Composition, form of production and packaging
Tablets covered with a film membrane of white or almost white color, oval, biconcave; on the cross-section of the nucleus from almost white to light yellow with a brown tinge, white to yellow inclusions are permissible.
1 tab.
amoxicillin (in the form of trihydrate) 250 mg
clavulanic acid (in the form of potassium clavulanate) 125 mg
Auxiliary substances: lactulose - 300 mg, crospovidone (kollidon CL) - 24 mg, croscarmellose sodium - 24 mg, talc - 8 mg, ascorbic acid 5 mg, magnesium stearate 5.2 mg, microcrystalline cellulose up to 1040 mg.
The composition of the film shell: a mixture for the preparation of the film coating Insta Moyshsled (hypromellose - 54%, ethyl cellulose - 5%, diethyl phthalate - 12%, titanium dioxide - 25%, talc - 4%) - up to 1089 mg.
5 pieces. - packings cellular planimetric aluminum (1, 2, 3) - packs cardboard.
7 pcs. - packings cellular planimetric aluminum (1, 2, 3) - packs cardboard.
14 pcs. - plastic bottles (1) - packs of cardboard.
15 pcs. - plastic bottles (1) - packs of cardboard.
14 pcs. - polymer cans (1) - packs of cardboard.
15 pcs. - polymer cans (1) - packs of cardboard.
Tablets covered with a film membrane of white or almost white color, oval, biconcave; on the cross-section of the nucleus from almost white to light yellow with a brown tinge, white to yellow inclusions are permissible.
1 tab.
amoxicillin (in the form of trihydrate) 500 mg
clavulanic acid (in the form of potassium clavulanate) 125 mg
Excipients: lactulose - 600 mg, crospovidone (kollidon CL) - 45 mg, croscarmellose sodium - 45 mg, talcum - 12 mg, ascorbic acid - 5 mg, magnesium stearate - 13.84 mg, microcrystalline cellulose up to 1730 mg.
The composition of the film shell: a mixture for the preparation of the film coating Insta Moysheld (54% for hypromellose, 5% for ethyl cellulose, 12% for diethyl phthalate, 25% for titanium dioxide, 4% for talc) to 1774.3 mg.
5 pieces. - packings cellular planimetric aluminum (1, 2, 3) - packs cardboard.
7 pcs. - packings cellular planimetric aluminum (1, 2, 3) - packs cardboard.
14 pcs. - plastic bottles (1) - packs of cardboard.
15 pcs. - plastic bottles (1) - packs of cardboard.
14 pcs. - polymer cans (1) - packs of cardboard.
15 pcs. - polymer cans (1) - packs of cardboard.
Tablets covered with a film membrane of white or almost white color, oval, biconcave; on the cross-section of the nucleus from almost white to light yellow with a brown tinge, white to yellow inclusions are permissible.
1 tab.
amoxicillin (in the form of trihydrate) 875 mg
clavulanic acid (in the form of potassium clavulanate) 125 mg
Auxiliary substances: lactulose - 300 mg, crospovidone (collidon CL) - 50 mg, croscarmellose sodium - 50 mg, talc - 10 mg, ascorbic acid - 5 mg, magnesium stearate - 18.5 mg, microcrystalline cellulose - up to 1850 mg.
The composition of the film shell: a mixture for the preparation of the film coating Insta Moyshedd (hypromellose - 54%, ethyl cellulose - 5%, diethyl phthalate - 12%, titanium dioxide - 25%, talc - 4%) - to 1887.7 mg.
5 pieces. - Cellular outline packaging (PVC / aluminum) (1, 2) - cardboard packs.
7 pcs. - Cellular outline packaging (PVC / aluminum) (1, 2) - cardboard packs.
5 pieces. - packings of cellular contoured aluminum (1, 2) - packs cardboard.
7 pcs. - packings of cellular contour aluminum (1, 2) - packs cardboard.
5 pieces. - plastic bottles (1) - packs of cardboard.
7 pcs. - plastic bottles (1) - packs of cardboard.
10 pieces. - plastic bottles (1) - packs of cardboard.
14 pcs. - plastic bottles (1) - packs of cardboard.
5 pieces. - polymer cans (1) - packs of cardboard.
7 pcs. - polymer cans (1) - packs of cardboard.
