Retarpen

Retarpen – an antibiotic from group of penicillin like G prolonged actions.

Form of release and structure

Dosage form – powder for preparation of suspension for intramuscular introduction of the prolonged action (1,2 million ME – on ~ 1,14 g in colourless glass bottles with a capacity of 5 ml, 1 bottle in a pack of cardboard, 100 bottles in a cardboard box (for hospitals); 2,4 million ME – on ~ 2,27 g in colourless glass bottles with a capacity of 15 ml, 1 bottle in a pack of cardboard, 50 bottles in a cardboard box (for hospitals)).

Active ingredient – a benzatina benzylpenicillin, in 1 bottle – 1,2 million international units (IU) (1,0256 g) or 2,4 million ME (2,0513 g).

Excipients: attracts, симетикон, sodium - the citrate buffer, povidone.

Indications to use

Treatment of the infections caused sensitive to a benzatin to benzylpenicillin by microorganisms in need of long impact on them:

• Scarlet fever;
• Acute tonsillitis;
• Pint;
• Frambeziya;
• Syphilis.

Prevention of the infections caused by sensitive microorganisms:

• Ugly face recurrence;
• The repeated attacks after acute rheumatic fever.

Contraindications

• Lactation period;
• Hypersensitivity to components of drug or another beta лактамным to antibiotics (cephalosporins or penicillin).

With care:

• Renal and/or liver failure;
• Diabetes mellitus;
• Dermatomycoses;
• Pseudomembranous colitis;
• Tendency to allergic reactions (allergic rashes, bronchial asthma);
• Pregnancy.

Route of administration and dosage

Retarpen is intended for intramuscular introduction. From powder prepare suspension, for this purpose enter water for injections into a bottle: in a dose of 1,2 million ME – 3 ml, in a dose of 2,4 million ME – 5 ml then carefully mix, rolling a bottle between palms of hands, avoiding formation of plentiful foam.

Solution is entered deeply into an upper outside quadrant of a big gluteus. To exclude hit of a needle and according to drug in a vessel, just before introduction it is necessary to make aspiration. In case of aspiration of blood or emergence of the expressed morbidity Retarpen's introduction should be stopped.

The recommended dosages at acute tonsillitis, scarlet fever, a frambeziya and pint:

• Adults and teenagers – 1,2 million ME once;
• Children with body weight from 30 kg – 1,2 million ME once;
• Children with body weight less than 30 kg – 600 thousand ME once.

The recommended doses at primary and secondary syphilis:

• Adults and teenagers – 2,4 million ME;
• Children with body weight from 30 kg – 600 thousand-2,4 million ME.

As a rule, rather single administration of drug. In case of resuming of clinical and/or laboratory displays of a disease conduct a repeated course.

At late stages of syphilis, including at a latent seropositive form, to adults and teenagers appoint on 1 injection 2,4 million ME within 3 weeks once a week.

At inborn syphilis (without signs of involvement of the central nervous system) appoint 50 thousand ME to each kilogram of body weight within 3 weeks once a week.

For prevention of acute rheumatic fever, an ugly face and a post-streptococcal glomerulonephritis Retarpen appoint in the following doses:

• Adults and teenagers – 1,2 million ME of 1 times in 3-4 weeks;
• Children with body weight from 30 kg – 1,2 million ME of 1 times in 3-4 weeks;
• Children with body weight less than 30 kg – 600 thousand ME of 1 times in 3-4 weeks.

The recommended treatment duration:

• In the absence of damage of heart – a minimum within 5 years or before achievement of age 21 years;
• At passing damage of heart – a minimum within 10 years or before achievement of age 21 years;
• At persistent damage of heart – a minimum within 10 years or before achievement of age of 40 years. Performing lifelong preventive therapy can be in certain cases shown.

Duration of prevention is established individually.

Special instructions:

• To patients with a renal failure Retarpen's dose is calculated taking into account function of kidneys: at the clearance of creatinine (CC)> 10 ml/minute – 75% of a usual dose, at KK <10 ml/minute – 20-50% (division of a single dose into several introductions in some cases can be required);
• Elderly patients before purpose of drug should estimate a condition of function of kidneys and by results, if necessary, to modify a dose;
• At a liver failure metabolism and excretion of penicillin can change that should be considered at selection of a dose.

Side effects

• Changes in laboratory indicators: often (> 1/100, <1/10) – positive forward reaction of Koombs, distortion of results of an electrophoresis of proteins of a blood plasma, increase in maintenance of 17 ketosteroids in urine (when using reaction of Tsimmermann), lozhnoyopolozhitelny reactions of definition of amino acids in urine (when using a ninhydrin method), false positive reactions to urobilinigen, false positive reactions of definition of glucose in urine (when using non-enzymatic methods), false positive reactions of definition of protein in urine when using a biuretic method, Folin-Chokalteu's method or techniques of precipitation (at use of trichloroacetic, sulphosalicylic acids);
• Other effects of the immunoallergic nature: acute intersticial nephrite, moderate tranzitorny increase in activity of serumal transaminases;
• Disturbances from the alimentary system: often – nausea, diarrhea, vomiting; infrequently (> 1/1000, <1/100) – a glossitis, stomatitis; frequency is unknown – pseudomembranous colitis;
• Infections and parasitic invasions: often – candidiasis;
• Disturbances from a nervous system: seldom (> 1/10 000, <1/1000) – neuropathy;
• Disturbances from immune system: seldom – allergic reactions (fever, urticaria, joint pains, a Quincke's disease, exfoliative dermatitis, an acute anaphylaxis with development of a collapse, a multiformny erythema, anaphylactoid reactions (a purpura, an asthmatic attack, symptoms from digestive tract)); very seldom – a toxic epidermal necrolysis, a malignant exudative erythema; frequency is unknown – a serum disease, Yarisha-Gerksgeymer's reaction; in the presence of the accompanying dermatomycoses – paraallergic reactions;
• Disturbances from blood and lymphatic system: very seldom (<1/10 000) – hemolitic anemia, thrombocytopenia, a leukopenia, an agranulocytosis;
• Disturbances from kidneys and urinary tract: seldom – intersticial nephrite, a nephropathy;
• Disturbances from a liver and biliary tract: frequency is unknown – a cholestasia, hepatitis;
• Disturbances from skin and hypodermic fabrics: frequency is unknown – pemphigoid;
• The general frustration and reactions in an injection site: frequency is unknown – local reactions (pain and infiltrates in the place of an injection), Nikolau's syndrome (an acute medicamentous vascular embolism of skin), Hoyn's syndrome (an acute penicillinic psychotic syndrome); at long therapy – superinfection.

