Zocef

Zocef is an antimicrobial drug from the 2nd generation cephalosporin subcategory. It contains the substance cefuroxime, which has a bactericidal effect on a relatively wide range of different microbes (gram-negative and -positive), including strains that help produce β-lactamases.

The active element of the drug is resistant to the action of β-lactamases, due to which it affects a relatively large number of amoxicillin- or ampicillin-resistant strains. Its bactericidal properties are manifested by disrupting the processes of binding of microbial cell membranes.

Indications Zocepha

It is used for various infections caused by bacteria that are sensitive to cefuroxime (or is used until the causative bacteria of the infection are identified):

• respiratory system lesions: bronchitis in the active or chronic stage, pulmonary abscess, postoperative infections of the sternum organs, infected bronchiectasis and bacterial pneumonia;
• infections in the throat, ears or nose: tonsillitis with sinusitis, otitis media, and also pharyngitis;
• urinary tract lesions: cystitis, pyelonephritis in the active or chronic phase, bacteriuria without symptoms;
• infections affecting soft tissues: erysipelas, cellulitis or infections that appear in wounds;
• diseases affecting joints with bones: osteomyelitis or septic arthritis;
• gynecological pathologies: inflammation in the pelvic area;
• treatment of gonorrhea (especially when penicillin cannot be used);
• infections, including peritonitis with septicemia and meningitis.

Prevention of infections in cases of increased risk of complications following operations in the peritoneum and sternum area, affecting the pelvis, as well as after orthopedic or cardiovascular procedures.

The use of Zocef alone for therapy is generally sufficient to achieve the desired effect, but if necessary, it can be combined with aminoglycosides or metronidazole (via injections, suppositories, or orally), especially as a prophylactic agent during gynecological or gastrointestinal surgeries.

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Release form

The medicinal substance is released in the form of an injection lyophilisate - inside glass vials, the volume of which is 0.75 or 1.5 g. Inside a separate box - 1 vial.

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Pharmacodynamics

Cefuroxime has been shown to be effective against the following bacteria in in vitro testing:

• gram-negative aerobes: Klebsiella with Providencia, Escherichia coli with Moraxella catarrhalis and Proteus mirabilis, as well as Haemophilus influenzae (with ampicillin-resistant strains), meningococci, Haemophilus parainfluenzae (with ampicillin-resistant strains), gonococci (with strains that produce penicillinase) and Salmonella;
• aerobes of the gram-positive type: pneumococci with Staphylococcus aureus, and in addition Streptococcus mitis (subcategory viridans) with epidermal types of staphylococci (with strains that help produce penicillinase, and without methicillin-resistant strains), subgroup B streptococci (Streptococcus agalactiae), pyogenic streptococci (with them other streptococci of the β-hemolytic form) and whooping cough bacilli;
• anaerobes: this includes gram-negative as well as -positive cocci, including peptococci and Peptostreptococcus species;
• microbes of gram-positive (including most clostridia) and gram-negative types (fusobacteria with bacteroides), as well as propionibacteria;
• Others: Borrelia burgdorferi.

Bacteria that demonstrate resistance to cefuroxime include pseudomonas, listeria monocytogenes, legionella with clostridia difficile, campylobacter, methicillin-resistant staphylococci (aureus and epidermidis), and Acinetobacter calcoaceticus.

Certain strains of bacteria that are resistant to the drug include Proteus vulgaris, Serratia, Enterococcus faecalis, Bacteroides fragilis, Citrobacter with Enterobacter, and Morgan's bacillus.

In vitro testing has shown that when the drug is combined with aminoglycosides, a significant additive effect is observed; sometimes synergism also develops.

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Pharmacokinetics

Serum Cmax values of cefuroxime are determined after a 30-45-minute interval from the moment of administration. The half-life of the component after an intramuscular or intravenous injection is approximately 70 minutes. Combined administration with probenecid inhibits the excretion of cefuroxime and leads to an increase in its serum level.

