Features of antibiotic treatment amoxiclav and side effects. Antibiotic amoxiclav for adults Li amoxiclav

Amoxiclav is a combined remedy containing the antibiotic amoxicillin from the penicillin group and clavulanic acid. The antibiotic Amoxiclav has a broad spectrum activity, acts against the microorganisms indicated in the instructions for use of amoxicillin.

Amoxiclav is available in the form of dosage forms:

tablets;
suspension powder;
lyophilisate for injection.

Amoxiclav tablets are oval, biconvex, coated with a white shell, yellowish at the break. They are released in dosage (mg):

amoxicillin - 250, 500, 850;
clavulanic acid - 125.

As disintegrants, talc, silicon dioxide, cellulose, Mg stearate, crospovidone are used. The shell contains povidone, titanium dioxide, triethyl hydrate, talc.

Powder for suspension is made with a concentration of:

amoxicillin, taken in the amount of 125 mg, clavulanes. to-ta 31.25 mg/5 ml;
250 and 62.5/5 ml;
400 and 57/5 ml;
Dosing pipette and spoon are enclosed in the package.

Powder for injection is packaged in vials containing:

1000 mg amoxicillin + 200 mg clavulanes. to-you;
500 mg and 100 mg.

How Amoxiclav works

Amoxiclav is a bactericidal antibiotic. Its effectiveness is determined by the properties of the components:

amoxicillin;
clavulanic acid.

Amoxicillin belongs to the group of semi-synthetic beta-lactam penicillins, the properties of which are described on the page.

In the stomach, amoxicillin is broken down by beta-lactamase enzymes produced by bacteria. To protect amoxicillin from the action of bacterial enzymes, clavulanate is introduced into the composition of the drug.

Clavulanic acid is a compound that blocks the destructive action of bacterial enzymes. Clavulanate, like antibiotics of the penicillin group, destroys the bacterial wall of microorganisms, but, compared with penicillins, the effectiveness of this action is negligible.

There is practically no activity in the acid against the group of enterococci, Pseudomonas aeruginosa, some activity is observed against gonococci, legionella.

Low activity of Amoxiclav is observed in relation to a group of atypical pathogens - mycoplasma, chlamydia, there is no activity in some cases against Klebsiella pneumoniae.

Pharmacokinetics

The maximum concentration is noted after 1 hour. There is no dependence on food.

The components of the drug are found in high concentrations in the lung tissue, peritoneum, pleural fluid, middle ear, paranasal sinuses.

Poorly penetrate the prostate, unable to overcome the blood-brain barrier, penetrate into the cerebrospinal fluid. However, the compounds are able to cross the placenta and are found, albeit in small amounts, in breast milk when treated during lactation.

The drug is excreted by the kidneys, the half-life is 1.5 hours.

Action spectrum

The antibiotic Amoxiclav detects a bactericidal property, inhibiting the synthesis of the walls of bacteria of the following groups:

gram-positive bacteria - Staphylococcus aureus, streptococcus, pneumococcus;
gram-negative - enterobacter, E. coli, Proteus, Haemophilus influenzae, Klebsiella group;
groups of anaerobes - including fusobacteria, as well as fragilis bacteroids, which are a common cause of intra-abdominal infections.

Indications Amoxiclav

The drug is prescribed for the treatment of:

community-acquired and hospital-acquired pneumonia, pleurisy, bronchitis;
tracheitis, laryngitis;
tonsillitis, chronic tonsillitis, pharyngitis;
otitis media;
sinusitis;
odontogenic infections;
abdominal infections;
skin diseases;
bacterial diseases of bones and joints;
genitourinary system;
bile ducts;
sepsis;
venereal diseases;
postoperative treatment, preoperative prophylaxis;
with bites of non-poisonous and poisonous insects and animals.

Contraindications

Contraindications to the use of Amoxiclav are diseases:

allergic nature - bronchial asthma, atomic dermatitis, allergy to penicillins, cephalosporins, carbapenems;
Infectious mononucleosis;
liver failure;
pathology of renal function;
lymphocytic leukemia;
weight up to 40 kg.

Amoxiclav is carefully prescribed for treatment during pregnancy. In the 1st trimester, drugs of this group are not used, strictly according to indications they are prescribed in the 2nd, 3rd trimesters of pregnancy.

Although Amoxiclav does not have a teratogenic effect, its use during pregnancy increases the risk of neonatal necrotizing inflammation of the colon.

There are no direct contraindications for use during lactation. But in the treatment of Amoxiclav and drugs from the group of its analogues in infants, oral candidiasis and diarrhea may develop.

Contraindications for the use of Amoxiclav are childhood, according to the instructions:

for suspension treatment - no contraindications, used from birth;
when using tablets - 12 years, this is due to the fact that there is no way to accurately divide the tablet so as not to violate the instructions;
in the treatment of Amoxiclav in injections - there are no age restrictions, the dosage is calculated by weight.

Amoxiclav is used with caution, with dosage adjustment indicated in the instructions, for pathologies of the digestive tract, pseudomembranous colitis.

How to use Amoxiclav, instructions

The medicine in tablets is used for adults, adolescents weighing more than 40 kg. The course of therapy is from 5 days to 2 weeks.

In mild forms of the course of the disease and odontogenic infections, it is prescribed, according to the instructions, for 5 days. Amoxiclav is best taken with food at the beginning, although the drugs in this group do not depend on food intake.

