In M, the introduction of benzylpenicillin is 1000,000 units. Bezylpenicillin Sodium Salt Crystal (Benzylpenicillin Sodium Salt Crystallic)

Bezylpenicillin sodium salt is an antibiotic group of biosynthetic penicillins for systemic use that has a bactericidal action.

Release form and composition

Dosage forms:

• powder for preparing a solution for intravenous (in / c) and intramuscular (in / m) administration: white powder with a weak specific smell [1,000,000 units (actions) or 500,000 units in vials, in a cardboard pack 1 or 10 vials for hospitals - in a carton of 50 bottles];
• powder for preparing the solution for in / m and subcutaneous (n / c) administration: white powder with a weak specific smell (1,000,000 units or 500,000 units in 10 ml bottles, in a cardboard pack 1, 5 or 10 bottles, for hospitals - in a carton of 50 bottles);
• powder for the preparation of the injection and local application: white powder with a weak specific smell (1,000,000 units or 500,000 units in bottles of 10 ml, or 20 ml, in a cardboard pack 1, 5 or 10 bottles, for hospitals - in 50 bottles cardboard box).

Each pack also contains instructions for the use of benzylpenicillin sodium salt.

In 1 vial contains a valid substance: benzylpenicillin sodium salt - 500,000 units or 1,000,000 units.

Pharmacological properties

Pharmacodynamics

Bezylpenicillin sodium salt is an antibacterial drug of a group of biosynthetic (natural) penicillins, has a bactericidal effect, the penicillinase is destroyed. The mechanism of the action of its active substance is due to the inhibition of transpeptide and the preventing the formation of peptide bonds. Violating the late stages of the synthesis of peptidoglycan of the cell wall causes lysis of dividing bacterial cells.

Benzylpenicillin shows activity for the following pathogens:

• gram-positive microorganisms: Bacillus Anthracis, Streptococcus Speciales (SPP.) (including Streptococcus Pneumoniae), Staphylococcus SPP. (not forming penicillinase), Corynebacterium SPP. (including Corynebacterium Diphtheriae), Actinomyces SPP.;
• gram-negative microorganisms: Neisseria Meningitidis, Neisseria Gonorrhoeae, Treponema SPP., SPIROCHAETES class.

Resistance to benzylpenicillin sodium salts show microorganisms producing penicillinase: Staphylococcus SPP., Most viruses, gram-negative bacteria, including Pseudomonas Aeruginosa, Rickettsia SPP., Simplest.

In recent years, the sensitivity to benzylpenicillin hemolytic streptococcal, gonococcal, staphylococci and pneumococci changes.

Pharmacokinetics

After the introduction of the introduction, the maximum concentration of benzylpenicillin in the blood plasma is achieved in approximately 0.5 hours.

Bonding with plasma proteins is 60%.

Benzylpenicillin penetrates through a placental barrier, with inflammation of meningeal shells - overcomes the hematorencephalic barrier. Widely distributed in the tissues, organs and body fluids (except for fabrics of the eye, liquor and prostate gland).

Examined through the kidneys unchanged. Half-life (T 1/2) 0.5-1 hour, with renal failure - from 4 to 10 hours or more.

Indications for use

The use of sodium salt benzylpenicillin is shown to treat the following bacterial infections caused by pecullen sensitive pathogens:

• respiratory tracts and ENT organs (ear, throat, nose): angina, bronchitis, community-hospital pneumonia, purulent pleurisy, scarlet patter, diphtheria, lung actinomycosis;
• grocery Ways: cholecystitis, cholangitis;
• urinary System: Syphilis, Gonorrhea, Custitis, Colpit, Endometritis, Endocervicitis, SalpingoForit, adnexitis;
• leather and soft fabrics, wound infections: impetigo, face, secondary infected dermatoses;
• animation: conjunctivitis, dacryocystitis, blepharitis;
• cardiovascular system: septic endocarditis;
• bone-muscular system: osteomyelitis;
• central nervous system: meningitis;
• other infections: Siberian ulcers, sepsis, peritonitis, etc.

