Aczel

Aksetin is a systemic antimicrobial drug. Contains the substance cefuroxime, which is included in the category of cephalosporins.

Indications Axetina

It is used for therapy in infections that have a variety of localizations and are provoked by the activity of microbes sensitive to cefuroxime. Among the diseases in which the drug is used:

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

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

Medication can be given in combination with other drugs (eg, with aminoglycosides or metronidazole).

Release form

The drug is sold as a lyophilizate for the manufacture of parenteral fluid, inside flasks that have a volume of 750 or 1500 mg. Inside a separate package, 10 or 100 such bottles.

Pharmacodynamics

Aksetin is an antimicrobial agent with powerful bactericidal properties. Sensitivity to cefuroxime shows a large number of pathogens, among which are forms that produce β-lactamase. Resistance to β-lactamases allows the drug to function 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 the components that are the basis of the bacterial cell walls.

In vitro tests, the efficacy of the medicament against the Röttger protein, Escherichia coli, Providence, Proteus mirabilis and Influenza sticks was found (including strains that are resistant to ampicillin). Also in the list of Haemophilus parainfluenzae (here the ampicillin-resistant strains are taken into account), moracelli catarrils, klebsiella, gonococci (among them strains producing penicillinase), salmonella and meningococci. In addition, it acts on pneumococci, Staphylococcus aureus, pyogenic streptococci and other β-lactam streptococci, epidermal staphylococci (including strains producing penicillinase and not resistant to methicillin), streptococcus mitis (viridans) and streptococci agalactia. The effect is on peptococci, pertussis wand, Peptostreptococcus species, fusobacteria, bacteroids, most of the strains of clostridia and propionibacteria.

The tests also showed that the susceptibility to cefuroxime is demonstrated by the strains of Borredorfer's Borrelia.

In laboratory as well as clinical testing, the stability of Campylobacter, Listeria monocytogenes, Clostridium Differite, as well as pseudomonad and Acinetobacter calcoaceticus with respect to cefuroxime was revealed. In addition, methicillin-resistant epidermal and golden staphylococci, enterobacteria with Morgan bacteria, cytrobacteria, common proteins, serrations, legionella with bacteriomas fragilis, and fecal enterococci demonstrate stability.

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

Pharmacokinetics

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

About 50% of serum cefuroxime is synthesized with proteins.

During the 24 hours after the administration of the drug is almost fully (up to 90% of the used portion) and in the unchanged state is removed 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 is by glomerular filtration and tubular secretion.

There is a significant decrease in Aksetin's indices inside the plasma in the case of dialysis procedures. The substance reaches high (higher than the minimum applicable inhibitory level) values within the synovium with bone tissues and intraocular fluid. If the patient has lesions of the brain membranes (for example, with meningitis), the medicine is found inside the liquor.

Dosing and administration

The lyophilizate is intended for the manufacture 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 make a remedy for injections of injections, injected water (3 ml) is added to a flask of 750 mg volume, after which it is shaken to obtain a uniform suspension.

To make liquid for intravenous bolus injection, 6 ml of injection water is used for 750 mg of the drug, after which the vial is shaken (for 1500 mg of Aksetin, a minimum of 15 ml of injection water is necessary).

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

It must be taken into account that in the case of storage of the prepared medicinal substance, it can change the saturation of the hue.

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

For adults, 0.75 g of medicament is often used 3 times a day (administration in / m or in / in the method). If the infection leads to a severe condition of the patient, the amount of the injected substance is increased to 1500 mg with 3-time use per day (large portions of the drug should be administered by IV). If required, 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 allowed to use cefuroxime in a portion of 0.75-1.5 g 2 times a day, with a subsequent transition to an internal medication intake.

Dimensions of dosage portions of drugs for children.

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

For newborns, the drug is prescribed in the portions used for older children, but they must be divided into 2-3 injections. In infants in the first weeks of life, the half-life of cefuroxime is longer than that of older children, which can lead to a lower incidence of drug use.

The sizes of portions of the medicine in different cases.

For the treatment of gonorrhea, 1500 mg of the drug is administered 1-fold or nyxes of 0.75 g of drugs are administered to each of the buttocks once a day.

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

Painful meningitis requires the use of 150-250 mg / kg of the drug per day (intravenous injections, divided by 3-4 injections).

Infants during the first weeks of life for the treatment of meningitis often use 0.1 g / kg of medication per day (intravenous use with the division of the dosage into 2-3 injections).

During the successive treatment of pneumonia, a dose of 1500 mg of the drug (intramuscularly or intravenously, the total daily dose of 3-4.5 g) is often performed in 48-72 hours. Next, the transition to taking the drug inside - 2 times a day for 0.5 g of substance (in the period of 7-10 days).

In the sequential treatment of a developed recurrence of bronchitis, which has a chronic nature, 0.75 g of the substance (intramuscular or intravenous, the total daily dosage amount is 1.5-2.25 g of the drug) is often performed in the range of 48-72- hours. Further, the patient is transferred to the internal use of drugs - 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, is calculated taking into account the severity of the infection and the clinical response of the patient.

Use of medicines for prophylaxis.

To prevent the emergence of complications of an infectious nature after pelvic, orthopedic or abdominal operations, 1500 mg of the substance is frequently administered together with induction of anesthesia. If required, a repeat injection of 0.75 g of the substance can be performed after 8 and 16 hours.

