Edicine

Antimicrobial drug for systemic use, antibiotic glycopeptide group - Edicin (Edicin) shows good results in the management of infectious and inflammatory processes.

[1], [2], [3]

Indications Edicine

Indications for the use of Edicyin are due to the physico-chemical characteristics of the active chemical compound vancomycin (vancomycin).

The main indications for the use of Edicyin are diseases that develop on the basis of inflammation caused by a different infection showing increased sensitivity to vancomycin. This is especially true in case of intolerance or ineffective treatment with cephalosporin or penicillin group drugs.

• Infectious lesion of the joint and bone tissue, for example, osteomyelitis.
• Sepsis.
• Enterocolitis is a common pathology of the gastrointestinal system, in which joint inflammation and thick (colitis) and thin (enteritis) guts occur.
• Infectious damage to lower respiratory tract systems and organs, including pneumonia, bronchitis, and so on.
• Endocarditis is an inflammation of the inner shell of the heart (endocardium).
• False-colonic colitis provoked by Clostridium difficile.
• Infection affecting the receptors of the central nervous system, for example, such as a minigitis.
• Infection of the epidermis and other tissues.

[4], [5], [6], [7], [8], [9], [10], [11], [12]

Release form

The main active chemical compound of Edicin is the substance of vancomycin hydrochloride. One gram of this substance corresponds to 1,000,000 IU of vancomycin. Its content in the unit of the drug is determined by the numbers: 0.5 mg or 1.0 mg. The form of release of a medicinal compound is a dried medicinal extract (lyophilizate) used in the manufacture of a liquid medicine for droppers. The liquid is released in vials of dark glass, later packed in a box of classical shape.

Pharmacodynamics

The main pharmacological properties of the drug in question are determined by the physico-chemical indices of the active chemical compound that forms the basis of the drug unit, vancomycin. Pharmacodynamics Edicyin is aimed at inhibiting the development and distribution of cells of pathogenic flora, increasing the permeability of already existing structures. This fact allows to block the development of new and elimination of existing units of invasive infection. This effect is achieved due to the ability of vancomycin to bind and penetrate the alanine-D-acyl-D-alanine mucopeptide, leading to a failure in combining the ribonucleic acids of the "aggressor".

Pharmacodynamics of the preparation Edicyin is especially biologically active with respect to aerobic gram-positive strains, as well as anaerobic gram-positive strains. These include:

1. Actinomyces spp ..
2. Listeria monocytogenes, Streptococcus agalactiae.
3. Corynebacterium diphtheriae.
4. Streptococcus spp., Including Streptococcus pyogenes, Streptococcus bovis, Streptococcus pneumonia, Streptococcus viridans, and strains resistant to the penicillin group.
5. Enterococcus faecalis.
6. Enterococcus spp ..
7. Staphylococcus spp., Including resistant-methicillin microorganisms, Staphylococcus epidermidis, strains of Staphylococcus aureus.
8. Clostridium spp.

Outside the living organism, vancomycin has no significant effect on gram-negative microscopic organisms, fungal representatives, protozoans, microscopic bacteria and viruses.

There is not any mutual opposition between Edicine and the antibiotics of other groups. Pharmacodynamics of Edicyin shows the maximum therapeutic effectiveness with acid-base factor pH 8. If it decreases to pH 6, the quality of the final result is sharply reduced. The drug remains active only on pathogenic microscopic organisms, passing the stage of reproduction.

[13], [14], [15], [16], [17],

Pharmacokinetics

The considered drug, when introduced into the body, is weakly absorbed by the mucosa of the digestive system. In the case of intraperitoneal drug intake (through the peritoneum), the pharmacokinetics of Edicyin can show a systemic adsorption result of about 60%.

When the patient enters the patient's body at the rate of 30 mg per kilogram of the patient's weight, his maximum amount in the blood is determined by a figure of approximately 10 mg / ml. This concentration level is fixed at the end of six hours after administration. In the case of intravenous Edicyin, such a high component providing a therapeutic effect is observed in many organs and systems of man: in pleura exudate and pleural effusion, in ascitic fluid of the abdominal cavity, in the layers of the auricle, exudate of the pericardial region, in the biological environment of the synovial (articular) zone , in the lubricant component of peritoneal filters, in the urine.

