Medicine Teicoplanin, instructions for use

Release form, packaging and composition of the drug Clinical-pharmacological group Pharmaco-therapeutic group Pharmacological action Indications for use Method of administration and doses Side effects Contraindications for use Use in children Special instructions Drug interactions

Registration Certificate Holder:

JODAS EXPOIM, LLC (Russia)

ATX Code:

J01XA02

Active substance:

Dosage form:

Teicoplanin

Release form, packaging and composition of the drug Teicoplanin

Lyophilisate for preparing a solution for intravenous and intramuscular administration

and taken orally in the form of a white to light yellow powder.

1 fl.
teicoplanin	200 mg

Excipients

: sodium chloride - 24 mg.

Composition of the supplied solvent: water for injection - 5 ml.

200 mg – bottles (1) + 1 amp. with solvent - cardboard packs. 200 mg – bottles (5) + 5 amps. with solvent - cardboard packs. 200 mg - bottles (10) + 10 amps. with solvent - cardboard packs.

Lyophilisate for preparing a solution for intravenous and intramuscular administration

and taken orally in the form of a white to light yellow powder.

1 fl.
teicoplanin	400 mg

Excipients

: sodium chloride - 24 mg.

Composition of the supplied solvent: water for injection - 5 ml.

400 mg – bottles (1) + 1 amp. with solvent - cardboard packs. 400 mg – bottles (5) + 5 amps. with solvent - cardboard packs. 400 mg – bottles (10) + 10 amps. with solvent - cardboard packs.

Pharmacological properties of the drug Teicoplanin

Glycopeptide antibiotic with bactericidal action. Forms a complex with acyl-D-alanyl-D-alanine of the bacterial membrane mucopeptide, blocks its formation, suppresses the formation of spheroplasts. It is well absorbed after intramuscular administration, bioavailability is about 90%, and in the blood it is 90–95% bound to plasma proteins. Penetrates very slowly into tissues and organs. The half-life is 150 hours. It is excreted mainly by the kidneys (up to 80%). Active against aureus and coagulase-negative staphylococci (including those resistant to methicillin and other β-lactam antibiotics), streptococci, enterococci (including Enterococcus faecium ), Listeria monocytogenes , micrococci, corynebacteria of the JK , gram-positive anaerobic bacteria, including Clostridium difficile , and peptococci. Antibiotic resistance develops slowly, and there is no cross-resistance with antibiotics from other groups.

pharmachologic effect

Antibiotic of glycopeptide structure. In vitro exhibits bactericidal activity against anaerobic and aerobic gram-positive microorganisms. Teicoplanin inhibits the growth of microorganisms sensitive to it by inhibiting the biosynthesis of the microbial cell wall at sites other than those in the microbial cell wall that are affected by beta-lactam antibiotics.

Active regarding

Staphylococcus spp. (including strains resistant to methicillin and other beta-lactam antibiotics), Streptococcus spp., Enterococcus spp., Listeria monocytogenes. Micrococcus spp, Corenebacterum spp. J/K group and gram-positive anaerobes, including Clostridium difficile, Peptococcus spp.

In vitro, synergism in bactericidal activity against Staphylococcus aureus has been demonstrated when teicoplanin is combined with aminoglycosides or imipinem. In vitro, the combination of teicoplanin with rifampicin showed an additive effect and synergism against Staphylococcus aureus. Synergy between teicoplanin and ciprofloxacin was observed against Staphylococcus epidermidis.

As a rule, cross-resistance with antibiotics of other groups is not typical, but Enterococcus spp. exhibits slight cross-resistance to teicoplanin and another glycopeptide, vancomycin.

Targocid (Teicoplanin) fl. 400 mg No. 1 – Instructions

Dosage form

Lyophilized powder for injection, 1 bottle per package.

Compound

1 bottle of lyophilized powder for injection contains teicoplanin 400 mg.

In a combined package with solvent - water for injection in an ampoule - 1 set.

Pharmacological properties

The main active ingredient Teicoplanin is a fermentation product of Actinoplans teicomyceticus, which has bactericidal activity against microorganisms - aerobes and anaerobes.

Capable of inhibiting the growth of microorganisms sensitive to it due to the ability to interfere with the synthesis of cell membranes in places that differ from those affected by beta-lactam antibiotics.

