Description
The powder is white to yellowish-white in color, with a tendency to caking.
Compound
1 bottle contains 2.0513 g of benzathine benzylpenicillin (corresponding to 2,400,000 IU).
Excipients: simethicone, mannitol, povidone, buffered sodium citrate, pH 7.
Pharmacotherapeutic group
Antibacterial agents for systemic use. Penicillins sensitive to beta-lactamases.
ATX code: J01CE08.
Pharmacological properties
Pharmacodynamics
Mechanism of action
The mechanism of action of benzathine benzylpenicillin is based on the inhibition of bacterial cell wall synthesis during the growth phase through blockade of penicillin binding proteins (PBPs), such as transpeptidases. This leads to a bactericidal effect.
Relationship between pharmacokinetics and pharmacodynamics
Efficacy largely depends on the length of time during which the level of the active substance remains above the MIC of the pathogen.
Mechanisms of resistance development
Resistance to benzathine benzylpenicillin may be due to the following mechanisms:
- inactivation by beta-lactamase: benzathine benzylpenicillin is not resistant to beta-lactamase and therefore has no effect on bacteria that produce beta-lactamase (for example, staphylococci or gonococci);
- decreased affinity of PBPs for benzathine benzylpenicillin: acquired resistance of pneumococci and some other streptococci to benzathine benzylpenicillin is caused by modifications of existing PBPs as a result of mutation. However, the resistance of methicillin (oxacillin)-resistant staphylococci is due to the formation of additional PBP with reduced affinity for benzathine benzylpenicillin;
- in gram-negative bacteria, insufficient penetration of benzathine benzylpenicillin through the outer cell wall can lead to insufficient inhibition of PBP;
- benzathine benzylpenicillin can be actively transported out of the cell by efflux pumps.
Benzathine benzylpenicillin is partially or completely cross-resistant to other penicillins and cephalosporins.
Limit values
Breakpoint values are based on values for benzylpenicillin. The following minimum inhibitory concentrations (MICs) have been established for sensitive and resistant microorganisms.
Minimum inhibitory concentrations (MICs) established by the European Committee on Antibiotic Susceptibility Assessment (EUCAST).
| Microorganism | Sensitive(mg/l) | Resistant(mg/l) |
| Staphylococcus spp. | ≤ 0,12 | > 0,12 |
| Streptococcus spp. groups A, B, C, G | ≤ 0,25 | > 0,25 |
| Streptococcus pneumoniae # | ≤ 0,06 | > 2 |
| Streptococcus Viridans group | ≤ 0,25 | > 2 |
| Neisseria meningitidis | ≤ 0,06 | > 0,25 |
| Neisseria gonorrhoeae | ≤ 0,06 | > 1 |
| Gram-negative anaerobes | ≤ 0,25 | > 0,5 |
| Gram-positive anaerobes | ≤ 0,25 | > 0,5 |
| Limit values regardless of type* | ≤ 0,25 | > 2 |
*based on serum pharmacokinetic parameters.
Prevalence of acquired resistance
The prevalence of acquired resistance in individual species varies geographically and over time, and local information on antibiotic resistance should be obtained, especially for severe infections. If local rates of antibiotic resistance call into question the effectiveness of benzylpenicillin, appropriate expert advice should be sought. Particularly in cases of severe infection or treatment failure, a microbiological diagnosis should be made to identify the pathogen and its susceptibility to benzylpenicillin. ° Data are derived from published literature, clinical experience and therapeutic recommendations.
^ Collective name for a heterogeneous group of streptococcal species. The degree of resistance may vary depending on the presence of streptococci
Pharmacokinetics
Suction
After intramuscular administration, benzylpenicillin is absorbed very slowly. Retarpen is the longest-acting penicillin depot drug. For many indications, 1-2 injections per month are sufficient. Consequently, the frequency of injections and local reactions can be reduced.
The time to reach peak concentration after injection is 24 hours in children and 48 hours in adults.
Distribution
About 55% of the administered dose is bound to plasma proteins. When using high doses of penicillin, therapeutically effective concentrations are achieved even in hard-to-reach places, such as heart valves, bone tissue, cerebrospinal fluid, empyema, etc.
Benzylpenicillin penetrates the placental barrier. 10-30% of the concentration of benzylpenicillin in maternal plasma was found in the fetal circulation. High concentrations are also achieved in amniotic fluid. In contrast, transfer into breast milk is low. The volume of distribution is about 0.3-0.4 l/kg in adults and about 0.75 l/kg in children.
Biotransformation and excretion
Excretion to a large extent (50 - 80%) occurs unchanged through the kidneys (85 - 95%) and, to a lesser extent, in the active form with bile (about 5%). The half-life in adults with normal renal function is approximately 30 minutes.
Special patient groups
Premature and newborn babies: due to the immaturity of the kidneys and liver at this age, the half-life is up to 3 hours or more. Therefore, the dosing interval should be at least 8-12 hours (depending on the degree of maturity of the kidneys and liver).
Elderly patients: Elimination processes may also be slower. The dose should be adjusted depending on the state of renal function.
Preclinical data
Reproductive studies in mice, rats and rabbits have shown no adverse effects on fertility or the fetus. There are no long-term studies in laboratory animals regarding carcinogenicity, mutagenicity and fertility.
Indications for use
Retarpen is used in adults, adolescents, children and newborns for the treatment and prevention of infections caused by pathogens sensitive to penicillin:
for treatment:
- erysipelas
- syphilis: early syphilis (primary and secondary)
- latent syphilis (exception: neurosyphilis and the presence of detected pathology in the cerebrospinal fluid)
- yaws
- pint
for prevention:
- rheumatic fever (chorea, rheumatic carditis)
- poststreptococcal glomerulonephritis
- erysipelas
When using Retarpen, general guidelines for the proper use of antibacterial drugs should be taken into account.
Doses and method of administration
The dose depends on the severity and type of infection, age and liver and kidney function of the patient. For some special indications (eg syphilis, rheumatic fever prophylaxis), international guidelines should be taken into account in addition to national or local guidelines.
Standard dose
Adults and adolescents: 1,200,000 IU once per week.
Children weighing > 30 kg: 1,200,000 IU once weekly.
Overweight children< 30 кг: 600000 МЕ один раз в неделю.
To prevent recurrence of the disease in patients with streptococcal infection, the shortest period of treatment should be 10 days. This can be achieved by a single administration of 600,000 IU of Retarpen, 1,200,000 IU of Retarpen or 2,400,000 IU of Retarpen.
Treatment of syphilis
primary and secondary stages
Adults and teenagers: 1 x 2,400,000 IU.
Treatment is repeated if clinical symptoms return or laboratory tests are persistently positive.
Duration of therapy: single dose.
last stage (latent seropositive syphilis)
Adults and adolescents: 2,400,000 IU once per week.
Children: 50,000 IU/kg body weight, but not more than 2,400,000 IU.
Duration of therapy: 3 weeks.
congenital syphilis (without neurological symptoms)
Newborns and young children: 1 x 50,000 IU/kg body weight.
Duration of therapy: single dose.
Treatment of yaws, pints
Adults and teenagers: 1 x 1,200,000 IU.
Children weighing > 30 kg: 1 x 1,200,000 IU.
Overweight children< 30 кг: 1 х 600000 МЕ.
Duration of therapy: single dose.
Prevention of rheumatic fever, post-streptococcal glomerulonephritis and erysipelas:
Adults and adolescents: 1 x 1,200,000 IU every 3-4 weeks.
Children weighing > 30 kg: 1 x 1,200,000 IU every 3-4 weeks.
Overweight children< 30 кг: 1 х 600000 МЕ каждые 3-4 недели.
Duration of therapy:
a) in the absence of involvement of heart damage in the pathological process: at least 5 years or up to 21 years.
b) with transitional involvement of heart damage in the pathological process: at least 10 years or up to 21 years.
c) with constant involvement of heart damage in the pathological process: at least 10 years or up to 40 years; sometimes lifelong prevention is necessary.
Special patient groups
If kidney function is impaired
|
Retarpen dose for adults, adolescents and children based on creatinine clearance |
|||
| Creatinine clearance, ml/min | 100-60 | 50-10 | <10 |
| Serum creatinine, mg% | 0,8-1,5 | 1,5-8,0 | 15 |
| Share of the usual daily dose of Retarpen | 100% | 75% |
20-50% (max. 1000000-3000000 IU/day) |
| Interval between injections | 1 single injection | 1 single injection | 2-3 single injections |
Benzylpenicillin can be eliminated by hemodialysis. There are no data on the effect of hemodialysis on plasma benzylpenicillin levels. Therefore, the question of prescribing Retarpen to patients on hemodialysis should be considered on a case-by-case basis.
In case of liver dysfunction
In cases of very severe liver and kidney dysfunction, delayed breakdown and elimination of penicillins may occur.
Mode of application
For intramuscular injections only. Retarpen should not be injected into areas with poor blood supply.
Injections should be administered deep intramuscularly into the upper outer gluteal quadrant, with the needle directed towards the iliac crest or the ventrogluteal region according to Hochstetter. The puncture should be made as perpendicular to the surface of the skin as possible, and the drug should be administered as far from large vessels as possible. A piston test should always be performed before administration. If blood aspiration or pain occurs during the injection, the injection should be stopped.
For children, injection into the anterior outer region of the thigh (quadriceps femoris) is preferable. If muscle mass is well developed, the deltoid muscle can be used for injections; in this case, attention should be paid to the radial nerve.
In infants and young children, to avoid damage to the sciatic nerve, the upper outer gluteal quadrant area should be used as an injection site only in exceptional cases (eg, extensive burns).
