Cefaxone

Cefaxon is a 3rd generation antimicrobial drug from the cephalosporin category.

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Indications Cefaxone

It is used in the treatment of people with infectious diseases of different localization (caused by flora that is sensitive to cephalosporins). Among these pathologies:

• infections in the abdominal area (including infections in the intestinal tract and gallbladder, as well as peritonitis), as well as sepsis;
• meningitis;
• infectious diseases affecting bones and joints, as well as the skin and connective tissues;
• infections developing in the lower respiratory tract and ENT organs;
• infectious pathologies affecting the urinary system, as well as STDs (this also includes gonorrhea);
• sometimes the drug is prescribed to people with low immune indicators, which is observed with various infections;
• Doctors may recommend Cefaxon for use after surgery to prevent infections.

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Release form

It is released in the form of powder for parenteral administration, in vials with a capacity of 0.25, 0.5 and 1 g. There is 1 such vial in a box.

Pharmacodynamics

Cefaxon contains the substance ceftriaxone, which has the form of Na salt. This component is developed exclusively for parenteral administration. The drug has a pronounced bactericidal effect, inhibits the binding of elements that are the basis of bacterial cell membranes, and prevents the development and growth of pathogenic organisms.

Aerobic (gram-negative and gram-positive) bacterial strains are sensitive to ceftriaxone activity. These include staphylococci (such as Staphylococcus aureus and Staphylococcus epidermidis), category B streptococci (Streptococcus agalactiae), category A streptococci (Streptococcus pyogenes), Streptococcus viridans, pneumococci, and Streptococcus bovis. In addition, this list includes Escherichia coli, Aeromonas spp., Ducrey's bacillus, Moraxella catarrhalis, Haemophilus influenzae, Alcaligenes spp., Haemophilus parainfluenzae, Citrobacter, Klebsiella, Morgan's bacillus, Moraxella spp., and certain strains of Enterobacter. At the same time, the drug acts on gonococci, meningococci, Plesiomonas shigelloides, Providencia, Proteus mirabilis, Proteus vulgaris, Salmonella, Yersinia, Vibrios, Shigella, and also certain strains of Pseudomonas aeruginosa.

The drug also has an effect on diseases caused by the activity of anaerobes, including clostridia, bacteroides, peptostreptococci and peptococci, as well as Fusobacterium spp.

It is important to remember that certain strains of bacteroides (those that produce β-lactamases) are resistant to the action of ceftriaxone.

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Pharmacokinetics

After parenteral injection of the drug, high levels of its active element are observed inside the body. The drug is concentrated inside tissues and various biological fluids (including blood plasma, bronchial and pulmonary tissues, sputum, tissues of the urogenital system, and also bone and cartilage with connective tissues).

If the patient has inflammation of the meninges, Cefaxon forms high pharmacological concentrations in the cerebrospinal fluid, but in individuals without damage to the meninges, the substance hardly passes through the BBB.

The active element of the drug is reversibly synthesized with plasma protein. The effect of intestinal microflora leads to inactivation of ceftriaxone.

About 50-60% of the unchanged substance is excreted through the kidneys, and another 40-50% (also unchanged) is excreted with bile. The half-life of ceftriaxone in adults with healthy liver and kidney function is 8 hours.

If the patient has problems with kidney and liver function, and also in elderly people and children, an increase in the half-life of the active element is observed.

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Dosing and administration

The powder is used to prepare a parenteral solution. The introduction of Cefaxon is allowed only in a hospital. The prepared solution can be administered intramuscularly or intravenously (along with this at a slow speed by jet or drip). It is necessary to observe the same time intervals between the procedures of drug administration.

An intramuscular injection should be made into the area of the upper outer quadrant of the buttock (no more than 1 g of the drug can be injected into one muscle at a time).

Jet intravenous injection should be slow (procedure time – within 2-4 minutes). By drip method, infusion (40 ml) is administered intravenously for at least half an hour.

To prepare a solution for intramuscular injection, the powder must be diluted in a 1% lidocaine solution (2 or 3.5 ml) – for dosages of 0.25, 0.5 or 1 g, respectively.

For intravenous jet injection, it is necessary to dissolve 1 g of the drug in injection water (10 ml).

To set up an intravenous drip, dilute 2 g of the drug in 40 ml of one of the following solvents: 0.9% sodium chloride solution, 5% levulose or glucose solution (a glucose-based solution can also be 10%). Other solvents cannot be used for Cefaxon.

The dose sizes of the medicine and the duration of the course of treatment are selected by the doctor.

