Ampicillin + Sulbactam - instructions for use, dose, 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 of microorganisms.

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 micro-organisms resistant to beta-lactam antibiotics. Sulbactam also binds to certain penicillin-binding proteins, so some strains are more sensitive to combination ampicillin + sulbactam, than to one beta-lactam antibiotic ampicillin.

Ampicillin + Sulbactam is active against the following microorganisms:

Aerobic Gram-positive bacteria: Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus (producing and non-producing beta-lactamase strains); Enterococcus faecalis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. groups viridans.

Aerobic Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Proteus mirabilis, Neisseria gonorrhoeae (producing and non-producing beta-lactamase strains); Klebsiella spp., Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Morganella morganii.

Anaerobic microorganisms: Clostridium spp., Peptococcus spp., Peptostreptococcus spp., Bacteroides spp., including Bacteroides fragilis.

Resistant to the drug microorganisms: Staphylococcus aureus (methicillin-resistant), Citrobacter freundii, Enterobacter cloacae, Pseudomonas aeroginosa, Serratia marcescens, Strenotropho-monas maltophilia, Clamydia spp., Clamydophila spp., Legionella pneumophila, Mycoplasma spp., Ureaplasma urealyticum.

Pharmacokinetics:

It 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 and intramuscular injection, high concentrations of sulbactam and ampicillin are achieved in the blood.

The half-life (T1 / 2) is approximately 1 hour (for ampicillin and sulbactam). 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 unchanged state and only about 25% in the form of metabolites.

In patients with severe renal insufficiency (creatinine clearance is equal to or less than 30 ml / min), the removal of sulbactam and ampicillin is disturbed to the same extent - T1 / 2 increases, which requires correction of doses and regimens.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ampicillin and sulbactam:

upper and lower respiratory tract: pneumonia, lung abscess, chronic bronchitis, empyema of the pleura;

ENT organs: sinusitis, tonsillitis, otitis media;

urinary tract and genital organs: pyelonephritis, pyelitis, cystitis, urethritis, prostatitis, endometritis;

bile ducts; cholecystitis, cholangitis;

skin and soft tissues: erysipelas, impetigo, secondarily infected dermatitis; gastrointestinal tract: dysentery, salmonellosis, salmonellae;

bones and joints.

Septic endocarditis, meningitis, peritonitis, sepsis, scarlet fever, gonococcal infection.

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

Contraindications:

Hypersensitivity to ampicillin and sulbactam, other beta-lactam antibiotics, infectious mononucleosis, lymphocytic leukemia.

Carefully:Hepatic and / or renal insufficiency.

Pregnancy and lactation:

Use during pregnancy is permissible if the expected benefit to the mother exceeds the potential risk to the fetus. If you need to use the drug during lactation at the time of treatment should stop breastfeeding.

Dosing and Administration:

Intramuscularly (in / m), intravenously (iv) (drip, jet).

Standard dosing regimen

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

Adults: for a mild infection, -1.5-3 g / day in 2 injections; at an average current - 3-6 g / day in 3-4 injections; in severe cases - 12 g / day in 3-4 injections.

Children: 150 mg / kg body weight per day (corresponding to 100 mg / kg / day ampicillin and 50 mg / kg / day sulbactam); the frequency of administration is 3-4 times a day.

Newborns under 1 week of age and premature infants - 75 mg / kg of body weight per day with an interval of 12 hours.

Use in patients with impaired renal function (creatinine clearance is equal to or less than 30 ml / min): it is necessary to increase the intervals between the administrations.

Duration of treatment: course of treatment - 5-14 days (if necessary, can be extended). After normalization of temperature and disappearance of other pathological symptoms, treatment is continued for another 48 hours.

In / in 5-7 days, then, if necessary, continue treatment, go to the / m introduction.

Dosing in special cases

Uncomplicated gonorrhea - 1,5 g intramuscularly, once. 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 - 1,5-3 g, depending on the degree of infectious risk, during anesthesia; then within 24 hours after the operation - in the same dose every 6-8 hours.

Preparation of solutions. Solution for parenteral use is prepared ex tempore.

