Cefoctam

Cefoctam is an antibiotic, a second-generation cephalosporin.

Indications Cefoxam

It is used in such situations:

• infections affecting the respiratory ducts (bronchitis or bronchiectasis, which have an infected character, pulmonary abscess or bacterial pneumonia, as well as infections occurring after surgery that affect the organs of the sternum);
• infectious lesions of the nose or throat ( tonsillitis, and in addition to this, sinusitis or pansinusitis, and at the same time pharyngitis);
• urinary tract infections (cystitis or pyelonephritis or bacteriuria proceeding without symptoms);
• soft tissue infections (associated with wounds, and in addition, erysipeloid or cellulitis);
• diseases affecting the joints or bones (osteomyelitis or arthritis having a septic nature);
• gynecological and obstetrical infections (gonorrhea or lesions affecting the pelvic organs);
• other infectious diseases (meningitis or septicemia);
• preventing the development of complications of an infectious nature after surgical procedures in the thoracic, vascular, gynecological, abdominal, and in addition proctological and orthopedic areas.

Release form

The release of the drug substance is realized in the form of a lyophilisate for injection fluid (0.75 or 1.5 g inside the bottle).

Pharmacodynamics

The drug has bactericidal properties, and also violates the processes of binding of the cell membranes of bacteria. The drug has a wide range of effects; It is resistant to the effects of a large number of β-lactamases, and therefore has an impact on many amoxicillin-or ampicillin-resistant strains.

Actively acts in relation to such organisms:

• Gram-negative aerobes (Klebsiella along with intestinal sticks, Haemophilus parainfluenzae and cuts (hemophilus-resistant strains), anti-ampicillin-resistant strains), antipsychists, providences, Proteus rettgeri, meningococci, Moraxella catarallis, along with acne-resistant, anti-cracks, and anti-marts; ;
• Gram-positive aerobes (golden or epidermal staphylococci (among them are strains that produce penicillinase, besides methicillin strains), pneumococci, pyogenic streptococci (and with them other β-hemolytic streptococci), streptococci of the subtype B (streptococcus aacragastus), and streptococcus subtyptococcus bacterium bacillus (including streptococcus streptococci) , as well as pertussis wand);
• anaerobes;
• Cocci of the gram-negative and-positive nature (in this list peptokokki and Peptostreptococcus species);
• Gram-positive (among them, most of the clostridia) and -negative microbes (in this category, fusobacteria and bacteroids), and also propionibacteria;
• the remaining microbes: Burgdorfer borrelia.

The following bacteria have resistance against cefuroxime: pseudomonads together with clostridium deficiency, and in addition campylobacter, listeria monocytogenes, Acinetobacter calcoaceticus, legionella, and also strains of epidermal or Staphylococcus aureus against relatively methicillin.

Separate microbial strains that are not sensitive to cefuroxime: faecal enterococcus along with the common protein, Morgan's bacterium, citrobacter, enterobacter, serration and fragilis bacteroids.

Pharmacokinetics

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

Indicators of synthesis with protein of blood plasma - within 33-50%. The therapeutic values of drugs are noted inside synovia, CSF (if the brain membranes are inflamed) and pleural fluid, and also inside sputum, bile, myocardium with bone tissues, the subcutaneous layer and epidermis. The drug penetrates the placenta and is excreted in the mother's milk. It should also be borne in mind that it passes through the BBB, if the patient has inflammation affecting the meninges.

About 85-90% of the substance is excreted through the kidneys in an unchanged state after 24 hours (50% of the drug is excreted through the kidney tubules, and another 50% is exposed to glomerular filtration).

The half-life after i / m or i / v injection is approximately 70 minutes (in newborns, it can lengthen by 3-5 times).

Dosing and administration

Introduce the medicinal substance must be in / in or in the / m method. Before you begin therapy, you should exclude the likelihood of intolerance in the patient by performing a skin test.

Adolescents older than 12 years of age or with a weight of more than 50 kg, and in addition, adults need to enter 0.75 g of drugs 2-3 times a day. If the infection is severe in nature or the drug has poor efficacy, it is allowed to increase the portion to 0.75 g 4 times a day.

For newborns (also premature) a portion of 30-100 mg / kg per day is required; It must be divided into several separate parts.

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Use Cefoxam during pregnancy

Cefoctam can pass through the placenta, but its safety in case of use during pregnancy has hardly been studied.

The active drug element in small concentrations is excreted with the mother's milk, which is why it is required to stop breastfeeding during therapy.

Contraindications

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

Side effects Cefoxam

The use of a therapeutic agent can cause the following side effects:

• lesions that are infectious in nature: mycoses in the genital area, fungal forms of infections that have a secondary type, as well as infections triggered by the activity of resistant bacteria;
• disorders of the lymph and blood system: thrombocyte, leuko- or granulocytopenia, hemolytic anemia, eosinophilia, elevated PTV values, increased creatinine levels, agranulocytosis and coagulation disorders;
• problems with digestive function: stomatitis, obstruction of the gastrointestinal tract, diarrhea, pancreatitis, nausea, and glossitis. Occasionally, a pseudomembranous form of enterocolitis occurs;
• symptoms of the hepatobiliary system: curable cholelithiasis, deposits of Ca salts inside the gallbladder, and also an increase in the blood values of liver enzymes (ALT, AST or alkaline phosphatase);
• lesions of the subcutaneous tissue or epidermis: urticaria, allergic dermatitis, pruritus, exanthema, PETN, rash, puffiness or erythema polyforme;
• urinary function disorders: kidney failure, oliguria, kidney calculus formation, glucosuria, and hematuria;
• systemic disorders: phlebitis, fever, chills, headaches, anaphylactoid or anaphylactic symptoms, as well as dizziness;
• change in laboratory test readings: false positive response to the Coombs test or samples for glucosuria or galactosemia.

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Overdose

When intoxicating with this remedy, there may be manifestations of cerebral irritation, including seizures.

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

Interactions with other drugs

Drugs that weaken platelet aggregation (among them salicylates with NSAIDs and sulfinpirazon), in combination with cefuroxime, inhibit the 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.

Diuretic drugs and potentially nephrotoxic antibiotics (such as aminoglycosides) can 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 cefuroxime clearance inside the kidneys, due to which its serum indices increase.

When drugs are combined 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 the blood and plasma parameters of sugar using the hexozokinase or glucose oxidase method.

Cefuroxime has no effect on the testimony of enzymatic methods for determining the presence of glycosuria.

Cefuroxime has an insignificant effect on testing methods, which are based on the recovery of copper (Fehling, Benedict or Klinitest). Its effect does not cause the development of a false positive reaction, which is observed when using some other cephalosporins.

The drug does not affect the data of tests of creatinine values, conducted using alkaline picrate.

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Storage conditions

Cefoctam must be kept at temperature values within the limits of 15-25 ° С.

Shelf life

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

Analogs

Analogues of drugs are Abicef, Cefur, Axsef, Spisef, Biofuroxime with Micrex, and in addition Zinatsef, Cefumax, Jokel with Cefunort, Kimacef with Furocef, as well as Enfexia and Cefurox with Cefutyl.

[4], [5], [6]