Tablet cephalosporins 3rd generation. III generation cephalosporins

Third generation cephalosporins are highly active against aerobic gram-negative bacteria. This is one of the most popular drugs representing 3rd generation cephalosporins.

Cephalosporins have a fairly wide spectrum of action, due to which they are actively used to treat infections (bacterial) of the upper respiratory tract, genitourinary, and digestive systems. In addition, 3rd generation cephalosporins produce a less inhibitory effect on the immune system, the reaction of the defense system is practically not reduced, interferon is released in normal quantities.

3rd generation cephalosporins

Antibiotics from this series have increased activity and can be used in the fight against the most complex infections.

Third generation cephalosporins - ATC classification of drugs

But in the fight against staphylococci, cephalosporins are practically not used. The tablets have a fairly broad spectrum of action.

Antibiotics of the cephalosporin group, use

Thanks to this, there are practically no side effects from the use of tablets. In addition, cephalosporins have virtually no effect on intestinal function.

The drug is presented in the form of film-coated tablets.

Most often, tablets are used for inflammatory processes of the respiratory system. If we consider 3rd generation cephalosporins for children, then the drug “Pancef” is worth remembering first.

Group drugs: Third generation cephalosporins

Some 3rd generation cephalosporins are used prophylactically after surgery. Zedex tablets have an excellent effect on microorganisms that have developed resistance to penicillins.

Cedex tablets are prescribed to children over 12 years of age to treat bacterial infections of the respiratory system. But for patients who are allergic to penicillins, tablets are contraindicated.

Third generation cephalosporin antibiotics are used to treat infections of the respiratory system, as well as simple infections of the skin and subcutaneous tissue.

Tablets can be prescribed to older people, as well as women during lactation. Many patients, due to their physiological characteristics, cannot take pills. For older people, cephalosporins can be prescribed in the form of an injection solution.

Another broad-spectrum cephalosporin antibiotic, which is offered in pharmacies in powder form. Cephalosporins in tablets are often used to treat diseases of bacterial etiology.

The first drug from this group was obtained in 1964 (cephalothin). Since then, a large number of cephalosporins have been successfully synthesized. Cephalosporin antibiotics today are divided into several generations.

3rd generation cephalosporins in injection ampoules

It follows that tablet forms are represented by only three generations. From the 1st generation, Cephalexin (Keflex) is produced in tablets.

As for the 3rd generation, this group includes Cefixime and Ceftibuten. Each generation has its own characteristics. It is important that 1st generation drugs are less resistant to beta-lactamases. 1st generation cephalosporin tablets kill staphylococci, streptococci, Neisseria, E. coli, Shigella and Salmonella.

Pharmacological group - Cephalosporins

2nd generation cephalosporin antibiotics are characterized by a wider spectrum of antimicrobial action. Most often, 3rd generation drugs are used to treat patients.

This remedy is taken orally in tablet form. The drug is not prescribed to children under 3 years of age or if the drug is intolerant.

Of the 2nd generation tablet drugs, Zinnat and its analogues can be taken. Of the third generation tablet forms, patients are often prescribed Suprax or Tsemidexor.

Third generation cephalosporins are not destroyed (by 3-lactamase, which can be produced by H. influenzae and N. gonorrhoeae, and by many p-lactamases produced by Enterobacteriaceae.

Third generation cephalosporins are valuable drugs for the treatment of bacterial meningitis.

It is worth noting that the improved molecular structure of these synthetic antibiotics allows for a minimum number of side effects on the body.

For what diseases are cephalosporin tablets prescribed?

The described drugs are used for secondary infections for out-of-hospital and in-patient treatment. They can also be used as maintenance therapy concomitantly with parenteral agents. A significant part of this group of medications is produced in the form of powders for the production of suspensions.

Children are most often prescribed 3rd generation cephalosporins in the form of a suspension. Few third-generation cephalosporins, particularly ceftazidime, are active against P. aeruginosa.

Cephalosporins in tablets are one of the most extensive groups of antibacterial agents that are widely used for the treatment of adults and children. Medicines in this group are highly popular due to their effectiveness, low toxicity and convenient form of administration.

General characteristics of cephalosporins

Cephalosporins have the following characteristics:

contribute to the provision of a bactericidal effect;
have a wide range of therapeutic effects;
in approximately 7-11% they cause the development of cross-allergy. Patients with penicillin intolerance are at risk;
the drugs do not contribute to the effect against enterococci and listeria.

Drugs in this group can only be taken as prescribed and under the supervision of a physician. Antibiotics are not intended for self-medication.

