Amoxiclav is a combination drug that belongs to the group of beta-lactam antibiotics. The therapeutic effects are provided by the active substances - amoxicillin - one of the best penicillin antibiotics and clavulanic acid - the most powerful known beta-lactamase inhibitor.
The combination of these substances leads to the appearance of special properties of Amoxiclav:
- irreversible blockade of β-lactamases of microorganisms, which allows amoxicillin to have an antibacterial effect even on resistant pathogens;
- high bioavailability;
- penetrates well into most tissues and body fluids, creating a high concentration that is necessary to destroy sensitive pathogenic bacteria.
The mechanism of action of amoxicillin in Amoxiclav is bactericidal activity - disruption of the synthesis of a component of the bacterial cell wall, which causes their dissolution. Clavulanic acid is a β-lactam inhibitor and exhibits equal activity against both gram-positive and gram-negative bacteria. Protects amoxicillin from destruction by enzymes - β-lactamases, thereby expanding the spectrum of action of amoxicillin.
Amoxiclav is manufactured by the pharmaceutical company Lek Pharmaceuticals dd in Slovenia. There are various dosage forms of the drug on the Ukrainian pharmaceutical market. This is an important point in choosing Amoxiclav when prescribing it to patients of different age categories and severity of the disease.
Advantages of using Amoxiclav:
- predictable effectiveness and non-toxicity of penicillins;
- wider spectrum of action, compared with amoxicillin and oral cephalosporins due to the presence of clavulanic acid;
- applicable in all age groups;
- food intake does not affect the absorption of the drug.
Among dosage forms, the ease of use of Amoxiclav suspension should be noted. The drug is equipped with a measuring syringe for dosing accuracy. The possibility of using the suspension three times in children minimizes the development of resistance and meets international requirements for rational antibiotic therapy.
Indications
Amoxiclav is intended for the treatment of bacterial infections caused by microorganisms sensitive to the drug:
- severe infections of the throat, nose, and ear (such as mastoiditis, peritonsillar infections, epiglotitis, and sinusitis with associated severe systemic signs and symptoms)
- exacerbation of chronic bronchitis (after confirmation of diagnosis)
- community-acquired pneumonia
- cystitis;
- pyelonephritis;
- infections of the skin and soft tissues, including bacterial cellulitis, animal bites, severe dentoalveolar abscesses with widespread cellulitis;
- infections of bones and joints, including osteomyelitis;
- intra-abdominal infections;
- genital infections in women.
Prevention of bacterial infections during major surgical interventions in the following areas:
- gastrointestinal tract;
- pelvic organs;
- chairman and neck;
- biliary tract.
When prescribing antibacterial drugs, one should be guided by the rules for their proper use.
Indications for use of Amoxiclav
The use of the drug is so widespread that some doctors starting their therapeutic practice prescribe it at every opportunity. In the situation with diseases of the otolaryngology organs, this is:
- otitis, including purulent;
- tonsillitis;
- sinusitis;
- pharyngolaryngitis.
When the urinary system is affected, Amoxiclav can also be prescribed. These diseases include chronic cystitis, prostatitis, and urethritis.
Diseases of the respiratory system are rarely treated without amoxicillin. For bronchitis of bacterial etiology and pneumonia, this particular drug is used. In addition, the antibiotic has shown its effectiveness against:
- infections affecting bones and connective tissue;
- soft tissue diseases caused by bacterial infection;
- cholecystitis;
- diseases of the pelvic organs.
Some types of surgery require the patient to take a course of antibiotics to prevent superinfection.
Compound
Active ingredients: amoxicillin, clavulanic acid;
1 bottle contains 1000 mg of amoxicillin in the form of sodium salt and 200 mg of clavulanic acid in the form of potassium salt.
Amoxicillin is a semisynthetic penicillin (beta-lactam antibiotics) that inhibits one or more enzymes, often referred to as penicillin binding proteins (PBPs), in the biosynthetic metabolism of bacterial peptidoglycan, an integral structural component of the bacterial cell wall. Inhibition of peptidoglycan synthesis leads to weakening of the cell wall, resulting in cell lysis and death.
Amoxicillin is sensitive to the breakdown of beta-lactamases produced by resistant bacteria; therefore, the spectrum of activity of amoxicillin as monotherapy does not include organisms that produce these enzymes.
