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Pharmacological properties

teicoplanin is a systemic glycopeptide antibiotic, a product of actinoplanes teichomyceticus fermentation, which has bactericidal activity against aerobic and anaerobic gram-positive bacteria. teicoplanin inhibits the growth of sensitive microorganisms by interfering with the biosynthesis of cell membranes in places other than the sites of beta-lactam antibiotics.

Antimicrobial spectrum. The maximum concentrations that allow differentiating sensitive strains (S) from strains with moderate sensitivity and strains with moderate sensitivity from resistant strains (R) are as follows: S ≤4 mg / L and R 16 mg / L.

The prevalence of acquired resistance to this drug in some types of pathogens may vary depending on geographic region and time. In this regard, it is useful to have information on the local prevalence of resistance, especially in severe infections. These data are only general guidelines indicating the likelihood of sensitivity of a particular bacterial strain to this antibiotic.

Tests in vitro confirm that teicoplanin is active against the following sensitive gram-positive aerobes: Bacillus, Enterococci, Listeria, Rhodococcus, Staphylococcus aureus, Staphylococcus non-aureus, Streptococcus, Streptococcus pneumonia, and anaerobes: Clostridococcus peonia, anacrobacterium peonia, anthrococentium peonia and anaerobes:

Microorganisms resistant to teicoplanin include gram-positive aerobes, such as Actinomyces, Erysipelothrix, Hetherofermentative Lactobacillus, Leuconostoc, Nocardia asteroidеs, Pediococcus, as well as gram-negative aerobes, such as cocci, bacilli and other microorganisms, such as microorganisms, microorganisms, and microorganisms.

Teicoplanin does not show cross-resistance with other classes of antibiotics.

Bactericidal synergy was observed in vitro with aminoglycosides against Enterococci and Staphylococci. The combination of teicoplanin and fluoroquinolones usually has an additive, sometimes synergistic effect against Staphylococci.

Pharmacokinetics

Absorption. It is not absorbed after oral administration. The bioavailability after injection is 94%.

Distribution (plasma concentrations). The character of the concentration distribution in the blood plasma after iv administration is two-phase (initially, the fast distribution phase, then the slow distribution phase) with T½ approximately 0.3 and 3 hours, respectively. After the distribution phase, slow elimination occurs, T½ which corresponds to 70-100 hours

Single dose. 5 minutes after an intravenous injection of a dose of 3 or 6 mg / kg body weight in healthy individuals, the plasma concentration reaches 54.3 and 111.8 mg / l, respectively. The residual plasma concentration 24 hours after the injection is 2.1 and 4.2 mg / L, respectively.

Repeated doses. In the case of administration of teicoplanin by a 30-minute infusion at a dose of 400 mg every 12 hours for 5 days in healthy individuals, the average residual plasma concentration after the first injection is 5.6 ± 0.7 mg / l, and after the second - 9, 4 ± 1.5 mg / l. After further injections, the concentration in the blood plasma stably exceeds 10 mg / l after 12 hours.

In the case of administration of the drug to patients with neutropenia on the first day of treatment by iv injection at a dose of 400 mg every 12 hours, 24 hours after the second injection, the residual concentration is 10.8 ± 5.7 mg / l.

In healthy individuals, after 6 i / m injections, 200 mg every 12 hours for the first 3 injections and every 24 hours for the last 3 injections, the residual concentration 24 hours after the last injection is 6.1 mg / l.

Binding to plasma proteins. It binds to albumin 90–95%.

Tissue distribution. The apparent volume of distribution at the saturation stage is in the range of 0.6–1.2 l / kg. After injection of teicoplanin labeled with a radioactive isotope, it was found that it quickly penetrates into tissues (especially skin and bone), then reaches high concentrations in the kidneys, trachea, lungs and adrenal glands. Teicoplanin is absorbed by white blood cells and increases their antibacterial activity.

Teicoplanin does not penetrate red blood cells, cerebrospinal fluid and adipose tissue.

After iv administration of a single dose of 400 mg, the following concentrations were observed in the tissues:

  • spongy layer of bone: 10.8 and 7.1 μg / g after 0.5 and 24 hours after injection, respectively;
  • compact bone layer 6.1 and 4.9 μg / g after 0.5 and 24 hours after injection, respectively;
  • synovial fluid with inflammation: the resulting concentrations were 4 and 1.4 mg / l at 6 and 24 hours after injection, respectively;
  • pulmonary tissue: the resulting concentration was 7.9 and 4.5 μg / g 30 and 60 min after injection, respectively;
  • pleural fluid: medium Cmax - 2.8 mg / l - achieved 6 hours after administration;
  • peritoneal fluid: the concentration was 27.9 mg / l 1 h after administration.

