Medoklav - instructions for use, dose, side effects, contraindications

Tablets 250 mg + 125 mg - white or almost white in color, shaped like a capsule, biconvex, covered with a film sheath, with an embossed "MS" on one side and a dividing risk on the other side.

Tablets 500 mg + 125 mg - white or almost white, shaped like a capsule, biconvex, covered with a film sheath.

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

ATX: & nbsp

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

Pharmacodynamics:

Medoklav® is a combined preparation containing amoxicillin and clavulanic acid. Amoxicillin is a semisynthetic antibiotic from the group of aminopenicillins with a broad spectrum of bactericidal action against many Gram-positive and Gram-negative microorganisms. Clavulanic acid is a natural β-lactam and has the ability to inactivate a variety of β-lactamases produced by microorganisms resistant to the action of most penicillins and many cephalosporins.

The combination of the two active components - amoxicillin and clavulanic acid - ensures the stability of amoxicillin to the destructive effect of β-lactamases, and effectively expands the spectrum of antimicrobial activity of amoxicillin, including bacteria that are usually resistant to it and many other β-lactam antibiotics.

Clavulanic acid suppresses II, III, IV and V types of beta-lactamases, is inactive for type I beta-lactamases produced Enterobacter spp., Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp. Clavulanic acid has a high tropic to penicillinases, due to which it forms a stable complex with the enzyme,which prevents the enzymatic degradation of amoxicillin under the influence of beta-lactamases.

Spectrum of antibacterial activity:

Gram-positive microorganisms

Aerobics: Enterococcus faecalis, Staphyloccocus aureus (except methicillin-resistant strains), Staphylococcus epidermidis (except methicillin-resistant strains), Staphylococcus saprophyticus (except methicillin-resistant strains), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus bovis, Enterococcus spp., Listeria spp..

Anaerobes: Clostridium spp. (Besides Clostridium difficile), Peptococcus spp., Peptostreptococcus spp., Propionibacterium spp., Actinomyces israelii.

Gram-negative microorganisms

Aerobics: Bordetella pertussis, Brucella spp, Campylobacter jejuni, Campylobacter coli, Citrobacter spp.. (moderately sensible), Enterobacter species, Escherichia coli, Eikenella corrodens, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae, Helicobacter pylori, Klebsiella spp., Legionella pneumophila, Moraxella catarrhalis, Morganella spp. (moderately sensitive), Neisseria gonorrhoeae, Neisseria meningitidis, Yersinia multocida, Proteus spp., Salmonella spp., Shigella spp., Vibrio cholerae, Yersinia enterocolitica (moderately sensitive).

Anaerobes: Bacteroides spp.(including Bacteroides fragilis), Fusobacterium spp.

Pharmacokinetics:

The pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. The combined use of amoxicillin and clavulanic acid does not affect the pharmacokinetic properties of each of these substances, as if they were applied separately. Both components are highly bioavailable. 80 - 90% of amoxicillin trihydrate, taken orally, is absorbed from the gastrointestinal tract. Amoxicillin Preserves stability in the presence of hydrochloric acid, food does not affect the degree of absorption.

The maximum concentration of amoxicillin in the blood is reached 1 hour after taking the drug and is (depending on the dose) an average of 5 μg / ml, and for clavulanic acid - about 2 μg / ml.

Both components of the drug quickly diffuse into most tissues and body fluids. High concentrations of active substances are found in sputum, bronchial secretion, pleural fluid, pulmonary and adipose tissue, prostate gland, etc.

Amoxicillin and clavulanic acid penetrate the placental barrier and are released in small amounts with milk.

Binding to plasma proteins is low in both amoxicillin and clavulanic acid: amoxicillin it binds to proteins by 17-21% (on average by 20%), clavulanic acid by 30%.

It is excreted mainly by the kidneys (glomerular filtration and tubular secretion): 50 -70% amoxicillin and 25-40% clavulanic acid are secreted unchanged by the kidneys during the first 6 hours after administration, in part small amounts are excreted through the intestine and lungs.Half-life after taking the drug at a dose of 375 and 625 mg for amoxicillin is 1 - 1.5 hours (on average - 1.3 hours), for clavulanic acid - about 1 hour (0.8-1.2 hours).

With a decrease in renal function, both components in the blood plasma are cumulated. Both components of the drug are removed by hemodialysis and insignificant amounts by peritoneal dialysis.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

- infection of the upper respiratory tract and ENT organs (sinusitis, pharyngitis, tonsillitis, otitis media, retropharyngeal abscess);

- infection of the lower respiratory tract (acute and chronic bronchitis, lobar and bronchopneumonia, empyema of the pleura, lung abscess);

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

- infection of the biliary tract (cholangitis, cholecystitis);

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

- intestinal infections (dysentery, salmonellosis, salmonella carriage),

- osteomyelitis.

Contraindications:

Hypersensitivity in the anamnesis on the antibiotics of the penicillin series, etc. beta-lactam antibiotics.

Infectious mononucleosis (including when there is a measles-like rash).

Children under 12 years (for this dosage form).

Carefully:

With pseudomembranous colitis in history, liver failure, severe impairment of kidney function.

Pregnancy and lactation:

In pregnancy, you can only use if the intended benefit for a pregnant woman exceeds the potential risk to the fetus;

During lactation: amoxicillin and clavulanic acid in small amounts excreted in breast milk, so when prescribing the drug should stop breastfeeding.

