Ampicillin+Sulbactam powder 1g+0.5g vial, 1pc

Composition

For 1 bottle:

Active ingredient: ampicillin sodium-1062.9 mg, which corresponds to the content of ampicillin-1000.00 mg, sulbactam sodium-547.2 mg, which corresponds to the content of sulbactam-500.00 mg

Pharmacological action

Pharmacotherapy group: Antibiotic-Penicillin semi-synthetic+beta-lactamase Inhibitor ATX Code: J01CRPharmacodynamics :

Ampicillin+sulbactam-the combined drug has a bactericidal effect against ampicillin-sensitive microorganisms, including beta-lactamase-producing strains.

Ampicillin is a semi-synthetic penicillin with a broad spectrum of activity that inhibits the synthesis of cell wall proteins of pathogenic microorganisms.

Sulbactam is an irreversible inhibitor of beta-lactamases; expands the spectrum of ampicillin activity against resistant strains whose resistance develops under the influence of beta-lactamases; does not change the activity of ampicillin against sensitive strains; binds to some nonicillin-binding bacterial proteins; shows synergy when used simultaneously with beta-lactam antibiotics. It is stable in aqueous solution and has independent antibacterial activity against the Neisseriaceae family and Acinetobacter spp. it is resistant to most plasmid beta-lactamases.

Ampicillin+sulbactam is active against the following microorganisms (including beta-lactamase producing strains): :

Aerobic gram-positive bacteria:  Staphylococcus aureus (beta-lactamase producing and non-producing strains) Staphylococcus epidermidis (beta-lactamase producing and non-producing strains) Staphylococcus saprophyticus (beta-lactamase producing and non-producing strains) Streptococcus pyogenes Streptococcus pneumoniae (including penicillin-resistant strains) Streptococcus spp. groups viridans Enterococcus faecalis Listeria monocytogenes.

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

Anaerobic microorganisms:  Bacteroides spp. including Bacteroides fragilis Clostridium spp. (except Clostridium difficile) Peptococcus spp. Peptostreptococcus spp.

Resistant: Methicillin-resistant Staphylococcus spp. Citrobacter spp. most strains of Enterobacter spp. Pseudomonas aeruginosa Mycobacterium spp. Clostridium difficile Chlamydia pneumoniae Mycoplasma pneumoniae.

Pharmacokinetics:

The maximum serum concentrations (Cmax) of ampicillin and sulbactam after intravenous (iv) use of 15 g and 3 g of the drug are 40-71 mcg / ml and 109-150 mcg / ml for ampicillin; 21-40 mcg/ml and 48-88 mcg/ml for sulbactam, respectively. After an intramuscular injection of 1.5 g ampicillin+sulbactam, the ampicillin cmax varies from 8 mcg / ml to 37 mcg / ml, and the sulbactam cmax varies from 6 mcg / ml to 24 mcg/ml. The degree of binding to plasma proteins is 28% for ampicillin and 38% for sulbactam. Both sulbactam and ampicillin are well distributed in various tissues and fluids.

Therapeutic concentrations after intravenous and intravenous use are created in peritoneal and pleural fluids interstitial fluid intestinal wall pelvic organs skin and subcutaneous tissue. Poorly penetrate the blood-brain barrier with inflammation of the meninges, the permeability to the cerebrospinal fluid increases.

The half-life (T 1/2) of ampicillin and sulbactam is on average about 1 hour. Both components of the drug are mainly excreted unchanged by the kidneys. 75% to 85% of the administered dose of ampicillin and sulbactam is excreted by the kidneys within the first 8 hours. In patients with varying degrees of renal dysfunction, T 1/2 of the drug components increases, which requires dose adjustment and the mode of use of the drug.

