Pensilina (Tablets, Powder) Instructions for Use

ATC Code

J01CR01 (Ampicillin and beta-lactamase inhibitor)

Active Substances

Ampicillin (Rec.INN registered by WHO)

Sulbactam (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Broad-spectrum penicillin antibiotic with a beta-lactamase inhibitor

Pharmacotherapeutic Group

Antibiotic, semi-synthetic penicillin + beta-lactamase inhibitor

Pharmacological Action

A combined broad-spectrum antibacterial agent.

Ampicillin is an antibiotic from the group of semi-synthetic penicillins, whose bactericidal action is associated with the inhibition of microorganism cell wall protein synthesis.

Sulbactam is an irreversible beta-lactamase inhibitor; it expands the spectrum of activity of ampicillin against resistant strains whose resistance develops under the influence of beta-lactamases; it does not alter the activity of ampicillin against susceptible strains; by binding to some penicillin-binding proteins of bacteria, it exhibits synergism when used simultaneously with beta-lactam antibiotics. It is stable in aqueous solution, has independent antibacterial activity against the Neisseriaceae family and Acinetobacter spp., and is resistant to the action of most plasmid beta-lactamases.

The Ampicillin+Sulbactam combination exhibits activity against 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. of the viridans group, 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

It penetrates into most tissues and body fluids; during inflammation, permeability into the cerebrospinal fluid increases sharply.

After IV and IM administration, high concentrations of sulbactam and ampicillin in the blood are achieved.

T_1/2 – 1 h (for ampicillin and sulbactam). It is excreted by the kidneys – 70-80%, mainly unchanged, as well as with bile and breast milk.

Sulbactam undergoes almost no metabolic transformations and is excreted by the kidneys, mainly unchanged and only about 25% as metabolites.

Indications

Treatment of infectious and inflammatory diseases caused by susceptible pathogens: respiratory tract infections (including pneumonia, lung abscess, chronic bronchitis, pleural empyema); ENT organ infections (including sinusitis, tonsillitis, otitis media); urinary tract and genital organ infections (pyelonephritis, pyelitis, cystitis, urethritis, prostatitis, endometritis); biliary tract infections (cholecystitis, cholangitis); skin and soft tissue infections (erysipelas, impetigo, secondarily infected dermatoses); gastrointestinal tract infections (dysentery, salmonellosis, salmonella carriage); bone and joint infections; septic endocarditis; meningitis; sepsis; peritonitis; scarlet fever; gonococcal infection.

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

ICD codes

Dosage Regimen

Powder

IM, IV (by drip at a rate of 60-80 drops/min, by stream – slowly, over 3-5 min).

IV administration is used for 5-7 days, then, if it is necessary to continue treatment, switch to IM use.

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

For mild infections – 1.5-3 g/day in 2 administrations; for moderate infections – 3-6 g/day in 3-4 administrations; for severe infections – 12 g/day in 3-4 administrations.

For uncomplicated gonorrhea – 1.5 g, once.

For prevention of surgical infections – 1.5-3 g, during anesthesia; then within 24 h after surgery – at the same dose every 6-8 h.

For children – in a daily dose of 150 mg/kg (100 mg/kg ampicillin and 50 mg/kg sulbactam); frequency – 3-4 times/day.

For newborns under 1 week of age and premature infants – every 12 h.

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

In chronic renal failure (creatinine clearance less than 30 ml/min) it is necessary to increase the intervals between administrations.

Tablets

For adults and children weighing more than 30 kg, the daily dose is 375-750 mg/day, for children weighing less than 30 kg – 25-50 mg/kg (depending on the severity of the infection). Frequency of administration – 2 times/day. The course of treatment is 5-14 days. For the treatment of uncomplicated gonorrhea, Sultamicillin may be prescribed once in a dose of 2.25 g (in combination with probenecid).

Adverse Reactions

From the digestive system nausea, vomiting, decreased appetite, diarrhea, increased activity of “hepatic” transaminases; rarely – pseudomembranous enterocolitis.

From the hematopoietic organs and hemostasis system anemia, leukopenia, thrombocytopenia.

From the nervous system drowsiness, malaise, headache.

Laboratory parameters azotemia, increased urea concentration, hypercreatininemia.

Allergic reactions urticaria, skin hyperemia, angioedema, rhinitis, conjunctivitis, fever, arthralgia, eosinophilia, in rare cases – anaphylactic shock.

Local reactions with IM administration – pain at the injection site; with IV – phlebitis.

Other with long-term treatment – superinfection caused by microorganisms resistant to the drug (candidiasis).

Contraindications

Hypersensitivity to the components of the drug; infectious mononucleosis; lactation period (breastfeeding).

With caution

Hepatic and/or renal failure, pregnancy.

Use in Pregnancy and Lactation

Use with caution during pregnancy. Contraindicated for use during lactation (breastfeeding).

Use in Hepatic Impairment

With caution: hepatic insufficiency.

Use in Renal Impairment

With caution: renal insufficiency.

Pediatric Use

Use is possible according to the dosing regimen.

Special Precautions

In patients with hypersensitivity to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

During course treatment, it is necessary to monitor the state of the function of the hematopoietic organs, liver and kidneys.

The development of superinfection due to the growth of microflora insensitive to the drug is possible, which requires an appropriate change in antibacterial therapy.

When treating patients with sepsis, the development of a bacteriolysis reaction (Jarisch-Herxheimer reaction) is possible.

Drug Interactions

Antacids, glucosamine, laxatives, food, aminoglycosides (when taken orally) slow down and reduce absorption.

Ascorbic acid increases absorption.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) – synergism of action; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) – antagonism of action.

Increases the effectiveness of indirect anticoagulants (by suppressing intestinal microflora, reduces the synthesis of vitamin K and the prothrombin index); reduces the effectiveness of oral contraceptives, drugs in the metabolism of which PABA is formed, and ethinyl estradiol (risk of “breakthrough” bleeding).

Diuretics, allopurinol, phenylbutazone, NSAIDs and other drugs that reduce tubular secretion increase the concentration of ampicillin in plasma.

Allopurinol increases the risk of skin rash.

Pharmaceutical incompatibility

With blood products or protein hydrolysates, aminoglycosides.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.