Cefepime

Cefepime is an antibiotic, belongs to the category of 4th generation cephalosporin drugs.

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Indications Cefepime

It is used to treat moderate or severe pneumonia caused by the activity of enterococci and streptococci, as well as Klebsiella and other bacteria sensitive to the effects of the drug.

In addition, the medication is used for the treatment of:

• for infections affecting the urinary system (uncomplicated or complicated type);
• in neutropenic fever;
• for infections affecting the epidermis and subcutaneous tissues (uncomplicated).

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

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Release form

The release of the therapeutic substance occurs in the form of a lyophilisate for injection liquid, in glass vials, 1 piece inside a box. It can also be produced in the amount of 10 vials inside a blister plate, 10 blisters inside a pack.

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Pharmacodynamics

The medicinal effect is aimed at destroying the cells of the bacterial membrane. The medicine has bactericidal properties.

The drug has a powerful antibacterial effect on strains resistant to the activity of aminoglycosides and 3rd generation cephalosporins. The active element penetrates into the cells of gram-negative bacteria at high speed. It has strong resistance to hydrolysis of many β-lactamases. The main target of Cefepime inside the cells is the protein synthesizing penicillin.

The medication affects the activity of gram-negative microorganisms and gram-positive microflora in in vitro tests, as well as in vivo (enterobacteria with Klebsiella, streptococci, Proteus, Escherichia coli, Clostridia, etc.).

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Pharmacokinetics

Indicators of the drug in the blood plasma after intramuscular or intravenous administration:

A portion of a medicinal preparation	30 minutes	60 minutes	2 hours	4 hours	8 hours	12 hours
0.5 g intravenously	38.2 mcg/ml	21.6 mcg/ml	11.6 mcg/ml	5 mcg/ml	1.4 mcg/ml	0.2 mcg/ml
1 g intravenously	78.7 mcg/ml	44.5 mcg/ml	24.3 mcg/ml	10.5 mcg/ml	2.4 mcg/ml	0.6 mcg/ml
2 g intravenously	163.1 mcg/ml	85.8 mcg/ml	44.8 mcg/ml	19.2 mcg/ml	3.9 mcg/ml	1.1 mcg/ml
0.5 g intramuscularly	8.2 mcg/ml	12.5 mcg/ml	12 mcg/ml	6.9 mcg/ml	1.9 mcg/ml	0.7 mcg/ml
1 g intramuscularly	14.8 mcg/ml	25.9 mcg/ml	26.3 mcg/ml	16 mcg/ml	4.5 mcg/ml	1.4 mcg/ml
2 g intramuscularly	36.1 mcg/ml	49.9 mcg/ml	51.3 mcg/ml	31.5 mcg/ml	8.7 mcg/ml	2.3 mcg/ml

In bile with urine and peritoneal fluid, as well as sputum, mucous bronchial secretions and gall bladder, as well as appendix with prostate, medicinal values of cefepime are also noted.

The average half-life of the drug is approximately 2 hours. Volunteers who were given doses of up to 2000 mg (at intervals of 8 hours) for 9 days did not experience any accumulation of the drug in the body.

During metabolism, the substance is converted into the component N-methylpyrrolidine, which quickly transforms into the oxide of this element. Average values of total clearance are 120 ml/minute.

Most of cefepime is excreted via the kidneys, primarily via glomerular filtration (mean intrarenal clearance is 110 ml/min). About 85% of the drug portion (unchanged component) is found in the urine, as well as 1% of the substance N-methylpyrrolidine, about 6.8% of the element N-methylpyrrolidine oxide, and about 2.5% of the component cefepime epimer.

Plasma protein synthesis of cefepime is less than 19%. The level of the drug in the blood serum is not significant.

People over 65 years of age (with healthy renal function) do not need to change the dose of the drug, although their renal clearance rates are lower.

