Ecoclave - instructions for use, doses, side effects, contraindications

Active substances:	250 mg + 125 mg	500 mg + 125 mg	875 mg + 125 mg
Amoxicillin trihydrate (in terms of amoxicillin)	250 mg	500 mg	875 mg
Potassium clavulanate (in terms of clavulanic acid)	125 mg	125 mg	125 mg
Excipients:
Lactulose	300.0 mg	600.0 mg	300.0 mg
Crospovidone (clolidone CL)	24.0 mg	45.0 mg	50.0 mg
Croscarmellose sodium	24.0 mg	45.0 mg	50.0 mg
Talc	8.0 mg	12.0 mg	10.0 mg
Magnesium stearate	4.0 mg	8.0 mg	10.0 mg
Cellulose microcrystalline to obtain a tablet without a shell mass	850.0 mg	1500.0 mg	1700.0 mg
Shell accessories:
Mixture for the preparation of a film coating with the shell "Insta Mojsheld" Sufficient for to obtain a tablet weighing: [hypromellose - 54.0%, ethyl cellulose -5.0%, diethylphthalate - 12.0%, titanium dioxide - 25.0%, talc - 4.0%]	890.0 mg	1537.5 mg	1734.0 mg

Description:

The tablets covered with a film membrane of white or almost white color, oval, biconcave. On a cross-section from white with a yellowish shade to light yellow with a brown shade, admissions of a white color are admissible.

Pharmacotherapeutic group:Antibiotic - penicillin semisynthetic + beta-lactamase inhibitor.

ATX: & nbsp

J.01.C.R.02 Amoxicillin in combination with enzyme inhibitors

Pharmacodynamics:

The combined preparation of amoxicillin and clavulanic acid is a beta-lactamase inhibitor. Amoxicillin - a semisynthetic antibiotic of a wide spectrum; acts bactericidal; inhibiting protein synthesis of the cell wall sensitive bacteria at the growth stage. Clavulanic acid has a high affinity for bacterial beta-lactamases and forms a stable complex with them. Thus, the biodegradation of amoxicillin with beta-lactamases is prevented, and the bactericidal activity of the antibiotic is preserved. Clavulanic acid inhibits beta-lactamase II-V type according to Richmond-Sykes classification and is not active against type I beta-lactamases produced by Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp.

The combined preparation of amoxicillin and clavulanic acid according to the results of in vitro and clinical trials is active against the following microorganisms:

Gram-positive aerobic microorganisms:

Staphylococcus aureus (strains producing and not producing beta-lactamases);

Gram-negative aerobic microorganisms:

Enterobacter spp. (despite the fact that most Enterobacter strains are resistant in vitro, the efficacy of the drug has been clinically proven in the treatment of infectious diseases caused by this pathogen of the urinary system);

Escherichia coli (strains producing and not producing beta-lactamases);

Haemophilus influenzae (strains producing and not producing beta-lactamases);

Klebsiella spp. (all known strains producing beta-lactamases);

Moraxella catarrhalis (strains producing and not producing beta-lactamases).

According to the results of in vitro studies, sensitivity to the combination of amoxicillin and clavulanic acid of the following microorganisms is indicated:

Gram-positive aerobic microorganisms:

Enterococcus faecalis **;

Staphylococcus epidermidis (strains that produce and do not produce beta-lactamases);

Staphylococcus saprophyticus (strains producing and not producing beta-lactamases);

Streptococcus pneumoniae ** (strains not producing beta-lactamases);

Streptococcus pyogenes ** (strains not producing beta-lactamases);

Streptococcus group viridans ** (strains not producing beta-lactamases).

Gram-negative aerobic microorganisms:

Eikenella corrodens (strains producing and not producing beta-lactamases);

Neisseria gonorrhoeae ** (strains producing and not producing beta-lactamases);

Proteus mirabilis ** (strains producing and not producing beta-lactamases).

Anaerobic microorganisms:

Bacteroides spp., Including Bacteroides fragilis (strains producing and not producing beta-lactamases); *

Fusobacterium spp. (strains producing and not producing beta-lactamases);

Peptostreptococcus spp. (beta-lactamase does not produce).

NOTE: ** - (clinically proven the effectiveness of amoxicillin in the treatment of a number of infections caused by these pathogens).

Pharmacokinetics:

Suction. After oral administration, both components of the drug are rapidly absorbed from the gastrointestinal tract. Absorption of active ingredients of the drug is optimal in case of its intake at the beginning of the meal.

After taking Inside at a dose of 250 mg + 125 mg:

- maximum concentration (Сmah) amoxicillin - 3.7 μg / ml, clavulanic acid - 2.2 μg / ml;

- time to reach the maximum concentration (Tmah) amoxicillin -, 1,1 h, clavulanic acid - 1.2 h;

- the area under the concentration-time curve (AUC) of amoxicillin is 10.9 mg-h / l. clavulanic acid -6.2 mg-h / l.

