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Ampicillin Biotika Injection 0,5g, 1,0g



                                                    AMPICILLIN 0,5 BIOTIKA
                                          AMPICILLIN 1,0 BIOTIKA

    Ampicillin 0,5 Biotika:         Ampicillinum natricum 0.53 g, responds to ampicillinum 0.5 g in injection vial

    Ampicillin 1,0 Biotika:         Ampicillinum natricum 1.06 g, responds to ampicillinum 1.0 g in injection vial

    1 g of Ampicillin Biotika contains 2.7 mmol Na.


Powder for solution for injection
Description of drug substance: white powder


4.1 Therapeutic indications
Ampicillin is an antibiotic drug of first choice in infections of lower airways with purulent expectoration, induced by pneumococci, hemophilia or mixed microflora; in acute bronchitis, broncholitis and in pneumonia in children (if there is no evidence of separate staphylococcal etiology, or in combination with oxacillin), in acute epiglottitis, in otitis media in newborns and children of preschool age; in nasosinusitis. In treatment of acute exacerbations of chronic bronchitis ampicillin is indicated primarily in mono-infection by pneumococci.
In infections of urinary tract ampicillin is administered only in second order, if it is not more suitable to use short-time sulfonamides, cotrimoxazol or oxytetracycline. If a microorganism is sensitive, ampicillin is indicated in infections of biliary tract, digestive tract, in purulent meningitis (particularly hemophiliac, pneumococcal, meningococcal, streptococcal and enterococcal etiology), in bacterial endocarditis, in septicemia or also in peritonitis.
Ampicillin is used also for treatment of typhoid fever or paratyphoid fever (if chloramphenicol cannot be used) and for sanation of bearers of salmonella in gall-bladder and biliary tract within a complete antibiotic-surgery treatment.
In heavy mixed infections (e.g. in peritonitis) ampicillin can be combined beneficially with amino-glycoside antibiotics of gentamicin type. 

4.2. Posology and method of administration
Ampicillin is applied parenterally especially in heavy infections, when high doses have to be applied, eventually for beginning of treatment which is continued with per oral application of ampicillin.
Daily dose is divided into 4 doses which are applied intramuscularly or intravenously in 6 hour intervals. Doses lower than 6 g daily per 1–1.5 in 4 – 6 partial doses, higher doses exceeding 6 g daily are applied by intravenous infusion.

Adults are applied usually the daily dose of 2 – 3 g, i.e. 500 mg each 4 to 6 hours, in heavy infections up to 200 mg/kg of body weight and day.
Daily dose for children is 1.7 – 2.3 g/m² of body surface or 50 – 400 mg/kg of body weight, i.e.:
children younger than 1 year 0.25 – 1.0 g
children from 1 to 6 years         1.0 – 2.0 g
children from 6 to 15 years         2.0 – 4.0 g

At treatment of bearers of salmonella the daily dose for adults is 6 – 8 g in doses in 6 hours intervals, thereof 4 times daily per 0.5 g i.v. in the first week of treatment and in the following weeks of treatment 1 g per os in 8 hours intervals. At the same time 1 g of probenecid is applied 2 times daily in order to maintain high plasmatic levels of ampicillin.
In heavy bacterial meningitis the daily application is up to 400 mg/kg of body weight by intravenous injection or infusion. Ampicillin may be applied also intrathecally in one daily dose: to children younger than 2 years 5 – 10 mg, to children from 2 to 12 years 10 – 20 mg, to adults 20 – 40 mg. In significantly impaired renal function the maintenance dose is reduced to 2/3, or even to 1/3 or the dosing interval is prolonged to 8 to 12 hours. By insufficient liver with prolonged biological half-life the doses have to be reduced accordingly. Application of the antibiotic in current infections should take 7 – 14 days, in more serious infections also longer. 
Injection solution of ampicillin is prepared immediately before the application.
For intramuscular application the solution is prepared by dissolving 0.5 g of ampicillin in 2 to 3 mL (1.0 g in 4 to 6 mL) of water for injection and injected deep intragluteally. 
Injection solution for slow intravenous injection is prepared by dissolving 0.5 g in 10 to 30 mL (1.0 g in 20 to 60 mL) of isotonic solution of sodium chloride.
Solution for intravenous infusion is prepared at a concentration of 0.2 to 3.0 % in suitable infusion solution.
Solution for intrathecal application is prepared at a concentration of 1 to 2 % in isotonic solution of sodium chloride.
Children younger than 2 years are applied 0.5 mL, children at the age from 2 to 12 years 1 mL and adults 2 mL of 1 – 2 % of solution of antibiotic in isotonic solution of sodium chloride.

