medicalmeds.eu Medicines Antibiotic of group of penicillin of a broad spectrum of activity with inhibitor beta лактамаз. Экоклав

Экоклав

Producer: JSC AVVA RUS Russia

Code of automatic telephone exchange: J01CR02

Release form: Firm dosage forms. Tablets.

Indications to use: Lower respiratory tract infections. Bronchitis. Pneumonia. Sinusitis. Tonsillitis. Average otitis. Pyelonephritis. Pyelitis. Cystitis. Urethritis. Bacterial prostatitis. Cervicitis. Salpingitis. Salpingo-oophoritis. Endometritis. Vaginitis. Septic abortion. Abscess. Phlegmon. Wound fever. Osteomyelitis.

General characteristics. Structure:

Active agents: amoxicillin (in the form of trihydrate) 250 mg; clavulanic acid (in the form of potassium clavulanate) 125 mg

Excipients: lactulose - 300 mg, кросповидон (коллидон CL) - 24 mg, croscarmellose sodium - 24 mg, talc - 8 mg, magnesium stearate - 4 mg, cellulose microcrystallic - to 850 mg.

Structure of a film cover: mix for preparation of a film covering "Insta Moystsheld" (a gipromelloza - 54%, ethyl cellulose - 5%, diethyl phthalate - 12%, titanium dioxide - 25%, talc - 4%) - to 890 mg.

Active agents: amoxicillin (in the form of trihydrate) 500 mg; clavulanic acid (in the form of potassium clavulanate) 125 mg

Excipients: lactulose - 600 mg, кросповидон (коллидон CL) - 45 mg, croscarmellose sodium - 45 mg, talc - 12 mg, magnesium stearate - 8 mg, cellulose microcrystallic - to 1500 mg.

Active agents: amoxicillin (in the form of trihydrate) 875 mg; clavulanic acid (in the form of potassium clavulanate) 125 mg

Excipients: lactulose - 300 mg, кросповидон (коллидон CL) - 50 mg, croscarmellose sodium - 50 mg, talc - 10 mg, magnesium stearate - 10 mg, cellulose microcrystallic - to 1700 mg.

Pharmacological properties:

The combined drug of amoxicillin and clavulanic acid - inhibitor beta лактамаз. Amoxicillin – a semi-synthetic antibiotic of a wide range; works bakteritsidno, oppressing synthesis of protein of a cell wall of sensitive bacteria at growth stage. Klavulanovy acid has high affinity to bacterial beta lactamelements and forms with them a stable complex. Thus, amoxicillin biodegradation by beta lactamelements is prevented, and bactericidal activity of an antibiotic remains. Klavulanovy acid inhibits beta lactamelements of the II-V type on classification of Richmond Sykes and is not active concerning the beta laktamaz of the I type produced by Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp.
The combined drug of amoxicillin and clavulanic acid by results of tests of in vitro and clinical trials is active concerning the following microorganisms:
Gram-positive aerobic microorganisms:
Staphylococcus aureus (the strains which are producing and not producing beta lactamelements);
Gram-negative aerobic microorganisms:
Enterobacter spp. (in spite of the fact that the majority of strains of Enterobacter in vitro are steady, efficiency of drug at treatment of the infectious diseases caused by this activator is clinically proved urinary systems);
Escherichia coli (the strains which are producing and not producing beta lactamelements);
Haemophilus influenzae (the strains which are producing and not producing beta lactamelements);
Klebsiella spp. (all known strains produce beta lactamelements);
Moraxella catarrhalis (the strains which are producing and not producing beta lactamelements).
On результатм the researches in vitro sensitivity to a combination of amoxicillin and clavulanic acid of the following microorganisms is shown:
Gram-positive aerobic microorganisms:
Enterococcus faecalis **;
Staphylococcus epidermidis (the strains which are producing and not producing beta lactamelements);
Staphylococcus saprophyticus (the strains which are producing and not producing beta lactamelements);
Streptococcus pneumoniae ** (beta лактамаз does not produce);
Streptococcus pyogenes ** (beta лактамаз does not produce);
Streptococcus viridans ** (beta лактамаз does not produce).
Gram-negative aerobic microorganisms:
Eikenella corrodens (the strains which are producing and not producing beta lactamelements);
Neisseria gonorrhoeae ** (the strains which are producing and not producing beta lactamelements);
Proteus mirabilis ** (the strains which are producing and not producing beta lactamelements).
Anaerobnyemikroorganizma:
Bacteroides spp., including Bacteroides fragilis (the strains which are producing and not producing beta lactamelements);
Fusobacterium spp. (the strains which are producing and not producing beta lactamelements);
Peptostreptococcus spp. (beta лактамаз does not produce).
NOTE: ** - (efficiency of amoxicillin at treatment of a number of the infections caused by these activators is clinically proved).
The lactulose which is a part Ekoklava as a bifidogenny factor is synthetic disaccharide which molecule consists of the remains of a galactose and fructose. Lactulose in a stomach and upper parts of intestines is not soaked up and not hydrolyzed. The lactulose which is released from tablets Ekoklava as substrate is fermented by normal microflora of a large intestine, stimulating growth of bifidobacteria and lactobacilli. As a result of hydrolysis of lactulose in a large intestine organic acids - milk, acetic and ant, suppressing growth of pathogenic microorganisms and reducing thereof products of nitrogen-containing toxic substances are formed.
Thus, lactulose in structure Ekoklava reduces the damaging action of an antibiotic on the normal intestinal microflora and risks of side effects connected with disbioza.

