Pharmacy No. 84. Delivery of medicines to your home and office.

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Benzylpenicillin

The drug is intended for intramuscular, intravenous, subcutaneous, endolumbar and intratracheal administration.

For moderate disease (infections of the lower respiratory tract, urinary and biliary tract, soft tissue infections and others) - 4-6 million units/day for 4 administrations.

For severe infections (sepsis, septic endocarditis, meningitis, etc.) - 10-20 million units per day; with gas gangrene - up to 40-60 million units.

The daily dose for children under 1 year of age is 50,000-100,000 units/kg, over 1 year of age – 50,000 units/kg; if necessary - 200,000-300,000 units/kg, for health reasons - increase to 500,000 units/kg. Frequency of administration - 4-6 times a day, intravenously - 1 - 2 times a day in combination with intramuscular injections.

It is administered endolumbarally for purulent diseases of the brain, spinal cord and meninges.

Depending on the disease and the severity of its course: adults - 5-10 thousand units, children - 2-5 thousand units once a day for 2-3 days intravenously, then prescribed intramuscularly.

For intravenous jet administration

a single dose (1-2 million units) is dissolved in 5-10 ml of sterile water for injection or 0.9% sodium chloride solution and administered slowly over 3-5 minutes.

For intravenous drip administration

2-5 million units are diluted with 100-200 ml of 0.9% sodium chloride solution or 5-10% dextrose solution and administered at a rate of 60-80 drops/min.

When administered by drip to children, a 5-10% dextrose solution (100-300 ml depending on the dose and age) is used as a solvent.

Solution of the drug for intramuscular administration

prepared immediately before administration by adding 1-3 ml of water for injection or 0.9% sodium chloride solution or 0.5% novocaine solution to the contents of the bottle.

Solutions are used immediately after preparation, avoiding the addition of other medications to them.

Subcutaneously

the drug is used to inject infiltrates at a concentration of 100-200 thousand units in 1 ml of 0.25-0.5% novocaine solution.

Preparation of a solution of the drug for endolumbar

Application: dilute the drug in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1 thousand units/ml.

Before injection (depending on intracranial pressure), 5-10 ml of cerebrospinal fluid is removed and added to the antibiotic solution in equal proportions. Inject slowly (1 ml/min), usually once a day for 2-3 days, then proceed to intravenous or intramuscular injections.

For suppurative processes in the lungs, a solution of the drug is administered intratracheally

(after thorough anesthesia of the pharynx, larynx and trachea). Usually 100 thousand units are used in 10 ml of 0.9% sodium chloride solution.

For eye diseases (acute conjunctivitis, corneal ulcer, gonoblennorrhea and others), eye drops are prescribed,

containing 20-100 thousand units in 1 ml of 0.9% sodium chloride solution or distilled water. Inject 1-2 drops 6-8 times a day.

For ear drops or nose drops

solutions containing 10-100 thousand units/ml are used. The duration of treatment with the drug, depending on the form and severity of the disease, is from 7-10 days to 2 months or more (for example, for sepsis, septic endocarditis).

BENZYLPENICILLIN SODIUM SALT

Directions for use and doses

Benzylpenicillin sodium salt is administered intramuscularly, intravenously, subcutaneously, locally.
Intravenously and intramuscularly:

for moderate disease (infections of the upper and lower respiratory tract, urinary and biliary tract, infection of soft tissues, etc.) - 4-6 million units/day for 4 administrations. For severe infections (sepsis, septic endocarditis, meningitis, etc.) - 10-20 million units/day; with gas gangrene - up to 40-60 million units/day.

The daily dose for children under 1 year of age is 50-100 thousand units/kg, over 1 year of age – 50 thousand units/kg; if necessary - 200-300 thousand units/kg, for “vital” indications - increase to 500 thousand units/kg. Frequency of administration: intramuscularly - 4-6 times a day, intravenously - 1-2 times a day in combination with intramuscular injections.

Subcutaneously

for infiltrating infiltrates at a concentration of 100-200 thousand units in 1 ml of 0.25-0.5% procaine solution.

In the cavity (abdominal, pleural, etc.)

a solution of benzylpenicillin sodium salt is administered to adults at a concentration of 10-20 thousand units per 1 ml, for children - 2-5 thousand units per 1 ml. Water for injection or 0.9% sodium chloride solution is used as a solvent. The duration of treatment is 5-7 days, followed by switching to intramuscular administration.

