Ampicillin + Sulbactam - Instructions For Use, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Ampicillin + Sulbactam

Latin name: Ampicillin + Sulbactam

ATX code: J01CR01

Active ingredient: ampicillin (Ampicillin) + sulbactam (Sulbactam)

Manufacturer: PJSC "Kraspharma" (Russia); Jodas Expoim Pvt. Ltd. (Jodas Expoim Pvt. Ltd.) (India); North China Pharmaceutical Huashen Co., Ltd. (North China Pharmaceutical Huasheng Co., Ltd.) (China)

Description and photo update: 2019-10-07

Ampicillin + Sulbactam is a combined broad-spectrum antibacterial drug.

Release form and composition

Ampicillin + Sulbactam is produced in the form of a powder for the preparation of a solution for intravenous (i / v) and intramuscular (i / m) administration: white with a yellow tint or white hygroscopic powdery mass [ampicillin + sulbactam 250 mg + 125 mg, 500 mg + 250 mg, 1000 mg + 500 mg or 2000 mg + 1000 mg in 10 or 20 ml clear glass vials, sealed with a rubber stopper, crimped with an aluminum / combination cap; solvent - water for injection (1 / 1.8 / 3.5 / 10 ml for 250 mg + 125 mg / 500 mg + 250 mg / 1000 mg + 500 mg / 2000 mg + 1000 mg, respectively) in ampoules made of neutral colorless glass or low density polyethylene; 1 bottle with the drug and 1 ampoule with a solvent in a cardboard box; for hospitals - 5, 10 or 100 vials with the drug and 5, 10 or 100 ampoules with a solvent, respectively,in a cardboard box; 10 vials with the drug (for 1000 mg + 500 mg) in a PVC pallet, 1 or 5 pallets in a cardboard box; 1 or 10 glass vials of 5 or 10 ml (for 2000 mg + 1000 mg) in a cardboard box / box, 1 or 5 vials of 5 ml each together with 2 or 10 ampoules of 5 ml solvent, respectively, 1 or 5 vials 10 ml each together with 1 or 5 ampoules of 10 ml solvent, respectively, with a knife for opening the ampoules; for hospitals - 1-50 vials in a cardboard box; 500 mg + 250 mg and 1000 mg + 500 mg in a glass vial with a volume of 10 ml, 1 or 10 vials in a cardboard box; 1 bottle with a 5 ml ampoule of solvent in a blister strip, in a cardboard box 1 package; 1 blister strip with 5 bottles and 1 with 5 ampoules of solvent complete with a knife / ampoule scarifier in a cardboard box;for hospitals - 1-50 vials in a cardboard box. Each pack also contains instructions for the use of Ampicillin + Sulbactam].

The composition of the drug for 1 bottle: ampicillin sodium + sodium sulbactam - 265.7 mg + 136.8 mg; 531.5 mg + 273.6 mg; 1062.9 mg + 547.2 mg; 2125.8 mg + 1094.4 mg (equivalent, respectively, ampicillin + sulbactam - 250 mg + 125 mg; 500 mg + 250 mg; 1000 mg + 500 mg; 2000 mg + 1000 mg).

Pharmacological properties

Pharmacodynamics

Ampicillin + Sulbactam is a combined agent that has a bactericidal effect against microorganisms sensitive to ampicillin, including strains that produce beta-lactamases.

Ampicillin is an antibiotic that belongs to the group of semi-synthetic penicillins and has a bactericidal effect by inhibiting the biosynthesis of the protein (mucopeptide) of the cell walls of pathogenic microorganisms during the period of their active reproduction.

Sulbactam is an irreversible inhibitor of most of the major beta-lactamases produced by microorganisms that are resistant to beta-lactam antibiotics. This substance does not lead to a change in the activity of ampicillin in relation to sensitive strains; forming a bond with individual penicillin-binding proteins of bacteria, demonstrates synergy against the background of simultaneous use with beta-lactam antibiotics. Sulbactam exhibits resistance to the action of most plasmid beta-lactamases and independent antibacterial activity against microorganisms of the Neisseriaceae family, genus Acinetobacter.

Ampicillin + Sulbactam is characterized by activity against the following microorganisms (including strains that reproduce beta-lactamases):

• gram-positive aerobes: Staphylococcus epidermidis, Staphylococcus aureus, Staphylococcus saprophyticus (strains that produce and do not produce beta-lactamase); Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus spp. viridans groups;
• gram-negative aerobes: Proteus mirabilis, Escherichia coli, Moraxella catarrhalis, Haemophilus influenzae, Neisseria gonorrhoeae (strains producing and not producing beta-lactamase); Proteus vulgaris, Klebsiella spp., Morganella morganii, Providencia stuartii, Providencia rettgeri;
• anaerobes: Peptostreptococcus spp., Peptococcus spp., Clostridium spp. (excluding Clostridium difficile), Bacteroides spp., including Bacteroides fragilis.

