Amoxicillin clavulanic acid suspension for children. Amoxicillin with clavulanic acid

05.06.2020

Amoxiclav (Lat. AMOXYCLAV, English Amoksiclav) - Antibiotic wide spectrum Actions related to the group of inhibitors of penicillins. Contains a combination of amoxicillin and clavulanic acid. It has a bactericidal effect due to the oppression of the synthesis of cell walls of microorganisms. Due to the high activity and good tolerability, it can be used as a drug for "empirical" (conducted before obtaining results of analyzes) antibiotic therapy. The spectrum of indications includes the infections of the ENT organs, the respiratory tract, the urogenital path, the skin, soft tissues, bones and joints.

The history of antibiotics began with the opening of the English scientist Alexander Fleming, who discovered antimicrobial properties active substance Mushroom Penicillum Notatum. In 1940, Ernst Chein and Howard Flori allocated the compound described by them in its pure form and called it penicillin. Since then, the drug has become used in medical practice.

In the 1950s It was found that the structural unit of Penicillin is the β-lactam ring. This discovery made possible synthesis of new antibacterial drugs. So, in 1960, meticillin was obtained, in 1961 - ampicillin, and in 1962 amoxicillin. The latter differed from its predecessors improved pharmacokinetic characteristics and higher antibacterial activity.

All penicillins were effective in relation to a wide range. infectious diseasesHowever, over time, they caused the emergence of the strains of microorganisms resistant to them. This effect It was explained by the ability of bacteria to produce β-lactamases - special enzymes that destroy β-lactam rings of antibiotics.

The search for substances capable of neutralizing the effect of harmful enzymes was made by various scientists since 1956. But the first success was achieved only in 1970 by the British pharmaceutical pharmaceutical company Beechham Pharmaceuticals (now GlaxosmithKline). From the culture of Streptomyces Clavuligeris, they allocated the first Blocator β-lactamaz - clavulanic acid. By combining a tool with amoxicillin, the developers received an inhibitory-proof antibiotic, to which the steady stamped bacteria strains turned out to be sensitive. The drug was released to the market in 1984 under the Augmentin brand.

In the mid-1980s. Scientific research on obtaining β-lactamase blockers also concluded Slovenian LEK Figure Permium. Its biochemists managed to derive its own cell culture for the synthesis of clavulanic acid. In 1989, the company registered Generic Augmentin, called Amoxiclav.

Properties

International unpatient name: amoxicillin / clavulanic acid (ang. AMOXICILLIN / CLAVULANIC ACID).

Title on the British Pharmacopoeia (BAN): Co-Amoxiclav (Eng. Co-amoxiclav).

Chemical names of operating substances according to the Nomenclature of the Jew:

1) amoxicillin -] -6 - [[[amino- (4-hydroxyphenyl) acetyl] amino] -3,3-dimethyl-7-oxo-4-TIA-1-Azabicycakeptane-2-carboxylic acid,

2) Clawulanic acid - (2R, 5R, Z) -3- (2-hydroxyethylidene) -7-oxo-4-oxa-1-azabicyclo-heptane-2-carboxylic acid.

Structural formulas:

Physical properties:

Amxicillin is white or slightly yellowish powder, a little soluble in water. Melting point - 403.3ºС. Molecular weight - 419.45.

Clawulanic acid - white powder, well soluble in water. Melting point - 283.9ºС. Molecular weight - 199,16.

Composition, output, packaging

The drug is produced in the form of tablets, powder for the preparation of suspensions and lyophilisate for the preparation of a parenteral solution with various dosages of active ingredients.

Dosage form	The content of amoxicillin in one dose of the drug, mg	Content of clavulanic acid in one dose of the drug, mg
Tablets coated with intestinal shell, 375 mg	250	125
Tablets coated with intestinal solubular shell, 625 mg	500	125
Tablets covered with intestinal-soluble shell, 1000 mg	875	125
Powder for cooking 9.14% suspension	400	57
Powder for cooking 6.25% suspension	250	62,5
Powder for cooking 3,125% suspension	125	31,25
Lyophilisate for the preparation of a parenteral solution in bottles of 0.6 g	500	100
Lyophilisate for the preparation of a parenteral solution in bottles of 1.2 g	1000	200
Dispersible Tablets (Amoxiclav Kviktab) 625 mg	500	125
Tablets dispersible 1000 mg	875	125

Tablets are fusing in dark glass bottles or blister. The contents of one package is designed for 5-14 days of use.

