Teicoplanin
Teicoplanin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Teicoplanin
ATX code: J01XA02
Active ingredient: teicoplanin (Teicoplanin)
Manufacturer: Jodas Expoim Pvt. Ltd. (Jodas Expoim Pvt. Ltd.) (India)
Description and photo update: 2019-10-07
Teicoplanin is an antibacterial drug.
Release form and composition
Dosage form - lyophilisate for the preparation of a solution for oral administration, intravenous (i / v) and intramuscular (i / v) administration: powder from white to light yellow (200 and 400 mg each in colorless glass vials with a volume of 30 ml, sealed with rubber stopper, crimped with an aluminum cap and covered with a protective plastic cap). The included solvent is water for injection: a clear, colorless, odorless liquid (5 ml each in colorless glass ampoules with a break line). Packing: in a cardboard box 1 bottle with the drug and 1 bottle with a solvent; in a cardboard box with or without dividing partitions 5 or 10 vials with the drug and, respectively, 5 or 10 ampoules with a solvent and instructions for the use of Teicoplanin;in a cardboard box 5 or 10 vials with the drug and, respectively, 5 or 10 ampoules with a solvent, placed on plastic trays.
The composition of the drug in 1 bottle:
- active substance: teicoplanin (a mixture of 50% monosodium salt and 50% zwitterions) - 200 or 400 mg;
- auxiliary component: sodium chloride.
Pharmacological properties
Pharmacodynamics
Teicoplanin is an antibacterial agent with a glycopeptide structure. Under in vitro conditions, it demonstrates activity against gram-positive aerobic and anaerobic microorganisms.
The drug inhibits the growth of bacteria sensitive to it by inhibiting the biosynthesis of the membrane of the microbial cell in places other than those exposed to beta-lactam antibiotics.
Teicoplanin is effective against diseases caused by the following microorganisms: Staphylococcus spp. (including strains resistant to methicillin and other beta-lactam antibiotics), Listeria monocytogenes, Streptococcus spp., Corynebacterium spp. J / K groups, Micrococcus spp., Enterococcus spp., Peptococcus spp., gram-positive anaerobes, including Clostridium difficile.
In vitro, when using teicoplanin in combination with imipenem or aminoglycosides, a synergistic bactericidal action was observed against Staphylococcus aureus, together with ciprofloxacin - against Staphylococcus epidermidis. In combination with rifampicin, additive and synergistic effects have been revealed against Staphylococcus aureus.
There are reports of an increase in the minimum inhibitory concentrations (MIC) of the drug for some strains of Staphylococcus haemolyticus.
Under in vitro conditions, the development of one-stage resistance to teicoplanin was not revealed, however, after multiple passages, multi-stage resistance was developed.
Teicoplanin usually does not cross-resistance with other antibiotic groups. However, Enterococcus spp. a slight cross-resistance to teicoplanin and another glycopeptide, vancomycin, is found.
When determining the sensitivity of microorganisms to the drug, discs containing 30 μg of teicoplanin are used. Strains with a diameter of the growth inhibition zone of at least 14 mm are considered susceptible, and those in which the growth inhibition zone has a diameter of up to 10 mm are considered resistant.
Pharmacokinetics
After a single intramuscular injection of teicoplanin at a dose of 3–6 mg / kg, bioavailability is about 90%.
After oral administration, the drug is not absorbed and does not enter the systemic circulation if there are no changes in the digestive tract. About 40% of the dose is detected in feces in a microbiologically active form.
After i.v. administration of a dose of 3-6 mg / kg, teicoplanin is distributed in the body in two phases: the first is a phase of rapid distribution with a half-life (T ½) from plasma of about 0.3 hours, the second is a phase of slower distribution with T ½ of about 3 h. Further, there is a slow elimination of the drug with a final T ½ of about 150 hours. Such a long T ½ allows you to enter teicoplanin once a day.
With the introduction of a dose of 6 mg / kg in the form of a 30-minute intravenous infusion after 12 hours and then every 24 hours, the minimum concentration of the drug in plasma (C min) 10 mg / L, according to the calculated data, could be reached by the 4th day … The calculated C max (maximum plasma concentration) and C min of teicoplanin in the equilibrium state, which are 64 and 16 mg / l, respectively, could be achieved by the 28th day of treatment. The drug is quickly distributed into the subcutaneous fat, bone tissue, synovial fluid, pleural fluid, lung tissue, myocardium and blistering fluid, but poorly penetrates into the cerebrospinal fluid.
The weak affinity bond with plasma proteins is 90–95%. With intravenous administration of teicoplanin at a dose of 3–6 mg / kg, the volume of distribution in an equilibrium state in adults is 0.94–1.41 l / kg; in children, this indicator does not differ significantly.
After parenteral administration of the drug, only about 3% of the dose is metabolized. Approximately 97% is excreted unchanged, of which 80% - through the kidneys.
After intravenous administration of a dose of 3–6 mg / kg, renal clearance is in the range of 10.4–12.1 mg / h / kg, total plasma clearance is 11.9–14.7 ml / h / kg.
