Ecoclav suspension powder for oral use 125+31.25mg/5ml bottle, 25g

Composition

>

of 5 ml of the finished suspension (one dosage spoon) contains:  

active ingredients:

amoxicillin trihydrate (in terms of amoxicillin) 125 mg,

potassium clavulanate (in terms of clavulanic acid) 31.25 mg;

excipients:

lactulose,

aspartame,

colloidal silicon dioxide (aerosil),

xanthan gum,

crospovidone (collidone CL-M),

citric acid anhydrous,

sodium citrate dihydrate,

sodium benzoate,

talc,

orange flavor,

mannitol (mannitol)

Pharmacological action

Ecoclav is 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 (beta-lactamase-producing and non-beta-lactamase-producing strains); Gram-negative aerobic microorganisms: Enterobacter spp. (although most Enterobacter strains are resistant in vitro, the drug has been clinically proven to be effective in treating 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 strains produce beta-lactamases). beta-lactamases); Moraxella catarrhalis (strains producing and not producing beta-lactamases). 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 that produce and do not produce beta-lactamases);Staphylococcus saprophyticus (strains that produce and do not produce beta-lactamases);Streptococcus pneumoniae** (does not produce beta-lactamases);Streptococcus pyogenes** (beta-lactamase does not produce);Streptococcus viridans** (beta-lactamase does not produce).

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 that produce and do not produce beta-lactamases);Fusobacterium spp. (strains that produce and do not produce beta-lactamases);Peptostreptococcus spp. (does not produce beta-lactamases).

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

Lactulose, which is part of Ecoclavas as a bifidogenic factor, is a synthetic disaccharide, the molecule of which consists of galactose and fructose residues. Lactulose in the stomach and upper intestines is not absorbed or hydrolyzed.

The Ecoclavalactulose released from tablets as a substrate is fermented by the normal microflora of the large intestine, stimulating the growth of bifidobacteria and lactobacilli. As a result of the hydrolysis of lactulose in the large intestine, organic acids are formed – lactic, acetic and formic, which inhibit the growth of pathogenic microorganisms and, as a result, reduce the production of nitrogen-containing toxic substances.

Thus, lactulose in the composition of Ecoclavas Reduces the damaging effect of the antibiotic on the normal intestinal microflora and the risks of side effects associated with dysbiosis.

Pharmacokinetics

Suction

  After oral use, both components of the drug are rapidly absorbed from the gastrointestinal tract. Absorption of the active ingredients of the drug is optimal if it is taken at the beginning of a meal.

After oral use at a dose of 125 mg+31.25 mg:

– Cmax of amoxicillin – 1.96 mcg/ml, clavulanic acid – 0.77 mcg/ml;- Tmax of amoxicillin – 1.5 h, clavulanic acid – 1.0 h;- AUC of amoxicillin – 9.19 mg h/l, clavulanic acid – 2.69 mg h/l. When using the drug, the concentration of amoxicillin in the blood serum is similar to that with oral use of equivalent doses of one amoxicillin.

The distribution of

Both components of the drug are characterized by a good level of distribution – therapeutic concentrations of amoxicillin and clavulanic acid are produced in a variety of organs and tissues, interstitial fluid: the lungs, middle ear, the abdominal organs, pelvic organs (prostate, uterus, ovaries), skin, fat, bone and muscle tissues; pleural, synovial and peritoneal fluids; 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 data on the negative effect on the fetus have not been published.

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

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.

Lactulose, which is part of the Ecoclav, does not affect the main pharmacokinetic parameters that characterize the bioavailability of amoxicillin and clavulanic acid.

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);
• infections 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 children who are breastfed.

Contraindications

• hypersensitivity (including to cephalosporins and other beta-lactam antibiotics);
• infectious mononucleosis;
• episodes of jaundice or liver dysfunction as a result of application of amoxicillin/clavulanic acid in history;
• children up to age 12 years or weighing less than 40 kg (for this dosage form);
• phenylketonuria (contains aspartame) for suspension.

With caution: severe hepatic insufficiency, 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, liver failure (more often in the elderly, men, with long-term therapy), colitis (including pseudomembranous), black “hairy” tongue, darkening of tooth enamel, increased activity of “liver” transaminases, increased bilirubin content and alkaline phosphatase activity.

Hematopoietic disorders: reversible increase in prothrombin time and bleeding time, thrombocytopenia, thrombocytosis, eosinophilia, leukopenia, agranulocytosis, hemolytic anemia.

Central nervous system disorders: 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.

Renal and urinary tract disorders: interstitial nephritis, crystalluria, hematuria.

Other: 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.

