Metronidazole

General characteristics. Structure:

Active agent: metronidazole of 250 mg.

Pharmacological properties:

Antiprotozoan means. Believe that the mechanism of action is connected with disturbance of structure of DNA of sensitive microorganisms. Gardnerella vaginalis, Giardia lamblia, Entamoeba histolytica, and also obligate anaerobic bacteria is active concerning Trichomonas vaginalis (including Bacteroides spp., Fusobacterium spp.).
Aerobic microorganisms are steady against metronidazole.
In a combination with amoxicillin shows activity concerning Helicobacter pylori. Believe that amoxicillin inhibits development of resistance of Helicobacter pylori to metronidazole.

Pharmacokinetics. It is well soaked up after intake. Bioavailability makes 80%. It is distributed in fabrics and liquids of an organism. Gets through a placental barrier and GEB. Linkng with proteins of a blood plasma - 20%. It is metabolized in a liver by oxidation and linkng with glucuronic acid. T1/2 makes 8 h. It is removed with urine (60-80%) and a stake (6-15%).

Indications to use:

Mecotic vaginitis and urethritis at women, a mecotic urethritis at men, the lambliasis, amoebic dysentery, mephitic gangrenes caused by microorganisms, sensitive to metronidazole, a combination therapy of the heavy mixed aerobic-anaerobic infections. Prevention of a mephitic gangrene at surgical interventions (especially on abdominal organs, urinary tract). Alcoholism.
In a combination with amoxicillin: chronic gastritis in an aggravation phase, a peptic ulcer of a stomach and duodenum in an aggravation phase, associated with Helicobacter pylori.
For external and topical administration: treatment of pink and vulgar eels, bacterial vaginoses, treatment is long not healing wounds, trophic ulcers.

Route of administration and doses:

Inside to adults and children 12 years - on 7.5 mg/kg each 6 h or on 250-750 mg of 3-4 times/days are more senior. To children up to 12 years - on 5-16.7 mg/kg of 3 times/days.
At in introduction by the adult and to children 12 years an initial dose are more senior makes 15 mg/kg, then 7.5 mg/kg each 6 h or depending on a disease etiology - on 500-750 mg each 8 h. Duration of courses of treatment and frequency of their carrying out is defined individually.
Intravaginalno - on 500 mg of 1 times for the night.
In a combination with amoxicillin (2.25 g/days) a daily dose of metronidazole - 1.5 g; frequency rate of reception - 3 times/days. For patients with the expressed renal failures (KK less than 30 ml/min.) and/or a liver a daily dose of metronidazole - 1 g (amoxicillin - 1.5 g/days); frequency rate of reception - 2 raznut.
Outwardly and locally apply 2 times/days, establish a dose individually.
The maximum daily dose for adults at intake and in introduction makes 4 g.

Features of use:

With care apply metronidazole at liver diseases.
In a combination with amoxicillin do not recommend to apply at patients more young than 18 years. In the course of treatment systematic control of a picture of peripheral blood is necessary.
During treatment of a mecotic vaginitis at women and a mecotic urethritis at men it is recommended to abstain from sex life; simultaneous treatment of both partners is obligatory.
During use of metronidazole more dark coloring of urine is observed.
During treatment by metronidazole it is necessary to avoid alcohol intake since owing to disturbance of oxidation of alcohol there can be an acetic aldehyde accumulation. As a result the reactions similar to those which are characteristic of Disulfiramum can develop (spastic abdominal pains, nausea, vomiting, a headache, sudden rush of blood to the person).

Side effects:

- From the alimentary system: nausea, vomiting, lack of appetite, metal smack in a mouth.
- From TsNS and a peripheral nervous system: headache, hypererethism, irritability, sleeplessness, dizziness, ataxy, weakness, confusion of consciousness, depression, peripheral neuropathy, spasms, hallucinations.
- Allergic reactions: skin rash, itch, small tortoiseshell.
- From system of a hemopoiesis: leukopenia.
- Local reactions: irritation.
- Other: an arthralgia, a burning sensation in an urethra.

Interaction with other medicines:

At simultaneous use with the antacids containing aluminum hydroxide with Colestyraminum absorption of metronidazole from a GIT decreases a little.

At simultaneous use metronidazole exponentiates effect of indirect anticoagulants.

At simultaneous use with Disulfiramum development of acute psychoses and disturbance of consciousness is possible.

It is impossible to exclude increase in concentration of carbamazepine in a blood plasma and increase in risk of development of toxic action at simultaneous use with metronidazole.

At simultaneous use with lansoprazoly the glossitis, stomatitis and/or emergence of dark coloring of language are possible; from lithium a carbonate - increase in concentration of lithium in a blood plasma and development of symptoms of intoxication is possible; with Prednisonum - removal of metronidazole from an organism owing to acceleration of his metabolism in a liver under the influence of Prednisonum increases. Reduction of efficiency of metronidazole is possible.

At simultaneous use with rifampicin the clearance of metronidazole from an organism increases; with Phenytoinum - perhaps small increase in concentration of Phenytoinum in a blood plasma, the case of development of toxic action is described.

At simultaneous use with phenobarbital removal of metronidazole from an organism, apparently, owing to acceleration of his metabolism in a liver under the influence of phenobarbital significantly increases. Reduction of efficiency of metronidazole is possible.

At simultaneous use with ftoruratsily toxic action amplifies, but not efficiency ftoruratsit.

The case of development of acute dystonia after reception of a single dose of chloroquine at the patient receiving metronidazole is described.

At simultaneous use with Cimetidinum the inhibition of metabolism of metronidazole in a liver is possible that can lead to delay of its removal and increase in concentration in a blood plasma.

At simultaneous use of ethanol for the patients receiving metronidazole development of disulfiramopodobny reactions is possible.

Contraindications:

Organic lesions of TsNS, disease of blood, abnormal liver function, the I trimester of pregnancy, hypersensitivity to metronidazole.

Use at pregnancy and feeding by a breast
Metronidazole quickly gets through a placental barrier. In II and III trimesters of pregnancy metronidazole is applied only according to vital indications.
Metronidazole is emitted with breast milk. In need of use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Use at abnormal liver functions
It is contraindicated at abnormal liver functions.
With care apply metronidazole at liver diseases.

Use for children
In a combination with amoxicillin do not recommend to apply at patients more young than 18 years.

Overdose:

There are no data.

Storage conditions:

To store drug in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 250 mg: 10 or 20 pieces.