Zepheter

Zephtera is a systemic drug with antimicrobial properties.

Indications of the zepheter

It is shown in the following cases: elimination of complicated skin infections (among them diabetic foot syndrome (infected), against which there is no osteomyelitis), which were provoked by gram-positive or gram-negative microbes.

Release form

It is available as a lyophilizate of infusion solutions. The volume of one glass vial with a medicine is 20 ml. One package can contain 1 or 10 such bottles.

Pharmacodynamics

Medocaryl ceftobiprole is a water-soluble prodrug that exerts bactericidal activity on a relatively large number of gram-positive microbes, among which are resistant to methicillin, staphylococci, penicillin-resistant pneumococci, and in addition entericococci-sensitive fecal ones. In addition, there is activity against a variety of gram-negative microorganisms, among which are strains of enterobacteria and Pseudomonas aeruginosa.

The active component is firmly synthesized with a number of important gram-negative and gram-positive microbes as well as PBP. Ceftobiprol is synthesized with PBP2a by staphylococci (among them are methicillin-resistant Staphylococcus aureus), which is why it actively acts against methicillin-resistant staphylococci.

There is evidence that ceftobiprole has activity against a variety of isolates of the following microbes, both in hospital infections and in vitro.

Aerobic bacteria (Gram-positive): Enterococcus fecal (exclusively isolates with sensitivity / resistance to vancomycin), Staphylococcus aureus (exclusively isolates with resistance / sensitivity to methicillin), Staphylococcus epidermis, Streptococcus agalactia, and in addition streptococcus pyogenic. Also coagulase-negative staphylococci (isolates that are resistant / sensitive to methicillin, amongst which are staphylococcus hemolytic, Staphylococcus hominis, staphylococcus saprophytic, and Staphylococcus lugdunensis), pneumococci (isolates that are resistant / moderately resistant / sensitive to penicillin) and streptococci from the viridans category.

Aerobic microorganisms (Gram-negative): Enterobacter cloaca, E. Coli, Klebsiella pneumonia, Proteus mirabilis and Pseudomonas aeruginosa. In addition, bacteria of the genus tsitrobacter (among them also Citrobacter frowni and Citrobacter koseri), as well as Enterobacter aerogenes, klebsiella oxytoca, moraxella cataralis and morgana bacterium. Along with this, microbes are from the genus Neisseria, Providence and Sercesia Marces.

Pharmacokinetics

Pharmacokinetic parameters in adults with the introduction of a single 1-hour infusion (size 500 mg) or reusable dosages (the same 500 mg) that were administered by 2-hour infusions every 8 hours are similar in both cases. On average, they are: plasma indices - 34.2 μg / ml (single) and 33.0 μg / ml (multiple); the AUC value was 116 μg.h / ml and 102 μg.h / ml; the half-life is 2.85 hours and 3.3 hours; the clearance level is 4.46 and 4.98 l / h.

The AUC and peak concentrations of ceftobiprole are increased according to the increase in dosage (the range is 125 mg / 1 g). The medicine reaches its equilibrium state on the first day of the course. In patients with healthy renal function, administration of the drug every 8 or 12 hours does not cause the accumulation of an active component in the body.

Synthesis with plasma protein is 16%, and the degree of this index is independent of the level of concentration of the substance. The stationary distribution volume is 18 liters and is approximately equal to the volume of human extracellular fluid.

Biotransformation from ceftobiprole medocaryl to the active element ceftobiprol is carried out quickly, after which it is catalyzed by plasma esterases. The indices of the prodrug are very small, it is found in urine and plasma only during the infusion. The active component is poorly metabolized, becoming a non-cyclic decay product, inactive microbiologically. Its index is very low - about 4% of the concentration of ceftobiprole.

Ceftobiprol is mainly excreted unchanged, through the kidneys, and the half-life of the substance is approximately 3 hours. The main mechanism of elimination is glomerular filtration, and a small part of the dosage passes through the tubular reabsorption.

Preclinical testing of probenicide showed that it does not affect the pharmacokinetic properties of ceftobiprole, which suggests that the latter lacks active tubular secretion. With a single administration of the drug, about 89% of the substance is observed in the urine under the guise of ceftobiprol in the active form (83%), and under the guise of an open ring decomposition product (about 5%) and a ceftobiprole medocaryl element (less than 1%).

