Retarpen instructions for use analogues. Complete instructions for using retarpen, list of analogues, reviews and prices
Syphilis and other diseases caused by spirochetes (yaws, pinta); acute tonsillitis, scarlet fever, erysipelas, wound infection (in combination with rapidly absorbed penicillin preparations); as monotherapy for the prevention of relapses of rheumatism, scarlet fever (contact with the patient), erysipelas and infections during tonsillectomy, tooth extraction (preferably in combination with rapidly absorbing penicillin preparations).
Release form of the drug Retarpen 2.4
powder for the preparation of a suspension for intramuscular administration of prolonged action 2.4 million IU; bottle (bottle) 15 ml, box (box) 50;
Pharmacodynamics of the drug Retarpen 2.4
It disrupts the synthesis of peptidoglycan, the supporting polymer of the cell wall. Active against gram-positive microorganisms, incl. Staphylococcus spp. (except for penicillinase-producing strains), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming bacilli Bacillus anthracis, some gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), Actinomyces israelii, and Treponema spp. Not effective against viruses (causative agents of influenza, polio, smallpox, etc.), mycobacterium tuberculosis, protozoa, rickettsia, fungi, as well as most gram-negative microorganisms.
Pharmacokinetics of the drug Retarpen 2.4
When administered intramuscularly, it creates a depot, slowly hydrolyzes to form benzylpenicillin, which is gradually absorbed and maintains a therapeutic concentration in the blood. long time. Cmax is reached 12–24 hours after injection.
On the 14th day after administration of 2.4 million units (1 unit - 0.6 mcg), the serum concentration is 0.12 mcg/ml; on the 21st day after administration of 1.2 million units - 0.06 mcg/ml.
Plasma protein binding - 40–60%. Diffusion in liquid is complete, in tissue - weak. Passes through the placental barrier, penetrates into breast milk.
Metabolized slightly, excreted mainly by the kidneys unchanged. Over 8 days, up to 33% of the administered dose is released.
Contraindications to the use of the drug Retarpen 2.4
Hypersensitivity (including to other beta-lactams).
Side effects of the drug Retarpen 2.4
From the gastrointestinal tract: stomatitis, glossitis.
Allergic reactions: anaphylaxis, urticaria, angioedema, erythema multiforme, exfoliative dermatitis.
Other: increased body temperature, arthralgia, Jarisch-Herxheimer reaction, pain and infiltrates at the injection site.
Method of administration and dosage of the drug Retarpen 2.4
V/m. Retarpen 1.2 is intended for the treatment of children and adults, Retarpen 2.4 - for adults. Adults with primary syphilis: once 2.4–4.8 million IU in 2 different places, for secondary syphilis: 2.4 million IU, per course 3 injections with an interval of 1 week.
For the treatment of yaws and pints: children 1.2 million IU once, adults 1.2–2.4 million IU once; people who have had contact with patients or patients with a latent form of infection - 1/2 dose.
For the treatment of infections caused by penicillin-sensitive pathogenic microorganisms (acute tonsillitis, scarlet fever, erysipelas and wound infections): children under 12 years of age - 1.2 million IU every 2-4 weeks depending on the severity of the infection, adults - 1.2-2 .4 million IU once a week.
Prevention of relapses of rheumatic attack and rheumatic endocarditis: children under 12 years of age 0.6–1.2 million IU every 4 weeks, adults - 1.2–2.4 million IU every 4 weeks.
To prevent scarlet fever in people who have had contact with sick people: children 1.2 million IU every 3–4 weeks, adults - 2.4 million IU.
For the prevention of infectious complications after tooth extraction, tonsillectomy and other minor surgical interventions: children and adults - 1.2 million IU, during extensive surgical interventions to prevent infectious complications for children - 1.2 million IU, adults - 1.2–2.4 million IU every 7–14 days until recovery.
Overdose of Retarpen 2.4
Not described.