Pharmacokinetics Edicycine shows a low level of binding to blood plasma proteins. This figure is about 55%. The drug does not show the ability to overcome the blood-brain barrier, but high placental infestation and penetration into breastmilk. With inflammation of the membranes of the brain and / or spinal cord (minigitis), the therapeutic concentration of the drug is observed in the cerebrospinal or cerebrospinal fluid (cerebrospinal fluid).

Vancomycin hydrochloride practically does not lend itself to biotransformation. If the adult patient has healthy kidneys, the half-life (T _1/2 ) of the drug falls within a time interval of four to six hours. In case of an anamnesis of a patient who is burdened with chronic renal insufficiency or in the event of stopping urine in the urinary bladder (anuria), the rate of utilization and removal of the drug from the patient's body is inhibited and can last up to seven to eight days.  

In the case of therapeutic treatment, involving multiple administration of the drug, it is possible to accumulate vancomycin.  

During the first day after taking the medicine, by glomerular filtration, with urine through the kidneys, about 75% of Edicine is excreted from the body. If the patient underwent a nephrectomy (removal of the kidney), then the withdrawal procedure is somewhat slowed down, and the mechanism of isolation is not known to date. It is only known that a moderate amount leaves with bile. If the drug enters the body orally, it is almost completely removed from the fecal masses and in small doses with peritoneal dialysis or hemodialysis.

[18], [19], [20], [21], [22],

Dosing and administration

To obtain the necessary medicinal effect, the method of application and dose should be prescribed only by a specialist. Vancomycin is administered to the patient only intravenously, intramuscular injection is not allowed. Not recommended any bolus injections, except for infusion into the body through the vein.

For adult patients, the starting dosage is usually set at 0.5 g, the slow administration of intravenous infusion is carried out every six hours, and with the administration of double-dose drugs (1 g), then twice a day with an interval of twelve hours. The speed of the dropper is not more than 10 mg / min, it takes at least an hour to administer the basic dosage (0.5 g). The concentration of vancomycin in the infusion solution should not be above 5 mg / ml.

For small patients, the dosage of the drug directly depends on the age of the child.

1. For newborns that are not yet seven days old, the starting dosage is calculated as 15 mg per kilogram of patient weight, further the dosage is reduced to 10 mg / kg. The drug is injected every twelve hours.
2. Breastfedi, who have not yet turned a month, the starting dosage is calculated as 10 mg per kilogram of the patient's weight, administered infusion every eight hours.
3. Children, age from one month and older, the starting daily dosage is calculated as 40 mg per kilogram of the patient's weight, divided into three infusions with an interval of eight hours.

The concentration of vancomycin in the infusion solution should not be above 2.5 - 5 mg / ml. The speed of the dropper is not more than 10 mg / min, it takes at least an hour to administer the basic dosage (0.5 g).

The maximum acceptable single dose for a small patient should not exceed 15 mg / kg. The same daily figure corresponds to a figure of 60 mg per kilogram of the body weight of the child and should not exceed the same figure for an adult patient - not more than 2 g daily.

For patients with renal dysfunction, correction of the amount of Edicine administered and / or the time interval between infusions is mandatory, depending on the level of insufficiency. In this situation, the starting amount is assigned at a rate of 15 mg per kilogram of the patient's weight. To determine the effective, but safe, interval between injected drugs, regular monitoring of creatinine clearance is carried out.

In order to obtain the required concentration of the solution (50 mg / ml), 500 mg of Edicyin should be dissolved in 10 ml of special pure water used for medical procedures. If the drug is 1 g, then water is taken, respectively, twice as much.

If it is necessary to obtain lower therapeutic concentrations, 500 mg of vancomycin is diluted with 100 ml of a special diluent. 1 g, respectively, diluted 200 ml. As a diluent, mainly 0.9% sodium chloride solution is taken, the second, often used preparation, is 5% glucose solution. The quantitative component of vancomycin in the prepared solution should not be more than 5 mg / ml.

If the solution was diluted to the desired concentration without any deviation from the requirements, using 0.9% sodium chloride or 5% glucose, the prepared medicine can be stored without the risk of loss of efficacy for two weeks in the refrigerator at a temperature of 2-8 ° C.

