Cefanthral

Cefanthral is an antimicrobial systemic drug from the category of cephalosporins of the 3rd generation. Also included in the group of other β-lactam type antibiotics.

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Indications of the cephanthral

It is used for the elimination of infectious lesions, provoked by the action of microbes sensitive to medicine:

• ENT-system (otitis, as well as angina);
• lesions affecting the respiratory system (pulmonary inflammation, bronchitis, abscess, as well as pleurisy);
• infection in the area of the urogenital system;
• infection of the blood, as well as bacteremia;
• infection with localization in the intra-abdominal area (this includes also peritonitis);
• lesions of soft tissues with skin;
• disorders affecting joints with bones;
• meningitis (except listeriosis form), as well as other infections in the central nervous system.

To prevent the occurrence of infections after performing surgical procedures in the digestive system, as well as after obstetric-gynecological or urological operations.

Release form

The release occurs in the form of lyophilizate, used in the manufacture of therapeutic solutions. In the box - 1 bottle with powder.

Pharmacodynamics

The element cefotaxime is a semisynthetic antibiotic from the 3rd generation of cephalosporins. It is used parenterally. It has bactericidal action and a wide range of drug activity.

Sensitivity to the medicine is possessed by:

• streptococci (except for category D), among which also pneumococcus;
• Staphylococcus aureus, as well as strains that produce and do not produce penicillinase;
• hay bacillus and mushroom stick;
• gonococci (strains that produce and do not produce penicillinase), meningococci and other types of Neisseria;
• E. Coli;
• Klebsiella (this includes also Friedlander's wand);
• Enterobacteria (individual strains are resistant) and serrations;
• Proteus (indolpositive, and in addition indolotritsatelnye types);
• Salmonella, Citrobacterium, Shigella, Providence, Yersinia;
• wand influenza and Haemophilus parainfluenzae (strains that produce / do not produce penicillinase, and in addition are resistant to ampicillin), as well as Borde-Zhangu bacteria;
• moraxelles, hydrophilic aeromonad, veylonelli, clostridia perfringens;
• eubacteria, propionic acid bacteria, fusobacteria, bacteroides, and at the same time Morganella.

Persistent sensitivity to the drug has: Pseudomonas aeruginosa, Acinetobacter, Helicobacter pylori, bacteroidoid fragilis and Clostridium Differite.

Resistance to cefanthral is shown by methicillin-resistant staphylococci, as well as streptococci from category D and listeria.

Pharmacokinetics

Absorption.

After 5 minutes after a one-time injection of drugs at a rate of 1 g, the serum level of the substance reaches 100 μg / ml. Peak values of the drug inside the blood are observed after a half an hour and equal 24 μg / ml. Bactericidal indices inside the blood remain for another 12 hours.

Distribution values.

Protein synthesis inside the blood plasma is approximately 25-40% (mean). Cefotaxime quickly passes into tissues with biological fluids. Effective drug concentrations are observed within synovia, peritoneal and pleural fluid. The drug passes through the BBB. During metabolism, an active degradation product is formed.

Excretion.

About 60-70% of the administered portion is excreted in the form of an unchanged substance along with urine, and the remainder is excreted as metabolic products. Part of the medicine is excreted with bile.

The half-life is equal to 1 hour after intravenous injection, and also 1-1.5 hours after the injection.

In elderly people, and in addition, if the kidneys are deficient, the elimination half-life is approximately doubled.

In newborns, the half-life of the drug reaches 0.75-1.5 hours, and in premature infants - about 1.4-6.4 hours.

Dosing and administration

The drug is used for the / m, as well as intravenous (drip or jet) injections.

Before using the medication, a skin test should be performed to determine sensitivity with respect to the antibiotic with lidocaine. If lidocaine is used for IV injections in the form of a solvent, data on the safety of this substance should be taken into account.

For jet injections, 1 g of lyophilizate should be diluted in injectable water (8 ml). The rate of administration should be low - the procedure lasts 3-5 minutes.

With IV infusion, a 50 ml solution of sodium chloride (0.9%) or glucose (5%) is required to dilute 1 g of lyophilizate. This infusion lasts for 50-60 minutes.

If I / m is administered, 1 g of the drug is diluted in sterile injectable water (4 ml) or in lidocaine solution (1%). The injection is made deep into the buttock muscle.

Selection by the attending physician of the duration of the therapeutic course occurs individually.

Children weighing more than 50 kg, and adults are required to use the drug in a dosage of 1 g, with intervals of 12 hours. In severe diseases, cefanthral in a dose of 1 g is administered 3-4 times / day.

During the day, patients are allowed to inject no more than 12 grams of solution.

Multiplicity of drug administration and serving sizes:

• treatment of infections of uncomplicated nature, and in addition to this defect in the area of the urinary system - the introduction of / in or in / m way of the first g of the drug at intervals of 12 hours;
• treatment for acute gonorrhea of uncomplicated nature - use in a dosage of 1 g, administered once a day intravenously or intramuscularly;
• elimination of infections of moderate severity - application of the solution in a dosage of 1-2 g, with intervals of 12 hours;
• therapy for severe forms of infectious disorders (such as meningitis) - the administration of drugs in a dose of 2 g at intervals of 6-8 hours.

For a child weighing less than 50 kg, the drug should be prescribed in a dose of 50-100 mg / kg / day. This portion should be divided into 3-4 intravenous or intravenous injection procedures. If the patient has a severe form of impairment (eg, meningitis), it is allowed to increase the daily dose to 100-200 mg / kg, with IV or IV injection 4-6 times.

Preterm infants and infants up to the first 7 days of life should be given 50 mg / kg of medication per day. This portion is divided into 2 equal parts and injected in / in the method.