The powder for obtaining a suspension is packaged in dark bottles with a dosing spoon or pipette. The glass has a label intended for the preparation of the established volume of the solution.

Florals with lyophilisate are placed in cardboard packs of 5 pieces.

Mechanism of action

Like all other beta-lactam antibiotics, amoxicillin exhibits bactericidal properties. The main target of its actions are peptides binding proteins that perform the role of enzymes in the synthesis of the cell walls of bacteria. The blockade of the building process leads to the death of microorganisms. Since peptides binding proteins are absent in humans, then at its cells amoxicillin toxic influence does not have.

Clawulanic acid is characterized by high affinity for beta lactamases, which are produced by bacteria and cause the hydrolysis of penicillins. Forming with aggressive enzymes strong chemical bonds, Clawulanate protects the antibiotic molecules from destruction. There is evidence that acid also shows its own bactericidal properties.

Spectrum of antimicrobial activity

In comparison with natural penicillins, amoxicillin has an extended spectrum of antibacterial activity.

The drug is detrimental to:

gram-positive cocci (Streptococcus Pneumoniae, Strept. Pyogenes, Viridans, Strept. Bovis, some strains of Staphylococcus Aureus, Staph. Epidermidis, Staph. Saprofiticus),
gram positive sticks (Listeria SPP. Enteroccocus SPP.),
gram-negative Cockki (NEISSERIA GONORRHOEAE, N. Meningitidis),
some gram-negative sticks (Haemophilus Influenzae, H. Ducreyi, Escherichia Coli, Helicobacter Pylori, Salmonella SPP., Yersinia Enterocolitica., Shigella SPP., Vibrio Cholerae),
anaerobic bacteria (peptococcus spp., Peptostreptococcus SPP., Clostridium SPP., Bacteroides SPP.),
actinomycetes (ActinoMyces Israelii).

Due to the combination with clavulanic acid, the antibiotic is also effective with respect to bacteria distinguishing beta lactamases:

methicillere-resistant strains (MRSA) Staphylococcus aureus,
Bordetella Pertussis,
Brucella SPP.,
klebsiella
moraxella
campylobacteria.

Natural resistance to inhibitor-proof amoxicillin manifests mycoplasm (Mycoplasma Hominis, Mycoplasma Pneumonia, Ureaplasma urealyticum. and etc.).

Clawulanate has a pronounced bactericidal effect on staphylococci, streptococcal, moraxelle and insignificant - on enterobacteria and a gemophilic wand.

Metabolism and elimination

The pharmacokinetic characteristics of amoxicillin and clavulanic acid are largely similar and practically do not change during combination therapy.

For oral reception Amoxicillin is easily absorbed by the intestinal mucous membranes. To the blood penetrates to 95% of the adopted dose of the drug. About 20% binds to plasma proteins.

The antibiotic is rapidly distributed in the body, creating therapeutic concentrations in palatine almonds, incomplete sinuses, mucousness of the pharynx and lower respiratory tract, drum cavity, pleura, saliva, bile, skin, spinal brain fluid, liver, muscle tissues, prostate gland, endometry and ovaries . The total amount of distribution is more than 20 liters.

The means is excreted in virtually unchanged. Half-life - 1-1.5 hours. In people with renal failure, this indicator may increase to 7.5 hours.

The bioavailability of clavulanic acid during oral administration is 70%. It also quickly sucks into the blood through the intestinal walls. The maximum concentration is achieved 1-2 hours after use. The substance accumulates in the same tissues and secrets as amoxicillin. Biotransformed in the liver. Metabolism products are eliminated through light, kidney and bile. The half-life is 1-1.5 hours, in patients with renal failure - up to 4.5 hours.

