Phenoxymethylpenicillin
Phenoxymethylpenicillin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Phenoxymethylpenicillin
ATX code: J01CE02
Active ingredient: phenoxymethylpenicillin (Phenoxymethylpenicillin)
Manufacturer: SINTEZ, JSC (Russia)
Description and photo updated: 2018-26-11
Phenoxymethylpenicillin is a natural antibacterial drug that belongs to the group of penicillins, which are destroyed by penicillinase.
Release form and composition
Dosage forms of Phenoxymethylpenicillin:
- tablets: almost white or white, round, cylindrical, beveled; at a dose of 250 mg - with a dividing line (100 mg each: 10 pcs. in blisters, in a cardboard bundle 1, 2 or 3 packs, in a cardboard box 250 or 960 packs; 10 pcs. in contoured non-cell packs, in cardboard box 250 packs; 250 mg: 10 pcs. in blisters, in a cardboard box 1, 2 or 3 packs, in a cardboard box 200 or 460 packs; 10 pcs. in blister-free blisters, in a cardboard box 200 packs);
- powder for preparation of suspension for oral administration: loose mass of white or almost white color, has a specific odor [in single-dose sachets: 2.5 g each, in a carton box 30 sachets, complete with or without a plastic cup; 5 g each, in a cardboard box 15 or 30 sachets, complete with or without a plastic cup; 40 g (600 mg of phenoxymethylpenicillin) in vials, in a cardboard box 1 bottle complete with a measuring spoon].
1 tablet contains:
- active substance: phenoxymethylpenicillin - 100 mg or 250 mg;
- auxiliary components: potato starch, calcium stearate, lactose monohydrate (milk sugar), talc.
1 sachet of powder (2.5 / 5 g) for preparation of oral suspension contains:
- active substance: phenoxymethylpenicillin - 37.5 / 75 mg;
- auxiliary components: citric acid monohydrate, sucrose (sugar), sodium benzoate, raspberry flavor.
1 ml of the finished suspension in the vial contains the active ingredient: phenoxymethylpenicillin - 12 mg.
Pharmacological properties
Pharmacodynamics
Phenoxymethylpenicillin - a penicillin antibiotic, is a derivative of benzylpenicillin (penicillin G). It has a bactericidal effect due to the suppression of peptidoglycan synthesis of the bacterial cell wall, causing the destruction of the walls and death of the bacterial cell.
The following microorganisms show sensitivity to the drug:
- gram-positive microorganisms that do not produce penicillinase: Streptococcus pneumoniae and other Streptococcus speciales (spp.) groups A, C, G, H, L and M, Staphylococcus spp., Corynebacterium spp., Corynebacterium diphtheriae, Listeria, Baccytogenus;
- gram-negative microorganisms (strains that do not produce penicillinase): Haemophilus influenzae, Neisseria meningitidis, Neisseria gonorrhoeae, Streptobacillus moniliformis;
- spirochetes: Leptospira spp., Treponema spp.;
- anaerobes: Clostridium spp., Actinomyces bovis.
The drug is active only against certain strains of enterococci (group D streptococci).
Penicillinase-producing strains of Staphylococcus spp., Most viruses and gram-negative bacteria, Mycobacterium tuberculosis, Entamoeba histolytica, Rickettsia spp. Are not sensitive to phenoxymethylpenicillin.
The action of a bacterial enzyme, penicillinase, causes the destruction of phenoxymethylpenicillin.
Pharmacokinetics
Phenoxymethylpenicillin is resistant to the acidic environment of the stomach.
After oral administration, 30-60% of the dose is absorbed in the alkaline medium of the small intestine. The maximum concentration of active agent is achieved through the plasma 1 / 2 hour and maintained for 3-6 hours. The concentration level of the drug is in direct proportion to the size of the dose taken. Simultaneous food intake reduces the absorption of phenoxymethylpenicillin.
Plasma protein binding is 60 to 80%.
The substance slowly penetrates into mucous membranes and most body fluids, into the parenchyma of the kidneys, liver and lungs, into the skin, muscles and walls of the small intestine. In the kidneys, it is determined in high concentrations, in the skin, liver and the wall of the small intestine - in smaller ones. The content of phenoxymethylpenicillin in bones is insignificant. The antibiotic crosses the placental barrier, small amounts are found in breast milk.