The use of cephalosporin drugs may contribute to the following undesirable side effects:

allergic reactions;
dyspeptic disorders;
phlebitis;
hematological reactions.

Classification of drugs

Cephalosporin antibiotics are usually classified by generation. List of drugs by generation and dosage form:

Generation	Preparations for internal use	Medicines for parenteral (intravenous, intramuscular) administration
1	Cephalexin	Cefazolin-based drugs: Cefamezin, Kefzol
2	Preparations based on cefuroxime-axeitil: Zinnat, Kimacef, Zinacef, Ceftin	Cefuroxime, Cefoxitin
3	Cefixime	Ceftriaxone, Cefotaxime, Cefoperazone
4		Cefepime, Meropenem, Aztreonam
5		Ceftaroline fosamil, Ceftobiprole

The main differences between generations: the spectrum of antibacterial effects and the degree of resistance to beta-lactamases (bacterial enzymes whose activity is directed against beta-lactam antibiotics).

1st generation drugs

The use of these drugs helps to provide a narrow spectrum of antibacterial action.

Cefazolin is one of the most popular drugs that helps to act against streptococci, staphylococci, and gonococci. After parenteral administration it penetrates into the affected area. A stable concentration of the active substance is achieved if the medicine is administered three times over 24 hours.

Indications for use of the drug are: effects of streptococci on soft tissues, joints, bones, skin.

It should be taken into account: Cefazolin was previously widely used to treat a large number of infectious pathologies. However, after more modern 3-4 generation medications appeared, Cefazolin is no longer used in the treatment of intra-abdominal infections.

2nd generation drugs

2nd generation drugs are characterized by increased activity against gram-negative pathogens. 2nd generation cephalosporins for parenteral administration based on cefuroxime (Kimacef, Zinacef) are active against:

gram-negative pathogens, Proteus, Klebsiella;
infections caused by streptococci and staphylococci.

Cefuroxime, a substance from the second group of cephalosporins, is not active against Pseudomonas aeruginosa, Morganella, Providence and most anaerobic microorganisms.

After parenteral administration, it penetrates into most organs and tissues, including the blood-brain barrier. This makes it possible to use the drug in the treatment of inflammatory pathologies of the lining of the brain.

Indications for the use of this group of funds are:

exacerbation of sinusitis and otitis media;
chronic form of bronchitis in the acute phase, development of community-acquired pneumonia;
treatment of postoperative conditions;
infection of the skin, joints, bones.

The dosage for children and adults is selected individually, depending on the indications for use.

2nd generation drugs for internal use

Medicines for internal use include:

tablets and granules for preparing Zinnat suspension;
Ceklor suspension - this drug can be taken by a child; the suspension has a pleasant taste. It is not recommended to use Ceclor during the treatment of exacerbation of otitis media. The drug is also available in the form of tablets, capsules and dry syrup.

Oral cephalosporins can be used regardless of food intake; the active component is excreted by the kidneys.

3rd generation drugs

The third type of cephalosporins was initially used in hospital settings for the treatment of severe infectious pathologies. Today, such drugs can also be used in outpatient clinics due to the increased resistance of pathogens to antibiotics. 3rd generation drugs have their own application features:

parenteral forms are used for severe infectious lesions, as well as for the detection of mixed infections. For more successful therapy, cephalosporins are combined with antibiotics from the 2-3 generation aminoglycoside group;
drugs for internal use are used to eliminate moderate hospital infections.

3rd generation agents for internal use (Cefixime, Ceftibuten)

3rd generation cephalosporins intended for oral administration have the following indications for use:

complex therapy of exacerbations of chronic bronchitis;
development of gonorrhea, shigillosis;
stepwise treatment, if necessary, internal administration of tablets after parenteral treatment.

Compared to 2nd generation drugs, 3rd generation cephalosporins in tablets demonstrate greater effectiveness against gram-negative pathogens and enterobacteria.

At the same time, the activity of Cefuroxime (2nd generation drug) in the treatment of pneumococcal and staphylococcal infections is higher than that of Cefixime.

Use of Cefatoxime

Indications for the use of parenteral forms of cephalosporins (Cefatoxime) are:

development of acute and chronic forms of sinusitis;
development of intra-abdominal and pelvic infections;
exposure to intestinal infection (Shigella, Salmonella);
severe conditions in which the skin, soft tissues, joints, and bones are affected;
detection of bacterial meningitis;
complex therapy of gonorrhea;
development of sepsis.

The drugs have a high degree of penetration into tissues and organs, including the blood-brain barrier. Cefatoxime may be the drug of choice in the treatment of newborns. When meningitis develops in a newborn child, Cefatoxime is combined with ampicillin.

