Pensilina - instructions for use, doses, side effects, contraindications

The antibacterial component of the drug is ampicillin - an antibiotic from the group of semisynthetic penicillins, which has a bactericidal effect on sensitive microorganisms during the active propagation phase by inhibiting the biosynthesis of the mucopeptide of the cell wall. Sulbactam does not have clinically significant antibacterial activity (except for Neisseriaceae and Acinetobacter), it is an irreversible inhibitor of most of the major beta-lactamases that are produced by microorganisms resistant to beta-lactam antibiotics. Sulbactam also binds to certain penicillin-binding proteins, so some strains are more sensitive to the combination than to a single beta-lactam antibiotic.

Ammiside is active against a wide range of Gram-positive and Gram-negative bacteria, including Staphylococcus aureus and Staphylococcus epidermidis (including penicillin-resistant and some methicillin-resistant strains); Streptococcus pneumoniae, Streptococcus faecalis and other streptococci, Haemophilus influenzae and Haemophilus parainfluenzae (strains producing and not producing beta-lactamases), Branhamella catarrhalis, Escherichia coli, Klebsiella spp., Proteus spp. (indol-positive indolotricary), Morganella morganii, Citrobacter spp. and Enterobacter spp., Neisseria meningitidis and Neisseria gonorrhoeae; anaerobes, including Bacteroides fragilis, Peptococcus spp., Peptostreptococcus spp.n close to it species.

Pharmacokinetics:

Ammiside penetrates well into most tissues and fluids of the human body. Penetration through the blood-brain barrier is low, however, it improves with inflammation of the meninges. After intravenous or intramuscular injection, high concentrations of sulbactam and ampicillin in the blood are reached; the half-life of both drugs is approximately one hour. It is excreted by the kidneys - 70-80%, mainly in unchanged form, as well as with bile and breast milk. Sulbactam is almost not subjected to metabolic transformations and is excreted by the kidneys mainly in the unmodified form and only about 25% in the form of metabolites.

In patients with severe renal insufficiency (creatinine clearance ≤30 ml / min) the removal of sulbactam and ampicillin is disturbed to an equal degree, so the ratio of their concentrations in the plasma does not change.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms: infections of the upper, lower respiratory tract and ENT organs (including sinusitis, otitis media and epiglottitis,bacterial pneumonia); urinary and genital tract infections (including pyelonephritis, endometritis, cystitis, urethritis); infection of the biliary tract (cholecystitis, cholangitis); intra-abdominal infections (including peritonitis); infection of the skin, soft tissues; infection of bones and joints.

Septic endocarditis, sepsis; gonococcal infections.

Prevention of postoperative complications in operations on the abdominal and pelvic organs.

Contraindications:Hypersensitivity to ampicillin and sulbactam and other beta-lactam antibiotics, infectious mononucleosis, lymphocytic leukemia, severe impairment of liver and kidney function.

Carefully:Pregnancy, lactation.

Pregnancy and lactation:

If it is necessary to use in pregnancy, you should evaluate the expected benefit to the mother and the potential risk to the fetus.

If necessary, use during lactation should stop breastfeeding.

Dosing and Administration:

The drug is administered intramuscularly or intravenously (drip, jet).

Standard dosing regimen

The following are the total doses of ampicillin and sulbactam (in a 2: 1 ratio).

Adults: from 1500 mg to 12000 mg per day.With a mild infection, 1500-3000 mg / day in 2 injections; at an average current - 3000-6000 mg / day in 3-4 injections; in severe cases - 12000 mg / day in 3-4 injections.

For children: 150 mg / kg body weight per day (corresponding to 100 mg / kg / day ampicillin and 50 mg / kg / day sulbactam) every 6-8 hours in accordance with the usual practice of ampicillin.

Newborns under 1 week of age (especially premature infants): 75 mg / kg of body weight per day with an interval of 12 hours.

Elderly patients: usual doses for adults, without adjustments for age.

Use in patients with impaired renal function (creatinine clearance ≤30 ml / min): In such a patient, Ammiside should be administered less frequently in accordance with the usual practice of using ampicillin, increasing the interval between injections of the drug.

Duration of treatment:

The duration of the course of therapy is 5-14 days, but in more severe cases it can be increased or additionally assigned ampicillin. As always with antibiotic therapy, Ammiside should be administered to the patient for at least 48 hours after the normalization of temperature and the disappearance of other pathological symptoms.

Dosing in special cases:

Uncomplicated gonorrhea single intramuscular injection of 1500 mg of Ammiside. In order to increase the duration of the content of sulbactam and ampicillin in the plasma should be administered simultaneously probenecid at a dose of 1000 mg orally.

Prevention of postoperative infections, depending on the degree of infectious risk, 1500-3000 mg of Ammiside is administered during the initial anesthesia. The dose can be repeated every 6-8 hours; in most surgical interventions, the drug is usually discontinued 24 hours after the operation unless the administration of the drug for therapeutic purposes is shown.

Method of preparation of solutions

For intramuscular injection: the contents of the vial are dissolved as follows:

The contents of the vial 375 mg in 1.0 ml of the solvent (0.5% lidocaine hydrochloride solution) 750 mg in 1.8 ml of the solvent 1500 mg in 3.5 ml of the solvent.

As with other intramuscular injections, Ammiside is injected into a relatively large muscle (gluteal), trial aspiration helps to avoid unintentional insertion into the blood vessel. The drug, diluted with lidocaine, can not be administered intravenously.

For intravenous administration: for the initial dilution the contents of the vial are diluted as follows:

The contents of the vial 375 mg in 1.0 ml of the solvent (water for injection) 750 mg in 1.8 ml of solvent 1500 mg in 3.5 ml of solvent.

