Clion - instructions for use, dose, side effects, contraindications

Antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group reacts with the deoxyribonucleic acid (DNA) of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active with respect to Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (incl. Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (P. bivia, P. buccae, P. disiens), and some gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The minimum inhibitory concentration for these strains is 0.125 μg / ml.

In combination with amoxicillin shows activity against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

Metronidazole is not sensitive to aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

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

Pharmacokinetics:

Absorption is high (bioavailability is not less than 80%). It has a high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including lungs, kidneys, liver, skin, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretion, seminal fluid, breast milk. Penetrates through the blood-brain and placental barrier. The volume of distribution: adults - about 0.55 l / kg, newborns - 0.54-0.81 l / kg.

The maximum concentration of the drug in the blood (C_mOh) is from 6 to 40 μg / ml, depending on the dose. Time to reach the maximum concentration (TC_mOh) - 1-3 hours. Communication with plasma proteins - 10-20%.

In the body, about 30-60% of metronidazole is metabolized by hydroxylation, oxidation and glucuronation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects.

The half-life (T_1/2) in normal liver function - 8 hours (6 to 12 hours), with alcoholic liver disease - 18 h (from 10 to 29 h), in neonates: born at term pregnancy - 28-30 weeks - about 75 hr, respectively 32 weeks 35 - 35 h, 36-40 weeks -. 25 hours excreted by the kidneys 60-80% (20% intact), through the intestine - 6-15%.

Kidney clearance - 10.2 ml / min.

In patients with impaired renal function after repeated administration of metronidazole cumulation in serum can be observed (hence patients with severe renal impairment receiving frequency to be reduced).

Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T_1/2 is reduced to 2.6 hours). When peritoneal dialysis is withdrawn in small quantities.

Indications:

Protozoal Infection: extraintestinal anabiaz including amebic liver abscess, intestinal amoebiasis (amoebic dysentery), trichomoniasis, giardiazis, balantidiasis, giardiasis, cutaneous leishmaniasis, Trichomonas vaginitis, urethritis Trichomonas.

Infections caused by Bacteroides spp. (incl. fragilis, B.distasonis, AT. ovatus, AT. thetaiotaomicron, AT. vulgatus): infections of bones and joints, infections of the central nervous system (CNS), incl. meningitis, brain abscess, bacterial endocarditis, pneumonia, empyema and lung abscess.

Infections caused by the species Bacteroides, including group AT.fragilis, species Clostridium, Peptococcus and Peptostreptococcus: infection of the abdominal cavity (peritonitis, liver abscess), pelvic infection (endometritis, endomyometritis, abscess of fallopian tubes and ovaries, vaginal vaginal infection after surgery), skin and soft tissue infections.

Infections caused by the species Bacteroides, including group AT. fragilis and species Clostridium: sepsis, pseudomemporous colitis (associated with the use of antibiotics).

Gastritis or duodenal ulcer associated with Helicobacter pylori, alcoholism.

Prevention of postoperative complications (especially interference on the colon, near-rectal area, appendectomy, gynecological operations).

Radiation therapy of patients with tumors - as a radiosensitizer, in cases where tumor resistance is caused by hypoxia in tumor cells.

Contraindications:

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

Children under 3 years (for this dosage form).

Carefully:BVariability (II-III trimesters), renal / hepatic insufficiency.

Pregnancy and lactation:During lactation it is recommended to stop breastfeeding.

Dosing and Administration:

Inside, during or after a meal, (or squeezed milk), without chewing.

With trichomoniasis - 250 mg twice a day for 10 days or 400 mg twice a day for 5-8 days. Women need to be additionally appointed metronidazole in the form of vaginal suppositories or tablets. If necessary, you can repeat the course of treatment or increase the dose to 0.75-1 g / day. Between the courses should be a break in 3-4 weeks. with the conduct of repeated control laboratory tests. An alternative scheme of therapy is the appointment of 2 g once to the patient and his sexual partner.

Children 2-5 years - 250 mg / day; 5-10 years - 250-375 mg / day; over 10 years - 500 mg / day. The daily dose should be divided into 2 divided doses. The course of treatment is 10 days.

With giardiasis - 500 mg twice a day for 5-7 days.