After oral administration at a dose of 500 mg + 125 mg:

- C amaxicillin - 6.5 μg / ml, clavulanic acid - 2.8 μg / ml;

- Tmah amoxicillin - 1.5 h, clavulanic acid - 1.3 h; :

- AUC amoxicillin 23.2 mg-h / l, clavulanic acid - 7.3 mg-h / l.

After oral administration at a dose of 875 mg + 125 mg:

- FROMmah amoxicillin - 8,8 mkg / ml, clavulanic acid - 2.07 mcg / ml;

- Tmah amoxicillin - 1.5 h, clavulanic acid - 1.5 h;

- AUC amoxicillin - 25.4 mg-h / l, clavulanic acid - 6.1 mg-h / l.

When the drug is used, concentrations of amoxicillin in the blood serum are similar to those for oral administration of equivalent doses of one amoxicillin.

Distribution. Both components of the preparation are characterized by a good volume of distribution - therapeutic concentrations of amoxicillin and clavulanic acid are created in various organs and tissues, interstitial fluid: the lungs, middle ear, abdominal organs, small pelvic organs (prostate gland, uterus, ovaries), skin, fat, bone and muscle tissues, pleural, synovial and peritoneal. liquids; plasma, bile, purulent discharge, sputum, bronchial secretion.

Amoxicillin and clavulanic acid have a moderate degree of binding to plasma proteins, respectively, by 18% and 25%.

Both components of the drug penetrate the placental barrier, but there is no published data on the negative effect on the fetus.

Amoxicillin and clavulanic acid in low concentrations are found in breast milk.

Metabolism, excretion. Approximately 60-70% of amoxicillin is excreted by the kidneys: by tubular secretion and by glomerular filtration. Clavulanic acid is actively metabolized in the liver and is excreted by glomerular filtration (40-65%), partially in the form of metabolites. The smaller part is excreted by the intestine.

With renal failure, the clearance of amoxicillin with clavulanic acid decreases, so dose adjustment is required.

Indications:

Infectious-inflammatory diseases caused by drug-susceptible pathogens:

- Infections of the lower respiratory tract (bronchitis, pneumonia);

- infections of the ENT organs (sinusitis, tonsillitis, otitis media);

- infections of the genitourinary system and pelvic organs (pyelonephritis, pyelitis, cystitis, urethritis, bacterial prostatitis, cervicitis, salpingitis, salpingoophoritis, endometritis, bacterial vaginitis, septic abortion, chancroid, gonorrhea);

- skin and soft tissue infections (erysipelas, impetigo, secondarily infected dermatoses, abscess, phlegmon, wound infection);

- infections of bones and joints (osteomyelitis).

Contraindications:

Hypersensitivity (including to cephalosporins and other beta-lactam antibiotics), infectious mononucleosis, episodes of jaundice or impaired liver function as a result of amoxicillin / clavulanic acid in history.

Children under 12 years of age or at a body weight of less than 40 kg (for this dosage form).

Chronic renal failure (creatinine clearance less than 30 ml / min)

for tablets with a dosage of 875 mg + 125 mg.

Carefully:

Severe hepatic insufficiency, diseases of the gastrointestinal tract (including colitis in history, associated with the use of penicillins), chronic renal failure.

Pregnancy and lactation:

The combined preparation of amoxicillin and clavulanic acid during pregnancy is recommended to be prescribed only in cases when the expected benefit from its administration for the mother exceeds the potential risk for the fetus.

The drug can be used during breastfeeding. Except for the risk of sensitization associated with the penetration of trace amounts of the active ingredients of this preparation into breast milk, no other adverse effects were found in infants fed breastfeeding.

Dosing and Administration:

Inside. The dosage regimen is set individually depending on the age and body weight of the patient, the severity of the course and localization of the infectious process, as well as the sensitivity of the pathogen.

The minimum course of antibiotic therapy is from 5 days. Treatment should not be continued for more than 14 days without reviewing the clinical situation.

Adults and children over 12 years of age or weighing more than 40 kg:

Mild and moderate infections - 1 tablet of 250 mg + 125 mg 3 times a day or 1 tablet of 500 mg + 125 mg 2 times a day.

Severe infections or infections of the lower respiratory tract - 1 tablet of 875 mg + 125 mg 2 times a day or 1 tablet of 500 mg + 125 mg 3 times a day.

Because the tablets contain the same amount of clavulanic acid (125 mg), it should be noted that 2 tablets of 250 mg + 125 mg are not equivalent a tablet of 500 mg + 125 mg.

The maximum daily dose of amoxicillin for adults and children over 12 years is 6 g, clavulanic acid is 600 mg.