In the liver, about 30–35% of the dose taken is metabolized.
T 1/2 (half-life) - from 1 / 2 to 3 / 4 hour.
With renal failure and in elderly patients, T 1/2 is lengthened.
Excretion: through the kidneys it is excreted unchanged - 25% and in the form of metabolites - 35% of the dose taken, through the intestines - about 30%.
Indications for use
According to the instructions, Phenoxymethylpenicillin is indicated for the treatment of mild to moderate infectious and inflammatory diseases caused by microorganisms sensitive to it, including the following:
- angina, scarlet fever, bronchitis, pneumonia, otitis media;
- purulent diseases of soft tissues and skin;
- tetanus;
- syphilis, gonorrhea;
- anthrax.
In addition, Phenoxymethylpenicillin is prescribed to prevent infection in the following cases:
- open wounds of various etiologies, including bites;
- burns;
- rheumatic attack and / or small chorea, glomerulonephritis, polyarthritis, endocarditis - prevention of streptococcal infections and their complications;
- tonsillectomy, tooth extraction and other minor surgical interventions in patients with congenital or acquired rheumatic heart diseases - to prevent bacterial endocarditis before and after the procedure;
- rheumatism - to prevent exacerbations;
- sickle cell anemia in children - for the prevention of pneumococcal pneumonia.
Contraindications
Absolute:
- pathologies of the gastrointestinal tract, which are accompanied by vomiting and diarrhea;
- achalasia of the cardia, gastroparesis, increased intestinal motility;
- severe course of infectious diseases, including the acute stage of severe pneumonia;
- pharyngitis, aphthous stomatitis;
- syndrome of glucose-galactose malabsorption, lactose intolerance, lactase deficiency;
- hypersensitivity to other beta-lactam antibiotics, including penicillins, cephalosporins, carbapenems;
- children's age: for powder - under 3 months; for tablets - under 3 years old;
- breast-feeding;
- individual intolerance to the components of the drug.
Phenoxymethylpenicillin should be prescribed with caution for allergic diseases (hay fever, bronchial asthma, diathesis), a history of allergic reactions, and during pregnancy.
The suspension should be taken with caution in patients with diabetes mellitus.
Instructions for the use of Phenoxymethylpenicillin: method and dosage
Pills
Phenoxymethylpenicillin tablets are taken orally, 1 / 2–1 hour before meals, with plenty of liquid.
Recommended dosage for patients over 12 years old:
- upper respiratory tract infections caused by Streptococcus spp. groups A, C, G, H, L and M (including scarlet fever and erysipelas): 125-250 mg 3-4 times a day. The tablets should be taken at intervals of 8-6 hours, respectively;
- Respiratory tract infections, including otitis media, caused by Streptococcus pneumoniae: 250-500 mg every 6 hours. After the restoration of normal body temperature, the intake should be continued for at least 2 days;
- infections of soft tissues and skin caused by Staphylococcus spp.: 250-500 mg 3-4 times a day (with an interval of 8-6 hours, respectively);
- bacterial infections of the oral cavity and pharynx - stomatitis, periodontitis, gingivitis, Vincent's pharyngitis, actinomycosis: 250–500 mg at intervals of 6–8 hours.
Recommended dosage of Phenoxymethylpenicillin for children under 12 years of age:
- children 3-6 years old: the daily dose is determined at the rate of 15-30 mg per 1 kg of the child's weight and divided into 3 doses every 8 hours;
- children 6-12 years old: at the rate of 10-20 mg per 1 kg of body weight per day, the dose received is divided into 3 doses per day.
The maximum daily dose for children should not exceed 50 mg per 1 kg of the child's weight, and the maximum single dose should not exceed the same dose for adults.
The doctor prescribes the duration of the course of therapy individually. Usually it is 5-7 days, in the treatment of infectious diseases caused by Streptococcus pneumoniae - at least 10 days.