Microorganisms showing drug resistance: Staphylococcus aureus (methicillin-resistant), Citrobacter spp., Pseudomonas aeroginosa, Enterobacter cloacae, Stenotrophomonas maltophilia, Serratia marcescens, Chlamydophila spp., Chlamydophila spp., Chlamydia spp., Chlamydia

Pharmacokinetics

After intravenous administration of 1.5 and 3 g of the drug, the maximum serum concentrations (C _max) in the blood are, respectively, 40–71 μg / ml and 109–150 μg / ml for ampicillin, and 21–40 μg / ml and 48–88 μg / ml for sulbactam. After i / m administration of the drug at a dose of 1.5 g, C _max can vary for ampicillin from 8 to 37 μg / ml and for sulbactam from 6 to 24 μg / ml.

Ampicillin binds to blood plasma proteins by 28%, and to sulbactam by 38%, both active substances are well distributed in most body fluids and tissues. After intramuscular and intravenous injections, therapeutic concentrations of the active components of the drug are observed in pleural, peritoneal and interstitial fluids, pelvic organs, intestinal wall, subcutaneous tissue and skin. The drug poorly penetrates the blood-brain barrier, however, with inflammation of the meninges, the degree of its permeability into the cerebrospinal fluid increases.

For ampicillin and sulbactam, the half-life (T _1/2) on average can be about 1 hour. Both active substances are excreted mainly unchanged by the kidneys. During the first 8 hours, 75–85% of the administered dose is eliminated by the kidneys, as well as with breast milk and bile. Sulbactam practically does not undergo biotransformation and is excreted by the kidneys, mainly in unchanged form, and approximately 25% in the form of metabolites.

Indications for use

Ampicillin + Sulbactam is recommended for use for the treatment of the following infectious and inflammatory diseases, excited by microorganisms sensitive to ampicillin and sulbactam:

• upper / lower respiratory tract infections: chronic bronchitis, lung abscess, pneumonia, pleural empyema;
• infections of LOP organs: tonsillitis, sinusitis, otitis media;
• infections of the gastrointestinal tract (GIT): salmonella, salmonellosis, dysentery;
• uncomplicated / complicated infectious lesions of the abdominal organs: cholangitis, cholecystitis, abdominal abscess, peritonitis;
• infectious and inflammatory diseases of the pelvic organs: salpingo-oophoritis, salpingitis, endometritis, tubo-ovarian abscess, pelvioperitonitis;
• infectious lesions of the urinary tract and genital organs: urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, endometritis;
• joint and bone infections;
• infections of soft tissues and skin: secondary infected dermatitis, impetigo, erysipelas;
• sepsis, scarlet fever, septic endocarditis, gonococcal infection, meningitis.

Ampicillin + Sulbactam is also indicated for the prevention of postoperative complications in operations on the abdominal and pelvic organs.

Contraindications

Absolute:

• lymphocytic leukemia;
• infectious mononucleosis (including the period when a measles rash appears);
• lactation period;
• hypersensitivity to the components of the drug, as well as other beta-lactam antibiotics.

Relative (Ampicillin + Sulbactam should be used with caution):

• hepatic and / or renal failure;
• period of pregnancy;
• bronchial asthma, pollinosis and other allergic diseases;
• chronic diseases of the gastrointestinal tract, including in the anamnesis; previous colitis due to the intake of antibacterial agents;
• elderly age.

If procaine / lidocaine is used as a solvent, hypersensitivity to local anesthetics of the amide type, severe heart failure, intracardiac conduction blockade, and severe shock may develop.

Ampicillin + Sulbactam, instructions for use: method and dosage

Ampicillin + Sulbactam is administered intravenously (drip and jet) and intramuscularly. The route of administration is determined depending on the severity of the infection and the prescribed dose.

All recommendations are given with an indication of the dose of the drug, which is the total for ampicillin and sulbactam, in a 2: 1 ratio.

For adults and adolescents over 12 years old and with a body weight of more than 40 kg for the treatment of infections of moderate severity, the drug is administered intravenously or intramuscularly every 6 hours, 1.5 g; with severe infection - 3 g at the same frequency of administrations. The maximum permissible daily dose of sulbactam should not be higher than 4 g, which corresponds to a maximum daily dose of the drug equal to 12 g. Treatment must be continued for at least another 2-3 days after the clinical symptoms of the disease have disappeared. The duration of therapy is 5-14 days, but in severe cases of the disease, it can be increased or additionally prescribed ampicillin.