The amoxicillin / clawnat combination penetrates well through the hematorecephalic and placental barriers. In nursing women, the drug is detected in breast milk.

Both connections are removed by hemodialysis. For long use Amoxiclav in the body is not cumulative.

Indications for use

Amoxiclav is used in infectious and inflammatory diseases caused by microorganisms sensitive to its action.

The list of readings includes infections:

ENT organs, upper and lower respiratory tract (otitis, sinusitis, pharyngitis, tonsillitis, bronchitis, etc.),
gOOD SYSTEM (cystitis, urethritis, pyelonephritis, salpingitis, cervicitis, gonorare, etc.),
skin (animal bites, roll, phlegmon),
biliary tract
bone and connective tissues,
brain shells (meningitis),
internal shell of the heart (endocarditis),
pokrovov abdominal cavity (peritonitis).

In combination with the metronidazole, the drug may be assigned to peptic disease digestive tractassociated with Helicobacter Pylori.

Contraindications

Amoxiclave should not be used for the following states:

increased sensitivity to penicillins or clavulanic acid,
jaundice or disruption of liver functions, provoked by amoxicillin intake, a history of
mononucleosis,
lympholoicosis.

Tablets are not intended for children under 12 years old.

Application with caution

Pregnancy and lactation period

Therapy for pregnant and lactating women is prescribed only if the intended benefit for the mother exceeds potential risks for the child.

In the US, the Amoxiclav is assigned a security category in (means that there was no adverse effect on the animal exposure to the fetus), in Australia - Category B1 (when using the drug in a limited number of pregnant women negative effects The fetus was not observed).

Impact on the ability to drive a car and other potentially hazardous mechanisms

In some patients, amoxiclave can cause headaches and dizziness, so in the period of use of the drug, caution should be observed during classes hazardous species Activities.

Method of application and dose

The drug is used inside or intravenously. The dosing mode is established individually, depending on the severity of the flow of infection and the type of pathogen.

Pills

With light forms of diseases, adults and children over 12 are prescribed:

tablets 375 mg to 1 every 8 hours,
or tablets 625 mg to 1 every 12 hours.

With severe pathology, shown:

tablets 625 mg to 1 every 8 hours,
or 1000 mg tablets 1 every 12 hours.

The duration of therapy is 5-14 days.

Suspension Powder

In the bottle with the drug should add water to the label. Before each use, the prepared solution must be vigorously shaking.

Depending on the age and severity of pathology, the suspension gives a child through a pipette (0.75-1.25 ml) or from a spoon (1 / 2-2 liters) 2-3 times a day.

The maximum daily dose of amoxicillin for children is 45 mg / kg of weight, clavulanic acid - 10 mg / kg of weight. The duration of treatment is 5-14 days.

Lyophilisate for the preparation of a solution for intravenous administration

0.6 g of lyophilisate is dissolved in 10 ml of water for injections, 1.2 g - in 20 ml of water for injection. The finished solution is administered intravenously slowly. For infusion, the prepared preparation is designed further in 50 (for 0.6 g) or 100 (for 1.2 g) ml of saline. The dropper is installed for 30-40 minutes.

Adults and children over 12 are administered 1.2 g of the drug every 6-8 hours, children under 12 - at the rate of 30 mg / kg of weight every 8-12 hours. Therapy duration is 5-14 days.

Side effects

Amoxiclav is well tolerated by most patients. In rare cases, it may be marked:

dyspeptic disorders (nausea, diarrhea, vomiting),
dizziness
headaches,
convulsions
reducing leukocyte levels and platelets,
cholestatic jaundice
hepatitis,
allergic reactions (itching, urticaria, anaphylactic shock, Stevens-Johnson syndrome),
kidney disorders,
candidiasis,
increase prothrombin time (with sharing intravenous solutions with anticoagulants).