For eye diseases

Prescribe
eye drops
containing 20-100 thousand units in 1 ml of sterile 0.9% sodium chloride solution or distilled water. Inject 1-2 drops 6-8 times a day. The solution is used freshly prepared.

For ear drops or nose drops

solutions containing 10-100 thousand units in 1 ml of sterile 0.9% sodium chloride solution or distilled water are used. Administer 1-2 drops 6-8 times a day.

The duration of treatment with benzylpenicillin, depending on the form and severity of the disease, is 7-10 days.

Solutions are used immediately after preparation, avoiding the addition of other medications to them.

For intramuscular administration

add 1-3 ml of water for injection, 0.9% sodium chloride solution or 0.5% procaine (novocaine) solution to the contents of the bottle. The resulting solution is injected deep into the muscle.

When benzylpenicillin is diluted in a procaine solution, cloudiness of the solution may be observed due to the formation of benzylpenicillin procaine crystals, which is not an obstacle to intramuscular and subcutaneous administration of the drug.

For intravenous jet administration

a single dose (1-2 million units) is dissolved in 5-10 ml of sterile water for injection or 0.9% sodium chloride solution and administered slowly over 3-5 minutes.

For intravenous drip administration

2-5 million units are diluted in 100-200 ml of 0.9% sodium chloride solution or 5-10% dextrose solution and administered at a rate of 60-80 drops/min. When administered dropwise to children, a 5-10% dextrose solution (30-100 ml depending on the dose and age) is used as a solvent.

For subcutaneous administration

the contents of the bottle are diluted in 0.25-0.5% procaine solution: 500 thousand units in 2.5-5 ml, 1 million units in 5-10 ml, respectively.

For intracavitary administration

the contents of the bottle are diluted in 0.9% sodium chloride solution or in water for injection: adults - 500 thousand units in 25-50 ml, 1 million units in 50-100 ml, respectively; children - 500 thousand units in 100-250 ml, 1 million units in 200-500 ml, respectively.

Eye drops

should be prepared ex tempore: the contents of the bottle are diluted in a 0.9% solution of sodium chloride or distilled water: 500 thousand units in 5-25 ml, 1 million units in 10-50 ml, respectively.

Ear drops and nasal drops:

the contents of the bottle are diluted in 0.9% sodium chloride solution or distilled water: 500 thousand units in 5-50 ml, 1 million units in 10-100 ml, respectively.

Substance-powder Benzathine benzylpenicillin (Benzathine benzylpenicillin)

Instructions for medical use of the drug

Description of pharmacological action

It disrupts the synthesis of peptidoglycan, the supporting polymer of the cell wall. Active against gram-positive microorganisms, incl. Staphylococcus spp. (except for penicillinase-producing strains), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming bacilli Bacillus anthracis, some gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), Actinomyces israelii, and Treponema spp. Not effective against viruses (causative agents of influenza, polio, smallpox, etc.), mycobacterium tuberculosis, protozoa, rickettsia, fungi, as well as most gram-negative microorganisms.

Indications for use

Syphilis and other diseases caused by Treponema pallidum (yaws), streptococcal infections (excluding infections caused by group B streptococci) - acute tonsillitis, scarlet fever, wound infections, erysipelas; rheumatism (prevention), prevention of postoperative complications.

Release form

Benzathine benzylpenicillin sterile substance-powder; aluminum can 2 kg polyethylene bag (bag) 1 Benzathine benzylpenicillin sterile substance-powder; aluminum can 3 kg polyethylene bag (bag) 1 Benzathine benzylpenicillin sterile substance-powder; aluminum can 4 kg polyethylene bag (bag) 1 Benzathine benzylpenicillin sterile substance-powder; aluminum can 5 kg polyethylene bag (bag) 1

Pharmacokinetics

After intramuscular administration, it is slowly hydrolyzed to release benzylpenicillin. TCmax in plasma - 12-24 hours after injection. On the 14th day after administration of 2.4 million units, the concentration in the blood serum is 0.12 mcg/ml; on day 21 after administration of 1.2 million units - 0.06 mcg/ml (1 unit = 0.6 mcg). Penetration into liquids is high, into tissues - low. Overcomes the placental barrier and penetrates into mother's milk. Bonding with plasma proteins is 40-60%. Metabolized slightly, excreted mainly by the kidneys unchanged. Over 8 days, up to 33% of the administered dose is released.

