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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.

A solution of the drug for intramuscular administration is 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 use: 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.

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

For ear drops or nasal 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

The drug is administered intramuscularly, intravenously, subcutaneously, endolumbarally, intratracheally.

For moderate disease (infections of the upper and lower respiratory tract, urinary and biliary tract, soft tissue infection, 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 - 4-6 times a day, intravenous - 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% NaCl 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% NaCl 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.

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

Endolumbar. The drug is diluted in sterile water for injection or in 0.9% NaCl solution at the rate of 1 thousand units/ml. Before injection (depending on the level of intracranial pressure), 5-10 ml of CSF 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 eye diseases (acute conjunctivitis, corneal ulcer, gonoblennorrhea, etc.), eye drops containing 20-100 thousand units in 1 ml of 0.9% NaCl solution or distilled water are sometimes prescribed. Inject 1-2 drops 6-8 times a day.

For ear drops or nasal drops, solutions containing 10-100 thousand units/ml are used.

Benzylpenicillin potassium salt is administered only intramuscularly and subcutaneously, in the same doses as benzylpenicillin sodium salt.

Benzylpenicillin procaine salt is administered only intramuscularly. Average therapeutic dose for adults: single - 300 thousand units, daily - 600 thousand units. The highest daily dose for adults is 1.2 million units. Children under the age of 1 year are prescribed 50-100 thousand units/kg/day, over 1 year - 50 thousand units/kg/day. The frequency of administration of the drug is 1-2 times a day.

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

Powder for the preparation of injection solution Benzylpenicillin (Benzylpenicillin)

Instructions for medical use of the drug

Description of pharmacological action

Antibiotic of the group of biosynthetic penicillins. 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. Strains of Staphylococcus spp. that produce penicillinase are resistant to the action of benzylpenicillin. Destroys in an acidic environment. The novocaine salt of benzylpenicillin, compared to the potassium and sodium salts, is characterized by a longer duration of action.

Indications for use

Severe generalized infections (meningitis, septicemia, disseminated gonococcal infection), streptococcal endocarditis, congenital syphilis, abscesses, respiratory tract infections (pneumonia), skin infections (erysipelas), lymphadenitis and lymphangitis, osteomyelitis, anthrax, tetanus, gas gangrene.

Release form

Benzylpenicillin powder for preparing a solution for intravenous and intramuscular administration 1 million units Benzylpenicillin powder for preparing a solution for intravenous and intramuscular administration 500 thousand units Benzylpenicillin powder for preparing a solution for intravenous and intramuscular administration 1 million units Benzylpenicillin powder for preparing a solution for intravenous and intramuscular administration 500 thousand units Benzylpenicillin powder for the preparation of a solution for intravenous and intramuscular administration 1 million units Benzylpenicillin powder for the preparation of a solution for intravenous and intramuscular administration 1 million units Benzylpenicillin powder for the preparation of a solution for injection 1 million IU Benzylpenicillin powder for the preparation of a solution for injection 1 million IU Benzylpenicillin powder for solution for injection 5 million IU Benzylpenicillin powder for solution for injection 5 million IU

Pharmacodynamics

It disrupts the synthesis of cell wall peptidoglycan and causes lysis of microorganisms. Active against gram-positive bacteria (strains of Staphylococcus spp. that do not form penicillinase, Streptococcus spp., including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming bacilli, anthrax bacilli, Actinomyces spp., as well as against gram-negative cocci (Neisseria meningitidis, Neisseria gonorrhoeae ), Treponema spp., Spirochaeta spp. Not effective against most gram-negative bacteria, rickettsia, viruses, protozoa, and fungi. With intramuscular administration of sodium and potassium salts of benzylpenicillin, Cmax in the blood is achieved in 30–60 minutes; after 3–4 hours, traces of the antibiotic are detected in the blood. Benzylpenicillin novocaine salt is slowly absorbed and has a prolonged effect; after a single injection in the form of a suspension, the therapeutic concentration of penicillin in the blood remains for up to 12 hours. Binding to blood proteins is 60%. Penetrates well into organs, tissues and biological fluids, with the exception of cerebrospinal fluid and the prostate. During inflammation of the meninges, it passes through the BBB. When instilled into the conjunctival sac in therapeutic concentrations, it is found in the stroma of the cornea (it practically does not penetrate into the moisture of the anterior chamber when applied topically). Therapeutic concentrations in the cornea and anterior chamber humor are created with subconjunctival administration (while the concentration in the vitreous body does not reach a therapeutic level). With intravitreal administration, T1/2 is about 3 hours. It is excreted by the kidneys through glomerular filtration (approximately 10%) and tubular secretion (90%) unchanged. In newborns and infants, excretion slows down; in case of renal failure, T1/2 increases to 4–10 hours.