Intraplasmic protein synthesis is in the range of 33-50%.

Within 24 hours from the moment of administration, almost all of the drug (85-90%) is excreted unchanged in the urine (the main part of the drug is excreted in the first 6 hours). Cefuroxime is not subject to metabolic processes, excreted through the secretion of tubules and CF.

Serum drug levels can be reduced by dialysis.

Cefuroxime indicators, having a higher level of MIC (MIC) in the main part of common pathogenic bacteria, are noted inside the synovium together with bone tissue and eye fluid. The component overcomes the BBB if the patient has inflammation affecting the membranes of the brain.

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Dosing and administration

Zocef can only be administered intramuscularly or intravenously.

General instructions.

For most infections, an adult needs a standard intravenous or intramuscular administration of 0.75 g of the substance, 3 times a day. If the infection is severe, the dose is increased to 3 times the use of 1.5 g of the drug per day. If necessary, the frequency of Zocef use can be increased to a 6-hour interval, and the total daily dosage will increase to 3-6 g. Individual infections can be treated according to the following regimen: 0.75 or 1.5 g 2 times a day (i/m or i/v) with subsequent transition to oral use.

Children need 0.03-0.1 g/kg per day (divided into 3-4 injections). For most lesions, a dosage of 0.06 g/kg per day can be used.

Newborns are prescribed the use of 0.03-0.1 g/kg per day (in 2-3 injections). It is necessary to take into account that the half-life of the substance during the first weeks after birth can be three to five times higher than the indicators determined in adults.

For gonorrhea, 1.5 g of the drug is used in 1 injection or in 2 injections (one in each buttock) in a dose of 0.75 g.

It is prescribed for monotherapy in case of meningitis of bacterial genesis (develops under the influence of sensitive microbial strains). An adult should take 3 g of the drug at 8-hour intervals. Children are usually administered 0.15-0.25 g/kg per day (the specified dosage is divided into 3-4 administrations). Newborns - intravenous administration of 0.1 g/kg per day.

Prevention.

Adults are usually given 1.5 g of the drug simultaneously with anesthesia during procedures in the pelvic or abdominal area, as well as orthopedic ones. It can be supplemented with an intramuscular injection of 0.75 g of the component after an 8- and 16-hour period.

In case of operations related to the lungs, heart or blood vessels, as well as the esophagus, the dosage is usually also 1.5 g (in combination with anesthesia). Additionally, 0.75 g of the drug is administered intramuscularly per day, 3 times, over 1-2 days.

When a patient undergoes a total joint replacement, 1.5 g of medicinal lyophilisate should be mixed with cement methyl methacrylate polymer (one packet volume is required), and then the monomer should be added in liquid form.

Sequential treatment procedures.

During the day for pneumonia, 1.5 g of Zocef should be used (IV or IM injections) 2-3 times (over a period of 48-72 hours). Then the patient is transferred to daily intake of tablets - 0.5 g 2 times, over a period of 7-10 days.

In case of chronically active bronchitis in the acute phase, 0.75 g of the drug is administered intramuscularly or intravenously 2-3 times a day (over a period of 48-72 hours), and then tablets are prescribed - 0.5 g of the drug should be taken 2 times a day for 5-10 days.

The duration of these therapeutic cycles is selected taking into account the clinical picture and the degree of intensity of infection.

Renal dysfunction.

Cefuroxime is excreted through the kidneys. Therefore, people with impaired renal function need to reduce the dose of the drug to compensate for its slow excretion. The standard dose does not need to be reduced (0.75-1.5 g 3 times a day), while the CC values are 20 ml per minute. In case of severe renal impairment (CC - in the range of 10-20 ml per minute), it is necessary to administer 0.75 g 2 times a day; with CC values less than 10 ml per minute - 0.75 g per day, once a day.

