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

Clinical and pharmacological group: & nbsp

Penicillins

Included in the formulation

Phenoxymethylpenicillin

powder inwards

SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Phenoxymethylpenicillin

pills inwards

SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

АТХ:

J.01.C.E. Penicillins sensitive to beta-lactamases

J.01.C.E.02 Phenoxymethylpenicillin

Pharmacodynamics:

Antibiotic group of biosynthetic penicillins. The mechanism of action is associated with inhibition of bacterial cell membrane synthesis.

The mechanism of antibacterial action of penicillins is associated with:

- blockade of the enzyme transpeptidase, which provides the connection of peptidoglycan chains with pentaglycine bridges, the final stage of the synthesis of the peptidoglycan polymer;

- inhibition of the endogenous inhibitor of autolysins, which play a key role in the cleavage of peptidoglycan in the fission of bacterial cells.

As a result, a breakdown in the structure of the peptidoglycan of a microbial cell and the subsequent death of bacteria occur. This determines the bactericidal effect.

Acid-resistant.

The spectrum of action is predominantly Gram-positive. It is active against aerobic gram-positive bacteria: Staphylococcus spp., Streptococcus spp. (incl.Streptococcus pneumoniae), Enterococcus spp. (some strains), Clostridium spp., Corynebacterium spp., Erysipelothrix rhusiopathiae, Listeria spp., Bacillus anthracis, Actinomyces spp .; aerobic gram-negative bacteria: Neisseria meningitidis, Neisseria gonorrhoeae; Pasteurella multocida, Streptobacillus spp .; anaerobic bacteria: Peptococcus spp., Peptostreptococcus spp., Fusobacterium spp., Clostridium spp. Also active in relation to Spirullinum minus, Treponema pallidum, Borrelia spp., Leptospira interrogans.

To phenoxymethylpenicillin it is stable Staphylococcus spp. (strains producing penicillinase).

Pharmacokinetics:When ingested quickly absorbed (30-60%) in the alkaline environment of the small intestine. The therapeutic concentration in the blood is created after 30 minutes and remains for 3-6 hours. The half-life from the plasma is 30-45 minutes. At 60-80% is bound by plasma proteins. High concentrations are recorded in the kidneys, smaller - in the liver, skin, small intestine wall. Passes through the placental barrier, in a small amount found in breast milk. Metabolised in the liver (30-35%). In newborns, seniors and with renal failure, the half-life period is prolonged. Excreted mainly in the urine (secreted in the renal tubules): 25% - unchanged and 35% - in the form of metabolites; about 30% is excreted with feces.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to phenoxymethylpenicillin, including bronchitis, pneumonia, tonsillitis, scarlet fever, otitis media, gonorrhea, syphilis, tetanus, anthrax, purulent skin and soft tissue diseases.

For the purpose of prevention: wounds of various etiologies (including bites); burns; prevention of streptococcal infections and their complications (including rheumatism / rheumatic attack, small chorea, polyarthritis, glomerulonephritis, endocarditis); prevention of bacterial endocarditis in patients with congenital or acquired rheumatic heart defects before and after small surgical interventions (tonsillectomy, tooth extraction); prevention of pneumococcal pneumonia in children with sickle-cell anemia; prevention of exacerbations of rheumatism.

ICD-10

I.A00-A09.A05.1 Botulism

I.A20-A28.A22 anthrax

I.A20-A28.A26.9 Erisipeloid, unspecified

I.A20-A28.A27.9 Leptospirosis, unspecified

I.A20-A28.A27.0 Leptospirosis ictero-hemorrhagic

I.A30-A49.A35 Other forms of tetanus

I.A30-A49.A36.9 Diphtheria, unspecified

I.A30-A49.A38 Scarlet fever

I.A30-A49.A42 Actinomycosis

I.A30-A49.A46 Erys

I.A30-A49.A49.1 Streptococcal infection, unspecified

I.A50-A64.A53.9 Syphilis, unspecified

I.A50-A64.A54.9 Gonococcal infection, unspecified

I.A65-A69.A69.2 Lyme disease

VI.G00-G09.G00.1 Pneumococcal meningitis

VI.G20-G26.G25.5 Other types of chorea

VIII.H65-H75.H66.9 Other otitis media, unspecified

IX.I00-I02.I01 Rheumatic fever with involvement of the heart

IX.I00-I02.I00 Rheumatic fever without mention of involvement of the heart

IX.I30-I52.I33 Acute and subacute endocarditis

IX.I80-I89.I88 Nonspecific lymphadenitis

X.J00-J06.J01 Acute Sinusitis

X.J00-J06.J02.9 Acute pharyngitis, unspecified

X.J00-J06.J03.9 Acute tonsillitis, unspecified

X.J00-J06.J04.0 Acute laryngitis

X.J10-J18.J18 Pneumonia without clarification of the pathogen

X.J10-J18.J18.0 Bronchopneumonia, unspecified

X.J30-J39.J31.2 Chronic pharyngitis

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J35.0 Chronic tonsillitis

X.J30-J39.J37.0 Chronic laryngitis

X.J40-J47.J40 Bronchitis, not specified as acute or chronic

XI.K00-K14.K05.3 Chronic periodontitis

XI.K00-K14.K12 Stomatitis and related lesions

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.M05-M14.M06.9 Rheumatoid arthritis, unspecified

XIII.M70-M79.M79.0 Rheumatism, unspecified

XIV.N00-N08.N00 Acute nephritic syndrome

XIV.N00-N08.N05 Nephritic syndrome, unspecified

XIX.S00-S09.S06 Intracranial injury

XIX.T08-T14.T14.0 Superficial injury of unspecified area of the body

XIX.T08-T14.T14.1 Open wound of unspecified area of the body

XIX.T20-T32.T30 Thermal and chemical burns, unspecified

XIX.T79.T79.3 Post-traumatic wound infection, not elsewhere classified

XXI.Z20-Z29.Z29.2 Another type of preventive chemotherapy

Contraindications:Hypersensitivity(including other β-lactam antibiotics - penicillins, cephalosporins, carbapenems), aphthous stomatitis and pharyngitis, severe infections, gastrointestinal diseases accompanied by vomiting and diarrhea.