Overdose

The drug poisoning is manifested by diarrhea, abdominal pain, sleep disorder, increased anxiety, sometimes savoring. Therapeutic measures include the washing of the stomach, the reception of enterosorbents and the conduct of symptomatic therapy.

special instructions

Patients with renal failure to take the preparation in reduced dosages or with increased intervals.

To reduce risk side Effects From the side of the digestive tract to use the drug better during food.

With long-term treatment, constant monitoring of the kidney function, liver and spleen is needed.

Interactions with other medicines

The absorption of amoxiclava from the digestive tract is oppressed by antacids, laxatives and glucosamine. Increases absorption ascorbic acid.

Simultaneous reception with diuretics, NSAIDs, allopurinol, phenylbutazone leads to an increase in the concentration of the drug in the blood.

Combined therapy of amoskiklaw and methotrexate should not be carried out, since this can provoke the reinforcement of the toxicity of the latter.

Bactericidal properties of the drug weaken rifampicin, macrolides, tetracyclines, sulfonamides.

Amoxiclave reduces the effectiveness of oral contraceptives, therefore, during the period of therapy and for another 14 days after its completion, it is necessary to use additional methods of contraception.

Conditions of vacation

On prescription.

Storage

For all forms: in a dry place, at a temperature not higher than 25ºС. Take care of children.

A cooked suspension is stored in the refrigerator (at a temperature of 2-8ºС) no longer than 7 days.

The cooked parenteral solution must be started to use for 20 minutes.

Shelf life

For all forms - 2 years.

Manufacturer

Amoxiclav produced by the Slovenian enterprise LEK, leading its history since 1946. The company's priority activities are the development and production of new medicines and biopharmaceutical products.

LEK production facilities are located in 16 countries, including Slovenia, Romania and Poland. Factory activities are certified by GMP standards. Since 2003, the company is part of the European Group of Sandoz enterprises.

Countries in which are produced

As of 2015, Amoxiclave applies in more than 50 states:

Russia,
Ukraine,
Belarus
Poland,
Romania
Croatia
Georgia,
Latvia,
Lithuania
Estonia,
Slovakia
Bosnia and Herzogovina,
Greece
Bulgaria,
some countries in Asia, Africa and Latin America.

The drug was allowed to sell local health institutions. The American FDA organization has been evaluated by Amoxiclava and allowed its use in people in the United States in 2002.

Since the end of the 80s, along with other amoxicillin / clavulanate preparations, amoxiclave is included in the List of Basic Medicines WHO.

In the US and EU countries, the drug is prohibited for veterinary use due to the growing resistance of microorganisms to penicillins.

Analogs

Amoxiclava analogues are amoxicillin / clavulanate preparations manufactured by other manufacturers:

Augmentin,
Panklav,
Ranxlav,
Rapiklav,
Clamor
Medoclav,
Ecoclav
Artilet
Bakoklave,
Verklav
Amoovikom,
Foraclav,
Fibell
Kuram,
Clasp
Amoxicillin + clavulanic acid, etc.

Different companies use unequal production technologies, so the final products may differ from each other by chemical purity, pharmacokinetic characteristics and antimicrobial activity. In large-scale clinical studies, high efficiency and safety of drugs Augmentin, Amoxiclav and Flemoclav Soluteab were confirmed.

Some analogues of amoxiclava and their manufacturers:

Publication Date: 2015-07-20
Last modified: 2020-01-31 Posted by:

Trade name of the drug	Manufacturer	Forms of release
Augmenten	Smithkline Beecham Pharmaceuticals (United Kingdom)	Powder for the preparation of a parenteral solution (in bottles of 600 and 1200 mg) powder for preparing the suspension (3.2%; 4.57%; 9.14%) tablets coated with film shell (375, 625 and 1000 mg)
Panklaw.	Hemofarm (Serbia)	Tablets coated with film shell (375 and 625 mg) Powder for cooking 9.14% suspension
Ranklaw.	RanBaxy (India)	Tablets covered with shell 375 mg and 625 mg
Rapiklav.	IPCA LABORATORIES (India)	Sheath-covered tablets (375 mg and 625 mg)
Medoclaw.	Medochemie Ltd (Cyprus)	Powder for preparing an injection solution (1200 mg) Powder for cooking 3.2% suspension, coated with film shell (1000, 625 and 375 mg)

