Axetin

Axetine is a systemic antimicrobial drug. It contains the substance cefuroxime, which belongs to the cephalosporin category.

Indications Axetina

It is used for therapy of infections with various localizations and caused by the activity of microbes sensitive to cefuroxime. Among the diseases for which the medicine is used:

• bronchitis, chronic or acute, pneumonia of bacterial origin, pulmonary abscess, infected bronchiectasis, as well as lesions in the sternum area that are postoperative in nature;
• pharyngitis in the chronic or acute phase, as well as sinusitis, tonsillitis or otitis;
• cystitis or pyelonephritis occurring in chronic or acute form, and along with this, bacteriuria developing asymptomatically;
• wound infections or cellulitis;
• osteomyelitis and septic form of arthritis;
• having infectious genesis of inflammation in the pelvic area;
• acute gonorrhea (the drug is used as a second-line agent in case of hypersensitivity to penicillins);
• septicemia, meningitis or peritonitis.

Axetine is used to prevent the occurrence of complications of infectious origin during surgical procedures (for example, in the sternum or peritoneum), and also during orthopedic or gynecological operations.

The medication can be prescribed in combination with other drugs (for example, with aminoglycosides or metronidazole).

Release form

The drug is released in the form of a lyophilisate for the manufacture of parenteral fluid, inside vials with a volume of 750 or 1500 mg. There are 10 or 100 such vials inside a separate package.

Pharmacodynamics

Axetine is an antimicrobial agent with powerful bactericidal properties. Sensitivity to cefuroxime is demonstrated by a large number of pathogenic bacteria, including forms producing β-lactamase. Resistance to β-lactamases allows the drug to act effectively in infections associated with amoxicillin- or ampicillin-resistant strains. The effect of cefuroxime is due to the effect it has on the binding processes of components that form the basis of bacterial cell walls.

In vitro tests have shown the drug to be effective against Proteus rettgeri, Escherichia coli, Providencia, Proteus mirabilis and Influenza bacillus (including strains that are resistant to ampicillin). Also on the list are Haemophilus parainfluenzae (including ampicillin-resistant strains), Moraxella catarrhalis, Klebsiella, gonococci (including strains that produce penicillinase), Salmonella and Meningococci. In addition, it acts on pneumococci, Staphylococcus aureus, pyogenic streptococci and other β-lactam streptococci, epidermal staphylococci (including strains that produce penicillinase and are not resistant to methicillin), Streptococcus mitis (category viridans) and Streptococcus agalactiae. It affects Peptococci, whooping cough bacillus, Peptostreptococcus species, Fusobacterium, Bacteroides, most strains of Clostridia and Propionibacterium.

Tests also showed that strains of Borrelia burgdorferi exhibit sensitivity to cefuroxime.

Laboratory and clinical testing have shown resistance to cefuroxime in Campylobacter, Listeria monocytogenes, Clostridium difficile, Pseudomonas and Acinetobacter calcoaceticus. In addition, resistance is demonstrated by methicillin-resistant Staphylococcus epidermidis and Staphylococcus aureus, Enterobacter with Morgan's bacteria, Citrobacter, Proteus, Serratia, Legionella with Bacteroides fragilis, and Enterococcus faecalis.

During tests it was determined that the combination of cefuroxime and aminoglycosides produces an additive effect.

Pharmacokinetics

Serum Cmax level of the active element develops after 30-45 minutes from the moment of intramuscular injection. On average, the half-life of cefuroxime after parenteral injection is 70 minutes (the method of administration is not important). When combined with probenecid, the half-life of the active element of the drug is prolonged (due to which serum cefuroxime levels increase).

About 50% of serum cefuroxime is synthesized with proteins.

Within 24 hours after administration, the drug is almost completely (up to 90% of the used portion) and unchanged excreted from the plasma. The main part of the applied dosage is excreted during the first 6 hours.

Cefuroxime is not metabolized within the body and its excretion occurs via glomerular filtration and tubular secretion.

A significant decrease in Axetine values inside the plasma is observed in the case of dialysis procedures. The substance reaches high (higher than the minimum applicable inhibitory level) values inside the synovium with bone tissue and intraocular fluid. If the patient has lesions of the meninges (for example, in meningitis), the drug is found in the cerebrospinal fluid.

Dosing and administration

The lyophilisate is intended for the production of parenteral fluid. The prepared substance is administered only intravenously or intramuscularly. Before the start of the treatment cycle, it is necessary to conduct a drug tolerance test.

To prepare a solution for intramuscular injections, add injection water (3 ml) to a 750 mg vial and shake to obtain a uniform suspension.

To prepare a liquid for intravenous bolus injection, 6 ml of injection water is used for 750 mg of the drug, after which the bottle is shaken (for 1500 mg of Axetine, at least 15 ml of injection water is required).

For infusions (which should last a maximum of half an hour), 1500 mg of lyophilisate is diluted in 50-100 ml of injection water. The finished substance is administered intravenously. Alternatively, the drug can be administered through a dropper tube for general infusion therapy.