Indications

Infectious and inflammatory diseases caused by ampicillin+sulbactam-sensitive strains of microorganisms:

infections of ENT organs (including sinusitis, otitis media, tonsillitis);

– infections of the respiratory system (acute and exacerbation of chronic bronchitis, pneumonia, lung abscess empyema);

– infectious endocarditis, bacterial meningitis sepsis;

– uncomplicated and complicated infections of the abdominal cavity (cholecystitis cholangitis, peritonitis, abscess of the abdominal cavity);

– urinary tract infections (acute and exacerbation of chronic pyelonephritis, pyelitis);

infectious-inflammatory diseases of the pelvic organs (salpingitis oophoritis tubo-ovarian abscess, endometritis pelvioperitonit);

– gonococcal infection:

– infections of the skin and soft tissues (erysipelas abscess of phlegmon wound and postoperative infection);

– infections of bones and joints.

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

Use during pregnancy and lactation

Use during pregnancy is only possible if the intended benefit to the mother exceeds the potential risk to the fetus.

Ampicillin and sulbactam pass into breast milk in low concentrations. If it is necessary to use the drug during lactation, stop breastfeeding.

Contraindications

Hypersensitivity to any of the components of the drug and other beta-lactam antibiotics; infectious mononucleosis (including when a crust-like rash appears) lymphocytic leukemia.

The safety of ampicillin+sulbactam in patients with end-stage chronic renal failure (creatinine clearance less than 5 ml / min) has not been established.

When using procaine lidocaine as a solvent – hypersensitivity to local anesthetics of the amide type severe shock blockage of intracardiac conduction severe heart failure.

With caution:

Bronchial asthma pollinosis and other allergic diseases liver failure chronic diseases of the gastrointestinal tract in the anamnesis previous colitis associated with the use of antibacterial drugs impaired renal function elderly age.

Side effects

Allergic reactions:  urticaria skin hyperemia pruritus angioedema rhinitis conjunctivitis fever arthralgia anaphylactic shock Stevens-Johnson syndrome erythema multiforme toxic epidermal necrolysis.

From the digestive system:  nausea vomiting decreased appetite diarrhea flatulence glossitis pseudomembranous colitis increased activity of” hepatic ” trans amine az.

From the side of hematopoietic organs:  hemolytic anemia decreased hemoglobin thrombocytopenia eosinophilia leukopenia neutropenia lymphopenia lymphocytosis thrombocytosis monocytosis false positive Coombs test.

From the central nervous system:  drowsiness headache.

Laboratory parameters:  azotemia increased urea concentration in blood plasma hypercreatininemia decreased serum protein leukocyturia cylindruria.

Local reactions:  with intravenous use-soreness at the injection site;with intravenous use-phlebitis thrombophlebitis.

Other: malaise chest pain sore throat dysuria edema bleeding; with prolonged treatment – candidiasis development of superinfection.

Interaction

When used concomitantly with indirect anticoagulants, ampicillin+sulbactam potentiates their effect; reduces the effectiveness of oral contraceptives, drugs whose metabolism produces paraaminobenzoic acid and ethinyl estradiol (the risk of “breakthrough” bleeding).

When used concomitantly with aminoglycosides, there is a pronounced synergism of bactericidal action against gram-positive and gram-negative bacteria.

Pharmacologically incompatible with blood products or protein hydrolysates aminoglycosides. When the drug is used simultaneously with aminoglycosides, do not mix the drugs in one syringe or one infusion system; with intravenous use, enter into different parts of the body; with intravenous use, enter separately following a certain sequence with as long a time interval between injections as possible, or use separate intravenous catheters.

Probenecid allopurinol phenylbutazone nonsteroidal anti-inflammatory drugs reduce the tubular secretion of ampicillin and sulbactam and increase their half-life. Diuretics reduce the clearance of penicillins.

Bactericidal antibiotics (including cephalosporins cycloserine vancomycin rifampicin aminoglycosides) have a synergistic effect; bacteriostatic antibiotics (including macrolides chloramphenicol lincosamides tetracyclines) – antagonistic. Concomitant use of ampicillin and allopurinol increases the risk of skin rash.

How to take it, course of use and dosage

Intravenous (jet and drip) intramuscularly. The route of use depends on the severity of the infection and the dose chosen. The following are the total doses of ampicillin and sulbactam (in a ratio of 2: 1).