Features of using Ceftriaxone

Ceftriaxone is similar to Cefatoxime in its spectrum of action. The main differences are:

the possibility of using Ceftriaxone once a day. When treating meningitis – 1-2 times every 24 hours;
double elimination, so no dose adjustment is required for patients with renal dysfunction;
additional indications for use are: complex treatment of bacterial endocarditis, Lyme disease.

Ceftriaxone should not be used in neonates.

4th generation drugs

4th generation cephalosporins are characterized by an increased degree of resistance and demonstrate greater effectiveness against the following pathogens: gram-positive cocci, enterococci, enterobacteria, Pseudomonas aeruginosa (including strains that are resistant to Ceftazidime). Indications for the use of parenteral forms are the treatment of:

nosocomial pneumonia;
intra-abdominal and pelvic infections - possible combination with drugs based on metronidazole;
infections of the skin, soft tissues, joints, bones;
sepsis;
neutropenic fever.

When using Imipenem, which belongs to generation four, it is important to take into account that Pseudomonas aeruginosa quickly develops resistance to this substance. Before using drugs with such an active substance, a study should be carried out to determine the sensitivity of the pathogen to imipenem. The drug is used for intravenous and intramuscular administration.

Meronem is similar in characteristics to imipenem. The instructions for use state that among the distinctive characteristics are:

greater activity against gram-negative pathogens;
less activity against staphylococci and streptococcal infections;
the drug does not contribute to the provision of anticonvulsant action, therefore it can be used in the complex treatment of meningitis;
Suitable for intravenous drip and jet infusion; intramuscular administration should be avoided.

The use of the 4th generation cephalosporin group antibacterial Azactam helps to provide a smaller spectrum of action. The medicine has a bactericidal effect, including against Pseudomonas aeruginosa. The use of Azactam may contribute to the development of the following unwanted side effects:

local manifestations in the form of phlebitis and thrombophlebitis;
dyspeptic disorders;
hepatitis, jaundice;
neurotoxicity reactions.

The main clinically significant task of this drug is to influence the life processes of aerobic gram-negative pathogens. In this case, Azactam is an alternative to drugs from the aminoglycoside group.

5th generation drugs

Means that belong to the 5th generation contribute to the provision of a bactericidal effect, destroying the walls of pathogens. Active against microorganisms that demonstrate resistance to 3rd generation cephalosporins and drugs from the aminoglycoside group.

5th generation cephalosporins are presented on the pharmaceutical market in the form of drugs based on the following substances:

Ceftobiprole medocaril is a medicine under the trade name Zinforo. Used in the treatment of community-acquired pneumonia, as well as complicated infections of the skin and soft tissues. Most often, patients complained of adverse reactions in the form of diarrhea, headache, nausea, and itching. Adverse reactions are mild in nature; their development should be reported to your doctor. Particular care is required in the treatment of patients with a history of seizures;
Ceftobiprole is the trade name of Zeftera. Available in powder form for the preparation of solution for infusion. Indications for use are complicated infections of the skin and appendages, as well as infection of the diabetic foot without concomitant osteomyelitis. Before use, the powder is dissolved in glucose solution, water for injection or saline. The product should not be used in the treatment of patients under 18 years of age.

5th generation agents are active against Staphylococcus aureus, demonstrating a broader spectrum of pharmacological activity than previous generations of cephalosporins.

One of the most common classes of antibacterial drugs are cephalosporins. According to their mechanism of action, they are inhibitors of cell wall synthesis and have a powerful bactericidal effect. Together with penicillins, carbapenems and monobactams they form a group of beta-lactam antibiotics.

Due to their wide spectrum of action, high activity, low toxicity and good tolerance by patients, these medications are the leaders in the frequency of prescriptions for the treatment of inpatients and account for about 85% of the total volume of antibacterial drugs.

For convenience, the list of drugs is presented in five generation groups.

First generation

History of discovery and mechanism of production

In 1945, Italian professor Giuseppe Brotzu, while studying the ability of wastewater to self-purify, isolated a strain of fungus capable of producing substances that suppress the growth and reproduction of gram-positive and gram-negative flora. During further research, a drug from the Cephalosporium acremonium culture was tested on patients with severe forms of typhoid fever, which led to rapid positive dynamics of the disease and a speedy recovery of patients.

The first cephalosporin antibiotic, cephalothin ®, was created in 1964 by the American pharmaceutical company Eli Lilly .

The source for production was cephalosporin C ® - a natural producer of mold fungi and a source of 7-aminocephalosporanic acid. In medical practice, semi-synthetic antibiotics are used, obtained by acylation at the amino group of 7-ACC.