Pharmacological Group: Suicidal inhibitors of β-lactamase; Antibiotics of Penicillin Group
Systematic (Jupak) Name: (2R, 5R, Z) -3- (2-hydroxyethylidene) -7-oxo-4-OKSA-1-Azabicycle heptane-2-carboxylic acid
Legal status: Released only on the recipe
Application: oral, intravenous
Bioavailability: "Well absorbed"
Metabolism: liver (extensive)
Half-life: 1 hour
Selection: Kidney (30-40%)
Formula: C 8 H 9 NO 5
Like. Mass: 199,16.

Clawulanic acid is a suicide β-lactamase inhibitor (manufactured by GlaxosmithKline), which is taken in combination with the antibiotics of the penicillin group to reduce certain types of antibiotic resistance. It is used to overcome resistance in bacteria separating β-lactamases, which otherwise inactivates most penicillins. In its most common form, potassium clavulanate is adopted in combination with amoxicillin (co-amoxyclav, corporate names of Augmentin, Tyclav (Beximco) synulox [veterinary drug], etc.) or ticarcillin (co-ticarklav, trademark Timemitin). Clawulanic acid is an example of Klava.

Sources

The name comes from the name of the type of Streptomyces Clavuligerus, which produces clavulanic acid. Clawulanic acid is generated during the biosynthesis of and sugar glyceraldehyde-3-phosphate.

History

Clawulanic acid was opened in 1974-1975. British scientists working in the pharmaceutical company Beecham. After several attempts, Beecham finally filed an application for patent protection of the drug in the United States in 1981, and in 1985 received US patents 4525352, 4529720 and 4560552.

Mechanism of action

Clawulanic acid has insignificant internal antimicrobial activity, despite the presence of a β-lactam ring, which is characteristic of β-lactam antibiotics. However, the similarity in the chemical structure of the molecule allows the molecule to interact with the enzyme β-lactamase, secreted by certain bacteria to impart resistance to β-lactam antibiotics. Clawulanic acid is a suicide inhibitor, covalently binding to the residue in the active center of β-lactamase. This rebuilds the clavulanic acid molecule, creating much more active forms that are attacked by other amino acids on the active site, constantly inactivating it, and thus inactivating the enzyme. This inhibition restores the antimicrobial activity of β-lactam antibiotics against the resistant bacteria secreting lactamase. Despite this, there are some strains of bacteria, even to such combinations.

Side effects

The use of clavulanic acid with penicillins is associated with increasing cases of cholestatic jaundice and acute hepatitis during or shortly after therapy. Jaundice is usually self-limiting and very rarely ends with a fatal outcome. The UK Medicine Safety Committee (CSM) recommends restricting such treatments such as the use of amoxicilline / clavulanic acid for treatment bacterial infectionscaused by amoxicillin resistant β-lactamas-producing strains, and that treatment usually should not exceed 14 days. Allergy was also reported on the possible development of allergies.

Availability:

Clawulanic acid is used in combination with amoxicillin or ticarcalline for the treatment of infectious inflammatory diseases caused by microorganisms sensitive to the applied combination. Recommended by recipe.

With the advent of soluble antibiotic drugs in Russia, such as amoxicillin clavulanic acid, we get what has long been waiting - drugs with a smaller probability of adverse reactions, with greater hope for recovery. Meanwhile, if you see, what is the real picture of the appointments of antimicrobial drugs (hereinafter referred to as LP) in our country, it can be noted that, despite those efforts that are made regarding the exception of some antimicrobial means From the arsenal of a practical doctor, the situation is still far from the ideal.

Nevertheless, we note the tendency to expand the use of drugs with proven efficacy. If we talk about treatment respiratory infectionsThis can be noted the main directions in the treatment of our patients are the fight against Str.pneumoniae, H.INFLUENZAE and MORAXELLA CATARRBALIS.