Metabolism. No teicoplanin metabolites have been identified. More than 80% of teicoplanin administered is excreted unchanged in the urine after 16 days.

Persons with normal renal function: teicoplanin is almost completely excreted in the urine unchanged. Final t½ product - 70-100 hours

In patients with renal failure, teicoplanin is excreted more slowly than in patients with normal renal function. There is a relationship between the final T½ and creatinine clearance.

Elderly: changes in the elimination of teicoplanin reflect only age-related deterioration of renal function.

Indications

Treatment of infections caused by gram-positive bacteria, including those sensitive and resistant to methicillin, as well as infections in patients with allergies to β-lactam antibiotics.

Adults

Treatment for infections of the skin and soft tissues; infections of the upper and lower urinary tract with and without complications; respiratory tract infections; infections of the ear, throat, nose; infections of bones and joints; septicemia; endocarditis; peritonitis associated with chronic peritoneal dialysis on an outpatient basis.

Prevention of infectious endocarditis with allergies to β-lactam antibiotics in dentistry or during manipulations / surgical interventions in the upper respiratory tract that are performed under general anesthesia; during surgical interventions on the genitourinary tract and gastrointestinal tract.

Children (except newborns)

Treatment for infections of the skin and soft tissues; infections of the upper and lower urinary tract with and without complications; respiratory tract infections; infections of the ear, throat, nose; infections of bones and joints; septicemia.

Application

When using antibacterial agents, it is necessary to strictly follow the established recommendations.

Prevention

Adults Prevention of infectious endocarditis: 400 mg iv during introductory anesthesia. Teicoplanin should be combined with aminoglycoside in patients with prosthetic heart valves.

Treatment

The duration of therapy depends on the type, severity and individual characteristics of the patients body.

Adults and elderly patients with normal renal function

Infections of the respiratory tract, infections of the skin and soft tissues, urinary tract, ear, throat, nose and other moderate infections:

  • loading dose: standard dose - 400 mg / day (usually 6 mg / kg / day) as a single intravenous injection (on the 1st day);
  • maintenance therapy: a standard dose of 200 mg / day (usually 3 mg / kg / day) as a single intravenous or intramuscular injection per day.

Septicemia, infections of bones and joints, endocarditis, severe lung diseases and other severe infections:

  • loading dose: standard dose - 400 mg (usually 6 mg / kg) iv every 12 hours, from the 1st to the 4th day;
  • maintenance therapy: a standard dose is 400 mg / day (usually 6 mg / kg / day) as a single intravenous or intramuscular injection per day.

Achieving the optimal dose helps determine the concentration of the antibiotic in the blood plasma. In the case of a moderate or more severe infection with the administration of loading doses, it is necessary to monitor the residual plasma concentrations to ensure that stable residual plasma concentrations of at least 10 mg / L are achieved (HPLC determination) or 15 mg / L ( determination by immunoenzymatic fluorescence polarization method (FPIA), as well as during maintenance therapy, to ensure that these concentrations are stable.

In maintenance therapy for septicemia and endocarditis, the transition to the IM route of administration depends on the clinical course of the disease.

In some particularly difficult clinical situations, when the minimum inhibitory concentrations of teicoplanin are high (4–8 mg / l), given the bacterial load, or when the pharmacokinetics of the drug in the blood plasma are difficult to predict (significant burns, intensive care, etc.), or provided low tissue distribution (bones, heart valves), the recommended loading dose is 3-5 injections of 12 mg / kg every 12 hours. If necessary, maintenance doses of ≥12 mg / kg can be prescribed.

Achieving the optimal dose helps determine the concentration of the antibiotic in the blood plasma.

When loading doses are received, it is necessary to monitor the residual plasma concentrations in order to make sure that stable residual plasma concentrations are achieved within 20–30 mg / L (HPLC) or 30–40 mg / L (FPIA), as well as during maintenance therapy to ensure that these concentrations are stable.

Children (except newborns) with normal renal function. The dose and duration of treatment depend on the type of severity of the infection:

  • loading dose: for the first three injections - 10-12 mg / kg every 12 hours;
  • maintenance therapy - 10 mg / kg / day.

