Benzylpenicillin - drugs (sodium salt, potassium salt, novocaine salt, benzathine benzylpenicillin, etc.), action, instructions for use (how to dilute, dosages, methods of administration), analogues, reviews, price. Benzylpenicillin sodium salt: inst
for medical use
medicinal product
Benzylpenicillin SODIUM SALT
Tradename
Benzylpenicillin sodium salt
International non-proprietary name
Benzylpenicillin
Dosage form
Powder for the preparation of a solution for intramuscular injection 1000000 units
Ingredients per bottle
active substance: benzylpenicillin sodium salt - 1000000 IU
Description
White powder or white powder with a slightly yellowish tint, prone to clumping, forming a stable suspension when water is added.
Pharmacotherapeutic group
Antibacterial drugs for systemic use. Penicillins penicillinase sensitive
ATC code J01SE01
Pharmacological properties
Pharmacokinetics
The maximum concentration in blood plasma when administered intramuscularly is reached after 20-30 minutes. The half-life of the drug is 30-60 minutes, with kidney failure 4-10 hours or more. Communication with plasma proteins - 60%. Penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, eye tissues and prostate. With inflammation of the meningeal membranes, it penetrates the blood-brain barrier. Crosses the placenta and enters breast milk. Excreted by the kidneys unchanged.
Pharmacodynamics
Bactericidal antibiotic from the group of biosynthetic ("natural") penicillins. Inhibits the synthesis of the cell wall of microorganisms. Active against gram-positive pathogens: staphylococci (non-forming penicillinase), streptococci, pneumococci, diphtheria corynebacteria, anaerobic spore-forming rods, anthrax rods, Actinomyces spp .; gram-negative microorganisms: cocci (Neisseria gonorrhoeae, Neisseria meningitidis), as well as against spirochetes.
Not active against most gram-negative bacteria (including Pseudomonas aeruginosa), Rickettsia spp., protozoa. Staphylococcus spp., which produce penicillinase, are resistant to the drug.
Indications for use
Croupous and focal pneumonia, pleural empyema, bronchitis
Sepsis, septic endocarditis (acute and subacute)
Peritonitis
Meningitis
Osteomyelitis
Pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, blennorrhea, syphilis, cervicitis
Cholangitis, cholecystitis
wound infection
Erysipelas, impetigo, secondarily infected dermatoses
Diphtheria
Scarlet fever
anthrax
Actinomycosis
Sinusitis, otitis media
Purulent conjunctivitis
Mode of application and doses
Benzylpenicillin sodium salt is administered intramuscularly. When administered intramuscularly, single doses in the moderate course of the disease (infections of the upper and lower respiratory tract, urinary and biliary tract, soft tissue infections, etc.) is 250,000 - 500,000 IU 4-6 times a day. In severe infections (sepsis, septic endocarditis, meningitis, etc.) - 10-20 million units per day; with gas gangrene - up to 40-60 million units.
Daily dose for children under the age of 1 year - 50,000 - 100,000 IU / kg, over 1 year - 50,000 IU / kg; if necessary - 200,000 - 300,000 U / kg, according to vital indications - an increase to 500,000 U / kg. Frequency rate of introduction - 4-6 times a day.
A solution of the drug for intramuscular administration is prepared immediately before administration by adding 1-3 ml of water for injection, 0.9% sodium chloride solution or 0.5% procaine (novocaine) solution to the contents of the vial. When dissolving benzylpenicillin in a solution of procaine, turbidity of the solution may occur due to the formation of crystals of benzylpenicillin procaine, which is not an obstacle to intramuscular administration of the drug. The resulting solution is injected deep into the muscle. The duration of treatment, depending on the severity of the disease, is from 7 to 10 days.
Side effects
Violation of the pumping function of the myocardium, arrhythmias, cardiac arrest, chronic heart failure (since hypernatremia may occur with the introduction of large doses)
Nausea, vomiting, stomatitis, glossitis, abnormal liver function
Impaired kidney function
Anemia, leukopenia, thrombocytopenia
Increased reflex excitability, meningeal symptoms, convulsions, coma
- allergic reactions: sometimes - hyperthermia, urticaria, skin rash, fever, chills, increased sweating, rash on mucous membranes, arthralgia, eosinophilia, angioedema, interstitial nephritis, bronchospasm, rarely - anaphylactic shock
- local reactions: soreness and induration at the site of intramuscular injection
Dysbacteriosis, development of superinfection (with prolonged use)
Contraindications
Hypersensitivity to penicillin and other ß-lactam antibiotics
Endolumbar injection in epilepsy.
Drug Interactions
Antacids, glucosamine, laxatives, aminoglycosides slow down and reduce the absorption of benzylpenicillin sodium salt. Ascorbic acid, when used together, increases the absorption of benzylpenicillin sodium salt.
Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Benzylpenicillin sodium salt increases the effectiveness of indirect anticoagulants (suppressing intestinal microflora, reduces the prothrombin index); reduces the effectiveness of oral contraceptives, medicines, during the metabolism of which para-aminobenzoic acid is formed.
Diuretics, allopurinol, blockers of tubular secretion, phenylbutazone, non-steroidal anti-inflammatory drugs, reducing tubular secretion, increase the concentration of benzylpenicillin sodium salt.
Allopurinol increases the risk of developing allergic reactions (skin rash).
Carefully: pregnancy, lactation, allergic diseases (bronchial asthma, hay fever), kidney failure.
Solutions of the drug are prepared immediately before administration. If after 2-3 days (maximum 5 days) after the start of the drug, there is no effect, you should switch to the use of other antibiotics or combination therapy. In connection with the possibility of developing fungal infections, it is advisable for long-term treatment benzylpenicillin to prescribe vitamins of group B, and if necessary - antifungal drugs. It should be borne in mind that the use of insufficient doses of the drug or too early termination of treatment often leads to the emergence of resistant strains of pathogens.
Pregnancy and lactation
The use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. If necessary, the appointment of the drug during lactation should stop breastfeeding.
Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
During the administration of the drug, care should be taken when administering vehicles, mechanisms and when performing other potentially dangerous species activities that require increased concentration of attention and speed of psychomotor reactions.
Overdose
Natural antibiotic of the penicillin group. Acid-resistant, destroyed by beta-lactamase (penicillinase).
In medical practice, benzylpenicillin sodium, potassium and novocaine salt are used.
White fine-crystalline powder of bitter taste. Slightly hygroscopic. Very easily soluble in water, soluble in ethanol and methanol. Easily destroyed by acids, alkalis and oxidizing agents. Enter in / m, in / in, s / c, endolumbally, intratracheally.
Benzylpenicillin potassium salt is a white fine crystalline powder of bitter taste. Hygroscopic. Very easily soluble in water, soluble in ethanol and methanol. Easily destroyed by acids, alkalis, oxidizing agents. Enter in / m, p / c.
Benzylpenicillin novocaine salt is a white, odorless, finely crystalline powder, bitter in taste. Hygroscopic. Slightly soluble in water, ethanol and methanol. We will hardly dissolve in chloroform. Forms a thin suspension with water. Resistant to light. Easily destroyed by the action of acids and alkalis. Enter only in / m.
Indications for use
Treatment of diseases caused by microorganisms sensitive to benzylpenicillin: lobar and focal pneumonia, pleural empyema, sepsis, septicemia, pyemia, acute and subacute septic endocarditis, meningitis, acute and chronic osteomyelitis, infections of the urinary and biliary tract, tonsillitis, purulent infections of the skin, soft tissues and mucous membranes, erysipelas, diphtheria, scarlet fever, anthrax, actinomycosis, treatment of pyoinflammatory diseases in obstetric and gynecological practice, ENT diseases, eye diseases, gonorrhea, blennorrhea, syphilis.
Release form
Benzylpenicillin sodium salt
cooking powder injection solution for intramuscular injection 500 thousand units; vial (vial)
Benzylpenicillin sodium salt
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 250 thousand units; bottle (bottle) box (box) 50
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 500 thousand units; bottle (bottle) carton pack 1
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 500 thousand units; vial (vial) carton pack 5
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 500 thousand units; vial (vial) carton pack 10
Benzylpenicillin sodium salt
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; bottle (bottle) carton pack 1
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; vial (vial) carton pack 5
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; vial (vial) carton pack 10
Benzylpenicillin sodium salt
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; bottle (bottle) box (box) cardboard 50
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 500 thousand units; bottle (bottle) box (box) cardboard 50
Benzylpenicillin sodium salt
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; bottle (bottle) box (box) cardboard 50
Benzylpenicillin sodium salt
0
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; bottle (bottle) box (box) cardboard 50
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; bottle (bottle) box (box) cardboard 1
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; bottle (bottle) box (box) cardboard 50
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; bottle (bottle) box (box) cardboard 1
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 1 million units; vial (vial)
Benzylpenicillin sodium salt
powder for the preparation of an injection solution for intramuscular injection 250 thousand units; vial (vial)
Pharmacodynamics
Antibiotic of the biosynthetic penicillin group. It has a bactericidal effect by inhibiting the synthesis of the cell wall of microorganisms.
Active against gram-positive bacteria: Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis; gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis; anaerobic spore-forming rods; as well as Actinomyces spp., Spirochaetaceae.
The strains of Staphylococcus spp., which produce penicillinase, are resistant to the action of benzylpenicillin. Decomposes in an acidic environment.
Novocaine salt of benzylpenicillin compared with potassium and sodium salts is characterized by a longer duration of action.