4.3. Contraindications 
Hypersensitivity to penicillins, heavy hepatic insufficiency, infectious disorders induced by strains resistant to ampicillin, especially by pseudomonades and staphylococci.
Because of possible development of hypersensitivity the relative contraindications are hypersensitivity to cephalosporins, any allergy in anamnesis, bronchial asthma, hay fever or urticaria, secondary infection during infection mononucleosis, lymphatic leukemia.

4.4. Special warnings and precautions for use
It is required to prove sensitivity of infectious agens in laboratory before the drug product is used. If the high doses of ampicillin are given, particularly for a longer time, it is necessary to check the hepatic function, especially the changes of S-AST, blood count and urine.
Drug product contains 2.7 mmol Na.
Allergic reaction is an indication for interruption of application of the drug product. In anaphylactic shock it is necessary to treat the blood circulation failure and breathing disorders by adrenaline, noradrenaline, hydrocortisone, to apply calcium and antihistamines. Proceed according to the principles on treatment of these reactions. 
Female patients who use per oral hormonal contraception should be warned of the necessity of alternative contraception.
Do not use alcohol during the application period of the drug product.

4.5. Interaction with other medicinal products and other forms of interaction 
Cross sensibilisation of penicillins and cephalosporins. In concomitant application with bacteriostatic antibiotics (tetracyclines, chloramphenicol, erythromycin and other) an antagonism occurs. In the contrary, the combination with aminoglycosides has synergic effect and expands antimicrobial spectrum, what is used in the therapy.
Concomitant application of diuretics decreases the plasmatic concentration of ampicillin.
Ampicillin can decrease the effect of per orally applied contraception containing estrogen in regard to its effect on bacterial flora of digestive tract.
In application with allopurinol increases the frequency of incidence of allergic skin reactions.
Concomitant application of probenecid decelerates the secretion; however in children to 2 years probenecid is contraindicated. In patients treated with anticoagulants there is a possibility of bleeding prolongation.

4.6. Pregnancy and lactation
Penicillins cross the placental barrier and in small quantity they pass into breast milk. Though the reproduction studies in mammalian did not prove any sings of fertility disorders or damages of fetus, ampicillin should be used in pregnancy only in really necessary cases. It is necessary to be careful in use of ampicillin in case of breast-feeding women in regard to the fact that ampicillin is secreted by breast milk. 

4.7. Effects on ability to drive and use machines
Data on effect of ampicillin on ability to drive and use machines are not available.

4.8. Undesirable effects
The risk of anaphylactic reaction, cross sensibilization with penicillins and cephalosporins cannot be excluded. Adverse reactions occur mostly between the 7th to 10th day from the beginning of treatment and appear in 10 to 15 % of patients. Skin disorders appear in 6 to 8 % (exanthema, urticaria, pruritus), rarely Stevenson-Johnson’s and Lyell´s syndromes. Digestive tract disorders can occur, as well as nausea, diarrhea, vomiting which are not usually the reasons for interruption of treatment and after its ending they retreat spontaneously. Pseudomembranous colitis may be developed very rarely. Rare incidence of psychic and nervous disorders (headache, somnipathy, personality disorders). The renal function impairments; edema; dyshematopoiesis (purpura, thrombocytopenia) are reported too. After intravenous or intramuscular application there can appear local skin irritation, pain feeling or thrombophlebitis around injection site.  

4.9. Overdose
In regard to large therapeutic range the overdose by ampicillin was not described. In potential overdose the therapeutic procedure would be symptomatic, or haemodialysis is indicated.


