Ceftriabol

Ceftriabol is a cephalosporin antibiotic with a high rate of medicinal effectiveness. It has a very wide range of bactericidal activity. It has the best effect on many gram-positive and -negative aerobes with anaerobes (this includes those who are resistant to semi-artificial and natural penicillins, 1st and 2nd generation cephalosporins, and aminoglycosides).

It does not show any effect against faecal enterococci, Listeria monocytogenes, Enterococcus faecium and methicillin-resistant staphylococci.

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Indications Ceftriabole

It is used for the following disorders:

• Bacterial infections caused by pathogens that are sensitive to ceftriaxone: meningitis and septicemia of bacterial origin, and lesions of the peritoneum (including peritonitis);
• diseases of an infectious and inflammatory nature in the area of the biliary tract and gastrointestinal tract: cholangitis with cholecystitis and empyema affecting the gallbladder;
• infectious and inflammatory lesions in the pelvic area: endometritis with parametritis, pelvic peritonitis and salpingo-oophoritis;
• active phase of otitis media;
• infections of joints, epidermis, bones and subcutaneous tissues;
• damage to the kidneys and urinary tract (with or without complications);
• tick-borne borreliosis;
• uncomplicated gonorrhea;
• lower respiratory tract infections: pleural empyema, lung abscess, or pneumonia.

Ceftriabol can be used to prevent infection in the event of surgery, as well as for infections in people with weakened immune systems.

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Release form

The drug is released in the form of a lyophilisate for intravenous and intramuscular injections, in 20 or 100 ml vials.

Pharmacodynamics

The pharmacokinetics of a drug is determined by the size of the dosage used.

With intravenous administration of 500, 1000 or 2000 mg of the drug, after half an hour its serum values are 82, 151 or 257 mg/l, respectively. After 120 minutes, a decrease in the values to 48, 67 and 154 mg/l is noted. After 24 hours, these values are 5, 9 and 15 mg/l.

With intramuscular injection, the Cmax level is recorded after 2 hours.

The bioavailability index of the drug is 100%.

Ceftriaxone can pass into fluids with tissues. During the day, its high levels are noted in the lungs, liver, heart, bile ducts, palatine tonsils with the middle ear, bones, prostate secretions, peritoneal together with pleural fluids, synovium and cerebrospinal fluid, as well as on the nasal mucosa. The drug passes into breast milk in minimal concentrations.

Excretion occurs in two ways: through the kidneys in an unchanged state (33-67%); the remainder of the unchanged element is excreted with bile, later being converted inside the intestine into inactive metabolic components excreted by the intestine.

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Dosing and administration

The medication should be administered intravenously or intramuscularly. Liquids containing Ca ions should not be used to dissolve the lyophilisate. In case of severe infections (or with a single use of a portion over 1000 mg), it is recommended to use the intravenous method.

The therapeutic regimen is selected individually by the doctor, taking into account the patient's age and condition, as well as the type of disease. In the case of severe liver damage (with normal kidney function) - or vice versa - a reduction in the dose of the drug is not required. For people with problems with both kidney and liver function, the daily dose without detecting plasma values of ceftriaxone should be a maximum of 2000 mg.

In case of intramuscular injection, 2000 mg of lyophilisate is dissolved in 1% lidocaine liquid (7 ml). The medicine should be administered deep into the gluteal muscle. Intravenous use of lidocaine is contraindicated.

For intravenous procedures, 2000 mg of the drug is diluted in 5% or 10% dextrose fluid or 0.9% NaCl (50 ml). It should be administered via infusion at a low speed - at least half an hour.

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Use Ceftriabole during pregnancy

Ceftriabol is prescribed to pregnant women only under strict indications, when the probable benefit is more expected than the risk of complications in the fetus. Therapy should be carried out under very careful constant supervision.

The medication cannot be used during lactation.

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Contraindications

Contraindicated for use in individuals with intolerance to ceftriaxone with penicillin, carbapenems and other cephalosporin antibiotics.

Use with extreme caution in cases of severe stages of kidney or liver disease and in ulcerative colitis of a non-specific nature, which is caused by the use of antibacterial drugs.

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Side effects Ceftriabole

Main side effects:

• digestive disorders: diarrhea, nausea, pseudomembranous colitis and vomiting;
• damage to the hematopoietic organs: thrombocyto-, neutro-, leukopenia or lymphopenia, anemia, thrombocytosis and eosinophilia;
• disorders associated with the urogenital tract: thrush or vaginitis;
• problems with the functioning of the nervous system: headaches or dizziness;
• signs of allergy: fever, itching, chills and rash;
• local manifestations: phlebitis, hardening in the area along the vein and pain (intravenous injection) or a feeling of severe tightness or warmth and hardening in the area of application (intramuscular injection).

Occasionally, abdominal pain, dyspepsia, jaundice, cramps, heart rhythm disorders, basophilia, nosebleeds, bronchial spasms and anaphylaxis may occur, as well as agranulocytosis, lymphocytosis or leukocytosis, as well as allergic pneumonitis. Hot flashes and hyperhidrosis may occur.

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Overdose

In case of intoxication, vomiting with confusion, diarrhea, and also nausea and convulsions are observed.

There is no antidote. Peritoneal or hemodialysis procedures do not reduce the substance levels. Symptomatic treatment is performed.

Interactions with other drugs

The lyophilisate can be combined with 0.9% NaCl, 5% and 10% dextrose solutions. To prepare the medicine, a mixed solvent can be used - 5% dextrose with 0.9% NaCl.

To dilute the powder, you cannot use solvents that contain Ca ions (including Hartmann and Ringer solutions).

The drug is not compatible with vancomycin, fluconazole, and aminoglycosides, so they cannot be combined in the same syringe or infusion system.

Combining the drug with NSAIDs increases the likelihood of bleeding.

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Storage conditions

Ceftriabol must be stored in a dark place at a temperature not exceeding 25°C.

Shelf life

Ceftriabol can be used for a 24-month period from the date of sale of the drug. The prepared solution retains its properties for 6 (temperature within 5-25°C) and 24 hours (temperature within 2-5°C).

Application for children

The drug should not be administered to newborns with hyperbilirubinemia or if they are given fluids that contain the Ca2+ component.

It is used with extreme caution in premature infants.

Analogues

The analogs of the drug are the substances Azaran, Cefson, Torotsef with Lendacin, as well as Medaxon, Broadsef-S, Stericef with Loraxone and Ceftrifin with Cefaxone.