The use of medicines in tablets

The dosage of the antibiotic Amoxiclav is calculated based on the danger of the disease:

in mild form:
- one tablet. (250 and 125) Amoxiclav with an interval of 8 hours;
- tablet (500 and 125) after 12 hours;
with a complicated course of the disease:
- with an interval of 8 hours tablet. (500+125);
- tablet. (875 and 125) after 12 hours;
with odontogenic infection - caries, periodontitis, gingivitis, sinusitis:
- one table. Amoxiclav (250 and 125) after 8 hours;
- tablet (500 and 125) after 12 hours.

In renal pathologies, the dosage of the antibiotic is revised downwards or increases the intervals between doses of the medicine.

Following the instructions, adults suffering from renal failure are initially prescribed a tablet (500 and 125) of Amoxiclav 12 hours later. Then the treatment regimen is adjusted by the attending physician.

How to take the suspension, instructions

Suspension is used for treatment from birth to adolescence 12 years old. The dose is more dependent on weight, and there is no direct relationship with age.

Instructions for babies up to 3 months

For children from birth to 3 months, the antibiotic, as indicated in the instructions, is prescribed at a daily dosage of 30 mg / kg of body weight. The medication is divided into 2 approaches.

Measuring pipette measure the drug solution:

for suspension with amoxicillin and clavulanic acid 125 and 31.25 mg/5 ml;
- weight 2 kg - 1.2 ml;
- 4 – 2,4;
- 4,8 – 2,9;
for suspension containing components 250 mg and 62.5 mg/5 ml;
- weight 2 kg - 0.6;
- 3,6 – 1,1;
- 4,8 – 1,4.

The use of Amoxiclav in suspension at 3 months. and more, instruction

Daily use of Amoxiclav for children after 3 months. calculated based on the dosage:

20 mg per kilogram of weight with a slight flow;
40 mg per kg with a complicated course of the disease.

The daily dosage is divided into 3 times with an interval of 8 hours.

With a mild course of the disease from 3 months of age, a single dosage is prescribed:

for a suspension containing amoxicillin + clavulanic acid 125 and 31.25 mg / 5 mg;
- child weight 5 kg - 1.3;
- 7 kg - 1.9;
- 17 kg - 4.5;
- 25 – 6,7;
- 35 – 9,3;
- 39 - 10.4 ml;
for suspension containing components 250 and 62.5 mg/ml;
- weight 5 kg - 0.7;
- 15 — 2;
- 17 - 2.3 ml;
- 35 – 4,7;
- 39 - 5.2 ml.

Suspension with amoxicillin 400, clavulanic acid 57 mg / 5 mg solution is used, following the instructions, for the treatment of children after 3 months.

Depending on the severity of the disease and the age of the child, two rubles / day are prescribed for the use of Amoxiclav in suspension:

from 3 months up to a year - 1, 25 ml at moderate, 2.5 ml in severe conditions;
from 1 year to 2 years - 2.5 ml, and in serious condition 3.75 ml;
2 - 4 years - take 3, 75, with complications 5;
4 years - 6 liters. - 5 or with complications 7.5;
6 l. - 12 l. - 6.5 or with deterioration 10 ml.

When preparing the suspension, boiled water is used, shake well before use.

Amoxiclav for injections

Dosage for intravenous administration calculated:

children weighing less than 4 kg - 30 mg / kg after 12 hours;
weighing more than 4 kg - 30 mg / kg after 8 hours, with complicated infections, the interval is reduced to 6 hours.

Adults and teenagers over 40 kg

Amoxiclav 1000 + 200 is prescribed as indicated in the instructions:

1.2 g after 8 hours in conditions of moderate severity;
1.2 g after 6 hours in severe pathologies.

Side effects

The use of Amoxiclav causes mainly the same side effects as the antibiotic amoxicillin present in the composition of the drug, which is described in the article.

Side effect, caused by the presence of clavulanic acid, can be manifested by nausea, vomiting, fever, increased activity of the hepatic transaminase group.

Most often, when taking the antibiotic Amoxiclav, there is no side effects or they rarely occur, which means that there is no need to stop the drug or adjust the dosage.

Drug Interactions

It is forbidden to take Amoxiclav simultaneously with drugs:

antibiotics;
- groups of macrolides - erythromycin, azithromycin;
- tetracyclines;
- sulfonamide groups;
- rifampicin;
anticoagulants (Warfarin) - the prothrombin time increases with simultaneous administration, i.e., the risk of thrombosis is increased;
alcohol - the load on the liver increases, as the antibiotic metabolizes in the liver;
diuretics, NSAIDs - increases the level of amoxicillin in the blood;
allopurinol - skin allergic reactions are noted;
methotrexate - increases the toxicity of methotrexate;
oral contraceptives - the effectiveness of contraception decreases.

Application features

Amoxiclav can cause dizziness, convulsions. Driving while taking antibiotics is not recommended.

Amoxiclav is released strictly according to the prescription. It is stored at a temperature not exceeding 25 C, where there is no access for children.

Data about deaths with an overdose or the appearance of severe effects when using an antibiotic, there is no.

Analogues

The analogues of the antibiotic Amoxiclav include a group of drugs: Amoxiclav Quiktab, Augmentin, Femoclav Solutab, Panklav, Arlet.

Apply Amoxiclav 500, like any other antibiotics, for the treatment of prostatitis can only be prescribed by the attending physician. The drug belongs to medicines broad action, has the ability to cause side effects if used improperly, that is, it can not only help, but also harm.

Its replacement with cheaper tablets with a similar composition in the treatment of prostatitis is allowed, but not recommended. The point is that the main active substance the drug is supplemented with acid, which increases its effectiveness and reduces the duration of the course.

