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

Benzylpenicillin is an antibiotic of a group of biosynthetic penicillins. The drug has a bactericidal effect. Benzylpenicillin by inhibiting the synthesis of the cell wall of microorganisms stops the multiplication of bacteria.

It is 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 sticks; and Actinomyces spp., Spirochaetaceae.

The drug is destroyed in an acidic environment.

To the action of benzylpenicillin resistant strains Staphylococcus spp., producing penicillinase.

Novocain salt of benzylpenicillin in comparison with potassium and sodium salts is characterized by a longer duration of action.

Pharmacokinetics:

After intramuscular injection, it is rapidly absorbed from the injection site. Widely distributed in tissues and body fluids. Benzylpenicillin well penetrates the placental barrier, the blood-brain barrier in the inflammation of the meninges.

The half-life is about 30 minutes.

The drug is excreted in the urine.

Indications:

Treatment of diseases caused by microorganisms susceptible to benzylpenicillin: acute and subacute bacterial endocarditis, meningitis, acute and chronic osteomyelitis, infections of the urinary and biliary tracts, angina, purulent infections of the skin, soft tissues and mucous membranes, erysipelas, diphtheria, scarlet fever, croupous and lobular pneumonia, empyema, sepsis, septicemia, pyemia, anthrax, actinomycosis, treatment of inflammatory diseases in obstetrics and gynecology, ENT diseases, eye diseases, gonorrhea, ophthalmia, syphilis.

ICD-10

I.A20-A28.A22 anthrax

I.A30-A49.A36 Diphtheria

I.A30-A49.A38 Scarlet fever

I.A30-A49.A39 Meningococcal infection

I.A30-A49.A40 Streptococcal septicemia

I.A30-A49.A42 Actinomycosis

I.A30-A49.A46 Erys

I.A50-A64.A50 Congenital syphilis

I.A50-A64.A51 Early syphilis

I.A50-A64.A52 Late syphilis

I.A50-A64.A54 Gonococcal infection

I.A50-A64.A54.3 Gonococcal infection of the eye

VI.G00-G09.G00 Bacterial meningitis, not elsewhere classified

VII.H10-H13.H10 Conjunctivitis

VII.H15-H22.H15.0 Sclerite

VII.H15-H22.H15.1 Episcleritis

VII.H15-H22.H16 Keratite

VIII.H65-H75.H66 Purulent and unspecified otitis media

IX.I30-I52.I33 Acute and subacute endocarditis

X.J00-J06.J01 Acute Sinusitis

X.J00-J06.J02 Acute pharyngitis

X.J00-J06.J03 Acute tonsillitis

X.J00-J06.J04 Acute laryngitis and tracheitis

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J20-J22.J20 Acute bronchitis

X.J30-J39.J31 Chronic rhinitis, nasopharyngitis and pharyngitis

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J35.0 Chronic tonsillitis

X.J30-J39.J37 Chronic laryngitis and laryngotracheitis

X.J40-J47.J42 Chronic bronchitis, unspecified

X.J85-J86.J86 Pythothrace

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K83.0 Cholangitis

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIII.M86-M90.M86 Osteomyelitis

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N10-N16.N11 Chronic tubulointerstitial nephritis

XIV.N30-N39.N30 Cystitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIV.N70-N77.N70 Salpingitis and oophoritis

XIV.N70-N77.N72 Inflammatory disease of the cervix

XIV.N70-N77.N73.0 Acute parametritis and pelvic cellulite

Contraindications:

Hypersensitivity to benzylpenicillin and other drugs from the group of penicillins and cephalosporins. Endolumbal administration is contraindicated in patients with epilepsy.

Carefully:

With caution apply in patients with impaired renal function, with heart failure, predisposition to allergic reactions (especially with drug allergies), with increased sensitivity to cephalosporins (due to the possibility of developing cross-allergies).

Pregnancy and lactation:

Use in pregnancy is possible only if the intended benefit of therapy for the mother 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, intravenously, subcutaneously, endolumbally.

When administered intramuscularly and intravenously to adults, the daily dose varies from 250,000 to 60 million 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 administration 4-6 times a day.

Endolumbally, the drug is administered depending on the disease and severity of the course: adults - 5000-10 000 units, children - 2000-5000 units. The drug is diluted in sterile water for injection or in a 0.9% solution of sodium chloride at a rate of 1,000 U / ml. Before injection (depending on the level of intracranial pressure), 5-10 ml cerebrospinal fluid and add it to the solution of the antibiotic in an equal proportion.

Subcutaneously benzylpenicillin are used to cut infiltrates (100 000-200 000 units per 1 ml of 0.25-0.5% solution of novocaine).

Benzylpenicillin novocaine salt is used only intramuscularly. The average therapeutic dose for adults: one-time - 300 000 units, daily - 600 000 units. Children under the age of 1 year - 50 000-100 000 units / kg per day, over 1 year - 50 000 units / kg per day. Multiplicity of administration 3-4 times a day.

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 andmore.

Side effects:

From the digestive system: diarrhea, nausea, vomiting.

Allergic reactions: increased body temperature, urticaria, skin rash, rash on the mucous membranes, joint pain, eosinophilia, angioedema. Cases of anaphylactic shock with a lethal outcome are described.

Effects due to chemotherapeutic action: candidiasis of the vagina, candidiasis of the oral cavity.

From the side of the central nervous system: when benzylpenicillin is used in high doses, and also with endolumbal administration, neurotoxic reactions such as nausea, vomiting, increased reflex excitability, symptoms of meningism, seizures, coma may develop.

Overdose:

Treatment is symptomatic.

Interaction:

Probenecid reduces the tubular secretion of benzylpenicillin, as a result of which the concentration of the latter in the blood plasma increases, the half-life increases.

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

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 drugs when treating 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.

Instructions

Benzylpenicillin (Benzylpenicillinum)