Trifamox IBL^® (Tablets, Powder) Instructions for Use

ATC Code

J01CR02 (Amoxicillin and beta-lactamase inhibitor)

Active Substances

Sulbactam (Rec.INN registered by WHO)

Amoxicillin (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 drug that includes a broad-spectrum penicillin antibiotic and a beta-lactamase inhibitor. It has a bactericidal effect against microorganisms sensitive to amoxicillin, including strains that produce beta-lactamases.

Amoxicillin is a broad-spectrum semi-synthetic penicillin from the aminopenicillin group. It acts bactericidally by inhibiting the synthesis of the cell wall proteins of pathogenic microorganisms. Active against aerobic gram-positive bacteria (including strains producing beta-lactamases) Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus pyogenes, Streptococcus anthracis, Streptococcus pneumoniae, Streptococcus viridans, Enterococcus faecalis, Corynebacterium spp., Listeria monocytogenes; anaerobic gram-positive bacteria Clostridium spp., Peptococcus spp., Peptostreptococcus spp.; aerobic gram-negative bacteria (including strains producing beta-lactamases) Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella spp., Salmonella spp., Shigella spp., Bordetella pertussis, Yersinia enterocolitica, Yersinia multocida, Gardnerella vaginalis, Neisseria meningitidis, Neisseria gonorrhoeae, Moraxella catarrhalis, Haemophilus influenzae, Campylobacter jejuni, Acinetobacter spp., Helicobacter pylori; anaerobic gram-negative bacteria (including strains producing beta-lactamases) Bacteroides spp., including Bacteroides fragilis.

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

Pharmacokinetics

Distribution

Amoxicillin is distributed in most tissues and biological fluids of the body. Amoxicillin crosses the placental barrier and is found in breast milk.

Plasma protein binding of amoxicillin is 20%, of sulbactam is 40%.

Elimination

The T_1/2 of amoxicillin and sulbactam is 1 hour.

Amoxicillin is excreted mainly by the kidneys (glomerular filtration and tubular secretion) – 70-80% and with bile – 5-10%. Sulbactam is almost completely excreted by the kidneys (75-85%) unchanged.

Sulbactam does not affect the pharmacokinetics of amoxicillin.

Indications

Infectious and inflammatory diseases caused by strains of microorganisms sensitive to amoxicillin

• Infections of the upper respiratory tract and ENT organs (acute and chronic sinusitis, tonsillitis, pharyngitis, retropharyngeal abscess, acute and chronic otitis media);
• Infections of the lower respiratory tract (acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia);
• Infections of the biliary tract (cholangitis, cholecystitis);
• Intestinal infections (salmonellosis);
• Infections of the genitourinary system (pyelonephritis, pyelitis, cystitis, urethritis, prostatitis);
• Infections of the pelvic organs (cervicitis, salpingitis, salpingo-oophoritis, tubo-ovarian abscess, endometritis, postpartum sepsis, pelvioperitonitis);
• Bacterial vaginitis;
• Gonorrhea;
• Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses, abscess, phlegmon, wound infection);
• Osteomyelitis;
• Endocarditis;
• Meningitis;
• Sepsis;
• Peritonitis;
• Postoperative infections.

Prevention of infectious and inflammatory diseases in surgery.

ICD codes

Dosage Regimen

Tablets

The dosage regimen is set individually depending on the severity of the course, localization of the infection, and sensitivity of the pathogen. Doses are set in terms of Amoxicillin.

The drug in the form of tablets is taken regardless of food intake.

For adults and adolescents over 12 years old, the drug is prescribed at 250 mg 3 times/day, for severe infections – 500 mg 3 times/day or 1 g 2 times/day.

For children aged 6-12 years, 250-500 mg 3 times/day is prescribed, for children aged 2-6 years – 250 mg 3 times/day.

The duration of treatment is 14 days.

Powder

The dosage regimen is set individually depending on the severity of the course, localization of the infection, and sensitivity of the pathogen. Doses are set in terms of Amoxicillin.

Treatment should be continued for at least another 2-3 days after the disappearance of clinical symptoms of the disease, but not more than 14 days. When treating infections caused by beta-hemolytic streptococcus, the drug is recommended to be used for at least 10 days.

The drug should be administered deep intramuscularly, intravenously as injections or infusions.

For adults and children over 12 years old, the average recommended dose is 1 g 2-3 times/day.

For prevention of postoperative infections during operations lasting less than 1 hour, the drug is administered intravenously at a dose of 1 g during induction anesthesia. For longer operations – 1 g every 6 hours for 24 hours. If the risk of infection is high, administration may be continued for several days.

For children aged 6 to 12 years, 500 mg 3 times/day is prescribed.

For children aged 2 to 6 years – 250 mg 3 times/day.

For children under 2 years old – 40-60 mg/kg 2-3 times/day.

For severe infections (especially those caused by gram-negative pathogens), the daily dose of the drug (in terms of Amoxicillin) can be increased to 100 mg/kg/day.

In patients with impaired renal function, the dosage regimen is adjusted depending on CC. For CC > 30 ml/min, no change in the dosage regimen is required; for CC 10-30 ml/min, treatment begins with intravenous administration of the drug at a dose of 1 g, then – 500 mg intravenously 2 times/day; for CC < 10 ml/min – 1 g, then 500 mg/day intravenously once/day.

During hemodialysis, the concentration of amoxicillin in the blood plasma decreases, therefore, during and at the end of dialysis, the drug is additionally administered intravenously at a dose of 500 mg.

In children with chronic renal failure, the drug is used in an average single dose with an increase in the intervals between administrations, as indicated for adults.