Clavulanic acid is a beta-lactam, structurally related to penicillins. It disables some beta-lactamase enzymes, thereby preventing the inactivation of amoxicillin. Clavulanic acid as monotherapy does not have a clinically useful antibacterial effect.
Directions for use and doses
Doses are given as amoxicillin/clavulanic acid content unless the dose of the individual component is indicated.
When choosing a dose of a drug to treat a specific infection, you must consider:
- expected pathogens and their expected sensitivity to antibacterial substances (see section “Peculiarities of application”);
- severity and location of infection;
- the patient's age, weight, and renal function status, as described below.
If necessary, alternative forms of Amoxiclav ® can be used (for example, with higher doses of amoxicillin and/or a different ratio of amoxicillin and clavulanic acid).
These dosage forms of Amoxiclav ® can be used in a daily dose of up to 3000 mg of amoxicillin and 600 mg of clavulanic acid. If it is necessary to use a higher dose of amoxicillin, a drug with a different amoxicillin/clavulanic acid ratio should be prescribed to avoid ultra-high daily doses of clavulanic acid.
The duration of treatment is determined by the doctor individually. Some infections (such as osteomyelitis) require long-term treatment. The duration of treatment should not exceed 14 days without assessing the results of use and the clinical picture (see Section “Peculiarities of use”).
Dosage for adults and children weighing ≥ 40 kg
Standard dose is 1000 mg/200 mg every 8:00.
Prevention of complications during surgical interventions.
For operations lasting less than 1 hour, the recommended dose is from 1000 mg / 200 mg to 2000 mg / 200 mg during induction of anesthesia (a dose of 2000 mg / 200 mg can be achieved using the appropriate intravenous form of the drug).
For operations lasting more than 1 hour, the recommended dose ranges from 1000 mg / 200 mg to 2000 mg / 200 mg when injecting anesthesia, a dose of 1000 mg / 200 mg can be administered 3 times within 24 hours.
If there are clinical signs of infection during surgery, a course of treatment with intravenous or oral administration of the drug should be prescribed in the postoperative period.
Dosage for children weighing <40 kg.
Children over 3 months: 25 mg/5 mg/kg every 8:00.
Children under 3 months of age or weighing less than 4 kg: 25 mg/5 mg/kg body weight every 12:00.
Features of drug administration.
Amoxiclav ® is administered by intravenous injection (stream) or by periodic infusion (drip). The drug cannot be administered intramuscularly.
For children under 3 months of age, Amoxiclav ® is prescribed only as an intravenous infusion.
Treatment can begin with the administration of Amoxiclav ® and continue with oral forms.
Preparation of solution for intravenous injection.
500 mg / 100 mg dissolve the contents of the vial in 10 ml of water for injection (final volume - 10.5 ml)
1000 mg / 200 mg dissolve the contents of the vial in 20 ml of water for injection (final volume - 20.9 ml).
Reconstituted solutions have a yellowish (pale straw) color. Use only clear solutions. The solution should be used within 20 minutes after recovery, inject the drug slowly over 3-4 minutes directly into a vein or through a catheter, drip-wise.
Preparation of solution for intravenous infusion
Reconstituted as shown above, the solution of 500 mg / 100 mg is then added without delay to 50 ml of infusion fluid or the solution of 1000 mg / 200 mg - up to 100 ml of infusion fluid (it is better to use a mini-container or burette). The infusion should be carried out over 30-40 minutes.
The solution for infusion is chemically and physically stable for 2-3 hours at a temperature of 25°C or 8:00 at a temperature of 5°C. From a microbiological point of view, it is better to administer the prepared solution immediately.
Various solvents can be used for intravenous infusions. A satisfactory concentration of the antibiotic is maintained at 5°C and at room temperature (25°C) in the recommended volumes specified in the instructions.