Dosing and Administration:

Inside, regardless of food intake. The dose is set individually depending on the severity of the disease, the localization of infection and the sensitivity of the pathogen.

Adults and children over 12 years of age (weight ≥40 kg): Usually the dose for a mild and moderate infection is: 1 tablet Medoklava® (250 mg + 125 mg) 3 times a day or 1 tablet 500 mg + 125 mg 2 times a day.

In severe infection - 1 tablet Medoblava® (500 mg + 125 mg) 3 times a day or 1 tablet Medoblava® (875 mg + 125 mg) 2 times a day.

The maximum daily dose of amoxicillin is 6 g, the maximum daily dose of clavulanic acid (potassium salt) for adults is 600 mg. The course of treatment is an average of 10 days (5-14 days).

In chronic renal failure, rapid dosing depends on the clearance of creatinine:

with creatinine clearance> 30 ml / min - no change in dosing regimen; at a creatinine clearance of 10-30 ml / min - 1 tablet 500 mg + 125 mg 2 times a day or 1 tab. 250 mg + 125 mg 2 times a day (depending on the severity of the course of the disease); with a clearance of creatinine <10 ml / min - 1 table. 500 mg + 125 mg / day in a single dose or 1 table. 250 mg + 125 mg once a day (depending on the severity of the disease). Tablets 875 mg + 125 mg should be given only to patients with a creatinine clearance greater than 30 ml / min.

For anuria, the interval between dosing should be increased to 48 hours or more.

For children under 12 years (weight less than 40 kg), it is preferable to prescribe the drug in the form of a suspension (dosage form: powder for the preparation of a suspension for oral administration).

Side effects:

From the digestive system: nausea, vomiting, diarrhea, increased activity of "liver" transaminases, glossitis, candidiasis of mucous membranes, enterocolitis, hemorrhagic or pseudomembranous colitis. In isolated cases - cholestatic jaundice, hepatitis.

From the central nervous system: headache, dizziness, psychomotor agitation, insomnia, anxiety, cramps.

Allergic reactions: skin rashes, itching, hives, erythematous rashes; rarely - multiforme exudative erythema, anaphylactic shock, angioedema; in isolated cases - exfoliative dermatitis, Stevens-Johnson syndrome.

From the hematopoietic system: anemia, thrombocytopenia, eosinophilia, leukopenia and agranulocytosis, a reversible increase in prothrombin time.

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

Other: arthritis, joint pain, fever, development of superinfection.

Overdose:

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

Treatment: gastric lavage, intake of activated charcoal, etc.Hemodialysis can be effective.

Interaction:

Antacids, glucosamine, laxatives, aminoglycosides slow down and reduce absorption, ascorbic acid increases absorption.

Probenecid reduces tubular secretion of amoxicillin, increasing the concentration of amoxicillin in the serum.

Bactericidal antibiotics, in particular, aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin have a synergistic effect.

Bacteriostatic antibiotics (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) have an antagonistic effect.

Strengthens the effect of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index).

Reduces the effectiveness of oral contraceptives.

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

Allopurinol increases the risk of developing exanthema.

Simultaneous reception with methotrexate increases the toxicity of methotrexate.

At simultaneous reception with preparations in the course of metabolism of which para- aminobenzoic acid (PABA), ethinyl estradiol is formed, there is a risk of development of bleeding "breakthrough".

Special instructions:

Make sure that there is no hypersensitivity to penicillins, cephalosporins and other allergens in the history. In patients who have increased sensitivity to penicillins, cross-reactions with cephalosporin antibiotics are possible.

In case of an allergic reaction, it is necessary to stop treatment and switch to alternative therapy. Allergic reactions can be stopped with antihistamines or, if necessary, with systemic glucocorticosteroids.

In patients with mononucleosis receiving aminopenicillin preparations, a high percentage of the risk of developing the erythematous eruption was noted. Therefore, ampicillins should not be administered to patients with mononucleosis

At course treatment it is necessary to monitor the state of the kidneys, liver and hematopoiesis system.

Patients with severe impaired renal function should adjust the dose of the drug or increase the interval between doses.

It should be remembered that 2 tablets Medoblava® 250 mg + 125 mg are not identical to 1 tablet of 500 mg + 125 mg because contain a different amount of clavulanic acid.

To reduce the risk of side effects from the gastrointestinal tract, you should use the drug while eating.

In laboratory diagnostics, when determining glucose in urine, it is recommended to use enzymatic reactions with glucosidase, since When using a Benedict reagent or Felling solution, false positive results can be obtained.

Form release / dosage:

Tablets coated with a film sheath 250 + 125 mg and 500 + 125 mg.

Packaging:

For 8 tablets in a blister of PVC / aluminum foil with an additional coating of PVC layer with aluminum foil.

2 blisters together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N014290 / 03

Date of registration:15.01.2009 / 24.06.2009

Expiration Date:Unlimited

The owner of the registration certificate:Medocemi Co., Ltd.Medocemi Co., Ltd. Cyprus

Manufacturer: & nbsp

MEDOCHEMIE, Ltd. Cyprus

Representation: & nbspMEDOKEMI LTD. MEDOKEMI LTD. Cyprus

Information update date: & nbsp26.04.2018

Illustrated instructions

Instructions

Medoflav® (Medoclav)