Sultasin

General characteristics. Structure:

Active agents                 of 500          mg +250 mg 1000 mg +500 mg
Sodium ampicillin
(in terms of ampicillin)        500                      mg 1000 mg
Sulbaktam of sodium
(in terms of sulbakta)          250                        mg 500 mg.

Pharmacological properties:

Сультасин® - a bactericidal antibiotic of a broad spectrum of activity, кислотоустойчив. Blocks synthesis of a peptidoglikan of a cell wall of microorganisms.

Effective agent is ampicillin - the semi-synthetic penicillinic antibiotic of a broad spectrum of activity collapsing β-lactamelements of bacteria.

Sulbaktam - irreversible inhibitor β-лактамаз which are allocated with the microorganisms steady against a beta laktamnym to antibiotics. Prevents hydrolysis and destruction of penicillin and cephalosporins β-lactamelements of steady microorganisms. Contacting penitsillinsvyazyvayushchy proteins, shows a synergism at simultaneous use with penicillin and cephalosporins. Sulbaktam is active only against Neisseria spp. and Acinetobacter spp.

It is active concerning gram-positive aerobes: Staphylococcus aureus (which are producing and not producing β-lactamelements strains), Staphylococcus epidermidis (which are producing and not producing β-lactamelements strains), Staphylococcus saprophyticus (which are producing and not producing β-lactamelements strains), Streptococcus pneumoniae (including the strains steady against penicillin), Streptococcus pyogenes, Streptococcus spp. groups viridans, Enterococcus faecalis, Listeria monocytogenes; gram-negative aerobes: Haemophilus influenzae (including the strains steady against ampicillin), Moraxella catarrhalis (which are producing and not producing β-lactamelements strains), Escherichia coli, Klebsiella spp., Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Morganella morganii, Neisseria gonorrhoeae (which are producing and not producing β-lactamelements strains), Neisseria meningitidis; anaerobe bacterias: Clostridium spp. (except Clostridium difficile), Peptococcus spp., Peptostreptococcus spp., Bacteroides spp., including Bacteroides fragilis.

Are steady against the drug Sultasin®: metitsillinoustoychivy Staphylococcus spp., majority of strains of Enterobacter spp., Cirobacter spp., Pseudomonas aeruginosa, Clostridium difficile, Mycobacterium spp., Chlamydia spp. and mycoplasmas.

 

Pharmacokinetics. Absorption and distribution

Later in/in and introductions in oil are reached high concentration of ampicillin and a sulbaktam in blood.

Ampicillin and to sulbakta get into the majority of fabrics and liquids of an organism, are allocated with breast milk. At an inflammation permeability in cerebrospinal fluid sharply increases.

Metabolism and removal

T1/2 of ampicillin and sulbaktam - 1 h. Are removed by kidneys - 70-80%, it is preferential in not changed look, and also with bile.

Sulbaktam is almost not exposed to metabolic transformations and also only about 25% in the form of metabolites are removed by kidneys, mainly, in not changed look.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:

— infections of a respiratory organs (including pneumonia, chronic bronchitis);

— infections of ENT organs (including sinusitis, tonsillitis, average otitis, quinsy);

— infections of urinary tract and generative organs (pyelonephritis, pyelitis, cystitis, urethritis, cervicitis, uncomplicated gonorrhea);

— infections of biliary tract (cholecystitis, cholangitis);

— GIT infections (peritonitis, abscess of an abdominal cavity);

— infections of skin and soft tissues (the ugly face, impetigo for the second time infected dermatitis);

— infections of bones and joints;

— sepsis;

— septic endocarditis;

— meningitis.

Prevention of postoperative complications at abdominal organs operations and a small pelvis.

Route of administration and doses:

The drug is administered in oil or in/in (kapelno with a speed of 60-80 thaws/min., struyno - slowly, within 3-5 min.). In/in enter within 5-7 days, then in need of continuation of treatment pass to introduction in oil.

Total doses of ampicillin and sulbaktam are provided below (in the ratio 2:1).

Adult at the easy course of an infection appoint 1.5-3 g/days in 2 introductions; at a medium-weight current - 3-6 g / in 3-4 introductions; at a heavy current - 12 g/days in 4 introductions.

At uncomplicated gonorrhea - 1.5 in oil once.

For prevention of surgical infections - 1.5-3 g in/in during anesthesia; then during 24 h after operation - in the same dose each 6-8 h.

To children drug is appointed in a daily dose at the rate of 150 mg/kg of body weight (100 mg/kg of ampicillin and 50 mg/kg of a sulbaktam); frequency rate - 3-4

At children from 1 month to 12 years (or with a body weight up to 40 kg) at therapy of heavy infections the dose is increased to 300 mg/kg/days

The newborn aged up to 1 week and to premature children drug each 12 h appoint in a dose 75 mg/kg (50 mg/kg of ampicillin and 25 mg/kg of a sulbaktam)/. A course of treatment - 5-14 days (if necessary it can be prolonged). After normalization of temperature and disappearance of other pathological symptoms treatment is continued during 48 h.