Characteristics of the drug

Amoxiclav belongs to the antibiotics of the penicillin series of semi-synthetic origin. Its peculiarity is that the main active ingredient of the drug - amoxicillin - is supplemented with clavulanic acid, in a ratio of 500 + 125 mg. It has a structure similar to amoxicillin, but is able to act on viruses and microbes that are resistant to penicillins.

Instructions for use Amoxiclav 500 + 125 mg includes a rather long list of indications. Antibiotic is effective in the treatment of infectious and viral diseases

Respiratory system, including ENT organs;
Urinary tract and genital organs - prostatitis, endometritis;
Skin, soft and bone tissues - abscesses, osteomyelitis, sepsis;
Bile ducts - cholecystitis.

In addition, the drug is actively practiced in surgery - to prevent and treat postoperative complications.

The action of the drug is based on the ability of the substances in its composition to destroy the cell membranes of bacteria and viruses, pathogenic microorganisms. Destroying them, Amoxiclav in as soon as possible reduces the intensity of the inflammatory process, and after 3-5 days the patient feels much better.

Scheme of admission and duration of the course

Adults should take Amoxiclav 500 tablets according to the instructions. The dosage and duration of the course can be adjusted by the attending physician in accordance with the intensity of the course of the disease and the individual characteristics of the patient's body, but the recommended values cannot be exceeded.

Antibiotics are able to suppress not only harmful bacteria, but also beneficial ones that protect the body and are the basis of immunity.

The duration of the course of treatment with Amoxiclav ranges from 5 to 14 days, and depends on the complexity of the course of the disease. Therapy should take place under the supervision of a physician, with monitoring of the patient's condition and monitoring of analyzes of his biological materials. Treatment is possible both in a hospital and on an outpatient basis, but with the condition of regular visits to the doctor. Based on the test results and the patient's well-being, the dosage may vary. The recommended scheme for taking Amoxiclav in tablets for prostatitis:

2 tablets per day, 500 mg;
3-4 tablets per day, 250 mg.

General daily dose for an adult should not exceed 1125 mg. After 5 days of admission, in the absence of a positive effect from the treatment, the issue of prolonging the course is decided. Only the attending physician can make such a decision, based on the patient's condition, the results of studying his blood, urine.

Usually, the treatment of prostatitis with the use of this drug does not require taking it for more than 10 days at the dosage described in the instructions for use of Amoxiclav 500 + 125 mg tablets. The content of two potent substances in the composition provides a quick therapeutic effect and an improvement in the patient's condition.

Contraindications and side effects

Treatment with penicillin antibiotics is not always possible. Before taking Amoxiclav, you need to make sure that there are no contraindications. Their list includes:

If the patient has one or more contraindications, the decision on therapy with Amoxiclav should not be made by one doctor, but by a group that includes several highly specialized doctors.

While taking the drug, side effects may develop, which the patient should immediately inform the attending physician. Symptoms such as:

Indigestion or malfunction of the intestines;
Inflammatory processes on the mucous membranes;
Increased salivation;
swelling or rashes on the skin;
A sharp drop or increase in blood pressure;
headaches or dizziness;
Nervous tics or convulsions;
Sweating, pallor skin after taking the drug.

With the manifestation of at least one of the listed side effects or any change in the patient's condition while taking the drug, it is necessary to reduce its dosage or completely cancel it.

Cost and analogues

How much Amoxiclav 500 + 125 mg tablets costs depends on the pricing policy of the pharmacy chain, the manufacturer and the amount of the drug in the package. In most regions, a package with 15 tablets costs no more than 300 rubles. Cheaper analogues of Amoxiclav:

Azithromycin;
Amosin;
Oksamp;
Ecoclave.

Broad-spectrum penicillin antibiotic with beta-lactamase inhibitor

Active ingredients

- (as trihydrate) (amoxicillin)
- clavulanic acid (in the form of potassium clavulanate) (clavulanic acid)

Release form, composition and packaging

The composition of the film shell:

15 pcs. - dark glass bottles (1) - packs of cardboard.
20 pcs. - dark glass bottles (1) - packs of cardboard.
21 pcs. - dark glass bottles (1) - packs of cardboard.

Film-coated tablets white or almost white, oval, biconvex.

Excipients: colloidal silicon dioxide, crospovidone, croscarmellose sodium, magnesium stearate, talc, microcrystalline cellulose.

The composition of the film shell: hypromellose, ethylcellulose, diethyl phthalate, macrogol 6000, titanium dioxide.

5 pieces. - blisters (3) - packs of cardboard.

15 pcs. - bottles (1) - packs of cardboard.

Film-coated tablets white or almost white, oblong, biconvex, with an imprint of "AMC" on one side, with a notch and an imprint of "875" and "125" on the other.

Excipients: colloidal silicon dioxide, crospovidone, croscarmellose sodium, magnesium stearate, talc, microcrystalline cellulose.

The composition of the film shell: hypromellose, ethyl cellulose, triethyl citrate, titanium dioxide, talc.

5 pieces. - blisters (2) - packs of cardboard.
7 pcs. - blisters (2) - packs of cardboard.

pharmachologic effect

Broad spectrum antibiotic; contains semi-synthetic penicillin amoxicillin and β-lactamase inhibitor clavulanic acid. Clavulanic acid provides a stable inactivated complex with these enzymes and provides amoxicillin resistance to the effects of β-lactamases produced by microorganisms.

Clavulanic acid, similar in structure to beta-lactam antibiotics, has a weak intrinsic antibacterial activity.