It is necessary to take into account that in case of storage of the prepared medicinal substance, it may change the saturation of the color.

The dosage of Axetin and the mode of its use are selected by a physician, taking into account the type of pathology and the general clinical condition of the patient.

For adults, 0.75 g of the drug is often used 3 times a day (administration intramuscularly or intravenously). If the infection leads to a serious condition of the patient, the amount of the administered substance is increased to 1500 mg with 3-times use per day (large portions of the drug should be administered intravenously). If necessary, the frequency of the procedure can be increased (6-hour intervals between injections), which will increase the total daily dosage to 3000-6000 mg of the substance.

Sometimes it is permissible to use cefuroxime in a dose of 0.75-1.5 g 2 times a day, followed by a transition to internal administration of the medication.

Sizes of dosage portions of medicines for children.

For children, 30-100 mg/kg of the substance is often used per day, and the dosage is divided into 3-4 administrations. On average, children need to use 60 mg/kg per day (this dosage is effective for most infections).

For newborns, the drug is prescribed in portions used for older children, but they must be divided into 2-3 administrations. In infants in the first weeks of life, the half-life of cefuroxime is longer than in older children, which is why the frequency of drug use may be lower.

Dosage sizes of medicine in different cases.

To treat gonorrhea, 1500 mg of the drug is administered once, or injections of 0.75 g of the drug are used in each buttock once.

For meningitis, the medication is used for monotherapy - in a dose of 3000 mg, 3 times a day (an 8-hour interval must be observed between injections; the total daily dosage is 9000 mg).

Children with meningitis are required to take 150-250 mg/kg of the drug per day (intravenous injections, divided into 3-4 doses).

For the treatment of meningitis in infants during the first weeks of life, 0.1 g/kg of the drug per day is often used (intravenous use with the dosage divided into 2-3 administrations).

During sequential treatment of pneumonia, 1500 mg of the drug is often administered 2-3 times a day (intramuscularly or intravenously; the total daily dose is 3-4.5 g) over 48-72 hours. Then the transition to taking the drug orally is made - 2 times a day, 0.5 g of the substance (over a period of 7-10 days).

In the sequential treatment of a relapse of chronic bronchitis, 2-3 injections of 0.75 g of the substance are often administered (intramuscularly or intravenously; the total daily dosage is 1.5-2.25 g of the drug) within 48-72 hours. The patient is then transferred to internal use of the drug - 2 times a day in the amount of 0.5 g (this cycle lasts 7-10 days).

In the case of sequential therapy, it is necessary to take into account that the period of transition from parenteral to oral administration, as well as the duration of the general treatment cycle, are calculated taking into account the severity of the infection and the clinical response of the patient.

Use of medicine for preventive purposes.

To prevent infectious complications after pelvic, orthopedic or abdominal surgery, 1500 mg of the substance is often administered with the induction of anesthesia. If necessary, a repeat injection of 0.75 g of the substance can be administered after 8 and 16 hours.

To prevent infection after surgical procedures on the lungs, heart with vessels and esophagus, 1500 mg of cefuroxime is generally administered with the induction of anesthesia. After using the initial dose, 0.75 g of the drug is prescribed 3 times a day for the next 24-48 hours.

In case of total joint replacement, 1500 mg of cefuroxime lyophilisate should be mixed with methyl methacrylate cement-polymer substance (1 packet) until the liquid monomer is added.

Dosage regimen for different groups of patients.

People with impaired renal filtration require a change in the dosage of the drug (because cefuroxime is mainly excreted in the urine).

Individuals with a CC level within 10-20 ml/minute should not administer more than 0.75 g of the substance 2 times a day.

Patients whose renal filtration values do not exceed 10 ml/minute are required to use a maximum of 0.75 g of the drug once a day. People undergoing dialysis should use the drug at the end of the session; in addition, additional addition of cefuroxime to the dialysis peritoneal fluid is allowed (usually about 0.25 g is required for every 2 l).

Persons receiving long-term arterial hemodialysis or high-speed hemofiltration (inpatient intensive care) are allowed to use 0.75 g of Axetin twice a day.

If the CC level exceeds 20 ml/minute, there is no need to change the dosage of the medication, although additional monitoring of the general condition of the patient is required (since in this condition the risk of negative symptoms increases).

Use Axetina during pregnancy

It is necessary to prescribe the drug very carefully in the first trimester (the use of drugs is allowed only in the presence of strict indications and in situations where safer drugs will be ineffective).

The drug is found in breast milk, so breastfeeding is prohibited when using it. Temporary discontinuation of breastfeeding is possible, followed by restoration under the supervision of a doctor.

Contraindications

Contraindicated for use in people with hypersensitivity to cefuroxime, and in addition, if there is a history of intolerance in the case of administration of cephalosporins.