In 1971, cefazolin was synthesized, which became the main antibacterial drug for a whole decade.

The first drug and the founder of the second generation was cefuroxime ®, obtained in 1977. The most frequently used antibiotic in medical practice, ceftriaxone ®, was created in 1982, is actively used and “does not lose ground” to this day.

A breakthrough in the treatment of Pseudomonas aeruginosa infection can be called the production of ceftazidime ® in 1983.

Despite the similarity in structure with penicillins, which determines a similar mechanism of antibacterial action and the presence of cross allergies, cephalosporins have an expanded spectrum of influence on pathogenic flora, high resistance to the action of beta-lactamases (enzymes of bacterial origin that destroy the structure of an antimicrobial agent with a beta-lactam cycle) .

The synthesis of these enzymes determines the natural resistance of microorganisms to penicillins and cephalosporins.

General features and pharmacokinetics of cephalosporins

All medications in this class are different:

bactericidal effect on pathogenic microorganisms;
easy tolerability and relatively low number of adverse reactions compared to other antimicrobial agents;
the presence of cross-allergic reactions with other beta-lactams;
high synergism with aminoglycosides;
minimal disruption of intestinal microflora.

The advantage of cephalosporins also includes good bioavailability. Cephalosporin antibiotics in tablets have a high degree of absorption in the digestive tract. The absorption of drugs increases when used during or immediately after a meal (with the exception of cefaclor ®). Parenteral cephalosporins are effective with both intravenous and intramuscular routes of administration. They have a high distribution index in tissues and internal organs. Maximum concentrations of medications are created in the structures of the lungs, kidneys and liver.

High levels of the drug in bile are provided by ceftriaxone ® and cefoperazone ® . The presence of a dual route of elimination (liver and kidneys) allows them to be used effectively in patients with acute or chronic renal failure.

Cefotaxime ® , cefepime ® , ceftazidime ® and ceftriaxone ® are able to cross the blood-brain barrier, creating clinically significant levels in the cerebrospinal fluid and are prescribed for inflammation of the meninges.

Pathogen resistance to antibacterial therapy

Medicines with a bactericidal mechanism of action are most active against organisms in the growth and reproduction phases. Since the wall of a microbial organism is formed by highly polymeric peptidoglycan, they act at the level of synthesis of its monomers and disrupt the synthesis of polypeptide cross bridges. However, due to the biological specificity of the pathogen, different, new structures and modes of functioning are possible between different species and classes.

Mycoplasma and protozoa do not contain a shell, and some types of fungi contain a chitinous wall. Due to this specific structure, the listed groups of pathogens are not sensitive to the action of beta-lactams.

The natural resistance of true viruses to antimicrobial agents is determined by the absence of a molecular target (wall, membrane) for their action.

Resistance to chemotherapeutic agents

In addition to natural resistance, determined by the specific morphophysiological characteristics of the species, resistance can be acquired.

The most significant reason for the formation of tolerance is irrational antibiotic therapy.

Chaotic, unreasonable self-prescription of medications, frequent discontinuation and switching to another drug, use of one drug for short periods of time, violation and underestimation of dosages prescribed in the instructions, as well as premature discontinuation of an antibiotic - lead to the appearance of mutations and the emergence of resistant strains that do not respond to classical regimens treatment.

Clinical studies have proven that long time intervals between the administration of an antibiotic completely restore the sensitivity of bacteria to its effects.

The nature of acquired tolerance

Mutation-selection

Rapid resistance, streptomycin type. Develops on rifampicin ®, nalidixic acid.
Slow, penicillin type. Specific for cephalosporins.

Transmission mechanism

Bacteria produce enzymes that inactivate chemotherapy drugs. The synthesis of beta-lactamases by microorganisms destroys the structure of the drug, causing resistance to penicillins (more often) and cephalosporins (less often).

Resistance and microorganisms

Most often, resistance is characteristic of:

- and enterococci;
coli;
Klebsiella;
Mycobacterium tuberculosis;
shigella;
Pseudomonas.

Cefuroxime ®

Recommended for the treatment of moderate and acute symptoms.
Not used for damage to the nervous system and meninges.
Used for preoperative antibiotic prophylaxis and medical cover of surgical intervention.
Prescribed for mild inflammatory diseases of the skin and soft tissues.
Included in the complex treatment of infections.

Step therapy is often used, with the administration of parenteral Cefuroxime ® sodium, followed by a transition to oral Cefuroxime ® axetil.

Cefaclor ®

It is not prescribed for acute otitis media, due to low concentrations in the fluid. ear. Effective for the treatment of infectious and inflammatory processes of bones and.

