Can pregnant women inject the medicine retarpen? Medicinal reference book geotar

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

pharmachologic effect

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.

Pharmacokinetics

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

Biotransforms in the body insignificantly. It is excreted mainly by the kidneys unchanged. Over 8 days, up to 33% of the administered dose is released.

Indications for use

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• syphilis (as monotherapy);
• yaws, pint;
• acute tonsillitis, scarlet fever.

Prevention of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• repeated attacks after acute rheumatic fever;
• recurrence of erysipelas;
• wound infection;
• infections during tonsillectomy or after tooth extraction.

Dosage regimen

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 prescribe 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.

Side effects

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;

rarely - a moderate increase in the activity of liver transaminases in the blood serum;

in some cases - pseudomembranous colitis.

Others: rarely - acute interstitial nephritis;

with long-term use, superinfection with resistant microorganisms and fungi may develop.

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.

special instructions

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.

Drug interactions

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 allergic reactions (skin rash) increases.

Contacts for inquiries

SANDOS PHARMACEUTICALS d.d., representative office, (Slovenia)

Representative office of JSC "Sandoz Pharmaceuticals d.d." (Slovenia) in the Republic of Belarus

A drug Retarpen- an antibacterial drug, the active and active substance of which is benzathine benzylpenicillin - these are beta-lactam antibiotics from the group of long-acting penicillins type G. It exhibits a bactericidal effect against sensitive microorganisms by suppressing the synthesis of cell wall mucopeptides.
Active against gram-positive pathogens: Staphylococcus spp. (penicillin-insoluble), Streptococcus spp., including Streptococcus pneumoniae, Corynebacterium diphtheriae, anaerobic spore-forming bacilli, Bacillus anthracis, Clostridium spp., Actinomyces israelii; gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, as well as Treponema spp. Strains of Staphylococcus spp., which produce penicillinase, which destroys benzylpenicillin, are resistant to the drug. Due to its long-lasting action, the drug is intended for the treatment of infections caused by Streptococcus spp. and Treponema pallidum.

Pharmacokinetics

.
When administered, benzathine benzylpenicillin is very slowly absorbed from the injection site, providing a prolonged effect.
Maximum serum concentrations are achieved 12-24 hours after injection. The long half-life ensures a stable and prolonged concentration of the drug in the blood: on the 14th day after administration of 2,400,000 IU, the concentration in the blood serum is 0.12 mcg/ml. The degree of binding to plasma proteins is approximately 55%.
Benzathine benzylpenicillin penetrates the placental barrier in small quantities, as well as into breast milk. The metabolism of the drug is negligible. It is excreted primarily by the kidneys unchanged; within 8 days, up to 33% of the administered dose is eliminated.

Indications for use

A drug Retarpen used to treat 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).
Also the drug Retarpen used for the prevention of: rheumatic diseases (chorea, rheumatic carditis); poststreptococcal glomerulonephritis; scarlet fever (after contact with a patient); faces; syphilis (after contact with a patient).

Mode of application

Before insertion Retarpena It is necessary to collect a history of drug tolerance from the patient and conduct a preliminary intradermal test to determine its tolerance.
Retarpen apply only intramuscularly!
To prepare the suspension, add 5 ml of water for injection to the vial. Use only freshly prepared suspension, shake for 20 seconds and inject immediately using a needle with a minimum thickness of 0.9 mm. Retarpen is injected into the upper quadrant of the gluteal muscle. To administer the drug, it is necessary to prick the needle perpendicular to the surface of the skin with a sharp movement, while avoiding the proximity of large vessels. If blood aspiration or pain occurs during administration of the drug, the injection should be stopped. Inject the drug as slowly as possible only under low pressure. Do not rub the injection site after administration. If repeated injections are necessary, the injection site should be changed. It is necessary to suction immediately before administering the drug 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.
Primary syphilis. A single dose of 2,400,000 MO of Retarpen, distributed over 2 injection sites.
Secondary syphilis. 2,400,000 IU of Retarpen at 2 injection sites.
If clinical manifestations recur or laboratory results remain positive, treatment should be repeated.
Late syphilis (seropositive latent syphilis). 2,400,000-4,800,000 IU weekly for 3-5 weeks.
Treatment of yaws.
1200000 - 2400000 IU once. Persons who have had contact with sick people or patients with a latent form of infection should be given half the dose.
Pint treatment.

