Name: Ampisulbin (Ampicillin, Sulbactam) 1.5 g. vial
Availability: InStock

Ampisulbin (Ampicillin, Sulbactam) 1.5 g. vial

$12.90

Manufacturer: Ukraine

Treatment of infections caused by microorganisms sensitive to the components of the drug:

infections of the upper and lower respiratory tract, including sinusitis, otitis media, epiglottitis and bacterial pneumonia;
urinary tract infections and pyelonephritis;
intra-abdominal infections, including peritonitis, cholecystitis, endometritis and pelvic inflammatory disease;
bacterial septicemia;
infections of the skin, soft tissues, bones and joints;
gonococcal infections.

The drug can be prescribed in the perioperative period in order to reduce the incidence of postoperative infections in patients who have undergone surgery in the abdominal and pelvic cavities and who may have infection in the abdominal cavity. In case of caesarean section or termination of pregnancy, the drug can be used prophylactically to reduce the incidence of postoperative sepsis.

It should be taken into account that sulbactam/ampicillin is ineffective against Pseudomonas aeruginosa.

When using the drug, it is necessary to take into account official recommendations regarding the appropriate use of antimicrobial substances.

Category: Antibacterial

Description

Description

Ingredients

active ingredient: ampicillin, sulbactam;

1 bottle contains 1.5 g of a sterile mixture of ampicillin sodium salt and sulbactam sodium salt in a ratio of 2: 1 in terms of ampicillin 1.0 g and sulbactam 0.5 g.

Dosage form

Powder for solution for injection.

Basic physical and chemical properties: white or white with a yellowish tint powder.

Pharmacotherapeutic group

Antibacterial agent for systemic use. Ampicillin and an enzyme inhibitor. ATX code J01C R01.

Pharmacodynamics

Mechanism of action

The mechanism of action of ampicillin is based on the inhibition of the synthesis of the bacterial cell wall (in the growth phase) by blocking penicillin-binding proteins (PSB), for example, transpeptidases. This leads to a bactericidal effect.

Inactivation of ampicillin, which is carried out by certain beta-lactamases, is inhibited when it is used in combination with sulbactam. Sulbactam protects ampicillin from cleavage by most staphylococcal beta-lactamases, as well as some beta-lactamases that are encoded by plasmids (eg, TEM, OXA, SHV, CTX-M), and certain beta-lactamases that are encoded by the chromosomes of gram-negative bacteria. These beta-lactamases are present, for example, in Escherichia coli, species of the genus Klebsiella, Proteus mirabilis and Haemophilus influenzae. The spectrum of antibacterial action of ampicillin extends to bacteria whose beta-lactamase can be inhibited by sulbactam.

Relationship between pharmacokinetics and pharmacodynamics

Efficacy mainly depends on the length of time during which the level of the active substance (ampicillin) exceeds the minimum inhibitory concentration (MIC) for a particular pathogen.

Mechanism of resistance

Resistance to ampicillin/sulbactam may be based on the following mechanisms:

Inactivation due to beta-lactamases: ampicillin/sulbactam does not show sufficient activity against bacteria that produce beta-lactamases, which are not inhibited by sulbactam.
Reduced affinity of PBPs to ampicillin: Acquired resistance to amoxicillin/clavulanic acid in pneumococci and other streptococci is based on mutations in existing PBPs. Methicillin (oxacillin)-resistant staphylococci are resistant due to the production of additional PBPs with reduced affinity for ampicillin and all other beta-lactam antibiotics.
In gram-negative bacteria, insufficient penetration of ampicillin through the outer cell wall can lead to insufficient inhibition of PBP.
Ampicillin can be actively transported out of the cell by efflux pumps.

There is partial or complete cross-resistance of ampicillin/sulbactam with penicillins, cephalosporins, and other beta-lactam antibiotic/beta-lactamase inhibitor combinations.