Has a wide spectrum antibacterial action. Active towards strains sensitive to amoxicillin, including strains producing β-lactamase, incl. aerobic Gram-positive bacteria: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus bovis, Enterococcus spp., Staphylococcus aureus (except methicillin-resistant strains), Staphylococcus epidermidis (except methicillin-resistant strains), Staphylococcus saprophyticus, Listeria spp.; aerobic Gram-negative bacteria: Bordetella pertussis, Brucella spp., Campylobacter jejuni, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae, Helicobacter pylori, Klebsiella spp., Moraxella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella multocida, Proteus spp., Salmonella spp., Shigella spp., Vibrio cholerae, Yersinia enterocolitica, Eikenella corrodens; gram-positive anaerobes: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Actinomyces israelii, Fusobacterium spp., Prevotella spp., Gram-negative anaerobes: Bacteroides spp.

Pharmacokinetics

The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar.

Suction

After taking the drug inside, both components are well absorbed from the gastrointestinal tract, food intake does not affect the degree of absorption. Cmax in the blood is reached 1 hour after taking the drug and is (depending on the dose) for amoxicillin 3-12 mcg / ml, for clavulanic acid - about 2 mcg / ml.

Distribution

Both components are characterized by a good volume of distribution in body fluids and tissues (lungs, middle ear, pleural and peritoneal fluids, uterus, ovaries). Amoxicillin also penetrates into the synovial fluid, liver, prostate gland, palatine tonsils, muscle tissue, gallbladder, the secret of the paranasal sinuses, saliva, bronchial secret.

Amoxicillin and clavulanic acid do not penetrate the BBB in non-inflamed meninges.

Active substances penetrate the placental barrier and are excreted in trace concentrations with breast milk. The degree of binding to plasma proteins is low.

Metabolism

Amoxicillin is partially metabolized, clavulanic acid appears to be extensively metabolized.

breeding

Amoxicillin is excreted by the kidneys almost unchanged by tubular secretion and glomerular filtration. Clavulanic acid is excreted by glomerular filtration, partly as metabolites. Small amounts can be excreted through the intestines and lungs. T 1/2 of amoxicillin and clavulanic acid is 1-1.5 hours.

Pharmacokinetics in special clinical situations

With severe kidney failure T 1/2 increases to 7.5 hours for amoxicillin and up to 4.5 hours for clavulanic acid. Both components are removed by hemodialysis and minor amounts by peritoneal dialysis.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

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

- infections of the lower respiratory tract (incl. acute bronchitis with bacterial superinfection, Chronical bronchitis, pneumonia);

– infections urinary tract;

- gynecological infections;

- skin and soft tissue infections, including human and animal bites;

- infections of bone and connective tissue;

– infections biliary tract(cholecystitis, cholangitis);

- odontogenic infections.

Contraindications

- an indication of a history of cholestatic jaundice or abnormal liver function caused by taking amoxicillin / clavulanic acid;

- Infectious mononucleosis;

- lymphocytic leukemia;

- hypersensitivity to antibiotics of the penicillin group, cephalosporins and other beta-lactam antibiotics (history);

- hypersensitivity to amoxicillin or clavulanic acid.

WITH caution prescribe the drug to patients with a history of pseudomembranous colitis, with liver failure, severe renal dysfunction, and also during lactation.

Dosage

Adults and children over 12 years of age (or weighing >40 kg) at mild or moderate infection appoint 1 tab. (250 mg + 125 mg) every 8 hours or 1 tab. (500 mg + 125 mg) every 12 hours, in case severe course infections and respiratory tract infections- 1 tab. (500 mg + 125 mg) every 8 hours or 1 tab. (875 mg + 125 mg) every 12 hours.

The drug in the form of tablets is not prescribed children under 12 years of age (weighing<40 кг).
The maximum daily dose of clavulanic acid (in the form of potassium salt) is for adults- 600 mg, for children- 10 mg/kg body weight. The maximum daily dose of amoxicillin is adults- 6 g, for children- 45 mg/kg body weight.

The course of treatment is 5-14 days. The duration of the course of treatment is determined by the attending physician. Treatment should not continue for more than 14 days without a second medical examination.

At odontogenic infections appoint 1 tab. (250 mg + 125 mg) every 8 hours or 1 tab. (500 mg + 125 mg) every 12 hours for 5 days.

At moderate renal failure (CC 10-30 ml / min) appoint 1 tab. (500 mg + 125 mg) every 12 hours, with severe renal failure (CC<10 мл/мин) - 1 tab. (500 mg + 125 mg) every 24 hours. anuria the interval between doses should be increased to 48 hours or more.

Side effects

From the digestive system: possible loss of appetite, nausea, vomiting, diarrhea; rarely - abdominal pain, transient increase in liver enzymes (ALT, AST), liver dysfunction; in isolated cases - cholestatic jaundice, hepatitis, pseudomembranous colitis.

Allergic reactions: erythematous rash, itching, urticaria; rarely - erythema multiforme exudative, angioedema, anaphylactic shock, allergic vasculitis; in isolated cases - exfoliative dermatitis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis.

From the hematopoietic system: rarely - reversible leukopenia (including neutropenia), thrombocytopenia; very rarely - hemolytic anemia, a reversible increase in prothrombin time (when used together with), eosinophilia, pancytopenia.

From the nervous system: dizziness, headache; very rarely - convulsions (may occur in patients with impaired renal function when taking the drug in high doses), hyperactivity, anxiety, insomnia.

From the urinary system: very rarely - interstitial nephritis, crystalluria.

Others: rarely - the development of superinfection (including candidiasis).

Side effects in most cases are mild and transient.

Overdose

There are no reports of death or the occurrence of life-threatening side effects due to an overdose of the drug.

Symptoms: abdominal pain, diarrhea, vomiting; anxiety, insomnia, dizziness are also possible; in some cases - convulsions.