At a renal failure and decrease in clearance of creatinine lower than 30 ml/min. are reasonable increase in intervals between introductions up to 12-24 h.

Rules of preparation of solution

Solution for parenteral use is prepared just before use.

For introduction in oil add to contents of a bottle of 0.75 g 2 ml, and a bottle of 1.5 g - 4 ml of water for injections, either 0.5% of solution of Procainum (novocaine), or 0.9% of solution of sodium of chloride. For introduction in oil cultivation of 0.5% lidocaine solution is admissible.

For in/in introductions the single dose is dissolved in 0.9% solution of sodium of chloride or 5% solution of a dextrose (glucose) in volume from 10 ml to 200 ml.

Features of use:

At the patients having hypersensitivity to penicillin cross allergic reactions with tsefalosporinovy antibiotics are possible.

At course treatment it is necessary to carry out control of a condition of functions of bodies of a hemopoiesis, a liver and kidneys.

Development of superinfection due to growth of microflora, insensitive to drug, is possible that demands corresponding change of antibacterial therapy.

At treatment of patients with sepsis development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.

Influence on ability to driving of motor transport and to control of mechanisms

Data on negative influence of the drug Sultasin® in the recommended doses on ability to driving of motor transport and control of mechanisms are absent.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, loss of appetite, anorexia, increase in activity of hepatic transaminases, pseudomembranous colitis.

From a nervous system: drowsiness, indisposition, headache.

From bodies of a hemopoiesis: anemia, leukopenia, thrombocytopenia.

Allergic reactions: small tortoiseshell, hyperemia of integuments, Quincke's disease, rhinitis, conjunctivitis, fever, arthralgia, eosinophilia, acute anaphylaxis.

Laboratory indicators: azotemia, increase in content of urea, giperkreatininemiya.

Local reactions: at introduction in oil - morbidity in an injection site; at in/in - phlebitis.

Others: at prolonged treatment - the superinfection caused by microorganisms, steady against drug, (candidiasis).

Interaction with other medicines:

Bactericidal antibiotics (including cephalosporins, Cycloserinum, Vancomycinum, rifampicin), aminoglycosides have sinergidny effect; bacteriostatic antibiotics (including macroleads, chloramphenicol, linkozamida, tetracyclines) - antagonistic.

Increases efficiency of indirect anticoagulants (suppresses intestinal microflora, reduces vitamin K synthesis, raises a prothrombin time).

Reduces efficiency of oral contraceptives, medicines in the course of which metabolism para-aminobenzoic acid and ethinylestradiol (risk of development of bleedings of "break") is formed.

Diuretics reduce clearance of penicillin.

Allopyrinolum, phenylbutazone, NPVP, пробенецид, reducing canalicular secretion, increase concentration of penicillin in plasma.

Allopyrinolum increases risk of development of allergic reactions (skin rash).

Pharmaceutical interaction

Сультасин® pharmaceutical it is incompatible with antibiotics of group of aminoglycosides, with products of blood or proteinaceous hydrolyzates. When Sultasin® and aminoglycosides are appointed jointly, it is necessary to enter them into different body parts and with time difference between injections not less than 1 h.

Contraindications:

— infectious mononucleosis;

— lactation period (breastfeeding period);

— hypersensitivity.

With care it is necessary to appoint at a liver and/or renal failure, pregnancy.

 

Use of the drug SULTASIN® at pregnancy and feeding by a breast
At pregnancy of Sultasin® it is necessary to apply only if the expected effect of therapy exceeds potential risk for a fruit.

Сультасин® it is contraindicated to use during breastfeeding.

 

Use at abnormal liver functions
With care it is necessary to appoint at a liver failure.

 

Use at renal failures
At a renal failure and decrease in clearance of creatinine lower than 30 ml/min. are reasonable increase in intervals between introductions up to 12-24 h.

 

Use for children

To children drug is appointed in a daily dose at the rate of 150 mg/kg of body weight (100 mg/kg of ampicillin and 50 mg/kg of a sulbaktam); frequency rate - 3-4

At children from 1 month to 12 years (or with a body weight up to 40 kg) at terapiityazhely infections the dose is increased to 300 mg/kg/days

The newborn aged up to 1 week and to premature children drug each 12 h appoint in a dose 75 mg/kg (50 mg/kg of ampicillin and 25 mg/kg of a sulbaktam)/. A course of treatment - 5-14 days (if necessary it can be prolonged). After normalization of temperature and disappearance of other pathological symptoms treatment is continued during 48 h.

Overdose:

Symptoms: manifestation of toxic action on TsNS (especially at patients with a renal failure); nausea, vomiting, diarrhea, disturbance of water and electrolytic balance (as a result of vomiting and diarrhea).

Treatment: symptomatic. It is removed by means of a hemodialysis.

Storage conditions:

Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature not above 20 °C. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Bottles of 10 ml (1) - packs cardboard.
Bottles of 10 ml (50) - boxes cardboard.