Teykoplanin

Teicoplanin is a glycopeptide-type antibiotic with bactericidal properties.

Indications Teykoplana

It is used to eliminate germ-positive infections caused by germs (this includes bacteria that have sensitivity or resistance 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 part of the urinary duct (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 procedures of peritoneal dialysis in outpatient settings.

Used to prevent the appearance of endocarditis of an infectious origin when intolerant to β-lactam antibiotics:

• during dental procedures or procedures in the upper part of the respiratory ducts, when general anesthesia is used;
• with surgical operations in the gastrointestinal tract or urogenital system.

Release form

Release of the medicine is made in the form of injection lyophilizate, in flakonchikah volume of 0.2 or 0.4 g. In pack 1, such a bottle, in addition to which is attached 1 bottle of solvent (injection water).

It can also be produced in cell packs with a volume of 3.2 ml - one piece per pack or 15 packs per carton.

Pharmacodynamics

The drug forms a bunch of acyl-D-alanyl-D-alanine located inside the wall of the bacterium mukopeptide, blocking its development and inhibiting the formation of spheroplasts. It shows activity against coagulase-negative and golden staphylococci (microbes that are resistant to methicillin and other β-lactam antibiotics), micrococci, streptococci, listeria monocytogenes, enterococci (among them enterococcus fecium), corynebacteria from the JK category, gram-positive anaerobes, among which clostridium diffifile, and peptococcus.

Resistance to drugs develops rather slowly, and there is no cross-resistance with antibiotics from other medicinal groups. The indicator of the prevalence of acquired resistance with respect to a given drug for certain types of pathogens may fluctuate with time and geographical location. Therefore, it will be useful to get acquainted with the data concerning the local prevalence of resistance, especially during therapy in severe stages of infection.

Pharmacokinetics

Suction.

The medicine is not absorbed when ingested. The level of bioavailability when injected is 94%.

Distribution processes.

The indicators of drug substance inside the blood serum are distributed in 2 stages (first follows a rapid distribution stage, and then - a slow one), the half-lives at which are respectively about 0.3 and 3 hours. After the distribution stage, a slow elimination is carried out, and its half-period is 70-100 hours.

Exchange processes.

Teicoplanin does not have metabolic products. More than 80% of the used substance is excreted unchanged together with urine after 16 days.

Excretion.

In people with a healthy renal function, the drug element is excreted unchanged-almost all along with the urine. The final half-life of the component is 70-100 hours.

Dosing and administration

Use for prevention.

To prevent the development of infective endocarditis in an adult, it is necessary to administer 0.4 g of drugs at the stage of introductory anesthesia. People with prosthetics in the field of heart valves need to combine Teicoplanin with 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 activity.

In infections affecting the respiratory system, the throat with ears and nose, urethra and soft tissues with epidermis, and in addition with other infections of moderate severity:

• loading dose: the size of the standard dosage per day is 0.4 g (often it corresponds to 6 mg / kg / day) in the form of a single injection (on the first day of the course);
• Supporting measures: the size of the standard portion is 0.2 g / day (often equal to 3 mg / kg / day) in the form of a one-time IM or IV injection a day.

Children (excluding newborns) with healthy kidney work.

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

• loading dosage: 3 initial injections are 10-12 mg / kg, which are administered at intervals of 12 hours;
• supporting procedures: administered at 10 mg / kg / day.

With moderate forms of infections not accompanied by neutropenia:

• the size of the loading dose: the initial 3 injections - in the amount of 10 mg / kg, with the introduction at intervals of 12 hours;
• supportive measures: administration of 6 mg / kg / day.

To select the optimal portion of the drug, you should determine the concentration of the active element of the drug inside the blood plasma.

Method of application.

The drug is administered in / in or in / m method. It is assumed that either a half-hour infusion of the drug, or the administration of the substance for 60 seconds.