3rd generation cephalosporin antibiotics

They penetrate the blood-brain barrier well and can be used for inflammatory and bacterial lesions of the nervous system.

Ceftriaxone ® and Cefoperazone ®

They are the drugs of choice for the treatment of patients with renal failure. Excreted through the kidneys and liver. Dose changes and adjustments are necessary only for combined renal and hepatic failure.

Cefoperazone ® practically does not cross the blood-brain barrier, therefore it is not used for meningitis.

Cefoperazone/sulbactam ®

It is the only inhibitor-protected cephalosporin.

It consists of a combination of cefoperazone ® with the beta-lactamase inhibitor sulbactam.

Effective in anaerobic processes, can be prescribed as a single-component therapy for inflammatory diseases of the pelvis and abdominal cavity. Also, it is actively used for severe hospital infections, regardless of location.

Cephalosporin antibiotics work well with metronidazole ® for the treatment of intra-abdominal and pelvic infections. They are the drugs of choice for severe, complicated infections. urinary tract. Used for sepsis, infectious lesions of bone tissue, skin and subcutaneous fat.

Prescribed for neutropenic fever.

Fifth generation drugs

Cover the entire spectrum of activity of the 4th and act on penicillin-resistant flora and MRSA.

Not assigned:

up to 18 years old;
patients with a history of seizures, epilepsy and renal failure.

Ceftobiprole ® (Zeftera ®) is the most effective treatment for diabetic foot infections.

Dosages and frequency of use of the main representatives of the group

Parenteral use

IV and IM administration is used.

Name	Calculation for adults	Dosages of cephalosporin antibiotics for children (in the column indicated from the calculation mg/kg per day )
Cefazolin ®	Prescribed at a rate of 2.0-6.0 g/day for three administrations. For preventive purposes, 1-2 g are prescribed an hour before the start of surgery.	50-100, divided by 2-3 times.
Cefuroxime ®	2.25-4.5 g per day, in 3 applications.	50-100 for 2 rubles.
Cefotaxime ®	3.0-8.0 g for 3 times. For meningitis up to 16 g in six injections. For gonorrhea, 0.5 g is prescribed intramuscularly, once.	From 40 to 100 in two injections. Meningitis - 100 for 2 rubles. No more than 4.0 g per day.
Ceftriaxone ®	1 g, every 12 hours. Meningitis - 2 g, every twelve hours. Gonorrhea - 0.25 g once.	For the treatment of acute otitis media, a dose of 50 is used, in three injections. not exceeding 1 g at a time.
Ceftazidime ®	3.0-6.0 g in 2 injections	30-100 for two times. For meningitis, 0.2 g in two doses.
Cefoperazone ®	From 4 to 12 g for 2-4 injections.	50-100 for three times.
Cefepime ®	2.0-4.0 g for 2 times.	At the age of over two months, 50 are used, divided into three administrations.
Cefoperazone/sulbactam ®	4.0-8.0 g for 2 injections.	40-80 for three applications.
Ceftobiprole ®	500 mg, every eight hours in the form of 120-minute IV infusions.	—

What antibiotics are classified as cephalosporins for oral use?

Name	Calculation for adults	Dosages of cephalosporin antibiotics for children (in the column are indicated at the rate of mg/kg per day)
Cephalexin ®	0.5-1.0 g four times a day.	Based on 45 for three uses.
	0.5-1.0 g four times a day.
	Prescribe 0.5 g twice a day.	12.5-25 twice a day.
Cefuroxime ®	0.25-0.5 g during meals, twice a day.	30, for 2 uses with meals. For the treatment of otitis media, the dose is increased by 40 in two doses.
	0.25-0.5 g during meals, twice a day.	For tonsillopharyngitis, the course of treatment is 10 days.
	0.25 every twelve hours.	Up to 20 in 2 times.
Cefaclor ®	0.25-0.5 g three times a day.	20-40 in three doses.
Cefixime ®	0.4 g for 2 uses.	At the age of over six months, 8 mg/kg is prescribed, divided into two doses.
Ceftibuten ®	Single dose 0.4 g.	9, for 1-2 uses.

Undesirable effects and drug combinations

Prescribing antacids significantly reduces the effectiveness of antibiotic therapy.
Cephalosporins are not recommended to be combined with anticoagulants and antiplatelet agents, thrombolytics - this increases the risk of intestinal bleeding.
Not combined with loop diuretics due to the risk of nephrotoxic effect.
Cefoperazone ® has a high risk of disulfiram-like effects when consumed with alcohol. Lasts up to several days after complete discontinuation of the drug. May cause hypoprothrombinemia.