Pharmacokinetics. Absorption. After intake both components of drug are quickly soaked up from digestive tract. Absorption of active ingredients of drug is optimum in case of its reception at the beginning of food.
After intake in a dose of 250 mg +125 mg:
- the maximum concentration (Cmax) of amoxicillin – 3.7 mkg/ml, clavulanic acid – 2.2 mkg/ml;
- time of achievement of the maximum concentration (Tmax) of amoxicillin – 1.1 h, clavulanic acid – 1.2 h;
- the area under a curve "concentration time" (AUC) of amoxicillin – 10.9 mg • h/l, clavulanic acid – 6.2 mg • h/l.
After intake in a dose of 500 mg +125 mg:
- Cmax of amoxicillin – 6.5 mkg/ml, clavulanic acid – 2.8 mkg/ml;
- Tmax of amoxicillin is 1.5 h, clavulanic acid – 1.3 h;
- AUC amoxicillin – 23.2 mg • h/l, clavulanic acid – 7.3 mg • h/l.
After intake in a dose of 875 mg +125 mg:
- Cmax of amoxicillin – 8.8 mkg/ml, clavulanic acid – 2.07 mkg/ml;
- Tmax of amoxicillin is 1.5 h, clavulanic acid – 1.5 h;
- AUC amoxicillin – 25.4 mg • h/l, clavulanic acid – 6.1 mg • h/l.
At use of drug of concentration of amoxicillin in blood serum are similar to those at oral administration of equivalent doses of one amoxicillin.

Distribution. Both components of drug are characterized by the good volume of distribution – therapeutic concentration of amoxicillin and clavulanic acid are created in various bodies and fabrics, intersticial liquid: lungs, middle ear, abdominal organs, bodies of a small pelvis (prostate gland, uterus, ovaries), skin; fatty, bone and muscular fabrics; pleural, synovial and peritoneal liquids; to plasma, bile, purulent separated, a phlegm, a bronchial secret.
Amoxicillin and clavulanic acid possess moderate extent of linkng with proteins of plasma, respectively, for 18% and 25%.
Both components of drug get through a placental barrier, however data on a negative impact on a fruit are not published.
Amoxicillin and clavulanic acid in low concentration are found in breast milk.

