An interval between introductions - 8 hours. Duration of a course of treatment is defined individually. The maximum daily dose - no more than 4 g. According to indications, depending on the nature of an infection, carry out transition to a maintenance therapy peroral forms of metronidazole. 

To children aged up to 12 years Metrogil enter 7,5 mg/kg of body weight into 3 receptions with a speed of 5 ml a minute. 

For prevention of a mephitic gangrene before planned operation on pelvic bodies and urinary tract to adults and children Metrogil is more senior than 12 years appoint in the form of infusions in a dose 500-1000 mg, in day of operation and next day - in a dose of 1500 mg/days (on 500 mg each 8 hours). In 1-2 days usually pass to a maintenance therapy with peroral forms of metronidazole. 

For patients with the expressed renal failures (KK less than 30 ml/min.) and/or a liver a daily dose of metronidazole of 1000 mg; (frequency rate of reception 2 times). 

Metrogil for intravenous injections is not recommended to mix with other medicines! 

Features of use:

With care appoint at diseases of kidneys, a liver. During administration of drug it is impossible to take alcohol as Metrogil has ability to cause disgust for alcoholic drinks. It is desirable to carry out long administration of drug under control of indicators of peripheral blood. 

Side effects:

From digestive tract: nausea, vomiting, diarrhea, lack of appetite, unpleasant metal smack in a mouth, epigastric pains; from the central nervous system: at prolonged use - a headache, dizziness, a hyperexcitability, depressions, a sleep disorder, weakness; in some cases – confusion of consciousness, a hallucination, spasm; from urinogenital system: a burning sensation in an urethra, overdevelopment of fungal flora of a vagina (candidiases); dermatological reactions: allergic reactions (skin rash, itch, small tortoiseshell); from skeletal systems: arthralgias; from the hemopoietic system: leukopenia. During Metrogil's reception it can be observed red-brown coloring of urine. 

Interaction with other medicines:

At Metrogil's use for injections interaction with other medicines is insignificant, however it is necessary to be careful at co-administration with some medicines: 

Warfarin and other indirect anticoagulants. Metronidazole strengthens effect of indirect anticoagulants that leads to increase in time of formation of a prothrombin. 

Disulfiramum (эспераль). Simultaneous use can lead to development of various neurologic symptoms therefore  it is not necessary to appoint Metrogil sick which accepted Disulfiramum within the last two weeks. 

Cimetidinum inhibits metronidazole metabolism that can lead to increase in its concentration in blood serum and to increase  in risk of development   of by-effects. 

 Co-administration of the drugs stimulating enzymes of a microsomal oxidation in a liver (phenobarbital, Phenytoinum) can accelerate Metrogil's elimination therefore its concentration in plasma goes down. 

At patients, it is long receiving treatment by lithium drugs in high doses, at Metrogil's reception increase in concentration of lithium in a blood plasma and development of symptoms of intoxication is possible. 

Antimicrobic action of Metrogil amplifies in a combination with streptocides and antibiotics. 

Metrogil for intravenous injections is not recommended to mix with other medicines! 

Contraindications:

- hypersensitivity to metronidazole or other nitroimidazolny derivatives; 

- organic lesions of TsNS; 

- blood diseases; 

- I trimester of pregnancy, 

- II and III trimesters of pregnancy - only according to vital indications; to nursing mothers - according to indications, with the simultaneous termination of breastfeeding. 

Overdose:

At administration of drug in high doses spasms and peripheral neuropathy were observed. In such cases it is necessary to carry out symptomatic therapy. Metronidazole is removed from an organism by a hemodialysis.

Storage conditions:

To store at the room temperature in the place, unavailable to children. Not to freeze. To protect from light. 

Issue conditions:

According to the recipe

Packaging:

One-time plastic bottles on 100 ml (5 mg/ml); glass ampoules on 20 ml (5mg/ml)