Cefepim

Cefepime is an antibiotic, is included in the category of cephalosporin medicines of the 4th generation.

[1]

Indications Cefepima

It is used for the treatment of moderate or severe pneumonia, triggered by the activity of enterococci with streptococci, and in addition klebsiella and other bacteria that are sensitive to the effects of the drug.

In addition, the medication is used for therapy:

• with infections that affect the urinary system (uncomplicated or complicated type);
• with neutropenic fever;
• in infections that affect the epidermis and subcutaneous tissue (uncomplicated nature).

The drug is prescribed for the treatment of complicated forms of infections that arise in the abdominal region (in combination with metronidazole).

[2], [3], [4], [5]

Release form

The release of the therapeutic substance takes place in the form of a lyophilizate for injection liquid, in flasks of glass, one piece inside the box. Also can be produced in the amount of 10 bottles inside the blister plate, 10 blisters inside the pack.

[6], [7], [8]

Pharmacodynamics

The drug effect is directed to the destruction of cells of the bacterial membrane. The medicine has bactericidal properties.

The drug has a powerful antibacterial effect against strains resistant to the activity of aminoglycosides and cephalosporins from the 3rd generation. The active element passes through the cells of gram-negative bacteria at high speed. It has a strong resistance to the hydrolysis of a variety of β-lactamases. The main purpose of Cefepime inside cells is a protein that synthesizes penicillin.

The medication affects the activity of gram-negative microorganisms and Gram-positive microflora in in vitro and in vivo tests (Enterobacteria with Klebsiella, Streptococcus, Proteus, Escherichia coli, Clostridium, etc.).

[9], [10]

Pharmacokinetics

The indices of the drug within the blood plasma after intramuscular or intravenous administration:

Batch of drug	30 minutes	60 minutes	2 hours	4 hours	8 ocloc'k	12 hours
0, 5 g intravenously	38.2 μg / ml	21.6 μg / ml	11.6 μg / ml	5 μg / ml	1.4 μg / ml	0.2 μg / ml
1 g intravenously	78.7 μg / ml	44.5 μg / ml	24.3 μg / ml	10.5 μg / ml	2.4 μg / ml	0.6 μg / ml
2 g intravenously	163.1 μg / ml	85.8 μg / ml	44.8 μg / ml	19.2 μg / ml	3.9 μg / ml	1.1 μg / ml
0, 5 g intramuscularly	8.2 μg / ml	12.5 μg / ml	12 μg / ml	6.9 μg / ml	1.9 μg / ml	0.7 μg / ml
1 g intramuscularly	14.8 μg / ml	25.9 μg / ml	26.3 μg / ml	16 μg / ml	4.5 μg / ml	1.4 μg / ml
2 g intramuscularly	36.1 μg / ml	49.9 μg / ml	51.3 μg / ml	31.5 μg / ml	8.7 μg / ml	2.3 μg / ml

 

Inside the bile with urine and peritoneal fluid, and in addition sputum, bronchial secretions and gall bladder mucosa, as well as an appendix with the prostate are also noted medication values of cefepime.

The average half-life of the drug is approximately 2 hours. In volunteers who received portions up to 2000 mg (at intervals of 8 hours) for 9 days, there was no accumulation of the drug inside the body.

In metabolism, the substance is converted into a component of N-methylpyrrolidine, which rapidly transforms into an oxide of this element. The average total clearance is 120 ml / minute.

Most of the cefepime is excreted through the kidneys, mainly by filtering the glomeruli (mean values of clearance within the kidneys are 110 ml / minute). Inside the urine, about 85% of the portion of the drug (unchanged component) is found, and in addition 1% of the substance is N-methylpyrrolidine, about 6.8% of the element is N-methylpyrrolidine oxide and about 2.5% of the cepepime epimer component.

Plasma synthesis of cefepime with protein is less than 19%. The level of the drug inside the blood serum does not matter.

People aged more than 65 years (with a healthy kidney function) do not need to change the portion of the drug, although the clearance in the kidneys is lower.

Tests conducted with the participation of patients with different severity of kidney failure showed that the half-life of the drug was prolonged. The average values of this indicator for people with severe forms of disorder (which need to conduct dialysis sessions) are 13 hours (conducting hemodialysis) or 19 hours (performing peritoneal dialysis).

[11], [12]

Dosing and administration

The medication is administered via an intravenous infusion (the procedure lasts a minimum of 30 minutes). Sometimes it is allowed and the introduction of the drug in / m method (for the treatment of pathologies of urogenital nature, provoked by E. Coli).

