Targocide

One of the representatives of powerful antibacterial drugs - glycopeptide antibiotics - is considered to be Targocid. The main substance of the drug is teicoplanin - an active antimicrobial ingredient.

Indications Targocida

Targocid is prescribed for infectious pathologies that were initially caused by gram-positive microorganisms. Targocid is recommended for bacteria resistant to Methicillin or for patients prone to allergies to β-lactam antibiotics.

From the age of 18, Targocid can be used for therapeutic purposes for the following pathologies:

• microbial dermatological lesions;
• microbial lesions of the urinary system;
• microbial pathologies of the respiratory organs;
• bacterial pathologies in otolaryngology;
• musculoskeletal infections;
• sepsis, endocarditis;
• Peritonitis caused by prolonged peritoneal dialysis.

Targocid is also appropriate for the prevention of bacterial endocarditis, as well as in dental and pulmonological practice, and during surgical interventions.

Targocid can be used in childhood (with the exception of the neonatal period).

Release form

Targocid is produced in the form of a lyophilized substance for the preparation of an injection solution.

The lyophilized substance is packaged in 400 mg vials. The drug is additionally supplied with a solvent in a 3.2 ml ampoule.

The lyophilisate substance is a light (almost white) homogeneous mass. The active ingredient is teicoplanin, and the auxiliary is sodium chloride.

Water for injection is included as a dissolving agent.

Pharmacodynamics

Targocid belongs to a series of glycopeptide antibacterial agents with systemic activity. It is an enzymatic product that affects aerobic and anaerobic gram-positive microbes.

The active ingredient inhibits the activity of sensitive bacteria by altering the process of biological synthesis of cell membranes in areas where β-lactam antibiotics do not act.

Targocid exhibits activity against gram (+) aerobes (bacilli, enterococci, listeria, rhodococci, staphylococci, streptococci) and anaerobes (clostridia, eubacteria, peptostreptococci, propionobacteria).

Resistant to the influence of Targocid are actinomycetes, erysipelothrix, heterofermentative lactobacilli, nocardia, pediococci, chlamydia, mycobacteria, mycoplasma, rickettsia, and treponema.

The antibiotic Targocid does not exhibit cross-resistance with other groups of antimicrobial drugs.

Aminoglycosides and fluoroquinolones have a synergistic effect.

Pharmacokinetics

Oral administration of the drug does not result in its absorption.

Bioavailability after intramuscular administration may be approximately 94%.

The type of plasma concentration distribution after intravenous infusion is two-stage (fast and slow distribution), with half-lives of 0.3 and three hours, respectively. At the end of the distribution stage, gradual elimination is observed, the half-life is from 70 to 100 hours.

Five minutes after intravenous infusion of Targocid in the amount of 3-6 mg/kg, the plasma concentration is 54.3 or 111.8 mg/liter, respectively. The residual content in plasma 24 hours after administration may be 2.1 or 4.2 mg/liter, respectively.

Plasma albumin binding ranges from 90 to 95%.

Distribution of the drug in tissues is 0.6-1.2 l/kg. The active ingredient of the drug penetrates well into various tissue layers - teicoplanin penetrates especially well into the skin and bone tissue. The active ingredient is absorbed by leukocytes, thereby increasing their antimicrobial effect.

Teicoplanin is not detected in erythrocytes, cerebrospinal fluid and lipid tissue.

No degradation products of the active ingredient Targocid were detected. More than 80% of the drug that entered the bloodstream was excreted unchanged in urine 16 days after administration.

Dosing and administration

Targocid is administered by injection or infusion, intravenously or intramuscularly.

• Initial dose of Targocid for adult patients:
  • 400 mg is administered intravenously up to 2 times a day for 1-3 days, after which they switch to 200-400 mg per day intravenously or intramuscularly;
  • in case of burn injury or endocarditis, the maintenance dose of the drug can be up to 12 mg per kg per day;
  • for pseudomembranous enterocolitis, administer 200 mg in the morning and evening;
  • As a prophylactic measure during surgery, 400 mg of the drug is administered intravenously at one time.
• Initial dose of Targocid for pediatric patients (2 months to 16 years):
  • 10 mg/kg intravenously every 12 hours three times, then 6-10 mg/kg daily intravenously or intramuscularly;
  • For children under 2 months of age, 16 mg/kg is prescribed on the first day (half-hour intravenous infusion), after which they switch to a maintenance dosage of 8 mg/kg daily intravenously.
• In case of impaired renal function, the amount of Targocid is adjusted from the fourth day, maintaining the drug level in the blood at 10 mg per liter. If creatinine clearance is from 40 to 60 ml per minute, the dosage is cut in half or administered every other day. If clearance is less than 40 ml per minute, or the patient undergoes hemodialysis, then a third of the original amount of the drug is administered every day or once every three days.
• In old age, with adequate renal function, there is no need to adjust the dosage.

