Ampisulbin

General characteristics. Structure:

Active ingredients: ampicillin, sulbactam;
1 bottle contains 1,5 g of sterile mix of ampicillin of sodium salt and a sulbaktam of sodium salt in the ratio 2:1, in terms of ampicillin of 1,0 g and to sulbakta of 0,5 g.

Pharmacological properties:

Pharmacodynamics. Амписульбин® – the combined drug possessing a wide range of antibacterial (bactericidal) action. Ampicillin – semi-synthetic penicillin of a broad spectrum of activity, is the bactericidal Ampisulbina® component, affects sensitive microorganisms in a phase of active reproduction by oppression of biosynthesis of a mukopeptid of a cell wall. Sulbaktam has no the expressed antibacterial activity, he strengthens
antimicrobic action of other antibiotics. Thanks to a combination of a sulbaktam of sodium and ampicillin of sodium the range and expressiveness of antimicrobic action of components of drug extends. Амписульбин® it is active in relation to the majority of gram-positive and gram-negative microorganisms: Staphylococcus spp. (including the strains producing β - lactamazu); Streptococcus spp., including S. pyogenes, S. viridans, S. pneumoniae, S. Faecalis; Haemophilus influenzae and H. parainfluenzae (including the strains producing β - lactamazu); Branhamella catarralis; Neisseria meningitidis, N.gonorrhoeae; Escherichia coli; Klebsiella spp.; Proteus spp. (indolpositive and indolnegative strains); Citrobacter spp.; Enterobacter spp.; Morganella morganii; Clostridium spp.;
asporous anaerobe bacterias – Peptococcus spp. and Peptostreptococcus spp.; Bacteroides spp., including Bacteroides fragilis.

Pharmacokinetics. Pharmacokinetic parameters of a sulbaktam and ampicillin match. The maximum concentration in blood and an elimination half-life of ampicillin at its use in combination with sulbaktamy are similar to the corresponding indicators at administration of one ampicillin in an equivalent dose. Амписульбин® it is well distributed in the majority of fabrics and liquids of an organism, well gets into bile, a phlegm, pus. Penetration into liquids of a head and spinal cord low, however amplifies in the presence of an inflammation of a meninx. Concentration of components in pleural and peritoneal liquid corresponds to concentration which are observed in blood serum. In low concentration it is found in breast milk. Depending on a dose and a way of introduction Ampisulbin® it is found in blood within 6-8 hours. Elimination half-life sostavlyaetprimerno 1 hour. It is removed preferential with urine (75-80%) in not changed look.
Pharmaceutical characteristics. Main physical and chemical properties: powder of color, white or white with a yellowish shade. Incompatibility. Амписульбин® it is inadmissible to mix in one capacity with other medicamentous means. Drug pharmaceutical is incompatible with tetracycline,
chloramphenicol (levomycetinum), Amphotericinum, clindamycin, erythromycin, lincomycin, metronidazole, polymyxin B, Acetylcysteinum, Chlorpromazinum, gidralaziny, dopamine, heparin, Metoclopramidum.

Indications to use:

Infections of upper and lower respiratory tracts (sinusitis, average otitis, bacterial pneumonia); infections of uric ways and pyelonephritis, intra belly infections (peritonitis, cholecystitis, endometritis); sepsis, infections of skin, soft tissues, bones and joints, and also gonococcal infections. Preoperative prevention of purulent complications in surgery, obstetrics and gynecology.

Route of administration and doses:

Before use carry out an intracutaneous test on hypersensitivity to an antibiotic and solvent. Амписульбин® apply intravenously and intramusculary. Such cultivations can be applied:

The general     Equivalent       Volume             Volume              Maximum
dose         dose                     of a bottle (ml)   of solvent      final
()          sulbaktama/                                (ml)                  concentration
               ampicillin (g)                                                     (mg/ml)
      0,375 0,125 - 0,25                                                    10 0,8 125 - 250
         0,75 0,25/0,5                                       10 1,6                   125/250
           1,5 0,5/1                                             20 3,2                 125/250
             3 1/2                                              20 6,4                  125/250
0,75                        0,25 - 0,5 100 ml                             of PBU 25 10 - 20
                              1,5 0,5 - 1 100 ml                            of PBU 50 10 - 20
3                                     1 - 2 100 ml                           of PBU 100 10 - 20

For intravenous administration of Ampisulbin® it is necessary to part with sterile water for injections or any other compatible solution and to allow to stand before total disappearance of the formed foam visually to estimate completeness of dissolution. The dose can be entered in the form of a bolyusny injection for at least 3 minutes. And at higher cultivation the dose can be entered both in the form of a bolyusny injection, and in the form of intravenous infusion throughout 15 − 30 minutes. Sulbaktam sodium sodium/ampicillin for parenteral use can also be entered deeply into a muscle; if injections painful, then for dissolution of powder it is possible to use 0,5% sterile solution of lidocaine of a hydrochloride for injections.
Use by the adult
As a rule, the dose of Ampisulbina® varies from 1,5 to 12 g/days for several receptions each 6 or 8 hours; the maximum daily dose of a sulbaktam makes 4 g. At less heavy infections the drug can be administered in 12 hours.

Weight of an infection            Daily dose of Ampisulbina®
                                        intramusculary,
                                       intravenously ()
Easy                               1,5 - 3 (from 0,5 + 1 to 1 + 2)
Moderately severe               to 6 (2 + 4)
Heavy                             to 12 (4 + 8)
       
Frequency rate of introduction of a dose depends on severity of a disease and function of kidneys of the patient. As a rule, treatment is continued on an extent of 48 hours after normalization of body temperature and disappearance of other pathological signs. Duration of a course of therapy makes 5 - 14 days, however in more hard cases it can be increased or in addition to appoint ampicillin.
1 500 mg of a sulbaktam of sodium/ampicillin of sodium contain about 115 g (5 mmol) of sodium.
For prevention of surgical infections the dose of Ampisulbina® makes 1,5 - 3, it should be entered into time of an anesthesia which provides enough time for achievement of effective concentration in serum and fabrics during operation. The dose can be entered repeatedly every 6 - 8 hours; in the majority of surgical interventions of use of an antibiotic, as a rule, stop in 24 hours after operation if introduction of Ampisulbina® with the medical purpose is not shown. For treatment of uncomplicated gonorrhea of Ampisulbin® it is possible to enter 1 time in a dose of 1,5 g. For the purpose of increase in duration of presence of a sulbaktam and ampicillin in plasma it is necessary to appoint at the same time пробенецид in a dose 1 g orally.
Use for treatment of children
During treatment of the majority of infections at newborns and children the dose of Ampisulbina® makes 150 mg/kg/days (that answers 50 mg/kg/days of a sulbaktam and 100 mg/kg/days of ampicillin).
To children, babies and newborns the drug is administered, as a rule, by each 6 - 8 hours according to customary practice of use of ampicillin.
The newborn during the first week of life (especially premature) drug, as a rule, appoint in a dose 75 mg/kg of body weight (that answers 25 mg/kg/days of a sulbaktam and 50 mg/kg/days of ampicillin) with an interval of 12 hours.
Use by the patient with an impaired renal function.
At patients with a heavy renal failure (the clearance of creatinine <30 ml/min.) removal of a sulbaktam and ampicillin is broken equally therefore their ratio in plasma does not change. Such patients of Ampisulbin® should enter less often according to customary practice of use of ampicillin. Strong solution for intramuscular use should be used for 1 hour after dissolution. Usage time of drug for intravenous infusion, depending on type of the chosen solvent, is given below:

                                                        Concentration Storage Time solvent
                                                  сульбактама / ampicillin    
                                                                                                       °C t=4 °C t=25
Sterile water for injections       to 45 mg/ml                               8      
                                                            45 mg/ml                                          48
                                                      to 30 mg/ml                                           72
0,9% sodium chloride solution       to 45 mg/ml                               8
                                                          45 mg/ml                                          48
                                                     to 30 mg/ml                                         72
M/6 sodium lactate solution            to 45 mg/ml                              8
                                                      to 45 mg/ml                                           8
5% aqueous solution            of glucose 15 − 30 mg/ml                         2
                                                      to 3 mg/ml                                 4
                                                      to 30 mg/ml                                           4
5% aqueous solution of a glyuzoza in      to 3 mg/ml                                4
0,45% sodium chloride solution    to 15 mg/ml                                           4
10% aqueous solution invert   to 3 mg/ml                                4
sugar                                          to 30 mg/ml                                          3
Ringer's solution lactat            to 45 mg/ml                              8
                                                     to 45 mg/ml                                           24

Features of use:

Before therapy it is necessary to exclude existence at the patient of hypersensitivity to ampicillin and other β-laktamny antibiotics. In the course of treatment systematic control of function of kidneys, a liver and a picture of peripheral blood is necessary. At bronchial asthma, hay fever and other allergic diseases drug is used along with desensibilizing
means. At use of high doses for patients with a renal failure perhaps toxic action on TsNS. Prolonged or repeated use can lead to rapid growth of resistant
microflorae, to development of the superinfection caused by resistant microorganisms. Ability to influence speed of response at control of motor transport or work with other mechanisms. During treatment by drug at some patients emergence of side reactions from the central nervous system is possible (see the section "Side reactions") therefore it is necessary to be careful at
control of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Allergic reactions: rash, an itch, a hyperemia, urticaria, rhinitis, conjunctivitis, it is rare – fever, a joint pain, an eosinophilia, exfoliative dermatitis, a purpura, a multiformny exudative erythema, Stephens-Johnson's syndrome, is very rare – a Quincke's edema, breath difficulty, an acute anaphylaxis.
From a digestive tract: nausea, vomiting, diarrhea, taste changes, an abdominal pain, stomatitis, a glossitis, dryness in a mouth, intestinal dysbacteriosis, gastritis, a coloenteritis, hemorrhagic colitis. In the course of treatment or within several weeks after the end of antibiotic treatment there is a probability of development of pseudomembranous colitis.
From a liver and gepatobiliarny system: hepatitis, cholestatic jaundice.
From the central and peripheral nervous system: at use of high doses for patients with a renal failure – dizziness, a headache, a tremor, spasms, neuropathy, a hyperphrenia.
Local reactions: hypostasis, an itch, a hyperemia in an injection site.
Laboratory indicators: moderate increase in activity of "hepatic" transaminases, lactate dehydrogenases, alkaline phosphatase, creatinine, lozhnopolozhitelena results of non-enzymatic glyukozurichesky tests and Koombs's reaction.
Others: reversible disturbances of a hemogenesis (leukopenia, thrombocytopenia, hemolitic anemia, agranulocytosis), intersticial nephrite, superinfection, candidiasis. At Ampicillin use by the patient with bacteremia (sepsis) reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.

Interaction with other medicines:

Амписульбин® increases effect of anticoagulants, antibiotics of an aminoglikozidny row, reduces effect of oral contraceptives. At simultaneous use of Ampisulbina® with peroral estrogensoderzhashchy drugs decrease in their efficiency due to easing hepatic is noted
circulation of estrogen. Probenetsid reduces canalicular secretion of Ampisulbina® therefore the risk of development of its toxic action increases. The probability of emergence of skin rash raises Allopyrinolum. High doses of Ampisulbina® reduce the level of an atenolol in a blood plasma therefore
it is recommended to use these drugs separately, at first to accept атенолол, and after it – Ampisulbin®.
Амписульбин® reduces clearance and increases toxicity of a methotrexate, strengthens digoxin absorption.
At interaction of ampicillin with macroleads, paromomitsiny, tetracyclines, chloramphenicol the effect of both drugs decreases. Амписульбин® can reduce effect of Natrium benzoicum.
At simultaneous use with blockers of β-adrenoceptors the probability of emergence of anaphylactic reactions increases.

Contraindications:

Hypersensitivity to drug components, to penicillin and other β-laktamny antibiotics; digestive tract diseases (the colitis connected with reception of antibiotics); infectious mononucleosis; serious illness of a liver and kidneys; feeding period breast; leukemia; HIV – infections.

Use during pregnancy or feeding by a breast. The teratogenic effect of Ampisulbina® is not revealed. However use of Ampisulbina® during pregnancy perhaps only in that case when the expected advantage for the woman exceeds potential risk for a fruit.
Амписульбин® gets into breast milk in low concentration. During treatment by drug it is necessary to stop feeding by a breast.
Children. It is necessary to be careful at drug use to children, especially if in the anamnesis of mother there is a hypersensitivity case to β-laktamny antibiotics.

Overdose:

At overdose perhaps toxic impact on the central nervous system (dizziness, a headache), the dispeptic phenomena (nausea, vomiting, a liquid chair), allergic reactions in the form of skin rash. In case of symptoms of overdose drug should be cancelled immediately and if necessary to carry out a symptomatic treatment: gastric lavage, use of activated
coal, salt laxatives, correction of water and electrolytic balance, hemodialysis. At an allergy the antihistaminic and desensibilizing means are shown.

Storage conditions:

Period of validity 3 years. To store in original packaging, at a temperature not over 25 ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 1,5 g in bottles; in bottles No. 10 in a pack.