5.1. Pharmacological properties

Pharmacotherapeutic group:     antibiotic 
ATC code:                             J01CA01

Penicillin semi-synthetic bactericidal broad-spectrum antibiotic, sensitive to beta-lactamase of golden staphylococci. Mechanism of bactericidal effect of ampicillin consists in blockage of synthesis of bacterial cell wall with consequent bacteriolysis. 
Antimicrobial spectrum: ampicillin acts on all strains of hemolytic streptococci (including streptococci of A and B groups), on viridating streptococci, pneumococci and enterococci (80 – 98 %), further on corynebacteria, listeria, Erysipelothrix insidiosa, bacillus of anthrax, and also on actinomyces, less on clostridia. From staphylococci, it has effect only on the strains, which do not produce beta-lactamase, i.e. about on 10 – 20 % of strains.
From gram-negative bacteria it has a good effect on gonococci and meningococci, on salmonellas (on about 90 % of strains). Less sensitive are haemophili and bordetella (about 60 – 70 % strains), Escherichia coli (60 %), shigella (40 – 90 %), klebsiella and enterobacteria (15 %), providencia and citrobacteria (30 %); from protea it acts on about 60 % of Proteus mirabilis strain, but only on 5 – 20 % of strains of other biotypes (Proteus vulgaris, morganii and rettgeri). From other strains sensitive are brucella, leptospira and treponema.
From anaerobes, most of gram-positive cocci and bacteria are sensitive, except B. fragilis. It does not act on yersinia, francisela, pseudomonades, mycobacteria, mycoplasmas, rickettsias, bedsonias, fungi and protozoa. 

5.2. Pharmacokinetic properties
After intramuscular, but particularly after intravenous application the maximal plasmatic concentration is reached in ½ - 1 hour and is 2 – 4 times higher than by per oral application of the same dose. Ampicillin enters well into most tissues and body cavities; it penetrates the cerebrospinal liquor of healthy persons, but in meningitis its level in liquor is significantly higher. The concentrations comparable with plasmatic ones are reached in liver and in kidneys. 
It crosses the placental barrier and in low concentrations it passes into breast milk. Ampicillin is secreted well into bile, where it creates therapeutically effective concentrations. 
It is eliminated by kidneys, mainly tubular secretion, only a little by glomerular filtration. Inhibitor of tubular secretion – probenecid prolongs half-life of ampicillin in organism and increases its plasmatic concentration. Within 24 hours 64 % of the applied dose is secreted by urine after intramuscular application, 70 % after intravenous application. Biological half-life is about 1 hour. In renal failure the biological half-life is prolonged to 12-20 hours. Ampicillin may be removed by haemodialysis.

5.3. Preclinical safety data
Ampicillin is practically non-toxic, the LD50 values were not determined because the doses of 5 g/kg of weight per or and 2 g/kg of weight intravenously were tolerated by mice without a death.
Reproduction studies and studies on teratogenity on animals did not prove any signs of fertility disorders or damage of fetus under the influence of ampicillin application.


6.1. List of excipients

6.2. Incompatibilities
In concomitant parenteral application of beta-lactamase antibiotics and aminoglycosides the mutual inactivation may occur. If these antibacterial substances are applied consequently one after another, they should be applied at different injection sites in a time interval of minimum 1 hour. These antibiotic groups should not be mixed in the same infusion bottle or applied by the same infusion tube. Ampicillin should not be added to infusion solutions because it is alkaline and may increase pH to the value of 8.0 and more.

6.3. Shelf life
36 months
Use immediately after dilution.

6.4. Special precautions for storage 
Store below 25 ºC. Store on a dry place, protect from light. 

6.5. Nature and contents of container
Vial with crimp of colorless glass, rubber stopper, aluminium crimp cap, box.
Package size: 1, 10 injection vials of 0.5 g
        1, 10 injection vials of 1.0 g

6.6. Instructions for use and other handling
For intramuscular or intravenous application.

BB Pharma a.s., Pod Višňovkou 1446/21, Prague, Czech republic

15 / 0548 / 92 - S


September 2013