Phenoxymethylpenicillin (Phenoxymethylpenicillinum)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePhenoxymethylpenicillinPhenoxymethylpenicillin
Dosage form: & nbsppills
Composition:

1 tablet contains:

active substance:

phenoxymethylpenicillin

100 mg

250 mg

Excipients:

calcium stearate

1.6 mg

4.0 mg

talc

2.4 mg

6.0 mg

potato starch

32 mg

80 mg

lactose monohydrate (milk sugar)

up to the weight of the tablet:

160 mg

400 mg
Description:

Round tablets white or almost white, flat cylindrical with a bevel. Without risks for a dosage of 100 mg, with a risk for a dosage of 250 mg.

Pharmacotherapeutic group:antibiotic-penicillin biosynthetic
ATX: & nbsp

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

J.01.C.E.02   Phenoxymethylpenicillin

Pharmacodynamics:

Phenoxymethylpenicillin - an antibacterial agent of the penicillin series for ingestion, a derivative of benzylpenicillin (penicillin G). It acts bactericidal, suppresses peptidoglycan synthesis of the bacterial cell wall, which leads to its destruction and to the death of the bacterial cell.

Phenoxymethylpenicillin is active against:

- Gram-positive microorganisms that do not produce penicillinase: Streptococcus spp. (groups A, C, G, H, L and M) (incl. Streptococcus pneumoniae), Staphylococcus spp.; Bacillus anthracis, Corynebacterium spp. (incl. Corynebacterium diphtheriae), Listeria monocytogenes;

- Gram-negative microorganisms (only against strains that do not produce penicillinase): Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Streptobacillus moniliformis;

- anaerobes: Actinomyces bovis., Clostridium spp.

- spirochete: Treponema spp., Leptospira spp.

He current on: strains Staphylococcus spp., producing penicillinase; Mycobacterium tuberculosis, most gram-negative bacteria, viruses, Rickettsia spp., Entamoeba histolytica.

Only isolated strains of enterococci (group streptococci D) are sensitive to the drug.

Phenoxymethylpenicillin is destroyed by the bacterial enzyme penicillinase.

Pharmacokinetics:

Phenoxymethylpenicillin is acid-fast, does not degrade in the acidic environment of the stomach.

Absorption in the alkaline medium of the small intestine 30-60%. It binds to blood plasma proteins by 60-80%. The therapeutic concentrations in the blood plasma are dose-dependent, they are created 30 minutes after taking the drug and remain for 3-6 hours.

The maximum concentration in the blood plasma is reached in 30-45 minutes after taking the drug.

Phenoxymethylpenicillin penetrates into different tissues of the body: the kidneys, liver, skin,lungs, mucous membranes, muscles, small intestine wall and most of the body's liquid media, especially in the presence of inflammatory processes; smaller concentrations are determined in bone tissue.

Passes through the placental barrier, in a small amount found in breast milk.

About 30-35% the drug is metabolized in the liver.

The half-life period is 30-45 minutes and it lengthens in the elderly, with renal insufficiency.

It is excreted mainly by the kidneys in unchanged form (25% the accepted dose) and in the form of metabolites (35% of the accepted dose); about 30% is excreted through the gastrointestinal tract.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to penicillin:

- infections of the upper respiratory tract, including scarlet fever and erysipelas caused by Streptococcus spp. groups A, C, G, H, L them;

- respiratory tract infections, including otitis media, caused by Streptococcus pneumonia;

- skin and soft tissue infections caused by Staphylococcus spp.;

- oral and pharyngeal infections (gingivitis, Vincent's pharyngitis, bacterial stomatitis, periodontitis, actinomycosis);

Prevention:

- relapses of rheumatic attack and / or small chorea;

- bacterial endocarditis in patients with congenital or rheumatic malformations heart before and after small surgical interventions (in t.ch. dental).

Contraindications:

- Hypersensitivity to the components of the drug (including other beta-lactam antibiotics - penicillins, cephalosporins, carbapenems);

- severe infection (including acute stage of severe pneumonia);

- diseases of the gastrointestinal tract, accompanied by vomiting and diarrhea;

- aphthous stomatitis and pharyngitis;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

- gastroparesis, cardiac spasm, or increased intestinal motility;

- children under 3 years.

Carefully:At allergic diseases (bronchial asthma, hay fever, diathesis), allergic reactions (in the anamnesis).
Pregnancy and lactation:

In pregnancy, phenoxymethylpenicillin can be used when the expected benefit to the mother exceeds the potential risk to the fetus.

During the period of taking the drug, breastfeeding should be abolished.

Dosing and Administration:

Inside, 30-60 minutes before meals, squeezed large amounts of liquid.

Adults and children over 12 years

Infections of the upper respiratory tract, including scarlet fever and erysipelas caused by Streptococcus spp. groups A, C, G, H, L and M: 125-250 mg every 6-8 hours.

Respiratory infections, including otitis media, caused by Streptococcus pneumonia: 250-500 mg every 6 h until normal body temperature is restored and for at least 2 more days.

Infections of the skin and soft tissues caused by Staphylococcus spp.: 250-500 mg every 6 to 8 hours.

Infections of the oral cavity and pharynx (gingivitis, Vincent pharyngitis, bacterial disease, periodontal disease, actinomycosis): 250-500 mg every 6-8 hours.