Pharmacokinetics

After intramuscular administration, it is quickly absorbed from the injection site. Widely distributed in tissues and body fluids. Benzylpenicillin penetrates well through the placental barrier and the blood-brain barrier during inflammation of the meninges. T1/2 - 30 min. Excreted in urine.

Use during pregnancy

During pregnancy, it is possible if the expected benefit to the mother outweighs the potential risk to the fetus. Breastfeeding should be stopped during treatment.

Contraindications for use

History of hypersensitivity to penicillins.

Side effects

Allergic reactions: anaphylactic shock, urticaria, Quincke's edema, fever/chills, headache, arthralgia, eosinophilia, interstitial nephritis, bronchospasm, skin rashes. Other: for sodium salt - impaired myocardial contractility; for potassium salt - arrhythmia, cardiac arrest, hyperkalemia. With endolumbar administration - neurotoxic reactions: nausea, vomiting; increased reflex excitability, meningeal symptoms, convulsions, coma.

Directions for use and doses

Dosage varies depending on the type and severity of the infection; Approximate recommended doses: adults - 1.8–3.6 g (3–6 million IU) per day in 4 (6) divided doses. For severe infections (meningitis, septicemia) - up to 200 (300) mg/kg (0.33–0.5 million IU/kg) per day in 4–6 divided doses. In these cases, treatment is started with a slow IV injection or a rapid infusion (20–40 ppm, using 5% glucose as a diluent). Children: 30–90 mg/kg (50,000–150,000 IU/kg) per day in 4–6 divided doses. This corresponds to approximately 240 mg 4 times daily for children 5 months to 2 years; 300–600 mg 4 times daily for children 2 to 6 years old and 450–900 mg 4 times daily for children 7–12 years old. For severe infections (meningitis, septicemia) - up to 300 mg/kg (0.5 million IU/kg) per day in 4-6 doses. In these cases, treatment is started with a slow intravenous injection or a rapid infusion (20–40 minutes, using 5% glucose as a diluent). Benzylpenicillin can also be used intramuscularly. Dilution of benzylpenicillin for infusion should be carried out immediately before use, since the activity of the antibiotic quickly decreases in infusion solutions. The duration of treatment depends on the indications and clinical picture. Recommended doses for certain diseases are: meningitis and/or septicemia caused by meningococci - 180–240 mg/kg (0.3–0.4 million IU/kg) per day in 4–6 doses, as a slow i.v. injections or infusions for at least 5 days; meningitis and/or septicemia caused by pneumococci - 240–300 mg/kg (0.4–0.5 million IU/kg) per day in 4–6 divided doses, as a slow IV injection or infusion over at least 10 days; infections caused by clostridia - 9-12 g (15-20 million IU) per day for adults and 180 mg/kg (0.3 million IU/kg) per day for 1 week as an addition to antitoxin therapy; streptococcal endocarditis - 6–12 g (10–20 million IU) per day for adults and 180 mg/kg (0.3 million IU) for children for 2–4 weeks; congenital syphilis - 30 mg/kg (50,000 IU/kg) per day IM or IV in 2 doses for 2 weeks.

Overdose

Symptoms: convulsions, impaired consciousness. Treatment: drug withdrawal, symptomatic therapy.

Interactions with other drugs

Probenecid, by reducing renal excretion, increases blood levels.

Precautions for use

IV, endolumbarally and into the cavities are administered only in a hospital setting. Benzylpenicillin preparations should be used only as directed and under the supervision of a physician. It must be remembered that the use of insufficient doses of benzylpenicillin (as well as other antibiotics) or stopping treatment too early 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 intramuscularly. IV and endolumbar administration is not allowed. Of all benzylpenicillin preparations, only the sodium salt is administered endolumbarally. For bronchial asthma, hay fever and other allergic diseases, benzylpenicillin is used with caution while prescribing antihistamines. If allergic reactions develop in patients, the drug should be discontinued. In weakened patients, newborns, and the elderly, long-term treatment may lead to the development of superinfection caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms). 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 2-3 days after starting the drug (maximum 5 days) no effect is observed, it is necessary to switch to treatment with another antibiotic or combination therapy.

Storage conditions

List B.: In a place protected from light, at a temperature not exceeding 30 °C. prepared solution for injection 24 hours (in the refrigerator 72 hours), for infusion - 12 hours (in the refrigerator - 24 hours).

Best before date

48 months

ATX classification:

J Antimicrobials for systemic use

J01 Antimicrobials for systemic use

J01C Beta-lactam antibiotics - penicillins

J01CE Penicillins, sensitive to beta-lactamases

J01CE01 Benzylpenicillin