Amoxiclav Forte 312.5 mg/5 ml 100 ml Suspension
Amoxiclav Forte 312.5 mg/5 ml 100 ml suspension
Latin name: Amoksiklav® Pharmacological group: Penicillins Composition and dosage form: 1 film-coated tablet, 375 or 625 mg, contains amoxicillin (in the form of trihydrate) 250 or 500 mg, respectively, and clavulanic acid (in the form of potassium salt) 125 mg; in bottles of 15 pcs., in a box 1 bottle. Powder for the preparation of 100 ml suspension for oral administration; in dark glass bottles, in a box 1 dark glass bottle with a dosage spoon. 5 ml of the finished suspension or forte suspension contain 125 and 31.25 mg or 250 and 62.5 mg of active substances, respectively. 1 bottle with lyophilized powder 600 mg and 1.2 g for the preparation of an injection solution contains amoxicillin (in the form of sodium salt) 500 or 1000 mg and clavulanic acid (in the form of potassium salt) 100 and 200 mg, respectively; There are 5 bottles in a box. Pharmacological action: Broad spectrum antibacterial. Blocks the synthesis of peptidoglycan of the membrane of microbial cells (amoxicillin), inhibits beta-lactamases (clavulanic acid). Clavulanic acid forms a stable inactivated complex with these enzymes and protects amoxicillin from the loss of antibacterial activity caused by the production of beta-lactamases by the main pathogens and opportunistic microorganisms. Active against gram-positive aerobes: Streptococcus pneumoniae, S.pyogenes, S.viridans, S.bovis, Staphylococcus aureus (except methicillin-resistant strains), S.epidermidis (except methicillin-resistant strains), Listeria spp., Enterococcus spp. Gram-negative aerobes: Bordetella pertussis, Brucella spp., Campylobacter jejuni, E.coli, Gardnerella vaginalis, H.influenzae, H.ducreyi, Klebsiella spp., Moraxella catarrhalis, N.gonorrhoeae, N.meningitidis, Pasteurella multocida, Proteus spp., Salmonella spp., Shigella spp., Vibrio cholerae, Yersinia enterocolitica. Anaerobes: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Actinomyces israelii. Pharmacokinetics: Rapidly absorbed after oral administration (food intake does not affect absorption). Cmax is reached 1 hour after administration. Cmax in plasma after a bolus injection of 1.2 g is 105.4 mg/l (for amoxicillin) and 28.5 mg/l (for clavulanic acid). It has a large volume of distribution - high concentrations are found in body fluids and tissues (lungs, pleural, peritoneal, synovial fluid, tonsils, bronchial secretions, prostate gland, peritoneal abscess, muscle tissue, adipose tissue, paranasal sinus secretions, middle ear, etc. .). Peak concentrations in body fluids are observed 1 hour after peak plasma concentrations are reached. Does not pass through the BBB when the meninges are not inflamed, passes through the placental barrier and penetrates into breast milk in trace concentrations. Weakly binds to plasma proteins. Amoxicillin is partially metabolized, clavulanic acid undergoes intensive metabolism. Amoxicillin is excreted by the kidneys almost unchanged by tubular secretion and glomerular filtration; clavulanic acid - by glomerular filtration, partly in the form of metabolites. Small amounts are excreted by the intestines and lungs. T1/2 is 1–1.5 hours, with severe renal failure it increases to 7.5 (for amoxicillin) and 4.5 hours (for clavulanic acid). It is removed during hemodialysis, and slightly - during peritoneal dialysis. Indications: Infectious diseases of the upper (acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillopharyngitis) and lower respiratory tract (acute and chronic bronchitis, pneumonia, pleural empyema); urinary tract infections (including cystitis, urethritis, pyelonephritis), gynecological infections (including salpingitis, salpingoophoritis, endometritis, septic abortion, pelvioperitonitis); biliary tract (cholecystitis, cholangitis), bone and connective tissue (including chronic osteomyelitis), skin and soft tissue (phlegmon, wound infection), odontogenic infections (periodontitis); sexually transmitted infections (gonorrhea, chancroid). Contraindications: Hypersensitivity; history of allergic reactions to antibiotics of the penicillin and cephalosporin group; cholestatic jaundice, hepatitis caused by taking penicillin antibiotics (in history); liver failure; infectious mononucleosis, lymphocytic leukemia. Use during pregnancy and breastfeeding: Possible if the expected effect of therapy exceeds the potential risk to the fetus. Breastfeeding should be stopped during treatment. Side effects: In most cases, side effects are weak and transient, most often affecting the gastrointestinal tract: loss of appetite, nausea, vomiting, diarrhea. Possible development of superinfection, stomatitis, vaginitis; in rare cases - pseudomembranous colitis with severe diarrhea. Allergic reactions