Active against Staphylococcus aureus and coagulase-negative staphylococci (including those resistant to methicillin and other beta-lactam antibiotics), streptococci, enterococci, Listeria monocytogenes, micrococci, corynebacteria of the JK group and gram-positive anaerobic bacteria, including Clostridium difficile and peptococci. Does not show cross-resistance with other classes of antibiotics.

During testing, there was no case of teicoplanin showing cross-resistance to antibiotics of other classes.

Blocks the synthesis of the cell wall of a microorganism in areas other than the action of beta-lactam antibiotics, inhibits the growth and reproduction of bacteria.

Pharmacokinetics

Bioavailability after a single intramuscular injection of 3–6 mg/kg body weight is 90%. After intravenous administration of the same dose, T1/2 is 150 hours, which allows maintaining therapeutic concentrations with a single administration. In plasma, 90–95% is bound to proteins. About 80% is excreted in the urine.

Indications for use

Targotsid is intended for the treatment of systemic infections caused by microflora sensitive to teicoplanin, including those that have already shown an allergy to beta-lactam antibiotics.

In particular, for the treatment of infections or as prophylaxis during surgical procedures at risk of infection:

skin and soft tissues;
upper and lower urinary tract, including with complications;
respiratory tract;
ENT organs;
bones and joints;
genitourinary organs or gastrointestinal tract.

Also used for the treatment of septicemia, endocarditis, peritonitis associated with regular peritoneal dialysis on an outpatient basis.

Directions for use and dosage

The exact duration of the therapeutic course is determined by the attending physician, depending on the type and strength of the infection.

Recommended dosage regimen for teicoplanin, if used for prophylaxis or treatment of a patient: 400 mg.

The dose can also be calculated based on the type and severity of the infection, from 6 to 12 mg per 1 kg of body weight, but not more than 400 mg per 1 administration.

The introduction is made:

intravenous stream, bolus (for at least 3-5 minutes);
intravenous drip, for at least 30 minutes;
intramuscularly (if the condition improves, according to the decision of the attending physician).

The drug is usually administered once a day, except for the treatment of septicemia, when the specified dosage is administered every 12 hours. In this case, intramuscular administration is also acceptable.

It is not recommended to exceed the recommended dosage.

Maintenance dosage – 200 mg, intramuscular administration is acceptable (except for the treatment of septicemia, when the maintenance dosage remains 400 mg per 1 administration).

When replacing heart valves, the drug is combined with aminoglycosides.

Pediatric dosages for severe infections:

initial - 10-12 mg per 1 kg of patient weight, administered every 12 hours;
maintenance – 10 mg per 1 kg of body weight every 24 hours.

Pediatric dosage for moderate degrees of infection:

initial - 10 mg per 1 kg of patient weight, administered every 12 hours;
maintenance – 6 mg per 1 kg of body weight every 24 hours.

In case of renal failure, the dose is reduced.

Contraindications

Targocid is not used if the patient has ever previously had hypersensitivity (allergy) to one of the components included in its composition.

Caution should be exercised during simultaneous treatment with nephrotoxic or ototoxic drugs - aminoglycosides, cyclosporines, furosemide.

Also contraindicated for use in the treatment of newborn infants.

Use during pregnancy and breastfeeding

Targotsid is contraindicated for use in pregnant women.

Lactation is suspended during treatment with this drug.

Overdose

Overdoses of this drug are extremely rare. Possible increased side effects.

In case of accidental overdose, symptomatic treatment should be used.

Hemodialysis and dialysis are not effective.

Side effects

The use of this drug in a patient may cause side effects such as:

rash, allergic urticaria, itching, angioedema, bronchospasm;
toxic epidermal necrolysis, erythema multiforme;
eosinophilia, leukopenia, thrombocytopenia, neutropenia, agranulocytosis;
nausea, vomiting, diarrhea;
increased creatinine levels (transient), renal failure (extremely rare);
dizziness, convulsions;
hearing impairment;
pain, phlebitis, erythema, abscesses at the injection site;
asthenia, tachycardia.

Storage conditions

The finished solution retains its properties for 24 hours.

Storage temperature should not exceed 30°C.

Best before date

3 years.

Vacation category

On prescription.

Indications for use

Severe infections caused by sensitive gram-positive microorganisms, incl. in patients with allergies to penicillins and cephalosporins: endocarditis; septicemia; bone and joint infections; lower respiratory tract infections; skin and soft tissue infections; urinary tract infections; peritonitis occurring during continuous ambulatory peritoneal dialysis (CAPD).

Prevention of infectious complications during dental and orthopedic operations when there is a risk of developing infections caused by gram-positive microorganisms.

