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

Excipients: lactose monohydrate 91.0 mg, povidone 39.00 mg, corn starch 30.0 mg, microcrystalline cellulose 32.00 mg, sodium carboxymethyl starch 32.00 mg, talc 19.50 mg, magnesium stearate 6.50 mg.

Description:

Round, slightly biconcave tablets with a risk on one side, white or slightly yellowish in color.

Pharmacotherapeutic group:antimicrobial and antiprotozoal agent

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

Pharmacodynamics:

Metronidazole is a synthetic antimicrobial drug from the group of nitroimidazoles, which is active mainly in relation to anaerobic microorganisms - gram-negative and gram-positive bacteria. 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 interacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Metronidazole active in a relationship: Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., a also obligate anaerobes 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., Peptostreptococcus spp.). The MIC for these strains is 0.125-6.25 μg / ml.

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

To Metronidazole insensitive 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:

Metronidazole is rapidly and almost completely absorbed after oral administration; bioavailability is from 90 to 100%. After 4-6 hours, the concentration of metronidazole in tissues and cerebrospinal fluid reaches 80-90% of the serum concentration. Only a small part of the drug - no more than 20% - binds to plasma proteins. The half-life of the active substance is 8 hours. The drug penetrates well into all organs of the tissue, passes through the placenta and the blood-brain barrier (GEB), mainly accumulates in the liver, bladder, kidneys, penetrates into the mother's milk.

Metronidazole is mainly metabolized in the liver. The main metabolites are derived as conjugates with glucuronic acid (glucuronides)mainly with urine. The metabolism of the drug is slow in patients with liver disease. In patients with renal insufficiency, metabolites may accumulate. Non-metabolized metronidazole is excreted mainly with urine. From 6 to 15% of the accepted dose is excreted by the intestine. Metronidazole and its metabolites are rapidly removed by hemodialysis. The level of presystemic metabolism of the active substance is extremely small.

Indications:

- Anaerobic bacterial infections (gynecological and abdominal infections, central nervous system infections, bacteremia, sepsis, endocarditis, infections of bones, joints, skin and soft tissues, periodontal infections, respiratory tract infections) caused by Bacteroides spp., Clostridium spp., Eubacterium spp., Peptococcus spp., Peptostreptococcus spp. and other anaerobes, sensitive to metronidazole (for adults and children).

- Treatment of enterocolitis caused by Clostridium difficile, and bacterial vaginosis.

- Prophylactic appointment before surgical intervention on the gastrointestinal tract and reproductive organs.

- Eradication of bacteria Helicobacter pylori (for adults).

- Treatment of intestinal and extraintestinal forms of amoebiasis and infections caused by Giardia lamblia and Trichomonas vaginalis (for adults and children).

Contraindications:

- Hypersensitivity to metronidazole and other drugs of the nitroimidazole group, and hypersensitivity to any other ingredients of the drug.

- Leukopenia (including anamnesis).

- Organic damage to the central nervous system (CNS) (including epilepsy).

- Hepatic insufficiency (in case of administration of large doses of the drug).

- Pregnancy (I trimester), lactation.

- Children under 3 years (for this dosage form).

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

Pregnancy and lactation:

The drug is contraindicated in the first trimester of pregnancy; Later, he can be appointed only if the benefit to the mother exceeds the possible risk to the fetus.

During treatment with metronidazole, breastfeeding should be discontinued.

Dosing and Administration:

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

Treatment anaerobic infections usually begin with intravenous infusions. Once this is possible, the treatment should be continued with pills.

For of adults the dose for oral intake is 400 mg 3 times a day.The duration of treatment is up to 7 days, however, if necessary and depending on the indications, the treatment can be prolonged; the maximum daily dose: 1.6 - 2 g.

For children from 8 years (body weight from 27 kg) (for this dosage form): the dose is 7.5 mg / kg body weight 3 times a day (which is 22.5 mg / day).

For treatment enterocolitis, caused by Clostridium difficile, it is recommended that 400 mg of the dose be administered intravenously 3-4 times a day for 10 days.

Treatment bacterial vaginosis spend a single appointment of 2 g of metronidazole or a dose of 400 mg twice a day for 7 days. Simultaneous treatment of the sexual partner is not required.

For eradication Helicobacter pylori 400 mg of metronidazole is taken 3-4 times a day for 7 days in combination with other prescribed drugs.

Treatment trichomonas infection is carried out 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 metronidazole (or a dose of metronidazole, equal to 2 g, can be divided into two doses - 2 tablets in the morning and 3 tablets at night). It is necessary to conduct treatment for a sexual partner.

Children (for this dosage form) 10 years and older: 400 mg / day. The daily dose should be divided into 2 divided doses. The course of treatment is 10 days.

Treatment lambliasis in adults is administered 400 mg metronidazole 2 times a day for 5 days; children (for a given dosage form: from 3 years and body weight from 16 kg) is prescribed 25-35 mg / kg / day in 2 divided doses for 5 days.

Intestinal forms of amoebiasis in adults are treated with 800 mg metronidazole every 8 hours for 5 days; the maximum daily dose is 2.5 g / day. Children (for a given dosage form: from 4 years and body weight from 17 kg) is prescribed 35-50 mg / kg / day in 3 divided doses for 5 days.