Pharmacokinetics
After i / m administration, it is rapidly absorbed from the injection site. Widely distributed in tissues and body fluids. Benzylpenicillin penetrates well through the placental barrier, the BBB during inflammation of the meninges.
T1/2 - 30 min. Excreted with urine.
Use during pregnancy
Use during pregnancy is possible only if the expected benefit of therapy for the mother outweighs the potential risk to the fetus.
If necessary, use during lactation should decide on the termination of breastfeeding.
Other special occasions when taking
Bronchial asthma, pollinosis, renal failure.
Contraindications for use
Hypersensitivity to benzylpenicillin and other drugs from the group of penicillins and cephalosporins. Endolumbar administration is contraindicated in patients suffering from epilepsy.
Side effects
From the side digestive system: diarrhea, nausea, vomiting.
Effects due to chemotherapeutic action: vaginal candidiasis, oral candidiasis.
From the side of the central nervous system: when using benzylpenicillin in high doses, especially with endolumbar administration, neurotoxic reactions may develop: nausea, vomiting, increased reflex excitability, symptoms of meningism, convulsions, coma.
Allergic reactions: fever, urticaria, skin rash, rash on mucous membranes, joint pain, eosinophilia, angioedema. Cases are described anaphylactic shock with a lethal outcome.
Dosage and administration
In / m, in / in (except novocaine salt of benzylpenicillin), s / c, endolumbally (only sodium salt of benzylpenicillin), in the cavity, intratracheally; in ophthalmology - instillations into the conjunctival sac, subconjunctival, intravitreal.
With the / m and / in the introduction: for adults - 2-12 million IU / day in 4-6 injections; with community-acquired pneumonia - 8-12 million units / day in 4-6 injections; with meningitis, endocarditis, gas gangrene - in / in 18-24 million units / day in 6 injections.
The duration of treatment with benzylpenicillin, depending on the form and severity of the disease, ranges from 7-10 days to 2 months or more (for example, with sepsis, septic endocarditis).
Overdose
Symptoms: convulsions, impaired consciousness.
Treatment: drug withdrawal, symptomatic therapy.
Interactions with other drugs
Probenecid reduces the tubular secretion of benzylpenicillin, resulting in an increase in the concentration of the latter in the blood plasma, and an increase in the half-life.
With simultaneous use with antibiotics that have a bacteriostatic effect (tetracycline), the bactericidal effect of benzylpenicillin decreases.
Precautions for use
In / in, endolumbally and into the cavity is administered only in a hospital setting.
It is necessary to use benzylpenicillin preparations only as directed and under medical supervision. It must be remembered that the use of insufficient doses of benzylpenicillin (as well as other antibiotics) or too early termination of treatment often leads to the development of resistant strains of microorganisms. If resistance occurs, treatment with another antibiotic should be continued.
Benzylpenicillin novocaine salt is administered only in / m. In / in and endolumbar introduction is not allowed. Of all benzylpenicillin preparations, only the sodium salt is administered endolumbally.
In bronchial asthma, hay fever and other allergic diseases, benzylpenicillin is used with caution while prescribing antihistamines.
With the development of allergic reactions in patients, the drug should be discontinued. In debilitated patients, newborns, elderly people with long-term treatment, the development of superinfection caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms) is possible. Due to the fact that with long-term oral administration of antibiotics, the intestinal microflora that produces vitamins B1, B6, B12, PP can be suppressed, it is advisable for patients to prescribe vitamins of group B to prevent hypovitaminosis.
If no effect is noted after 2–3 days after the start of the drug (maximum 5 days), it is necessary to switch to treatment with another antibiotic or combination therapy.
Special instructions for admission
Use with caution in patients with impaired renal function, with heart failure, a predisposition to allergic reactions (especially with drug allergy), with hypersensitivity to cephalosporins (due to the possibility of developing cross-allergy).
If after 3-5 days after the start of the application of the effect is not observed, you should switch to the use of other antibiotics or combination therapy.
In connection with the possibility of developing fungal superinfection, it is advisable to prescribe antifungal drugs in the treatment with benzylpenicillin.
It should be borne in mind that the use of benzylpenicillin in subtherapeutic doses or early termination of treatment often leads to the emergence of resistant strains of pathogens.
Storage conditions
List B.: In a dry place, at a temperature not exceeding 20 ° C.
Best before date
Belonging to ATX-classification:
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- Application instruction of Benzylpenicillin sodium salt
- Composition of the drug Benzylpenicillin sodium salt
- Indications for benzylpenicillin sodium salt
- Storage conditions of the drug Benzylpenicillin sodium salt
- Shelf life of the drug Benzylpenicillin sodium salt
ATC code: Antimicrobials for systemic use (J) > Antimicrobials for systemic use (J01) > Beta-lactam antibiotics - penicillins (J01C) > Beta-lactamase sensitive penicillins (J01CE) > Benzylpenicillin (J01CE01)
Release form, composition and packaging
powder for preparation. r-ra d / w / m injection 1 million units: fl. 10 or 50 pcs.Reg. No.: 5115/01/10/15/16 dated 24.08.2015 - Valid
Powder for solution for intramuscular injection white.