During hemodialysis, 0.75 g of the substance should be administered intravenously or intramuscularly at the end of each session. In addition to parenteral injections, the drug can be added to the dialysis fluid (0.25 g/2 l of fluid is required).

People undergoing long-term hemodialysis (arterial) or rapid hemofiltration in intensive care should be administered 0.75 g of the drug twice a day. If hemofiltration is performed at a low rate, the regimen required for therapy in renal dysfunction is observed.

Specifics of drug use.

Before administering the drug, 0.25 g of the substance is diluted with injection liquid (1 ml). For a portion of 0.75 g, 3 ml of liquid is required. The container with this mixture should be shaken until a suspension of opaque form is formed.

For intravenous injections, 0.25 g of the drug must be diluted in at least 2 ml of liquid; 0.75 g - in at least 6 ml of liquid; 1.5 g - in 15 ml. For infusions lasting no longer than half an hour, 1.5 g of the drug is diluted in 50-100 ml of a special injection liquid. These substances are used either intravenously or using a dropper for infusions.

Diluted solutions may change the saturation of their color during storage.

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Use Zocepha during pregnancy

Although preclinical tests have not revealed any teratogenic or mutagenic effects of Zocef, it should not be used during pregnancy (especially in the first trimester) without strict indications.

During the period of therapy, you should stop breastfeeding.

Contraindications

Contraindicated for use in people with severe intolerance to cephalosporins.

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Side effects Zocepha

Side effects include:

• invasions or infections: occasionally, there is an overgrowth of resistant bacteria (eg, Candida);
• blood dysfunction: eosinophilia or neutropenia is often observed. Sometimes leukopenia, a positive Coombs test, or a decrease in the hemoglobin level appear. Thrombocytopenia develops rarely. Cephalosporins can be absorbed through the surface of the walls of red blood cells and demonstrate interaction with antibodies, leading to a positive Coombs reaction, which can affect the procedure for determining the blood group or (single) lead to hemolytic anemia;
• immune damage: sometimes urticaria or epidermal rashes and itching are observed. Drug fever develops occasionally. Isolated cases of anaphylaxis, and also tubulointerstitial nephritis or epidermal vasculitis;
• digestive disorders: discomfort in the gastrointestinal tract is occasionally noted; isolated cases include pseudomembranous colitis;
• problems associated with the hepatobiliary system: usually there is a transient increase in the values of intrahepatic enzymes; sometimes - bilirubin levels temporarily increase. These disorders usually occur in people with existing liver disease, there is no information on the negative impact on the liver;
• lesions of the subcutaneous layers and epidermis: TEN or SJS, as well as erythema multiforme, occur sporadically;
• urinary tract disorders: serum creatinine or blood urea nitrogen levels increase occasionally, and the CC index decreases;
• systemic and local manifestations: disorders in the injection area are often observed, including thrombophlebitis and pain. The appearance of pain in the injection area is more likely when using high doses, but this is not a reason to cancel the drug.

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Overdose

Cephalosporin poisoning can cause signs of cerebral irritation, leading to seizures.

Cefuroxime levels can be reduced through peritoneal or hemodialysis sessions. Symptomatic measures are also taken.

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Interactions with other drugs

Zocef is able to affect the intestinal flora, which significantly weakens estrogen reabsorption and reduces the effectiveness of complex oral contraception.

During the use of the drug, plasma and blood sugar levels should be determined using hexose kinase or glucose oxidase tests.

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Storage conditions

Zocef must be stored in a place inaccessible to children. Temperature values - no more than 25 ° C. The prepared liquid can be kept at this temperature for a maximum of 6 hours, and at values up to 6 ° C - a maximum of 24 hours.

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Shelf life

Zocef can be used for a period of 24 months from the date of manufacture of the medicinal substance.

Analogues

Analogues of the drug are Aksef, Cefutil, Zinnat and Auroxetil with Cefumax, as well as Euroxim, Cetyl and Zinacef with Cefoctam, Mikrex and Kimacef with Cefuroxime.

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