Abscess of the liver and other extraintestinal forms of amoebiasis treated in the same doses over a period of 7-10 days. The maximum daily dose for children: 35-50 mg / kg / day.

When ulcerative gingivitis adults is prescribed 500 mg 2 times a day for 3-5 days.

When preventive prescription before surgery on the gastrointestinal tract and reproductive organs recommended adults and children over 12 years: 600 - 1200 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 it is already permitted to take inside) - 600 mg / day for 7 days.

When severe renal dysfunction (creatinine clearance less than 10 ml / min) daily dose should be reduced by 2 times.

Side effects:

Violations of the blood and lymphatic system: agranulocytosis, leukopenia, neutropenia, thrombocytopenia.

Immune system disorders: angioedema, anaphylactic shock.

Disorders of the psyche: psychotic disorders, including confusion, hallucinations, depression, insomnia, irritability, increased excitability.

Disturbances from the nervous system: peripheral sensory neuropathy, headache, convulsions, dizziness, reported on the development of encephalopathy and subacute cerebellar syndrome (impaired coordination and synergy of movements, ataxia, dysarthria, gait disturbance, nystagmus, tremor) that are reversible after metronidazole withdrawal, aseptic meningitis.

Disturbances on the part of the organ of sight: transient visual impairments, such as diplopia, myopia, vagueness of contours of subjects, decreased visual acuity, impaired color perception, neuropathy / neuritis of the optic nerve.

Disorders from the digestive system: pain in epigastrium, nausea, vomiting, diarrhea, glossitis, stomatitis, metallic taste in the mouth, decreased appetite, anorexia, dryness of the oral mucosa, constipation, pancreatitis (reversible cases), discoloration and tongue / (because of the growth of fungal microflora).

Disturbances from the liver and bile ducts: increased activity of "hepatic" enzymes (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase), development of cholestatic or mixed hepatitis and hepatocellular liver damage, sometimes accompanied by jaundice.

In patients treated with metronidazole in combination with other antibacterial agents, cases of hepatic insufficiency that required liver transplantation were observed.

Disturbances from the skin and subcutaneous tissues: skin rash, skin itching, skin hyperemia, urticaria, pustular skin rash,Stevens-Johnson syndrome, toxic epidermal necrolysis.

Infringements from kidneys and urinary tract: staining of urine in a brownish-reddish color, due to the presence in the urine of a water-soluble metronidazole metabolite, dysuria, polyuria, cystitis, urinary incontinence, candidiasis.

General disorders and disorders at the site of administration: fever, nasal congestion, arthralgia, weakness.

Laboratory and instrumental data: flattening of the T wave on the electrocardiogram.

Overdose:

Too high doses can cause side effects, mainly nausea, vomiting and dizziness; in more severe cases, there may be ataxia, paresthesia and seizures.

Treatment is symptomatic. There is no specific antidote.

Interaction:

Patients should inform the doctor if they are taking any other medicines.

Metronidazole enhances the action warfarin and other anticoagulants coumarinovogo number, so with the simultaneous administration of a dose of these drugs must be reduced.

Phenytoin and barbiturates reduce the effectiveness of metronidazole; at the same time, the efficacy of phenytoin and barbiturates may increase.

With the simultaneous administration of metronidazole and lithium the neurotoxicity of lithium increases.

Cimetidine increases the half-life of metronidazole.

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

Sulfonamides enhance the antimicrobial effect of metronidazole.

Because of the development of acute psychosis, simultaneous treatment with metronidazole and disulfiram. Patients should not be assigned metronidazole within two weeks the field of treatment with disulfiram.

Special instructions:

Patients with severe hepatic insufficiency metronidazole should be administered with caution, because as a result of slowing metabolism, the concentration of metronidazole and its metabolites in plasma increases.

Because of the slowing down of excretion, care must be taken when choosing a dose of metronidazole in patients with renal insufficiency. In such patients, the dose should be reduced by half.

Metronidazole should be used with extreme caution in patients with bone marrow and central nervous system depression, as well as in elderly patients.The appearance of ataxia, dizziness and any other deterioration in the neurological status of patients requires discontinuation of treatment.

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

Metronidazole should be avoided in patients with porphyria.

With long-term treatment with metronidazole (more than 10 days), one should observe the picture of peripheral blood and liver function.

Can immobilize treponema and lead to Nelson's false positive test.

When treating trichomonadal vaginitis in women and trichomoniasis in men, it is necessary to abstain from sexual activity. Treatment does not stop during menstruation. After therapy with trichomoniasis, control tests should be performed for 3 consecutive cycles before and after menstruation.

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

During treatment and for three days after treatment with metronidazole, the patient should not take alcoholic beverages,since it is possible to develop a disulfiram-like reaction.

Effect on the ability to drive transp. cf. and fur:PThe drug may have a negative effect on psychophysiological abilities, especially if it is simultaneously taken with alcohol.

Form release / dosage:

Tablets, 400 mg.

Packaging:

For 10 tablets in a glass bottle of amber color (type III), ukuporenny transparent polyethylene lid with a white top.

One bottle in a cardboard box together with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014472 / 02

Date of registration:23.06.2008 / 28.01.2014

Expiration Date:Unlimited

Date of cancellation:2018-04-12

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp12.04.2018

Illustrated instructions

Instructions

Efloran (Efloran®)