For uncomplicated gonorrhea, it is recommended to use Ampicillin + Sulbactam at a dose of 1.5 g once.

To prevent the development of postoperative infection, administration is prescribed at a dose of 1.5–3 g during anesthesia, and for 24 hours after the surgery, every 6–8 hours at the same dose.

Children aged 1 month to 12 years, or with a body weight of less than 40 kg, it is recommended to use the drug in a daily dose of 0.15 g per 1 kg of body weight, divided into 3-4 injections, in severe cases, it is possible to increase the daily dose to 0.3 g / kg. The course of treatment should not exceed 14 days.

Premature infants and children of the first week of life Ampicillin + Sulbactam is prescribed in a daily dose of 0.075 g / kg, divided into 2 injections, for children aged 7 to 28 days - in a dose of 0.15 g / kg divided by 3 intravenous infusions per day …

In order to prepare a solution for intramuscular administration, sterile water for injection, 0.5% lidocaine solution or 0.5% procaine solution are used as a solvent. In a bottle with 0.75 or 1.5 g of the drug, pour 2 or 4 ml of solvent, respectively. It is impossible to perform intravenous injections with a drug diluted with lidocaine / procaine.

To prepare a solution for intravenous jet infusion, Ampicillin + Sulbactam at a dose of 1.5 g is diluted with 12 ml of water for injection or 0.9% sodium chloride solution. It is recommended to introduce the prepared solution slowly over 3-5 minutes.

In order to prepare a solution for intravenous drip infusion of 1.5-3 g Ampicillin + Sulbactam is diluted with 12 ml of water for injection, and then 150-200 ml of 0.9% sodium chloride solution or 5% dextrose solution is added to the resulting liquid, after which is carried out in / in infusion at a rate of 60–80 drops per minute.

Side effects

• digestive system: decreased appetite, glossitis, flatulence, vomiting, nausea, diarrhea, pseudomembranous colitis, increased activity of hepatic transaminases;
• central nervous system (CNS): headache, malaise, drowsiness; extremely rare - convulsions;
• hematopoietic organs: decreased hemoglobin levels, hemolytic anemia, monocytosis, leukopenia, thrombocytopenia, neutropenia, eosinophilia, lymphocytosis, lymphopenia, thrombocytosis, false positive Coombs' test;
• allergic reactions: pruritus, skin flushing, urticaria, conjunctivitis, rhinitis, arthralgia, fever, anaphylactic shock, Quincke's edema, exudative erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis;
• local reactions: soreness at the injection site (intramuscular injection), thrombophlebitis / phlebitis (intravenous infusion);
• laboratory indicators: a decrease in the level of serum protein, an increase in the plasma content of urea in the blood, azotemia, cylindruria, leukocyturia, hypercreatininemia;
• others: swelling, sore throat, chest pain, bleeding, dysuria; with a long course - the development of superinfection, candidiasis.

Overdose

Symptoms of an overdose of the drug Ampicillin + Sulbactam may include: nausea, diarrhea, vomiting, imbalance in water and electrolyte balance (due to vomiting and diarrhea), neurological disorders, including convulsions (mainly against the background of functional disorders of the kidneys).

Treatment for this condition is prescribed symptomatic, in severe cases, the drug is removed using hemodialysis.

special instructions

In the course of a long course of use of Ampicillin + Sulbactam, it is required to periodically monitor the activity of the kidneys and liver, as well as a complete blood count.

In the presence of hypersensitivity to penicillins, the risk of possible cross-allergic reactions with cephalosporin antibiotics is aggravated. Before starting treatment, it is necessary to find out if the patient has had previous allergic reactions to beta-lactam antibiotics. If an allergic reaction develops, the drug should be immediately withdrawn and appropriate treatment should be carried out. If necessary, intravenous infusions of glucocorticosteroid hormones are administered, epinephrine (adrenaline) is administered, oxygen is supplied, and measures are prescribed to improve airway patency, including intubation.

During the period of therapy, as well as after 2-3 weeks after its completion, there is a possibility of developing diarrhea caused by Clostridium difficile - pseudomembranous colitis. If this complication occurs in a mild form, it is enough to cancel the drug treatment and prescribe the use of ion exchange resins (colestipol, cholestyramine), patients with severe diarrhea should compensate for the loss of electrolytes, fluids and protein, and prescribe vancomycin or metronidazole. Taking drugs that inhibit intestinal motility is prohibited in this case.