Treatment of other infections caused by microorganisms sensitive to the drug (acute tonsillitis, scarlet fever, erysipelas, erysipeloid, infected wounds and bite wounds).
2400000 MO Retarpena weekly.
Prevention of rheumatic fever and rheumatic endocarditis, chorea, post-glomerulonephritis and erysipelas.
1,200,000 - 2,400,000 IU of Retarpen once every 4 weeks.
The duration of prophylaxis is determined individually.
Prevention of scarlet fever in persons who have had contact with patients.
2400000 MO Retarpen one time.
For streptococcal diseases, the course of treatment should be at least 10 days to prevent complications. As a rule, one injection of Retarpen 2400000 MO is sufficient.

Side effects

The following adverse reactions are grouped by class of body system and frequency of occurrence of reactions: very often (≥ 1/10), often (≥ 1/100,<1/10), нечасто (≥ 1/1000, <1/100), редко (≥ 1/10000, <1/1000), очень редко (<1/10000), частота неизвестна (частота не может быть оценена из-за отсутствия данных).
Infections and infestations: common - resistant bacterial and fungal infections (including candidiasis).
From the blood and lymphatic system: very rarely - hemolytic anemia, leukopenia, thrombocytopenia, agranulocytosis, eosinophilia.
From the immune system: rarely - hypersensitivity reactions, including rash, urticaria, Quincke's edema, erythema multiforme, exfoliative and contact dermatitis, fever, joint pain, laryngospasm, bronchospasm, anaphylactic shock sometimes with collapse and death, anaphylactoid reactions (asthma, purpura, gastrointestinal symptoms); frequency unknown - serum sickness; during the treatment of syphilis, due to the release of endotoxins, the Jarisch-Herxheimer reaction may develop, which is characterized by the following symptoms: fever, chills, myalgia, headache, exacerbation of skin symptoms, tachycardia, vasodilation with changes in blood pressure (the reaction can be dangerous in cardiac -vascular syphilis or conditions in which there is a serious risk of increased local damage, such as optic atrophy). Patients with dermatomycosis may develop paraallergenic reactions as a result of possible joint antigenicity between penicillins and dermatophyte metabolites. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
From the nervous system: rarely - neuropathy.
From the digestive tract: often - diarrhea, nausea; rarely - stomatitis, glossitis, vomiting; frequency unknown - pseudomembranous colitis, black coloration of the tongue.
From the digestive system: frequency unknown - hepatitis, cholestasis.
From the skin: frequency unknown - pemphigoid.
From the urinary system: rarely - nephropathy, interstitial nephritis.
General disorders: frequency unknown - pain, infiltration at the injection site, Wan syndrome, Hoigne syndrome and Nicolau syndrome.

Contraindications

Contraindications to the use of the drug Retarpen are: hypersensitivity to the components of the drug, beta-lactam antibiotics (penicillin and carbapenems), soy, peanuts. History of cross-sensitivity to cephalosporins (5-10% of cases). For the treatment of diseases requiring high concentrations of penicillin in blood serum and cerebrospinal fluid (severe pneumonia, empyema, sepsis, pericarditis, meningitis, peritonitis, arthritis, congenital neurosyphilis), water-soluble sodium salt of benzylpenicillin should be used. History of urticaria, hay fever, severe allergic reactions and bronchial asthma.

Pregnancy

A drug Retarpen can be used after a careful assessment of the benefit/risk ratio.
Benzathine benzylpenicillin passes into breast milk in small quantities. Concentrations in milk can range from 2% to 15% of maternal plasma concentrations. There have been no reports of adverse reactions in infants, but possible sensitization or interference with intestinal flora should be taken into account. Breastfeeding should be stopped if diarrhea, candidiasis or rash occurs in the baby.
Infants who are on combination feeding should be switched to feeding with baby food during the mother's treatment with Retarpen. Breastfeeding can be resumed 24 hours after stopping treatment.

Interaction with other drugs

Penicillin drugs that have a bactericidal effect should not be used in combination with bacteriostatic antibiotics.

Combination with other antibiotics is only possible when a synergistic effect or any additional effect can be expected. The individual components of the therapeutic combination should be prescribed at full dose (the dose of the more toxic component may be reduced if a synergistic effect is shown).
It should be borne in mind the possibility of competitive inhibition of 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.
Simultaneous use Retarpena with methotrexate reduces the excretion of the latter and can lead to increased toxicity. Combining Retarpen and methotrexate is not recommended.
With simultaneous use, the effectiveness of indirect anticoagulants increases. When used with oral anticoagulants, the effect of antivitamins K and the risk of bleeding may increase. It is recommended to periodically determine the level of the international normalized index (INI) and accordingly adjust the use of antivitamin K drugs during and after treatment with retarpen.
The use of benzathine benzylpenicillin may in some cases lead to 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 with concomitant use.
Allopurinol increases the risk of allergic reactions (skin rashes).
Aspirin, probenecid, thiazide diuretics, furosemide, ethacrynic acid increase the half-life of benzylpenicillin, increasing its concentration in the blood plasma, as a result of which the risk of developing its toxic effect by affecting the tubular secretion of the kidneys increases.