The maximum permissible injection volume for one site is 5 ml. Therefore, no more than 5 ml of the prepared injection suspension should be injected into one site at any time.
The drug should be administered as slowly as possible, without applying significant effort. After the injection, do not massage or rub the injection site.
When administered intramuscularly, severe reactions may occur at the injection site, especially in young children. Where possible, alternative treatments, such as intravenous administration of a suitable penicillin, should be considered, taking into account, first and foremost, the therapeutic indication and treatment regimen and weighing the risk-benefit ratio.
Preparation of the suspension
The contents of the 2,400,000 IU vial are diluted in at least 5 ml of water for injection. Shake vigorously for 20 seconds and immediately inject using a minimum 0.9 mm needle. Only one dose is taken. Only freshly prepared suspensions are used. Before administering the dose, you must ensure that the end of the injection needle is not in a blood vessel. With repeated doses, it is necessary to change the injection site.
Side effect
Contraindications
Hypersensitivity to benzathine benzylpenicillin, to any other penicillin or to any of the excipients listed in the "Composition" section.
- History of severe immediate hypersensitivity reaction (eg, anaphylactic) to other beta-lactam antibiotics (eg, cephalosporins, carbapenem or monobactam).
Overdose
In very high doses, penicillins can cause nervous excitability or epileptiform seizures. If overdose is suspected, clinical monitoring and symptomatic treatment are recommended. Benzylpenicillin can be eliminated by hemodialysis.
Precautionary measures
Retarpen should not be injected into areas with poor blood supply.
Before starting treatment, information should be collected about the patient's history of hypersensitivity reactions to penicillins, cephalosporins or other beta-lactam antibiotics.
Severe and sometimes fatal hypersensitivity reactions have occurred in patients treated with penicillins. These reactions are more common in people with a history of hypersensitivity to penicillin and in individuals susceptible to atopy.
If allergic reactions occur, treatment should be discontinued and appropriate treatment prescribed. Before starting treatment, if possible, a hypersensitivity test should be performed.
The patient should be aware of the possible occurrence of allergic reactions and the need to report them.
Caution should be exercised in patients suffering from:
allergic diathesis or bronchial asthma. There is an increased risk of developing a hypersensitivity reaction.
renal failure;
liver dysfunction.
Some exposed patients may experience severe immediate hypersensitivity reactions after the first administration. In this regard, the patient should remain under observation for half an hour after the injection.
When treating syphilis, as a result of the bactericidal effect of penicillin on pathogens, the Jarisch-Herxheimer reaction may develop.
2 to 12 hours after administration, headaches, fever, sweating, chills, myalgia, arthralgia, nausea, tachycardia, high blood pressure followed by hypotension may appear. These symptoms disappear after 10-12 hours.
Patients should be informed that this is a common, transient complication of antibiotic therapy. To suppress or weaken the Jarisch-Herxheimer reaction, appropriate therapy should be prescribed.
For long-term treatment (more than 5 days), it is recommended to carry out blood and kidney function tests.
It is necessary to monitor the growth of microbial resistance. If secondary infections develop, appropriate measures should be taken.
It is necessary to consider the possibility of developing severe and persistent diarrhea, pseudomembranous colitis associated with the administration of an antibiotic (bloody/mucous, watery diarrhea, dull pain, diffuse abdominal pain or colic, fever, sometimes tenesmus), such symptoms can be life-threatening. In these cases, the drug should be immediately discontinued and therapy should be prescribed based on the results of the detected pathogens. Antiperistaltic drugs are contraindicated.
Neurological complications cannot be ruled out in patients with congenital syphilis, and forms of penicillin that produce higher concentrations in the cerebrospinal fluid should be used in such patients.
For diseases such as acute pneumonia, empyema, sepsis, meningitis or peritonitis, which require higher serum concentrations of penicillin, alternative treatment, for example, with a water-soluble alkaline salt of benzylpenicillin, should be considered.
Application Notes
If accidentally administered subcutaneously, painful lumps may occur. In such cases, ice packs help.
In case of unintentional intravascular injection, Hoyne's syndrome (symptoms of shock with mortal fear, confusion, hallucinations, possible cyanosis, tachycardia and movement disorders, but without the development of vascular insufficiency) caused by microemboli of the suspension may develop. Symptoms resolve within an hour. If the case is severe, parenteral sedatives are recommended.
In case of inadvertent intra-arterial injection, especially in children, serious complications may develop, such as vascular occlusions, thrombosis and gangrene. The initial signs are pale spots on the skin of the buttocks. As a result of high injection pressure, retrograde flow of fluid into the common iliac artery, aorta, or spinal arteries may occur.
Repeated injections into a limited area of muscle tissue, which are associated with long-term depot penicillin therapy (for example, in the treatment of syphilis), can cause tissue damage and increase local vascularization.