Interactions of the drug Retarpen 2.4 with other drugs
Competitively inhibits the excretion of anti-inflammatory, antirheumatic and antipyretic drugs (indomethacin, phenylbutazone and salicylates). Should not be combined with bacteriostatic drugs.
When used in combination with other antibiotics, the dose of the more toxic component may be reduced if a synergistic effect is shown).
Precautions when taking the drug Retarpen 2.4
Before starting therapy, microscopic and serological studies are necessary for at least 4 months.
When prescribed to patients diabetes mellitus Long-term absorption of Retarpen from the muscle depot should be taken into account. Prescribe with caution to patients prone to allergic reactions.
If such reactions develop, therapy is stopped (administration of adrenaline, antihistamines and corticosteroids is necessary).
During long-term antibiotic therapy, it is necessary to pay attention to the excessive proliferation of resistant microorganisms.
Special instructions when taking the drug Retarpen 2.4
Shake the prepared suspension vigorously before use. The drug cannot be administered subcutaneously, intravenously, intralumbarally or into the body cavity.
Storage conditions for the drug Retarpen 2.4
List B.: In a place protected from light, at a temperature below 25 °C.
Shelf life of the drug Retarpen 2.4
The drug Retarpen 2.4 belongs to the ATX classification:
J Antimicrobials for systemic use
J01 Antimicrobials for systemic use
J01C Beta-lactam antibiotics - penicillins
J01CE Penicillins sensitive to beta-lactamases
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 due to 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
Prevalence of acquired resistance individual species characterized by geographic and temporal dependence, and local information on antibiotic resistance should be obtained, especially in the case of 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 not revealed negative influence 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, you should take into account general guidelines on the appropriate use of antibacterial drugs.
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 consistently 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 children younger age: 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.
Retarpen is an antibiotic drug from the penicillin group.
Release form and composition
The drug is produced in the form of a powder for the preparation of an injection solution.
1 bottle contains the active substance - benzathine benzylpenicillin:
- Retarpen 1.2 – 1.2 million IU (10 ml bottles, 1 or 100 bottles in cardboard boxes);
- Retarpen 2.4 – 2.4 million IU (15 ml in bottles, 1 or 50 bottles in cardboard boxes).
Indications for use
Retarpen is prescribed for the treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the action of the drug, such as:
- Pint, yaws;
- Syphilis (as monotherapy);
- Acute tonsillitis, scarlet fever.
The drug is also used for prophylaxis in the following cases:
- Repeated attacks after acute rheumatic fever;
- Wound infections;
- Recurrences of erysipelas;
- Infections after tooth extraction or tonsillectomy.
Contraindications
The use of Retarpen is contraindicated in case of hypersensitivity to beta-lactam antibiotics (pecillins and cephalosporins).
The drug should be prescribed with caution if the patient:
- Pseudomembranous colitis;
- Tendency to allergic reactions;
- Kidney failure.
Retarpen can be used by pregnant women only if the expected benefit to the mother is higher than the potential risk to the fetus.
If it is necessary to prescribe the drug to nursing women, the issue of interrupting breastfeeding should be decided.
Directions for use and dosage
The drug is administered deeply intramuscularly (intravenous administration is prohibited).
For syphilis, Retarpen is prescribed to adults:
- For preventive treatment – 2.4 million IU once;
- For primary – 2 injections with an interval of 7 days at a dosage of 2.4 million IU;
- For early latent and secondary - 3 injections with an interval of 7 days, 2.4 million IU.
For preventive therapy of a child born to a mother with syphilis who has not undergone treatment, Retarpen is prescribed 3 injections with an interval of 7 days at a dose of 5000 IU/kg body weight. The dosage should be divided in half and administered into different buttocks. For preventive therapy of a child due to seroresistance or insufficient treatment, the mother is given 2 injections with an interval of 7 days.
For the treatment of pint and yaws (endemic treponematoses) the following is prescribed:
- Children - 1.2 million IU once;
- Adults – 2.4 million IU.