Treatment: in the case of a recent intake of the drug (less than 4 hours), it is necessary to carry out a gastric lavage and prescribe to reduce the absorption of the drug; the patient should be under medical supervision, if necessary, carry out symptomatic therapy. effective hemodialysis.

drug interaction

With the simultaneous use of Amoxiclav with antacids, glucosamine, laxatives, aminoglycosides, absorption slows down, with - increases.

Diuretics, allopurinol, phenylbutazone, NSAIDs and other drugs that block tubular secretion increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).

With the simultaneous use of Amoxiclav and anticoagulants, an increase in prothrombin time is noted. Therefore, this combination is prescribed with caution.

With the simultaneous use of Amoxiclav enhances the toxicity of methotrexate.

With the simultaneous use of Amoxiclav with allopurinol, the risk of developing exanthema increases.

The simultaneous use of Amoxiclav with disulfiram should be avoided.

The combination of amoxicillin with rifampicin is antagonistic (there is a mutual weakening of the antibacterial action).

Amoxiclav should not be used simultaneously with bacteriostatic antibiotics (macrolides, tetracyclines), sulfonamides due to a possible decrease in the effectiveness of Amoxiclav.

Probenecid reduces the excretion of amoxicillin by increasing its serum concentration.

With the simultaneous use of Amoxiclav reduces the effectiveness of oral contraceptives.

special instructions

Due to the fact that in a large number of patients with infectious mononucleosis and lymphocytic leukemia treated with ampicillin, the appearance of an erythematous rash was observed, the use of antibiotics of the ampicillin group for such patients is not recommended.

During the course of treatment, the functions of hematopoiesis, liver and kidneys should be monitored.

In patients with severely impaired renal function, an adequate correction of the dosing regimen or an increase in the intervals between dosing is required.

In order to reduce the risk of developing adverse reactions from the gastrointestinal tract, the drug should be taken with meals.

Since the 250mg + 125mg and 500mg + 125mg tablets of the combination of amoxicillin and clavulanic acid contain the same amount of clavulanic acid - 125mg, then 2 tablets of 250mg + 125mg are not equivalent to 1 tablet of 500mg + 125mg.

When using Amoxiclav, a false positive reaction is possible when determining the level of glucose in the urine using Benedict's reagent or Felling's solution (it is recommended to use enzymatic reactions with glucosidase).

Influence on the ability to drive vehicles and control mechanisms moderate renal failure (CC 10-30 ml / min)

Amoxiclav is a very interesting combined antibacterial drug, consisting of amoxicillin and clavulanic acid. In this case, it makes sense to talk about each of its ingredients. So, amoxicillin, as you know, is a semi-synthetic antibiotic from the penicillin group. Its target is the bacterial cell wall. He gets to it by inhibiting penicillin-binding enzymes involved in the synthesis of the main structural component of the bacterial cell wall - peptidoglycan. Inhibition of the synthesis of the latter is manifested in the loss of strength of the bacterial cell wall, which leads to the complete destruction of the microorganism. In this rosy reality, there is one, but a serious "but": amoxicillin is not an invulnerable terminator and can be easily neutralized by the action of beta-lactamases, which have learned to produce evolutionarily "advanced" bacteria that have become adept at forming antibiotic resistance. Thus, the spectrum of action of amoxicillin in the "solo" mode is limited only by those microorganisms that are not able to produce the above enzymes. And here clavulanic acid, structurally related to penicillins due to its morphological "beta-lactam" nature, comes to the fore. This substance is able to suppress some beta-lactamases, thereby preventing the inactivation of amoxicillin and expanding the range of its bactericidal capabilities. That is, those bacteria that usually showed to him, as well as to other penicillins and cephalosporins, complete indifference (read: resistance) also fall under his targeted “fire”.

By itself, clavulanic acid does not have any therapeutic benefit and does not have an antibacterial effect.

Amoxiclav deals with Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, Enterobacter spp., Escherichia coli, Klebsiella spp., Haemophilus influenzae, Moraxella catarrhalis, Clostridium spp., Peptococcus spp., Peptostreptococcus spp., Proteus vulgaris, Pro, Shigella spp., Salmonella spp., Yersinia enterocolitica, Yersinia multocida, Bordetella pertussis, Neisseria gonorrhoeae, Neisseria meningitidis, Gardnerella vaginalis, Haemophilus ducreyi, Campylobacter jejuni, Bacteroides spp.

Amoxiclav is available in the following dosage forms: powder for solution for intravenous administration, powder for suspension for oral administration and tablets. Dispersible (i.e. soluble) tablets are also produced under the name "amoxiclav quiktab". There are whole schemes for taking amoxiclav, depending on the causative agent of the infection, the severity of the disease and the age of the patient. In any case, given the prescription order for dispensing this drug from pharmacies, the dosage regimen and duration of treatment is determined by the attending physician.

Pharmacology

Combined preparation of amoxicillin and clavulanic acid, a beta-lactamase inhibitor. It acts bactericidal, inhibits the synthesis of the bacterial wall.

Active against aerobic gram-positive bacteria (including beta-lactamase producing strains): Staphylococcus aureus; aerobic gram-negative bacteria: Enterobacter spp., Escherichia coli, Haemophilus influenzae, Klebsiella spp., Moraxella catarrhalis. The following pathogens are sensitive only in vitro: Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus anthracis, Streptococcus pneumoniae, Streptococcus viridans, Enterococcus faecalis, Corynebacterium spp., Listeria monocytogenes; anaerobic Clostridium spp., Peptococcus spp., Peptostreptococcus spp.; as well as aerobic gram-negative bacteria (including beta-lactamase producing strains): Proteus mirabilis, Proteus vulgaris, Salmonella spp., Shigella spp., Bordetella pertussis, Yersinia enterocolitica, Gardnerella vaginalis, Neisseria meningitidis, Neisseria gonorrhoeae, Haemophilus ducreyi, Yersinia multocida ( formerly Pasteurella), Campylobacter jejuni; anaerobic gram-negative bacteria (including beta-lactamase producing strains): Bacteroides spp., including Bacteroides fragilis.