For intramuscular injection: to the contents of the vial (0.75 g or 1.5 g) is added respectively 2 ml or 4 ml of water for injections or 0.5%, 1%, 2% lidocaine solution.

When treating children under the age of 1 year, do not dissolve the drug in lidocaine solutions. The drug, diluted with lidocaine, can not be administered intravenously.

For intravenous administration:

- 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% solution of dextrose, injected at a rate of 60-80 drops per minute.

- for blasting: the solution prepared at initial dilution containing a single dose of the drug is dissolved in 10-20 ml of a 0.9% solution of sodium chloride, injected slowly for 3-5 minutes.

Side effects:

Allergic reactions: urticaria, skin hyperemia, rash, itching, angioedema,rhinitis, conjunctivitis, fever, arthralgia, bronchospasm, serum sickness, anaphylactic shock, polymorphic erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the digestive system: nausea, vomiting, decreased appetite, diarrhea, pseudomembranous colitis, impaired liver function (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 (less than 0.01%) reported the appearance of seizures.

Laboratory indicators: transient increase in activity of alanine aminotransferase (ALT) and aspartate 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 (less than 0.01%) - cases of interstitial nephritis, with long-term treatment - superinfection caused by drug-resistant microorganisms (candidiasis).

If any of the side effects listed in the manual are aggravated, or you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

Symptoms: manifestations of toxic effects on the central nervous system, including convulsions (especially in patients with renal insufficiency); nausea, vomiting, diarrhea, violation of water-electrolyte balance (as a consequence of vomiting and diarrhea).

Treatment: maintenance of water-electrolyte balance, symptomatic therapy. In severe cases; hemodialysis.

Interaction:

Pharmaceutically incompatible with blood products or protein hydrolysates, aminoglycosides.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) have a synergistic effect; bacteriostatic medicinal products (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic. Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of oral contraceptives, drugs,in the process of metabolism of which paraaminobenzoic acid is formed (risk of bleeding "breakthrough").

Diuretics, allopurinol, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that reduce tubular secretion, increase the concentration of ampicillin in plasma. Allopurinol increases the risk of skin rash.

If you are taking other medications, consult your doctor..

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.

When treating patients receiving a diet low in sodium, it must be taken into account that 1500 mg of the drug contains about 115 mg (5 mmol) of sodium.

In patients who are hypersensitive to penicillins, there may be cross-allergic reactions with cephalosporin antibiotics.

In course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

It is possible to develop superinfection due to the growth of insensitive microflora, which requires a corresponding change in antibacterial therapy.

After the expiry date of the drug, unused vials should be carefully opened, the contents dissolved in a large amount of water and drained into the drain.

Effect on the ability to drive transp. cf. and fur:

Care should be taken when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular injection 0.5 g + 0.25 g, 1.0 g + 0.5 g of active substances.

Packaging:

In bottles of glass with a capacity of 10 ml.

The solvent is "Water for Injection" in ampoules of glass with a volume of 5 ml. 1 bottle with instructions for use in a pack of cardboard.

1 bottle with the drug and 1 ampoule with a solvent in a contoured cell package (NLC) from a polyvinyl chloride film. One KNU with instructions for use in a pack of cardboard.

5 bottles with the preparation and 5 ampoules with a solvent in separate NLC from a polyvinyl chloride film. One KNU with vials and one KYU with ampoules and instructions for use in a pack of cardboard.

In a pack with KNU put a knife for opening ampoules or a scarifier ampoule. When using ampoules with notches, rings or break points, the ampoule opener opener or ampoule scarifier is allowed not to be inserted.

10 bottles with instructions for use in a cardboard box.

For hospitals:

- 50 bottles with an equal number of instructions for use in a cardboard box;

-1 bottle (from 1 to 50 bottles with an equal number of instructions for use) in a box of cardboard.

Storage conditions:In a protected spotlight at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003730 / 01

Date of registration:14.08.2009 / 08.02.2013

Expiration Date:Unlimited

The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp22.08.2017

Illustrated instructions

Instructions

Ampicillin + Sulbactam (Ampicillin + Sulbactam)