may occur: itching, skin rashes; in sensitive patients, immediate hypersensitivity reactions may develop (angioedema, bronchospasm, rarely - anaphylactic shock). It is extremely rare that a transient increase in the level of transaminases in the blood plasma can be observed. There are isolated reports of cholestatic jaundice, hepatitis, and liver dysfunction. Interaction: When used simultaneously with methotrexate, the toxicity of methotrexate increases, with allopurinol - the incidence of exanthema, and with anticoagulants - the prothrombin time is prolonged. Reduces the effectiveness of oral contraceptives. Concomitant use with disulfiram should be avoided. The effectiveness of Amoxiclav is weakened by combination with bacteriostatic antibiotics (macrolides, tetracyclines), combination with rifampicin is antagonistic. Probenecid reduces the excretion of amoxicillin, increasing its serum concentration. Pharmaceutically incompatible with solutions containing blood, proteins, lipids, glucose, dextran, bicarbonate. Do not mix in a syringe or infusion bottle with other drugs. Incompatible with aminoglycosides. Overdose: Symptoms: in most cases nausea, diarrhea, vomiting, possible - agitation, insomnia, dizziness, in some cases - seizures. There are no reports of deaths or life-threatening side effects. Treatment: symptomatic, in case of recent use (less than 4 hours), remove the drug from the gastrointestinal tract (gastric lavage, taking activated charcoal to reduce absorption), hemodialysis is effective. Method of administration and dosage: Orally, adults and children weighing more than 40 kg - 375 or 625 mg (depending on the severity of the infection) every 8 hours (table). Suspension for oral administration - children from 3 months to 1 year - 1/2 measuring spoon 3 times a day (suspension 156.24 mg/5 ml), 1-7 years - 1/2 measuring spoon (suspension forte) or 1 measuring spoon (suspension 156.24 mg/5 ml) 3 times a day; children 7–14 years old - 2 measuring spoons (suspension 156.24 mg/5 ml) or 1 spoon (suspension forte) 3 times a day. 1 measuring spoon corresponds to 156.25 mg/5 ml, 1/2 measuring spoon corresponds to 78.13 mg/2.5 ml). The suspension is prepared by adding 86 ml of water in 2 portions to the dry substance, the forte suspension - 85 ml of water in 2 portions, followed by shaking until the powder is completely dissolved. The maximum daily dose of amoxicillin is 6 g (for adults) and 45 mg/kg (for children); clavulanic acid (in the form of potassium salt) - 600 mg (for adults) and 10 mg/kg (for children). In case of renal failure, it is necessary to reduce the dose or increase the interval between doses (with Cl 10-30 ml/min, the interval between doses is 12 hours, less than 10 ml/min - 24 hours). IV, slowly (over 3-4 minutes) or as an infusion (over 30-40 minutes), adults and children over 12 years old - 1.2 g every 8 hours (in severe cases - every 6 hours) , children from 3 months to 12 years - 30 mg/kg (in terms of all Amoxiclav) every 8 hours (in severe cases - every 6 hours). Children up to 3 months: premature and newborns - 30 mg/kg (in terms of the entire Amoxiclav) every 12 hours, from 0 to 3 months - every 8 hours. The course of treatment is 5-14 days. To prepare a solution for intravenous injection, the contents of a 600 mg bottle are dissolved in 10 ml of water for injection, the contents of a 1200 mg bottle are dissolved in 20 ml of water for injection. To prepare a solution for intravenous infusion: 600 mg, resuspended in 10 ml of water for injection, added to 50 ml of infusion fluid; 1200 mg, resuspended in 20 ml water for injection to 100 ml infusion fluid. Precautions: Prescribed with caution to patients prone to allergic reactions to cephalosporins and other beta-lactam antibiotics (risk of cross-sensitivity), with severe impairment of liver and kidney function (dosage regimen adjustment is necessary). Special instructions: High concentrations give a false-positive reaction to glucose in urine when using Benedict's reagent or Felling's solution (it is recommended to use enzymatic reactions with glucose oxidase). Storage conditions: List B. In a dry place, at a temperature below 25 °C. The finished suspension is in the refrigerator.
Features of application
Use during pregnancy or breastfeeding
Pregnancy. Reproductive studies in animals of oral and parenteral forms of Amoxiclav ® did not reveal any teratogenic effects. One study in women with premature rupture of membranes reported that prophylactic use of the drug may be associated with an increased risk of necrotizing enterocolitis in the newborn. As with the use of other medicines, the use of Amoxiclav ® should be avoided during pregnancy, especially in the first trimester, unless, in the opinion of a doctor, such use is necessary.
