Трихопол®

General characteristics. Structure:

Active ingredient: 5 mg metronidazole.

Excipients: sodium hydrophosphate, citric acid monohydrate, sodium chloride, water for injections.

Is effective anti-protozoan and antibacterial agent of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Metronidazole 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 metronidazole (aerobes and anaerobe bacterias) metronidazole works synergy with antibiotics, effective against usual aerobes.

The mechanism of effect of metronidazole 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 of metronidazole 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, medullispinal liquid, 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.

Removal of metronidazole 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 the metronidazole kumulirovaniye 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:

Metronidazole, solution for infusions, is shown 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;
• 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:

Intravenously. Intravenous administration of metronidazole 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 metronidazole is entered by 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 12 years metronidazole are more senior 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.

Aged up to 12 years administration of metronidazole intravenously kapelno according to the same scheme in a single dose of 7,5 mg/kg of body weight is recommended to children. The maximum daily dose at children aged up to 12 years – 22,5 mg/kg of body weight.

For patients with the expressed renal failures (clearance of creatinine less than 30 ml/min.) and/or a liver the daily dose of metronidazole makes 1000 mg, frequency rate of introduction 2 times.

Metronidazole, solution for infusions, it is not recommended to mix with other medicines!

Features of use:

With care appoint at diseases of kidneys, a liver.

During treatment ethanol reception is contraindicated (possibly development of disulfiramopodobny reactions: abdominal pain of spastic character, nausea, vomiting, a headache, sudden rush of blood to the person).

It is desirable to carry out long administration of drug under control of indicators of peripheral blood.

At a leukopenia the possibility of continuation of treatment depends on risk of development of infectious process.

Emergence of an ataxy, dizziness and any other deterioration in the neurologic status of patients demands the treatment termination.

Can immobilize treponemas and lead to the false positive test of Nelson. During reception of metronidazole red-brown coloring of urine can be observed.

Use during pregnancy and feeding by a breast. Metronidazole gets through a placenta therefore it is not necessary to appoint drug in the first trimester of pregnancy, further it is necessary to apply only if the potential advantage of use of drug for mother, exceeds possible risk for a fruit.

As metronidazole gets into breast milk, reaching in it the concentration close to concentration in a blood plasma, it is recommended to stop breastfeeding during treatment by drug.

Side effects:

From digestive tract: epigastric pains, nausea, vomiting, diarrhea, locks, intestinal colic, a loss of appetite, anorexia, taste disturbance, unpleasant "metal" smack in a mouth, dryness in a mouth, a glossitis, stomatitis; very seldom — an aberration of results of tests for a functional condition of a liver, cholestatic hepatitis, jaundice, pancreatitis.

From the central nervous system: at prolonged use — a headache, dizziness, an incoordination of movements, an ataxy, peripheral neuropathy, a hyperexcitability, irritability, a depression, a sleep disorder, drowsiness, weakness; in some cases — confusion of consciousness, a hallucination, spasm; very seldom — encephalopathy.

From urinogenital system: a dysuria, cystitis, a polyuria, an urine incontience, vulvovaginal candidiasis, a colpodynia, coloring of urine in red-brown color.

Allergic reactions: skin rash, itch, small tortoiseshell, mnogoformny exudative erythema, nose congestion, fever.

From the musculoskeletal device: mialgiya, arthralgias.

From the hemopoietic system: leukopenia; seldom — an agranulocytosis, a neutropenia, thrombocytopenia, a pancytopenia.

Local reactions: thrombophlebitis (pain, a hyperemia or puffiness in the place of an injection).
Others: flattening of a tooth of T on an ECG; extremely seldom — ototoxicity; pustulous rashes; gynecomastia.

Interaction with other medicines:

At use of metronidazole, solution for infusions, interaction with other medicines slightly, 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 (Esperal). Simultaneous use can lead to development of various neurologic symptoms therefore it is not necessary to appoint metronidazole sick which accepted Disulfiramum within the last two weeks. Similar to Disulfiramum causes intolerance of ethanol.
- 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 metronidazole elimination therefore its concentration in plasma goes down.

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

Antimicrobic effect of metronidazole amplifies in a combination with streptocides and antibiotics.

At the combined reception of metronidazole and cyclosporine increase in concentration of cyclosporine in a blood plasma can be observed.

Metronidazole reduces clearance of a ftoruratsil that can cause increase in toxicity of the last.

At simultaneous use metronidazole can increase plasma concentration of a bisulfan.

It is not recommended to combine with not depolarizing muscle relaxants (a vekuroniya bromide).

Contraindications:

• Hypersensitivity to metronidazole or other nitroimidazolny derivatives;
• organic lesions of the central nervous system (including epilepsy);
• leukopenia (including in the anamnesis);
• liver failure (in case of purpose of high doses);
• I trimester of pregnancy;
• lactation period.

With care:

• Pregnancy II and III trimesters (only according to vital indications);
• renal and/or liver failure.

Overdose:

Too high doses can become the reason of strengthening of side effects, mainly, of nausea, vomitings and dizzinesses; in more hard cases the ataxy, paresthesias and spasms can be noted.

Symptomatic treatment. The specific antidote is absent.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Not to use after the expiry date specified on packaging. Period of validity: ampoules  — 3 years, bottles  — 2 years.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions of 5 mg/ml. On 20 ml in ampoules of colourless hydrolytic glass I of a class. On 10 ampoules together with the Application instruction place in a cardboard pack. On 100 ml in bottles from polyethylene of high pressure with a tip for infusional set. On 1 bottle together with the Application instruction place in a cardboard pack.