As a rule, they are well tolerated by patients, however, the high frequency of cross-allergic reactions with penicillins should be taken into account.

Dyspeptic disorders are the most common, and pseudomembranous colitis is rare.

Less commonly, hemolytic anemia may occur.

Ceftriaxone ® is not prescribed to newborns, due to the high risk of developing kernicterus (due to the displacement of bilirubin from binding with blood plasma albumin), and is not prescribed to patients with biliary tract infections.

Various age groups

Cephalosporins 1-4 generations are used to treat women during pregnancy, without restrictions and the risk of teratogenic effect.

Fifth, it is prescribed in cases where the positive effect for the mother is higher than the possible risk for the unborn child. Little penetration into breast milk, however, administration during lactation can cause dysbacteriosis of the oral and intestinal mucosa in a child. Also, it is not recommended to use the fifth generation, Cefixime ®, Ceftibuten ®.
In newborns, higher dosages are recommended due to slow renal excretion. It is important to remember that Cefipime ® is allowed only from the age of two months, and Cefixime ® from the age of six months.
In elderly patients, dosage adjustments should be made based on the results of renal function tests and biochemical blood tests. This is due to an age-related slowdown in the excretion of cephalosporins.

In case of pathology of liver function, it is necessary to reduce the dosage used and monitor liver tests (ALAT, ASAT, thymol test, levels of total, direct and indirect bilirubin).

On our website you can get acquainted with most groups of antibiotics, complete lists of drugs included in them, classifications, history and other important information. For this purpose, a section “” has been created in the top menu of the site.

Cephalosporin antibiotics are highly effective drugs. They were discovered in the middle of the last century, but in recent years new means have been developed. There have been five generations of such antibiotics. The most common are cephalosporins in the form of tablets, which cope well with various infections and can be well tolerated even by small children. They are easy to use, and doctors quite often prescribe them for the treatment of infectious diseases.

History of the appearance of cephalosporins

In the 40s of the last century, the Italian scientist Brodzu, who studied the causative agents of typhus, discovered a fungus that had antibacterial activity. Was found to be quite effective against gram-positive and gram-negative bacteria. Later, these scientists isolated a substance from this fungus, called cephalosporin, on the basis of which antibacterial drugs were created, united in the group of cephalosporins. Due to their resistance to penicillinase, they began to be used in cases where penicillin was ineffective. The first cephalosporin antibiotic drug was Cephaloridin.

Today, there are already five generations of cephalosporins, which combine more than 50 drugs. In addition, semi-synthetic drugs have been created that are more stable and have a wide spectrum of action.

Effect of cephalosporin antibiotics

The antibacterial effect of cephalosporins is explained by their ability to destroy enzymes that form the basis of the bacterial cell membrane. They show their activity exclusively against microorganisms that grow and multiply.

First and second generation of drugs have shown their effectiveness against streptococcal and staphylococcal infections, but they were destroyed by the action of beta-lactamases, which are produced by gram-negative bacteria. The latest generations of cephalosporin antibiotics have proven to be more stable and are used for various infections, but they have shown to be ineffective against streptococci and staphylococci.

Classification

Cephalosporins divided into groups according to various criteria: effectiveness, spectrum of action, route of administration. But the most common classification is by generation. Let's take a closer look at the list of cephalosporin drugs and their purposes.

1st generation drugs

The most popular medicine is Cefazolin, which is used against staphylococci, streptococci and gonococci. It reaches the affected area via parenteral administration, and the highest concentration of the active substance is achieved if the drug is administered three times a day. The indication for the use of Cefazolin is the negative effect of staphylococci and streptococci on joints, soft tissues, skin, and bones.

It is necessary to pay attention to the fact that relatively recently this the drug was widely used for the treatment of a large number of infectious diseases. But with the advent of more modern 3rd and 4th generation medications, it was no longer prescribed for the treatment of intra-abdominal infections.

2nd generation drugs

2nd generation cephalosporin antibiotics are characterized by increased activity against gram-negative bacteria. Medicines such as Zinacef, Kimacef are active against:

Cefuroxime– a drug that is not active against Morganella, Pseudomonas aeruginosa, most anaerobic microorganisms and providences. As a result of parenteral administration, it penetrates into most tissues and organs, due to which the antibiotic is used in the treatment of inflammatory diseases of the meninges.

Ceclor suspension It is prescribed even to children, and it has a pleasant taste. The drug can be produced in the form of tablets, dry syrup and capsules.