Clavulanic acid inhibits II, III, IV and V types of beta-lactamases, is not active against type I beta-lactamases produced by Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp. Clavulanic acid has a high tropism for 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.

Pharmacokinetics

After oral administration, both components are rapidly absorbed in the gastrointestinal tract. Simultaneous food intake does not affect absorption. T Cmax - 45 min. After oral administration at a dose of 250/125 mg every 8 hours C max amoxicillin - 2.18-4.5 mcg / ml, clavulanic acid - 0.8-2.2 mcg / ml, at a dose of 500/125 mg every 12 hours C max amoxicillin - 5.09-7.91 mcg / ml, clavulanic acid - 1.19-2.41 μg / ml, at a dose of 500/125 mg every 8 hours max amoxicillin - 8.82-14.38 mcg / ml, clavulanic acid - 1.21-3.19 mcg / ml.

After intravenous administration at doses of 1000/200 and 500/100 mg C max amoxicillin - 105.4 and 32.2 μg / ml, respectively, and clavulanic acid - 28.5 and 10.5 μg / ml.

The time to reach the maximum inhibitory concentration of 1 μg / ml for amoxicillin is similar when applied after 12 hours and 8 hours in both adults and children.

Communication with plasma proteins: amoxicillin - 17-20%, clavulanic acid - 22-30%.

Both components are metabolized in the liver: amoxicillin - by 10% of the administered dose of the dose, clavulanic acid - by 50%.

T 1/2 after taking a dose of 375 and 625 mg - 1 and 1.3 hours for amoxicillin, 1.2 and 0.8 hours for clavulanic acid, respectively. T 1/2 after intravenous administration at a dose of 1200 and 600 mg - 0.9 and 1.07 h for amoxicillin, 0.9 and 1.12 h for clavulanic acid, respectively. It is excreted mainly by the kidneys (glomerular filtration and tubular secretion): 50-78 and 25-40% of the administered dose of amoxicillin and clavulanic acid are excreted, respectively, unchanged during the first 6 hours after administration.

Release form

Powder for solution for intravenous administration from white to yellowish-white.

Colorless glass bottles (5) - packs of cardboard.

Dosage

Inside, in / in.

Doses are given in terms of amoxicillin. The dosage regimen is set individually depending on the severity of the course and localization of the infection, the sensitivity of the pathogen.

Adults and children over 12 years of age or weighing 40 kg or more: 500 mg 2 times / day or 250 mg 3 times / day. For severe infections and respiratory tract infections - 875 mg 2 times / day or 500 mg 3 times / day.

The maximum daily dose of amoxicillin for adults and children over 12 years old is 6 g, for children under 12 years old - 45 mg / kg of body weight.

The maximum daily dose of clavulanic acid for adults and children over 12 years of age is 600 mg, for children under 12 years of age - 10 mg / kg of body weight.

When preparing a suspension, syrup and drops, water should be used as a solvent.

When administered intravenously, adults and adolescents over 12 years of age are administered 1 g (according to amoxicillin) 3 times a day, if necessary, 4 times a day. The maximum daily dose is 6 g. For children aged 3 months to 12 years, 25 mg / kg 3 times a day; in severe cases - 4 times a day; for children under 3 months: premature and in the perinatal period - 25 mg / kg 2 times a day, in the postperinatal period - 25 mg / kg 3 times a day.

Duration of treatment - up to 14 days, acute otitis media - up to 10 days.

For the prevention of postoperative infections during operations lasting less than 1 hour, during induction anesthesia, a dose of 1 g is administered intravenously. For longer operations - 1 g every 6 hours during the day. If there is a high risk of infection, administration may be continued for several days.

In chronic renal failure, the dose and frequency of administration are adjusted depending on the CC: with CC more than 30 ml / min, dose adjustment is not required; with CC 10-30 ml / min: inside - 250-500 mg / day every 12 hours; IV - 1 g, then 500 mg IV; with CC less than 10 ml / min - 1 g, then 500 mg / day in / in or 250-500 mg / day orally in one dose. For children, doses should be reduced in the same way.

Overdose

Symptoms: dysfunction of the gastrointestinal tract and water and electrolyte balance.

Treatment: symptomatic. Hemodialysis is effective.

Interaction

Antacids, glucosamine, laxative drugs, aminoglycosides slow down and reduce absorption; ascorbic acid increases absorption.

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

Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index). While taking anticoagulants, it is necessary to monitor the indicators of blood clotting.

Reduces the effectiveness of oral contraceptives, drugs, in the process of metabolism of which PABA is formed, ethinyl estradiol - the risk of bleeding "breakthrough".

Diuretics, allopurinol, phenylbutazone, NSAIDs, and other drugs that block tubular secretion increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).

Allopurinol increases the risk of skin rashes.

Side effects

On the part of the digestive system: nausea, vomiting, diarrhea, gastritis, stomatitis, glossitis, increased activity of hepatic transaminases, in isolated cases - cholestatic jaundice, hepatitis, liver failure (more often in the elderly, men, with long-term therapy), pseudomembranous and hemorrhagic colitis ( may also develop after therapy), enterocolitis, black "hairy" tongue, darkening of tooth enamel.