In chronic renal insufficiency, dose adjustment and frequency of administration are carried out depending on the creatinine clearance (CK):

with QC more than 30 ml / min dose adjustment is not required;

with QC10-30 ml / min: 1 tablet of 250 mg + 125 mg twice a day (for mild and moderate infections) or 1 tablet of 500 mg + 125 mg twice a day (for severe infections or infections of the lower respiratory tract);

with QC less than 10 ml / min: 1 tablet of 250 mg + 125 mg once a day (for mild and moderate infections) or 1 tablet of 500 mg + 125 mg once a day (for severe infections or infections of the lower respiratory tract) ;

Patients on hemodialysis: 1 tablet of 500 mg + 125 mg or 2 tablets of 250 mg + 125 mg every 24 hours in combination with 1 dose during hemodialysis and 1 dose after hemodialysis, as the concentration of amoxicillin and clavulanic acid decreases.

Side effects:

The drug is well tolerated. Side effects occur rarely, are mostly mildly expressed and are transient in nature.

From the digestive system: nausea, vomiting, diarrhea, gastritis, stomatitis, glossitis, cholestatic jaundice, hepatitis, liver failure (more common in the elderly, women, long-term therapy), colitis (including pseudomembranous), black "hairy" tongue, darkening of the tooth enamel, increased activity of " hepatic "transaminases, an increase in bilirubin and alkaline phosphatase activity.

On the part of the organs of hematopoiesis: reversible increase in prothrombin time and bleeding time, thrombocytopenia, thrombocytosis, eosinophilia, leukopenia, agranulocytosis, hemolytic anemia.

From the central nervous system: dizziness, headache, hyperactivity, anxiety, behavior change, convulsions.

Allergic reactions: urticaria, erythema eruptions, multiforme exudative erythema, anaphylactic shock, angioedema, exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), allergic vasculitis, a syndrome similar to serum sickness, acute generalized exanthematous pustulosis.

From the side of the kidneys and urinary tract: interstitial nephritis, crystalluria, hematuria.

Other: Candidiasis, development of superinfection.

Overdose:

Symptoms: a violation of the function of the gastrointestinal tract and water electrolyte balance.

Treatment: symptomatic. Hemodialysis is effective.

Interaction:

It is not recommended to use a combined preparation of amoxicillin and clavulanic acid simultaneously with probenecid.Probenecid lowers the tubular secretion of amoxicillin, so their joint use can lead to an increase and persistence of amoxicillin concentration in the serum, while the serum concentration of clavulanic acid does not change.

Antacids, glucosamine, laxatives slow down and reduce the absorption of amoxicillin; ascorbic acid - Increases.

Allopurinol increases the risk of skin rashes.

Diuretics, allopurinol, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that block tubular secretion, increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).

Like other broad-spectrum antibiotics, the combination drug amoxicillin and clavulanic acid may reduce the effectiveness of oral contraceptives, and patients should be informed about this.

In the literature, rare cases of an increase in the international normalized ratio (INR) in patients with joint use of acenocoumarol or warfarin and amoxicillin are described.If it is necessary to simultaneously prescribe a combined preparation of amoxicillin and clavulanic acid with indirect anticoagulants, prothrombin time or INR should be carefully monitored when the drug is prescribed or withdrawn.

Special instructions:

The severity of gastrointestinal symptoms decreases when taking the drug at the beginning of the meal.

At course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

It is possible to develop superinfection by selecting the resistant forms of the pathogen.

There may be false-positive results in determining glucose in the urine. In this case, it is recommended to use a glucose oxidant method for determining the concentration of glucose in the urine.

Patients with increased sensitivity to penicillins are possible cross-allergic reactions with cephalosporin antibiotics. In the case of suspected infectious mononucleosis, the drug should not be used because patients with this disease amoxicillin can cause a skinlike skin rash, which makes it difficult to diagnose the disease.

Effect on the ability to drive transp. cf. and fur:

Given the likelihood of side effects from the central nervous system, care should be taken when driving vehicles and working with mechanisms.

Form release / dosage:

The tablets covered with a film cover 250 mg + 125 mg, 500 mg + 125 mg, 875 mg + 125 mg.

Packaging:For 5 or 7 tablets in a contour mesh box made of aluminum foil multilayer foil and aluminum foil printed lacquered. For 14 or 15 tablets with a dosage of 250 mg + 125 mg and 500 mg + 125 mg, 5, 7, 10 or 14 tablets with a dosage of 875 mg + 125 mg in a plastic bottle with a screw cap with a first opening control with a moisture absorbing insert or a polymer can. with a screw cap with the control of the first opening with a moisture absorbing insert.

For 1, 2 or 3 contour cell packs with a dosage of 250 mg + 125 mg and 500 mg + 125 mg, 1 or 2 circuit cells at a dosage of 875 mg + 125 mg or 1 bottle or jar, together with instructions for use, are placed in a pack of cardboard .

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008275/10

Date of registration:17.08.2010

The owner of the registration certificate:AVVA RUS, OJSC AVVA RUS, OJSC Russia

Manufacturer: & nbsp

AVVA RUS, OJSC Russia

Representation: & nbspAVVA ENG JSC AVVA ENG JSC Russia

Information update date: & nbsp17.06.2013

Illustrated instructions

Instructions

Ecoclave® (Ecoclav®)