1000000 units - bottles (10) - packs of cardboard.
1000000 units - bottles (50) - cardboard boxes.
Description medicinal product Benzylpenicillin SODIUM SALT was created in 2012 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Belarus. Date of update: 07/16/2013
Bactericidal antibiotic from the group of biosynthetic ("natural") penicillins. Inhibits the synthesis of the cell wall of microorganisms. Active towards Gram-positive pathogens:
- staphylococci (not forming penicillinase), streptococci, pneumococci, diphtheria corynebacteria, anaerobic spore-forming rods, anthrax rods, Actinomyces spp .;
- Gram-negative microorganisms: cocci (Neisseria gonorrhoeae, Neisseria meningitidis), as well as against spirochetes. Not active for most Gram-negative bacteria, rickettsiae, viruses, protozoa. To the action of the drug resistant penicillinase-forming strains microorganisms. Decomposes in an acidic environment.
Benzylpenicillin can be used alone, as well as in combination with other bactericidal antibiotics.
Cmax in blood plasma with i / m administration is achieved in 20-30 minutes. T 1/2 of the drug is 30-60 minutes, with renal failure 4-10 hours or more. Communication with plasma proteins - 60%. Penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, eye tissues and prostate. With inflammation of the meningeal membranes, it penetrates the blood-brain barrier. Passes through the placenta and passes into breast milk. Excreted by the kidneys unchanged.
- bacterial infections caused by susceptible pathogens: lobar and focal pneumonia, pleural empyema, bronchitis;
- sepsis, septic endocarditis (acute and subacute), peritonitis;
- meningitis;
- osteomyelitis;
- infections of the genitourinary system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, blennorrhea, syphilis, cervicitis), biliary tract infections (cholangitis, cholecystitis), wound infection, infections of the skin and soft tissues: erysipelas, impetigo, secondarily infected dermatoses;
- diphtheria;
- scarlet fever;
- anthrax;
- actinomycosis;
- ENT diseases, eye diseases.
Dosage and duration of use depend on the indications and severity clinical picture. Treatment should be continued for two days after disappearance clinical symptoms diseases.
Usually the daily dose for children under 12 years old is 50,000 U / kg, for adults - 1,000,000-3,000,000 U / day.
Premature babies and newborns (BT approx. 3.5 kg): 30000-100000 IU/kg/day
Children under 1 year (BT up to 10 kg): 30000-100000 IU/kg/day
Children from 1 to 12 years (BT from 10 to 38 kg): 30000 IU / kg / day.
Adults (BT from 40 kg and above): 1000000-5000000 IU/day
Special cases of dosage:
- in the presence of sensitive microorganisms, adults receive 20000000-80000000 IU / day.
Sepsis caused by gram-negative pathogens(Escherichia coli, Enterobacter aerogenes, Alcaligenes faecalis, Salmonellae, Shigellae and Proteus mirabilis:
Bacterial endocarditis: in the presence of sensitive microorganisms, adults receive 10,000,000-80,000,000 IU / day / in combination with 120-240 mg of gentamicin per day or 1-2 g of streptomycin per day / m.
Meningitis: due to an increased tendency to convulsive reactions, adults should not prescribe the drug in doses exceeding 20000000-30000000 IU / day, and children - no more than 12000000 IU / day.
Sick with streptococcal infection treatment should be carried out for at least 10 days.
Congenital syphilis: 50000 IU/kg/day for 10-14 days.
Prevention of diphtheria:
- 300000-600000 IU/day
Neurosyphilis: 2400000 IU / day for 10-14 days in combination with probenecid.
Acute uncomplicated gonorrhea: single dose for both men and women 4500000 IU.
Chronic complicated gonorrhea: daily dose of 3,000,000 units for 5-7 days for both men and women.
Dissolve the contents of the vial in 5-8 ml of water for injection; shake well before use to mix; enter by deep intramuscular injection into the upper outer square of the gluteal muscle or into the upper gluteal field according to the Hochstetter method; with repeated injections, change the injection site.
Sodium salt of benzylpenicillin 500,000 IU 3-6 times / day.
In patients with severe degrees of hepatic and/or renal insufficiency it is desirable to specify single doses or intervals between doses in terms of creatinine clearance.
Dosage based on creatinine clearance:
From the gastrointestinal tract: stomatitis and glossitis are occasionally noted. Nausea, vomiting. Antibiotic-induced diarrhea should raise suspicion for pseudomembranous colitis (possibility of emergence of resistant organisms or fungi) and further treatment should be specific to the causative organism. When superinfection occurs, appropriate measures should be taken.
