Cefoctam

Cefoctam is an antibiotic, a second-generation cephalosporin.

Indications Cefoctama

It is used in the following situations:

• infections affecting the respiratory tract (bronchitis or bronchiectasis of an infected nature, pulmonary abscess or pneumonia of bacterial origin, as well as infections that occur after surgery and affect the organs of the sternum);
• infectious lesions of the nose or throat ( tonsillitis, and also sinusitis or pansinusitis, and also pharyngitis);
• infections of the urinary tract (cystitis or pyelonephritis, or asymptomatic bacteriuria);
• infections affecting soft tissues (associated with wounds, as well as erysipeloid or cellulitis);
• diseases affecting joints or bones (osteomyelitis or arthritis of a septic nature);
• gynecological and obstetric infections (gonorrhea or lesions affecting the pelvic organs);
• other infectious pathologies (meningitis or septicemia);
• prevention of the development of complications of an infectious nature after surgical procedures in the thoracic, vascular, gynecological, abdominal, and also proctological and orthopedic areas.

Release form

The medicinal substance is released in the form of a lyophilisate for injection liquid (0.75 or 1.5 g per vial).

Pharmacodynamics

The drug has bactericidal properties and also disrupts the processes of binding of bacterial cell membranes. The drug has a wide spectrum of action; it is resistant to the influence of a large number of β-lactamases, therefore it has an effect on many amoxicillin- or ampicillin-resistant strains.

It is active against the following organisms:

• gram-negative aerobes (Klebsiella together with Escherichia coli, Haemophilus parainfluenzae and Haemophilus influenzae (including strains resistant to ampicillin), Proteus mirabilis, Providencia, Proteus rettgeri, meningococci, Moraxella catarrhalis together with gonococci (including strains producing penicillinase) and Salmonella;
• gram-positive aerobes (golden or epidermal staphylococci (including strains that produce penicillinase, except for methicillin strains), pneumococci, pyogenic streptococci (and other β-hemolytic streptococci), subtype B streptococci (streptococcus agalactiae), streptococcus mitis (viridans category), as well as whooping cough bacilli);
• anaerobes;
• cocci of gram-negative and -positive nature (in this list peptococci and Peptostreptococcus species);
• gram-positive (including most clostridia) and -negative microbes (in this category fusobacteria and bacteroides), as well as propionibacteria;
• other microbes: Borrelia burgdorferi.

The following bacteria are resistant to cefuroxime: pseudomonads together with Clostridium difficile, as well as campylobacter, Listeria monocytogenes, Acinetobacter calcoaceticus, legionella, as well as methicillin-resistant strains of Staphylococcus epidermidis or Staphylococcus aureus.

Selected microbial strains that are not sensitive to cefuroxime include Enterococcus faecalis and Proteus spp., Morgan's bacillus, Citrobacter, Enterobacter, Serratia, and Bacteroides fragilis.

Pharmacokinetics

When used in a dosage of 0.75 g, the Cmax values in the blood serum are noted after 30-45 minutes, amounting to about 27 mcg/ml. After an intravenous injection of 0.75 or 1.5 g, at the end of the infusion, the peak values are 50 and 100 mcg/ml, respectively.

The synthesis rates with blood plasma protein are within 33-50%. Therapeutic values of the drug are observed inside the synovium, cerebrospinal fluid (if the meninges are inflamed) and pleural fluid, as well as inside sputum, bile, myocardium with bone tissue, subcutaneous layer and epidermis. The drug penetrates the placenta and is excreted with breast milk. It is also necessary to take into account that it passes through the BBB if the patient has inflammation affecting the meninges.

About 85-90% of the substance is excreted unchanged through the kidneys after 24 hours (50% of the drug is excreted through the renal tubules, and another 50% undergoes glomerular filtration).

The half-life after an intramuscular or intravenous injection is approximately 70 minutes (in newborns it can be extended by 3-5 times).

Dosing and administration

The drug must be administered intravenously or intramuscularly. Before starting therapy, the possibility of intolerance in the patient must be excluded by performing a skin test.