Special instructions

Before Retarpen's appointment it is necessary to collect carefully the anamnesis of the patient regarding possible hypersensitivity to penicillin and/or another beta лактамным to antibiotics.

Considering risk of development heavy allergic, sometimes even fatal reactions, patients should be warned about need of drug withdrawal and the immediate address to the doctor in case of allergy symptoms in them.

In 5-10% of cases allergic reactions to penicillin can be cross with allergic reactions to cephalosporins in this connection penicillin is contraindicated to patients with instructions in the anamnesis on an allergy to cephalosporins.

Patients with skin allergic rashes and bronchial asthma have an increased risk of development of reactions of hypersensitivity therefore at least within 30 minutes after an injection they have to be under observation of the doctor. In case of allergic reaction it is necessary to cancel drug and to carry out if there is a need, symptomatic and/or antishock therapy.

At treatment of syphilis Yarisha-Gerksgeymer's reaction (a fever, fever, other local and general symptoms) can develop what patients have to be warned about.

At patients with a diabetes mellitus delay of absorption of drug in a system blood stream is possible.

Retarpen it is impossible to enter intravenously, subcutaneously, endolyumbalno, into perigastriums, and also into fabrics with the broken perfusion.

If solution accidentally gets under skin, there can be a painful consolidation. Applying of ice to an injection site allows to reduce morbidity.

At accidental intravascular introduction emergence of passing feeling of alarm and a vision disorder is possible. These symptoms usually pass within an hour. If the symptomatology is expressed strongly, administration of sedatives can be necessary.

At accidental intra arterial introduction of Retarpen, especially at children, such serious complications as a necrosis of fabrics (gangrene) and thrombosis of arteries can be observed. Their initial manifestations – pale spots on rump skin. As a result of high pressure in the place of an injection the retrograde throwing of drug in the general ileal artery, spinal arteries or an aorta is possible.

During treatment it is necessary to control periodically function of kidneys and a picture of peripheral blood.

Not to allow damage of a sciatic nerve, the peripheral area of an outside upper quadrant of a buttock for administration of drug at children and teenagers is used only in exceptional cases (for example, at widespread burns).

Grinding of a buttock after an injection is not recommended.

In case of suspicion of syphilis before Retarpen's appointment it is necessary to make a dark field method and then within 4 months serological researches. At inborn syphilis it is also necessary to investigate cerebrospinal fluid (SPZh). If (neurosyphilis) is not possible to exclude involvement in process of the central nervous system, it is necessary to use other drugs of penicillin which get into SMZh better.

In case of emergence during treatment of persistent heavy diarrhea it is necessary to suspect pseudomembranous colitis (it can be shown by a watery chair with slime/blood impurity, tenesmus, a diffusion spastic abdominal pain, fever). As this state can threaten life, it is necessary to cancel immediately Retarpen and to appoint the corresponding therapy taking into account sensitivity of the revealed pathogen. Not to use the drugs braking an intestines peristaltics.

Patients who adhere to a hyposalt diet have to consider the content of sodium in drug: in a dose of 1,2 million ME – 11 mg (0,48 mmol), in a dose of 2,4 million ME – 22 mg (0,96 mmol).

Due to the risk of fungal infections during treatment reasonablly simultaneous use of vitamins of group B and vitamin C. At suspicion on development of a fungal infection use of antifungal drug is required (for example, levorinum or nystatin).

At Retarpen's use in an insufficient dose, at too early termination of treatment, and also at long-term therapy resistant strains of activators can appear.

In rare instances povidone – one of Retarpen excipients – can collect in reticuloendothelial system owing to what development of a granuloma of which tumors can be formed further is possible.

During treatment it is necessary to be careful when driving the car and performing potentially dangerous types of works.

Medicinal interaction

Retarpen it is not necessary to apply along with bacteriostatic antibiotics (for example, chloramphenicol, macroleads, tetracyclines, linkozamida). The combination to other antibiotics is possible only when the additive effect of use of a combination of drugs is supposed synergy or at least.

It is not necessary to enter a benzatin benzylpenicillin in one syringe with other medicines.

With care Retarpen it is necessary to apply along with non-steroidal anti-inflammatory drugs (salicylates, phenylbutazone, indometacin), probenetsidy, Allopyrinolum since perhaps competitive inhibition of removal of drugs from an organism.

Retarpen increases efficiency of indirect anticoagulants therefore at use of this combination it is necessary to control carefully INR (the international normalized relation).

Digoxin increases risk of development of bradycardia.

Benzatina benzylpenicillin reduces removal of a methotrexate owing to what increase in its toxicity is possible.

Terms and storage conditions

To store in protected from light, the place, unavailable to children, at a temperature up to 25 °C.

Period of validity – 4 years.

It is possible to store the solution prepared from powder in the refrigerator no more than 24 hours.