Contraindications

Absolute:

• breast-feeding;
• increased sensitivity to other penicillins, cephalosporins and benzylpenicillin.

In addition, the endoomumbal administration of the drug to patients with epilepsy is contraindicated.

It is recommended to prescribe benzylpenicillin sodium salt in renal failure, patients with heart failure, diseases of allergic genesis (including drug hypersensitivity, urticule, polynosis, bronchial asthma) and in the case of diagnosed hypersensitivity to β-lactam antibiotics of cephalosporins (due to probable development Cross allergies).

During pregnancy, the use of the drug is possible only in cases where the expected clinical effect for the mother exceeds a potential threat to the fetus.

Bezylpenicillin sodium salt, instructions for use: method and dosage

The finished solution of benzylpenicillin of the sodium salt is introduced into / in (drip or inkidno), in / m, p / k, domesticly (in the abdominal, pleural and other cavities), intrathecal (endolumboral), locally.

Before the first introduction must be verified in the tolerability of the drug and novocaine (if it is used as a solvent). To do this, patients should be carried out intradermal sample.

Prepare a solution of benzylpenicillin sodium salt must be immediately before the administration procedure, depending on the method of application, following the following requirements:

• introduction Solution: As a solvent for the contents of the vial 1,000,000, it requires 5 ml of sterile water for injection or 0.9% sodium chloride solution;
• a solution for drip / in administration: 0.9% sodium solution of chloride or 5% solution of glucose in a volume of 100-200 ml per 2,000,000-5,000,000 units of antibiotic is used as a solvent;
• introduction solution: the contents of the vial are dissolved in sterile water for injection, 0.9% sodium solution of chloride or 0.5% solution, using 1-3 ml of solvent;
• the solution for the introduction of P / K: The powder is dissolved in a 0.25-0.5% removal solution (Novocain), observing the following proportions: 500,000 units require 2.5-5 ml, per 1,000,000 units - 5-10 ml solvent;
• the solution for administering to the cavity of the body: to dissolve the antibiotic when introduced into the abdominal, pleural or other cavity, sterile water for injection or 0.9% solution of sodium chloride is used;
• solution for intrathecal administration: The contents of the vial are dissolved in sterile water for injection or 0.9% solution of sodium chloride in proportion to 1000 units of the active substance - 1 ml of solvent. The resulting solution is mixed with the spinal fluid extracted from the spinal channel (SMF) in equal shares, 5-10 ml of the antibiotic solution is added to 5-10 ml of SMF;
• eye drops [prepare Ex Tempore (as needed)]: Sterile water for injection of 5-25 ml per 500,000 units or a 0.9% sodium solution of chloride is added to the vial of 5-25 ml per 5-50 ml sodium solution for 1,000,000;
• drops in the nose and ear drops: Sterile water for injection of 5-50 ml per 500,000 units or 0.9% solution of sodium chloride is added to the contents of 5-50 ml of 10-100 ml sodium solution per 1,000,000 units.

The solution can be introduced in / in the solution slowly for 3-5 minutes or drip, at a speed of 60-80 drops in 1 minute.

The injection is produced in the upper outer square of the buttocks deep into the muscle.

Intrathectly benzylpenicillin sodium salt should be administered at a speed of 1 ml per minute.