Usually susceptible microorganism species

Aerobic gram-positive bacteria: Staphylococcus aureus (methicillin-sensitive), Enterococcus faecalis, Streptococcus pneumoniae and other streptococci.

Aerobic gram-negative bacteria: Haemophilus influenzae and Haemophilus parainfluenzae, Moraxella catarrhalis, Neisseria gonorrhoeae and Neisseria meningitidis.

Anaerobic bacteria: Bacteroides fragilis and other species of this genus.

Species that can acquire resistance in isolated cases

Aerobic gram-positive bacteria: Enterococcus faecium, Staphylococcus epidermidis.

Aerobic gram-negative bacteria: E. coli, bacteria of the genus Klebsiella and Proteus.

Naturally resistant microorganisms

Aerobic gram-positive bacteria: Staphylococcus aureus (methicillin-resistant).

Aerobic gram-negative bacteria: Pseudomonas aeruginosa, Enterobacter cloacae, species of the genus Citrobacter, Morganella morganii, Serratia and all enterobacteria that produce type I beta-lactamase.

Benchmarks

For ampicillin/sulbactam, the following EUCAST minimum inhibitory concentration (mcg/mL) targets are recommended: sensitive ≤ 2, resistant ≥ 8.

The level of resistance can vary with geographic location and time, so for the treatment of severe infections, it is desirable to have local information on resistance for individual species. If necessary, expert advice should be sought if the local level of resistance reaches such proportions that the benefit of the drug is called into question for at least some types of infections. During the treatment of severe infections or in cases of resistance to therapy, it is recommended to establish a microbiological diagnosis, including pathogen identification and clindamycin susceptibility testing.

Indications

Treatment of infections caused by microorganisms sensitive to the components of the drug:

infections of the upper and lower respiratory tract, including sinusitis, otitis media, epiglottitis and bacterial pneumonia;
urinary tract infections and pyelonephritis;
intra-abdominal infections, including peritonitis, cholecystitis, endometritis and pelvic inflammatory disease;
bacterial septicemia;
infections of the skin, soft tissues, bones and joints;
gonococcal infections.

It should be taken into account that sulbactam/ampicillin is ineffective against Pseudomonas aeruginosa.

When using the drug, it is necessary to take into account official recommendations regarding the appropriate use of antimicrobial substances.

Contraindications

Hypersensitivity to the components of the drug.

Hypersensitivity to penicillins and cephalosporins in history.

Infectious mononucleosis or lymphatic leukemia.

If a 0.5% sterile solution of lidocaine hydrochloride for injection or another local anesthetic is used to reconstitute the powder, the contraindications indicated in the Instructions for Medical Use for the relevant medicinal product must be taken into account.

Dosage and administration

The drug Ampisulbin® is used intramuscularly or intravenously (as a bolus injection or infusion).

To prepare for use, the drug should be diluted with sterile water for injection or other compatible solution. After adding the solvent, wait a few minutes until the foam disappears completely, then visually assess the completeness of dissolution.

Dissolve the drug with at least 3.2 ml of water for injection (or other compatible solution), respectively. Administer intramuscularly as a bolus injection (over at least 3 minutes). With a higher dilution, the dose can be administered both as a bolus and as an infusion (within 15-30 minutes).

When administered intramuscularly, the drug should be injected deep into the muscle; if the injections are painful, 0.5% sterile lidocaine hydrochloride injection or other local anesthetic that is appropriate can be used to reconstitute the powder.

The maximum final concentration of sulbactam / ampicillin is 125 mg / 250 mg in 1 ml.

Treatment of infections caused by microorganisms sensitive to sulbactam and ampicillin:

Use by adults

Depending on the severity of the infection, a daily dose of Ampisulbin® 1.5 g to 12 g should be administered in divided doses every 6 to 8 hours (every 12 hours for less severe infections); the maximum daily dose should not exceed 12 g for Ampisulbin® (4 g for sulbactam).