Rules for the preparation of solutions for intramuscular and intravenous administration

For intramuscular administration: add 5 ml of water for injections to the contents of the vial (500 mg + 250 mg or 1000 mg + 500 mg).

Only freshly prepared solutions should be used.

For intravenous administration, a single dose is dissolved in 0.9% sodium chloride solution or 5% dextrose (glucose) solution in a volume from 10 ml (for intravenous bolus injection) to 100-200 ml (for intravenous infusion).

For intravenous infusion: dilution with Ringer’s lactate solution is acceptable.

When diluting with Ringer’s lactate solution, the infusion solution is prepared in 2 stages: first, sterile water for injections is used, then the resulting solution is diluted with Ringer’s lactate solution.

For intravenous bolus injection, the prepared solution is administered slowly.

For intravenous infusion, the prepared solution is administered slowly by drip over 15-60 minutes.

Adverse Reactions

From the digestive system: nausea, vomiting, diarrhea, dyspepsia, pain in the epigastric region, increased activity of hepatic transaminases, cholestatic jaundice, hepatitis, pseudomembranous colitis.

Allergic reactions: urticaria, angioedema, respiratory disorders, multiform exudative erythema, anaphylactic shock, exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis.

From the hematopoietic system anemia, thrombocytopenia, thrombocytopenic purpura, eosinophilia, leukopenia and agranulocytosis.

From the CNS hyperactivity, agitation, anxiety, insomnia, confusion, behavioral changes.

Local reactions burning and pain at the injection site; in some cases – phlebitis at the site of intravenous administration.

Other: candidomycosis, development of superinfection, interstitial nephritis.

Contraindications

• Infectious mononucleosis (including when a measles-like rash appears);
• Ulcerative colitis (including that associated with antibiotic use);
• Crohn’s disease;
• Herpesvirus infection;
• Simultaneous use of allopurinol (in the presence of skin allergic reactions when using penicillins);
• History of colitis associated with the use of penicillins;
• Hypersensitivity to the components of the drug;
• Hypersensitivity to other beta-lactam antibiotics.

With caution, the drug should be used in cases of severe hepatic insufficiency, gastrointestinal diseases, chronic renal failure, and in elderly patients (due to the possible risk of developing renal failure).

Use in Pregnancy and Lactation

The use of the drug Trifamox IBL^® during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

Use in Hepatic Impairment

With caution, the drug should be used in cases of severe hepatic insufficiency.

Use in Renal Impairment

In chronic renal failure, the dose is calculated depending on the creatinine clearance indicators. For CC greater than 30 ml/min, no dose reduction is required; for CC 10-30 ml/min, treatment begins with intravenous administration of 1 g, then 500 mg intravenously or 250-500 mg orally 2 times/day; for CC less than 10 ml/min – intravenously 1 g, then 500 mg/day or 250-500 mg/day orally in one dose. For children, doses should be reduced in the same way.

Hemodialysis reduces the concentration in the blood serum, in connection with which, during and at the end of dialysis, an additional 500 mg is administered intravenously.

With caution, the drug should be used in cases of chronic renal failure, and in elderly patients (due to the possible risk of developing renal failure).

Pediatric Use

In children with chronic renal failure, the drug is used in an average single dose with an increase in the intervals between administrations, as indicated for adults.

Geriatric Use

The drug should be used with caution in elderly patients (due to the possible risk of renal failure).

Special Precautions

Treatment of patients suffering from asthma, eczema, or pollinosis should be carried out under medical supervision.

Since Amoxicillin reduces the effectiveness of oral contraceptives, women taking progestogenic and estrogenic contraceptive agents are advised to use alternative or additional methods of contraception.

A false-positive result of reactions when testing for glucose in urine by the colorimetric method is possible, as well as a reversible increase in prothrombin time.

Amoxicillin can reduce the concentration of total protein in blood plasma.

Amoxicillin in high concentration contributes to a decrease in blood glucose concentration.

With prolonged use of the drug, periodic monitoring of kidney function, liver function, and a complete blood count is necessary.

Due to the high concentration of amoxicillin in urine, it may precipitate on the walls of the catheter, therefore periodic monitoring of catheter patency is necessary.

Effect on the ability to drive vehicles and mechanisms

There are no data on the negative effect of the drug Trifamox IBL^® in recommended doses on the ability to drive vehicles or operate machinery. However, given the likelihood of developing side effects from the central nervous system, caution should be exercised when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: impaired gastrointestinal function (nausea, vomiting, diarrhea) and water-electrolyte balance. In some cases – reversible interstitial nephritis with oliguric renal failure due to amoxicillin overdose.

Treatment: it is recommended to discontinue the drug. Symptomatic therapy is carried out. Amoxicillin and Sulbactam can be removed from the body by dialysis. Renal function recovers after discontinuation of the drug.

Drug Interactions

With simultaneous use of the drug Trifamox IBL^® and bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin), a synergism of action is observed; with bacteriostatic agents (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) – antagonism.

The use of probenecid may cause a decrease in renal tubular secretion, leading to a prolonged increase in the plasma concentration of amoxicillin.

With simultaneous use of the drug Trifamox IBL^® with methotrexate, the excretion of the latter is slowed down.

Trifamox IBL^® enhances the effectiveness of indirect anticoagulants (monitoring of blood coagulation parameters is necessary).

Trifamox IBL^® reduces the effectiveness of oral contraceptives.

With simultaneous use of the drug Trifamox IBL^® with ethinylestradiol, the risk of breakthrough bleeding increases.

With simultaneous use of the drug Trifamox IBL^® with allopurinol, the risk of skin manifestations of allergic reactions increases.

Storage Conditions

The drug should be stored out of the reach of children, in a dry place, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is dispensed by prescription.

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.