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

In the case of a complete replacement of the joint, 1500 mg of cefuroxime lyophilizate with methyl methacrylate cement-polymer substance (1 pack) must be mixed until a liquid monomer is added.

Dosage regimen for different groups of patients.

People with weakened renal filtration need to change the dosage of the drug (therefore, as cefuroxime is mainly excreted together with urine).

Persons 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 require a maximum of 0.75 g of 1-fold drug per day. People who are on dialysis should use the drug at the end of the session; In addition, additional addition of cefuroxime to the dialysis peritoneal fluid is possible (often approximately 0.25 g for every 2 liters).

Persons receiving long-term hemodialysis of arterial character or hemofiltration at high speed (intensive therapy in a hospital) are allowed to use 2 times a day for 0.75 g of Aksetin.

At a QC level exceeding 20 ml / minute, you do not need to change the dosage of the medication, although you must additionally observe the general condition of the patient (since in this condition the risk of negative symptoms increases).

Use Axetina during pregnancy

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

The medication is found inside the mother's milk, so breast-feeding during its use is prohibited. Possible temporary cancellation of breastfeeding with further recovery under the supervision of a doctor.

Contraindications

It is contraindicated to use people with hypersensitivity to cefuroxime, and in addition, if there is an anamnesis indicating the appearance of intolerance in the case of cephalosporins.

Side effects Axetina

When using Aksetin negative symptoms often occur rarely and have a mild severity. They can be associated with the underlying pathology and vary with the available indications for use.

Among the side symptoms that can appear after the administration of cefuroxime:

• lesions that are infectious or invasive in nature: superinfection (often due to prolonged use of drugs);
• violations in the blood system: a positive result of Coombs test, a decrease in serum hemoglobin, leuko- or neutropenia, hemolytic anemia, and eosinophilia. Cephalosporins, including cefuroxime, are able to be absorbed through the walls of erythrocytes, after which they interact with antibodies and give a positive Coombs test, which can lead to problems in determining the blood group, and also to develop a hemolytic form of anemia (singly);
• immune disorders: urticaria, generalized itching, rashes, drug hyperthermia, tubulointerstitial nephritis, and in addition anaphylaxis, Quincke edema and vasculitis. Before starting treatment, it is necessary to perform a sensitivity test;
• problems with the function of the gastrointestinal tract: pseudomembranous variety of colitis, vomiting, digestive disorders, transient hyperbilirubinemia and changes in the results of liver samples (mainly if the patient has hepatic disease);
• defeat of the subcutaneous layer with the epidermis: TEN, Stevens-Johnson syndrome and erythema erythema;
• disturbances in the function of the urogenital system: development of hypercreatininemia and an increase in serum nitrogen urea levels.

In addition, with parenteral use of drugs may occur thrombophlebitis or pain in the area of the injection. The dependence of such reactions on the dosage size is observed (in case of using large portions, the risk of pain in the area of drug administration increases).

[1]

Overdose

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

If a patient develops an overdose, it is necessary to stop the medication immediately (at a low infusion rate) and to prescribe symptomatic procedures. If intoxication has a severe degree of severity, a reduction in cefuroxime within the serum may be indicated by a dialysis session.

Interactions with other drugs

The medication is able to weaken the medicinal effect of oral contraception - as it changes the intestinal microflora and disrupts estrogenic absorption inside the gastrointestinal tract. It is required to use additional contraceptive preparations having a different principle of therapeutic influence, all the time of joint administration of Aksetin.

When using cefuroxime, only hexose kinase or glucose oxidase methods of measuring serum sugar values should be used. The effect of the drug on the glucosuria test data was not recorded using enzyme methods.

The drug can modify the test data, carried out using methods that are based on copper recovery processes (among them Benedict's tests with Feling, and Klinist), but the development of false positive responses in such procedures was not observed (a similar effect is characteristic of some other cephalosporins).

Aksetin does not affect the readings of tests of creatinine levels, in which an alkaline picrate is used.

Do not mix the drug with aminoglycoside drugs inside one injection system or a syringe.

A solution of baking soda can change the shade of cefuroxime, so it is not recommended to use it in the manufacture of injections of the drug. However, if a patient needs to enter sodium bicarbonate through infusion, cefuroxime can be used through the dropper tube.

1500 mg of the drug, diluted in injectable water (15 ml), can be combined with metronidazole (a ratio of 0.5 g / 0.1 l). Such liquids remain active during 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 are used per 50 ml of injection water) continue to be active for 6 hours (at room temperature) and 24 hours if the storage temperature of 4 ^on C).

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

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

The medication is allowed to mix with most of the fluids for infusions. For example, the drug remains active for the next 24 hours (in room conditions) after dilution in such solutions:

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

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

Compatibility is also noted (stability up to 24 hours in room conditions) with infusion liquids containing heparin (in a dosage of 10-50 U / ml), in 0.9% NaCl for infusions along with CaK ( 10-40 meq / L) in 0.9% infusion NaCl.

[2], [3]

Storage conditions

Aksetin must be kept out of the reach of small children. You can not save a formulation fluid, but the impossibility of immediate introduction, it can be stored at a temperature elevations within 2-8 ^on C for a maximum of 24 hours.

Shelf life

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

Analogues

Analogues of the medication are preparations of Zinnat, Proxim, Cetil with Zinatsef, Cefumax, Cefutil with Aksef and Cefuroxime with Bactilem.