2nd generation cephalosporin drugs are prescribed in the following cases:

exacerbation of otitis media and sinusitis;
treatment of postoperative conditions;
chronic bronchitis in the form of exacerbation, the occurrence of community-acquired pneumonia;
infection of bones, joints, skin.

3rd generation drugs

Initially, third generation cephalosporins were used in hospital settings for treatment of severe infectious diseases. Currently, such drugs are also used in outpatient clinics due to the increased resistance of pathogens to antibiotics. 3rd generation drugs are prescribed in the following cases:

Cefixime and Ceftibuten, intended for internal use, are used to treat gonorrhea, shigellosis, exacerbations of chronic bronchitis.

Cefatoxime, which is administered parenterally, helps in the following cases:

The drug is distinguished by a high degree of penetration into organs and tissues, including the blood-brain barrier. Cefatoxime can be used in the treatment of newborns if they develop meningitis, and it is combined with ampicillins.

4th generation drugs

Antibiotics of this group appeared quite recently. Such medicines are made only in the form of injections, since in this case they have a better effect on the body. 4th generation cephalosporins They are not produced in tablets, because these medications have a special molecular structure, which is why the active components are not able to penetrate the cellular structures of the intestinal mucosa.

4th generation drugs have increased resistance and show greater effectiveness against pathogenic infections such as enterococci, gram-positive cocci, Pseudomonas aeruginosa, and enterobacteria.

Parenteral antibiotics are prescribed for the treatment of:

One of the 4th generation drugs is Imipenem, but you should know that Pseudomonas aeruginosa can quickly develop resistance to this substance. This antibiotic is used for intramuscular and intravenous administration.

Next drug – Meronem, its characteristics are similar to Imipenem and has the following properties:

greater activity against gram-negative bacteria;
low activity against streptococcal infections and staphylococci;
does not have an anticonvulsant effect;
used for intravenous jet or drip infusion, but you should refrain from intramuscular administration.

Azactam drug has a bactericidal effect, but its use causes the development of the following adverse reactions:

the formation of thrombophlebitis and simply phlebitis;
jaundice, hepatitis;
dyspeptic disorders;
neurotoxicity reactions.

5th generation drugs

Fifth generation cephalosporins have a bactericidal effect, promoting the destruction of the walls of pathogens. Such antibiotics are active against microorganisms that have developed resistance to third-generation cephalosporins and drugs from the aminoglycoside group.

Zinforo - this drug is used for the treatment of community-acquired pneumonia, complicated infections of soft tissues and skin. Its adverse reactions are headache, diarrhea, itching, nausea. Patients with convulsive syndrome should take Zinforo with caution.

Zefter– such a medicine is produced in the form of a powder, from which a solution for infusion is prepared. It is prescribed for the treatment of appendages and complicated skin infections, as well as for infections of the diabetic foot. Before use, the powder should be dissolved in glucose solution, saline or water for injection.

5th generation drugs are active against Staphylococcus aureus and demonstrate a much wider range of pharmacological activity than previous generations of cephalosporin antibiotics.

Thus, cephalosporins are a fairly large group of antibacterial drugs used to treat diseases in adults and children. Medicines of this group are very popular due to their low toxicity, effectiveness and convenient form of administration. There are five generations of cephalosporins, each of which differs in its spectrum of action.

This group of cephalosporins exhibits antipseudomonal activity for the first time. According to the antibacterial spectrum against gram-positive microbes, they are weaker than the drugs of the first 2 generations.

Cefotaxime (claforan). The most famous antipseudomonal cephalosporin. In addition, it can be used to treat infections caused by gram-negative pathogens such as anaerobes. The drug is prescribed 1.0 g 2 times a day intramuscularly or intravenously.

Ceftriaxone. The properties of the drug are close to claforan. Has a prolonged effect. Prescribed 1.0 g 1 time per day intramuscularly or intravenously.

Moxalactam. Practically no different from 3rd generation drugs. Prescribe 1.0 g 2 times a day intramuscularly or intravenously.

Ceftizoxime. The drug is prescribed 0.5 g intramuscularly or intravenously. Available in bottles of 0.5 g.

Oral cephalosporins 3rd generation.

Drugs of this generation have improved pharmacological characteristics. Their half-life has increased, which allows them to be prescribed 1-2 times a day. The antibacterial spectrum has expanded. Resistance to the action of b-lactamases produced by gram-negative microorganisms, with the exception of Pseudomonas aeruginosa, has increased.

Cefpodaxime. Penetrates well into the lungs and bronchi. Excreted in urine and bile. The drug is prescribed for bronchitis and pneumonia caused by atypical flora, otitis media and sinusitis. The usual dose for adults is 0.1 -0.2 g, 2 times a day. Available in tablets of 0.1 and 0.2 g.