Allergic: due attention should be given side effects, namely anaphylaxis, urticaria, fever, joint pain, angioedema, erythema multiforme and exfoliative dermatitis.
Due to bacteriolysis, in infections caused by endotoxin-producing bacteria such as salmonella, leptospira or treponema (treatment for syphilis), a Jarisch-Herxheimer (Jarish-Herxheimer) reaction may occur due to bacteriolysis.
Hematological:hemolytic anemia, leukopenia, thrombocytopenia or eosinophilia.
Violation of the pumping function of the myocardium.
Rarely, with pre-existing nephropathy, albuminuria and hematuria may occur. Oliguria or anuria, observed in some cases when prescribing benzylpenicillin, usually disappears 48 hours after stopping treatment. Diuresis can be restored by administration of a 10% mannitol solution.
- cases of hypersensitivity to penicillin (including other β-lactam antibiotics);
- allergic reactions to penicillin require immediate discontinuation of the drug and the necessary therapeutic measures. In patients with hypersensitivity to cephalosporins there may be cross-reactions of hypersensitivity (5-10% of cases).
Carefully prescribe penicillin to patients with allergies.
Banal infections do not require treatment with benzylpenicillin.
Application for violations of liver function
In patients with severe hepatic insufficiency, it is desirable to select single doses or intervals between doses individually (see section "Dosage regimen").
Application for violations of kidney function
In patients with severe renal insufficiency, it is desirable to select single doses and intervals between doses individually (see section "Dosage regimen").
As a rule, the daily dose for children under 12 years of age is 50,000 units / kg.
Premature babies and newborns (BT approx. 3.5 kg):
- 30000-100000 IU/kg/day
Children under 1 year (BT up to 10 kg):
- 30000-100000 IU/kg/day
Children from 1 to 12 years (BT from 10 to 38 kg):
- 30000 IU / kg / day.
With the development of allergic reactions, treatment with benzylpenicillin should be stopped immediately, and, if necessary, symptomatic treatment should be prescribed.
Precautions must be observed in the treatment of patients with cardiopathy, hypovolemia (with inflammation of the circulating blood volume), epilepsy, nephropathy and liver pathology.
When administered in high doses for more than five days, studies of electrolyte balance, kidney and liver function, and hematological tests are recommended.
Patients receiving benzylpenicillin may have a false-positive urine test for sugar.
In patients with diabetes, there may be a delay in the absorption of benzylpenicillin from intramuscular depots.
It is possible to use benzylpenicillin during pregnancy and lactation as prescribed by a doctor.
With prolonged treatment with antibiotics, the possibility of the emergence of resistant strains of microorganisms and fungi should be taken into account.
In the case of sexually transmitted diseases, if syphilis is suspected, dark field and serological tests should be performed before starting treatment and thereafter for at least 4 months.
Antacids, glucosamine, laxatives, food, aminoglycosides - slow down and reduce the absorption of benzylpenicillin sodium salt; ascorbic acid increases absorption.
With the simultaneous use of anti-inflammatory, antirheumatic and antipyretic drugs, especially indomethacin, phenylbutazone and salicylates, with benzylpenicillin, suppression of the competitive type of excretion mechanism can be observed. Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Benzylpenicillin sodium salt increases the effectiveness 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 breakthrough bleeding. Diuretics, allopurinol, blockers of tubular secretion, phenylbutazone, non-steroidal anti-inflammatory drugs, reducing tubular secretion, increase the concentration of benzylpenicillin sodium salt. Allopurinol when used together increases the risk of developing allergic reactions (skin rash).
| benzylpenicillin sodium
Analogues (generics, synonyms)
Benzylpenicillin sodium
Recipe (international)
S.: Dissolve in sterile isotonic sodium chloride solution and inject under the skin, intramuscularly 4 times a day
Rp.: Benzylpenicillini-natrii 500,000 IU
S.: Inject into the muscle 500,000 IU of the drug 4 times a day. Pre-dilute it in 2 ml of sterile isotonic sodium chloride solution (child 10 years old)
Rp.: Benzylpenicillini-natrii 250,000 IU
S.: Dilute the contents of the vial in 4 ml of sterile isotonic sodium chloride solution and inject 2 ml (125,000 IU) into a vein 2 times with an interval of 3 hours (child 5 years old)
Active substance
Benzylpenicillin (Benzylpenicillin)
pharmachologic effect
Benzylpenicillin is active against gram-positive microorganisms (staphylococci, streptococci, pneumococci, the causative agent of diphtheria, anaerobic / able to exist in the absence of oxygen / spore-forming rods, anthrax rods), gram-negative cocci (gonococci, meningococci), as well as against spirochetes, some actinomycetes and others microorganisms. The drug is ineffective against most gram-negative bacteria, rickettsia, viruses, protozoa, fungi.
