Teicoplanin

Teicoplanin is a glycopeptide antibiotic with bactericidal properties.

Indications Teicoplanina

It is used to eliminate infections caused by gram-positive microbes (this includes bacteria that are sensitive or resistant to methicillin). This group includes, for example, people with intolerance to β-lactam antibiotics:

• lesions affecting soft tissues and epidermis;
• infections in the lower and upper urinary tract (may also be accompanied by complications);
• lesions in the respiratory system;
• infections that occur in the throat, ears, or nose;
• endocarditis;
• infectious lesions of joints or bones;
• septicemia;
• Peritonitis caused by regular outpatient peritoneal dialysis procedures.

It is used to prevent the occurrence of endocarditis of infectious origin in case of intolerance to β-lactam antibiotics:

• during dental procedures or procedures in the upper respiratory tract area when general anesthesia is used;
• during surgical operations in the gastrointestinal tract or urogenital system.

Release form

The drug is released in the form of an injection lyophilisate, in vials of 0.2 or 0.4 g. The pack contains 1 such vial, in addition to which 1 vial with a solvent (injection water) is included.

It can also be produced in 3.2 ml cell packs – 1 piece per pack or 15 packs per box.

Pharmacodynamics

The drug forms a bond with acyl-D-alanyl-D-alanine of the mucopeptide located inside the bacterial wall, blocking its development and inhibiting the process of spheroplast formation. It demonstrates activity against coagulase-negative and Staphylococcus aureus (this includes microbes resistant to methicillin and other β-lactam antibiotics), micrococci, streptococci, Listeria monocytogenes, enterococci (including Enterococcus faecium), Corynebacteria from the JK category, gram-positive anaerobes, including Clostridium difficile, and peptococci.

Resistance to drugs develops quite slowly, and there is no cross-resistance with antibiotics from other drug groups. The prevalence rate of acquired resistance to a given drug in individual types of pathogens may fluctuate depending on time and geographic location. Therefore, it is useful to familiarize yourself with the data on the local prevalence of resistance, especially during therapy at severe stages of infections.

Pharmacokinetics

Suction.

The drug is not absorbed when taken orally. The bioavailability level when administered by injection is 94%.

Distribution processes.

The drug's indicators inside the blood serum are distributed in 2 stages (first there is a fast distribution stage, and then a slow one), the half-life of which is about 0.3 and 3 hours, respectively. After the distribution stage, slow elimination occurs, and its half-life is 70-100 hours.

Exchange processes.

Teicoplanin has no metabolic products. More than 80% of the administered substance is excreted unchanged in the urine after 16 days.

Excretion.

In people with healthy renal function, the medicinal element is excreted unchanged - almost entirely in the urine. The terminal half-life of the component is 70-100 hours.

Dosing and administration

Use for prevention.

To prevent the development of infectious endocarditis in adults, 0.4 g of the drug should be administered at the stage of induction of anesthesia. People with prosthetics in the area of heart valves should combine Teicoplanin with an aminoglycoside.

Application for therapy.

The duration of the course is determined by the type and severity of the disease, as well as the individual characteristics of the patient.

For adults and elderly people with normal renal function.

In infections affecting the respiratory system, throat with ears and nose, urethra and soft tissues with epidermis, as well as other moderate infections:

• loading dose: the standard daily dosage is 0.4 g (often equivalent to 6 mg/kg/day) in the form of a single injection (on the first day of the course);
• supportive measures: the standard dose size is 0.2 g/day (often equal to 3 mg/kg/day) in the form of a single intramuscular or intravenous injection per day.

Children (excluding newborns) with healthy kidney function.

The portion size and duration of the course are determined by the severity of the disease:

• loading dose: 3 initial injections of 10-12 mg/kg, administered at 12-hour intervals;
• supportive procedures: 10 mg/kg/day is administered.

For moderate forms of infections not accompanied by neutropenia:

• size of the loading dose: initial 3 injections – 10 mg/kg, administered at intervals of 12 hours;
• supportive measures: administration of 6 mg/kg/day.

To select the optimal dose of medication, it is necessary to determine the concentration of the active element of the drug in the blood plasma.

Method of application.