For other infections (wound infections in the acute phase, erysipelas, scarlet fever, acute tonsillitis), depending on the severity of the condition, the following is prescribed:
- Children under 12 years old - 600 thousand IU every 3 days or 1.2 million IU every 2-4 weeks;
- Adults – 1.2 million IU or 2.4 million IU once a week.
To prevent the development of repeated attacks after acute rheumatic fever, Retarpen is used once every 3 weeks:
- Children weighing less than 25 kg - 600 thousand IU;
- Children weighing more than 25 kg - 1.2 million IU;
- Adolescents and adults – 2.4 million IU each.
The duration of prophylaxis is determined by the doctor individually.
When prescribing the drug to patients with impaired renal function, it is possible to adjust the dosage regimen, determined by the value of creatinine clearance:
- With CC 10-50 ml per minute - 75% of the recommended daily standard dose;
- With CC less than 10 ml per minute - 25-50%.
For the prevention of recurrence of erysipelas during seasonal relapses, adults are prescribed 2.4 million IU once every 4 weeks for 3-4 months. For frequent relapses, the drug is administered once every 3-4 weeks, 2.4 million IU for 2-3 years. Children are prescribed 600 thousand IU once every 2 weeks or 1.2 million IU every 3-4 weeks.
To prevent infections after tooth extraction or tonsillectomy, adults are administered the drug every 1-2 weeks until complete recovery, 2.4 million IU; children - 600 thousand IU.
Side effects
When using Retarpen, allergic reactions may develop: difficulty breathing, urticaria, joint pain, fever, exfoliative dermatitis, angioedema, erythema multiforme, anaphylaxis.
During the treatment of syphilis, the Jarisch-Herskheimer reaction may develop, which is associated with the release of endotoxins.
During treatment with Retarpen, the following reactions from individual systems and organs are possible:
- Hematopoietic system. Often – reversible anemia, leukopenia, thrombocytopenia;
- Digestive system. Often – stomatitis, glossitis, nausea, vomiting, diarrhea, candidiasis; rarely - a moderate increase in the activity of liver transaminases in the blood serum; in some cases - pseudomembranous colitis;
- Other. Rarely – acute interstitial nephritis; with prolonged use, superinfection with resistant microorganisms and fungi may develop.
The use of beta-lactam antibiotic drugs in high dosages, especially in renal failure, can cause encephalopathy (convulsions, movement disorders, impaired consciousness).
Children may develop local reactions to the administration of Retarpen.
special instructions
The drug cannot be administered subcutaneously, endolumbarally, intravenously or intracavity.
With accidental intravascular administration of Retarpen, disturbances may occur in the form of a transient feeling of anxiety and visual impairment (Wanier syndrome). To avoid this, before intramuscular injection, aspiration must be performed to identify possible needle penetration into the vessel.
If syphilis is suspected during the treatment of sexually transmitted diseases, microscopic and serological studies should be carried out before starting treatment and then for 4 months.
Due to the possibility of fungal diseases occurring during therapy, it is recommended to additionally take vitamins C and B, and, if necessary, levorin and nystatin.
When prescribing the drug to patients following a diet with limited salt intake, it should be taken into account that the sodium content per 600 thousand IU of Retarpen is 0.24 mmol or 5.5 mg.
If any allergic reactions develop, the administration of the drug is stopped and appropriate treatment is prescribed. During therapy, severe allergic reactions (including anaphylactic shock) may develop. If a history of hypersensitivity to penicillin is indicated, the drug is strictly contraindicated.
In 5-10% of cases, a cross-allergic reaction between cephalosporins and penicillins was observed, and therefore, if a history of allergic reactions to cephalosporins is indicated, the prescription of penicillins is contraindicated.
It should be taken into account that the use of Retarpen in insufficient doses or stopping treatment too early can lead to the emergence of resistant strains of pathogens.