Tests conducted on patients with varying degrees of kidney failure have shown that the drug's half-life is prolonged. The average half-life in patients with severe forms of the disorder (who require dialysis sessions) is 13 hours (hemodialysis) or 19 hours (peritoneal dialysis).

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Dosing and administration

The medication is administered via intravenous infusion (the procedure lasts at least 30 minutes). Sometimes, the medication can also be administered intramuscularly (for the treatment of urogenital pathologies caused 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 the drug at intervals of 8 hours. Therapy should be carried out until complete recovery (usually this occurs within 10 days).

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

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

People undergoing hemodialysis sessions are given 1000 mg of the drug on the first day of the antibacterial cycle, and then 500 mg daily (for the treatment of neutropenic fever, the dose is increased to 1000 mg). The drug must be infused immediately after the hemodialysis procedure.

Scheme for dilution of lyophilisate for intravenous injection: it is necessary to use 5% dextrose solution for this (0.9% NaCl solution can also be used). 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 can also be used.

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Use Cefepime during pregnancy

The use of Cefepime during pregnancy is permitted only in cases where the potential benefit to the woman is more likely to outweigh the risk of complications to the fetus.

The drug is excreted in breast milk (in small amounts), which is why breastfeeding should be discontinued during therapy.

Contraindications

The use of the drug is contraindicated in the presence of hypersensitivity to the active ingredient of the drug, cephalosporins with penicillins, as well as β-lactams.

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Side effects Cefepime

The drug may provoke the development of an allergy, which manifests itself as an epidermal rash, fever, TEN, itching, MEE and anaphylactoid symptoms.

Therapy may also result in the development of a positive Coombs test result.

After an intramuscular injection, redness and pain appear in the area where the procedure is performed. With intravenous injection, phlebitis occasionally occurs.

Other side effects include:

• disorders of the nervous system: dizziness, anxiety, confusion or restlessness, convulsions, headaches and paresthesia;
• problems with urinary function: renal dysfunction;
• gastrointestinal symptoms: constipation, dyspeptic symptoms, epigastric pain, pseudomembranous colitis, nausea and vomiting;
• disorders of hematopoiesis: bleeding occasionally occurs during antibacterial treatment, and in addition, leukopenia or anemia occurs. The level of neutrophils with platelets may also decrease;
• disorders of the respiratory system: the appearance of a cough;
• problems with cardiovascular function: increased heart rate, peripheral edema and dyspnea;
• indications for diagnostic and laboratory tests: increased PT values, hypercalcemia or hyperbilirubinemia, diagnosis of hypercreatininemia, as well as increased values of alkaline phosphatase or urea and liver enzymes;
• other symptoms: the appearance of chest pain, oropharyngeal candidiasis, asthenia, pain in the throat or back, as well as superinfections.

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Overdose

Intoxication causes potentiation of side effects. Manifestations of overdose: state of coma or stupor, feeling of confusion, myoclonus, and hallucinations.

Symptomatic procedures are used for treatment. Hemodialysis can be used.

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Interactions with other drugs

Cefepime may increase ototoxicity and adverse effects on the kidneys when combined with aminoglycosides.

The medicinal substance is prohibited to be combined with heparin and other antimicrobial drugs.

The drug should not be administered in combination with metronidazole.

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Storage conditions

Cefepime should be kept in a place inaccessible to small children. Temperature values should not exceed 25 ^o C. The prepared injection can be stored for a maximum of 24 hours (if the temperature is up to 25 ^o C), and up to 1 week (if the medicine is kept in the refrigerator).

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Shelf life

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

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Application for children

The medicine should not be prescribed to infants under 2 months of age.

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Analogues

The drug's analogues are Ladef, Efipim, Maksipim, as well as Movizar and Tsepim.

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Reviews

Cefepime receives positive feedback from patients commenting on it on forums. Its high medicinal effectiveness and the fact that it is tolerated without complications (if all doctor's instructions are followed) are noted.