Dosing and administration

The freeze-dried injection powder is dissolved in 10 ml of water and then in a 5% solution of glucose. After the powder is diluted, the vial must be shaken. To completely dissolve it is necessary to wait about 10 minutes. Before starting dilution in a solution of infusion, you should wait until the foam formed in the tank settles.

To eliminate the infectious processes provoked by gram-positive microbes, it is required to administer 500 mg of medication every 12 hours (in the form of infusions lasting 1 hour). In people with diabetic foot syndrome (an infected type), the administration regimen after every 12 hours has not been studied.

As a rule, the treatment course lasts approximately 1-2 weeks, depending on the place of development of the infectious process, the course of the pathology and the clinical response of the patient.

[2], [3]

Use of the zepheter during pregnancy

With the help of preclinical testing it was possible to find out that ceftobiprol does not have teratogenic activity and does not affect fetal weight, ossification, and intrauterine development. But at the same time testing for use of the drug by pregnant women was not carried out.

The test results, by means of which the effect of the drug on the reproductive system of animals was checked, can not be interpolated to the human system. In this regard, Zefter is allowed to appoint pregnant only in situations where the possible benefit to the mother's health exceeds the risk of developing fetal negative effects.

Contraindications

Among the contraindications of drugs:

• intolerance of the active substance or any of the auxiliary elements that make up the drug, as well as other cephalosporins;
• presence in the patient's history of an allergy to β-lactams;
• children under 18 years of age.

Cautiously appoint at:

• renal insufficiency (the coefficient of cleansing of creatinine is below 50 ml / min);
• epileptic seizures;
• seizures (available in history);
• pseudomembranous form of colitis (available in history).

Side effects of the zepheter

Clinical testing has shown that most often the use of the drug causes such side effects

The freeze-dried injection powder is dissolved in 10 ml of water and then in a 5% solution of glucose. After the powder is diluted, the vial must be shaken. To completely dissolve it is necessary to wait about 10 minutes. Before starting dilution in a solution of infusion, you should wait until the foam formed in the tank settles.

To eliminate the infectious processes provoked by gram-positive microbes, it is required to administer 500 mg of medication every 12 hours (in the form of infusions lasting 1 hour). In people with diabetic foot syndrome (an infected type), the administration regimen after every 12 hours has not been studied.

As a rule, the treatment course lasts approximately 1-2 weeks, depending on the place of development of the infectious process, the course of the pathology and the clinical response of the patient.

Such as nausea (approximately 12%), manifestations at the site of drug administration (8%), and in addition vomiting, headaches and diarrhea (about 7%), and dysgeusia (approximately 6%). Usually, nausea is quite small, it quickly disappears, without the need to abolish drugs. This side effect was less common in people who had 2-hour infusions (about 10%). People who were given 1-hour procedures, this indicator is higher - 14%. Other negative reactions:

• organs of the National Assembly: dizziness often develops;
• subcutaneous tissue and skin: mainly there are eruptions (papular, macular, as well as maculopapular and generalized forms), and besides it is itching;
• organs of the digestive tract: often there are diarrheal phenomena, there are only occasional colitis, triggered by clostridium caused by the difficile;
• metabolic phenomena: often manifested hyponatremia;
• invasions and infectious processes: fungi usually develop (in the area of the vagina and vulva, and also on the skin and mouth);
• the immune system: usually hypersensitivity reactions (among such hives and intolerance of drugs); occasionally anaphylaxis may develop;
• hepatobiliary system: an increase in the parameters of liver enzymes (including an increase in the parameters of AST and ALT).

[1]

Storage conditions

The drug should be kept in a temperature of 2-8 ° C, in a place that is closed from sunlight. Packaging must be original. The storage location should also not be accessible to young children.

[4], [5], [6]

Shelf life

Zephter is suitable for use within 2 years from the date of release of the medicinal product. The finished solution can be stored for 1 hour under conditions of a temperature of 25 ° C, and also for 24 hours at a temperature of 2-8 ° C.

[7]