Sulmacefta (Powder) Instructions for Use

Marketing Authorization Holder

Alpharma, LLC (Russia)

Manufactured By

Ruzpharma, LLC (Russia)

Primary Packaging

Ruzpharma, LLC (Russia)

Secondary Packaging

Ruzpharma, LLC (Russia)

Or

Altegra, JSC (Russia)

Quality Control Release

Ruzpharma, LLC (Russia)

Or

Altegra, JSC (Russia)

ATC Code

J01CR01 (Ampicillin and beta-lactamase inhibitor)

Active Substances

Ampicillin (Rec.INN registered by WHO)

Sulbactam (Rec.INN registered by WHO)

Dosage Forms

	Sulmacefta	Powder for preparation of solution for intravenous and intramuscular administration 250 mg+125 mg: vial.
		Powder for preparation of solution for intravenous and intramuscular administration 500 mg+250 mg: vial.
		Powder for preparation of solution for intravenous and intramuscular administration 1000 mg+500 mg: vial.
		Powder for preparation of solution for intravenous and intramuscular administration 2000 mg+1000 mg: vial.

Dosage Form, Packaging, and Composition

Powder for preparation of solution for intravenous and intramuscular administration white or almost white with a yellowish tint.

Glass vials with a capacity of 10 ml (1) – cardboard packs.
Glass vials with a capacity of 20 ml (1) – cardboard packs.

Powder for preparation of solution for intravenous and intramuscular administration white or almost white with a yellowish tint.

Glass vials with a capacity of 10 ml (1) – cardboard packs.
Glass vials with a capacity of 20 ml (1) – cardboard packs.

Powder for preparation of solution for intravenous and intramuscular administration white or almost white with a yellowish tint.

Glass vials with a capacity of 20 ml (1) – cardboard packs.

Powder for preparation of solution for intravenous and intramuscular administration white or almost white with a yellowish tint.

Glass vials with a capacity of 20 ml (1) – cardboard packs.

Clinical-Pharmacological Group

Broad-spectrum penicillin antibiotic with a beta-lactamase inhibitor

Pharmacotherapeutic Group

Systemic antibacterial agents; beta-lactam antibacterial agents, penicillins; combinations of penicillins, including combinations with beta-lactamase inhibitors

Pharmacological Action

A combined broad-spectrum antibacterial agent.

Ampicillin is an antibiotic from the group of semisynthetic penicillins, the bactericidal action of which is associated with the inhibition of microbial 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

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

High concentrations of sulbactam and ampicillin in the blood are achieved after intravenous and intramuscular administration.

T_1/2 – 1 h (for ampicillin and sulbactam). 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 infections (including sinusitis, tonsillitis, otitis media); urinary tract and genital infections (pyelonephritis, pyelitis, cystitis, urethritis, prostatitis, endometritis); biliary tract infections (cholecystitis, cholangitis); skin and soft tissue infections (erysipelas, impetigo, secondarily infected dermatoses); gastrointestinal infections (dysentery, salmonellosis, salmonella carriage); bone and joint infections; septic endocarditis; meningitis; sepsis; peritonitis; scarlet fever; gonococcal infection.

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

ICD codes

Dosage Regimen

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

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

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

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 hours after surgery – at the same dose every 6-8 hours.

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 hours.

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 hours.

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

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 intramuscular administration – pain at the injection site; with intravenous – phlebitis.

Other with prolonged 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 dosage 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, a bacteriolysis reaction (Jarisch-Herxheimer reaction) may develop.

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 metabolized to form PABA, and ethinylestradiol (risk of breakthrough bleeding).

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

Allopurinol increases the risk of developing a 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.