Use during pregnancy

Benzathine benzylpenicillin penetrates the placental barrier and is excreted in breast milk. Use during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.

Contraindications for use

Hypersensitivity (including to cephalosporins, carbapenems and other penicillins). Bronchial asthma. Hay fever. Tendency to allergic manifestations.

Side effects

Allergic reactions: rash on the skin and mucous membranes, urticaria, fever, eosinophilia, joint pain, erythema multiforme, exfoliative dermatitis, Quincke's edema, anaphylactic shock. From the cardiovascular system and blood (hematopoiesis, hemostasis): anemia, thrombocytopenia, leukopenia, coagulation disorders. Other: headache, stomatitis, glossitis; local phenomena: pain at the injection site, infiltrates, abscesses, fistulas, peripheral neuritis; with long-term therapy - superinfection caused by drug-resistant microorganisms and fungi.

Directions for use and doses

V/m. Adults for the prevention and treatment of infectious diseases in a dose of 300,000–600,000 units once a week or 1.2 million units (for the treatment of rheumatism - up to 2.4 million units) 2 times a month. To prevent relapses of rheumatism - 600,000 units once a week for 6 weeks in combination with acetylsalicylic acid or other NSAIDs. Children are administered at the rate of 5,000–10,000 units/kg once a week or at the rate of 20,000 units/kg 2 times a month (more frequent injections are not allowed). Treatment of syphilis is carried out according to special instructions. The average dose is 2.4 million units 2-3 times with an interval of 8 days.

Interactions with other drugs

Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) have an antagonistic effect. Increases the effectiveness of indirect anticoagulants. Reduces the effectiveness of oral contraceptives and ethinyl estradiol (risk of breakthrough bleeding). Diuretics, allopurinol, NSAIDs - reduce tubular secretion and increase concentration. Allopurinol increases the risk of allergic reactions (skin rash).

Precautions for use

It must be administered strictly intramuscularly to a significant depth; an aspiration test is performed before injection. If it enters the vessels, embolism and ischemia may develop. If two injections are necessary, they are given in different buttocks. If blood appears in the syringe during an intramuscular injection (indicating that the needle has entered a blood vessel), the syringe should be removed and injected elsewhere. At the end of the injection, the injection site is pressed with a cotton swab, which prevents the drug from entering the muscle tissue into the subcutaneous tissue (rubbing the buttock after the injection is not recommended). With accidental intravascular administration, a transient feeling of depression, anxiety and visual disturbances (Wanier syndrome) may occur. If an allergic reaction develops, treatment is stopped immediately. When the first signs of anaphylactic shock appear, it is necessary to take urgent measures to remove the patient from this state: administration of norepinephrine, glucocorticoids, etc., and, if necessary, mechanical ventilation. When treating sexually transmitted diseases, if syphilis is suspected, microscopic and serological studies are necessary before starting therapy and then for 4 months. Due to the possibility of developing fungal infections, it is advisable to prescribe nystatin and levorin. Due to the fact that with long-term oral administration of antibiotics, the intestinal microflora that produces vitamins B1, B6, B12 can be suppressed, it is advisable for patients to prescribe B vitamins to prevent hypovitaminosis. It must be taken into account that the use of the drug in insufficient doses or stopping treatment too early often leads to the emergence of resistant strains of pathogens.

Special instructions for use

Use with caution in patients with impaired renal function, in case of predisposition to allergic reactions (especially with drug allergies), with increased sensitivity to cephalosporins (due to the possibility of developing cross-allergy). It is not recommended for use in the treatment of neurosyphilis (since the required plasma concentration is not achieved). IV and endolumbar administration is not allowed.

Storage conditions

List B. In a place protected from light.

Best before date

24 months

ATX classification:

J Antimicrobials for systemic use

J01 Antimicrobials for systemic use

J01C Beta-lactam antibiotics - penicillins

J01CE Penicillins, sensitive to beta-lactamases

J01CE08 Benzathine benzylpenicillin