Extensillin
Extensillin: 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. In case of impaired renal function
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Extencilline
ATX code: J01CE08
Active ingredient: benzathine benzylpenicillin (benzathine benzylpenicillin)
Manufacturer: Sandoz (Austria), Sanofi-Aventis (France)
Description and photo updated: 2018-26-11
Extensillin is a penicillin antibiotic that is destroyed by penicillinase.
Release form and composition
The drug is produced in the form of a lyophilized powder for preparing an injection solution: from cream to white [600 thousand or 1.2 million International Units (IU) in a 5 ml glass vial, or 2.4 million IU in a 15 ml vial; 50 vials in a cardboard box].
The composition of the drug in 1 bottle:
- active substance: benzathine benzylpenicillin - 600 thousand, 1.2 or 2.4 million IU (equivalent to 459 mg, 918 mg and 1836 mg, respectively);
- additional components: sodium citrate, sodium carboxymethyl cellulose, povidone.
Pharmacological properties
Pharmacodynamics
Benzathine benzylpenicillin is a beta-lactam antibiotic that belongs to the group of long-acting type G penicillins. The substance exhibits a bactericidal effect against sensitive microorganisms due to inhibition of the synthesis of structural components (mucopeptides) of the bacterial cell wall. Extensillin acts on Treponema pallidum and Streptococcus pyogenes, which induce yaws and syphilis.
Pharmacokinetics
After intramuscular (i / m) administration, the active substance is very slowly hydrolyzed, leading to the release of benzylpenicillin. The maximum concentration (C max) of the agent is observed 12-24 hours after the injection. Due to the long half-life of the substance, a stable level of its content in the blood is achieved for a long time. On the 14th day after i / m administration at a dose of 2.4 million IU, the serum concentration of benzathine benzylpenicillin is 0.12 μg / ml. On the 21st day after injection at a dose of 1.2 million IU, the concentration of the active substance in 89–97.4% of patients is 0.06 μg / ml (1 IU = 0.6 μg).
Extensillin is characterized by complete penetration into fluids, very weak into tissues. It binds to plasma proteins by 40-60%. The drug undergoes minor biotransformation, is excreted mainly by the kidneys, passes through the placental barrier and is excreted in breast milk.
Indications for use
According to the instructions, Extensillin is recommended for use for the treatment of infectious lesions, excited by bacteria sensitive to benzathine benzylpenicillin, including:
- articular rheumatism during an exacerbation (prevention);
- syphilis and other diseases caused by treponemes, including pint and yaws (treatment).
Contraindications
Contraindication to the use of Extencillin is hypersensitivity to its constituents, as well as to other beta-lactam antibiotics (cephalosporins and penicillins).
Instructions for the use of Extensillin: method and dosage
Extensillin is injected deep into the / m.
Recommended dosage regimen:
- relapses of articular rheumatism (for prophylaxis): every 15 days for adults 1 administration in a dose of 2.4 million IU, for children (taking into account age) - from 600 thousand to 1.2 million IU;
- yaws and pint - endemic treponematoses (therapy): once for adults at a dose of 1.2–2.4 million IU, for children (weighing less than 45 kg) - from 600 thousand to 1.2 million IU;
- syphilis (therapy): for adults every 8 days, 1 injection at a dose of 2.4 million IU.
Prior to the procedure, the lyophilized powder contained in the vial should be diluted with water for injection at the rate of 2 ml of solvent per 600 thousand IU of the drug. Before administration, the solution must be thoroughly mixed by rolling the bottle with the drug between the palms of the hands, while avoiding excessive foam formation.
Entering Extensillin IV is unacceptable!
Side effects
- digestive system: candidiasis, nausea, diarrhea, vomiting; in some cases - pseudomembranous colitis;
- allergic reactions: fever, urticaria, difficulty breathing, eosinophilia, exfoliative dermatitis, erythema multiforme, Quincke's edema; in isolated cases - anaphylactic shock.
Other symptoms of immunoallergic genesis rarely observed during therapy include: a temporary moderate increase in serum transaminase levels, acute interstitial nephritis, reversible thrombocytopenia, leukopenia, anemia.
The use of high doses of beta-lactam antibiotics, especially in patients with renal insufficiency, can lead to the development of encephalopathy (movement disorders, seizures, impaired consciousness).
In children, there may be local effects on Extencillin injection.
Overdose
There is no data.
special instructions
If any allergic reaction occurs, it is necessary to immediately stop the administration of the drug and begin appropriate treatment.
During the period of Extencillin therapy, there is a threat of developing very severe allergic reactions (including anaphylactic shock), which can be fatal. As a result, when collecting anamnesis, it is necessary to pay special attention to the tolerability of previous treatment with drugs from the penicillin group. If there is a history of allergies to the latter, the use of benzathine benzylpenicillin is categorically contraindicated.
The risk of cross-allergy with cephalosporins should also be taken into account, and therefore, in the presence of a history of allergic reactions to cephalosporins, the use of penicillins is contraindicated.
Patients following a hypersaline diet should remember that a dose of 600 thousand IU of the drug contains sodium in an amount of 5.5 mg or 0.24 mmol.
Application during pregnancy and lactation
Extensillin passes through the placental barrier and enters breast milk. As a result, the use of the drug during pregnancy is allowed only if the expected benefit from the treatment for the mother significantly exceeds the possible threat to the health of the fetus.
If an antibiotic is needed during lactation, breastfeeding should be discontinued.
With impaired renal function
In the presence of renal failure, it is recommended to reduce the daily dose of Extencillin, taking into account creatinine clearance (CC):
- CC less than 10 ml / min - the dose is reduced by 50-75%;
- CC 10-50 ml / min - the dose is reduced by 25%.
Drug interactions
With the simultaneous use of benzathine benzylpenicillin with probenecid, allopurinol, nonsteroidal anti-inflammatory drugs (salicylates, phenylbutazone, indomethacin), there is a risk of competitive inhibition of the excretion of drugs from the body.
Analogs
Extensillin analogues are: Benzicillin-1, Bicillin-1, Retarpen 2.4 and Retarpen 1.2.
Terms and conditions of storage
Store in a place protected from light and moisture, out of the reach of children, at a temperature not exceeding 25 ° C.
The shelf life of the lyophilisate is 4 years, the prepared solution is no more than 24 hours if stored in a refrigerator.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Extensillin
There are very few reviews of Extensillin. Patients note the effectiveness of the drug when used according to the indications for use, as well as a convenient dosage regimen and good tolerability of therapy. Almost all patient complaints are related to the lack of the drug on sale.
Price for Extensillin in pharmacies
The price of Extensillin is unknown, due to the fact that the drug is currently 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!