The drug is administered intravenously or intramuscularly. Either a half-hour infusion of the drug or the introduction of the substance over 60 seconds is assumed.

The solution should be prepared as follows: the solvent is slowly introduced into the vial with the lyophilisate, and then it should be gently shaken, placing it between the palms, until the substance is completely dissolved. It is necessary to ensure that no bubbles appear in the liquid. If foam appears, hold the vial vertically until it disappears. Such an isotonic solution (pH 7.5) can be stored for a maximum of 24 hours at a temperature of no more than 25 ° C, or for 1 week at a temperature of 5 ± 3 ° C.

The prepared liquid can be administered by injection or diluted with the following substances:

• 0.9% NaCl solution. The diluted substance retains its properties for 24 hours (temperature level up to 25°C) or 1 week (temperature level up to 4°C);
• a solution made on the basis of sodium lactate. The diluted liquid can be kept at 25°C for up to 24 hours or 1 week at 4°C;
• 5% glucose solution or 0.18% NaCl solution in combination with 4% glucose (these solutions can be stored at temperatures up to 25°C for a maximum of 24 hours);
• solution used for peritoneal dialysis procedures (1.36% or 3.86% glucose). It can be kept at a temperature not exceeding 4°C for up to 28 days.

Teicoplanin remains stable for 48 hours if the temperature does not exceed 37°C, and the drug itself is a component of solutions used for peritoneal dialysis sessions (they contain heparin or insulin).

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Use Teicoplanina during pregnancy

Animal tests have not shown any teratogenic effects, but there is insufficient clinical data on humans. Given the high efficacy of teicoplanin, it can be prescribed to pregnant women when there is a need for its use for vital indications (regardless of the gestational age). In such cases, it is necessary to check the newborn's hearing (otoacoustic emission) - due to the fact that teicoplanin can have an ototoxic effect.

There is no information on the passage of the active element Teicoplanin into breast milk, which is why it is recommended to refrain from using the drug during breastfeeding.

Contraindications

Contraindication is hypersensitivity to teicoplanin.

Side effects Teicoplanina

The use of the drug may lead to the appearance of certain side effects:

• symptoms of hypersensitivity: urticaria, rashes, fever, itching, cold and erythema, as well as anaphylactic manifestations (such as anaphylaxis, bronchospasm and Quincke's edema) and exfoliative dermatitis;
• lesions of the subcutaneous layers and epidermis: severe bullous manifestations (such as TEN and Stevens-Johnson syndrome, and in addition, in exceptional cases, erythema multiforme);
• liver disorders: transient increase in transaminase or alkaline phosphatase values;
• disorders of hematopoietic and lymphatic function: development of thrombocyto-leuko- or neutropenia (rarely in severe form), as well as agranulocytosis (curable if therapy is discontinued), often appearing with the introduction of large doses of drugs in the first month of treatment;
• problems with digestion: vomiting, diarrhea or nausea;
• urinary and renal dysfunction: transient increase in creatinine levels, renal failure, which often develops in people with severe forms of infection and the presence of underlying pathology, or in people taking other drugs that have the ability to reveal nephrotoxic effects;
• reactions from the nervous system: hearing loss, dizziness, tinnitus, disorders affecting the vestibular apparatus, and headaches. There are isolated data on the development of seizures;
• local symptoms: phlebitis, abscess, pain and erythema;
• other: development of superinfection (increase in the number of resistant bacteria).

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Overdose

It is not possible to remove the drug using hemodialysis sessions, so symptomatic measures will be required in case of poisoning.

Interactions with other drugs

Due to the increased risk of developing negative symptoms, Teicoplanin should be used with caution in people who use it in combination with ototoxic or nephrotoxic medications (for example, cyclosporine with aminoglycosides, as well as amphotericin B with furosemide).

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Storage conditions

Teicoplanin should be kept in a place out of reach of children. Temperature values – up to 25°C.

Shelf life

Teicoplanin can be used for 2 years from the date of release of the drug.

Use in children

It is prohibited to prescribe the medicine to newborn babies.

Analogues

Analogues of the drug are the drugs Glitake with Targocid, as well as Teicoplanin-Pharmex.