Children from 3 to 6 years administered in a daily dose of 15-30 mg / kg (3-6 tablets of 100 mg, or 1-2 tablets of 250 mg), an average of 100-125 mg (1 tablet of 100 mg or Have2 tablets 250 mg) 3 times a day;

from 6 to 12 years administered in a daily dose of 10-20 mg / kg (3-8 tablets of 100 mg, or 1-3 tablets of 250 mg) on ​​average 200-250 mg (2 tablets of 100 mg or 250 mg 1 tablet) 3 times per day .

Duration of treatment: usually 5-7 days; infections caused by Streptococcus pneumoniae - not less than 10 days.

Children under 3 years preferably the appointment of Phenoxymethylpenicillin in the form of a suspension (the preparation is available as a powder for the preparation of a suspension). The maximum daily dose for children is 50 mg / kg. The maximum single and daily doses for children should not exceed the maximum single and daily doses for an adult.

To prevent recurrence of rheumatic attacks and / or small chorea - 125-500 mg twice a day for a long time.

In patients receiving the drug for the prevention of rheumatic attacks, the dose should be doubled before the scheduled surgical interventions (tonsillectomy, tooth extraction) and in postoperative prevention.

For the prevention of bacterial endocarditis after small surgical interventions (including dental) for adults and older children (body weight greater than 30 kg) with heart defects - appoint 2 g for 1 hour before the intervention and 500 mg every 6 hours after it for 2 days. Children with body weight less than 30 kg: 1 g for 1 hour before the intervention and 500 mg after 6 hours after it.

In severe chronic renal failure and anuria the interval between doses is increased to 12 h.

For patients with hepatic insufficiency the necessary dose of the drug should not be reduced because of the low toxicity of phenoxymethylpenicillin.

Side effects:

Frequency of side effects: "very often" (≥1 / 10), "often" (≥1 / 100, <1/10), "infrequently" (≥1 / 1000, <1/100), "rarely" (≥ 1/10 000, <1/1000), "very rarely" (<1/10 000), including individual messages.

Allergic reactions: infrequently - urticaria, skin hyperemia, angioedema, rhinitis, conjunctivitis, rarely - fever, serum sickness, arthralgia, eosinophilia, very rarely anaphylactic shock.

From the hematopoiesis: rarely - hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia, pancytopenia.

From the digestive system: infrequently, dyspeptic disorders (nausea, vomiting, diarrhea), glossitis, stomatitis, vesiculitis cheilitis (associated with the irritant effect of the drug on the mucous membranes), decreased appetite, dry mouth, impaired taste, rarely pseudomembranous colitis.

Other: rarely - interstitial nephritis, vasculitis.

Overdose:

Symptoms: nausea, vomiting, diarrhea; with a significant overdose - convulsions.

Treatment: cancellation of the drug, gastric lavage, symptomatic therapy.

Phenoxymethylpenicillin is excreted during hemodialysis. There are no specific antidotes.
Interaction:

Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the formation of vitamin K); reduces the effectiveness of oral contraceptives and drugs,in the process of metabolism of which paraaminobenzoic acid is formed.

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

Antacids, glucosamine, laxative drugs, aminoglycosides and food slow down and reduce the absorption of phenoxymethylpenicillin; ascorbic acid - raises it.

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

Diuretics, allopurinol, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that reduce tubular secretion, increase the concentration of phenoxymethylpenicillin and enhance its effect.

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

Special instructions:

In the treatment of severe infections (pneumonia), parenteral forms of penicillin are required. With prospective staphylococcal infections, bacteriological studies are recommended.

Prolonged or repeated administration may cause the development of superinfections, the causative agents of which are resistant strains of bacteria or fungi.

When developing allergic reactions phenoxymethylpenicillin should be canceled and assigned appropriate therapy.

The development of severe persistent diarrhea against the background of drug treatment may be a symptom of pseudomembranous colitis. Since this condition can threaten the life of the patient, the drug should be immediately discontinued and, guided by the results of bacteriological research, prescribe appropriate treatment (for example, vancomycin orally 250 mg 4 times / day).

With prolonged use of the drug, it is necessary to periodically examine the cellular composition of peripheral blood and assess the functional state of the kidneys and liver.

Treatment with phenoxymethylpenicillin can cause a false positive reaction in the nonenzymatic 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.

Effect on the ability to drive transp. cf. and fur:

Care should be taken when driving vehicles, mechanisms and when carrying out work requiring rapidity of psychomotor reactions.

Form release / dosage:Tablets, 100 mg and 250 mg.
Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10 tablets in a contour non-cellular package of paper with a polymer coating on both sides or a polyethylene coating.

1, 2 or 3 contour packagings together with instructions for use put in a pack of cardboard.

200 or 250 contour non-cellular, 460 or 960 cell packs (for tablets dosages of 250 mg and 100 mg, respectively) are placed in carton boxes with an equal number of instructions for use for delivery to hospitals.

Storage conditions:

In a dry, dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date printed on the package.
Terms of leave from pharmacies:On prescription
Registration number:LS-000139
Date of registration:11.02.2010
The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia
Manufacturer: & nbsp
Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia
Information update date: & nbsp20.09.2015
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