With simultaneous use of Retarpen the following is noted:
- Antagonism of action - bacteriostatic antibiotics (lincosamides, chloramphenicol, macrolides, tetracyclines);
- Synergistic action - bactericidal antibiotics (cycloserine, cephalosporins, rifampicin, vancomycin, aminoglycosides).
When used simultaneously with allopurinol, the risk of developing skin rashes (allergic reactions) increases.
Analogs
Analogs of Retarpen are based on the active substance - Benzicillin-1, Bicillin-1, Extencillin.
Terms and conditions of storage
Store out of reach of children, protected from light at temperatures up to 25 °C.
The shelf life of the drug is 4 years.
powder for preparation. susp. intramuscular injection 2.4 million IU: vial. 1 or 50 pcs.Reg. No.: 1120/94/99/05/07/10 dated 07/09/2010 - Valid
Powder for the preparation of a suspension for intramuscular administration white or white with a yellowish tint.
Excipients: simethicone, mannitol, povidone, isotonic citrate buffer.
Bottles with a capacity of 15 ml (1) - cardboard packs.
Bottles with a capacity of 15 ml (50) - cardboard boxes.
Description of the drug RETAPEN based on officially approved instructions for use of the drug and made in 2007. Update date: 04/18/2007
Antibiotic of the penicillin group G, destroyed by penicillinase, prolonged action. The mechanism of the bactericidal effect on sensitive microorganisms is due to the suppression of the synthesis of cell membrane mucopeptides.
Active regarding gram-positive microorganisms: Staphylococcus spp. (non-penicillinase-forming), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming rods:
- Actinomyces israelii, Bacillus anthracis, Clostridium spp.;
- gram-negative microorganisms: Neisseria meningitidis, Neisseria gonorrhoeae, and also against Treponema spp., causing syphilis and yaws. Also effective against Streptococcus pyogenes A.
To the drug stable strains of Staphylococcus spp., producing penicillinase that destroys benzylpenicillin.
Suction and distribution
After an intramuscular injection of benzathine, benzylpenicillin is very slowly hydrolyzed, releasing benzylpenicillin. Cmax in blood serum is achieved 12-24 hours after injection. Long T1/2 provides a stable and long-term concentration of benzathine benzylpenicillin in the blood:
- on the 14th day after administration of the drug at a dose of 2.4 million IU, the serum concentration is 0.12 mcg/ml. Diffusion of the drug in body fluids is complete, diffusion into tissues is very weak. Plasma protein binding - 40-60%. In small quantities it penetrates the placental barrier and is excreted in breast milk.
Metabolism and excretion
It is slightly biotransformed in the body. It is excreted mainly by the kidneys unchanged. Over 8 days, up to 33% of the administered dose is released.
Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
- syphilis (as monotherapy);
- yaws, pint;
- acute tonsillitis, scarlet fever.
- repeated attacks after acute rheumatic fever;
- recurrence of erysipelas;
- wound infection;
- infections during tonsillectomy or after tooth extraction.
Prevention of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
The drug is administered deep intramuscularly. Cannot be administered intravenously!
To prepare a suspension for intramuscular administration, 5 ml of water for injection should be added to the bottle under aseptic conditions. Before use, mix thoroughly by rolling the bottle between the palms of your hands, trying to avoid the formation of excessive foam. The prepared suspension can be stored in the refrigerator for no more than 24 hours.
At syphilis adults for preventive treatment, 2.4 million IU is prescribed once; at primary syphilis the drug is prescribed in a dose of 2.4 million IU 2 times 1 IM injection with an interval of 7 days; at secondary and early latent syphilis- at a dose of 2.4 million IU 3 times, 1 intramuscular injection with an interval of 7 days.
For preventive therapy child, born to an untreated mother with syphilis, the drug is prescribed at a dose of 5000 IU/kg body weight, 1 IM injection with an interval of 7 days. Course - 3 injections. The dose should be divided in half and administered into different buttocks.
