RU2274446C2 - Agent for topical injection chemoanesthesia - Google Patents

Abstract

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to therapy of topical suppurative-inflammatory processes. Agent represents an aqueous isoosmotic solution comprising 0.25% of novocaine, 1% of cefazolin sodium salt and 0.77% of sodium chloride. Invention provides the development of optimal conditions for safety mechanical moving of agent in intercellular space under positive hydrodynamic pressure in the permanent state from the injection point in direction to side of deeply localized pathological focus and eliminates the pain component of the inflammatory response.

EFFECT: valuable medicinal properties of agent.

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Description

The invention relates to medicine, in particular to analgesic therapy of local infectious processes, and can be used in the treatment of acute purulent-inflammatory processes in the uterus.

Known tool (Mashkovsky MD Medicines. A manual for doctors. T.1. 14th ed. M .: New wave. - 2000. P.293) for infiltration anesthesia according to the method of A. V. Vishnevsky (tight creeping infiltration) - 500-1000 ml of 0.125-0.250% solution of novocaine (procaine hydrochloride), to which a solution of adrenaline hydrochloride (0.1%) is added 1 drop per 2 - 5-10 ml of novocaine solution.

However, such an agent cannot have a bacteriostatic effect on the population of pathogenic microorganisms, since it does not contain a chemotherapeutic agent, therefore, local anesthesia by creeping tissue infiltration when 500-1000 ml of solution is introduced into them under increased hydrodynamic pressure does not provide an antimicrobial effect. Moreover, this solution increases the volume of tissues, dilutes intercellular fluid, blood and lymph, and thus leads to a decrease in the concentration of immunoglobulins and other molecular and cellular components of the body's defense system, which reduces the effectiveness of the antimicrobial effect of the latter.

Injection of 500-1000 ml of 0.125-0.250% solution of novocaine into the body leads to the introduction of up to 2.5 grams of novocaine into the body, which increases the likelihood of developing a resorptive effect of local anesthetic, side effects and complications.

In addition, the osmotic activity of the indicated solution of novocaine before and after adding a few drops of a solution of adrenaline hydrochloride to it remains 8-9 times lower than the isosmotic level (280-290 mOsmol / l of water) due to the low osmotic activity of these agents in the indicated concentrations. Therefore, because of its hypoosmoticity, this agent does not correspond to the physicochemical state of plasma, lymph, and other normal intercellular fluid and, therefore, is potentially dangerous for the patient’s body cells at the injection sites, since the cells swell under the influence of the hypoosmotic solution and the tissues swell. In turn, excessive hydration and swelling of cells and tissues can lead to damage and easier vulnerability to pathogenic microorganisms, which leads to additional tissue damage.

A drug is known (State Register of Medicines. T.2. Typical Clinical and Pharmacological Articles. M. 2000. S.81-82) containing benzylpenicillin sodium or potassium salt, 100000-200000 units of which are dissolved in 1 ml of 0.25- 0.5% solution of novocaine. It is administered subcutaneously for chipping off the infiltrate.

However, such a tool cannot be introduced into other organs and tissues that require a large volume of solution. In particular, due to the presence of an excessively high concentration of a chemotherapeutic agent in it, it cannot be introduced into fiber located in confined spaces. Moreover, the chemotherapeutic agent itself, in spite of this and for this reason, does not have an antimicrobial effect in deep tissues, far from the injection site under the skin due to the hyperosmoticity of the solution, since a solution of 0.25-0.5% novocaine solution having 1 ml osmotic activity within 33-66 mOsm / l of water, 10-20 grams of benzylpenicillin sodium or potassium salt increases the osmotic pressure of the solution by an additional 440-880 mOsm / l of water. Therefore, this tool cannot be used for local chemoanesthesia by injecting several tens of milliliters by tight creeping infiltration of various body tissues.

Therefore, because of its hyperosmoticity, this agent does not correspond to the physicochemical state of plasma, lymph, and other normal biological body fluids and, therefore, is potentially dangerous for our body cells at injection sites and even for blood cells inside a syringe where a drop of blood enters before injecting the solution into a vein to control the localization of the location of the end of the needle. Cells (in particular, red blood cells, white blood cells and lymphocytes) are wrinkled under the influence of a hyperosmotic solution. Excessive dehydration can lead to their reversible and irreversible damage, to a decrease in functional activity, which reduces the effectiveness of the struggle of white blood cells with microorganisms.

In addition, the injection of 100 ml of a solution of this drug leads to the introduction of up to 20,000,000 UNITS of benzylpenicillin sodium or potassium salt, that is, in fact the maximum allowable daily dose of the antibiotic. Injection of such high doses of benzylpenicillin increases the likelihood of side effects and complications, in particular, excitability, symptoms of meningism, convulsions, and coma may appear.

The goal is achieved in that the agent for local injection chemoanesthesia, containing novocaine, a betalactam antibiotic and water, additionally contains sodium chloride, and cefazolin sodium salt as an antibiotic in the following ratio, wt.%:

Novocaine 0.25 Cefazolin sodium 1.00 Sodium chloride 0.77 Water for injection Rest.

The use of novocaine in a concentration of 0.25% allows the solution to be administered by injection in a volume of up to 100 ml, not reaching the maximum permissible doses, reducing toxicity, the severity of the resorptive effect and the likelihood of side effects, but maintaining a high local anesthetic activity.