On the part of the hematopoietic organs: a reversible increase in prothrombin time and bleeding time, thrombocytopenia, thrombocytosis, eosinophilia, leukopenia, agranulocytosis, hemolytic anemia.

From the nervous system: dizziness, headache, hyperactivity, anxiety, behavioral changes, convulsions.

Local reactions: in some cases - phlebitis at the site of intravenous injection.

Allergic reactions: urticaria, erythematous rashes, rarely - exudative erythema multiforme, anaphylactic shock, angioedema, extremely rarely - exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), allergic vasculitis, a syndrome similar to serum sickness, acute generalized exanthematous pustulosis .

Others: candidiasis, development of superinfection, interstitial nephritis, crystalluria, hematuria.

Indications

bacterial infections caused by susceptible pathogens: infections of the lower respiratory tract (bronchitis, pneumonia, pleural empyema, lung abscess);
infections of ENT organs (sinusitis, tonsillitis, otitis media);
infections of the genitourinary system and pelvic organs (pyelonephritis, pyelitis, cystitis, urethritis, prostatitis, cervicitis, salpingitis, salpingo-oophoritis, tubo-ovarian abscess, endometritis, bacterial vaginitis, septic abortion, postpartum sepsis, pelvic peritonitis, soft chancre, gonorrhea);
infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses, abscess, phlegmon, wound infection);
osteomyelitis;
postoperative infections;
infection prevention in surgery.

Contraindications

hypersensitivity (including to cephalosporins and other beta-lactam antibiotics);
infectious mononucleosis (including with the appearance of a measles-like rash);
phenylketonuria;
episodes of jaundice or impaired liver function as a result of the use of amoxicillin / clavulanic acid in history;
CC less than 30 ml / min (for tablets 875 mg / 125 mg).

With caution: pregnancy, lactation, severe liver failure, gastrointestinal diseases (including a history of colitis associated with the use of penicillins), chronic renal failure.

Application features

Use during pregnancy and lactation

With caution: pregnancy, lactation.

Application for violations of liver function

Contraindicated in episodes of jaundice or abnormal liver function as a result of the use of amoxicillin / clavulanic acid in history.

With caution: severe liver failure

Application for violations of kidney function

Patients on hemodialysis - 250 mg or 500 mg orally in a single dose or 500 mg IV, an additional 1 dose during dialysis and 1 more dose at the end of the dialysis session.

Use in children

Children under 12 years old - in the form of a suspension, syrup or drops for oral administration. A single dose is set depending on age: children under 3 months - 30 mg / kg / day in 2 divided doses; 3 months and older - for mild infections - 25 mg / kg / day in 2 doses or 20 mg / kg / day in 3 doses, for severe infections - 45 mg / kg / day in 2 doses or 40 mg / kg / day days in 3 doses.
The maximum daily dose of amoxicillin for children under 12 years old is 45 mg/kg of body weight.

The maximum daily dose of clavulanic acid for children under 12 years old is 10 mg/kg of body weight.

special instructions

During the course of treatment, it is necessary to monitor the state of the function of the hematopoietic organs, liver and kidneys.

In order to reduce the risk of side effects from the gastrointestinal tract, the drug should be taken with food.

Perhaps the development of superinfection due to the growth of microflora insensitive to it, which requires a corresponding change in antibiotic therapy.

May give false positive results in the determination of 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.

After dilution, the suspension should be stored for no more than 7 days in the refrigerator, but do not freeze.

In patients with hypersensitivity to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

There have been cases of development of necrotizing enterocolitis in newborns, in pregnant women with premature rupture of the membranes.

Since the tablets contain the same amount of clavulanic acid (125 mg), it should be noted that 2 tablets of 250 mg (for amoxicillin) are not equivalent to 1 tablet of 500 mg (for amoxicillin).

In this article, you can read the instructions for using the drug Amoxiclav. Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Amoxiclav in their practice are presented. A big request to actively add your reviews about the drug: did the medicine help or not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Analogues of Amoxiclav in the presence of existing structural analogues. Use for the treatment of various infectious diseases in adults, children, as well as during pregnancy and lactation. Alcohol use and possible consequences after taking Amoxiclav.

Amoxiclav- is a combination of amoxicillin - a semi-synthetic penicillin with a wide spectrum of antibacterial activity and clavulanic acid - an irreversible beta-lactamase inhibitor. Clavulanic acid forms a stable inactivated complex with these enzymes and provides amoxicillin resistance to the effects of beta-lactamases produced by microorganisms.

Clavulanic acid, similar in structure to beta-lactam antibiotics, has a weak intrinsic antibacterial activity.

Amoxiclav has a wide spectrum of antibacterial action.

Active against amoxicillin-sensitive strains, including strains producing beta-lactamase, incl. aerobic gram-positive bacteria, aerobic gram-negative bacteria, anaerobic gram-positive bacteria, gram-negative anaerobes.

Pharmacokinetics

The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Both components are well absorbed after oral administration, food intake does not affect the degree of absorption. Both components are characterized by a good volume of distribution in body fluids and tissues (lungs, middle ear, pleural and peritoneal fluids, uterus, ovaries, etc.). Amoxicillin also penetrates into the synovial fluid, liver, prostate gland, palatine tonsils, muscle tissue, gallbladder, sinus secretions, saliva, bronchial secretions. Amoxicillin and clavulanic acid do not penetrate the BBB in non-inflamed meninges. Amoxicillin and clavulanic acid cross the placental barrier and are excreted in breast milk in trace concentrations. Amoxicillin and clavulanic acid are characterized by low plasma protein binding. Amoxicillin is partially metabolized, clavulanic acid appears to be extensively metabolized. Amoxicillin is excreted by the kidneys almost unchanged by tubular secretion and glomerular filtration. Clavulanic acid is excreted by glomerular filtration, partly as metabolites.