• iN / V / M Introduction: Adults - 250,000-500 000 € 4-6 times a day for the treatment of medium severity infections. The daily dose of the drug in severe infections can be from 10,000,000 to 20,000,000 units, with gas gangrene - up to 40,000,000-60,000,000. The daose dose for children is determined taking into account the weight of the child: under the age of 1 year - 50,000-100,000 units per 1 kg of the child's weight, older than 1 year - 50,000 units per 1 kg. If necessary, it can be increased to 200,000-300,000 units per 1 kg of body weight, and according to life indicators and up to 500,000 units per 1 kg. The daily dose is divided by 4-6 administrations. V / in benzylpenicillin sodium salt is usually administered 1-2 times a day, the remaining part of the daily dose is introduced in / m;
• introduction P / K: In the form of gluing infiltrates with a solution with a concentration of 100,000-200,000 units per 1 ml of 0.25-0.5% solution of the procaine;
• introduction to the body cavity: adults - a concentration of a solution of 10,000-20,000 units in 1 ml of solvent, children - 2000-5000 units of 1 ml. The duration of treatment is 5-7 days. Then the patient is translated on the introduction of benzylpenicillin sodium salt;
• intrathectly (endoomumbo) with purulent diseases of the brain shells, head and spinal cord: adults - in a daily dose of 5000-10,000 units, children over the age of 1 year - 2000-5000 units, 1 time per day for 2-3 days, further the patient is transferred to the introduction;
• locally (only powder for the preparation of solution for injection and local application): eye diseases - instillation 1-2 cap 6-8 times a day of eye drops containing 20,000-100,000 units in 1 ml of sterile naCl solution 0.9% or distilled water; The solution is used freshly prepared. Ear or nose diseases - instillation of 1-2 drops 6-8 times a day of freshly prepared drops containing 10,000-100,000 units in 1 ml of sterile solution NaCl 0.9% or distilled water.

The duration of the treatment of benzylpenicillin sodium salt The doctor establishes individually taking into account the shape and severity of the disease. The course can be 7-10 days, and with sepsis, septic endocarditis and other heavy pathologies up to 60 days or more.

During syphilis and gonor, the treatment is carried out on a specially developed scheme.

Side effects

• from the immune system: the reaction of hypersensitivity in the form of skin rash, itching, urticaria, fever, chills, edema, arthralgia, exfoliative dermatitis, multiforous exudative erythema, angioedema edema (swelling of quinque), anaphylactic shock (including injecting administration of benzylпenicillin sodium salts, with fatal outcome);
• from the nervous system: noise in the ears, headache, dizziness; In the endolumbal administration, neurotoxicosis is possible (nausea, vomiting, convulsions, symptoms of meningism), coma;
• from the cardiovascular system: violation of the pump function of myocardium, blood pressure fluctuations;
• from the lymphatic system and blood: leukopenia, thrombocytopenia, hemolytic anemia, eosinophilia, agranulocytosis, positive results of the Cumbas test;
• from the digestive system: Candidiasis of the oral cavity, stomatitis, nausea, diarrhea, glossitis, pseudomembrane colitis, functional liver disorders;
• from the urogenital system: candidiasis of the vagina, interstitial jade;
• by respiratory authorities: bronchospasm;
• reactions at the injection site: soreness and sealing at a / m application; In the case of a suspension to enter the introduction into the vascular bed - violation, dizziness, the noise in the ears, the feeling of fear, a short-term loss of consciousness.

Overdose

• symptoms: nausea, vomiting, reflex arousal, headache, Malgy, arthralgia, cramps, symptoms of meningism, coma. Toxic effect on the central nervous system more often occurs during endolumbal administration;
• treatment: Immediate termination of the use of the drug, the purpose of symptomatic therapy.

special instructions

The purpose of the benzylpenicillin sodium salt is shown only in pathologies caused by microorganisms sensitive to the drug. When developing, the resistance of benzylpenicillin should be replaced by another antibiotic.

If the clinical effect is missing after 3-5 days of the drug, correction / replacement of the treatment regimen is necessary. In this case, it is possible to additional appointment of other antibiotics or synthetic chemotherapeutic agents, or the translation of the patient to receive a new antibiotic. The probability of developing adverse reactions and the degree of their severity may increase.

When conducting a test on hypersensitivity, the patient must be under the supervision of medical staff for 0.5 hours. In the event of symptoms of allergic reactions to benzylpenicillin, sodium salt, it should be canceled and appointed appropriate treatment, including epinephrine, antihistamines, corticosteroids. It should be taken into account that patients with hypersensitivity to cephalosporins in history against the background of the drug may appear cross-allergies.