Overdose

The use of high doses of beta-lactam antibiotics, especially in liver failure, can cause the development of encephalopathy (confusion, impaired movement). Penicillins in extremely large doses can cause neuromuscular irritability or epileptic-like seizures. Potentially in case of overdose Retarpen Gastrointestinal symptoms and electrolyte imbalances are possible.
Treatment: symptomatic and supportive therapy, hemodialysis. A specific antidote is unknown.

Storage conditions

In a place protected from light, at temperatures below 25 °C.
Keep out of the reach of children.

Release form

Retarpen - powder for suspension for injection.
Packaging: powder in a bottle. 50 bottles in a cardboard box.

Compound

1 bottle Retarpen contains benzathine benzylpenicillin 2,400,000 IU.
Excipients: simethicone, mannitol (E 421), povidone, sodium.

Additionally

Before starting therapy, microscopic and serological studies are necessary for at least 4 months. When prescribing to patients with diabetes, prolonged 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.

Main settings

Name:	RETAPEN
ATX code:	J01CE08 -

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.

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 this is precisely why the medicine is not prescribed for bacterial diseases of mild and moderate severity (damage to the ENT organs, urinary tract, lungs, bronchi, etc.).

Information about the medication manufacturer

Retarpen (international name Retarpen) is produced by the 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 the independent use of 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 a dose prescribed by the doctor. The manufacturer provides a dosage of 2.4 or 1.2 IU of the 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 of structural components of the shell during the development of the microorganism, thus causing irreversible destruction of 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 the structure of the 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, and 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 administration of the medicinal solution is sufficient.

Retarpen is used intramuscularly. The injection is made in the upper part of the buttock, the needle is inserted at a right angle, trying to avoid the area where large blood vessels are located. If bleeding or severe pain occurs, stop the injection.

Patients often ask how to dilute Retarpen lyophilisate. The drug must 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.

Diagnosis	Features of dosage and use
Syphilis (disease manifestation or secondary stage)	Adults and adolescents: 2.4 IU once Children: 50,000 IU/kg once (but not more than 2.4 IU in total) A repeated course of therapy is necessary with further progression of the disease (laboratory and objective signs)
Latent seropositive syphilis	Adults and teenagers: 2.4 IU once a week Children: 50,000 IU/kg weekly Total duration of therapy: 3 weeks (3 injections)
Congenital syphilis (without neurological symptoms)	Infants (from the first day of life): 50,000 IU/kg once
Non-venereal syphilis, pint	Adults and teenagers: 1.2 IU Children weighing over 30 kg: 1.2 IU Children weighing up to 30 kg: 600,000 IU The drug is administered once
Prevention of rheumatoid fever, glomerulonephritis against the background of streptococcal infection, erysipelas	Adults and teenagers: 1.2 IU every 21 to 28 days Children weighing up to 30 kg: 1.2 IU every 3-4 weeks Children weighing up to 30 kg: 600,000 IU every 3-4 weeks The duration of treatment is determined as follows: Without heart damage: for 5 years or until age 21. For heart disease: at least 10 years of age or up to 21 years of age. Persistent cardiac involvement: at least 10 years or until age 40. Sometimes emergency prevention is required
Dosage in certain categories of patients
Creatinine clearance 100-60 ml/min Serum creatinine level 0.8-15	The dose is left unchanged
Creatinine clearance 5 -10 ml/min Serum creatinine level 1.5-8.0	The dosage is reduced by 25%
Creatinine clearance up to 10 ml/min Serum creatinine level 15	The dose is reduced by 50-80%, while the volume of the solution is divided into 2-3 injections

Possible adverse reactions

The list of the most common side effects includes:

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

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

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 use of 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 contraceptives, 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 in 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, the active drug substance passes into breast milk, which requires stopping 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.

Analogs

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 to the established therapy regimen. 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. The approximate price of one bottle of Retarpen is 60 euros. The cost will be lower if you order several packages at the same time.

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 a skin rash (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.