Subsequent injections increase the likelihood of the suspension entering the blood, either through direct injection into a blood vessel, due to the pressure of the injected suspension itself, or through depot migration. Therefore, during long-term therapy, it is recommended to administer each injection at a great distance from the previous injection.
Impact on diagnostic laboratory test results
- Patients receiving 10 million IU (equivalent to 6 g) benzylpenicillin or more per day often develop a positive direct Coombs test (≥ 1% before<10%). После отмены пенициллина, результаты прямой антиглобулиновый пробы могут оставаться положительными от 6 до 8 недель.
- Determination of protein in urine using precipitation techniques (sulfosalicylic acid, trichloroacetic acid), the Folin-Cicalteu-Lowry method or the biuret method may lead to false-positive results. Therefore, determination of protein in urine must be carried out using other methods.
- Determination of urinary amino acids using the ninhydrin method may also give false-positive results.
- Penicillins bind to albumin. When using the electrophoresis method to determine albumin, false bisalbuminemia can be obtained.
- During benzylpenicillin therapy, nonenzymatic detection of glucose and urobilinogen in urine may give false-positive results.
- During benzylpenicillin therapy, determination of 17-ketosteroids (using the Zimmerman test) in urine may give increased values.
In case of renal dysfunction, delayed excretion of povidone must be taken into account.
Due to the presence of povidone in the drug, it cannot be ruled out that after frequent or long-term use, in very rare cases, povidone may be deposited in the reticuloendothelial system or locally, leading to the development of tumor-like granulomas.
Interaction with other drugs
Simultaneous administration of benzylpenicillin is not recommended with:
Based on the general principle of not combining bactericidal and bacteriostatic antibiotics, Retarpen should not be combined with bacteriostatic antibiotics.
Caution should be exercised when used together:
Probenecida
The use of probenecid results in inhibition of benzylpenicillin secretion by the renal tubules, resulting in increased serum concentrations and prolongation of the half-life. Probenecid also inhibits the transport of penicillin from the cerebrospinal fluid, so simultaneous administration of probenecid reduces further penetration of benzylpenicillin into brain tissue.
Methotrexate
When used simultaneously with Retarpen, the excretion of methotrexate is reduced. This may lead to increased toxicity of methotrexate. Combination with methotrexate is not recommended.
Anticoagulants
The simultaneous use of Retarpen with oral anticoagulants may enhance their effect and increase the risk of bleeding. It is recommended to regularly monitor the international normalized ratio (INR) and adjust the dosage of vitamin K antagonists accordingly during and after treatment with Retarpen.
Compatibility Information
Compatibility data with water for injection is available.
Pregnancy and breastfeeding
Pregnancy
Benzathine benzylpenicillin crosses the placenta. Animal studies do not indicate direct or indirect harmful effects due to reproductive toxicity. Retarpen can be used during pregnancy for appropriate indications and taking into account the benefits and risks.
Breast-feeding
Benzathine benzylpenicillin passes into breast milk in small quantities. Concentrations in breast milk can range from 2 to 15% of maternal serum concentrations.
Although no adverse effects have been reported to date in breastfed infants, the possibility of sensitization or harmful effects on intestinal microflora should be considered. Breastfeeding should be stopped if diarrhea, candidiasis or rash occurs in the baby.
Infants who are also receiving formula should not be fed breast milk during treatment with Retarpen. Breastfeeding can be resumed after cessation of treatment after 24 hours.
Fertility
No fertility studies have been conducted in humans. Reproduction studies in mice, rats and rabbits did not reveal any negative effects on fertility. There are no long-term fertility studies in laboratory animals.
50 bottles along with instructions for use in a cardboard box.
Manufacturer
Sandoz GmbH, Biochemistrasse 10, A-6250 Kundl, Austria.
A bottle of powder for the preparation of a suspension for intramuscular administration contains 1.2 or 2.4 million IU of the active substance benzathine benzylpenicillin .
Release form
Powder for preparing a suspension for intramuscular administration.
pharmachologic effect
Pharmacodynamics and pharmacokinetics
Active antibacterial substance - benzathine benzylpenicillin . The main component is obtained from mold fungi. It is bactericidal against microbial cells.
The mechanism of action of the antibiotic Retarpen is based on suppression of the process of synthesizing the bacterial cell wall. Lasts for a long time. Effective against gram-positive flora, spore-forming, anaerobic rods, gram-negative flora, treponema.
Retarpen does not act on staphylococci that produce penicillinase.
Indications for use
Retarpen is prescribed for diseases caused by streptococci, Treponema pallidum: rheumatism , erysipelas.
The drug is prescribed for the prevention of postoperative complications.
Contraindications
Retarpen is not used in case of hypersensitivity to benzylpenicillin, hay fever .
The drug is contraindicated in.