The long-term use of benzylpenicillin is required to accompany the regular control of the function of the kidney function, electrolyte balance and blood formula.

The use of subterapeutic doses of benzylpenicillin or premature cancellation of the drug often causes the appearance of resistant strains of pathogens.

In case of a patient, heavy diarrhea occurs during the diagnosis of its reason, it is necessary to take into account the risk of development in a patient of pseudomembranous colitis. Therefore, the introduction of benzylpenicillin sodium salt is recommended to be canceled.

In order to prevent the development of fungal superinfection, it is advisable to simultaneously appoint antifungal agents.

When mixing benzylpenicillin with PRAMIN, it is possible to clouding a solution that admits the introduction of the drug.

Application during pregnancy and lactation

The use of the drug with breastfeeding is contraindicated.

During the period of tooling, the use of benzylpenicilline sodium salt is allowed only in cases where the expected clinical effect for the mother, according to the doctor, exceeds a potential threat to the fetus.

If you need to appoint an antibiotic during lactation, breastfeeding is required to stop.

Childcare

In pediatric practice of benzylpenicillin, sodium salt is used according to indications in compliance with the recommended dosing mode.

Breast-age children should prescribe a drug with caution.

With violations of the kidney function

With extreme caution, the benzylpenicilline sodium salt for the treatment of patients with renal failure should be used.

Medicinal interaction

The combination of benzylpenicillin sodium salt with aminoglycosides, macrolides, sulfanilamine means arises synergism of action.

Ingravation of benzylpenicillin activity cause beta-lactamase inhibitors.

With the simultaneous use of other bacteriostatic drugs (including chloramphenicol), the therapeutic effect of the drug is reduced.

With concomitant therapy with non-steroidal anti-inflammatory means (NSAIDs), diuretics, channel secretion blockers, allopurinol increases T1 / 2 benzylпenicillin, increases its blood plasma concentration and toxic risk. In addition, allopurinol increases the risk of developing skin rash.

Combine benzylpenicillin sodium salt with NSAIDs, ethinyl estradiol is not recommended. It is possible to reduce the contraceptive effect of oral contraceptives.

Against the background of the use of benzylпenicillin, the effect of indirect anticoagulants increases, the clearance is reduced and the toxicity of methotrexate increases.

Store at temperatures from 15 to 25 ° C in the place protected from moisture.

Shelf life - 3 years.

The active ingredient: 500000 DF - 0.3 g or 1000000 DF - 0.6 g of benzylpenicillin sodium salt.

Biosynthetic penicillin antibiotic.

Pharmacodynamics. Penicillin antibiotic biosynthetic from the group of penicillins, active against gram-positive bacteria (Staphylococcus spp., Streptococcus spp, Corynebacterium diphtheriae, anaerobic spore-forming rods, sticks), and against Spirochaetaceae, Gram negative cocci (Neisseria gonorrhoeae, N.meningitidis), Actinomycetaceae.

Resistant to the action of benzylpenicillin stamps of staphylococci, forming penicillinase, since this enzyme destroys the benzylpenicillin molecule. The drug is not active with respect to most gram-negative bacteria, Rickettsia (Rickettsia SPP.), Viruses, simplest.

Pharmacokinetics. Benzylpenicillin is well absorbed in parenteral administration, does not have a cumulative action, quickly derived from the body with urine. With intramuscular administration, the maximum concentrations of the drug in the blood are created after 30-60 minutes, after 3-4 hours in the blood traces of the antibiotic are detected.

The level of concentrations and the duration of the circulation of benzylpenicillin in the blood depends on the value of the dose administered.

The antibiotic penetrates well into the tissue and fluid of the body: in the spinal fluid, the norm is found in a small amount, with inflammation of the meninglic shells, its concentration in the liquor increases.

Bacterial infections caused by sensitive pathogens: a bruboral and focused, Empiama pleura ,; Septic (acute and subacute), purulent infections of the skin, soft tissues and mucous membranes (including, secondly infected dermatoses), purulent, ENT infections (aneg), gas, Siberian ulcers, lungs, urine and biliary infections ways, treatment of purulent-inflammatory diseases in obstetric and gynecological practice, eye disease (incl. sharp gonococcal, Gonoblenory).