Breastfeeding period. Both active components of the drug are excreted into breast milk (there is no information on the effect of clavulanic acid on a breastfed infant). Accordingly, a breastfed infant may develop diarrhea and fungal infection of the mucous membranes, so breastfeeding should be stopped. The possibility of allergic reactions should be taken into account. Amoxiclav ® can be used during breastfeeding only when, in the opinion of the doctor, the benefits of use will outweigh the risks.
Children
Use for children from the first days of life.
The ability to influence the reaction rate when driving vehicles or other mechanisms
Studies on the ability of the drug to influence the reaction rate when driving vehicles or other mechanisms have not been conducted. However, undesirable effects may occur (such as allergic reactions, dizziness, convulsions), which may affect the ability to drive a car or use other machinery (see section “Adverse Reactions”).
Overdose
Symptoms. Symptoms of gastrointestinal upset and fluid and electrolyte imbalance may occur. Crystalluria associated with taking amoxicillin has been observed, which in some cases led to renal failure (see section "Peculiarities of use").
In patients with impaired renal function and in patients taking high doses of the drug, seizures may occur.
Deposition of amoxicillin in bladder catheters has been recorded, mainly after administration in high doses. The patency of catheters should be regularly checked (see Section “Peculiarities of Application”).
Treatment. Gastrointestinal disorders can be treated symptomatically with attention to fluid/electrolyte balance.
Amoxicillin/clavulanic acid can be removed from the bloodstream using hemodialysis.
Interaction with other drugs and other types of interactions
Anticoagulants for oral use. Oral anticoagulants and penicillin antibiotics are widely used in practice without reports of interactions. However, cases of an increase in the international normalization coefficient have been described in patients taking acenocoumarol or warfarin and who were prescribed a course of treatment with amoxicillin. If concomitant use of drugs is necessary, the prothrombin index or international normalization ratio (INR) should be carefully monitored when amoxicillin is added or discontinued. In addition, it may be necessary to adjust the dose of anticoagulants for oral use (see Sections “Peculiarities of use” and “Adverse reactions”).
Methotrexate. Penicillins may reduce the elimination of methotrexate, causing a potential increase in toxicity.
Probenecid. Concomitant use of probenecid is not recommended. Probenecid reduces the renal tubular secretion of amoxicillin. Concomitant use of probenecid may lead to an increase in the level and duration of amoxicillin (but not clavulanic acid) presence in the blood.
Mycophenolate mofetil. In patients treated with mycophenolate mofetil, predose concentrations of the active metabolite MPA may decrease by approximately 50% after initiation of oral amoxicillin with clavulanic acid. This change in predose level may not be entirely consistent with the change in total MPA exposure. Therefore, a change in mycophenolate mofetil dosage is usually not required unless there is clinical evidence of graft dysfunction. However, close monitoring is necessary during coadministration and for some time after antibiotic therapy.
Amoxiclav: instructions for adults
The main rule of taking antibiotics is to follow the prescribed course of treatment. The mistake patients make is that at the first sign of a retreat in the symptoms of the disease, many give up treatment, believing that long-term antibiotic therapy causes irreparable damage to all body systems. However, in fact, this is precisely how resistant colonies of microorganisms are formed, which over time adapt to life even under the influence of an antibiotic. For example, for cystitis, a one-time dose of the drug relieves pain and pain already on the second day of treatment. But this is only the absence of symptoms.
The bacteria that caused this damage to the urinary system have not yet died, they have only lost their ability to provoke unpleasant symptoms of the disease. Stopping treatment early will allow the surviving bacteria to evolve so that the next time taking the same drug does not prevent them from multiplying and being active.
A single and daily dose is prescribed by the attending physician, because it depends on the severity of the disease and the patient’s condition. As a rule, the maximum dosage of Amoxiclav in the amount of 875 + 125 does not exceed twice the dose of the drug per day with an interval of 12 hours. To achieve maximum effect, you need to stick to the same hour of taking the drug. The duration of the course, regardless of the single dose and the number of prescribed doses, cannot be shorter than 7 days.
Note!
Description of the drug Amoxiclav por. d/r-ra d/in. 1000mg/200mg vial. No. 5 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