The duration of the therapeutic course of Targocid is assessed individually: the doctor takes into account the severity of the bacterial infection and the clinical response of the patient's body. If the treatment is carried out for endocarditis or osteomyelitis, its duration can be 21 days or more, but Targocid should not be used for more than four months.

To breed Targocid, follow these steps:

• the solvent from the ampoule is introduced into the vial with lyophilized powder until completely dissolved;
• Do not shake the medicine to avoid foaming;
• if foam does form, it is necessary to leave the preparation alone for 15-20 minutes;
• the solution is extracted from the bottle using a syringe;
• The drug is administered by injection or additionally diluted with isotonic solution, dextrose or Ringer's solution for intravenous infusion.

Use Targocida during pregnancy

Testing of the drug Targocid on experimental animals did not result in teratogenic manifestations. However, experts believe that clinical information on the effect of Targocid on the body of a pregnant woman is currently insufficient.

Since Targocid has a high therapeutic antibacterial effect, its use in pregnant patients is possible, but with special caution. At any stage of gestation, it is necessary to monitor the development of the fetus, and after the birth of the baby, its hearing functionality should be checked, since Targocid may have an ototoxic effect.

Due to insufficient information, treatment with Targocid is not recommended for breastfeeding patients.

Contraindications

It is not recommended to prescribe treatment with the antibiotic Targocid in case of hypersensitivity to this drug, as well as to use it during the neonatal period (28 days after the birth of the baby).

Relative contraindications are:

• hypersensitivity to vancomycin (risk of cross-reaction);
• insufficient renal function;
• the need for long-term treatment (long-term treatment with Targocid is possible only with regular monitoring of hearing function, blood count, liver function and urinary system);
• concomitant administration of other oto- and nephrotoxic medications (aminoglycoside drugs, cyclosporine, ethacrynic acid, amphotericin, furosemide, etc.).

Side effects Targocida

The course of treatment with Targocid may be accompanied by some unexpected reactions from the body:

• hypersensitivity reaction (rash, hyperthermia, cold, dermatitis, anaphylaxis);
• skin manifestations (epidermal necrolysis, erythema);
• liver disorders;
• changes in the blood picture (decrease in the number of leukocytes and platelets, agranulocytosis);
• dyspepsia;
• transient increase in creatinine, poor renal function;
• dizziness, headaches, hearing loss, tinnitus, vestibular disorders, convulsions;
• pain at the injection site, abscess formation, phlebitis;
• development of superinfection.

Overdose

There are cases when children were given incorrectly calculated doses of Targocid. For example, there is information about the intravenous administration of 400 mg of the drug (95 mg per kg of weight) to a child aged 29 days: the baby showed clear signs of overexcitement.

Other cases do not indicate the development of any specific symptoms: situations with an overdose of Targocid in patients aged from 29 days to eight years are considered (dosages from 35 mg/kg to 104 mg per kg of weight were mistakenly administered).

In case of excessive administration of Targocid, hemodialysis is ineffective. Therapy is carried out using symptomatic medications.

Interactions with other drugs

Targocid should not be combined with other medications that have a toxic effect on the organs of hearing and kidneys. Such medications include: Streptomycin, Furosemide, Cyclosporine, Neomycin, Tobramycin, Cisplatin, etc.).

There is evidence of clinical incompatibility of Targocid with aminoglycosides.

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Storage conditions

Store Targocid in rooms with temperatures from +15 to +30°C, out of reach of children.

After diluting the preparation, it is better to use it immediately, or it can be stored for 24 hours at a temperature of +4°C.

Shelf life

Packages with Targocid can be stored for up to 3 years, under appropriate conditions.