Do not forget that before any infusion the injected solution must be visually checked for the absence of foreign bodies and impurities, as well as the probability of changing the hue of the liquid.

The prepared solution is allowed to be prescribed for internal administration through the mouth (orally) or, if necessary, via a nasogastric tube.

For oral administration, the solution is prepared somewhat differently: 0.5 g of the vial is diluted with 30 ml of pure sterile water for injection.

Special food additives in the form of syrups and perfumes are used to improve the taste characteristics of Edicine in the case of its appointment as a drink.

For adult patients, usually starting dosage is prescribed in 0.5 g - 1 g, diluted in three to four oral doses. With medical necessity, the amount of the drug can be increased, but the daily amount should not exceed 2 g. The duration of the therapeutic course is from seven to ten days.

To small patients the daily dosage is calculated as 40 mg, taken for one kilogram of the weight of the baby and divided into three to four inputs. The duration of the therapy is from seven to ten days.

Persons with liver function problems (enzyme deficiency) should not adjust the dose of Edicyin.

[35], [36], [37]

Use Edicine during pregnancy

Proceeding from the fact that vancomycin shows a fairly good placental invasion and easily penetrates into breastmilk, the use of Edicine during pregnancy, especially in the first trimester, when the laying and formation of all organs and systems of the future human body is categorically contraindicated. The use of remedial therapy in the second and third trimester of fetal gestation is possible only in case of serious vital signs, when the real help for a woman's health substantially outweighs the expected complications that may arise during embryo development.

Edicycine is assigned to group C by the FDA risk category for FDA when using drugs by pregnant women. This means that animal experiments have shown a negative effect of the drug on the embryo, and no necessary studies have been performed in pregnant women, but the potential benefits associated with the use of this drug in a future mother may justify its use, despite the risk for the baby.

If there is a therapeutic need for treatment of a young mother during the period when she feeds her newborn baby with a breast, then during the therapy it is recommended to stop breastfeeding the baby with mother's milk.

Contraindications

A particular systemic effect, resulting in the emergence of negative symptoms, the drug in question has no effect. Therefore, contraindications to the use of Edicyin are insignificant and limited to the following pathologies:

• Increased individual intolerance of the components of the drug.
• Inflammatory process in the nerve, which provides the function of hearing - neuritis of the auditory nerve.
• The first trimester of pregnancy.
• Time of feeding a newborn baby with breast milk.

[23], [24], [25], [26], [27], [28], [29], [30]

Side effects Edicine

Each organism is individual and has its own level of sensitivity. Therefore, the administration of a chemical compound at the dosages necessary to produce the expected therapeutic effect is sometimes capable of causing side effects of Edicyin.

• This may be a vertex that manifests itself in such a symptomatology:
  • Deterioration of hearing.
  • The appearance of an unpleasant constant noise accompaniment.
  • Nausea, with a strong intensity provoking an emetic reflex.
  • Enhanced function of sweat producing glands.
  • Cardiopalmus.
• Neutropenia reversible nature.
• Diarrhea.
• Eosinophilia - an increase in the quantitative level of eosinophils in the blood plasma.
• Pseudomembranous colitis is a serious pathology of the colon, developing as a complication of antibiotic therapy.
• Rashes, itching.
• Thrombocytopenia - a decrease in the number of platelets less than 150 · 109 / l, which is accompanied by increased bleeding and problems with stopping bleeding.
• Leukopenia - a decrease in the quantitative level of leukocytes below 4,0 * 109 / l.
• Rare cases of agranulocytosis - a sharp decrease in the content of granulocytes in the blood (less than 1x109 / l, neutrophilic granulocytes less than 0.5x1x109 / l).
• Post-infusion reaction of the body with rapid administration of the drug.
• Nephrotoxicity, in rare cases inclusive, to the provocation of renal insufficiency.
• With prolonged use of large doses or combination with aminoglycosides, there is a possibility of nitrogen growth in urea, as well as plasma concentrations of creatinine.
• Interstitial nephritis can rarely develop. Such a result can be obtained if the patient has a renal function impaired or one of the aminoglycosides is administered in parallel.
• Exfoliative dermatitis.
• Dizziness.
• Spasm of the muscles of the bronchi and muscular tissues of the back and neck.
• Inflammation, leading to the destruction of the walls of blood vessels (vasculitis).
• Hyperemia.
• Toxic epidermal necrolysis is the response of the body to the injection of a drug.
• Falling blood pressure.
• Fever.
• If the infusion requirements are violated, there may be a local reaction to the input:
  • Thrombophlebitis is an inflammatory process that affects the walls of the veins with clotting of the blood clot (thrombus).
  • Pain symptomatology in the area of injection.
  • The process of tissue cell necrosis in the area of infusion.