With an infection of moderate severity (without neutropenia):

  • loading dose: for the first three injections - 10 mg / kg every 12 hours;
  • maintenance therapy - 6 mg / kg / day.

Achieving the optimal dose helps determine the concentration of the antibiotic in the blood plasma.

In the case of a moderate or more severe infection, when receiving the drug in loading doses, it is necessary to monitor the residual plasma concentrations to ensure that stable residual plasma concentrations of at least 10 mg / L (HPLC) or 15 mg / L (FPIA) are achieved, and also during maintenance therapy to ensure that these concentrations are stable.

In some particularly difficult clinical situations, when the minimum inhibitory concentrations of teicoplanin are high (4–8 mg / l), given the bacterial load, or when the pharmacokinetics of the drug in the blood plasma are difficult to predict (significant burns, intensive care, etc.), or provided low tissue distribution (bones, heart valves), when receiving the drug in loading doses, it is necessary to monitor the residual concentration in the blood plasma to make sure that stable residual concentrations in blood plasma between 20 and 30 mg / l (HPLC) or 30–40 mg / l (FPIA), and during maintenance therapy to ensure that these concentrations are stable.

Adults and elderly patients with renal failure (impaired renal function). During the first 3 days, compliance with the standard treatment regimen is recommended:

  • if creatinine clearance is 40-60 ml / min, the standard dose should be divided in half (enter the initial dose every 2 days or half the dose daily);
  • if creatinine clearance is 40 ml / min, as well as for patients on hemodialysis, the dose should be reduced to 1/3 (administer the same dose once every 3 days or daily 1/3 doses). Teicoplanin is not excreted during hemodialysis.

For patients with impaired renal function and secondary peritonitis resulting from continuous ambulatory peritoneal dialysis, a dosage regimen of 20 mg of teicoplanin per 1 liter of dialysis fluid and a loading dose of 200 mg iv are recommended (for patients with elevated body temperature).

Achieving the optimal dose helps determine the concentration of the antibiotic in the blood plasma. In the case of a moderate or more severe infection, when receiving the drug in loading doses, it is necessary to monitor the residual plasma concentrations in order to ensure that stable residual plasma concentrations of at least 10 mg / L (HPLC) or 15 mg / L (FPIA) are achieved, and also during maintenance therapy to ensure that these concentrations are stable.

At some particularly severe clinical concentrations, when the minimum inhibitory concentrations of teicoplanin are high (4–8 mg / l), given the bacterial load, or when the pharmacokinetics of the drug in the blood plasma are difficult to predict (significant burns, intensive care, etc.), or in conditions low tissue distribution (bones, heart valves), when receiving the drug in loading doses, it is necessary to monitor residual plasma concentrations to ensure stable residual concentrations are achieved in blood plasma between 20 and 30 mg / l (HPLC) or 30–40 mg / l (FPIA), and during maintenance treatment to ensure that these concentrations are stable.

Mode of application. Enter in / in or / m. The introduction is carried out for 1 min or by infusion for 30 minutes

Directions for preparation of solution: type in the syringe the entire contents of the ampoule with the solvent and slowly enter into the vial with the active substance. Gently shake the bottle between the palms until the powder is completely dissolved. Avoid the formation of bubbles. If foam occurs, leave the bottle upright until it disappears completely. Thus prepared isotonic (pH 7.5) solution can be stored for no more than 48 hours at room temperature and 7 days at 4 ° C.

Ready solution can be injected or diluted:

  • 0.9% r-rum sodium chloride, r-r based on sodium lactate (Ringer-lactate, Hartmann). After dilution in such solutions, the drug can be stored for no more than 24 hours at a temperature not exceeding 25 ° C or 7 days at 4 ° C;
  • 5% glucose solution (a prepared solution prepared in this way can be stored for 24 hours at a temperature not exceeding 25 ° C);
  • 0.18% solution of sodium chloride and 4% glucose (a solution prepared in this way can be stored for 24 hours at a temperature not exceeding 25 ° C);
  • solution for peritoneal dialysis containing 1.36% or 3.86% glucose (a solution prepared in this way can be stored for 28 days at 4 ° C).

Teicoplanin maintains its stability for 48 hours at a temperature of 37 ° C in the composition of the solutions for peritoneal dialysis, which contain insulin or heparin.