If drug therapy is received by patients adhering to a diet low in salt, then they should take into account that 1500 mg of the drug contains an average of 115 mg (5 mmol) of sodium.

In patients using Ampicillin + Sulbactam, there is a threat of superinfection, which requires discontinuation of the drug and the appointment of appropriate treatment. A false positive Coombs' test and a false positive urine glucose test can also be recorded.

When treating patients with sepsis, a bacteriolysis reaction may occur (Yarish-Herxheimer reaction).

Influence on the ability to drive vehicles and complex mechanisms

The negative effect of Ampicillin + Sulbactam on the ability to drive transport or to work with complex equipment has not been identified. At the same time, in view of the possible appearance of such side effects from the central nervous system as headache, drowsiness, etc., caution should be exercised when practicing potentially dangerous activities during therapy.

Application during pregnancy and lactation

During pregnancy, Ampicillin + Sulbactam can be used only when the expected benefit from the treatment to the mother significantly outweighs the possible risk to the fetus.

It was found that ampicillin and sulbactam in small amounts are excreted in breast milk. If necessary, drug therapy during lactation should stop breastfeeding.

Pediatric use

In patients under 18 years of age, Ampicillin + Sulbactam is used only as directed by the attending physician, according to the indicated dosage regimen.

With impaired renal function

In the presence of renal failure, antibacterial therapy must be carried out with caution. In patients with severe renal failure with creatinine clearance (CC) reaching 30 ml / min or below this value, the elimination of sulbactam and ampicillin changes in the same way - T _1/2 is lengthened, which requires individual selection of the drug dose, method and modes of administration.

Correction of the dosage regimen Ampicillin + Sulbactam in patients with impaired renal function is carried out taking into account the values of CC and T _1/2:

• CC ≥ 30 ml / min; T _1/2 - 1 hour: every 6-8 hours, 1.5-3 g;
• CC = 15-29 ml / min; T _1/2 - 5 hours: every 12 hours, 1.5–3 g;
• CC = 5-14 ml / min; T _1/2 - 9 hours: every 24 hours for 1.5-3 g.

In the presence of renal failure in children (CC below 30 ml / min), the drug is prescribed in usual single doses - 0.05–0.075 g / kg, increasing the intervals between injections, as recommended in adults.

In the presence of end-stage chronic renal failure, with CC below 5 ml / min, the safety of drug therapy has not been established.

For violations of liver function

In the presence of liver failure, Ampicillin + Sulbactam should be prescribed with caution.

Use in the elderly

Elderly patients are advised to use Ampicillin + Sulbactam with caution.

Drug interactions

• aminoglycosides, blood products, protein hydrolysates: pharmaceutical incompatibility of the drug with these agents has been established; when used simultaneously with aminoglycosides, solutions should not be mixed in one syringe or one infusion system, intramuscular injections should be made in different parts of the body, and with intravenous infusions, the drugs must be administered separately in compliance with a certain sequence with a maximum time interval between injections or use separate intravenous catheters;
• indirect anticoagulants: their effectiveness increases against the background of suppression of the intestinal microflora, a decrease in the production of vitamin K and the prothrombin index;
• chloramphenicol, tetracyclines, lincosamides, macrolides, sulfonamides and other bacteriostatic antibiotics: antagonistic effect is noted;
• vancomycin, cephalosporins, aminoglycosides, rifampicin, cycloserine and other bactericidal antibiotics: a synergistic effect appears;
• oral contraceptives, drugs, in the process of metabolism of which ethinylestradiol and para-aminobenzoic acid are formed (the threat of breakthrough bleeding is aggravated): the effectiveness of these drugs is weakened;
• diuretics: reduce the clearance of penicillins;
• non-steroidal anti-inflammatory drugs, allopurinol, probenecid, phenylbutazone and other drugs that reduce tubular secretion: increases the plasma level of ampicillin;
• allopurinol: increased likelihood of skin rash.

Analogs

Analogues of Ampicillin + Sulbactam are: Sultasin, Complisan, Libakcil, Pensilina, etc.

Terms and conditions of storage

Store out of the reach of children, protected from sunlight, at a temperature not exceeding 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Ampicillin + Sulbactam

Extremely rare reviews of Ampicillin + Sulbactam, found on medical sites, indicate the effectiveness of the drug in the treatment of infectious and inflammatory lesions caused by microorganisms sensitive to ampicillin and sulbactam. There are no complaints about side effects.

Price for Ampicillin + Sulbactam in pharmacies

The reliable price for Ampicillin + Sulbactam is unknown, since the antibacterial drug is currently not available for sale in the pharmacy chain.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!