The drug is injected intramuscularly, in the cavity (abdominal, pleural, etc.) or subcutaneously. In the cavity, the drug is administered only in the conditions of the hospital!

Intramuscularly: in the agent infections, the one-time dose of the drug is usually 250000-500000; Daily - 1000000-2000000; With severe infections, up to 10,000,000-200,000 units per day; With gas gangrene - up to 40,000,000-60,000,000 units.

The daily dose for children under the age of 1 is 50,000-100,000 units / kg, older than 1 year - 50,000 units / kg; If necessary, the daily dose can be increased to 200,000-300,000 units / kg, according to life indications - up to 500,000 units / kg. The multiplicity of drug administration is 4-6 times a day.

For intramuscular administration, 1-3 ml of sterile water for injection or 0.9% solution of sodium chloride, or 0.5% solution of the procaine is added to the contents of the vial.

Subcutaneously, the drug is used to glue infiltrates at a concentration of 100,000-200000 units in 1 ml of 0.25-0.5% solution of the procaine.

In the cavity (abdominal, pleural, etc.) The solution of the drug adult is administered at a concentration of 10,000-20,000 units in 1 ml, children - 2,000-5,000 units in 1 ml. Dissolve in sterile water for injection or 0.9% solution of sodium chloride. The duration of treatment is 5-7 days later, followed by the transition to intramuscular administration.

Application during pregnancy and in breastfeeding period. Application during pregnancy is possible only when the estimated benefits exceeds the potential risk to the fetus. If you need to use during the lactation period, it is necessary to resolve the issue of cessation of breastfeeding.

If after 3-5 days after the start of the use of the effect, it is not noted, it is necessary to proceed to the use of other antibiotics or combined therapy.

In connection with the possibility of the development of fungal superinfection, it is advisable for long-term treatment with benzylpenicillin, if necessary, prescribe antifungal drugs.

It should be borne in mind that the use of insufficient doses of benzylpenicillin or too early cessation of treatment often leads to the emergence of resistant strains of pathogens.

During the administration of the drug, caution should be taken when driving vehicles, mechanisms and when performing other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

At the beginning of the course of treatment (especially in the treatment of congenital syphilis) - fever, increased sweating, aggravation of the disease, the reaction of Yarisha-Gersheimer.
From the cardiovascular reaction: reduction of the pump function of myocardium.

Local reactions: soreness and sealing in place in / m administration.

With long-term use: dysbacteriosis, the development of superinfection.

In the endolumbal administration - neurotoxic reactions:, increasing reflex excitability, meningeal symptoms, coma.

The probenecide reduces the channel secretion of benzylpenicillin, thereby increasing the concentration of the latter in the blood plasma, the half-life increases.

With simultaneous use with antibiotics that have a bacteriostatic action (macrolides, chlorazphenicol, lincoosamide, tetracycline), the bactericidal effect of benzylпenicillin decreases.

Increases the efficiency of indirect anticoagulants (suppressing the intestinal microflora, reduces the prothrombin index); Reduces the effectiveness of oral contraceptives, drugs, in the process of metabolism of which para-aminobenzoic acid is formed, ethinyl estradiol - the risk of developing the "breakthrough" bleeding.

Diuretics, Allopurinol, Kanalis secretion blockers, phenylbutazone, non-steroidal anti-inflammatory drugs, reducing the tubular secretion, increase the concentration of benzylпenicillin.

Allopurinol increases the risk of developing allergic reactions (skin rash).

Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergide effect.

Increased sensitivity to benzylpenicillin and other preparations from a group of penicillins and cephalosporins, the lactition period.

Carefully. Pregnancy, lactation period, severe, allergic diseases (including,).

Symptoms: cramps, violation of consciousness.

Treatment: cancellation of the drug, symptomatic therapy.