Ecoclav pills 250mg+125mg, 15pcs

Composition

Composition for 1 tablet:

Active ingredients, mg: Amoxicillin trihydrate 286.92 573.85 1004.30 (based on amoxicillin) 250.00 500.00 875.00 potassium clavulanate + microcrystalline cellulose (1: 1) 297.82 297.82 297.82(based on clavulanic acid) 125.00 125.00 125.00

Excipients, mg: lactitol 300.00 600.00 300.00 hyprolose 52.00 86.50 92.50 crospovidone (collidone CL) 24.00 45.00 50.00 talc 8.00 12.00 10.00 magnesium stearate 5.20 13.84 18.50 microcrystalline cellulose to obtain a tablet without a shell weighing 1040.00 1730.00 1850.00

Excipients of the shell before obtaining a tablet with a shell weight, mg: Insta Moistscheld film coating mixture [hypromellose-54.0%, ethylcellulose-5.0%, diethyl phthalate-12.0%, titanium dioxide-25%, talc-4%] 1089.00 1774.30 1895.00

Pharmacological action

Pharmacotherapy group.

Antibiotic-penicillin semi-synthetic + beta-lactamase inhibitor.

ATX code. J01CR02

Pharmacological properties.

Pharmacodynamics .

A combined preparation of amoxicillin and clavulanic acid, a beta-lactamase inhibitor. Amoxicillin is a semi-synthetic broad-spectrum antibiotic that acts as a bactericidal agent, inhibiting cell wall protein synthesis in 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 by beta-lactamases is prevented, and the bactericidal activity of the antibiotic is preserved. Clavulanic acid inhibits type II-V beta-lactamases according to the Richmond-Sykes classification and is not active against type I beta-lactamases produced by Pseudomonas aeruginosa, Serratia spp., and Acinetobacter spp.

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

Gram-positive aerobic microorganisms:

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

Gram-negative aerobic microorganisms:

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

Escherichia coli (strains that produce and do not produce beta-lactamases);

Haemophilus influenzae (strains that produce and do not produce beta-lactamases);

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

Moraxella catarrhalis (beta-lactamase-producing and non-beta-lactamase-producing strains).

According to the results of in vitro studies, the following microorganisms are sensitive to the combination of amoxicillin and clavulanic acid: :

Gram-positive aerobic microorganisms:

Enterococcus faecalis **;

Staphylococcus epidermidis (strains producing and not producing 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 viridans group ** (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 (beta-lactamase producing and non-beta-lactamase producing strains);

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

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

NOTE: * * – (amoxicillin has been clinically proven effective in treating a number of infections caused by these pathogens).

Pharmacokinetics.

Suction. Both active ingredients of Ecoclav®, amoxicillin and clavulanic acid, are rapidly and well absorbed when taken orally.

Absorption of the active ingredients of Ecoclav® is optimal if the drug is taken at the beginning of a meal.

The following are data on the pharmacokinetic parameters of amoxicillin and clavulanic acid obtained in separate studies when healthy volunteers took on an empty stomach: – 1 tablet of the drug,250 mg + 125 mg (375 mg) (amoxicillin + clavulanic acid, respectively); – 2 tablets of the drug,250 mg + 125 mg (375 mg); – 1 tablet of the drug,500 mg + 125 mg (625 mg); – 2 tablets of the drug,875 mg + 125 mg (1000 mg); – 500 mg of amoxicillin;

– 125 mg of clavulanic acid.

Preparations Dose (mg) Cmax (mg/ l) Tmax (h) AUC (mg×h/ L) T 1/2 (h)

Amoxicillin 250 mg + 125 mg (amoxicillin +clavulanic acid) 250 3,7 1,1 10,9 1,0250 mg + 125 mg (amoxicillin +kavelenova acid),2 tablets of 500 5,8 1,5 1,3500 of 20.9 mg + 125 mg (amoxicillin +clavulanic acid) 500 6,5 1,5 23,2 1,3

875 mg + 125 mg (amoxicillin +clavulanic acid) 1750 11,64 ±2,78 1,50 (1,0-2,5) 53,52 ±12,31 1,19 ±0,21 Amoxicillin,500 mg 500 6,5 19,5 1,3 1,1Clavulanic acid250 mg + 125 mg (amoxicillin +clavulanic acid) 125 2,2 1,2 6,2 1,2250 mg + 125 mg (amoxicillin +clavulanic acid),2 tablets of 250 4,1 1,3 11,8 1,0 clavulanic acid,125 mg 125 3,4 0,9 7,8 0.7500 in mg + 125 mg (amoxicillin +clavulanic acid) 125 2,8 1,3 7,3 0,8875 mg + 125 mg (amoxicillin +clavulanic acid) 250 2,18 ±0,99 1,25 (1,0 -2,0) 10,16 ±3,04 0,96 ±0,12

C_max – the maximum concentration in the blood plasma.

Tmax – time to reach the maximum concentration in the blood plasma.

AUC – area under the concentration-time curve.

T_1/2 is the elimination half-life.