Indications

Infections caused by susceptible strains of microorganisms:

infections of the upper respiratory tract and ENT organs (including acute and chronic sinusitis, acute and chronic otitis media, pharyngeal abscess, tonsillitis, pharyngitis);
infections of the lower respiratory tract (including acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia);
urinary tract infections;
gynecological infections;
skin and soft tissue infections, including animal and human bites;
bone and connective tissue infections;
biliary tract infections (cholecystitis, cholangitis);
odontogenic infections.

Release form

Powder for the preparation of an injection solution for intravenous administration (4) 500 mg, 1000 mg.

Powder for suspension for oral administration 125 mg, 250 mg, 400 mg (a convenient children's form of the drug).

Film-coated tablets 250 mg, 500 mg, 875 mg.

Instructions for use and dosage

Adults and children over 12 years of age (or over 40 kg body weight): The usual dose for mild to moderate infections is 1 tablet 250 + 125 mg every 8 hours or 1 tablet 500 + 125 mg every 12 hours for severe infections. and respiratory tract infections - 1 tablet 500 + 125 mg every 8 hours or 1 tab. 875 + 125 mg every 12 hours. Tablets are not prescribed for children under 12 years of age (less than 40 kg of body weight).

The maximum daily dose of clavulanic acid (in the form of potassium salt) is 600 mg for adults and 10 mg/kg of body weight for children. The maximum daily dose of amoxicillin is 6 g for adults and 45 mg/kg of body weight for children.

Dosage for odontogenic infections: 1 tab. 250 +125 mg every 8 hours or 1 tab. 500 + 125 mg every 12 hours for 5 days.

Dosage for renal insufficiency: for patients with moderate renal insufficiency (Cl creatinine - 10-30 ml / min), the dose is 1 table. 500 + 125 mg every 12 hours; for patients with severe renal insufficiency (Cl creatinine less than 10 ml / min), the dose is 1 table. 500 + 125 mg every 24 hours

Side effect

Side effects in most cases are mild and transient.

loss of appetite;
nausea, vomiting;
diarrhea;
stomach ache;
itching, urticaria, erythematous rash;
angioedema;
anaphylactic shock;
allergic vasculitis;
exfoliative dermatitis;
Stevens-Johnson syndrome;
reversible leukopenia (including neutropenia);
thrombocytopenia;
hemolytic anemia;
eosinophilia;
dizziness, headache;
convulsions (may occur in patients with impaired renal function when taking the drug in high doses);
sense of anxiety;
insomnia;
interstitial nephritis;
crystalluria;
development of superinfection (including candidiasis).

Contraindications

hypersensitivity to any of the components of the drug;
a history of hypersensitivity to penicillins, cephalosporins and other beta-lactam antibiotics;
a history of indications of cholestatic jaundice and / or other abnormal liver function caused by taking amoxicillin / clavulanic acid;
infectious mononucleosis and lymphocytic leukemia.

Use during pregnancy and lactation

Amoxiclav can be prescribed during pregnancy if there are clear indications.

Amoxicillin and clavulanic acid are excreted in breast milk in small amounts.

special instructions

During the course of treatment, the functions of the hematopoietic organs, liver and kidneys should be monitored.

In patients with severely impaired renal function, an adequate correction of the dosing regimen or an increase in the intervals between dosing is required.

In order to reduce the risk of developing adverse reactions from the gastrointestinal tract, the drug should be taken with meals.

Laboratory tests: High concentrations of amoxicillin give a false positive reaction to urine glucose when using Benedict's reagent or Felling's solution. Enzymatic reactions with glucosidase are recommended.

It is forbidden to use Amoxiclav with the simultaneous use of alcohol in any form, since the risk of hepatic disorders is seriously increased when they are taken simultaneously.

Influence on the ability to drive vehicles and control mechanisms

There are no data on the negative effect of Amoxiclav in recommended doses on the ability to drive a car or work with mechanisms.

drug interaction

With the simultaneous use of the drug Amoxiclav with antacids, glucosamine, laxatives, aminoglycosides, absorption slows down, with ascorbic acid it increases.

Diuretics, allopurinol, phenylbutazone, NSAIDs and other drugs that block tubular secretion increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).

With the simultaneous use of Amoxiclav increases the toxicity of methotrexate.

With the simultaneous use of Amoxiclav with allopurinol, the incidence of exanthema increases.

Co-administration with disulfiram should be avoided.

In some cases, taking the drug may lengthen the prothrombin time, in this regard, care should be taken when prescribing anticoagulants and the drug Amoxiclav.

The combination of amoxicillin with rifampicin is antagonistic (there is a mutual weakening of the antibacterial action).

Amoxiclav should not be used simultaneously with bacteriostatic antibiotics (macrolides, tetracyclines), sulfonamides due to a possible decrease in the effectiveness of Amoxiclav.

Probenecid reduces the excretion of amoxicillin by increasing its serum concentration.

Antibiotics reduce the effectiveness of oral contraceptives.

Antibiotic analogs Amoksiklav

Structural analogues for the active substance:

Amovicomb;
Amoxiclav Quiktab;
Arlet;
Augmentin;
Bactoclav;
Verclave;
Klamosar;
Liklav;
Medoklav;
Panklav;
ranclave;
Rapiclav;
Taromentin;
Flemoklav Solutab;
Ecoclave.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.