Recommended serving sizes for adolescents aged 12 and over, and adults:

• on average, 1-2 g of the drug must be administered per day (the required dose is administered once per day);
• to eliminate severe infections, it is permissible to increase the daily dosage to 4 g of the drug;
• For adults, to treat gonorrhea, it is necessary to administer 0.25 g of the drug intramuscularly once;
• To prevent the development of infection after surgery, a single standard dose of the drug should be administered 0.5-1.5 hours before the procedure.

Recommended serving sizes for children under 12 years of age:

• newborns need to be administered the drug daily at an average of 20-50 mg/kg of body weight;
• For the treatment of meningitis in children, the drug is allowed to be administered at a dosage of 100 mg/kg of body weight, but not more than 4 g/day.

Children under 12 years of age are usually given Cefaxone in a dosage of 20-50 mg/kg of weight, but a maximum of 2 g per day. When treating severe stages of infections, the dose may be increased to 75 mg/kg of weight, but a maximum of 3 g/day. Doses exceeding 50 mg/kg may only be administered intravenously by drip – over a period of at least half an hour.

For children whose weight exceeds 50 kg, the medicine, regardless of age, is prescribed in portions that are recommended for adults.

Depending on the type of pathogen, the duration of treatment can range from 4 to 14 days.

Recommended doses for people with kidney problems.

It should be taken into account that the maximum recommended daily dose for people whose creatinine clearance level is less than 10 ml/minute is 2 g of ceftriaxone.

If long-term use of the drug is expected, the patient's blood counts must be monitored.

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Use Cefaxone during pregnancy

The use of Cefaxon is completely prohibited in the 1st trimester. The doctor must exclude the possibility of pregnancy before prescribing this drug. In the 2nd and 3rd trimesters, the appropriateness of prescribing the drug is determined by the attending physician.

Nursing mothers should stop breastfeeding before starting to use the drug.

Contraindications

Contraindications include hypersensitivity to ceftriaxone, as well as other antimicrobial drugs from the cephalosporin category, as well as penicillins.

Use with caution in individuals with hyperbilirubinemia, and also (especially) in newborn infants.

Side effects Cefaxone

When treated with Cefaxon, patients may sometimes experience the following side effects:

• dysfunction of the nervous system: the appearance of headaches or dizziness, the development of asthenia;
• gastrointestinal disorders: vomiting or bowel disorders, development of stomatitis or glossitis, increased activity of liver enzymes. Pseudomembranous colitis is occasionally observed;
• symptoms from the hematopoietic system: development of leukopenia, thrombocytopenia or granulocytopenia, as well as hemolytic anemia and eosinophilia. Disorders of blood clotting processes are observed sporadically;
• allergy symptoms: development of urticaria, angioedema, exanthema, allergic dermatitis, as well as anaphylaxis and erythema multiforme;
• others: development of oliguria, chills, pain in the right hypochondrium, as well as hypercreatininemia and thrush.

In addition, parenteral administration of drugs may cause local symptoms, including a feeling of pain (after an intramuscular injection) and phlebitis (after an intravenous injection).

Sedimentation on the walls inside the gallbladder is observed sporadically - they can be detected during an ultrasound procedure. This symptom usually goes away after discontinuing the use of the drug. If the patient experiences pain, it is necessary to switch to conservative treatment.

Overdose

Due to ceftriaxone intoxication, the severity of side effects may be potentiated in patients.

The drug has no specific antidote. In case of overdose, symptomatic measures are required. It should be taken into account that hemodialysis or peritoneal dialysis procedures will be ineffective in such cases.

Interactions with other drugs

When eliminating severe infections, it is considered advisable to combine Cefaxon with aminoglycoside drugs (they mutually enhance each other's medicinal properties). But they must be administered separately, because they are incompatible for parenteral injections.

The ready-to-administer solution of Cefaxon is not compatible with other parenteral substances (except for solutions indicated in the instructions as recommended for the preparation of infusion).

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Storage conditions

When stored under standard conditions at a temperature of 15-25°C, Cefaxon can be used for 3 years from the date of manufacture of the drug.

The prepared medicinal solution has therapeutic properties for 6 hours if stored at 25°C, and for 24 hours if the temperature is no more than 5°C.

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Shelf life

3 years.

Reviews

Cefaxon is considered to be quite an effective remedy - its high-quality and effective effect is noted in the reviews of many patients. Among its disadvantages are the rather high cost of the drug, as well as the presence of a large number of side effects.