Metabolism, removal. About 60-70% of amoxicillin are removed by kidneys: by canalicular secretion and glomerular filtering. Clavulanic acid actively metabolizes in a liver and is removed by glomerular filtering (40-65%), partially in the form of metabolites. A smaller part is removed by intestines.
At a renal failure the clearance of amoxicillin with clavulanic acid decreases therefore dose adjustment is required.
The lactulose which is a part Ekoklava does not exert impact on the key pharmacokinetic parameters characterizing bioavailability of amoxicillin and clavulanic acid.

Indications to use:

The infectious and inflammatory diseases caused by activators, sensitive to drug:
— lower respiratory tract infections (bronchitis, pneumonia);
— infections of ENT organs (sinusitis, tonsillitis, average otitis);
— infections of urinogenital system and bodies of a small pelvis (pyelonephritis, pyelitis, cystitis, urethritis, bacterial prostatitis, cervicitis, salpingitis, salpingo-oophoritis, endometritis, bacterial vaginitis, septic abortion, venereal ulcer, gonorrhea);
— infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis, abscess, phlegmon, a wound fever);
— infections of bones and joints (osteomyelitis).

Route of administration and doses:

Inside. The mode of dosing is set individually depending on age and the body weight of the patient, weight of a current and localization of infectious process, and also sensitivity of the activator.
The minimum course of antibacterial therapy - of 5 days. It is longer not necessary to continue treatment 14 days without review of a clinical situation.
To adults and children 12 years or with body weight more than 40 kg are more senior:
Slight and medium-weight infections – 1 tablet on 250 mg +125 mg 3 times a day or 1 tablet on 500 mg +125 mg 2 times a day.
Heavy infections or lower respiratory tract infections – 1 tablet on 875 mg +125 mg 2 times a day or 1 tablet on 500 mg +125 mg 3 times a day.
As tablets contain identical amount of clavulanic acid (125 mg), it is necessary to consider that 2 tablets on 250 mg +125 mg are not equivalent to 1 tablet on 500 mg +125 mg.
The maximum daily dose of amoxicillin for adults and children is more senior than 12 years - 6 g, clavulanic acid - 600 mg.
At a chronic renal failure carry out dose adjustment and frequency rates of reception depending on the clearance of creatinine (CC):
— at KK more than 30 ml/min. of dose adjustment are not required;
— at KK of 10-30 ml/min.: 1 tablet on 250 mg +125 mg of 2 times/days (at slight and medium-weight infections) or 1 tablet on 500 mg +125 mg of 2 times/days (at heavy infections or lower respiratory tract infections);
— at KK less than 10 ml/min.: 1 tablet on 250 mg +125 mg of 1 time/days (at slight and medium-weight infections) or 1 tablet on 500 mg +125 mg of 1 time/days (at heavy infections or lower respiratory tract infections);
The patients who are on a hemodialysis: 1 tablet on 500 mg +125 mg or 2 tablets on 250 mg +125 mg each 24 hours in combination with 1 dose during a hemodialysis and 1 dose after a hemodialysis as concentration of amoxicillin and clavulanic acid decreases.

Features of use:

Expressiveness of gastrointestinal symptoms decreases at administration of drug at the beginning of food.

At course treatment it is necessary to carry out control of a condition of function of bodies of a hemopoiesis, a liver and kidneys.

Development of superinfection due to selection of resistant forms of the activator is possible.

False positive results when determining content of glucose in urine can be revealed. In this case it is recommended to apply a glyukozooksidazny method of definition of concentration of glucose in urine.

At the patients having hypersensitivity to penicillin cross allergic reactions with tsefalosporinovy antibiotics are possible.

In case of suspicion on an infectious mononucleosis drug should not be used as with this disease amoxicillin can cause korepodobny skin rash in patients that complicates diagnosis of a disease.

Considering probability of development of side effects from the central nervous system, it is necessary to be careful at control of vehicles and work with moving mechanisms.

