Benzylpenicillin - instructions for use, dose, side effects, contraindications

Benzylpenicillin, an antibiotic from the group of biosynthetic penicillins. Active against gram-positive bacteria (strains Staphylococcus spp. not forming penicillinase, Streptococcus spp., including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming sticks, anthrax rods, Actinomyces spp., as well as against gram-negative cocci {Neisseria meningitidis, Neisseria gonorrhoeae), Treponema spp., Spirochaeta spp.. Staphylococcus strains forming penicillinase are resistant to the action of benzylpenicillin, since this enzyme destroys the benzylpenicillin molecule.

The drug is not active against most gram-negative bacteria, rickettsia (Rickettsia spp.), viruses, protozoa.

Pharmacokinetics:

Benzylpenicillin is well absorbed when administered parenterally, does not have a cumulative effect, is rapidly excreted from the body with urine.

With intramuscular injection, 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 found.

The level of concentration and duration of circulation of benzylpenicillin in the blood depends on the amount of the administered dose. The antibiotic penetrates well into the tissues and body fluids: in the cerebrospinal fluid it is normally found in a small amount, with inflammation of the meningeal membranes, its concentration in the cerebrospinal fluid rises.

Indications:

Bacterial infections caused by susceptible pathogens: croup and focal pneumonia, empyema of the pleura, bronchitis; septic endocarditis (acute and subacute), wound infection, purulent infections of the skin, soft tissues and mucous membranes (incl.rheumatism, impetigo, secondarily infected dermatoses), purulent pleurisy, peritonitis, sepsis, osteomyelitis, infections of the ENT organs (angina), meningitis, diphtheria, gas gangrene, scarlet fever, gonorrhea, leptospirosis, syphilis, anthrax, lung actinomycosis, and biliary tract, the treatment of purulent-inflammatory diseases in obstetric and gynecological practice, eye diseases (including acute gonococcal conjunctivitis, corneal ulcer, gonoblenorea).

Contraindications:

Hypersensitivity to benzylpenicillin and other drugs from the group of penicillins and cephalosporins, lactation.

Carefully:

Pregnancy, lactation, severe hepatic insufficiency, renal failure, allergic diseases (including bronchial asthma, pollinosis).

Pregnancy and lactation:

Use in pregnancy is possible only if the intended benefit exceeds the potential risk to the fetus. If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.

Dosing and Administration:

The drug is administered intramuscularly, in the cavity (abdominal, pleural, etc.) or subcutaneously.

In the cavity the drug is administered only in a hospital!

Intramuscularly: for infections of medium severity, a single dose of the drug is usually 250 000-500 000 units; daily - 1 000 000-2 000 000 units; in severe infections, up to 10,000,000-20,000,000 units per day are administered; with gas gangrene - up to 40 000 000-60 000 000 units. The daily dose for children under the age of 1 year is 50 000-100 000 units / kg, over 1 year - 50 000 units / kg; if necessary, the daily dose can be increased up to 200 000-300 000 units / kg, according to vital indications - up to 500 000 units / kg. Multiplicity of the drug 4-6 times a day.

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

Subcutaneously the preparation is used to cut infiltrates in a concentration of 100,000-200,000 units per 1 ml of 0.25-0.5 % solution of procaine.

In the cavity (abdominal, pleural, etc.) solution of the drug to adults is administered at a concentration of 10 000-20 000 units per ml, children - 2 000-5 000 units per 1 ml. Dissolve in sterile water for injection or 0.9% solution of sodium chloride. Duration of treatment is 5-7 days with the subsequent transition to intramuscular injection.

Side effects:

Allergic reactions: hyperthermia, urticaria, skin rash, rash on mucous membranes, arthralgia, eosinophilia, angioedema, interstitial nephritis, bronchospasm, anaphylactic shock.

At the beginning of the course of treatment (especially in the treatment of congenital syphilis) - fever, chills, increased sweating, exacerbation of the disease, the reaction of Jarisch-Gerxheimer.

From the side of cardiovascular reaction: decrease in pumping function of the myocardium.

Local reactions: pain and tightness at the site of the IM.

With prolonged use: dysbiosis, development of superinfection.

With endolumbal introduction - Neurotoxic reactions: nausea, vomiting, increased reflex excitability, meningeal symptoms, convulsions, coma.

Overdose:

Symptoms: convulsions, impaired consciousness.

Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Probenecid reduces the tubular secretion of benzylpenicillin, thereby increasing the concentration of the latter in blood plasma, the half-life increases.

When used simultaneously with antibiotics that have a bacteriostatic effect (macrolides, chloramphenicol, lincosamides, tetracycline), the bactericidal action of benzylpenicillin decreases

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 which produces paraaminobenzoic acid, ethinyl estradiol - the risk of bleeding "breakthrough".

Diuretics, allopurinol, tubular secretion blockers, phenylbutazone, non-steroidal anti-inflammatory drugs, reducing tubular secretion, increase the concentration of benzylpenicillin.

Allopurinol increases the risk of allergic reactions (skin rashes). Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergistic effect.

Special instructions:

If after 3-5 days after the start of the application of the effect is not observed, you should proceed to use other antibiotics or combination therapy.

In connection with the possibility of developing fungal superinfection, it is advisable to prescribe antifungal preparations if necessary for prolonged treatment with benzylpenicillin.

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.

Effect on the ability to drive transp. cf. and fur:During the administration of the drug, care should be taken when driving vehicles, mechanisms and other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Powder for the preparation of solution for injection 500,000 units and 1,000,000 units.

Packaging:

Powder for solution for injection and 500,000 IU 1,000,000 IU vials of glass tube for medicaments capacity of 10 ml, hermetically sealed with rubber stoppers, crimped aluminum caps.

50 bottles are placed in a box of cardboard with an enclosure of instructions for the medical use of the drug to an equal number of bottles (for hospitals).

1, 5 or 10 vials are placed in an individual pack of cardboard together with instructions for medical use.

Storage conditions:

In a dry place, at a temperature not exceeding 20 ° С. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001578 / 01-2002

Date of registration:16.06.2008 / 27.04.2012

Expiration Date:Unlimited

The owner of the registration certificate:BIOCHEMIST, OJSC BIOCHEMIST, OJSC Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp22.01.2017

Illustrated instructions

Instructions

Benzylpenicillin (Benzylpenicillin)