The solution should be prepared in the following way: the solvent is slowly introduced into the vial with the lyophilizate, and then it must be gently shaken, located between the palms, until the substance dissolves completely. It is necessary to ensure that no bubbles appear in the liquid. When the foam appears, you need to hold the bottle upright until it disappears. This isotonic solution (pH 7.5) allows a maximum of 24 hours to be maintained at a temperature of no more than 25 ° C, or during the first week at a temperature of 5 ± 3 ° C.

The prepared liquid is allowed to be injected or diluted with the help of such substances:

• 0.9% NaCl solution. The diluted substance retains its properties for 24 hours (temperature index to 25 ° C) or 1-week (temperature level up to 4 ° C);
• solution, made on the basis of lactic sodium. The diluted liquid may be contained at 25 ° C up to 24 hours or 1 week at 4 ° C;
• 5% glucose solution or 0.18% solution of NaCl in combination with 4% glucose (these solutions can be stored at temperatures up to 25 ° C for a maximum of 24 hours);
• a solution used for peritoneal dialysis procedures (1.36% or 3.86% glucose). It can be kept at a temperature of no higher than 4 ° C up to 28 days.

The stability of Teicoplanin persists for 48 hours, if the temperature does not exceed 37 ° C, and the preparation itself is an integral part of the solutions used for peritoneal dialysis sessions (they contain heparin or insulin).

[2]

Use Teykoplana during pregnancy

Tests conducted on animals showed no teratogenic effects, but there is not enough clinical information on humans. Taking into account the high effectiveness of the therapeutic effect of teicoplanin, it can be prescribed to pregnant women when there is a need for its use for vital indications (without reference to the term of pregnancy). In such cases, it is necessary to check the newborn's hearing (otoacoustic emission) - due to the fact that teicoplanin can have ototoxic effects.

There is no information on the passage of the active element of Teicoplanin into the mother's milk, which is why it is recommended to abandon the use of drugs during breastfeeding.

Contraindications

Contraindication is the presence of high sensitivity to teicoplanin.

Side effects Teykoplana

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

• symptoms of hypersensitivity: urticaria, rashes, fever, itching, colds and erythema, and in addition anaphylactic manifestations (such as anaphylaxis, bronchial spasm and Quincke edema) and exfoliative form of dermatitis;
• lesions of the subcutaneous layers and epidermis: bullous manifestations in severe degree (such as TEN and Stevens-Johnson syndrome, and in addition, in exceptional cases, polyforma erythema);
• hepatic disorders: a transient increase in the values of transaminases or alkaline phosphatase;
• disorders of the hematopoietic and lymphatic function: development of thrombocytopoietic or neutropenia (occasionally in severe form), as well as agranulocytosis (treatable under the condition of discontinuation of therapy), often appearing when large portions of drugs are administered in the first month of treatment;
• problems with digestive activity: vomiting, diarrhea or nausea;
• disorders of urinary and renal function: transient increase in creatinine, kidney 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 detect nephrotoxic effects;
• reactions from the NA: hearing loss, dizziness, ear noise, disorders affecting the vestibular apparatus, as well as headaches. There are separate data on the development of seizures;
• local symptoms: phlebitis, abscess, pain and erythema;
• Other: development of superinfection (increase in the number of resistant bacteria).

[1]

Overdose

To withdraw the medicine with the help of hemodialysis sessions will not succeed, therefore poisoning will require symptomatic measures.

Interactions with other drugs

Because of the increased risk of developing negative symptoms, use of Teicoplanin with caution is necessary for people who use it in combination with ototoxic or nephrotoxic medicines (eg, cyclosporine with aminoglycosides, and in addition amphotericin B with furosemide).

[3], [4]

Storage conditions

Teykoplanin must be kept in a place that is closed from children's access. Temperature values are up to 25 ° С.

Shelf life

Teikoplanin is allowed to be used for 2 years after the release of the drug.

Use in children

It is forbidden to prescribe medication to newborn babies.

Analogues

Analogues of the medication are Glayteik preparations with Targocid, and also Teicoplanin-Farmex.