Prevention of recurrence of small chorea and / or rheumatic attack is carried out in a dose of 125-500 mg 2 times a day for a long period. Patients receiving phenoxymethylpenicillin for the prevention of rheumatic fever should double the dose before elective surgery (tonsillectomy, tooth extraction) and continue taking the double dose after surgery.
Adults and children weighing more than 30 kg, with congenital or rheumatic heart defects, for the prevention of bacterial endocarditis during minor surgical interventions (including dental) immediately 1 hour before the operation are prescribed 2000 mg of the drug. During two of it after the operation, the patient continues to receive a dose of 500 mg every 6 hours. Children with a body weight of up to 30 kg are shown to take 1000 mg 1 hour before and 500 mg 6 hours after surgery.
In severe chronic renal failure and anuria, Phenoxymethylpenicillin is used in the usual dose, but the interval between doses is increased to 12 hours.
Powder for oral suspension
The finished suspension is taken orally, 1 / 2-1 hour before meals, with plenty of liquid.
To prepare the suspension, pour 2.5 ml of chilled boiled water into a glass to dissolve the contents of one package at a dose of 37.5 mg or 5 ml for a sachet at a dose of 75 mg. To the contents of the vial (600 mg phenoxymethylpenicillin), add 50 ml of water. Then mix thoroughly until a homogeneous suspension is obtained. After each use, rinse the glass and measuring spoon with water and store in a clean place.
Recommended dosage of Phenoxymethylpenicillin for adults and children over 5 years old:
- mild form of upper respiratory tract infections, scarlet fever, erysipelas caused by Streptococcus spp.: 150-300 mg at intervals of 6-8 hours. Course duration - 10 days;
- respiratory tract infections, otitis media caused by Streptococcus pneumoniae: 300-600 mg at intervals of 6 hours before and for at least 2 days after the restoration of normal body temperature;
- mild infectious pathologies of the skin and soft tissues caused by Staphylococcus spp.: 300-600 mg at intervals of 6-8 hours. The course of treatment is 7 days;
- mild and moderate severity of fusospirochetosis, gingivitis, Vincent's pharyngitis: 300-600 mg at intervals of 6-8 hours;
- prevention of recurrence of small chorea and rheumatic fever: 150-300 mg 2 times a day for a long period.
Recommended dosage for children under 5 years of age:
- children from 3 to 12 months of age: 75 mg with an interval of 6 hours;
- children from 1 to 5 years: 150 mg at intervals of 6 hours.
The doctor prescribes the duration of the course of treatment depending on the clinical indications.
When performing surgeries on the upper respiratory tract and in dentistry in patients with congenital or acquired (including rheumatic) heart defects, phenoxymethylpenicillin is used to prevent bacterial endocarditis. Adults are prescribed 2000 mg of the drug 1 hour before the operation and 1000 mg 6 hours after its completion. Children with a body weight of up to 27 kg take 1000 mg 14 hours before the operation, then 500 mg after 6 hours after the operation.
Treatment of patients with severe chronic renal failure is carried out in usual doses, increasing the interval between doses to 12 hours.
Side effects
- on the part of the hematopoietic organs: rarely - agranulocytosis, thrombocytopenia, hemolytic anemia, pancytopenia, leukopenia;
- allergic reactions: infrequently - rhinitis, conjunctivitis, skin hyperemia, urticaria, angioedema; rarely - fever, arthralgia, eosinophilia, serum sickness; very rarely - anaphylactic shock;
- from the digestive system: infrequently - dry mouth, nausea, vomiting, taste disturbances, diarrhea, loss of appetite, glossitis, stomatitis, vesicular cheilitis; rarely - pseudomembranous colitis;
- others: rarely - vasculitis, interstitial nephritis.
Overdose
Symptoms: diarrhea, nausea, vomiting; against the background of a significant overdose - convulsions.
Treatment: there is no specific antidote. Gastric lavage is recommended immediately. Cancel phenoxymethylpenicillin. Appointment of symptomatic therapy, if necessary, a hemodialysis session.
special instructions
For the treatment of severe infectious diseases (including pneumonia), it is necessary to use parenteral forms of penicillin.
If you suspect staphylococcal infections, the appointment of the drug should be made based on the results of bacteriological studies.