The use of cefazolin in the form of sodium salt ensures high safety of the drug with its local effect on body tissues, allows for a pronounced local antimicrobial effect due to the more pronounced antimicrobial properties inherent to cefazolin, and also because this antibiotic has a wide spectrum of antimicrobial action. In addition, the use of cefazolin sodium salt reduces the likelihood of allergic reactions. The use of this antibiotic in a concentration of 1% allows you to enter solutions with a volume of up to 100 ml, not reaching the maximum permissible doses, thus minimizing the resorptive effect, toxicity and the likelihood of side effects, as well as their severity.

The introduction of additional sodium chloride at a concentration of 0.77% allows you to raise the osmotic activity of the solution to the level of isosmoticity, namely, up to 280-290 mOsm / l of water, that is, bring this physicochemical indicator of the drug in full compliance with the level of osmotic activity of blood, lymph other body fluids.

In this regard, the injection of this agent into the body tissue creates the best conditions for realizing the task of mechanically promoting it in the intercellular space under positive hydrodynamic pressure without changing the cell volume due to the lack of dehydrating and hydrating activity. Therefore, this agent does not have an osmotic damaging effect on cells and tissues, it moves easier and further unchanged from the injection site towards a deep lying pathological focus, it well removes the pain component of the inflammatory reaction (possessing the properties of a local anesthetic), and has a pronounced and effective antimicrobial effect ( possessing the properties of the bactericidal action of a broad-spectrum antibiotic), does not change the osmotic state of the blood after absorption, therefore, it increases the effective the treatment of local purulent-inflammatory processes, reduces a single, daily and course dose of the administered antibiotic and novocaine, reduces the likelihood and severity of the development of local and general side effects, including allergic reactions, increases the safety of the drug in patients with diabetes mellitus, as well as during intravenous anesthesia , since it allows to avoid aggravation of hypo- or hyperosmotic coma. Using the tool reduces the frequency of surgical interventions, reduces the duration and cost of treatment.

Example 1. Patient K., 23 years old and weighing 49 kg, admitted to the gynecological department with a diagnosis of Acute right-sided pyosalpinx, pelvioperitonitis, was prescribed daily injections of 80 ml of a solution of 0.25% novocaine, each 1 ml of which contained 200,000 units of benzylpenicillin sodium salt (single dose of 16000000 IU of benzylpenicillin sodium salt), under the aponeurosis of the external oblique muscle of the abdomen in the middle third of the inguinal canal on both sides. In this case, the total volume of this solution was divided as follows: 60 ml was administered on the right and 20 ml on the left. However, within 0.5 hours after the injection of the first daily dose, the patient had such side effects as headache, nausea, vomiting and fever. Due to the appearance of these side effects, the drug was canceled. From the next day of hospitalization under the aponeurosis of the external oblique muscles of the abdomen in the middle third of the inguinal canal, injections of an agent containing 0.25% novocaine, 1% cefazolin sodium salt and 0.77% sodium chloride were prescribed. Moreover, 60 ml injections were prescribed on the right, and 20 ml of the indicated chemoanesthesia agent on the left. These injections were performed daily for 5 consecutive days. On the 5th day the pain syndrome completely disappeared, the body temperature returned to normal, the pyosalpinx resolved, the functional and laboratory health indicators returned to normal. The patient was discharged in satisfactory condition, avoiding surgical treatment.

Example 2. Patient B., 19 years old, weighing 54 kg, was admitted to the gynecological department with a diagnosis of "Left-sided abscess of Douglas space, pelvic peritonitis." For the purpose of treatment, daily injections of 100 ml of a solution of 0.25% novocaine, each 1 ml of which contained 200,000 units of benzylpenicillin sodium salt (single dose of 20,000,000 units of benzylpenicillin sodium salt), under the aponeurosis of the external oblique muscle of the abdomen in the middle third of the inguinal canal on both sides were prescribed. . At the same time, the total volume of this solution was divided as follows: on the right, 80 ml was prescribed, and on the left - 20 ml. Course therapy for 4 consecutive days did not lead to a clinical improvement in the patient’s health status and normalization of the functional and laboratory indicators of her health. In this regard, the drug was canceled and under the aponeurosis of the external oblique muscles of the abdomen in the middle third of the inguinal canal, injections of the drug containing 0.25% novocaine, 1% cefazolin sodium salt and 0.77% sodium chloride were prescribed. In this case, 80 ml injections were prescribed on the right, and 20 ml of the indicated chemoanesthesia agent on the left. These injections were performed daily for 6 consecutive days. On the 3rd day, the pain syndrome significantly decreased, body temperature returned to normal, the purulent-inflammatory focus resolved on the 4th day and the pain syndrome completely disappeared, on the 7th day the functional and laboratory health indicators returned to normal. The patient was discharged in satisfactory condition, avoiding surgical treatment.

Claims (1)

An agent for local injection chemoanesthesia containing novocaine, a beta-lactam antibiotic and water, characterized in that it additionally contains sodium chloride, and as a beta-lactam antibiotic - cefazolin sodium salt in the following ratio, wt.%: Novocaine 0.25 Cefazolin sodium 1.00 Sodium chloride 0.77 Water for injection Rest