Side effects
Long-term therapy with Retarpen can lead to the development superinfections . During treatment, headaches may occur, , anemia, stomatitis , exfoliative , arthralgia , fever , anaphylactic shock , hypocoagulation, leukopenia.
Retarpen, instructions for use (Method and dosage)
The drug is administered exclusively intramuscularly.
When two injections are prescribed, they are given in different buttocks.
For the treatment of congenital syphilis For young children and newborns, 1.2 million units are administered once or divided into two injections.
Primary seronegative syphilis: Retarpen is administered intramuscularly at a dose of 2.4 million units.
Secondary fresh syphilis and primary seropositive syphilis: 2.4 million units, after 7 days the injection is repeated.
Tertiary syphilis: 2.4 million units each, course of therapy is 3-5 weeks.
Flambesia: 1-2 injections of 1.2 million units.
Scarlet fever, acute tonsillitis, erysipelas, wound infections: treatment begins with benzylpenicillin, then Retarpen is administered.
Seizure prevention: intramuscularly 2.4 million units every 15 days.
Overdose
May cause encephalopathy, confusion, movement disorders, neuromuscular irritability and seizures.
Treatment according to symptoms. Maintenance therapy, hemodialysis. There is no specific antidote.
Interaction
Aminoglycosides, cephalosporins and other bactericidal antibacterial agents have synergistic effect .
Tetracycline antibiotics, lincosamides, macrolide antibiotics, and other bacteriostatic drugs have a strong antagonistic action .
Retarpen reduces prothrombin index , suppresses intestinal microflora, increases efficiency indirect anticoagulants , has little effect on the effectiveness of hormonal contraceptives.
Diuretics, phenylbutazone, tubular secretion blockers, non-steroidal drugs increase the concentration of penicillins. With simultaneous administration of allopurinol, the risk of developing allergies in the form of skin rash increases.
Terms of sale
Requires a prescription.
Storage conditions
In a dark place, out of reach of children, at a temperature of no more than 30 degrees Celsius.
Best before date
No more than 4 years.
special instructions
Administration of the drug Retarpen intravenously or subcutaneously is unacceptable. If the drug accidentally enters the lumen of the vessel, there is a disturbance in visual perception, a transient feeling of depression and anxiety.
The package contains 5 bottles of 1.2 IU. The active ingredient is benzathine benzylpenicillin. Manufacturer: Pfizer (under US license) India. Our specialists will help you find the nearest pharmacy in Moscow, St. Petersburg, Yekaterinburg, Krasnoyarsk, Novosibirsk, Samara, Tyumen, Chelyabinsk, Saratov, Engels, Belarus (Minsk), where you can buy Penidure 1.2 million IU. If your request comes from other regions, we will be able to help you individually.
For decades, the drug Penidure (complete Retarpen) has occupied a worthy place in the arsenal of infectious disease specialists, venereologists, urologists, rheumatologists and pediatricians. Its main active ingredient, benzathine benzylpenicillin, is capable of suppressing the growth of bacteria. The advantage of this antibiotic is its ability to accumulate in the body and have an effect on pathogens for a long time.
The recommendation to buy Retarpen (Penidure) is often heard by patients who have been diagnosed with syphilis. The drug has been successfully used to treat this “popular” venereal disease since the middle of the last century. In Europe, America and African countries, it became the leading remedy in the fight against this contagious and insidious disease, dangerous with serious consequences (tertiary syphilis) in the absence of adequate treatment. The cause of the disease is the bacteria Treponema pallidum, which can enter the body through sexual contact with an already infected partner, as well as through blood transfusion. Syphilis can also be transmitted to a child during pregnancy from a sick mother.
What diseases does Penidure treat (a complete analogue of Retarpen):
The antibiotic Penidure/Retarpen is also effective in the treatment of scarlet fever, a disease from which thousands of people of all ages died a hundred years ago. This drug, which can kill streptococcal bacteria that cause scarlet fever, tonsillitis and erysipelas, is also prescribed for children.
Rheumatism is another serious consequence of an attack on the body by colonies of streptococcal bacteria. This disease, which often develops as a complication after an infectious disease, affects not only the joints, but also the heart, skin and brain. Swelling and pain in the joints are only external manifestations of rheumatism. Injections of the drug are usually prescribed to prevent relapses of rheumatism.
Instructions for use of the drug Penidure:
An objective decision about the need to use antibiotics must be made by a doctor, who will determine in what quantity Retarpen or its full analogue Penidure should be purchased, and also prescribe a dose and treatment regimen. As a rule, when treating primary syphilis, 1-2 injections are prescribed; in case of advanced disease, at the stage of tertiary syphilis, the course of treatment can reach 5 weeks, 1-2 amps each. weekly. When treating scarlet fever and acute tonsillitis, adult patients are given 1-2 injections per week, children - 0.6 million IU once every 3 days or daily.
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Name: RETAPEN, Sandoz
pharmacodynamics. Benzathine benzylpenicillin is a long-acting beta-lactam antibiotic of the penicillin type G group. It has a bactericidal effect against sensitive microorganisms by suppressing the synthesis of cell wall mucopeptides.
Active against gram-positive pathogens: Staphylococcus spp.(penicillinase-non-forming), Streptococcus spp., including Streptococcus pneumoniae, Corynebacterium diphtheriae, anaerobic spore-forming rods, Bacillus anthracis, Clostridium spp., Actinomyces israelii; gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, and also regarding Treponema spp. Strains are resistant to the drug Staphylococcus spp., producing penicillinase, which destroys benzylpenicillin. Due to its long-lasting effect, the drug is used to treat infections caused by Streptococcus spp. And Treponema pallidum.
Pharmacokinetics. When administered intramuscularly, benzathine benzylpenicillin is very slowly absorbed from the injection site, providing a prolonged effect.
Cmax in blood plasma is achieved 12-24 hours after injection. Long T½ provides a stable and long-lasting concentration of the drug in the blood plasma: on the 14th day after administration of 2,400,000 IU, the concentration in the blood plasma is 0.12 mcg/ml. The degree of binding to plasma proteins is ≈55%.
Benzathine benzylpenicillin penetrates the placental barrier in small quantities, as well as into breast milk. Biotransformation of the drug is insignificant. It is excreted mainly by the kidneys in unchanged form; up to 33% of the administered dosage is excreted within 8 days.
Composition and release form
por. d/p susp. d/in. 2400000 IU fl., No. 50
No. UA/4005/01/01 from 03/23/2011 to 03/23/2016
Indications
treatment of infections caused by microorganisms sensitive to the drug:
- acute tonsillitis;
- scarlet fever;
- erysipelas (chronic), erysipeloid;
- infected wounds and bite wounds;
- syphilis and other diseases caused by treponemes (yaws, endemic syphilis, pinta).
Prevention (used only as a prophylactic):
- rheumatic diseases (Sydenham's chorea, rheumatic carditis);
- poststreptococcal glomerulonephritis;
- scarlet fever (after contact with a sick person);
- recurrence of erysipelas;
- syphilis (after contact with a patient).
Application
Before administration, it is necessary to collect a history of drug tolerance from the patient and conduct a preliminary intradermal test to determine its tolerance.
Retarpen is used only intramuscularly!
To prepare the suspension, add 5 ml of water for injection to the vial. Use only freshly prepared suspension, which must be shaken for 20 seconds and injected urgently using a needle with a thickness of at least 0.9 mm. Retarpen is injected into the upper quadrant of the gluteal muscle. If repeated injections are necessary, the injection site should be changed. It is necessary to suction immediately before administering the medicine to avoid the needle getting into the blood vessels. No more than 5 ml of suspension should be injected into one place at a time.
Treatment of syphilis
Preventive treatment. 2,400,000 IU of Retarpen (divided into 2 injection sites) once.
Primary syphilis. 2,400,000 IU of Retarpen (divided into 2 injection sites) with an interval of 7 days (course - 2 injections).
Secondary fresh and early latent syphilis. 2,400,000 IU of Retarpen (divided into 2 injection sites) with an interval of 7 days (course - 3 injections).
Treatment of yaws and pinta (endemic treponematoses). 1 injection of Retarpen 2400000 IU once.
Treatment of other infections caused by microorganisms sensitive to the drug (acute tonsillitis, scarlet fever, erysipelas, erysipeloid, infected wounds and bite wounds). 1 injection of Retarpen 2,400,000 IU weekly.
Prevention of relapses of rheumatic attack and rheumatic endocarditis, chorea, post-streptococcal glomerulonephritis. 1 injection of Retarpen 2400000 IU 1 time every 4 weeks.
The duration of the warning is set individually.
Prevention of recurrence of erysipelas. For seasonal relapses - 1 injection of Retarpen 2,400,000 IU once every 4 weeks for 3-4 months annually; for frequent relapses - 1 injection of Retarpen 2,400,000 IU once every 3-4 weeks for 2-3 years.
Prevention of scarlet fever in persons who have had contact with patients. 1 injection of Retarpen 2,400,000 IU weekly. For streptococcal diseases (including tonsillitis, scarlet fever), the course of treatment should be at least 10 days to prevent complications. Basically, 1 injection of Retarpen 2,400,000 IU is enough.
Prevention of infections during tonsillectomy or after tooth extraction. 1 injection of Retarpen 2,400,000 IU every 7-14 days until complete recovery.
Contraindications
hypersensitivity to beta-lactam antibiotics (penicillins and cephalosporins). For the treatment of diseases requiring high concentrations of penicillin in the blood plasma and cerebrospinal fluid (severe pneumonia, empyema, sepsis, pericarditis, meningitis, peritonitis, arthritis, congenital neurosyphilis), water-soluble sodium salt of benzylpenicillin should be used. History of severe allergic reactions and asthma. Childhood.