Therapy for pulmonary pneumonia: intravenous injection of 1-2 g of the drug (twice a day) for 10 days.

Empirical treatment of neutropenic fever: intravenous administration of 2 g of drugs with intervals of 8 hours. To conduct therapy it is necessary up to full convalescence (usually it occurs or happens for 10 days).

Therapy for infections in the urogenital area: iv injection of 500-1000 mg LS at intervals of 12 hours. The treatment cycle is about 7-10 days.

If the patient has a severe form of the above pathologies, the size of the portion is increased to 2 g, and the course of therapy lasts 10 days.

People who undergo hemodialysis on the first day of the antibacterial cycle are administered 1000 mg of the drug, and then 500 mg are used daily (for the treatment of neutropenic fever, the dose is increased to 1000 mg). The drug is required to be poured immediately after the hemodialysis procedure.

Scheme of lyophilizate dilution for intravenous injection: it is necessary to use a 5% dextrose solution (0.9% NaCl solution can also be used). A complete dissolution of the powder is required.

Before performing an intramuscular injection, the powder is dissolved in a special injection liquid containing paraben or benzyl alcohol. A 0.5% or 1% lidocaine solution may also be used.

[17], [18], [19], [20], [21]

Use Cefepima during pregnancy

Use Cefepime during pregnancy is allowed only in cases where the likely help to a woman is more expected than the risk of complications in the fetus.

The medicine is excreted with the mother's milk (small portions), which is why during the therapy it is necessary to refuse breastfeeding.

Contraindications

Contraindicated use of drugs in the presence of increased sensitivity to the active element of the drug, cephalosporins with penicillins, as well as β-lactams.

[13]

Side effects Cefepima

The medication can trigger the occurrence of an allergy that manifests itself as an epidermal rash, febrile condition, TEN, itching, MEE and anaphylactoid symptoms.

Also, therapy can lead to the development of a positive response from the Coombs test.

After an injection in / m, there is redness and pain in the area of the procedure. With iv injection rarely occur phlebitis.

Among other adverse events:

• disturbances in the work of the National Assembly: dizziness, feelings of anxiety, confusion or anxiety, convulsive syndrome, headaches and paresthesia;
• problems with urinary function: disorders of renal activity;
• symptoms from the gastrointestinal tract: constipation, dyspepsia, epigastric pain, pseudomembranous form of colitis, nausea and vomiting;
• disorders of hematopoietic processes: occasionally with antibacterial treatment there are bleeding, and in addition there is leukopenia or anemia. Also, the level of neutrophils with platelets may decrease;
• violations in the respiratory system: the appearance of a cough;
• problems with the function of CAS: increased heart rate, peripheral swelling and dyspnea;
• indications of diagnostic and laboratory tests: increased values of PTV, hypercalcemia or hyperbilirubinemia, diagnosis of hypercreatininaemia, and an increase in the values of alkaline phosphatase or urea and hepatic enzymes;
• other signs: the appearance of pain behind the breastbone, candidiasis oropharyngeal nature, asthenia, pain in the throat or back, and also, superinfection.

[14], [15], [16]

Overdose

Intoxication causes potentiation of side effects. Manifestations of an overdose: a state of coma or stupor, a sense of confusion, myoclonia, and hallucinations.

For treatment, symptomatic procedures are performed. You can use hemodialysis.

[22], [23]

Interactions with other drugs

Cefepime can enhance ototoxicity, as well as adverse effects on the kidney when combined with aminoglycosides.

Medicamentous substance is forbidden to be combined with heparin and other antimicrobial drugs.

The drug should not be taken in combination with metronidazole.

[24], [25], [26]

Storage conditions

Cefepime is required to be kept in a place inaccessible for infiltration of small children. The temperature values - not above the level 25 ^of C. The finished injection allows to store up to 24 hours (when the temperature in this case is up to 25 ^on C), as well as to the 1st week (if the drug is contained in the refrigerator).

[27], [28]

Shelf life

Cefepime is allowed to be used within 36 months of the release of the therapeutic agent.

[29], [30]

Application for children

Do not administer the medication to infants until 2 months.

[31], [32], [33],

Analogues

The analogues of the medication are funds Ladef, Efipim, Maxipim, as well as Movizar and Tsepim.

[34], [35]

Reviews

Cefepim receives positive feedback from patients commenting on it on the forums. It is noted for its high drug efficiency and the fact that it is tolerated without complications (if all medical instructions are observed).