10 pieces. - polymer cans (1) - packs of cardboard.
14 pcs. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Combined drug, which includes amoxicillin and clavulanic acid, an inhibitor of О±-lactamase.
Amoxicillin is a semisynthetic broad-spectrum antibiotic; acts bactericidal, inhibiting the synthesis of the protein of the cell wall of sensitive bacteria at the growth stage.
Clavulanic acid has a high affinity for bacterial ОІ-lactamases and forms a stable complex with them. Thus, biodegradation of amoxicillin with О±-lactamases is prevented, and bactericidal activity of the antibiotic is preserved. Clavulanic acid inhibits type II II-V lactamase according to the Richmond-Sykes classification and is not active against type I ОІ-lactamases produced by Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp.
The combination of amoxicillin and clavulanic acid by results of in vitro and clinical trials is active against the following microorganisms : Gram-positive aerobic microorganisms - Staphylococcus aureus (strains producing and not producing? -lactamases); Gram-negative aerobic microorganisms - Enterobacter spp. (despite the fact that most Enterobacter strains are stable in vitro, the efficacy of the drug has been clinically proven in the treatment of infectious diseases of the urinary system caused by this pathogen), Escherichia coli (strains producing and not producing? -lactamases), Haemophilus influenzae (strains producing and not producing ОІ-lactamases), Klebsiella spp. (all known strains produce? -lactamases), Moraxella catarrhalis (strains producing and not producing? -lactamases).
According to the results of in vitro studies, sensitivity to the combination of amoxicillin and clavulanic acid in the following microorganisms is shown: gram-positive aerobic microorganisms - Enterococcus faecalis **, Staphylococcus epidermidis (strains producing and not producing? -lactamases), Staphylococcus saprophyticus (strains that produce and do not produce? - lactamase), Streptococcus pneumoniae ** (? -lactamases does not produce), Streptococcus pyogenes ** (? -lactamase does not produce), Streptococcus viridans ** (? -lactamases does not produce); Gram-negative aerobic microorganisms - Eikenella corrodens (strains producing and not producing? -lactamases), Neisseria gonorrhoeae ** (strains producing and not producing? -lactamases), Proteus mirabilis ** ( strains producing and not producing? -lactamases); anaerobic microorganisms - Bacteroides spp., including Bacteroides fragilis (strains producing and not producing? -lactamases), Fusobacterium spp.(strains producing and not producing? -lactamases), Peptostreptococcus spp. (? -lactamase does not produce).
Note: ** - Amoxicillin has been clinically proven for treating a number of infections caused by these pathogens.
PHARMACOKINETICS
Suction
After oral administration, both components of the drug are rapidly absorbed from the digestive tract. Absorption of active ingredients of the drug is optimal in case of its intake at the beginning of the meal. After oral administration at a dose of 250 mg + 125 mg C max of amoxicillin is 3.7 Ојg / ml, clavulanic acid - 2.2 Ојg / ml; time to reach the maximum concentration (T max ) amoxicillin - 1.1 h, clavulanic acid - 1.2 h; AUC amoxicillin - 10.9 mg h / l, clavulanic acid - 6.2 mg h / l. After oral administration at a dose of 500 mg + 125 mg C max of amoxicillin is 6.5 Ојg / ml, clavulanic acid is 2.8 Ојg / ml; T max 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 in a dose of 875 mg + 125 mg C max of amoxicillin is 8.8 Ојg / ml, clavulanic acid - 2.07 Ојg / ml; T max 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 good Vd - therapeutic concentrations of amoxicillin and clavulanic acid are created in various organs and tissues, interstitial fluid: lungs, middle ear, abdominal organs, pelvic organs (prostate gland, uterus, ovaries), skin; fatty, 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 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 and excretion
Approximately 60-70% of amoxicillin is excreted by the kidneys through tubular secretion and 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 smallest part is excreted through the intestine.
Pharmacokinetics in special clinical cases
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).
DOSING MODE
The drug is taken orally. 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
For mild and moderate infections , 1 tablet is prescribed. 250 mg + 125 mg 3 times / day or 1 tab. 500 mg + 125 mg 2 times / day.