Carefully:Use with caution in patients with allergic diseases (bronchial asthma, hay fever, diathesis), with anamnesis for allergic reactions to cephalosporin antibiotics (possibly a cross-allergic reaction).

Pregnancy and lactation:

Category of recommendations FDA is not defined. Phenoxymethylpenicillin penetrates the placental barrier, in small quantities with breast milk. To date, there has been no adverse effect of phenoxymethylpenicillin on the fetus or the baby.

During pregnancy and lactation (breastfeeding), phenoxymethylpenicillin can be used according to indications. However, before starting treatment, the expected benefit of therapy for the mother and the potential risk to the fetus or child should be carefully weighed.

In experimental studies, embryotoxic, teratogenic and mutagenic effects of phenoxymethylpenicillin have not been established.

Dosing and Administration:Inside (0.5-1 h before meals). Dosage regimen and duration of treatment is determined individually depending on the nature of the disease, age, etc. The average single dose for adults and children over 12 years is 0.25-0.5 g, daily - 1.5 g or more. When treating oral penicillin preparations, it is usually recommended to divide the total daily dose by 2-3 doses. Children under 1 year in a daily dose of 20-30 mg / kg, from 1 to 6 years - 15-30 mg / kg, from 6 to 12 years - 10-20 mg / kg. The course of treatment is usually 5-7 days. Treatment should be continued within 3 days after the disappearance of symptoms. To prevent complications in patients with streptococcal infections, treatment should last at least 10 days. For prophylaxis postoperativebacterial complications for adults and children weighing 30 kg or more for 30-60 minutes before surgery - 2 grams, then 0.5 g every 6 hours for 2 days or longer.

Side effects:

Allergic reactions: itching, urticaria, skin hyperemia, rhinitis, conjunctivitis, bronchospasm, erythema multiforme, exfoliative dermatitis, fever, arthralgia, angioedema, anaphylactic shock, anaphylactoid reactions.

On the part of the digestive system: anorexia, nausea, vomiting, flatulence, diarrhea, dry mouth, taste disorder, glossitis, stomatitis, vesiculitis cheilitis (associated with irritant effect on mucous membranes), pseudomembranous colitis.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): leukopenia, agranulocytosis, thrombocytopenia, eosinophilia, hemolytic anemia, pancytopenia.

Other: interstitial nephritis, pharyngitis, vasculitis, superinfection.

Overdose:

Symtomas: excitation of the central nervous system (agitation, hallucinations, convulsions).

Treatment: hemodialysis, symptomatic therapy.

Interaction:

Indomethacin reduces excretion (competition for tubular transport systems), increases the activity of phenoxymethylpenicillin, increases the risk of side effects.

Neomycin for oral administration may reduce the absorption of phenoxymethylpenicillin, leading to a weakening effect.

Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin), aminoglycosides - Synergy of action; basteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonism.

Diuretics, allopurinol, phenylbutazone, NSAIDs (eg, indomethacin) and others drugs that reduce tubular secretion (competition for tubular transport systems) increase the concentration of phenoxymethylpenicillin. Increase the risk of side effects.

Phenoxymethylpenicillin weakens the effect hormonal contraceptives and drugs, in the process of metabolism which forms para-aminobenzoic acid.

Increases the risk of bleeding "breakthrough" against the background of taking ethinyl estradiol.

Antacids, glucosamine, laxatives, food, aminoglycosides slow down and reduce absorption; ascorbic acid it increases.

Probenecid reduces excretion.

Allopurinol increases the risk of allergic reactions (skin rashes).

Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the formation of vitamin K);

Special instructions:

When developing allergic reactions phenoxymethylpenicillin should be abolished and appropriate therapy prescribed.

It is necessary to avoid the use of phenoxymethylpenicillin in combination with bacteriostatic antibiotics.Combination with other antibiotics is allowed if an additive or synergistic effect is expected.

Phenoxymethylpenicillin is not prescribed for vomiting and diarrhea. In these cases, absorption is disrupted.

With prolonged treatment, the possibility of growing resistant strains of bacteria and fungi should be considered.

With persistent diarrhea, the possibility of developing pseudomembranous colitis should be considered.

With prolonged use, periodic monitoring of the pattern of peripheral blood and indicators of liver and kidney function is recommended.

When using phenoxymethylpenicillin, false-positive results of the reaction are possible in the non-enzymatic determination of glucose in urine and in the analysis for urobilinogen and the results of quantitative determination of amino acids in urine by the ninhydrin method

With the proposed staphylococcal infection, bacteriological testing is recommended. Before the planned surgical interventions (tonsillectomy, extraction of teeth, etc.), in the postoperative period, patients who receive penicillin for antirheumatic prophylaxis should double the dose.

Do not assign phenoxymethylpenicillin with violations of absorption from the digestive tract.

In severe pneumonia, empyema, sepsis, pericarditis, meningitis, arthritis and osteomyelitis, in an acute stage, it is necessary to switch to parenteral administration of penicillins. In combination with other antibiotics with proven synergistic effect, the dose of a more toxic preparation can be reduced. In patients with anuria, the dose should be reduced or the interval between doses should be increased.

Instructions

Phenoxymethylpenicillin (Phenoxymethylpenicillinum)