Retarpen injections. Complete instructions for using retarpen, list of analogues, reviews and prices

Retarpen is a long-acting penicillin antibiotic intended for the treatment of infections caused by flora sensitive to its influence. The active substance of the drug is destroyed under the influence of penicillinase secreted by some bacteria, so the list of indications for use is limited to fairly severe diseases.

The effectiveness of Retarpen for borreliosis and syphilis has been proven. The drug is often prescribed for the treatment and prevention of rheumatoid complications caused by streptococcal flora.

Steady concentrations of the active ingredient are maintained for 2-4 weeks after use, which provides a pronounced therapeutic effect. But that is why the medicine is not prescribed for bacterial diseases of the lungs and moderate degree severity (damage to the ENT organs, urinary tract, lungs, bronchi, etc.).

Information about the medication manufacturer

Retarpen is produced (international name Retarpen) pharmaceutical company Sandoz (Austria), a division of Novartis Corporation. Sandoz is one of the world's largest manufacturers of antibiotics. The company is a leader in the production of antibacterial agents of the penicillin class, including those in combination with clavulanic acid (trade name Amoxiclav).

Instructions for use

Experts categorically prohibit independent use any antibacterial drugs. The same applies to Retarpen. The medication is intended for use according to a specially developed regimen for the treatment of serious infections. Self-medication is contraindicated, since the wrong dose and non-compliance with the therapy protocol can cause resistance of the bacterial flora. Before starting the therapeutic course, you must read the instructions for use.

Composition and dosage form

The medication is available in the form of a lyophilisate (powder) for the preparation of a solution for injection. Injections are given intramuscularly in the dose prescribed by the doctor. The manufacturer provides a dosage of 2.4 or 1.2 IU active component.

Description and composition

The active ingredient is benzathine benzylpenicillin in the form of a lyophilisate, packaged in bottles. Additionally, the medicine also includes auxiliary components that ensure the maintenance of therapeutic properties throughout the shelf life - sodium citrate, mannitol, simethicone.

Pharmacological group

In accordance with the classification system generally accepted in medicine and pharmacy, Retarpen is a long-acting antibacterial drug (antibiotic) of the β-lactam penicillin class.

Pharmacodynamic aspects

The action of the active substance is associated with its effect on the outer cell membrane of bacteria. Benzathine benzylpenicillin inhibits the synthesis structural components membranes during the development of the microorganism, thus causing irreversible destruction of the pathogenic flora. The product has a bactericidal effect that lasts for a long period.

The instructions for use describe the mechanisms of development of drug resistance. These include the destruction of the active component of the drug by β-lactamases (this enzyme is usually produced by staphylococci). Gram-negative bacteria differ in structure cell membrane, which reduces the therapeutic effectiveness of Retarpen. The development of resistance as a result of mutation of pathogens has also been reported.

Pharmacokinetic parameters

Absorption. After an intramuscular injection, absorption of the active component occurs quite slowly. Therefore, for most diseases, 1-2 injections per month are sufficient. Peak plasma concentrations are observed after 24 hours in children and 48 hours in adults.

Distribution. About 50-55% of the administered amount of the drug binds to plasma proteins. When the drug is prescribed in high dosages, benzylpenicillin is found in hard-to-reach tissues - heart valves, bones, cerebrospinal fluid and pleural fluid. Penetrates the placental barrier and enters the fetal bloodstream; it is found in high concentrations in the amniotic fluid. The volume of distribution is 0.3-0.4 l/kg in adults and 0.75 l/kg in children.

Biotransformation. The medicine practically does not undergo metabolic transformations.

Elimination. Up to 80% of the total amount of the active substance is excreted in its original form, mainly by the kidneys (85-95%) with urine, the remaining dose is conjugated with bile.

Pharmacokinetic parameters may change in newborns due to insufficient development of the liver and kidneys, patients with impaired function of these organs, and elderly patients.

Information about the main active ingredient

Benzathine benzylpenicillin is a naturally occurring substance with a complex chemical structure. The empirical formula is C48H56N6O8S2. ATX code J01CE08.

The compound exhibits bactericidal activity against the following representatives of pathogenic flora:

• staphylococci (not producing penicillinase);
• streptococci;
• pneumococci;
• corynebacteria;
• clostridium;
• actinomycetes;
• gonorrhea pathogens;
• Treponem.

But taking into account the characteristics of use and duration of action, benzathine benzylpenicillin is often prescribed for infections caused by streptococci or treponema.

Indications for use

Retarpen is prescribed for the following diseases:

• erysipelas;
• acute and latent course of syphilis;
• Lyme disease ( tick-borne borreliosis);
• tropical granuloma (sometimes the disease is called non-venereal syphilis);
• pint (infection caused by Treponema carateum).

The drug is also prescribed for prophylactic purposes to prevent:

• rheumatic (autoimmune) complications of streptococcal infection, including damage to the kidneys, myocardium, cartilage tissue;
• syphilis, scarlet fever (after contact with a sick person);
• erysipelas.

There is evidence of the effectiveness of the drug in the treatment of tonsillitis and scarlet fever. But in case of uncomplicated course of these pathologies, many doctors prefer to replace Retarpen with another broad-spectrum antibiotic in the form of tablets.

List of contraindications and restrictions for use

Do not prescribe in case of individual hypersensitivity to antibiotics from the group of penicillins, cephalosporins and β-lactams; allergic reaction to soy protein (contained in auxiliary ingredients).

The medication is used with caution for allergic diseases (rhinitis, hay fever, contact dermatitis, etc.). The use of Retarpen is not advisable for infections caused by flora sensitive to the action of the drug, but requiring high concentrations of the antibiotic in the cerebrospinal fluid.