Side effects
allergic reactions: skin rash, urticaria, itching, fever, joint pain, angioedema, exfoliative dermatitis, erythema multiforme, difficulty breathing, anaphylactic shock with collapse, anaphylactoid reactions (asthma, purpura, gastrointestinal symptoms). When treating syphilis, the Jarisch-Herxheimer reaction may develop due to the release of endotoxins.
From the gastrointestinal tract: stomatitis, glossitis, nausea, vomiting, diarrhea, candidiasis, cases of the development of pseudomembranous colitis have been described when using benzathine benzylpenicillin.
In rare cases, a moderate transient increase in the level of transaminases in the blood plasma is observed.
From the hematopoietic system: positive Coombs test, hemolytic anemia, leukopenia, thrombocytopenia, neutropenia, prolonged bleeding time, in isolated cases - agranulocytosis.
From the nervous system: headache, dizziness, neuropathy.
From the urinary system: nephropathy. In rare cases, acute interstitial nephritis is observed.
Other: reactions at the injection site. Long-term use of antibiotics can lead to the development of secondary superinfections caused by resistant microorganisms and fungi.
The drug contains povidone, so very rarely the latter can accumulate in the reticuloendothelial system or local depots, which can lead to the development of granuloma.
special instructions
the drug is used only intramuscularly. Before starting treatment with Retarpen, patients should be tested for drug tolerance. When prescribing medication to patients with diabetes mellitus, it is necessary to take into account the reduced absorption of Retarpen from the muscle depot.
The drug should be prescribed with caution if there is a tendency to allergic reactions or liver failure.
If allergic reactions occur, therapy should be stopped and symptomatic treatment prescribed with epinephrine, antihistamines and corticosteroids.
With accidental intravascular administration of Retarpen, a feeling of depression, fear, anxiety may appear, hallucinations, fainting, development of cyanosis, tachycardia, motor impairment (syndrome) may appear. Hoigne). Symptoms disappear within 1 hour. In case of severe reaction, administration of sedatives is indicated.
During long-term treatment with the drug, periodic monitoring of blood counts and kidney function is recommended.
For sexually transmitted diseases with suspected syphilis, microscopic and serological studies should be performed before starting therapy, and then for 4 months.
To suppress or alleviate the Jarisch-Herxheimer reaction, when using Retarpen for the first time, 50 mg of prednisolone or its equivalent is administered. In patients with syphilis at a stage manifested by damage to the cardiovascular system, blood vessels and meninges, the Jarisch-Herxheimer reaction can be prevented by using prednisolone 50 mg/day or an equivalent steroid for 1-2 weeks.
During long-term treatment with the drug, the possibility of the development of resistant microorganisms and fungi should be taken into account.
In the presence of severe and persistent diarrhea, the possibility of developing pseudomembranous colitis caused by the use of antibiotics should be considered. In this case, you should immediately stop administering the medication and prescribe appropriate therapy. In this case, drugs that inhibit peristalsis are contraindicated.
During pregnancy and breastfeeding. The drug is not intended for the treatment of syphilis during pregnancy.
Benzathine benzylpenicillin passes into breast milk. Breastfeeding should be stopped during treatment.
Children. The drug is not prescribed to children.
The ability to influence the reaction speed when driving a vehicle or operating machinery. Unknown.
Interactions
penicillin drugs that have a bactericidal effect should not be used in combination with bacteriostatic antibiotics. Combination with other antibiotics is possible when a synergistic effect or some additional result is expected. The individual components of the therapeutic combination should be prescribed at full dose (the dosage of the more toxic component may be reduced if a synergistic effect is shown).
One should keep in mind the ability to competitively inhibit the process of excretion from the body when using benzathine benzylpenicillin simultaneously with anti-inflammatory, antirheumatic and antipyretic drugs (indomethacin, phenylbutazone, salicylates in high doses) or probenecid.
When used simultaneously, the effectiveness of indirect anticoagulants increases.
The use of benzathine benzylpenicillin may in some cases cause a decrease in the effectiveness of oral contraceptives.
To prevent unwanted chemical reactions, the Retarpen suspension should not be mixed with other injection solutions.
Benzathine benzylpenicillin should be administered with caution to patients receiving digoxin as there is a risk of bradycardia during concomitant use.
Allopurinol will increase the risk of allergic reactions (skin rashes).
Overdose
the use of beta-lactam antibiotics in high doses, especially in liver failure, can cause the development of encephalopathy (confusion, impaired movement). Penicillins in extremely high doses can cause neuromuscular irritability or epileptic-like seizures. Potentially, overdose may cause gastrointestinal symptoms and electrolyte imbalance.
Treatment: symptomatic and supportive therapy, hemodialysis. A specific antidote is unknown.