For oral solution: pseudomembranous colitis caused by Clostridium difficile (associated with the use of antibacterial drugs).

Instructions for use TEICOPLANIN-TF

Teicoplanin-TF should be administered intramuscularly or intravenously (as a bolus injection over 5 minutes or as an infusion over 15-30 minutes).

The dose and route of administration of the drug are determined depending on the sensitivity of the pathogen, the severity of the infection, as well as the state of the patient’s renal function.

Adults and elderly patients with normal renal function

In the treatment of infections of the upper and lower respiratory tract, skin and soft tissues, urinary tract, ENT organs and other moderate infections

The loading dose is 400 mg IV or IM every 12 hours for the first 1-3 injections, then 200 mg IV or IM 1 time/day.

In the treatment of septicemia, bone and joint infections, endocarditis, complicated respiratory tract infections and other severe infections

the loading dose is 800 mg IV every 12 hours for the first 3-5 injections; The maintenance dose is up to 12 mg/kg IV or IM 1 time/day. During maintenance therapy in the treatment of septicemia and endocarditis, the transition to the intramuscular route of administration depends on the clinical course of the disease.

For the prevention of infectious complications during orthopedic or maxillofacial operations

During anesthesia, 400 mg of the drug is administered intravenously.

In particularly severe clinical situations, when the MIC of teicoplanin is high (4-8 mg/l), taking into account bacterial loads, or when the pharmacokinetics of the drug in the blood serum is difficult to predict (major burns, intensive care, etc.), or in conditions of low tissue distribution (bones, heart valve), the recommended loading dose is 3-5 injections of 12 mg/kg every 12 hours. If necessary, maintenance doses of up to 12 mg/kg and higher can be prescribed.

To select the optimal dose, it is necessary to determine the concentration of the antibiotic in the blood plasma. When using the drug in a loading dose, it is necessary to monitor residual plasma concentrations to ensure that the values are within the range of 20-30 mg/l (HPLC) or 30-40 mg/l (ELISA). During maintenance therapy, residual plasma concentrations should also be monitored to ensure that values remain stable.

For pseudomembranous colitis

Teicoplanin-TF is prescribed 100-200 mg 2 times a day for 7-14 days. The recommended dose of Teicoplanin-TF after dissolution is taken orally.

Children

Initial dose for children aged 2 months to 12 years

is 10 mg/kg IV every 12 hours 3 times, then 6-10 mg/kg IV 1 time/day;
for children under 2 months of age
- 16 mg/kg (as a 30-minute IV infusion) on the first day, the maintenance dose is 8 mg/kg IV 1 time/day.

In case of moderate or more severe infection, when using the drug in a loading dose, it is necessary to monitor residual plasma concentrations to ensure that the indicators are at least 10 mg/l (HPLC) or 15 mg/l (ELISA). During maintenance therapy, residual plasma concentrations should also be monitored to ensure that values remain stable.

In patients with
impaired renal function,
dose adjustment begins on the 4th day to maintain the serum concentration of Teicoplanin-TF at 10 mg/l.
When CC is 30-80 ml/min,
the maintenance dose is either reduced by half or administered once every 2 days.
Patients with CC less than 30 ml/min or patients on hemodialysis
are administered 1/3 of the dose daily or 1 time every 3 days. Teicoplanin-TF is not eliminated by hemodialysis.

For patients with renal impairment and secondary peritonitis resulting from continuous peritoneal dialysis

, the recommended dosage regimen is 20 mg per 1 liter of dialysis fluid; the loading dose for such patients is 200 mg.

In particularly severe clinical cases, when the MIC of teicoplanin is high (4-8 mg/l), taking into account bacterial loads, or when the pharmacokinetics of the drug in the blood serum is difficult to predict (major burns, intensive care, etc.), or in conditions of low tissue distribution (bones, heart valve) when using the drug in a loading dose, it is necessary to monitor residual plasma concentrations to ensure that the values are within the range of 20-30 mg/l (HPLC) or 30-40 mg/l (ELISA). During maintenance therapy, residual plasma concentrations should also be monitored to ensure that values remain stable.

Rules for preparing the solution

200 mg or 400 mg of Teicoplanin-TF is dissolved in 3 ml of one of the following solvents:

0.9% sodium chloride solution, lactated Ringer's solution, 5% glucose solution, 0.18% sodium chloride solution and 4% glucose solution, peritoneal dialysis solution containing 1.36% or 3.86% glucose. The solvent should be introduced into the vial slowly, gently shaking the vial until the powder is completely dissolved, avoiding the appearance of foam. If foam appears, the bottle with the solution must be left in an upright position for at least 15 minutes to reduce its amount. The resulting solution can be used for intramuscular administration.