Side effects:

Drug is well transferred. Side effects arise seldom, happen preferential slight and have tranzitorny character.
From the alimentary system: nausea, vomiting, diarrhea, gastritis, stomatitis, a glossitis, cholestatic jaundice, hepatitis, a liver failure (is more often at elderly, men, at long therapy), colitis (including pseudomembranous), black "hairy" language, darkening of an adamantine substance of tooth, increase in activity of "hepatic" transaminases, increase in content of bilirubin and activity of an alkaline phosphatase.
From bodies of a hemopoiesis: reversible increase in a prothrombin time and bleeding time, thrombocytopenia, thrombocytosis, eosinophilia, leukopenia, agranulocytosis, hemolitic anemia.
From the central nervous system: dizziness, headache, hyperactivity, alarm, change of behavior, spasm.
Allergic reactions: urticaria, erythematic rashes, multiformny exudative erythema, acute anaphylaxis, Quincke's disease, exfoliative dermatitis, malignant exudative erythema (Stephens-Johnson's syndrome), allergic vasculitis, syndrome similar to a serum disease, acute generalized exanthematous пустулез.
From kidneys and urinary tract: intersticial nephrite, crystalluria, hamaturia.
Others: candidiasis, development of superinfection.

Interaction with other medicines:

It is not recommended to use the combined drug of amoxicillin and clavulanic acid along with probenetsidy. Probenetsid reduces canalicular secretion of amoxicillin therefore their combined use can lead to increase and a persistention of concentration of amoxicillin in serum, at the same time serumal concentration of clavulanic acid does not change.

Diuretics, Allopyrinolum, phenylbutazone, the non-steroidal anti-inflammatory drugs and other medicines blocking canalicular secretion increase concentration of amoxicillin (clavulanic acid is removed generally by glomerular filtering).

Antacids, glycosamine, purgatives slow down and reduce amoxicillin absorption; ascorbic acid - raises.

Allopyrinolum increases risk of developing of skin rash.

As well as efficiency of oral contraceptives can reduce other antibiotics of a broad spectrum of activity, the combined drug of amoxicillin and clavulanic acid, and patients need to be informed on it.

In literature exceptional cases of increase in the international normalized relation (INR) at patients at combined use of an atsenokumarol or warfarin and amoxicillin are described. In need of simultaneous primeneniyakombinirovanny drug of amoxicillin and clavulanic acid with indirect anticoagulants the prothrombin time or MNO have to monitorirovatsya carefully at appointment or drug withdrawal.

Contraindications:

— hypersensitivity (including to cephalosporins and another beta лактамным to antibiotics);
— infectious mononucleosis;
— episodes of jaundice or an abnormal liver function as a result of use of amoxicillin/clavulanic acid in the anamnesis;
— children's age up to 12 years or at body weight less than 40 kg (for this dosage form);
— a chronic renal failure (clearance of creatinine less than 30 ml/min.) for tablets with a dosage of 875 mg +125 mg.
With care: a heavy liver failure, digestive tract diseases (including the colitis in the anamnesis connected using penicillin), a chronic renal failure.

Use of the drug EKOKLAV® at pregnancy and feeding by a breast
It is recommended to appoint the combined drug of amoxicillin and clavulanic acid at pregnancy only in cases when the expected advantage of its reception for mother exceeds potential risk for a fruit.
Drug can be used during breastfeeding. Except for the risk of a sensitization connected with penetration into breast milk of trace amounts of active ingredients of this drug, any other adverse effects at the babies who are on breastfeeding it was not revealed.

Use at abnormal liver functions
With care it is applied at a heavy liver failure

Use at renal failures
It is contraindicated at a chronic renal failure (clearance of creatinine less than 30 ml/min.) for tablets with a dosage of 875 mg +125 mg.
At a chronic renal failure carry out dose adjustment and frequency rates of reception depending on the clearance of creatinine (CC).

Use for children
It is contraindicated to children up to 12 years or at body weight less than 40 kg (for this dosage form).