Indications for use
For parenteral administration:
- treatment of severe infections caused by sensitive gram-positive microorganisms, including those resistant to other antibiotics (penicillins, including cephalosporins and methicillin), including these infections in patients who are allergic to penicillins and cephalosporins;
- treatment of infections of the urinary tract, lower respiratory tract, bones and joints, skin and soft tissues, as well as septicemia, endocarditis and peritonitis caused by continuous ambulatory peritoneal dialysis (CAPD);
- prevention of infectious complications during orthopedic and dental operations in cases where there is a risk of developing an infectious process caused by gram-positive microorganisms.
For oral administration: pseudomembranous colitis caused by Clostridium difficile (associated with taking antibacterial drugs).
Contraindications
The use of Teicoplanin is contraindicated in the presence of hypersensitivity to its components, as well as during lactation.
The drug should be used with caution in the following cases:
- renal failure;
- liver failure;
- hypersensitivity to vancomycin;
- pregnancy (only if the potential benefits exceed the possible risks);
- long-term treatment with Teicoplanin;
- simultaneous use of ototoxic and nephrotoxic agents: cyclosporine, furosemide, cisplatin, colistin, aminoglycosides, ethacrynic acid, amphotericin B.
Teicoplanin, instructions for use: method and dosage
Teicoplanin is taken orally, injected intramuscularly and intravenously as a 3-5-minute injection or a 30-minute infusion. For newborns, only intravenous infusion is allowed.
Solution preparation:
- Into the vial with the lyophilisate slowly add 3.2 ml of sterile water.
- Gently shake the bottle, avoiding the formation of foam (the powder must completely dissolve). If the solution turns out to be foamy, it should be set aside for about 15 minutes to reduce the amount of foam.
- Slowly remove the solution from the vial, piercing the rubber stopper in the middle with a needle.
The reconstituted 3.2 ml solution will contain 200 or 400 mg teicoplanin (depending on the dosage chosen). It is important to properly prepare and remove the solution, otherwise a smaller dose may be administered than required.
The prepared solution is isotonic and has a pH of 6.5–7.5. It can be administered in this form or additionally diluted with 0.9% sodium chloride solution, 5% glucose solution, Ringer's solution, Hartman's solution and peritoneal dialysis solution containing 1.36 or 3.86% glucose.
Doses for adults and adolescents from 16 years of age with normal renal function
In case of moderately severe infections of the urinary tract, lower respiratory tract, skin and soft tissues on the first day, an intravenous dose of 400 mg is recommended, subsequently the maintenance dose is 200 mg 1 time per day intramuscularly or intravenously.
In severe infections of the joints and bones, endocarditis and septicemia, the first three doses are 400 mg intravenously at intervals of 12 hours, then 400 mg intramuscularly or intravenously 1 time per day. The minimum concentration of the drug in the blood serum should be at least 10 mg / l. The maximum concentration, determined 1 hour after intravenous administration of a dose of Teicoplanin 400 mg, is usually in the range of 20-50 mg / L.
Standard doses of the drug 200 and 400 mg correspond to dosages of 3 and 6 mg / kg, respectively. Patients weighing more than 85 kg are advised to adjust the dose depending on body weight, following the same treatment regimen: 3 mg / kg - for moderately severe infections, 6 mg / kg - for severe infections. In some cases (for example, with endocarditis and burns), the maintenance daily dose may be increased to 12 mg / kg.
For peritonitis, which has developed as a complication of CAPD, a single loading dose is 400 mg IV. In the first week of treatment, 20 mg / l is prescribed, the drug is added to each reservoir with a solution for dialysis, in the second week, a dose of 20 mg / l is added to every second reservoir, in the third week, the same dose is added to the reservoir with a solution for night dialysis …
For antimicrobial prophylaxis during orthopedic and dental operations (for example, to prevent endocarditis in patients with an artificial heart valve), Teicoplanin is administered once intravenously during induction of anesthesia at a dose of 400 mg or 6 mg / kg with a body weight of more than 85 kg.
In case of pseudomembranous colitis caused by Clostridium difficile, Teicoplanin is administered orally, 200 mg 2 times a day.
Dosing regimen for children aged 2 months to 16 years
For children from 2 months to 16 years old, for the treatment of diseases caused by most gram-positive infections, the first three doses of the drug are administered intravenously at 10 mg / kg at intervals of 12 hours, the further maintenance dose is 6 mg / kg once a day intravenously or i / m, with neutropenia and severe infections, the maintenance dose is 10 mg / kg once a day i / v.
Children under 2 months of age, including newborns, are given a dose of 16 mg / kg IV on the first day, then 8 mg / kg once a day IV. In this age group of patients, IV administration is always carried out by a 30-minute infusion.
Dosage regimen for adults with renal impairment
In the first three days of treatment, the dose of Teicoplanin is not adjusted. Starting from the fourth day, the dose is determined so that the concentration of the drug in the serum is maintained at 10 mg / L.
With moderate renal failure [creatinine clearance (CC) 40-60 ml / min], either reduce the maintenance dose by 2 times, or introduce a standard dose every 2 days.