To use the drug in the form of infusions, the resulting solution is diluted to 100 ml.

For oral administration, 200 mg or 400 mg of Teicoplanin-TF is dissolved in 10 ml of water.

To avoid administering a dose less than required, make sure that the drug is completely dissolved. The prepared solution should be carefully removed from the bottle.

Directions for use and doses

The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed.

Administered intravenously (in the form of injection or infusion) or intramuscularly.

It is administered to newborns only as an intravenous infusion.

The dose and regimen depend on the patient’s age, indications, and clinical situation.

Teicoplanin

Teicoplanin is administered parenterally (intravenously or intramuscularly).

Intravenous (IV) administration can be done by either IV injection over 3-5 minutes, or IV infusion over 30 minutes. In newborns, the drug should be administered only as an intravenous infusion.

Dosage regimen for adults and adolescents 16-18 years of age with normal renal function

Treatment of infections caused by drug-sensitive gram-positive bacteria (endocarditis; septicemia; bone and joint infections; lower respiratory tract infections; skin and soft tissue infections; urinary tract infections)

For moderately severe skin and soft tissue infections, urinary tract infections, and lower respiratory tract infections, the initial dose of teicoplanin is 400 mg once daily IV on the first day, followed by a maintenance dose of 200 mg once daily IV or intramuscularly (IM).

For the treatment of severe bone and joint infections, septicemia, endocarditis, the initial dose is 400 mg IV every 12 hours for the first three doses, followed by a maintenance dose of 400 mg IV or IM once daily. For severe infections, the minimum serum concentration should not be lower than 10 mg/l. Maximum concentrations determined 1 hour after intravenous administration of 400 mg are usually in the range from 20 to 50 mg/l.

In some cases (in burn patients or in patients with endocarditis), the maintenance dose can be up to 12 mg/kg body weight per day. Standard doses of 200 mg and 400 mg correspond to doses of 3 mg/kg and 6 mg/kg body weight.

In patients weighing more than 85 kg, it is recommended to adjust the dose of the drug based on body weight, adhering to the same therapeutic regimen: moderately severe infections 3 mg/kg, severe infections 6 mg/kg.

Patients with peritonitis that developed as a complication of continuous ambulatory peritoneal dialysis

After a single loading dose of 400 mg intravenously, in the first week, 20 mg/L is injected into each reservoir with a peritoneal dialysis solution, in the second week, 20 mg/L is injected into every second reservoir with a peritoneal dialysis solution, in the third week, 20 mg/L into the peritoneal dialysis solution reservoir for overnight dialysis.

Antimicrobial prophylaxis during orthopedic surgery, during dental operations (for example, prevention of endocarditis in patients with artificial heart valves): 400 mg teicoplanin (or 6 mg/kg if the patient weighs more than 85 kg) as a single intravenous injection during induction anesthesia

Pseudomembranous colitis caused by C. difficile:

200 mg teicoplanin orally twice daily.

Dosage regimen in children

Children over 2 months up to 16 years:

For most Gram-positive infections, the recommended initial dose is 10 mg/kg body weight IV at 12-hour intervals for the first three doses, followed by a maintenance dose of 6 mg/kg body weight administered IM or IV once daily.

For severe infections and neutropenia, the recommended initial dose is 10 mg/kg body weight IV at 12-hour intervals for the first three doses, followed by a maintenance dose of 10 mg/kg body weight administered IV once daily.

Children under 2 months, including newborns:

The recommended initial dose is 16 mg/kg body weight IV on the first day, followed by a maintenance dose of 8 mg/kg body weight IV once daily. IV administration should be carried out by IV infusion over 30 minutes.

Dosage regimen in elderly patients

With normal renal function, no dosage adjustment is required.

Dosage regimen in adults with renal failure

Until the 4th day of treatment with teicoplanin, no dosage adjustment is required. From the fourth day onwards, the administered dose should maintain the serum teicoplanin concentration at 10 mg/l.

For moderate renal failure (creatinine clearance 40-60 ml/min): the maintenance dose should be halved, either by administering the previous dose once every two days, or by administering half the dose once a day.