Then for intravenous infusion: a solution prepared at initial dilution containing a single dose of the drug is dissolved in 100-200 ml of a 0.9% solution of sodium chloride or 5-10% glucose solution. Enter with a speed of 60-80 drops per minute.

-for blasting: Cooked with an initial dilution of a solution containing a single dose of the drug is dissolved in 10-20 ml of 0.9% sodium chloride and injected slowly, over 3-5 minutes. Shake before use.

Side effects:

Allergic reactions: urticaria, flushing of the skin, angioedema, rhinitis, conjunctivitis, fever, arthralgia, eosinophilia, in rare cases - a rash, itching, rarely - bronchospasm, eosinophilia, serum sickness, anaphylactic shock, is very rare: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the gastrointestinal tract: nausea, vomiting, loss of appetite, diarrhea, pseudomembranous enterocolitis, liver dysfunction (cholestatic jaundice).

On the part of the organs of hematopoiesis and the system of hemostasis: anemia, hemolytic anemia, leukopenia, neutropenia, lymphopenia, thrombocytopenia and eosinophilia.

From the nervous system: drowsiness, malaise, headache, very rarely reported the appearance of seizures.

Laboratory indicators: transient increase in activity of alanine aminotransferase (ALT) and aspartic aminotransferase (ACT), Hyperbilirubinemia, azotemia, increased urea concentration, hypercreatininaemia.

Local reactions: phlebitis, soreness along the vein, soreness in the place of intramuscular injection.

Other: Very rarely reported cases of interstitial nephritis, with long-term treatment - superinfection caused by drug-resistant microorganisms (candidiasis).

Overdose:It should be borne in mind that high concentrations of beta-lactam antibiotics in the cerebrospinal fluid can cause disruption of the central nervous system, including convulsions. how ampicillin, and sulbactam are removed from the circulatory system by hemodialysis, therefore, when they are overdosed in patients with impaired renal function, in order to accelerate the elimination of drugs from the body, hemodialysis is recommended.

Interaction:

Anticoagulants: penicillins can alter platelet aggregation and indicators of hemocoagulation (increase the effect of anticoagulants).

Preparations with bacteriostatic action (chloramphenicol, erythromycin, sulfonamide preparations and tetracyclines): antagonistic action.

Oral contraceptives containing estrogen: reduces efficiency oral contraceptives, drugs, in the process of metabolism which produces paraaminobenzoic acid, and ethinyl estradiol (risk of bleeding "breakthrough").

Methotrexate: the joint administration of penicillins led to a decrease in the clearance of methotrexate and an increase in its toxicity. Such patients should be carefully observed.

Probenecid, diuretics, allopurinol, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that reduce tubular secretion, increase the concentration of ampicillin and sulbactam in the plasma, lead to their longer preservation in the blood, prolong the half-life and increase the risk of toxicity.

Sulbactam is compatible with most solutions for intravenous administration, however ampicillin and, consequently, Ammiside is less stable in solutions containing dextrose or other carbohydrates; is not pharmaceutically compatible with blood products or protein hydrolysates, aminoglycosides.

Influence on laboratory indicators: non-enzymatic methods for determining the concentration of glucose in the urine, using Benedict, Feling or Klinist's reagents can give a false positive result. It was noted that the use of ampicillin in pregnant women led to a transient decrease in plasma levels of the total bound estriol, estriol-glucuronide, and also bound estrone and estradiol.

Allopurinol: increases the risk of skin rash.

Bactericidal antibiotics: (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) have a synergistic effect.

Special instructions:

In the treatment of penicillins, serious and sometimes fatal allergic (anaphylactic) reactions are described. In case of an allergic reaction, it is necessary to cancel the drug and prescribe the appropriate treatment. If necessary, designate epinephrine (adrenalin), oxygen, glucocorticosteroid hormones intravenously and take measures to improve airway patency, including intubation.

In the treatment of patients with sepsis, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

In the treatment of patients receiving a diet low in sodium, it must be taken into account that 1500 mg of Ammiside contains approximately 115 mg (5 mmol) of sodium.

As with any antibiotic, constant monitoring is important to identify signs of excess growth in insensitive microorganisms, including fungi. When superinfection occurs, the drug should be discontinued and / or an adequate therapy should be prescribed.

During prolonged therapy with the drug, it is recommended to periodically monitor the indices of the function of the internal organs, including the kidneys, the liver and the hematopoiesis system. This is especially important for newborns (especially premature babies) and young children.

Form release / dosage:Powder for solution for intramuscular injection: 1000 mg + 500 mg, 500 mg + 250 mg, 250 mg + 125 mg.

Packaging:

Powder for solution for intramuscular injection: 1000 mg + 500 mg, 500 mg + 250 mg, 250 mg + 125 mg in a vial of colorless glass sealed with a cork made of bromobutyl rubber, crimped with an aluminum ring or an aluminum cap "flip off".

Solvent (solution of lidocaine hydrochloride 0.5%): 3.5 ml, 1.8 ml, 1 ml in a vial of colorless glass.

For 1 bottle with the drug and 1 ampoule with a solvent, along with instructions for use in a cardboard pack. 100 bottles of the drug are placed in a cardboard box (for hospitals) with instructions for use (50 pieces).

Storage conditions:

At a temperature of no higher than 25 ° C, in a dry, dark place.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014013 / 01

Date of registration:12.02.2009 / 07.04.2017

Expiration Date:Unlimited

The owner of the registration certificate:Mustafa Nevzat Ilach Sanai A.Sh.Mustafa Nevzat Ilach Sanai A.Sh. Turkey

Manufacturer: & nbsp

MUSTAFA NEVZAT ILAC SANAYII, A.S. Turkey

Information update date: & nbsp20.08.2017

Illustrated instructions

Instructions

Pensilina (Pensilina)