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

Powder from white to almost white with a faint fruity smell. When dissolved in water, a suspension is formed from almost white to pale yellowish with a characteristic fruiting odor.

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

ATX: & nbsp

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

Pharmacodynamics:

The medofluor 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 tropiosto to penicillinases, due to which it forms a stable complex with the enzyme, which prevents enzymatic degradation of amoxicillin under the influence of beta-lactamases.

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 5pp.(vyonecha 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 internally 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 make (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 placenta and are released in small amounts with milk.

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

It is mainly excreted by the kidneys (glomerular filtration and tubular secretion): 50 to 70% of amoxicillin and 25 to 40% of 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. The half-life after taking the drug in 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 (D, 8 - 1.2 hours). With a decrease in kidney function occurs cumulation of both components in blood plasma. Both components of the drug are removed by hemodialysis and insignificant amounts by peritoneal dialysis.

Indications:

Infectious-inflammatory diseases caused by sensitive strains of microorganisms:

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

- infections of the lower respiratory tract (acute and chronic bronchitis, lobar and bronchopneumonia, pleural empyema, 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).

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:

For oral administration, regardless of food intake. However, for optimal absorption and reduction of possible side effects from the gastrointestinal tract, the drug is recommended to be taken with meals. The dose is set individually depending on the age, body weight and severity of the infection. The standard dose is 20-40 mg / kg / day, divided into 3 doses.

Age	Body mass	Single dose (calculation for amoxicillin). Multiplicity of appointment 3 times a day.
Up to 1 year	2-9 kg	1.5 - 2.5 ml (37.5 mg - 62.5 mg)
From 1 to 5 years	10-18 kg	5.0 ml (125 mg) - 10.0 ml (250 mg)
6 to 9 years	19-28 kg	10.0 ml (250 mg) - 15.0 (375 mg)
10 to 12 years	29 - 39 kg	15.0 ml (375 mg) 20.0 ml (500 mg)
12 years and over	More than 40 kg	Usually the dose for mild and moderate infections is 250 mg (10.0 ml) 3 times a day or 500 mg (20 ml) 2 times a day

The maximum daily dose of amoxicillin for children is 45 mg / kg of body weight, the maximum daily dose of clavulanic acid is 10 mg / kg of body weight. The average course of treatment is 10 days (5-14 days).

In severe cases, doses can be doubled.

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

- for children under 12 years:

with creatinine clearance> 30 ml / min - no change in dosing regimen; at a clearance of creatinine 10-30 ml / min - 15 mg + 3.75 mg / kg (0.6 ml) 2 times / day; with the clearance of creatinine <10 ml / min - 15 mg + 3.75 mg / kg (0.6 ml) 1 time / day.

For proper dosing to children younger than 3 months and children with renal insufficiency, it is recommended to use a syringe with graduation.

Patients on hemodialysis are prescribed 15 mg + 3.75 mg / kg 1 time / day. Before the hemodialysis session, an additional 15 mg + 3.75 mg / kg is administered and a further dose of 15 mg + 3.75 mg / kg is administered after the hemodialysis session to restore the concentration of active components in the blood.

-for children over 12 years and adults:

with creatinine clearance> 30 ml / min - no change in dosing regimen; at the clearance of creatinine 10-30 ml / min - 500 mg (20.0'ml) 2 times a day or 250 mg (10.0 ml) 2 times a day;

with creatinine clearance <10 ml / min - 500 mg (20.0 ml) once a day or 250 mg (10.0 ml) once a day.

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

Method of preparing the suspension: prepare immediately before use. The powder in the vial is dissolved with boiled and chilled water, gradually mixing and adding to the label on the vial label. Then leave for 5 minutes until complete dissolution. Before each use, shake well. The ready-made Medoblava suspension is placed in a refrigerator and used for 7 days.

Side effects:

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

From the central nervous systems: 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,reversible increase in prothrombin time.

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

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

Overdose:

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

Treatment: washing the stomach, taking activated carbon, 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, NSAIDs and other 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.

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.

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

Patients with mononucleosis who receive aminopenicillin preparations have a high percentage of the risk of developing the eruptive rash. 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.

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

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

It is possible to develop superinfection due to the growth of insensitive microflora, which requires a corresponding change in antibacterial therapy.

Form release / dosage:

Powder for suspension for oral administration 125 mg + 31.25 mg / 5 ml.

Packaging:

11.78 g of powder in 100 ml glass bottles of brown glass. Screw with a screw cap: inside is an aluminum protective gasket with an atoxy-polyvinyl chloride coating.

1 bottle with instructions for use and a dosage spoon with a capacity of 5 ml is placed in a cardboard box.

Storage conditions:

The closed vial should be stored in a dry and protected from light place at a temperature not exceeding 25 ° C.

The prepared suspension should be stored in a refrigerator (2 ° - 8 ° C).

Keep out of the reach of children.

Shelf life:

Closed bottle of powder - 2 years.

The prepared suspension is 7 days.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N014290 / 02

Date of registration:20.11.2008

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

Medoklav (Medoclav)