In severe renal failure (creatinine clearance less than 40 ml/min) and in patients on hemodialysis: the maintenance dose should be reduced by three times, either by administering the previous dose every third day, or by administering 1/3 of the previous dose once a day .

Teicoplanin is not excreted during hemodialysis.

Duration of treatment

The therapeutic response in most patients with infections caused by pathogens sensitive to the antibiotic is observed within 48-72 hours after the start of drug administration.

The total duration of treatment is determined individually and depends on the type and severity of the infection and the clinical response of the individual patient.

For endocarditis and osteomyelitis, treatment for 3 weeks or more is recommended; in this case, Teicoplanin should not be administered for more than 4 months.

Preparation of the solution

3.2 ml of sterile water should be slowly introduced into the Teicoplanin vial, gently shaking the vial until the powder is completely dissolved, while avoiding the formation of foam. It is very important that the entire drug is dissolved, even the part that is located near the stopper.

When shaking the solution, foam forms, which makes it difficult to extract the required volume of solution. However, if teicoplanin is completely dissolved, the foam does not change the concentration of the remaining solution of 200 mg in 3.2 ml in a vial of Teicoplanin 200 mg and 400 mg in 3.2 ml in a vial of Teicoplanin 400 mg. If the solution turns out to be foamy, then you should leave it to stand for about 15 minutes to reduce the amount of foam.

You should slowly remove the teicoplanin solution from the bottle, trying to remove it completely by piercing the middle of the rubber stopper with a needle.

The reproduced solution will contain 200 mg of teicoplanin in 3.2 ml in a vial of Teicoplanin 200 mg and 400 mg in 3.2 ml in a vial of Teicoplanin 400 mg. It is important that the solution is prepared correctly and that the solution is carefully removed from the bottle; Improper preparation of the solution may lead to the administration of a smaller dose than required.

The prepared solution is isotonic and has a pH of 6.5-7.5.

The prepared solution can be administered directly by injection or further diluted with 0.9% sodium chloride solution, Ringer's solution, Hartmann's solution, 5% glucose solution, peritoneal dialysis solution containing 1.36% or 3.86% glucose.

Side effect

From the digestive system:

nausea, vomiting, diarrhea.

From the hematopoietic system:

agranulocytosis, leukopenia, neutropenia, thrombocytopenia, eosinophilia.

From the liver and biliary tract:

increased activity of liver transaminases and/or alkaline phosphatase in the blood serum.

From the urinary system:

increased serum creatinine concentrations, renal failure.

From the nervous system:

dizziness, headache, convulsions with intravenous administration.

Hearing and labyrinth disorders:

hearing loss, tinnitus and vestibular disorders.

Allergic reactions:

rash, itching, fever, chills, bronchospasm, anaphylactic reactions, anaphylactic shock, urticaria, angioedema, rare reports of exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, including Stevens-Johnson syndrome.

Infusion reactions:

erythema or “flushing” of blood to the upper body.

Local reactions:

erythema, pain at the injection site, thrombophlebitis, abscess at the site of intramuscular injection.

Other:

superinfection.

Contraindications for use

Hypersensitivity to teicoplanin.

Carefully:

patients with hypersensitivity to vancomycin (risk of cross-hypersensitivity); in patients with renal failure (requires correction of the dosage regimen, monitoring of hearing status, hematological parameters, indicators of renal and liver function); in patients undergoing long-term treatment (monitoring of hearing status, hematological parameters, kidney and liver function parameters is required); with simultaneous treatment with other ototoxic and nephrotoxic drugs: aminoglycosides, colistin, amphotericin B, cyclosporine, cisplatin, furosemide and ethacrynic acid.

special instructions

Hearing, hematological, hepatic and renal toxicity of teicoplanin have been reported. Therefore, the state of hearing, hematological parameters, functional state of the liver and kidneys should be monitored, especially in patients with renal failure, in patients who are treated with teicoplaniv for a long time and in patients simultaneously receiving treatment with other oto- and nephrotoxic drugs (aminoglycosides, colistin, amphotericin B , cyclosporine, cisplatan, furosemide and ethacrynic acid). Superinfection: as with other antibiotics, the use of teicoplanin, especially if it is prolonged, can lead to excessive proliferation of microorganisms (bacteria or fungi) that are insensitive to teicoplanin; in the event of superinfection developing during treatment, appropriate measures must be taken. Impact on the ability to drive vehicles and machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, because Teicoplanin may cause dizziness and other side effects that may affect these abilities.