Children from 3 years - 250 mg / day, 5-8 years - 375 mg / day, over 8 years - 500 mg / day (in 2 divided doses). The course of treatment is 5 days.

With giardiasis - 15 mg / kg / day in 3 divided doses for 5 days.

Adults: with asymptomatic amoebiasis (if a cyst is detected), the daily dose is 1-1.5 g (500 mg 2-3 times a day) for 5-7 days.

With chronic amebiasis daily dose of 1.5 g in 3 divided doses for 5-10 days, with acute amoebic dysentery - 2.25 g in 3 divided doses until symptoms stop.

With liver abscess - The maximum daily dose - 2.5 g in 1 or 2-3 doses, for 3-5 days, in combination with antibiotics (tetracyclines) and other methods of therapy.

Children from 3 years old - 1/4 of the adult dose, 3-7 years - 1/3 of the adult dose, 7-10 years - 1/2 dose of the adult.

With balantidiasis - 750 mg 3 times a day for 5-6 days.

With ulcerative stomatitis adults are prescribed 500 mg twice a day for 3-5 days; children in this case, the drug is not shown.

With pseudomembranous colitis - 500 mg 3-4 times a day.

For eradication of Helicobacter pylory - 500 mg 3 times a day for 7 days (as part of combination therapy, for example, combination with amoxicillin 2.25 g / day).

In the treatment of anaerobic infection the maximum daily dose is 1.5-2 g.

In the treatment of chronic alcoholism prescribe 500 mg / day for a period of up to 6 (not more) months.

For the prevention of infectious complications - 750-1500 mg / day in 3 divided doses 3-4 days before surgery, or once 1 g in the first day after the operation. In 1-2 days after the operation (when already allowed ingestion) - 750 mg / day for 7 days.

With severe renal dysfunction (CC less than 10 ml / min) daily dose should be reduced by half.

Side effects:

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

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

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

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

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

Interaction:

Strengthens the action indirect anticoagulants, which leads to an increase in the time of prothrombin formation.

Similarly to disulfiram, causes intolerance ethanol.

Simultaneous application with disulfiram can lead to the development of various neurological symptoms (the interval between appointment - at least 2 weeks).

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

Simultaneous administration of drugs stimulating enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin), can accelerate the elimination of metronidazole, as a result of which its concentration in the plasma decreases.

With simultaneous reception with drugs lithium, the concentration of the latter in the plasma and the development of symptoms of intoxication may increase.

It is not recommended to combine with nondepolarizing muscle relaxants (vecuronium bromide).

Sulfonamides enhance the antimicrobial effect of metronidazole.

Special instructions:

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

In combination with amoxicillin it is not recommended to use in patients younger than 18 years.

With prolonged therapy, it is necessary to monitor the blood picture.

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

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

Can immobilize treponema and lead to a false test of Nelson.

Stains urine in a dark color.

When treating trichomonas vaginitis in women and trichomoniasis in men, it is necessary to abstain from sexual activity. It is necessary to simultaneously treat sexual partners. Treatment does not stop during menstruation. After therapy with trichomoniasis, control tests should be performed for three consecutive cycles before and after menstruation.

After treatment of Giardiasis, if symptoms persist, through. 3 -4 weeks to conduct 3 stool analysis at intervals of several days (in some successfully treated patients lactose intolerance caused by invasion can persist for several weeks or months, recalling the symptoms of giardiasis).

Form release / dosage:Tablets, 250 mg.

Packaging:

For 10 tablets per contour cell pack, 2 packs with instructions for use in the pack.

Storage conditions:

At a temperature of 15 to 30 ° C, in a dark place out of the reach of children.

Shelf life:

5 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N002284 / 01

Date of registration:27.12.2007

Expiration Date:Unlimited

The owner of the registration certificate:GEDEON RICHTER-RUS, CJSC GEDEON RICHTER-RUS, CJSC Russia

Manufacturer: & nbsp

GEDEON RICHTER-RUS, CJSC Russia

Representation: & nbspGEDEON RICHTER-RUS CJSCGEDEON RICHTER-RUS CJSCRussia

Information update date: & nbsp29.01.2018

Illustrated instructions

Instructions

Clion (Klion)