Such an antimicrobial drug like amoxicillin occupies the leading position in our country. Its high activity has been confirmed against beta-hemolytic streptococci groups A, pneumococci, hemophilic sticks (not producing beta lactamase). Combined drug amoxicillin + Clawulanic Acid characterized by a greater completeness and speed of suction than ampicillin, has high level Penetration into almonds, maxillary sines, the cavity of the middle ear, the bronchopile system. Compared to ampicillin trihydrate, amoxicillin with clavulanic acid has a big advantage - a smaller molecule size, which facilitates its penetration into a microbial cell, a greater bioavailability, which does not depend on the meal, especially characteristic of a soluble dosage form of this drug made according to SOLUTAB technology. "(Flexin Soluteab). High bioavailability in the case of antimicrobial LPs is important not only from the point of view of the effect of the drug, but also on the risk of developing the intestinal dysfrece. After all, then the amount of antibiotic, which did not compare in the systemic bloodstream, will remain in the lumen of the intestine, which increases the likelihood of dysbiotic lesions and diarrhea.

The subject of our discussion is a combination of amoxicillin and clavulanic acid in soluble dosage form (hereinafter referred to as LF). It is worth mentioning that the creation of soluble LF is actual including in terms of compliance: despite the fact that liquid LFs are designed to children, and solid (capsules and tablets) - adults, many adults due to individual preferences or other reasons (elderly, lying The patient) would like to use liquid LF. Traditional liquid LFs, such as syrups, have limitations at the concentration of LPs associated with the solubility limit of the drug itself, suspension - the optimal antibiotic ratio / stabilizer. The solution of this problem was the emergence of Soluteab technology, in which active substances placed in microgranules, each of which is covered with a shell dissolving in an alkaline medium fine intestine.

Amoxicillin in microgranulum retains stability in an acidic environment. When taking conventional amoxicillin, some of it dissolves in the stomach, so we lose a certain percentage of the drug. When taking the dissolution of the LD occurs in the upper section of the small intestine, which leads to a more rapid, maximum full absorption and the smallest negative effect on the stomach. Drug Technologies "SOLUTAB" allows you to achieve an increase in bioavailability, and not only amoxicillin, but also clavulanic acid.

According to the following image, you can make sure that the dispersed LFs have significant advantages over usual, not only in terms of pharmacokinetics, but also compliance: the ability to receive "lying patients" without the risk of "jams" capsules or tablets in the folds of the esophagus, one LF for adult and Child, the ability to choose - dissolve the tablet or take it entirely. It is impossible not to note the minimum effect of Soluteab Flemcomka on the intestinal microfloral, which is ensured by the minimum residual concentration of the drug in the intestine.

Currently, an increase in the detection of strains of pathogenic microorganisms producing beta-lactamases is noted. These enzymes produce actual causative agents of respiratory infections: H.INFLUENZAE, MORAXELLA CATARRBALIS, E. coli. The use of inhibitory penicillins is one of the most promising directions Overcoming resistance associated with beta-lactamas products.

Inhibitors are irreversibly bind to beta lactamases (the so-called suicidal effect) both outside the cell (in gram-positive bacteria) and inside it (in gram-negative), and make it possible to make an antimicrobial effect. The result of using inhibitors is a sharp decrease in the minimum overwhelming concentration (IPC) of the antibiotic and, therefore, a significant increase in the efficiency of the drug, which is clearly seen by the example of the comparison of the activity of amoxicillin and its combination with clavulanic acid.

Clavulanic ACID enhances the antibiotic action not only due to the blockade of enzymes, but also due to the anti-cultural effect (decrease in the concentration of microorganisms in a unit of volume), as well as post-beta-lactamazo-braking effect on some pathogens. The meaning of the latter is that under the action of clavulanate, the microbial cell ceases to produce beta-lactamase for some time, which gives amoxicillin an additional "degree of freedom". The post-beta-lactamazo-brake effect is preserved at least for 5 hours. After the acid begins its work, and if the microbial cell does not produce beta-lactamase for 5 hours, naturally increases the activity of amoxicillin.