Infants from 8 days to 1 month of life should use 50-100 mg / kg of the drug per day. The dosage is divided into 3 equal portions and administered as an intravenous injection.

To prevent the emergence of infections as a result of surgery, it is necessary before administering the patient anesthesia to perform a one-time injection of the 1st g of drugs. If necessary, repeat this procedure after 6-12 hours.

If a person has problems with kidney function, the dosage of Cephanthral should be reduced. At CC values up to 10 ml / minute, it is necessary to reduce the daily portion of medicines by half.

Use of the cephanthral during pregnancy

Use cefantral during pregnancy is prohibited.

For the duration of therapy, breastfeeding should be abandoned.

Contraindications

Among the contraindications:

• hypersensitivity to cephalosporin antibiotics and other β-lactam antibiotics, and also lidocaine intolerance (with an / m introduction);
• presence of bleeding;
• a history of enterocolitis (especially the ulcerative form of colitis, which has a nonspecific character);
• AV blockade, until the heart rate was determined;
• heart failure in severe degree.

It is forbidden to inject the medicine in / m in children younger than 2.5 years.

Side effects of the cephanthral

The use of the solution can cause the appearance of such side effects:

• digestive disorders: the appearance of swelling, vomiting, abdominal pain, nausea and diarrhea, as well as the development of dysbiosis. Occasionally there is glossitis or stomatitis, and in addition colitis is pseudomembranous;
• allergy symptoms: the appearance of itching, rashes, bronchial spasm, hyperemia, urticaria, polyiform erythema, TEN and Stevens-Johnson syndrome. In addition, the development of edema Quincke, fever and anaphylactic manifestations. Occasionally, anaphylaxis is noted;
• lesions of the hepatobiliary system: development of functional hepatic disorders, hepatitis, jaundice, acute stage of liver failure, and in addition to this cholestasis;
• biochemical data: an increase in the values of liver transaminases, alkaline phosphatase, LDH and bilirubin, and in addition to the level of creatinine and urea nitrogen. At the same time, a positive test of Coombs may be noted;
• lesions of peripheral blood flow: the development of neutro-, thrombocyto- and granulocytopenia, and besides this transient leukopenia, anisocytosis with agranulocytosis, hypocoagulation, hemolytic form of anemia and eosinophilia with hypoprothrombinemia;
• disorders of the HC function: the appearance of dizziness, a feeling of weakness or severe fatigue, and also convulsions and headaches. Also, curable encephalopathy can develop;
• manifestations in the field of administration: infiltrate infiltration and pain sensations in the injection site, pain spreading along the vein, and in addition phlebitis and tissue inflammation;
• symptoms caused by biological effects: superinfection may occur (among them also vaginitis with candidiasis);
• other: the appearance of hemorrhages or bleeding, the development of a hemolytic form of anemia of an autoimmune nature or tubulointerstitial nephritis, as well as arrhythmia (if a rapid jet injection is performed).

During therapy for infections that are caused by the activity of spirochaetes, complications (such as the Yarisch-Gerxheimer reaction) are possible. As a result, chills, fever, pain in the joints and headaches can develop.

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Overdose

Among the signs of poisoning: leuko- or thrombocytopenia, fever, hemolytic form of anemia in the acute stage, skin symptoms, gastrointestinal tract, liver, stomatitis, dyspnoea, anorexia, and, in addition, kidney failure, temporary hearing loss, encephalopathy in particular in persons with kidney failure) and loss of spatial orientation.

The drug has no special antidote. Plasma values of cefotaxime can be reduced by peritoneal dialysis or hemodialysis. If necessary, perform symptomatic procedures.

If the victim develops anaphylaxis, urgent action is required. After the appearance of the first symptoms of the reaction of intolerance (such as urticaria, rashes, nausea, loss of consciousness and headache), it is necessary to stop the administration of the drug. In case of severe signs of hypersensitivity or anaphylactic manifestations, it is necessary to conduct appropriate measures (enter the patient with SCS or epinephrine). If other clinical conditions develop, additional methods may be needed, such as the use of receptor antagonists and artificial respiration. With the development of vascular insufficiency, resuscitation procedures are required.

Interactions with other drugs

Combination with nephrotoxic agents (eg, aminoglycosides), as well as diuretic drugs with potent effects (such as furosemide or ethacrynic acid), polymyxin and colistin increases the likelihood of kidney failure.

In therapy with cefotaxime, the effectiveness of oral contraception may be weakened, and therefore additional contraceptive agents are required during treatment.

The medicine is forbidden to combine with bacteriostatic antibiotics (for example, with erythromycin, tetracyclines, and in addition chloramphenicol), because it can cause antagonistic effects.

It is forbidden to mix cefotaxime and aminoglycoside solutions inside one syringe - they need to be administered separately.

Combined use with nifedipine increases the bioavailability level of cefotaxime by 70%.

Probenecid leads to the blocking of tubular excretion of cefotaxime, and also prolongs its half-life.

It is forbidden to combine cefanthral with lidocaine:

• for the introduction of IV injection;
• in infants younger than 2.5 years;
• Persons with a history of intolerance against lidocaine;
• people with cardiac blockade.

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Storage conditions

Cefanthral should be kept out of the reach of small children. Temperature values are not higher than 25 ° C.

After the preparation of the therapeutic solution for intravenous injection, the drug can be stored for another 12 hours at temperature elevations not exceeding 25 ° C, as well as a maximum of 7 days in the original pack - at temperatures ranging from 2-8 ° C (refrigerator ).

A ready-made solution for intravenous injections is allowed to store a maximum of 24 hours at a temperature level of no more than 25 ° C, and a maximum of 5 days at temperature values of 2-8 ° C.

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Shelf life

Cefanthral is allowed to be used for 3 years from the date of manufacture of the medicament.