For preventive therapybaby due to insufficient treatment of the mother or seroresistance - 1 injection intramuscularly with an interval of 7 days. Course - 2 injections.
For treatment of yaws and pinta (endemic treponematoses) adults- 2.4 million IU each; children prescribed once, 1.2 million IU.
At other infections (acute tonsillitis, scarlet fever, erysipelas, wound infections in the acute phase) adults prescribe 1.2 million IU or 2.4 million IU once a week; children up to 12 years- 600 thousand IU every 3 days or 1.2 million IU every 2-4 weeks, depending on the severity of the infection.
For prevention of recurrent attacks after acute rheumatic fever adults and teenagers prescribed 2.4 million IU once every 3 weeks;
children weighing more than 25 kg- 1.2 million IU once every 3 weeks;
children weighing less than 25 kg- 600 thousand IU once every 3 weeks. The duration of prophylaxis is determined individually.
When prescribing the drug patients with impaired renal function correction of the dosage regimen is required depending on the magnitude of creatinine clearance. At QC from 10 to 50 ml/min administer 75% of the recommended daily standard dose; at CC less than 10 ml/min - 25-50%.
For prevention of recurrence of erysipelasadults at seasonal relapses prescribe 2.4 million IU once every 4 weeks for 3-4 months annually; at frequent relapses- 2.4 million IU once every 3-4 weeks for 2-3 years; children- 600 thousand IU once every 2 weeks or 1.2 million IU every 3-4 weeks.
For prevention of infections after tonsillectomy or tooth extraction adults- 2.4 million IU each; children- 600 thousand IU each. The drug is administered every 7-14 days until complete recovery.
Allergic reactions: urticaria, fever, joint pain, angioedema, exfoliative dermatitis, erythema multiforme, difficulty breathing, anaphylaxis.
When treating syphilis, the Jarisch-Herskheimer reaction may develop due to the release of endotoxins.
From the hematopoietic system: reversible anemia, leukopenia, thrombocytopenia.
From the digestive system: stomatitis, glossitis, nausea, vomiting, diarrhea, candidiasis;
Others: rarely - acute interstitial nephritis;
The use of beta-lactam antibiotics in high doses can cause (especially in renal failure) the development of encephalopathy (impaired consciousness, movement disorders, convulsions).
Children may develop local reactions to the administration of the drug.
Use during pregnancy and breastfeeding
The use of the drug during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.
If it is necessary to prescribe the drug during lactation, the issue of stopping breastfeeding should be decided.
Benzathine benzylpenicillin penetrates the placental barrier in small quantities and is excreted in breast milk.
It cannot be administered subcutaneously, intravenously, endolumbarally, or into the body cavity.
With accidental intravascular administration, a transient feeling of anxiety and visual disturbances (Wanier syndrome) may occur. In order to avoid such an injection, aspiration should be performed before intramuscular injection in order to identify possible needle entry into the vessel.
If syphilis is suspected during the treatment of sexually transmitted diseases, then before starting therapy and then for 4 months, microscopic and serological studies are necessary.
Due to the possibility of the development of fungal diseases during drug therapy, B vitamins and vitamin C should be prescribed, and, if necessary, nystatin and levorin.
When prescribing the drug to patients on a diet with limited salt intake, it should be taken into account that the sodium content per 600 thousand IU of the drug is 5.5 mg or 0.24 mmol.
If any allergic reactions occur, it is necessary to stop administering the drug and prescribe appropriate treatment. Severe allergic reactions may occur (up to the development of anaphylactic shock). When collecting anamnesis, attention should be paid to the tolerability of previous penicillin therapy. If there is a history of hypersensitivity to penicillin, the drug is strictly contraindicated.
In 5-10% of cases, a cross-allergic reaction is observed between penicillins and cephalosporins. In this regard, if there is a history of allergic reactions to cephalosporins, the prescription of penicillins is contraindicated.