Amoxicillin in combination with clavulanic acid manifests significant effect potentation. The addition of beta-lactamase inhibitor creates anti-indesses, which is important for the treatment of mixed infections, often encountered, for example, in obstetric and gynecological practice.

Let's return to the issues of the pharmacokinetics of the drug under consideration. There is an objective difference in the absorption of amoxicillin and clavulanic acid due to the difference in the acid-base properties of these substances. Amoxicillin is a weak base, and clavulanate is weak acid. As a result, LD data has different absorption constants, and conditions for incomplete absorption of Clavulanate are created.

Accordingly, there are differences and suction time - absorption occurs not only with different constants, but at different speeds. This is the second condition, due to which clavulanic acid "derses" with suction and retains the residual concentration in the intestine, which creates prerequisites for the adverse action of the acid on the intestinal mucous membrane - 20-25% of patients receiving conventional LF of this drug, which respond to diarrhea therapy, Forcing them to abandon medication.

How to level absorption differences? After all, the more acid is absorbed in the intestine, the smaller its residual toxic effect on the intestinal mucous membrane. Negative reactions associated with incomplete absorption of beta-lactamase inhibitor are diarrhea, pseudomambranous colitis, nausea, changes in flavoring sensations. SOLUTAB technology due to the use of microcapsulated form allows you to dramatically increase the absorption constant of the inhibitor, while the absorption constant of the antibiotic increases slightly (only 5%). When using Flemclav Soluteab, fewer side effects are expected. Now, for example, in the Russian Federation, a study is conducted, the preliminary results of which showed the absence of data unwanted effectsWhat is observed for the first time in relation to amoxicillin / clavulanate, at the same time there are data on the microbiological confirmation of the activity of this drug, clinical improvement and recovery.

There are differences in the permeability of various LF Amoxycillini + Acidi Clavulanici, having a different molecular weight. In this graph, it is clearly clear how the permeability is distinguished for ordinary LFs having a molecular weight of 600-800 g / mol, from the SOLUTAB Flemkelava (200-400 g / mol).

It has been established that the frequency of diarrhea during reception directly depends on the variability of the suction of Clawulanate. When applying conventional Tableted LF amoxicillin with clavulanate, including original drugIt fails to achieve uniform and fast acid absorption. In the case of Flemoclav Solutab, we get a much more encouraging result: the absorption differences of clavulanate from the tablet adopted entirely or pre-dissolved, insignificant. At the same time, we can observe and increasing the concentration of clavulanate in blood serum - using conventional LFs, a concentration can be achieved slightly more than 2 μg / ml, when using a non-volatile - almost 3 μg / ml.

Modern developments in the field of pharmacy affecting the pharmacokinetic properties of antimicrobial means allow you to improve therapeutic effect Antibiotic therapy in parallel with a decrease in the number and severity of adverse reactions. The new soluble AMOXYCILLINUM / ACIDUM CLAVULANICUM - Flemoclav Soluteab - is a fundamentally new quality breakthrough in the technology of drugs. Increased absorption ACIDI Clavulanici increases the protection and effectiveness of amoxycillini and at the same time reduces the likelihood of side effects associated with clavulanic acid, primarily a post-libeotic diarrhea. The unique LF ensures an increase in the "pharmacodynamic load" on the pathogens of infections, which contributes to more complete eradication and as a result of the prevention of new antibiotic pressure with the risk of formation of resistant bacteria strains. At the same time, LF "SOLUTAB" is extremely convenient for adult patients who prefer suspension tablets and for childhood patients.