[31], [32], [33], [34]

Overdose

If the preparation of a solution for intravenous or oral administration and during the process of infusion itself fails to meet the requirements and recommendations, the probability of obtaining high doses of the drug is minimized. But if, however, an overdose, for whatever reason, has occurred, then one can observe an increase in the intensity of manifestations of side effects.

In this situation, symptomatic therapy is prescribed. A positive result can also be made by parallel hemofiltration and hemoperfusion.

[38], [39], [40], [41]

Interactions with other drugs

In case of unqualified complex therapy, it is often possible to observe the induction or, conversely, the activation of the characteristics of a particular drug. To avoid unforeseen results and to achieve the maximum expected efficiency, it is necessary to know the consequences of the interaction of Edicyin with other drugs. Otherwise, it is possible to inflict irreparable damage on the patient's health.

Simultaneous administration of vancomycin with such drugs and drug groups as aminoglycoside antibiotics, loop diuretics, polymyxins, amphotericin B, cyclosporins, bacitracin or cisplatin are capable of provoking hearing problems and pathological changes in the kidneys.

If the complex treatment includes drugs related to nephrotoxic or neurotoxic pharmacological preparations, most of it refers to viomiozin, ethacrynic acid, polymyxin B, colistin, as well as  neuromuscular blocking agents, there is a medical need for closer monitoring of the patient's condition during therapy .

Kolestyramin reduces the pharmacodynamic characteristics of Edicine. Tandem use of anesthetics, dramatically increases the likelihood of developing hypotension, manifestations of allergic symptoms in the form of itching and urticaria. Further mutual use can lead to the development of abnormal reddening of the skin, histamine-like tides, anaphylactoid reaction of the body and anaphylactic shock. But to reduce the frequency and intensity of such negative manifestations can be with the introduction of vancomycin at a very low rate (taking 0.5 g of the drug stretches more than an hour) and before receiving anesthetic.

It is worthwhile to caution that special precautions are needed when introducing Edicine to newborn babies, especially if they are premature babies. It is necessary to regularly check the level of the active substance in the blood plasma.

During the whole therapy it is necessary to carry out periodic control studies:

• Comparative audiogram, a graph that allows you to monitor the state of a person's hearing.
• Monitoring of kidney work status monitoring:
  • Examination of urine.
  • Indicators of nitrogen in urea.
  • Determination of the level of creatinine.
• It is not superfluous to determine the quantitative index of vancomycin in the blood serum. This is especially true for elderly patients and patients who have a history of renal insufficiency.

[42], [43], [44], [45], [46]

Storage conditions

To maintain the high pharmacodynamic and pharmacokinetic characteristics of the drug in question, it is necessary to very clearly fulfill all storage conditions of Edicyin, since this directly affects the duration of effective drug work.

 The storage conditions of Edicyin are very often found in the instructions for the use of many other drugs, because they are quite standard.

1. The temperature characteristics in the room where Edicyin is stored should not exceed 25 degrees Celsius.
2. The product should not be exposed to direct sunlight.
3. The drug should not be available to small researchers.
4. The medicine must be stored in a room with a lowered moisture index.

[47], [48], [49], [50], [51]

Shelf life

If all the requirements for storing the medicinal preparation of Egilok were met, the expiry date and effective use for therapeutic purposes shall extend for two years (or 24 months) from the date of issue. If at least one of the storage conditions has been violated, the time interval for the effective use of the drug in question is reduced. At the end of the final shelf life, further use of the drug is unacceptable.

[52], [53], [54], [55]