In severe infections or infections of the lower respiratory tract , 1 tablet is prescribed. 875 mg + 125 mg 2 times / day or 1 tab. 500 mg + 125 mg 3 times / day.
Since 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 to 1 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 failure , dose adjustment and frequency of administration are performed depending on the CC:
- with QC more than 30 ml / min dose adjustment is not required;
- with KK 10-30 ml / min: 1 tab. 250 mg + 125 mg 2 times / day (for mild and moderate infections) or 1 tab. 500 mg + 125 mg 2 times / day (for severe infections or infections of the lower respiratory tract);
- with QC less than 10 ml / min: 1 tab. 250 mg + 125 mg 1 time / day (for mild and moderate infections) or 1 tab. 500 mg + 125 mg 1 time / day (for severe infections or infections of the lower respiratory tract).
Patients on hemodialysis are prescribed 1 tablet. 500 mg + 125 mg or 2 tab. 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 EFFECT
The drug is well tolerated. Side effects occur rarely, mostly weakly expressed and are transient in nature.
From the side of the digestive system: nausea, vomiting, diarrhea, gastritis, stomatitis, glossitis, cholestatic jaundice, hepatitis, hepatic insufficiency (more often in the elderly, men, with prolonged therapy), colitis (including pseudomembranous), black hairy tongue, enamel, increased activity of hepatic transaminases, an increase in bilirubin and alkaline phosphatase activity.
From the hemopoietic system: reversible increase in prothrombin time and bleeding time, thrombocytopenia, thrombocytosis, eosinophilia, leukopenia, agranulocytosis, hemolytic anemia.
From the side of the central nervous system: dizziness, headache, hyperactivity, anxiety, behavior change, convulsions.
From the urinary system: interstitial nephritis, crystalluria, hematuria.
Allergic reactions: urticaria, erythema rheumatism, erythema multiforme exudative, anaphylactic shock, angioedema, exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), allergic vasculitis, a syndrome similar to serum sickness, acute generalized exanthematous pustulosis.
Other: Candidiasis, development of superinfection.
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;
- chronic renal failure (CK less than 30 ml / min) for tablets with a dosage of 875 mg + 125 mg.
With caution should prescribe the drug for severe hepatic insufficiency, gastrointestinal diseases (including with colitis in the history associated with the use of penicillins), chronic renal failure.
PREGNANCY AND LACTATION
The drug EcoKlav В® is recommended to prescribe during pregnancy only in cases when the expected benefit from its reception for the mother exceeds the potential risk to 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.
APPLICATION FOR FUNCTIONS OF THE LIVER
With adiposity , the drug should be prescribed for chronic renal failure.
Contraindicated in chronic renal failure (CK less than 30 ml / min) for tablets with a dosage of 875 mg + 125 mg.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With the severity of the drug should be prescribed for severe hepatic insufficiency.
The use of the drug is contraindicated in cases of jaundice or a violation of liver function as a result of the use of amoxicillin / clavulanic acid in the anamnesis.
APPLICATION FOR CHILDREN
The drug is prescribed for children from 12 years old or with a body weight of more than 40 kg.
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.
In patients who have increased sensitivity to penicillins, cross-allergic reactions with antibiotics of the cephalosporin group are possible.
In case of suspected infectious mononucleosis, the drug should not be used, as in patients with this disease, amoxicillin can cause a skinlike skin rash, which makes it difficult to diagnose the disease.
Impact on the ability to drive vehicles and manage mechanisms
Given the likelihood of side effects from the CNS, caution should be exercised in situations requiring increased concentration of attention, incl. when driving vehicles and working with machinery.
OVERDOSE
Symptoms: a violation of the function of the gastrointestinal tract and water-electrolyte balance.
Treatment: conduct symptomatic therapy. Hemodialysis is effective.
DRUG INTERACTION
It is not recommended to use EcoKlav В® 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, NSAIDs 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 drug EcoklavВ® can reduce the effectiveness of oral contraceptives; patients should be informed about this.
In the literature, rare cases of an increase in INR in patients with the joint use of acenocoumarol or warfarin and amoxicillin are described. If it is necessary to simultaneously prescribe the preparation EcoKlav В® with indirect anticoagulants prothrombin time or INR should be carefully monitored when the drug is prescribed or withdrawn.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years. Do not use after the expiration date.