Video on the topic

MNN: Amoxicillin, clavulanic acid

Manufacturer: Kraspharma OJSC

Anatomy-therapeutic-chemical classification: Amoxicillin in combination with beta lactamase inhibitors

Registration number in Kazakhstan: № RK-LS-5№020148

Registration period: 30.09.2013 - 30.09.2018

Instruction

Tradename

Amoxicillin + Clawulanic Acid

International non-proprietary title

Dosage form

Powder for preparing a solution for intravenous administration 0.5 g + 0.1 g; 1.0 g +0.2

Structure

One bottle contains

active substances: Amoxicillin sodium in terms of amoxicillin - 0.5 g; 1.0 g

clawulanate potassium in terms of clavulanic acid - 0.1 g; 0.2 g

About writing

Powder from white to white with a yellowish color shade.

Pharmacotherapeutic group

Beta-lactam antibacterial preparations are penicillins. Penicillins in combination with beta lactamase inhibitors. Clawulanic acid +.

Amoxicillin

ATH code J01SR02.

Pharmacological properties

Pharmacokinetics

After intravenous administration of the drug in doses 1.2 and 0.6 g, the mean values \u200b\u200bof the maximum concentration in the blood plasma (Cmax) amoxicillin are 105.4 and 32.2 μg / ml, clavulanic acid - 28.5 and 10.5 μg / ml, respectively. Both components are characterized by a good amount of distribution in liquids and tissues of the body (light, middle ear, pleural and peritoneal liquid, uterus, ovaries). Amoxicillin also penetrates into synovial fluid, liver, prostate gland, palatine almonds, muscle tissue, gall-bubble, secret putty sinuses Nose, bronchial secret. Amoxicillin and clavulanic acid do not penetrate the hematorecephalic barrier with unrevenched brain shells.

The active substances penetrate the placental barrier and in trace concentrations are distinguished with breast milk.

Bonding with plasma proteins is 17-20% for amoxicillin, for clavulanic acid - 22-30%.

Metabolized both components in the liver. Amoxicillin is partially metabolized - 10% of the administered dose, clavulanic acid is subjected to intensive metabolism - 50% of the administered dose.

After intravenous administration Amoxicillin preparation + Clawulanic acid in doses 1.2 and 0.6 g of half-life (T1 / 2) for amoxicillin is 0.9 and 1.07 hours, for clavulanic acid 0.9 and 1.12 h.

Amoxicillin is excreted by the kidneys (50-78% of the administered dose) in virtually unchanged form by the tubular secretion and glomerular filtration. Clawulanic acid is excreted by kidney by glomerular filtration unchanged, partially as metabolites (25-40% of the administered dose) within 6 hours after taking the drug.

Small quantities can be excreted through the intestines and lungs.

Pharmacodynamics

The drug is a combination of semi-synthetic penicillin of amoxicillin and beta lactamase inhibitor - clavulanic acid. Suitable bactericidal, inhibits the synthesis of the bacterial wall.

Active in relation to:

aerobic gram-positive bacteria (including strains producing beta lactamases): Staphylococcus aureus, StareLococcus Epidermidis, Streptococcus Pyogenes, Streptococcus Pneumoniae, Streptococcus Viridans, Enterococcus SPP, Corynebacterium SPP., Listeria monocytogenes;

anaerobic gram-positive bacteria: Clostridium SPP., Peptococcus SPP., Peptostreptococcus SPP.;

aerobic gram-negative bacteria(including strains producing beta lactamases) : Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella spp., Salmonella spp., Shigella spp., Bordetella pertussis, Yersinia enterocolitica, Gardnerella vaginalis, Neisseria meningitidis, Neisseria gonorrhoeae, Moraxella catarrhalis, Haemophilus influenzae, Haemophilus ducreyi, Yersinia multocida (formerly Pasteurella ), Campylobacter jejuni;

anaerobic gram-negative bacteria(including strains producing beta lactamases): Bacteroides SPP., Including Bacteroides Fragilis.

Clawulanic acid suppresses II, III, IV and V Types of beta lactamas, inactive in relation to beta lactamases I type, produced by Enterobacter SPP., Pseudomonas Aeruginosa, Serratia SPP., Acinetobacter SPP. Clawulanic acid has a high tropiness to penicillinases, due to which it forms a stable complex with an enzyme, which prevents the enzymatic degradation of amoxicillin under the influence of beta-lactamas.