Pharmacological properties of the drug Betaclave
Betaclave is a combination drug that contains amoxicillin (a broad-spectrum penicillin antibiotic) and clavulanic acid (a powerful irreversible β-lactamase inhibitor). Amoxicillin inhibits the last stage of bacterial cell wall construction by inhibiting the activity of transpeptidases, enzymes involved in the synthesis of peptidoglycan, which is an important component of the outer membrane of bacteria. Inadequate synthesis of peptidoglycan causes the formation of a deformed, osmotically unstable outer membrane, which leads to destruction and death of the bacterial cell. Penicillins can also damage the bacterial cell wall by inhibiting the activity of an inhibitor of murein hydrolase, an enzyme involved in cell division. Clavulanic acid has little antibacterial activity, but it acts as a potent irreversible inhibitor of β-lactamases. It forms stable inactive complexes with enzymes and, as a result, prevents the breakdown of amoxicillin. Betaclave has a bactericidal effect on gram-positive and some gram-negative bacteria, including bacteria producing β-lactamases and microorganisms resistant to amoxicillin: gram-positive aerobic bacteria - Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus agalactiae, Staphylococcus aureus, Staphylococcus epidermidis, List eria monocytogenes, Enterococcus faecalis, Enterococcus faecium, Corynebacterium spp., Bacillus anthracis, Nocadia asteroides; gram-negative aerobic bacteria - Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Proteus spp., Klebsiella spp., Neisseria gonorrhoeae, Neisseria meningitidis, Bordetella pertussis, Brucella spp., Pasteurella multocida, Salmonella spp., Shigella spp., Vibrio cholerae, Yerisinia enterocolitica ; anaerobic bacteria - Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Fusobacterium spp. 5 minutes after intravenous administration of 1.2 g of Betaclava, the concentration of amoxicillin in the blood serum is 99 mcg/ml, and the concentration of clavulanic acid is 27 mcg/ml. When taken orally, the absorption of amoxicillin in the gastrointestinal tract is 90%, clavulanic acid - 60%. After absorption, 30% of clavulanic acid and 20% of amoxicillin are bound to blood proteins. Amoxicillin and clavulanic acid readily penetrate body tissues and fluids, with the exception of the brain and CSF. The degree of their accumulation is dose-dependent. Amoxicillin and clavulanic acid easily penetrate the placental barrier and are excreted in small amounts in breast milk. An infant may experience sensitization to the components of the drug. The half-life of amoxicillin and clavulanic acid is about 1 hour. Clavulanic acid is intensively metabolized in the liver, excreted primarily by the kidneys, and partially excreted in feces and exhaled air. The renal elimination of amoxicillin from the body is carried out mainly by tubular secretion, and clavulanic acid - mainly by glomerular filtration, therefore probenecid does not affect the excretion of clavulanic acid. In the first 6 hours, 60–80% of amoxicillin in active form is excreted in the urine. For clavulanic acid, this amount is 30–50%. A decrease in creatinine clearance to a level of ≤10 ml/min leads to the accumulation of clavulanic acid in the body.
Indications for use of the drug Betaclave
Infections caused by gram-positive and gram-negative bacteria sensitive to the drug: ENT organs and respiratory tract - acute sinusitis, otitis media, recurrent tonsillitis, acute bronchitis, chronic bronchitis in the acute phase, pneumonia, empyema, lung abscess; skin and soft tissues - boils and abscesses, phlegmon, infected wounds, including after animal bites; genitourinary system - cystitis, urethritis, pyelonephritis, septic abortion, pelvic infections, chancroid, gonorrhea; other infections - osteomyelitis, sepsis, diverticulitis, liver abscess, biliary tract infections and periodontal infections; prevention of infections during surgical interventions on the gastrointestinal tract, pelvic organs, head and neck, heart, kidneys, biliary tract, as well as joint replacement.