Long-term use of phenoxymethylpenicillin must be accompanied by regular monitoring of peripheral blood, the functional state of the kidneys and liver.
It should be borne in mind that long-term use or frequent administration of the drug increases the risk of developing superinfections caused by strains of bacteria or fungi resistant to phenoxymethylpenicillin.
When symptoms appear, the development of allergic reactions requires immediate withdrawal of Phenoxymethylpenicillin.
Due to the existing risk of developing pseudomembranous colitis against the background of the use of non-steroidal anti-inflammatory drugs (NSAIDs) and the associated threat to the patient's life, one should carefully approach the diagnosis of severe persistent diarrhea that occurs during antibiotic treatment. When diarrhea appears, taking the tablets should be stopped and a bacteriological examination of the discharge should be carried out. Further therapy is carried out in accordance with the test results.
Ninhydrin urine amino acids, non-enzymatic urine glucose, and urobilinogen can give false positive results.
Patients with diabetes should take into account that the content of carbohydrates in the maximum daily dose of Phenoxymethylpenicillin in the form of a suspension corresponds to 13.1 XE (bread unit).
Influence on the ability to drive vehicles and complex mechanisms
Taking Phenoxymethylpenicillin can negatively affect the speed of psychomotor reactions, therefore, patients are advised to be careful when driving and working with complex mechanisms.
Application during pregnancy and lactation
The use of an antibiotic during gestation is allowed in cases where the expected therapeutic effect for the mother is much higher than the potential threat to the fetus.
The use of the drug during lactation is contraindicated, if it is necessary to prescribe Phenoxymethylpenicillin - breastfeeding should be canceled.
Pediatric use
It is contraindicated to prescribe the drug in the form of tablets for the treatment of children under the age of 3 years, powder - up to 3 months.
Subject to these age restrictions, phenoxymethylpenicillin is prescribed for the treatment of children according to indications.
With impaired renal function
In severe chronic renal failure and anuria, the usual dose of phenoxymethylpenicillin is prescribed, but the interval between doses is increased to 12 hours.
Drug interactions
- drugs that cause a decrease in tubular secretion, allopurinol, phenylbutazone, diuretics, other NSAIDs: help to increase the concentration of phenoxymethylpenicillin and enhance its action;
- ascorbic acid: increases the rate of absorption of the drug and the amount of absorbed substance;
- cephalosporins, cycloserine, rifampicin, vancomycin and other bactericidal antibiotics, aminoglycosides: able to demonstrate synergism with phenoxymethylpenicillin;
- macrolides, tetracyclines, chloramphenicol, lincosamides and other bacteriostatic antibiotics: cause antagonism of action, which results in partial or complete absence of the therapeutic effect of each of the drugs;
- indirect anticoagulants: against the background of suppression of intestinal microflora, their effect is enhanced, the formation of vitamin K decreases;
- ethinyl estradiol: may increase the risk of breakthrough bleeding;
- oral contraceptives: there is a decrease in contraceptive activity;
- drugs metabolized to form para-aminobenzoic acid: their effectiveness is inhibited;
- antacids, laxatives, glucosamine, aminoglycosides: cause a slowdown and decrease in the absorption of the antibiotic;
- allopurinol: the risk of developing allergic reactions in the form of a skin rash is increased.
Analogs
Analogues of Phenoxymethylpenicillin are Cliacyl, Vepikombin, Ospin, Megacillin shouted, Retarpen, Sulacillin, Extensillin, Bicillin, Benzylpenicillin, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at a temperature of 15 to 25 ° C, protected from moisture and light.
Shelf life: tablets - 4 years; powder for suspension for oral administration - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about phenoxymethylpenicillin
Most of the reviews about Phenoxymethylpenicillin are positive. Patients point to the high efficacy of the drug in the treatment of diseases of an infectious genesis, but at the same time note the need for strict adherence to the dosage regimen prescribed by the doctor.
Reports of the development of adverse events are rare; more often, the antibiotic is well tolerated. The cost of the drug is called affordable, but they say that recently it has been difficult to acquire.
Price for Phenoxymethylpenicillin in pharmacies
The price of Phenoxymethylpenicillin is currently unknown because the drug is not available for sale.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