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).

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

Allopurinol increases the risk of skin rashes.

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 concomitant use of the combined drug amoxicillin and clavulanic acid with indirect anticoagulants is necessary, prothrombin time or INR should be carefully monitored when prescribing or discontinuing the drug.

How to take, course of use and dosage

The suspension is taken orally. The dosage regimen is set individually depending on the patient’s 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. The duration of treatment of acute uncomplicated otitis media is 5-7 days, in children under 2 years – 7-10 days.

A single dose is set depending on age and body weight (calculated according to amoxicillin):Children under 3 months – 30 mg / kg / day in 2 divided doses; Children from 3 months and older:— low doses (for the treatment of skin and soft tissue infections, as well as chronic tonsillitis) – 20 mg / kg / day in 3 doses— – high doses (for the treatment of otitis media, sinusitis, lower respiratory tract infections, urinary tract infections) – 40 mg/kg/day in 3 doses. Children weighing 40 kg or more should be given doses similar to adults. The suspension can be used in adults with difficulty swallowing.

Recommended dosage regimen for adults: 20 ml of suspension at a dosage of 125 mg+31.25 mg/5 ml or 10 ml of suspension at a dosage of 250 mg+62.5 mg/5 ml 2-3 times / day. The maximum daily dose of amoxicillin for adults and children over 12 years of age is 6 g, for children under 12 years of age – 45 mg/kg of body weight. The maximum daily dose of clavulanic acid for adults and children over 12 years of age is 600 mg, for children under 12 years of age – 10 mg/kg.

Patients with impaired renal function:

Dose adjustment is based on the maximum recommended dose of amoxicillin and creatinine clearance.

Children: Creatinine clearance greater than 30 ml / min no dose adjustment is required;

Creatinine clearance 10-30 ml / min – 15 mg / 3.75 mg / kg 2 times / day, the maximum dose is 500 mg+125 mg (20 ml of suspension at a dosage of 125 mg+31.25 mg/5 ml or 10 ml of suspension at a dosage of 250 mg+62.5 mg/5 ml) 2 times/day;

Creatinine clearance less than 10 ml / min – 15 mg / 3.75 mg / kg 1 time / day, the maximum daily dose is 500 mg+125 mg (20 ml of suspension at a dosage of 125 mg+31.25 mg/5 ml or 10 ml of suspension at a dosage of 250 mg+62.5 mg/5 ml);

Adults: creatinine Clearance more than 30 ml/min dose adjustment is not required;creatinine Clearance 10-30 ml/min,500 mg+125 mg (20 ml of a suspension at a dosage of 125 mg+31.25 mg/5 ml or 10 ml suspension in a dosage of 250 mg+62.5 mg/5 ml) 2 times/day;Creatinine clearance less than 10 ml/min,500 mg+125 mg (20 ml of a suspension at a dosage of 125 mg+31.25 mg/5 ml or 10 ml suspension in a dosage of 250 mg+62.5 mg/5 ml) 1 time/day;

Patients undergoing hemodialysis: Dose adjustment is based on the maximum recommended dose of amoxicillin

for children-15 mg / 3.75 mg / kg 1 time / day.

Before the hemodialysis session, one additional dose of 15 mg/3.75 mg/kg should be taken. To restore the concentration of active components of the drug in the blood, a second additional dose of 15 mg/3.75 mg / kg should be taken after a hemodialysis session.

Adults – 500 mg+125 mg (20 ml of suspension at a dosage of 125 mg+31.25 mg/5 ml or 10 ml of suspension at a dosage of 250 mg+62.5 mg/5 ml) once every 24 hours.

An additional 1 dose during the dialysis session and another dose at the end of the dialysis session (to compensate for the decrease in serum concentrations of amoxicillin and clavulanic acid)

Suspension preparation method: The suspension is prepared immediately before use. The powder in the bottle is pre-shaken, then, adding a small amount of boiled and cooled to room temperature water, mixed to obtain a homogeneous suspension, then add water to the label on the bottle. For accurate dosage of the suspension, use a double-sided dosage spoon, which must be rinsed well with water after each application. After dilution, the suspension should be stored for no more than 7 days in the refrigerator, but not frozen.

Overdose

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

Treatment: symptomatic. Hemodialysis is effective.

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 the glucose content in the urine. In this case, it is recommended to use the glucose oxidase 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.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

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

Form of production

Powder for the preparation of a suspension for oral use

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Amoxicillin, Clavulanic Acid

Conditions of release from pharmacies

By prescription

Dosage form

suspension for oral use

Purpose

Children as prescribed by a doctor, Children over 3 months of age

Indications

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