Side effects Axetina

When using Axetin, negative symptoms often occur rarely and are mild. They may be associated with the underlying pathology and change depending on the existing indications for use.

Side effects that may occur after administration of cefuroxime include:

• lesions of infectious or invasive nature: superinfection (often due to long-term use of drugs);
• disorders in the blood system: a positive Coombs test, decreased serum hemoglobin levels, leuko- or neutropenia, hemolytic anemia, and eosinophilia. Cephalosporins, including cefuroxime, can be absorbed through the walls of red blood cells, after which they interact with antibodies and give a positive Coombs test, which can cause problems with determining the blood group, as well as the development of a hemolytic form of anemia (single);
• immune disorders: urticaria, generalized pruritus, rashes, drug hyperthermia, tubulointerstitial nephritis, as well as anaphylaxis, Quincke's edema and vasculitis. Before starting treatment, it is necessary to perform a sensitivity test;
• problems with gastrointestinal function: pseudomembranous colitis, vomiting, digestive disorders, transient hyperbilirubinemia and changes in liver test results (mainly if the patient has liver disease);
• damage to the subcutaneous layer with the epidermis: TEN, Stevens-Johnson syndrome and erythema polymorphum;
• dysfunction of the urogenital system: development of hypercreatininemia and an increase in serum urea nitrogen levels.

In addition, when using the drug parenterally, thrombophlebitis or pain in the injection area may occur. Such reactions depend on the dosage size (if large doses are used, the risk of pain in the injection area increases).

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Overdose

Intoxication with drugs from the cephalosporin group can cause manifestations that are associated with cerebral irritation (for example, the occurrence of seizures). In addition, poisoning increases the risk and severity of side effects characteristic of the substance cefuroxime.

If the patient has developed an overdose, it is necessary to immediately stop the administration of the drug (at a low infusion rate) and prescribe symptomatic procedures. If the intoxication is severe, a dialysis session may be prescribed to reduce the cefuroxime levels in the serum.

Interactions with other drugs

The drug is capable of weakening the medicinal effect of oral contraception - as it changes the intestinal microflora and disrupts estrogen absorption in the gastrointestinal tract. It is necessary to use additional contraceptive drugs that have a different principle of therapeutic effect, all the time of co-administration of Axetin.

When using cefuroxime, only hexose kinase or glucose oxidase methods for measuring serum sugar levels should be used. No effect of the drug on glucosuria testing data using enzymatic methods has been reported.

The drug may alter the results of tests performed using methods based on copper reduction processes (including the Benedict and Fehling tests, as well as the Clintest), but the development of false-positive responses in such procedures has not been observed (a similar effect is characteristic of some other cephalosporins).

Axetine does not interfere with creatinine tests that use alkaline picrate.

The drug must not be mixed with aminoglycoside agents within the same injection system or syringe.

Baking soda solution can change the color of cefuroxime, so it is not recommended to use it when making injections of the drug. However, if the patient needs to administer sodium bicarbonate through an infusion, it is allowed to use cefuroxime through a dropper tube.

1500 mg of the drug, diluted in injection water (15 ml), can be combined with metronidazole (ratio 0.5 g/0.1 l). Such liquids remain active for the next 24 hours under standard room temperature conditions.

1500 mg of cefuroxime and 1000 mg of azlocillin, which are dissolved in 15 ml of injection water (or 5000 mg of azlocillin is used in 50 ml of injection water) remain active for 6 hours (at room temperature) and 24 hours (if the storage temperature is 4 ^o C).

Cefuroxime (5 mg/ml dose) in 5-10% injection xylitol may be kept at room temperature for a maximum of 24 hours.

The drug can be mixed with lidocaine solutions (the concentration should be maximum 1%).

The drug can be mixed with most infusion fluids. For example, the drug remains active for the next 24 hours (at room temperature) after dilution in the following solutions:

• 0.9% NaCl;
• 5% injectable glucose;
• 0.18% NaCl with 4% injection glucose;
• 5% glucose with 0.9%, 0.45% or 0.225% NaCl;
• 10% injectable glucose;
• Ringer's lactate or Ringer's;
• Hartman.

The stability of the drug (after mixing with 0.9% NaCl and 5% glucose) does not change when combined with sodium hydrocortisone phosphate.

Compatibility is also noted (stability for up to 24 hours under room conditions) with infusion fluids containing heparin (at a dosage of 10-50 U/ml), in 0.9% NaCl for infusions together with CaK (portion 10-40 mEq/l) in 0.9% infusion NaCl.

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Storage conditions

Aksetin should be kept in a place closed to small children. The finished medicinal liquid should not be stored, but if immediate administration is not possible, it can be stored at a temperature of 2-8 ^o C for a maximum of 24 hours.

Shelf life

Axetine can be used within 2 years from the date of manufacture of the pharmaceutical product.

Analogues

The analogs of the drug are Zinnat, Proxim, Cetyl with Zinacef, Cefumax, Cefutil with Aksef and Cefuroxime with Baktilem.