Patients with severe renal insufficiency (CC <40 ml / min) and patients receiving hemodialysis, either reduce the standard dose by 3 times, or enter the usual dose every 3 days.
Teicoplanin is not excreted during hemodialysis.
Duration of treatment
In most infections caused by pathogens sensitive to Teicoplanin, a therapeutic response develops within 48–72 hours after starting treatment.
The general duration of therapy is determined by the doctor depending on the clinical picture, the type of infection and the severity of its course.
Osteomyelitis and endocarditis should be treated for at least 3 weeks.
The maximum duration of the drug is 4 months.
Side effects
Teicoplanin is generally well tolerated. The resulting adverse reactions are usually mild and transient. Severe disorders requiring discontinuation of therapy are rare.
Possible side effects:
- local reactions: pain at the injection site, erythema, thrombophlebitis, abscess at the intramuscular injection site;
- infusion reactions: rush of blood to the upper body, erythema (these reactions occurred in patients who had not previously received teicoplanin, they did not recur with subsequent injections of lower doses or at a reduced rate, therefore they were not specific for a particular concentration of solution and infusion rate);
- hypersensitivity reactions: chills, fever, itching, rash, urticaria, anaphylactic shock, anaphylactic reactions, angioedema; very rarely - exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, including Stevens-Johnson syndrome;
- from the kidneys: increased serum creatinine levels, renal failure;
- from the liver: an increase in the activity of hepatic transaminases, an increase in alkaline phosphatase in the blood serum;
- on the part of the blood: neutropenia, leukopenia, thrombocytopenia, agranulocytosis, eosinophilia;
- from the gastrointestinal tract: diarrhea, nausea, vomiting;
- from the central nervous system: headache, dizziness; with intravenous administration - convulsions;
- from the organ of hearing, labyrinth disorders: ringing in the ears, vestibular disorders, hearing loss;
- others: superinfection (overgrowth of microorganisms that are not sensitive to teicoplanin).
Overdose
There are known cases of erroneous administration of excessive doses (from 35.7 to 104 mg / kg) to children under 8 years of age. One 29-day-old newborn was agitated after an IV dose of 400 mg (95 mg / kg). The rest of the patients did not have any symptoms or abnormal laboratory parameters.
Hemodialysis does not remove the drug from the body. Treatment is symptomatic.
special instructions
Cross-sensitivity may develop in patients with known hypersensitivity to vancomycin, so caution should be exercised.
When using Teicoplanin, especially long-term, there is a possibility of developing superinfection, i.e. reproduction of microorganisms insensitive to the drug. In this case, appropriate treatment is required.
Hematological, renal and hepatic toxicity of teicoplanin, its toxic effect on the hearing organ have been reported. In this regard, it is recommended to monitor the functional state of the kidneys and liver, hematological parameters and the state of hearing, especially in patients with renal failure and patients who receive the drug for a long time or simultaneously take other nephro- and / or ototoxic drugs, such as ethacrynic acid, amphotericin B, colistin, cyclosporin, furosemide, cisplatin, aminoglycosides.
Influence on the ability to drive vehicles and complex mechanisms
In some patients, during therapy, side effects occur that can negatively affect the speed of reactions and the ability to concentrate (for example, dizziness). In this regard, patients are advised to take precautions.
Application during pregnancy and lactation
In animal studies, no teratogenic effects of the drug have been identified, however, clinical experience with pregnancy in humans is insufficient to assess the degree of safety of the antibiotic. During pregnancy or if it is suspected, Teicoplanin can be prescribed by a doctor only if the expected benefit from the forthcoming therapy justifies the potential risks.
There is no information on the penetration of the drug into breast milk. Women who need antibiotic therapy with Teicoplanin are advised to stop breastfeeding.
Pediatric use
Teicoplanin can be used in children from birth.
With impaired renal function
In patients with impaired renal function, the drug is used with caution. Correction of dosage regimen is required.
For violations of liver function
Teicoplanin has hepatic toxicity and should be used with caution.
Use in the elderly
Elderly patients with normal renal function do not need to change the dose of the drug. In the event of a decrease in renal function, appropriate recommendations for correcting the therapy regimen should be followed.
Drug interactions
Teicoplanin is pharmaceutically incompatible with aminoglycosides.
Side effects may develop with the simultaneous or sequential use of teicoplanin and nephro- or ototoxic drugs such as cyclosporin, amikacin, kanamycin, streptomycin, cephaloridin, furosemide, gentamicin, neomycin, colistin, tobramycin, cisplatin, amphotericin B, ethacrynic acid.
Analogs
Teicoplanin analogs are: Vancomabol, Vancomycin, Vankorus, Vibativ, Xidalba, Orthocid, Editsin, etc.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C, out of reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Teicoplanin
The drug appeared on the pharmaceutical market quite recently, therefore, today there are no reviews of Teicoplanin on specialized medical sites and forums.
Price for Teicoplanin in pharmacies
The price of Teicoplanin depends on the dosage, the region of sale and the pharmacy chain. The approximate cost of 1 bottle at a dose of 200 mg is 890 rubles, 1 bottle at a dose of 400 mg is 1480 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