Dosage Features

The dose and duration of therapy depends on the type and severity of the infection, the age and functional activity of the patient's liver.

• adults and adolescents: 1.2 IU of diluted medication every 7 days;
• children weighing more than 30 kg: the dose is 1.2 IU weekly;
• children weighing up to 30 kg: 600 IU per week.

The duration of treatment should be determined to prevent recurrence of streptococcal infection. For uncomplicated diseases, a single dose is sufficient. medicinal solution.

Retarpen is used intramuscularly. The injection is given in top part buttocks, the needle is inserted at a right angle, trying to avoid the area where large blood vessels are located. If bleeding occurs or severe pain, the injection is stopped.

Patients often ask how to dilute Retarpen lyophilisate. The drug should not be mixed with anything other than water for injection (combination in the same syringe with local anesthetics, saline, etc. is contraindicated). To prepare the injection, a 5 ml ampoule of solvent is required. The result is a suspension that is used immediately. The drug is administered slowly; if necessary, two injections are given in different buttocks.

Possible adverse reactions

List of the most common side effects includes:

• candidiasis;
• exacerbation of bacterial infections (with incorrect selection dose or resistance of the pathogen);
• allergic reactions up to anaphylactic shock with fatal outcome;
• bowel disorders;
• pain, swelling at the injection site.

Complications associated with massive release of toxins as a result of death are also possible. large quantity pathogenic flora.

Drug interactions

The simultaneous administration of Retarpen with antibiotics is possible only to improve the results of therapy. In this case, antibacterial agents of another group are prescribed to expand the spectrum of bactericidal action.

Parallel taking NSAIDs slows down the elimination of benzylpenicillin from the body.

Use caution when using medications with cytostatics (in particular, methotrexate) due to the risk of increasing the toxic effects of the latter.

Retarpen enhances the effect of anticoagulants, which can cause uncontrolled bleeding.

When used simultaneously with hormonal contraception it is necessary to use other methods of contraception.

Salicylates and diuretics increase the level of antibacterial substances in the blood, which increases the likelihood of complications.

Alcohol compatibility

Alcohol is contraindicated due to the risk of side effects from the liver.

Special instructions and precautions

The medication is intended for intramuscular injections only. Before the first procedure, you must ensure that there is no allergic reaction. For patients with a history of allergies (including food allergies), the drug is administered in a hospital setting if all the necessary medications are available to relieve anaphylaxis.

Only for health reasons, Retarpen is prescribed to patients with lesions of the hematopoietic system, Epstein-Barr virus, impaired renal and liver function, and mycoses.

Against the background of diabetes mellitus, the absorption of the drug slows down.

After the injection, the patient must remain under medical supervision for 12 hours. If Retarpen is used to treat syphilis, after the first injection the following are possible:

• headache;
• hot flashes of sweating;
• temperature increase;
• tremor;
• pain in muscles and joints;
• nausea and vomiting;
• fluctuations blood pressure;
• increased heart rate.

These symptoms go away on their own and do not require cessation of treatment.

With a long course of therapy, monitoring of kidney and liver parameters is mandatory. The effectiveness of the treatment is assessed using objective symptoms and blood tests.

If an antibiotic solution is accidentally injected into a vein or artery, measures must be taken to prevent the risk of complications and skin reactions.

If a prolonged stool disorder occurs, pseudomembranous colitis should be excluded.

Benzathine benzylpenicillin penetrates the placental barrier, so the drug is prescribed only after assessing the risk/benefit ratio. Also active medicinal substance Fall into breast milk, which requires suspension of lactation.

On the day of the injection (and the next 24-48 hours), you must refrain from driving and work that requires concentration.

Overdose

Storage conditions

At room temperature.

Best before date

Is 4 years.

Discontinuation of therapy

Possibly at the discretion of the doctor after receiving the results of laboratory tests and complete elimination of pathogenic flora.

Analogues

The following drugs are analogues of Retarpen in composition and release form:

• Extencilline, manufactured by Sanofi Aventis, France;
• Bicillin 1 is produced in Russia by the Sintez company.

Retarpen is characterized by maximum bioavailability and therapeutic effectiveness. This allows you to eliminate pathogenic flora after the first injection, prevent complications and shorten the course of treatment as much as possible. According to experts, Bicillin 1 is several times inferior in clinical effectiveness to its original analogues. Therefore it is necessary to adhere established scheme therapy. In any case, only the attending physician can decide what to replace Retarpen with.

Price and where to buy

The medicine is not available for sale in domestic pharmacies, since the antibiotic is not registered in Russia. There is an option to order from intermediaries who can buy and organize delivery of Retarpen in the required quantity and required dosage from Europe.

Given the long shelf life and storage conditions, the medicine is often already available in warehouses in Moscow or St. Petersburg. In this case, the product will be sent shortly after placing your order online or by phone. In most cases, the drug is purchased directly in Germany, extremely rarely - in Poland. approximate price One bottle of Retarpen costs 60 euros. The cost will be lower if you order several packages at the same time.

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 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, capable of killing 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 infectious disease, affects not only the joints, but also the heart, skin and brain. Swelling and pain in the joints - only external manifestations 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 complete analogue Penidure, and will also prescribe a dose and treatment regimen. As a rule, in the treatment of 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 of 1-2 amps. 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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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 and slowly hydrolyzes to form benzylpenicillin, which is gradually absorbed and maintains a therapeutic concentration in the blood for a 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 and enters 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

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 there may be headaches, , 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 children younger age and newborns are administered 1.2 million units 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 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: intramuscular 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 pronounced effect 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. In case of accidental hit medicine there is a violation in the lumen of the vessel visual perception, transient feeling of depression, anxiety.

J.01.C.E.08 Benzathine benzylpenicillin