Use of the drug Betaclave
Powder for the preparation of injection solution The drug is administered by intravenous infusion over 3–4 minutes. The dose depends on the severity of the infectious disease, the age and body weight of the patient, as well as renal function. Adults and children over the age of 12 years are usually prescribed 1.2 g every 8 hours, and for severe infections - every 6 hours. Children aged 3 months to 12 years with body weight ≤40 kg are prescribed 30*–55* * mg/kg body weight every 8 hours, and for severe infections - every 6 hours. Newborns (under 1 month), including premature ones, are prescribed 30*–55** mg/kg every 12 hours, and severe infections - every 8 hours. Infants (1–3 months) are prescribed 30*–55** mg/kg every 8 hours. To prevent postoperative infections, 1.2 g of the drug is administered intravenously before anesthesia. If the surgical intervention lasts 1 hour, the patient can be given 3 more injections every 8 hours. The duration of use of the drug in adults and children should not exceed 14 days, provided that the clinical need for further use of the drug has not been re-evaluated. If the patient's condition allows, it is recommended to switch to taking the drug for oral administration.
Dosing of the drug for renal failure
Kidney function | Adults | Children |
| Creatinine clearance 0.5 ml/s (30 ml/min) | No dosage adjustment required | No dosage adjustment required |
| Creatinine clearance 0.16–0.5 ml/s (10–30 ml/min) | Initial dose: 1.2 g, then 600*** mg every 12 hours | 30* mg/kg every 12 hours |
| Creatinine clearance ≤0.16 ml/s (10 ml/min) | Initial dose: 1.2 g, then 600*** mg every 24 hours | 30* mg/kg every 24 hours |
| Patients undergoing hemodialysis | Initial dose - 1.2 g, then 600*** mg every 24 hours and 600*** mg after the end of hemodialysis | 30* mg/kg every 24 hours and 15* mg/kg after the end of hemodialysis |
Notes: *30 mg corresponds to 25 mg amoxicillin and 5 mg clavulanic acid; **55 mg corresponds to 45 mg amoxicillin and 10 mg clavulanic acid; ***600 mg corresponds to 500 mg amoxicillin and 100 mg clavulanic acid.
The solution for injection must be prepared immediately before administration. When dissolved, a transparent pink solution is formed, which later becomes yellow or slightly opalescent. The contents of the bottle should be dissolved in at least 20 ml of water for injection or 0.9% sodium chloride solution for injection and administered intravenously slowly (over 3–4 minutes). Tablets Take orally without chewing, with a glass of water, immediately before meals. Adults, adolescents and children weighing 40 kg are prescribed 1 Betaclava tablet every 12 hours (2 times a day). The duration of taking the drug should not exceed 14 days without repeated medical examination. The dose of the drug for patients with impaired renal function should be reduced. In case of moderately severe renal failure (creatinine clearance 0.5 ml/s or 30 ml/min), no dose adjustment is required. In case of renal failure with a creatinine clearance of 0.16–0.5 ml/s or 10–30 ml/min, 1 Betaclava tablet (625 mg) is prescribed every 12 hours (2 times a day).
Overdose
Symptoms Adverse reactions from the digestive tract and disturbances in water and electrolyte balance may occur. Amoxicillin-induced crystalluria has been reported, leading to renal failure in some cases.
Seizures may occur in patients with impaired renal function or those receiving high doses.
Treatment. Symptomatic, correction of water and electrolyte balance. The drug can be removed from the circulation by hemodialysis.
Side effects of the drug Betaclave
The most common symptoms are diarrhea, nausea and vomiting. During treatment, superinfection caused by resistant microorganisms may develop. It is possible to develop candidal stomatitis and vaginitis or pseudomembranous colitis with severe and persistent diarrhea. In this case, the drug should be discontinued and adequate treatment prescribed. Hypersensitivity reactions are possible, such as pruritus, maculopapular rash, urticaria, exfoliative dermatitis, toxic epidermal necrolysis and vasculitis, arthralgia, myalgia, angioedema, bronchospasm, anaphylactic shock, erythema multiforme, and in isolated cases, Stevens-Johnson syndrome. In some cases, an increase in the activity of liver enzymes was noted, in isolated cases - cholestatic jaundice, hepatitis, liver failure, interstitial nephritis and hematuria, liver failure. The latter most often develops in men, elderly people (over 65 years old) and with a treatment duration of 14 days. Possible development of leukopenia, thrombocytopenia, eosinophilia, anemia, including hemolytic anemia. Side effects from the central nervous system occur extremely rarely. Dizziness, headache, confusion, hallucinations and seizures may occur. These effects may occur mainly in patients with renal failure or when the drug is administered in very high doses. Possible pain, swelling and thrombophlebitis at the injection site.