Contraindications

Hypersensitivity to teicoplanin. newborns. the use of this drug during lactation is not recommended (see use during pregnancy and lactation).

Side effects

On the part of the immune system: rash, urticaria, erythema, pruritus, fever, colds, anaphylactic reactions (angioedema, bronchospasm, anaphylactic shock), exfoliative dermatitis;

on the part of the skin and subcutaneous tissue: very rarely - severe bullous skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis, in exceptional cases, erythema multiforme);

on the part of the hepatobiliary system: a temporary increase in the level of transaminases and / or alkaline phosphatase;

on the part of the blood system and lymphatic system: eosinophilia, leukopenia, thrombocytopenia, neutropenia (rarely severe) or agranulocytosis (reversible after discontinuation of treatment), which especially develops when the drug is used in high doses and in the 1st month of therapy;

from the digestive tract: nausea, vomiting, diarrhea;

on the part of the kidneys and urinary tract: a temporary increase in creatinine; very rarely - renal failure, usually occurs in patients with severe infection, the presence of the underlying disease and / or in patients receiving other drugs that are able to exhibit nephrotoxic effects;

from the nervous system: dizziness, headache, cases of seizures have been reported;

on the part of the hearing organ: hearing loss, tinnitus, disorders of the vestibular apparatus;

local reactions: pain, phlebitis, erythema, abscess;

others: superinfection (increase in the number of insensitive microorganisms).

Also, rarely reported cases of erythema and hot flashes in the upper body after the use of the solution, which appeared without information about the previous use of teicoplanin and did not recur at the next application with a decrease in the rate of administration or a decrease in concentration. These cases were not specific to concentration or rate of administration.

special instructions

It is necessary to correct the dose for patients with renal failure (see application). a regular detailed blood test should be performed during prolonged treatment and / or use in high doses (especially in the 1st month of therapy) simultaneously with regular monitoring of liver and kidney function.

When using teicoplanin, cases of ototoxicity, toxic effects on the hematopoietic system and cases of hepatotoxicity and nephrotoxicity have been reported.

It is necessary to conduct repeated studies of kidney function and hearing, especially in such situations:

  • with prolonged treatment of patients with renal failure;
  • with the simultaneous and further use of drugs that can have a neurotoxic and / or nephrotoxic effect (aminoglycosides, colistin, amphotericin, cyclosporine, cisplatin, furosemide and ethacrylic acid).

This medicine should be used with caution in patients with hypersensitivity to vancomycin, since cross-sensitivity is possible. However, the presence of a history of "red man syndrome" associated with the use of vancomycin is not a contraindication to the use of teicoplanin.

This medicine contains sodium. The sodium content is less than 1 mmol per dose, that is, in practice, it is believed that this drug is “sodium free”.

Use during pregnancy and lactation

Pregnancy. In studies of teicoplanin in animals, teratogenic effects were not revealed, and clinical data are insufficient. However, due to the high therapeutic effect of the drug Gliteik, its use is possible if during pregnancy there is a need for its reception for health reasons (regardless of gestational age). In this case, the auditory function of the newborn (otoacoustic emission) should be checked, taking into account the possibility of the ototoxic effect of teicoplanin.

Lactation. There is no data on the penetration of teicoplanin into breast milk, so breastfeeding during treatment with Gliteik is not recommended.

Children. The drug is contraindicated in newborns.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. It is recommended to refrain from driving vehicles or working with machinery in connection with the possible risk of fainting.

Interactions

Special warnings related to the mismatch of the international normalized ratio (many): numerous cases of increased anticoagulant activity have been reported in patients receiving oral antibiotic therapy. in conditions of infection or severe inflammatory process, the age and general condition of the patient are favorable risk factors. under such conditions, it is difficult to determine to what extent the infection itself or its treatment play a role in the imbalance.

Despite this, some classes of antibiotics are more involved in this effect, in particular fluoroquinolones, macrolides, cyclins, co-trimoxazole and some cephalosporins.

Due to the increased potential risk of adverse reactions, teicoplanin should be used with caution in patients who simultaneously use nephrotoxic or ototoxic drugs, such as aminoglycosides, amphotericin B, cyclosporine and furosemide.

Overdose

Gliteik is not removed from the circulating blood by hemodialysis. if symptoms of an overdose occur, symptomatic therapy is prescribed.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° c.

Tags: Gliteake