When using Ecoclav®, plasma concentrations of amoxicillin are similar to those when taking equivalent doses of amoxicillin orally.

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

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 data on the negative effect on the fetus have not been published.

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

Metabolism, elimination. Approximately 60-70% of amoxicillin is excreted by the kidneys: by tubular secretion and glomerular filtration.

Clavulanic acid is actively metabolized in the liver and is eliminated by glomerular filtration (40-65%), partly in the form of metabolites. A smaller part is excreted by the intestines.

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

Indications

Infectious and inflammatory diseases caused by drug-sensitive pathogens:

– infections of the lower respiratory tract (bronchitis, pneumonia);

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

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

infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses, abscess, cellulitis, wound infection);

– infections of bones and joints (osteomyelitis).

Use during pregnancy and lactation

The combined preparation of amoxicillin and clavulanic acid during pregnancy is recommended to be prescribed only in cases where the expected benefit of taking it for the mother exceeds the potential risk to the fetus. The drug can be used during breastfeeding. With the exception of the risk of sensitization associated with the penetration of trace amounts of the active ingredients of this drug into breast milk, no other adverse effects were detected in infants who are breastfed.

Contraindications

– hypersensitivity to amoxicillin, clavulanic acid, other components of the drug or penicillins;

– congenital fructose intolerance, galactose, galactosemia, glucose-galactose malabsorption;

– severe reactions of immediate hypersensitivity (e. g., anaphylaxis) to other beta-lactam antibiotics (e. g., cephalosporins, carbapenems, monobactam) in the anamnesis;

– previous episodes of jaundice or abnormal liver function with the combination of amoxicillin with clavulanic acid in history;

– children’s age up to 12 years or weighing less than 40 kg.

With caution.

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

Side effects

The drug is well tolerated. Side effects are rare, mostly mild, and transient in nature.

From the digestive system: nausea, vomiting, diarrhea, gastritis, stomatitis, glossitis, cholestatic jaundice, hepatitis, hepatic failure (most often in older men with long-term therapy), colitis (including pseudomembranous), black ‘hairy’ tongue, darkening of the tooth enamel, increased activity of ‘liver’ transaminases, increased bilirubin and alkaline phosphatase activity.

From the side of hematopoietic organs: 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 changes, seizures.

Allergic reactions: urticaria, erythematous rashes, erythema multiforme, 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 services: candidiasis, development of superinfection.

Interaction

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

Allopurinol increases the risk of skin rashes.

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

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

The literature describes rare cases of an increase in the international normalized ratio (INR) in patients with the combined use of acenocoumarol or warfarin and amoxicillin. If a combination of amoxicillin and clavulanic acid is required to be co-administered with indirect anticoagulants, prothrombin time or INR should be carefully monitored when prescribing or discontinuing the drug.

How to take, course of use and dosage

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

The minimum course of antibacterial 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.

Since the tablets contain the same amount of clavulanic acid (125 mg), please note that 2 tablets of 250 mg+125 mg are not equivalent to 1 tablet

of 500 mg+125 mg.

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

In chronic renal failure have a correction dose and multiplicity of reception, depending on creatinine clearance (CC):

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

if CC 10-30 ml/min: 1 tablet of 250 mg+125 mg 2 times a day (in light and moderate infections) or 1 tablet of 500 mg+125 mg 2 times a day (in severe infections or infections of the lower respiratory tract);

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

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

Overdose

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

Treatment: symptomatic. Hemodialysis is effective.

Description

Capsule-shaped biconvex tablets, film-coated in white or almost white color. On a cross-section, the core is white or almost white to light yellow with a brownish tinge of color, white to yellow inclusions are acceptable.

Special instructions

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

During the course of treatment, it is necessary to monitor the state of function of the hematopoietic organs, liver and kidneys.

It is possible to develop superinfection due to the selection of resistant forms of the pathogen.

False positive results may be detected when 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.

In patients with hypersensitivity to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

If infectious mononucleosis is suspected, the drug should not be used, since in patients with this disease, amoxicillin can cause a crust-like skin rash, which makes it difficult to diagnose the disease.

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

Form of production

Film-coated tablets,250 mg + 125 mg,500 mg + 125 mg,875 mg + 125 mg.

5 or 7 tablets in a contour cell package made of aluminum foil multilayer and aluminum foil printed varnished.

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 low-pressure polyethylene bottle with a screw-on lid with a first opening control with a moisture-absorbing insert or a polymer jar made of low-pressure polyethylene with a screw-on lid with a first opening control with a moisture-absorbing insert.

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

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 0 C. Keep out of the reach of children.

Shelf

life is 2 years. Do not use after the expiration date.

Active ingredient

Amoxicillin, Clavulanic Acid

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults by doctor’s prescription, Children by doctor’s prescription, Children over 12 years of age

Indications

Skin Infections, Urinary Tract Infections, Bronchitis, Sinusitis, Cholecystitis, Pneumonia, Pharyngitis, Otitis Media, Osteomyelitis, Sore Throat, Periodontitis, Tonsillitis