Cefixime (cefspan) It has a wide spectrum of bactericidal action on some types of gram-positive bacteria and a number of gram-negative microorganisms. Accumulates in blood serum, urine and bile.

The drug is prescribed 0.2 g 2 times a day or 0.4 g 1 time a day.

The course of treatment is 7-10 days. Available in tablets of 0.2 and 0.4 g; in the form of a suspension – 10 mg/5 ml.

Cefprozil (cefzil). Widely used in children's practice. The main indications for prescribing the drug are otitis media, sinusitis, diseases of the upper and lower respiratory tract.

Adults are prescribed 0.25-0.5 g 1 or 2 times a day, children - at the rate of 15 mg/kg body weight. Available in tablets of 0.25 and 0.5 g, as well as in the form of a suspension - 125 or 250 mg/5ml.

Ceftibuten (cedex). Has the ability to quickly penetrate body tissues. One of the most effective cephalosporins for the treatment of chronic otitis media in children and acute sinusitis in adults.

Adults are prescribed 0.4 g once a day, children – at a rate of 9 mg/kg

body weight once a day, but not more than 0.4 g per day.

Available in capsules of 0.4 g. 5 capsules per package, as well as in powder form (7.5 g in a bottle) for preparing a suspension.

1st generation of cephalosporins.

Their spectrum of action is very wide and greater than that of previous generations. They are equally highly active against both (+) and gram(-) bacteria. They are effective in the presence of bacterial resistance to cephalosporins of other generations. Highly resistant to β-lactamases. Secondary resistance to fourth-generation drugs develops slowly. All IV generation drugs are administered only parenterally (IV or IM).

These include cefepime, cefpirome (Keyten), cefclidine, cefquin, cefosprom.

The main drug of this generation is cefepime (maxipim). Used as a reserve antibiotic in the treatment of severe hospital infections of various locations.

Carbapenems.

There are 2 generations of carbapenems known. The first generation includes: imipenem, the second generation includes meropenem.

Bactericidal preparations. They have a pronounced post-antibiotic effect. Highly active antibiotics. These are the most active antibiotics against gram(+) bacteria and bacteroids and are highly active against gram(-) (second only to fluoroquinolones.

The spectrum of their antibacterial action is ultra-wide, the widest among all antibiotics. The spectrum of antibacterial action of carbapenems is equal to 4 antibacterial drugs (for example, 3rd generation cephalosporin, aminoglycoside, metronidazole and ampicillin).

Natural resistance to carbapenems in chlamydia, mycoplasmas, mycobacterium tuberculosis, fungi, protozoa and methicillin-resistant staphylococci.

Secondary (induced) resistance of microorganisms to carbapenems develops rarely and slowly. Unlike all other β-lactam antibiotics, they are not destroyed by β-lactamases. Carbapenems are administered only parenterally (IV or IM), and drugs intended for IV administration can only be administered IV. Drugs intended for intramuscular administration can only be administered intramuscularly.

Carbapenems cannot be used with other β-lactam antibiotics (cephalosporins, penicillins, monobactams) due to antagonism.

Carbapenems are low-toxic drugs with a wide range of therapeutic effects.

Indications for use. Carbapenems are reserve antibiotics for the treatment of severe infections in patients when other antibiotics are ineffective. They are used for the following infections:

1. Intra-abdominal infection. Moreover, they can be a replacement for dual antimicrobial therapy (aminoglycoside + metronidazole)

2. Obstetric and gynecological infection.

3. Severe infections in newborns.

4. Complicated urinary infections.

5. Hospital-acquired pneumonia and lower respiratory tract infections.

6. Sepsis.

7. Infections in patients with neutropenia.

8. Meningitis. In this case, the drug of choice is meropenem, as it penetrates better into the brain and has less neurotoxicity.

Monobactams.

The entire group is represented by one synthetic β-lactam antibiotic, aztreonam (azactam).

Has a bactericidal effect. The spectrum of action is narrow. The drug affects gram(-) bacteria, including Pseudomonas aeruginosa. The spectrum of antibacterial action resembles aminoglycosides, but does not have the toxic effects of the latter. Secondary resistance to azactam develops slowly and rarely. Penetrates well into tissues, excluding the brain.

Azactam is administered intramuscularly or intravenously.

It is excreted from the body unchanged by the kidneys. In case of renal failure, the dose is reduced. Azactam is a low-toxic drug.

Azactam may be an alternative to aminoglycosides, because its toxicity is significantly lower.

It is used for sepsis, peritonitis, severe brain infection.

Related information.