Special instructions for the use of the drug Betaclave
The drug should be used with extreme caution in patients with hypersensitivity to cephalosporins and other β-lactam antibiotics due to possible cross-hypersensitivity. The drug should be prescribed with caution to patients with liver failure (including patients with a history of liver failure). Betaclave can increase the activity of transaminases (AlAT and AST), alkaline phosphatase and bilirubin levels in the blood serum. With prolonged use of the drug, it is recommended to monitor hematological parameters, as well as the functional state of the kidneys and liver. In patients with moderate to severe renal failure, it is recommended to increase the interval between drug administration. During the treatment period, superinfection caused by drug-resistant microorganisms ( Clostridium difficile, Candida spp. ) may develop. In case of severe and persistent diarrhea, which may indicate the development of pseudomembranous and hemorrhagic colitis, it is necessary to stop using the drug and prescribe appropriate treatment. The drug is not recommended for use in patients with lymphocytic leukemia or infectious mononucleosis, since such patients are more likely to develop allergic skin reactions when treated with amoxicillin. During treatment, patients should take sufficient fluids as the risk of crystalluria and renal failure may increase. When high concentrations of amoxicillin are created at room temperature, the urine may precipitate on the walls of the catheter installed in the bladder, so the patency of the catheter should be checked regularly. Betaclava, a powder for the preparation of an injection solution, contains 63 mg (2.74 mmol) sodium and 39.2 mg (1 mmol) potassium, which is important to consider in patients following a diet low in sodium and potassium. After parenteral administration, pain or inflammation may be observed at the injection site of the drug, which is due to the presence of potassium in its composition. Although there are no reports of a negative effect of Betaclava on the fetus or on the newborn when taking the drug during pregnancy, Betaclave can be prescribed during pregnancy only if the expected therapeutic effect for the mother exceeds the potential risk to the fetus. Both active components of Betaclava penetrate the placental barrier and are excreted into breast milk. Breastfeeding during treatment with Betaclava may contribute to the development of hypersensitivity to the components of the drug in an infant. Taking Betaclava does not affect the ability to drive vehicles or operate machinery. During treatment with the drug, a high concentration of amoxicillin in the urine may give a false-positive result for determining glucose in the urine using non-enzymatic methods. During treatment with Betaclava, a false positive result from the Coombs test is also possible.
Note!
Description of the drug Betaclave por. d/oral. susp. 400mg/57mg/5ml fl. 70ml 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.
Drug interactions Betaclave
Caution must be exercised when treating patients who are taking oral anticoagulants, since their simultaneous use with Betaclave may enhance the effect of these drugs and cause bleeding. When amoxicillin is used concomitantly with allopurinol, a skin rash may develop. The simultaneous use of Betaclava and probenecid increases the concentration of amoxicillin in the blood serum, while the concentration of clavulanic acid does not change. With the simultaneous use of Betaclava and methotrexate, the concentration of methotrexate in the blood serum increases, as well as its toxicity. The drug reduces the effectiveness of oral hormonal contraceptives.
Storage conditions
This medicine does not require special temperature storage conditions.
Store in original packaging to protect from moisture.
The prepared suspension should be stored in the refrigerator at a temperature of 2°C to 8°C.
Keep out of the reach of children.
Shelf life: 3 years.
Product description certified by the manufacturer KRKA
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Verified by
Likar Turumkulova Irina