Severity of infection

Daily dose of Ampisulbin® (g)

Light

Medium

heavy

1.5-3 (from 0.5 + 1 to 1 + 2)

up to 6 (2 + 4)

up to 12 (4 + 8)

Use in children, infants and newborns

Children, infants and newborns (1 week of age and older) should usually be given a daily dose of 150 mg/kg body weight (corresponding to 100 mg/kg/day ampicillin and 50 mg/kg/day sulbactam) divided into equal parts every 6 or 8 hours.

In newborns during the first week of life (especially preterm infants), the drug should generally be given at a dose of 75 mg/kg/day (corresponding to 25 mg/kg/day sulbactam and 50 mg/kg/day ampicillin) in divided doses every 12 hours .

For the prevention of surgical infections, the dose of Ampisulbin® is 1.5-3 g, it should be administered during induction of anesthesia, which provides enough time to achieve effective concentrations in blood serum and tissues during surgery. The dose can be repeated every 6-8 hours; the use of the drug, as a rule, should be stopped 24 hours after the operation, except in cases where the administration of the drug Ampisulbin® is intended for therapeutic purposes.

For the treatment of uncomplicated gonorrhea, Ampisulbin® can be administered once at a dose of 1.5 g intravenously or intramuscularly. In order to prolong the concentration of sulbactam and ampicillin in the blood plasma, probenecid 1 g orally should be administered simultaneously.

Use in patients with impaired renal function

In patients with severe renal insufficiency (creatinine clearance < 30 ml / min), the elimination of sulbactam and ampicillin slows down equally, so their ratio in blood plasma does not change. For such patients, the intervals between doses of Ampisulbin® should be extended in accordance with the usual practice of using ampicillin.

Table 2

Creatinine clearance (ml/min)	Interval between doses
> 30	6-8 hours
15-29	12 hours
5-14	24 hours
< 5	48 hours

Patients who are on dialysis

Both sulbactam and ampicillin are equally eliminated by hemodialysis. Therefore, Ampisulbin® should be used immediately after dialysis and then, at the beginning of the next dialysis, applied at intervals of 48 hours.

Use in patients with impaired liver function

For patients with impaired liver function, dosage adjustment is not required.

Use in elderly patients

In the absence of renal insufficiency, dosage adjustment of Ampisulbin® for elderly patients is not required.

The duration of treatment depends on the severity of the infection and is usually 5-14 days, but in more severe cases it may be extended or ampicillin may be added. As a rule, treatment should be continued for another 48 hours after the normalization of body temperature and the disappearance of other signs of symptoms of a bacterial infection.

The duration of treatment for infections caused by hemolytic streptococci should be at least 10 days in order to avoid rheumatoid fever and glomerulonephritis.

Dissolution instructions

A concentrated solution for intramuscular use should be used within 1 hour after reconstitution.

The time of use of the drug for intravenous infusion, depending on the type of solvent chosen, is indicated below:

Table 3

Solvent	Concentration sulbactam/ampicillin	Storage time (watch)
		t=25 °С	t=4 °С
Sterile water for injection	up to 45 mg/ml 45 mg/ml up to 30 mg/ml	8	48 72
0.9% sodium chloride solution	up to 45 mg/ml 45 mg/ml up to 30 mg/ml	8	48 72
5% aqueous glucose solution	15-30 mg/ml up to 3 mg/ml up to 30 mg/ml	2 4	4
5% aqueous glucose solution in 0.45% sodium chloride solution	up to 3 mg/ml up to 15 mg/ml	4	4
10% aqueous solution of invert sugar	up to 3 mg/ml up to 30 mg/ml	4	3
Sodium lactate solution	up to 45 mg/ml up to 45 mg/ml	8	8
Ringer’s lactate solution	up to 45 mg/ml up to 45 mg/ml	8	24

Ampisulbin (Ampicillin, Sulbactam) 1.5 g. vial