Benzylpenicillin, when administered intramuscularly, is rapidly absorbed into the blood and is found in body fluids and tissues; in the cerebrospinal fluid penetrates in small quantities. The maximum concentration in the blood is observed after intramuscular injection after 30-60 minutes.
With subcutaneous administration, the rate of absorption is less constant, usually the maximum concentration in the blood is observed after 60 minutes. 3-4 hours after a single intramuscular or subcutaneous injection, only traces of the antibiotic are found in the blood. To maintain concentration at a high enough therapeutic effect level, it is necessary to make injections every 3-4 hours. intravenous administration the concentration of penicillin in the blood decreases rapidly. When taken orally, the drug is poorly absorbed and destroyed. gastric juice and penicillinase (an enzyme) produced by the intestinal microflora. It is excreted mainly by the kidneys.
The concentration and duration of circulation of benzylpenicillin in the blood depend on the size of the administered dose. The antibiotic penetrates well into tissues and body fluids. In the cerebrospinal fluid, it is normally found in small quantities, but with inflammation of the meninges, its concentration increases.
It should be remembered that strains of staphylococci that form the enzyme penicillinase, which destroys benzylpenicillin, are resistant to the action of benzylpenicillin. The low activity of benzylpenicillin against bacteria of the intestinal group, Pseudomonas aeruginosa and other microorganisms is also associated to a certain extent with their production of penicillinase.
Mode of application
For adults:
Individual. Enter in / m, in / in, s / c, endolumbally.
With the / m and / in the introduction
Adults: the daily dose varies from 250,000 to 60 million units.
If necessary, the daily dose can be increased to 200,000-300,000 IU / kg, according to vital indications - up to 500,000 IU / kg. The frequency of administration is 4-6 times / day.
Endolumbalno: depending on the disease and the severity of the course, adults - 5000-10000 IU, children - 2000-5000 IU. The drug is diluted in sterile water for injection or in a 0.9% solution of sodium chloride at the rate of 1 thousand units / ml. Before injection (depending on the level intracranial pressure) extract 5-10 ml of CSF and add it to the antibiotic solution in equal proportions.
P / c: used for chipping infiltrates (100,000-200,000 IU in 1 ml of 0.25% -0.5% Novocain solution).
The duration of treatment with benzylpenicillin, depending on the form and severity of the course of the disease, can range from 7-10 days to 2 months or more.
For kids: Introduction to / m and / in
For children: the daily dose for children under 1 year is 50,000-100,000 IU / kg; older than 1 year - 50,000 IU / kg.
Indications
Bacterial infections caused by pathogens sensitive to penicillin: community-acquired pneumonia, pleural empyema, bronchitis; peritonitis; osteomyelitis; infections of the genitourinary system (pyelonephritis, pyelitis, cystitis, urethritis, cervicitis), biliary tract infections (cholangitis, cholecystitis); wound infection, skin and soft tissue infections: erysipelas, impetigo, secondarily infected dermatoses; diphtheria; scarlet fever; anthrax; actinomycosis; infections of ENT organs; gonorrhea, syphilis.
Contraindications
Hypersensitivity; epilepsy (for endolumbar administration), hyperkalemia, arrhythmias (for potassium salt).
Side effects
- From the gastrointestinal tract:
stomatitis and glossitis are occasionally noted. Nausea, vomiting. Antibiotic-induced diarrhea should raise suspicion for pseudomembranous colitis (possibility of emergence of resistant organisms or fungi) and further treatment should be specific to the causative organism. When superinfection occurs, appropriate measures should be taken.
– Allergic:
due attention should be paid to side effects, namely anaphylaxis, urticaria, fever, joint pain, angioedema, erythema multiforme and exfoliative dermatitis.
– Hematological:
hemolytic anemia, leukopenia, thrombocytopenia or eosinophilia.
Due to bacteriolysis, in infections caused by endotoxin-producing bacteria such as salmonella, leptospira or treponema (treatment for syphilis), a Jarisch-Herxheimer (Jarish-Herxheimer) reaction may occur due to bacteriolysis.
Violation of the pumping function of the myocardium.
Rarely, with pre-existing nephropathy, albuminuria and hematuria may occur. Oliguria or anuria, observed in some cases when prescribing benzylpenicillin, usually disappears 48 hours after stopping treatment. Diuresis can be restored by administration of a 10% mannitol solution.
Release form
In vials of 125,000 IU, 250,000 IU, 500,000 IU, 1,000,000 IU. Ointment (in 1 g 10,000 IU) 15 g in a tube
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Name:
Name: Benzylpenicillin sodium salt (Benzylpenicillin Natrium)
Indications for use:
It is used for diseases caused by microorganisms sensitive to benzylpenicillin: lobar and focal pneumonia (pneumonia), acute and subacute septic (associated with the presence of viruses in the blood) endocarditis (inflammation of the internal cavities of the heart), wound infections, purulent infections of the skin, soft tissues and mucous membranes membranes, purulent pleurisy (purulent inflammation of the membranes of the lung), peritonitis (inflammation of the peritoneum), cystitis (inflammation Bladder), septicemia (a form of blood infection by microorganisms) and pyemia (a form of sepsis, in which microbes are brought into the blood stream internal organs where secondary abscesses develop - cavities filled with pus), acute and chronic osteomyelitis(inflammation bone marrow and adjacent bone tissue) different forms angina, diphtheria, erysipelas, purulent inflammatory diseases in obstetric-gynecological and otorhinolaryngological practice (treatment of diseases of the ear, throat, nose); with inflammatory diseases of the eye, meningitis (inflammation of the meninges), scarlet fever, gonorrhea, blennorrhea (acute purulent inflammation of the outer shell of the eye), syphilis, anthrax, actinomycosis (fungal disease) and others infectious diseases.
Pharmachologic effect:
Benzylpenicillin is active against gram-positive microorganisms (staphylococci, streptococci, pneumococci, the causative agent of diphtheria, anaerobic / able to exist in the absence of oxygen / spore-forming rods, anthrax rods), gram-negative cocci (gonococci, meningococci), also against spirochetes, some actinomycetes and other microorganisms . The drug is ineffective against most gram-negative bacteria, rickettsia, viruses, protozoa, fungi.
Benzylpenicillin, when administered intramuscularly, is rapidly absorbed into the blood and is found in body fluids and tissues; in the cerebrospinal fluid penetrates in small quantities. The maximum concentration in the blood is observed after intramuscular injection after 30-60 minutes. With subcutaneous administration, the absorption rate is less constant, usually the highest concentration in the blood is observed after 60 minutes. After 3-4 hours, after a single intramuscular or subcutaneous injection, only traces of the antibiotic are found in the blood. In order to maintain the concentration at a level high enough for a therapeutic effect, it is necessary to make injections every 3-4 hours. With intravenous administration, the concentration of penicillin in the blood decreases rapidly. When taken orally, the product is poorly absorbed and destroyed by gastric juice and penicillinase (an enzyme) produced by the intestinal microflora. It is excreted mainly by the kidneys.
The concentration and duration of circulation of benzylpenicillin in the blood depend on the size of the administered dose. The antibiotic penetrates well into tissues and body fluids. In the cerebrospinal fluid, it is found normally in a non-cordial amount, however, with inflammation of the meninges, its concentration increases.
It should be remembered that strains of staphylococci that form the enzyme penicillinase, which destroys benzylpenicillin, are resistant to the action of benzylpenicillin. The low activity of benzylpenicillin against bacteria of the intestinal group, Pseudomonas aeruginosa and other microorganisms is also associated to a certain extent with their production of penicillinase.
Benzylpenicillin sodium salt method of administration and dosage:
Before prescribing a product to a patient, it is desirable to determine the susceptibility of the microflora to it that caused the disease in this patient. Benzylpenicillin is administered intramuscularly, usually deep into the muscles. Benzylpenicillin sodium salt is administered intravenously (stream or drip) at serious illnesses(sepsis / blood infection with microbes from the focus of purulent inflammation /, meningitis, etc.).
With intramuscular and intravenous administration of benzylpenicillin sodium salt, single doses for moderate infections (diseases of the urinary and biliary tract, soft tissue infection, etc.) are usually 250,000-500,000 IU; per diem - 1,000,000-2,000,000 units. In severe infections (sepsis, septic endocarditis, meningitis, etc.), up to 10,000,000-20,000,000 units per day are administered; with gas gangrene - up to 40,000,000-60,000,000 IU per day.
For intravenous jet administration, a single dose of benzylpenicillin sodium salt (1,000,000-2,000,000 units) is dissolved in 5-10 ml of sterile water for injection or isotonic sodium chloride solution and injected slowly over 3-5 minutes.
For intravenous drip, dilute 2,000,000-5,000,000 IU in 100-200 ml of isotonic sodium chloride solution or 5-10% glucose solution and inject at a rate of 60-80 drops per minute. When administered dropwise to children, a 5-10% glucose solution is used as a solvent (30-100 ml, depending on the dose and age).
Endolumbarally (into the spinal canal) benzylpenicillin sodium salt is administered for purulent diseases of the head and spinal cord and meninges. Depending on the nature of the disease, adults are prescribed 5000-10,000 IU, children - from 2000 to 5000 IU. Dilute the product in sterile water for injection or isotonic sodium chloride solution at the rate of 1000 IU per 1 ml. Before injection (depending on the level of intracranial pressure), 5-10 ml of cerebrospinal fluid is removed from the spinal canal and added to the antibiotic solution in equal proportions. Enter slowly (1 ml per minute), usually once a day for 2-3 days, then proceed to intramuscular injections.
Subcutaneously, benzylpenicillin sodium salt is used for chipping infiltrates (seals) 100,000-200,000 IU in 1 ml of 0.25-0.5% novocaine solution.
In the cavity (abdominal, pleural / cavity between the membranes of the lungs / etc.), a solution of benzylpenicillin sodium salt is injected at a concentration of 10,000-20,000 IU per 1 ml for adults and 2000-5000 IU per 1 ml for babies. Dissolve in sterile water for injection or isotonic sodium chloride solution. The duration of administration is 5-7 days, then they switch to intramuscular administration.
For children, benzylpenicillin is prescribed in different daily doses: at the age of up to 1 year - 50,000-100,000 IU per 1 kg of body weight, over 1 year old - 50,000 IU / kg. In severe infections (meningitis, sepsis, severe forms acute pneumonia) the daily dose can be increased to 200,000-300,000 U / kg, and in exceptional cases (for health reasons) - up to 500,000 U / kg.
The daily dose is divided into 4-6 injections.
For lung diseases (chronic bronchitis, pneumonia, lung gangrene, etc.), penicillin aerosol is often used: a single dose for adults is 100,000-300,000 units. Dilute in 3-5 ml of distilled water; apply 1-2 times a day; duration of inhalation - 10-30 minutes. In suppurative processes in the lungs, a solution of the product is also injected intratracheally (into the trachea) after thorough anesthesia (pain relief) of the pharynx, larynx and trachea. Usually 100,000 units are used in 10 ml of isotonic sodium chloride solution.
In diseases of the eyes (acute conjunctivitis / inflammation of the outer membrane of the eye /, ulcer of the cornea / transparent membrane of the eye /, gonoblenorrhea / acute purulent inflammation of the outer membrane of the eye caused by the causative agent of gonorrhea - gonococcus / etc.) is sometimes prescribed eye drops containing 20,000-100,000 IU of the sodium salt of benzylpenicillin in 1 ml of isotonic sodium chloride solution or distilled water. Enter 1-2 drops 6-8 times every day.
As ear drops or nose drops, solutions containing 10,000-100,000 IU per 1 ml are used.
Solutions of the product are used immediately after preparation, avoiding the addition of other drugs to them.
Treatment with benzylpenicillin, depending on the form and severity of the course of the disease, can last from 7-10 days to 2 months. and more (with sepsis, septic endocarditis, etc.). If after 3-5 days after the start of treatment there is no effect, it is necessary to switch to the use of other antibiotics or to administer benzylpenicillin together with other antibiotics or synthetic chemotherapeutic products.
Benzylpenicillin sodium salt contraindications:
Benzylpenicillin and all other penicillin products are contraindicated in penicillin hypersensitive patients suffering from bronchial asthma, urticaria, hay fever and others allergic diseases, as well as people with hypersensitivity and unusual reactions when taking other antibiotics and other medicinal products.
Epilepsy is also a contraindication to endolumbar administration.
The drug should be administered with caution to patients with an indication of allergic reactions in history (case history).
Benzylpenicillin sodium salt side effects:
Benzylpenicillin sodium salt and other penicillin products can cause various side effects. Some patients, especially those with increased susceptibility, have a headache, an increase in body temperature, urticaria, a rash on the skin and mucous membranes, joint pain, eosinophilia (an increase in the number of eosinophils in the blood), angioedema (allergic) edema and other allergic reactions; cases of anaphylactic shock (an allergic reaction of an immediate type) with a fatal outcome are described.
In case of severe allergic reactions, epinephrine, glucocorticoids, antihistamine products (diphenhydramine, etc.), calcium chloride are prescribed. The enzyme product peniiillinase is also used. With severe allergic reactions prescribed prednisolone or other glucocorticosteroids.
At the first signs of anaphylactic shock, measures should be taken to remove the patient from this state (administration of adrenaline, diphenhydramine, calcium chloride, use of cardiac drugs, inhalation of oxygen, warming, etc.; immediately after removing the patient from the state of asphyxia / lack of breathing / and shock enter 1,000,000 penicillinase).
The use of very large doses of penicillin, and especially with endolumbar administration, can cause neurotoxic effects (nausea, vomiting, increased reflex excitability, symptoms of meningism / the appearance of symptoms of meningitis in a sick person without the presence of an infectious agent in the cerebrospinal fluid /, convulsions, coma / unconsciousness /). Endolumbar injections must be carried out with great care.
When prescribing benzylpenicillin and products containing penicillin, it is necessary to find out if the patient had any complications (toxic-allergic reactions) during the previous use of penicillin.
In connection with the possibility of fungal lesions of the mucous membranes and skin, especially in newborns, the elderly and debilitated patients, it is advisable to prescribe vitamins of group B and vitamin C during penicillin treatment, and if necessary, nystatin or levorin.