It must be taken into account that using the drug in insufficient doses or stopping therapy too early often leads to the emergence of resistant strains of pathogens.
When using benzathine benzylpenicillin simultaneously with NSAIDs (indomethacin, phenylbutazone, salicylates), allopurinol, probenecid, one should keep in mind the possibility of competitive inhibition of drug excretion from the body.
When used simultaneously with bactericidal antibiotics (cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides), a synergistic effect is observed; with bacteriostatic - (macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonism.
Increases the effectiveness of indirect anticoagulants (suppressing intestinal microflora, reduces the potrombin index); reduces the effectiveness of oral contraceptives, drugs, during the biotransformation of which para-aminobenzoic acid is formed, ethinyl estradiol (the likelihood of breakthrough bleeding increases).
When used simultaneously with allopurinol, the risk of developing allergic reactions (skin rash) increases.
SANDOS PHARMACEUTICALS d.d., representative office, (Slovenia)
Representative office of JSC "Sandoz Pharmaceuticals d.d." (Slovenia) in the Republic of Belarus
1,200,000 units - 10 ml bottles (100) - cardboard boxes.
1,200,000 units - 10 ml bottles (1) - cardboard packs.
pharmachologic effect
Antibiotic of the group of biosynthetic penicillins. The mechanism of action is based on a violation of the synthesis of peptidoglycan - a mucopeptide of the cell membrane, which leads to inhibition of the synthesis of the cell wall of the microorganism, suppression of the growth and reproduction of bacteria.
Active against gram-positive bacteria, gram-negative cocci, Actinomyces spp., Spirochaetaceae.
Inactive against strains of Staphylococcus spp. that produce penicillinase.
Has a prolonged effect.
Pharmacokinetics
When administered intramuscularly, it is slowly absorbed from the injection site, providing a prolonged effect. Poorly penetrates the BBB. Metabolized by hydrolysis to benzylpenicillin. Due to prolonged absorption, benzylpenicillin is detectable in urine for 12 weeks after a single dose.
Indications
Infectious and inflammatory diseases caused by pathogens sensitive to benzathine benzylpenicillin, incl. , yaws, pinta, acute tonsillitis, scarlet fever, erysipelas, wound infection; prevention of exacerbations of rheumatism, scarlet fever (after contact with patients), erysipelas; prevention of infectious complications after tonsillectomy or tooth extraction.
Contraindications
Hypersensitivity to benzathine benzylpenicillin and other penicillin antibiotics.
Dosage
Injected intramuscularly. For adults, a single dose varies from 300,000 units to 2.4 million units; for children, a single dose is 5000-10,000 units/kg. The frequency and duration of use depend on the etiology of the disease.
Side effects
From the hematopoietic system:, thrombocytopenia, leukopenia, blood clotting disorders.
Effects due to chemotherapeutic action: with long-term treatment, superinfection with resistant microorganisms and fungi may develop.
Allergic reactions: urticaria, rash on the mucous membranes, fever, joint pain, eosinophilia, angioedema, erythema multiforme, exfoliative dermatitis, stomatitis, glossitis, in exceptional cases - anaphylactic and anaphylactoid reactions.
Drug interactions
When used simultaneously with NSAIDs (in particular, indomethacin, phenylbutazone and salicylates), one should keep in mind the possibility of developing competitive inhibition of drug excretion from the body.
In combination with antibiotics that act bacteriostatically, there is a decrease in the bactericidal effect of benzathine benzylpenicillin.
Combination with other antibiotics is possible only if the synergism of action is expected.
special instructions
Use with caution in patients with impaired renal function, in case of predisposition to allergic reactions (especially with drugs), with increased sensitivity to cephalosporins (due to the possibility of developing cross-allergy).
Pregnancy and lactation
Benzathine benzylpenicillin penetrates the placental barrier and is excreted in breast milk. Use during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.
For impaired renal function
Use with caution in patients with impaired renal function.