Teenagers over 12 years of age or weighing more than 50 kg, and adults should also be given 0.75 g of the drug 2-3 times a day. If the infection is severe or the drug is not very effective, the dose may be increased to 0.75 g 4 times a day.

For newborns (including premature babies), a dose of 30-100 mg/kg per day is required; it must be divided into several separate parts.

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Use Cefoctama during pregnancy

Cefoctam can cross the placenta, but its safety when used during pregnancy has been little studied.

The active ingredient of the drug is excreted in small concentrations in breast milk, which is why it is necessary to stop breastfeeding during therapy.

Contraindications

It is contraindicated to use the medication in case of intolerance to cephalosporins (in case of hypersensitivity to penicillins, there is a risk of developing a cross-reaction).

Side effects Cefoctama

The use of the therapeutic agent may provoke the appearance of the following side effects:

• lesions of an infectious nature: mycoses in the genital area, fungal infections of a secondary type, as well as infections caused by the activity of resistant bacteria;
• disorders of the lymph and blood system: thrombocytopenia, leukopenia or granulocytopenia, hemolytic anemia, eosinophilia, increased PT values, increased creatinine levels, agranulocytosis and coagulation disorders;
• problems with digestive function: stomatitis, obstruction of the biliary tract, diarrhea, pancreatitis, nausea, and glossitis. Rarely, pseudomembranous enterocolitis occurs;
• symptoms from the hepatobiliary system: curable cholelithiasis, deposits of Ca salts inside the gallbladder, and also an increase in blood levels of liver enzymes (ALT, AST or ALP);
• lesions of subcutaneous tissue or epidermis: urticaria, allergic dermatitis, itching, exanthema, TEN, rash, swelling or erythema multiforme;
• urinary dysfunction: renal failure, oliguria, formation of kidney stones, glucosuria, and hematuria;
• systemic disorders: phlebitis, fever, chills, headaches, anaphylactoid or anaphylactic symptoms, and dizziness;
• changes in laboratory test results: false positive result in the Coombs test or tests for glucosuria or galactosemia.

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Overdose

In case of intoxication with this agent, manifestations of cerebral irritation may appear, including convulsions.

To eliminate the disorder, hemodialysis or peritoneal dialysis procedures are performed, as well as the necessary symptomatic measures.

Interactions with other drugs

Medicines that weaken platelet aggregation (including salicylates with NSAIDs and sulfinpyrazone), in combination with cefuroxime, inhibit intestinal microflora, preventing the binding of vitamin K. As a result, the likelihood of bleeding increases.

Anticoagulants potentiate the anticoagulant effect, which also increases the risk of bleeding.

Diuretics and potentially nephrotoxic antibiotics (aminoglycosides are one such) may cause nephrotoxic effects. Combination with aminoglycosides leads to addiction, and sometimes synergism develops.

Probenecid weakens the secretory activity of the tubules and reduces the level of clearance of cefuroxime in the kidneys, due to which its serum levels increase.

When combining drugs with oral contraception, intestinal microflora is suppressed, as a result of which intestinal reabsorption of estrogens is weakened, which leads to a decrease in the therapeutic effectiveness of contraceptives.

During therapy with cefuroxime, it is recommended to determine blood and plasma sugar levels using the hexose kinase or glucose oxidase method.

Cefuroxime does not affect the results of enzyme methods for determining the presence of glucosuria.

Cefuroxime has a minor effect on copper reduction assays (Fehling, Benedict or Clinistest). Its effect does not cause the development of a false-positive reaction, which is observed with some other cephalosporins.

The drug does not affect the data of creatinine tests carried out using alkaline picrate.

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Storage conditions

Cefoctam must be maintained at temperatures between 15-25°C.

Shelf life

Cefoctam can be used within 24 months from the date of manufacture of the drug.

Analogues

The analogs of the drug are Abitsef, Cefur, Aksef, Spizef, Biofuroxime with Mikrex, as well as Zinacef, Cefumax, Yokel with Cefunort, Kimacef with Furocef, as well as Enfexia and Cefurox with Cefutil.

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