Storage conditions
at a temperature not exceeding 30 ° C in a place protected from light.
Retarpen is a broad-spectrum antibiotic. Used to treat diseases complicated by Treponema pallidum, streptococcus, and staphylococcus.
Indications for use
The drug is prescribed for the treatment of syphilis, rheumatism, scarlet fever, acute tonsillitis and to eliminate the inflammatory process caused by erysipelas. It can also be used to treat open, infected wounds. Often the medicine is prescribed to prevent infection with syphilis and scarlet fever, and to prevent the recurrence of erysipelas.
Composition of the drug
One bottle contains 2.4 million IU of benzathine benzylpenicillin.
Medicinal properties
The active component of the drug, retarpen 2.4, is made on the basis of mold, which has antiseptic properties against pathogenic microorganisms. Once in the body, the antibiotic inhibits the synthesis of the cell wall of the harmful microbe. The product has a long-lasting effect in the body. Retarpen helps to cope with many types of pathogenic microorganisms except staphylococci that synthesize penicillinase. The drug belongs to the class of natural antibiotics. It easily penetrates the body tissues and is excreted mainly by the kidneys and partly by the liver. In infants and the elderly, elimination is somewhat slower.
Release forms
Average price: 3500 rub.
The product is available in powder form, from which a long-acting liquid is prepared for intramuscular administration. The powder is packaged in bottles with a capacity of 15 ml (2,400,000 IU of active substance, which is why the drug received its name - retarpen 2 4). In a hospital setting, you can purchase medicine in 50 bottles in one large box. The color of the powder is white, sometimes with a creamy tint.
Mode of application
Retarpen 2 4 is injected exclusively deep into the muscles. If more than one injection is indicated, then injections should be given alternately in different buttocks. If a baby is diagnosed with congenital syphilis, then the child is given 1,200,000 IU of the drug (half a bottle) once or in two injections. If primary seronegative syphilis is detected in an adult, then 2,400,000 IU of antibiotic should be administered once. For secondary syphilis, the entire bottle is administered once, and a second injection is given a week later in the same amount. For tertiary syphilis, 2.4 million IU is administered, the course of therapy lasts for 21-37 days. For the treatment of flambesia, only 1-2 injections of 1.2 million IU are required once. For the treatment and prevention of attacks of rheumatism of the joints, one bottle of diluted product is administered every 15 days. For scarlet fever, sore throat and erysipelas, benzylpenicillin is first prescribed, and then, if there is no proper treatment result, retarpen is prescribed.
During pregnancy and breastfeeding
Teratogenic and embryotoxic effects of benzylpenicillin are completely absent. This means that if it is really necessary to take this antibiotic during pregnancy, then it is possible. The active substance can pass into breast milk, so it is better to temporarily interrupt breastfeeding during drug therapy.
Contraindications
Do not use if you have bronchial asthma, hay fever, or if you are hypersensitive to the active ingredient.
Precautionary measures
The drug is used with caution by allergy sufferers and patients with allergic diathesis. With such diagnoses, the drug is administered under control, and the patient is observed for half an hour after administration of the antibiotic. You should always have adrenaline ready for injection. To avoid pinching the sciatic nerve in a child, injections should be given exclusively in the upper outer gluteal quadrant.
Cross-drug interactions
In combination with cephalosporin antibiotics and rifampicin, the bactericidal effect on the body increases. Tetracyclines, lincosamides and chloramphenicol, on the contrary, weaken the effects of retarpen 2 4 on the body. Allopurinol in combination with benzathine benzylpenicillin may cause or worsen an allergic reaction. Diuretics and tubular secretion blockers increase the concentration of penicillins. Also, the drug itself worsens the intestinal microflora and lowers the prothrombin index.
Side effects
Overdose
In case of overdose, the development of encephalopathy, impaired coordination of movements, convulsions, impaired neuromuscular communication, and delirium is noted.
Conditions and shelf life
The medicine is stored in a dark corner at a temperature of up to 30 degrees Celsius. Shelf life: 4 years from the date of manufacture indicated on the package. Keep away from children.
Analogs
Bicillin
Sintez OJSC, Russia
Price – 10-20 rubles
The active ingredient is benzathine benzylpenicillin. It is a complete analogue of retarpen and is available in powder form for intramuscular administration.
Pros:
- Low cost
- Proven effectiveness.
Minuses:
- There is only one form of application
- Allergic reactions often occur.
Amosin
Sintez OJSC, Russia
Price – 50-70 rubles per package
The active ingredient is amoxicillin. Refers to antibiotics with a pronounced bactericidal effect. Amosin is indicated for meningitis, gonorrhea, sepsis and leptospirosis. Available in the form of powder, suspension and solution for injection.
Pros:
- Cheap
- Copes well with diseases.
Minuses:
- Weakens the effect of oral contraceptives
- Lots of side effects.