In adults and children over 12 years of age and weighing more than 40 kg for the treatment of moderate infections,15 g is administered intravenously or intravenously every 6 hours.

For severe infections – 3 g every 6 hours. The maximum daily dose of sulbactam should not exceed 4 g which corresponds to a daily dose of the drug equal to 12 g

Treatment should be continued for at least another 2-3 days after the clinical symptoms of the disease disappear.The duration of treatment is 5-14 days, but in more severe cases, it can be increased or ampicillin can be prescribed additionally.

With uncomplicated gonorrhea – 15 g once.

To prevent postoperative infection – 15-3 g during anesthesia, then within 24 hours after surgery in the same dose every 6-8 hours.

In children older than 1 month and under 12 years of age (or weighing less than 40 kg) the drug is administered at a dose of 150 mg / kg per day, which is divided into 3-4 injections. If the infection is severe, the dose may be increased to 300 mg / kg / day. The duration of the course of therapy should not exceed 14 days.

In premature newborns and children of the first week of life, the daily dose of the drug is 75 mg / kg, which is divided into two injections.

In children aged from 7 days to 28 days, the drug is prescribed at a dose of 150 mg / kg per day divided into 3 intravenous injections.

In patients with impaired renal function, the dosage regimen is adjusted depending on the values of creatinine clearance (CC).

In children with renal insufficiency (creatinine clearance less than 30 ml / min), the drug is administered in normal single doses (50-75 mg/kg), increasing the intervals between injections as indicated in adults.

Preparation of solutions:

To prepare the solution for intravenous use, sterile water for injection is used as a solvent 05% procaine solution 05% lidocaine solution. 4 ml of solvent is added to a vial containing 15 g of the drug.

To prepare a solution for intravenous injection,12 ml of water for injection and 09% sodium chloride solution are added to a vial containing 15 g of the drug. Enter slowly for 3-5 minutes.

To prepare a solution for intravenous drip use,15-3 g of the drug is dissolved in 15 ml of water for injection, then the resulting solution is added to 150-200 ml of 10% sodium chloride solution or 5% dextrose solution and administered at a rate of 60-80 drops per minute.

Overdose

Symptoms: neurological disorders up to seizures (especially in patients with impaired renal function) nausea vomiting diarrhea impaired water and electrolyte balance (as a result of vomiting and diarrhea).

Treatment: symptomatic therapy; in severe cases – hemodialysis.

Description

White or white powder with a yellowish tinge of color.

Special instructions

With prolonged use of the drug, it is necessary to periodically monitor the functions of the kidneys, liver and general blood test.

Before starting therapy, a thorough medical history should be collected for previous allergic reactions to beta-lactam antibiotics. If an allergic reaction develops, the drug should be discontinued immediately.

When using the drug both during use and 2-3 weeks after discontinuation of treatment, diarrhea caused by Clostridium difficile (pseudomembranous colitis) may develop. In mild cases, discontinuation of treatment and the use of ion-exchange resins (colestyramine colestipol) is sufficient; in severe cases, compensation for fluid loss of electrolytes and protein is indicated by the appointment of vancomycin or metronidazole. Do not use medications that inhibit intestinal motility.

When using ampicillin+sulbactam (as well as other antibiotics), superinfection may develop, which requires discontinuation of the drug and the appointment of appropriate treatment.

It is possible to detect a false positive Coombs test or a false positive test for glucose in the urine (using the Benedict or Fehling method).

When treating patients with sepsis, a bacteriolysis reaction (Yarish-Gerksheimer reaction) may develop.

Influence on the ability to drive vehicles and mechanisms:

There are no data on the negative effect of the drug in the recommended doses on the ability to drive a vehicle or work with mechanisms. However, given the likelihood of side effects from the central nervous system, caution should be exercised when engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 3 years.

Do not use the product after the expiration date.

Active ingredient

Ampicillin, [Sulbactam]

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection