Gynecology

4th generation cephalosporins in tablets

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Oral cephalosporins are well absorbed in the gastrointestinal tract. Bioavailability depends on the specific drug and varies from 40-50% (cefixime) to 95% (cefalexin, cefadroxil, cefaclor). Cefaclor, cefixime, and ceftibuten may be slightly slower if you have food. Cefuroxime axetil during hydration is hydrolyzed to release active cefuroxime, and food contributes to this process. Parenteral cephalosporins are well absorbed after i / m administration.

Cephalosporins are distributed in many tissues, organs (except the prostate gland) and secrets. High concentrations are found in the lungs, kidneys, liver, muscles, skin, soft tissues, bones, synovial, pericardial, pleural, and peritoneal fluids. In bile, ceftriaxone and cefoperazone create the highest levels. Cephalosporins, especially cefuroxime and ceftazidime, penetrate well into the intraocular fluid, but do not create therapeutic levels in the posterior chamber of the eye.

The ability to overcome the BBB and create therapeutic concentrations in the CSF is most pronounced in 3rd generation cephalosporins - cefotaxime, ceftriaxone and ceftazidime, as well as cefepime, belonging to the 4th generation. Cefuroxime moderately passes through the BBB only with inflammation of the lining of the brain.

Most cephalosporins are practically not metabolized. The exception is cefotaxime, which is biotransformed to form an active metabolite. The drugs are mainly excreted by the kidneys, and very high concentrations are created in the urine. Ceftriaxone and cefoperazone have a double excretion route - by the kidneys and liver. The half-life of most cephalosporins varies between 1–2 hours. Cefixime, ceftibuten (3–4 hours) and ceftriaxone (up to 8.5 hours) have a longer half-life, which makes it possible to administer them once a day. In renal insufficiency, the dosing regimens of cephalosporins (except ceftriaxone and cefoperazone) require correction.

Warnings

Allergy. Cross to all cephalosporins. Allergies to first-generation cephalosporins may occur in 10% of patients with penicillin allergy. Cross-allergy to penicillins and cephalosporins II-III generation occurs much less frequently (1-3%). If there is a history of immediate-type allergic reactions (for example, urticaria, anaphylactic shock) to penicillins, then first-generation cephalosporins should be used with caution. Cephalosporins of other generations are safer.

Pregnancy. Cephalosporins are used during pregnancy without any restrictions, although there have been no adequate controlled studies of their safety for pregnant women and the fetus.

Lactation. Cephalosporins in low concentrations penetrate into breast milk. When used by nursing mothers, the intestinal microflora may change, the child's sensitization, skin rash, candidiasis. Be wary when using breastfeeding. Do not use cefixime and ceftibuten, due to the lack of appropriate clinical studies.

Pediatrics. In newborns, an increase in the half-life of cephalosporins is possible due to delayed renal excretion. Ceftriaxone, which has a high degree of binding to plasma proteins, can displace bilirubin from its association with proteins, so it should be used with caution in newborns with hyperbilirubinemia, especially in preterm.

Geriatrics. Due to changes in renal function in elderly people, the excretion of cephalosporins may slow down, which may require correction of the dosage regimen.

Impaired renal function. Due to the fact that most cephalosporins are excreted from the body by the kidneys mainly in the active state, the dosage regimens of these AMPs (except ceftriaxone and cefoperazone) for renal failure are subject to correction. When using cephalosporins in high doses, especially when combined with aminoglycosides or loop diuretics, a nephrotoxic effect is possible.

Liver dysfunction. A significant part of cefoperazone is excreted with bile, therefore, in severe liver diseases, its dose should be reduced. In patients with liver pathology, there is an increased risk of hypoprothrombinemia and bleeding when using cefoperazone, and vitamin K is recommended for prophylaxis.

Dentistry With prolonged use of cephalosporins may develop oral candidiasis.

Drug interactions

Antacids reduce the absorption of oral cephalosporins in the gastrointestinal tract. There should be at least 2 hours intervals between taking these medications.

When combined with cefoperazone anticoagulants and antiplatelet agents, the risk of bleeding increases, especially gastrointestinal. It is not recommended to combine cefoperazone with thrombolytics.

In the case of alcohol consumption during treatment with cefoperazone, a disulfiram-like reaction may develop.

The combination of cephalosporins with aminoglycosides and / or loop diuretics, especially in patients with impaired renal function, may increase the risk of nephrotoxicity.

Patient Information

Inside the cephalosporins, it is desirable to take, drinking plenty of water. Cefuroxime axetil must be taken with food, all other drugs - regardless of the meal (with the appearance of dyspeptic phenomena, we can take it during or after a meal).

Liquid dosage forms for ingestion should be prepared and taken in accordance with the attached instructions.

Strictly observe the prescribed mode of administration during the entire course of treatment, do not skip doses and take them at regular intervals. If you skip a dose, take it as soon as possible, do not take it, if it is almost time to take the next dose, do not double the dose. To withstand the duration of therapy, especially for streptococcal infections.

Consult a doctor if improvement does not occur within a few days or new symptoms appear. If a rash, hives or other signs of an allergic reaction appear, stop taking the medicine and consult a doctor.

Do not take antacids within 2 hours before and after taking the cephalosporin inside.

During treatment with cefoperazone and for two days after its completion, alcohol should be avoided.

General information

4th generation cephalosporins are considered relatively new. Oral forms in this group are absent. The remaining three are presented by means for oral administration and parenteral administration. Cephalosporins have high performance and relatively low toxicity. Because of this, they occupy one of the leading positions in the frequency of use in clinical practice of all antibacterial agents.

Indications for use for each generation of cephalosporins depend on their pharmacokinetic properties and antibacterial activity. Medicines have a structural similarity with penicillins. This predetermines a single mechanism of antimicrobial effects, as well as cross-allergy in a number of patients.

Activity spectrum

Cephalosporins have a bactericidal effect. It is associated with impaired formation of bacterial cell walls. In the series from the first to the third generation, there is a tendency to a significant expansion of the spectrum of action and an increase in the antimicrobial activity of gram-negative microbes with a slight decrease in the effect on gram-positive microorganisms. The common property of all means is the absence of a significant effect on enterococci and some other microbes.

Many patients are interested in why not release 4-generation cephalosporins in pills? The fact is that these medicines have a special molecular structure. This prevents the active ingredients from penetrating into the cell structures of the intestinal mucosa. Therefore, 4th generation cephalosporins in tablets are not available. All medicines of this group are intended for parenteral administration. 4th generation cephalosporins are produced in ampoules with a solvent.

4th generation cephalosporins

Preparations of this group are prescribed exclusively by specialists. This is a relatively new category of drugs. Cephalosporins 3, 4 generations have a similar range of effects. The difference is in fewer side effects in the second group. The tool "Cefepim", for example, is close to the third generation of medicines in a number of parameters. But due to some features in the chemical structure, it has the ability to penetrate through the outer wall of gram-negative microorganisms. At the same time, Cefepime is relatively resistant to hydrolysis with beta-lactamases (chromosomal) C-class. Therefore, besides the characteristics characteristic of cephalosporins of the 3rd generation (Ceftriaxone and Cefotaxime products), the drug exhibits such features as:

  • effect on hyperproducts microbes beta-lactamase (chromosomal) C-class,
  • high activity regarding non-fermenting microorganisms,
  • higher resistance to hydrolysis of beta-lactamase with a spread spectrum (the value of this feature is not completely clear).

Metabolism and excretion

Most cephalosporins do not decay. The exception is the drug "cefotaxime". It is biotransfected with the subsequent formation of the active product. Cephalosporins of the 4th generation are excreted, as well as representatives of the others, mainly by kidneys. When excreted in the urine are found quite high concentrations.

Medicines "Cefoperazon" and "Ceftriaxone" differ in a double way of excretion - the liver and kidneys. For most cephalosporins, the half-life is within one to two hours. A longer time is required for Ceftibuten, Cefixime (3-4 hours), and Ceftriaxone (up to 8.5 hours). This makes it possible to assign them once a day. Against the backdrop of renal insufficiency, the dosage of medication requires adjustment.

Side effects

Antibiotics - 4th generation cephalosporins - cause a number of negative consequences, in particular:

  • Allergy. Patients may have erythema multiforme, rash, urticaria, serum sickness, eosinophilia. Side effects of this category also include anaphylactic shock and fever, angioedema, bronchospasm.
  • Hematologic reactions. Among them, it is worth highlighting the positive Coombs test, leukopenia, eosinophilia (rarely), hemolytic anemia, and neutropenia.
  • Nervous disorders. At use of the increased doses at patients with renal dysfunction convulsions are noted.
  • On the part of the liver: increased transaminase activity.
  • Digestive disorders. Diarrhea, pseudomembranous colitis, vomiting and nausea, and pain in the abdomen are quite common among the negative consequences. In the event of liquid stool with blood fragments, the drug is canceled.
  • Local reactions. These include infiltration and pain in the area of ​​intramuscular injection and phlebitis with intravenous injection.
  • Other effects are expressed in the form of vaginal candidiasis and mouth.

Indications and contraindications

4th generation cephalosporins are prescribed for severe, low-level predominantly infections caused by multi-resistant microflora. These include empyema, abscess in the lung, pneumonia, sepsis, damage to the joints and bones. 4th generation cephalosporins are shown in infections of the complicated type in the urinary tract, against the background of neutropenia and other immunodeficiency states. Medicines are not prescribed for individual intolerance.

Precautionary measures

When applying marked cross-type allergies. Patients with penicillin intolerance have a similar response to first-generation cephalosporins. Cross-allergy when using the second or third category is less common (1-3% of cases). In the presence of a history of immediate-type reactions (for example, anaphylactic shock or urticaria), first-generation drugs are prescribed with caution. Preparations of the following categories (especially the fourth) are safer.

Lactation and pregnancy

Cephalosporins are prescribed in the prenatal period without special restrictions. However, adequate controlled drug safety studies have not been conducted. In low concentrations, cephalosporins can enter milk. Against the background of the use of the drug during lactation, changes in the intestinal microflora, candidiasis, skin rash, and child sensitization are likely.

Pediatrics and Geriatrics

When used in newborns, an increase in elimination half-life against the background of delayed renal excretion is likely. In elderly patients, a change in renal function is observed, and therefore a slowdown in the elimination of drugs is likely. This may require adjustments in the regimen and dosage regimen.

Renal dysfunction

Since most cephalosporins are eliminated through the kidney system, predominantly in active form, the dosage regimen must be adjusted to the specific features of the organism. When using high doses, especially in combination with loop diuretics or aminoglycosides, a nephrotoxic effect is likely to occur.

Liver dysfunction

Some drugs are excreted in the bile, and therefore the dosage should be reduced for patients with severe liver pathologies. In these patients, there is a high predisposition to bleeding and hypoprothrombinemia when using the drug "Cefoperazone". Vitamin K is recommended for prophylactic purposes.

What is the difference 4 generation cephalosporins?

Pathogenic agents synthesize beta-lactamase - an enzyme that protects the membrane membrane of their cells. The main objective of the antibiotic is the destruction of the cell, and the membrane membrane prevents this. 7-ACC destroys both types of beta-lactamase:

When beta-lactamase is destroyed, the cells cannot exist, the contents are released into the environment, are captured by phagocytes and removed from the body in the same way as any decomposition products.

All four generations of cephalosporins inhibit the synthesis of beta-lactamase, but only drugs 4 generations are directed to the chromosomal type of the enzyme. The instructions to Cefepim and Cefpiroma contain information that treatment during pregnancy should be carried out only if the likely benefit to the mother is greater than the potential threat to the development of the fetus. This means that only the attending physician can assess whether it is necessary to prescribe 4th generation cephalosporins, or to use less potent drugs. If treatment is required during lactation, there are 3 options for action:

  • suspend feeding
  • roll up the feeding and transfer the baby to artificial feeding,
  • choose another drug.

When is the medicine prescribed?

The impact of drugs of the 4th generation includes all infectious diseases, in the formation of which take part:

  • enterococci and enterobacteria,
  • staphylococci and streptococci,
  • meningococci and gonococci,
  • proteobacteria, including salmonella,
  • Helicobacter pylori.

These microorganisms cause more than 80% of all cases of infectious inflammatory processes.

A distinctive feature of gram-negative bacteria is the presence of additional protection on the cell wall.

With the breakdown of lipopolysaccharides, which are part of the membrane, toxic substances, endotoxins, are released. If a large number of pathogenic agents are simultaneously destroyed, endotoxins, entering the blood and lymphatic systems, cause the patient to:

  • headache, heaviness in the head,
  • weakness, muscle pain, aching joints,
  • nausea and vomiting
  • lack of appetite,
  • temperature increase to 38 ° C and more,
  • lowering blood pressure
  • in severe cases - delirium, confusion, shortness of breath, fainting,
  • Without medical care, death from toxic shock is possible.

When the immune system destroys gram-negative microorganisms, intoxication occurs with the decay products of their cellular structures, including endotoxins.

If treatment is started immediately, as diagnosed, intoxication has minimal effects on the body. When running cases, intoxication takes life-threatening forms. 4th generation cephalosporins can be used in combination with drugs that clean the circulatory system, with sorbents and diuretics.

Main indications for appointment

If a lab smear, scrape or blood test revealed one or more Gram-negative microorganisms, the attending physician selects antibiotics. Most often, cephalosporins are prescribed:

  1. For diseases of the genitourinary system: cystitis, urethritis, prostatitis, gonorrhea, epididymitis, salpingoophoritis, pyelonephritis and others.
  2. In diseases of the respiratory system: lung abscess, tracheitis and bronchitis, pneumonia, pleural empyema.
  3. With abscesses, carbuncles and furuncles of the skin, with wounds complicated by purulent inflammatory process.

Цефалоспорины иногда назначают пациентам со сниженными иммунным статусом, но в принятии такого решения врач учитывает потенциальную пользу и потенциальный вред для больного.

Contraindications

In order to reduce the harmful effects of cephalosporins on the gastrointestinal tract and increase the bioavailability of drugs, 4 generations of medicines have been created, which are administered parenterally:

Previous generations included oral cephalosporins, which increased the chance of side effects and reduced the bioavailability of 7-ACC. 4th generation cephalosporins also have contraindications, but they are much smaller than those of 1-2 generation tablets. There are restrictions on reception, you can not use:

  • during pregnancy and during breastfeeding,
  • newborns up to 2 months of age,
  • in chronic non-compensated kidney diseases,
  • with an individual allergic reaction.

The frequency of allergies to 7-ACA and other components of the drug, according to clinical trials, does not exceed 1%. Hypersensitivity patients have an increased chance of allergies:

  • 1-3 generations of cephalosporins, because 4-generation cephalosporins have a similar chemical composition,
  • to all antibiotics that also affect beta-lactamase and cause the release of endotoxin.

Studies have been conducted to study allergies to various groups of antibiotics. The findings suggest that 10% of all patients with penicillin allergy were also allergic to cephalosporins. In addition to the allergic reaction, an increased number of complications and side effects were noted. The use of Cefepime and Cefpiroma most often occurs in the hospital, so even if there are any complaints about side effects, doctors can immediately take steps to improve the patient's well-being. In some cases, for example, in case of complications of the kidneys, it is necessary to change the course of treatment and select another drug. The most likely (with a frequency of up to 1%) side effects:

  1. On the part of the digestive system: jaundice, hepatitis, vomiting and nausea, constipation or loose stools, pain in the epigastrium, belching, heartburn, flatulence, colic.
  2. In case of allergies: skin rash, urticaria, fever, sweating, shortness of breath.
  3. Since the cardiovascular system: angina, increased or slowed heart rate, raising or lowering the tone of blood vessels.
  4. On the part of the nervous system and psyche: psychomotor agitation, headache, insomnia, cramps and spasms of smooth muscles.
  5. On the part of the respiratory system: shortness of breath, cough.

Intravenous administration of 4th generation cephalosporins should be carried out in accordance with the professional standards of nursing. Otherwise, postinjection phlebitis is encountered.

4th generation tablet cephalosporins

Cephalosporins are referred to as beta-lactam drugs. They represent one of the largest classes of antibacterial drugs.

4th generation cephalosporins are considered relatively new. Oral forms in this group are absent. The remaining three are presented by means for oral administration and parenteral administration. Cephalosporins have high performance and relatively low toxicity. Because of this, they occupy one of the leading positions in the frequency of use in clinical practice of all antibacterial agents.

Indications for use for each generation of cephalosporins depend on their pharmacokinetic properties and antibacterial activity. Medicines have a structural similarity with penicillins. This predetermines a single mechanism of antimicrobial effects, as well as cross-allergy in a number of patients.

Cephalosporins have a bactericidal effect. It is associated with impaired formation of bacterial cell walls. In the series from the first to the third generation, there is a tendency to a significant expansion of the spectrum of action and an increase in the antimicrobial activity of gram-negative microbes with a slight decrease in the effect on gram-positive microorganisms. The common property of all means is the absence of a significant effect on enterococci and some other microbes.

Many patients are interested in why not release 4-generation cephalosporins in pills? The fact is that these medicines have a special molecular structure. This prevents the active ingredients from penetrating into the cell structures of the intestinal mucosa. Therefore, 4th generation cephalosporins in tablets are not available. All medicines of this group are intended for parenteral administration. 4th generation cephalosporins are produced in ampoules with a solvent.

Preparations of this group are prescribed exclusively by specialists. This is a relatively new category of drugs. Cephalosporins 3, 4 generations have a similar range of effects. The difference is in fewer side effects in the second group. Means "Cefepim", for example, in a number of parameters close to the third generation of drugs. But due to some features in the chemical structure, it has the ability to penetrate through the outer wall of gram-negative microorganisms. At the same time, Cefepime is relatively resistant to hydrolysis with beta-lactamases (chromosomal) C-class. Therefore, besides the characteristics characteristic of cephalosporins of the 3rd generation (Ceftriaxone and Cefotaxime products), the drug exhibits such features as:

  • effect on hyperproducts microbes beta-lactamase (chromosomal) C-class,
  • high activity regarding non-fermenting microorganisms,
  • higher resistance to hydrolysis of beta-lactamase with a spread spectrum (the value of this feature is not completely clear).

This group includes one drug, Cefoperazone / Sulbactam. Compared with mono-agent, the combined drug has an expanded spectrum of activity. It affects anaerobic microorganisms, most enterobacteria strains capable of producing beta-lactamase.

Parenteral cephalosporins 3, 4 generations are very well absorbed when injected into a muscle. Medicines for oral administration are characterized by high absorption in the gastrointestinal tract. Bioavailability will depend on the particular medication. It ranges from 40–50% (for Cefixime, for example) to 95% (for Cefaclor, Cefadroxil, Cefalexin). Certain oral medications may be slowed by food intake. But such a drug as "Cefuroxime asceticus" during the absorption undergoes hydrolysis. Faster release of the active ingredient in this contributes to food.

4th generation cephalosporins are well distributed in many tissues and organs (except the prostate), as well as secrets. In high concentrations, medications are found in peritoneal and synovial, pericardial and pleural fluids, bones and skin, soft tissues, liver, muscles, kidneys and lungs. The ability to undergo the BBB and form therapeutic concentrations in the cerebrospinal fluid is more pronounced in third-generation drugs such as Ceftazidime, Ceftriaxone, as well as Cefotaxime, and a representative of the fourth, Cefepime.

Most cephalosporins do not decay. An exception is the drug "Cefotaxime". It is biotransfected with the subsequent formation of the active product. Cephalosporins of the 4th generation, as well as representatives of the others, are excreted mainly by the kidneys. When excreted in the urine are found quite high concentrations.

Medications "Cefoperazone" and "Ceftriaxone" differ in a double way of excretion - the liver and kidneys. For most cephalosporins, the half-life is within one to two hours. A longer time is required for Ceftibuten, Cefixime (3-4 hours), and Ceftriaxone (up to 8.5 hours). This makes it possible to assign them once a day. Against the backdrop of renal insufficiency, the dosage of medication requires adjustment.

Antibiotics - 4th generation cephalosporins - cause a number of negative consequences, in particular:

  • Allergy. Patients may have erythema multiforme, rash, urticaria, serum sickness, eosinophilia. Side effects of this category also include anaphylactic shock and fever, angioedema, bronchospasm.
  • Hematologic reactions. Among them, it is worth highlighting the positive Coombs test, leukopenia, eosinophilia (rarely), hemolytic anemia, and neutropenia.
  • Nervous disorders. At use of the increased doses at patients with renal dysfunction convulsions are noted.
  • On the part of the liver: increased transaminase activity.
  • Digestive disorders. Diarrhea, pseudomembranous colitis, vomiting and nausea, and pain in the abdomen are quite common among the negative consequences. In the event of liquid stool with blood fragments, the drug is canceled.
  • Local reactions. These include infiltration and pain in the area of ​​intramuscular injection and phlebitis with intravenous injection.
  • Other effects are expressed in the form of vaginal candidiasis and mouth.

4th generation cephalosporins are prescribed for severe, low-level predominantly infections caused by multi-resistant microflora. These include empyema, abscess in the lung, pneumonia, sepsis, damage to the joints and bones. 4th generation cephalosporins are shown in infections of the complicated type in the urinary tract, against the background of neutropenia and other immunodeficiency states. Medicines are not prescribed for individual intolerance.

When applying marked cross-type allergies. Patients with penicillin intolerance have a similar response to first-generation cephalosporins. Cross-allergy when using the second or third category is less common (1-3% of cases). In the presence of a history of immediate-type reactions (for example, anaphylactic shock or urticaria), first-generation drugs are prescribed with caution. Preparations of the following categories (especially the fourth) are safer.

Cephalosporins are prescribed in the prenatal period without special restrictions. However, adequate controlled drug safety studies have not been conducted. In low concentrations, cephalosporins can enter milk. Against the background of the use of the drug during lactation, changes in the intestinal microflora, candidiasis, skin rash, and child sensitization are likely.

When used in newborns, an increase in elimination half-life against the background of delayed renal excretion is likely. In elderly patients, a change in renal function is observed, and therefore a slowdown in the elimination of drugs is likely. This may require adjustments in the regimen and dosage regimen.

Since most cephalosporins are eliminated through the kidney system, predominantly in active form, the dosage regimen must be adjusted to the specific features of the organism. When using high doses, especially in combination with loop diuretics or aminoglycosides, a nephrotoxic effect is likely to occur.

Some drugs are excreted in the bile, and therefore the dosage should be reduced for patients with severe liver pathologies. In such patients, there is a high predisposition to bleeding and hypoprothrombinemia when using the drug "Cefoperazone". Vitamin K is recommended for prophylactic purposes.

Cephalosporins in tablets belong to the group of antibiotic drugs. Submitted drugs are used mainly to combat diseases that are bacterial in nature. Let us consider in more detail the pharmacological effects, indications and features of the use of this type of medication.

Cephalosporins are antibiotic drugs with a high degree of effectiveness. These drugs were discovered in the middle of the 20th century. To date, there are 5 generations of cephalosporins. At the same time, antibiotics of the 3rd generation are very popular.

The pharmacological effect of these drugs lies in the ability of their main active ingredients to damage bacterial cell membranes, which leads to the death of pathogens.

Cephalosporins (especially 4 generations) are extremely effective in combating infectious diseases, the emergence and development of which is associated with the pathological activity of so-called gram-negative bacteria.

4th generation cephalosporins give positive results even in those cases when antibiotic drugs belonging to the penicillin group turned out to be completely ineffective.

Cephalosporins in pill form are prescribed to patients suffering from certain infectious diseases of a bacterial nature, and also as a means of preventing the development of infectious complications during surgical intervention. Experts identify the following indications for use of the preparations presented:

  1. Cystitis.
  2. Furunculosis.
  3. Urethritis.
  4. Otitis media
  5. Gonorrhea.
  6. Bronchitis in acute or chronic form.
  7. Pyelonephritis.
  8. Angina streptococcal.
  9. Sinusitis.
  10. Shigellosis.
  11. Infectious lesions of the upper respiratory tract.

It is worth noting that the spectrum of action and scope of cephalosporins largely depend on the generation to which the antibiotic drug belongs. Consider this question in more detail:

  1. 1st generation cephalosporins are used to combat uncomplicated infections affecting the skin, bones and joints.
  2. Indications for the use of 2nd generation cephalosporins are diseases such as tonsillitis, pneumonia, chronic bronchitis, pharyngitis, lesions of the urinary tract, which are bacterial in nature.
  3. 3rd generation cephalosporins are prescribed for diseases such as bronchitis, infections of the urinary system, shigellosis, gonorrhea, impetigo, Lyme disease.
  4. 4th generation cephalosporins can be indicated for sepsis, joint damage, pulmonary abscesses, pneumonia, pleural empyema. It is worth emphasizing that the group of 4th generation cephalosporin preparations is not available in the form of tablets due to its specific molecular structure.

These antibiotic drugs are contraindicated only in the case of individual sensitivity and allergic reactions to the main active ingredient - cephalosporin, as well as in patients younger than 3 years.

In some cases, the use of cephalosporins may develop side effects. The most common adverse reactions include the following:

  1. Nausea.
  2. Attacks of vomiting.
  3. Diarrhea.
  4. Stomach upset.
  5. Headaches that are similar in nature with manifestations of migraine.
  6. Allergic reactions.
  7. Pain in the abdomen.
  8. Disturbances in the functioning of the kidneys.
  9. Hepatic disorders.
  10. Dysbacteriosis.
  11. Dizziness.
  12. Urticaria and the appearance of a rash on the skin.
  13. Blood clotting disorder.
  14. Eosinophilia.
  15. Leukopenia

In most cases, the occurrence of the above side effects associated with prolonged and uncontrolled reception of cephalosporins.

The choice of the drug, the determination of the dosage and duration of the therapeutic course should be made exclusively by the attending physician, taking into account the diagnosis, the severity of the disease, the age and the general health of the patient. In addition, in order to avoid the occurrence of adverse reactions, it is necessary to strictly follow the instructions for use of the drug and take drugs that prevent the development of dysbiosis.

Cephalosporins in the form of tablets are in particular demand and popularity. The fact is that this form of antibiotic drugs has certain advantages. These factors include the following factors:

Preparations of cephalosporins tablets in adult patients prescribed by a doctor in the appropriate dosage. The duration of the therapeutic course is from a week to 10 days, depending on the severity of the disease. Pediatric patients receive medication 2-3 times a day, the dosage is calculated individually, taking into account the weight of the child.

Cephalosporins are recommended to be used after meals, which contributes to their better absorption by the body. In addition, according to the instructions for use, together with the drugs of the presented group, it is necessary to take medicines of antifungal nature and means that prevent the development of dysbacteriosis.

An appropriate summary is attached to each specific drug, which must be carefully studied before starting the course of treatment and then strictly follow the instructions provided in the instructions.

There are various tablets of cephalosporins, each of which has certain features and clinical properties. Consider them in more detail:

  1. Cephalexin belongs to the 1st generation cephalosporin group. Submitted drug is highly effective in the fight against streptococci and staphylococci. Cephalexin is prescribed for infectious and inflammatory diseases. Side effects include the possible development of allergic reactions in case of intolerance to penicillin.
  2. Cefixime belongs to the 3rd generation cephalosporins. Данное лекарственное средство обладает ярко выраженным антибактериальным эффектом, подавляя деятельность практически всех известных болезнетворных микроорганизмов. Цефиксим характеризуется наличием фармакокинетических свойств, хорошим проникновением в ткани.The drug has a high degree of effectiveness in the fight against Pseudomonas aeruginosa, enterobacteria.
  3. Ceftibuten. The drug belongs to the 3rd generation cephalosporins. The drug is available in the form of tablets and suspensions. Ceftibuten is characterized by a high degree of resistance to the effects of specific substances secreted for protective purposes by pathogens.
  4. Cefuroxime acetyl belongs to the 2nd generation cephalosporins group. The presented drug is very effective in the fight against pathogens such as enterobacteria, moraxella and hemophilus. Cefuroxime acetyl is taken several times a day. The dosage is determined depending on the form and severity of the disease, the age category of the patient. With long-term administration, side effects such as diarrhea, nausea, vomiting, and changes in the clinical picture of the blood may occur.
  5. Zinnat is one of the most common drugs belonging to the 2nd generation cephalosporins group. This drug is used to treat furunculosis, pyelonephritis, pneumonia, infections of the upper and lower respiratory tract and other diseases caused by the pathological activity of pathogenic microorganisms that are susceptible to cefuroxime.

Cephalosporins are highly effective and effective antibiotic drugs used in the field of modern medicine to combat infectious diseases. Tablets form of medicines enjoys a particularly widespread, characterized by a minimum range of contraindications and side effects.

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

General characteristics of cephalosporins

Cephalosporins have the following characteristics:

  • contribute to the bactericidal action,
  • have a wide range of therapeutic effects,
  • approximately 7-11% cause the development of cross-allergy. At risk are patients with penicillin intolerance,
  • drugs do not contribute to the impact against enterococci and listeria.

Reception of drugs of this group can be carried out only for the purpose and under the supervision of a doctor. Antibiotics are not intended for self-medication.

The use of cephalosporins drugs may contribute to the following undesirable side reactions:

  • allergic reactions
  • dyspeptic disorders
  • phlebitis,
  • hematological reactions.

Cephalosporins are usually classified by generations. The list of drugs by generations and dosage forms:

Cephalosporins and their effects

Cephalosporins are a large class of beta-lactam antibiotics based on 7-aminocephalosporanic acid. For the first time the drug of this group was created in 1948 and tested on the causative agent of typhoid.

Cephalosporins are well combined with a number of other antibiotics, so a number of complex drugs are now being produced. Forms of release of medicines of this group are various - solution for injections, powders, tablets, suspensions. Oral forms are the most popular among patients.

The classification by generation is:

Despite the great resistance of the latest generations of drugs to the destructive action of bacterial enzymes, the third generation have the highest popularity.

The means of the first generation are still widely used in therapy, but are gradually being supplanted by modern cephalosporins.

How do cephalosporins of 3.4 generations work? Their bactericidal activity is based on the suppression of the synthesis of bacterial cell walls. Drugs from any list are resistant to the influence of enzymes (beta-lactamase) bacteria - gram-negative, gram-positive.

Pharmaceuticals act on almost all the most common microbes - staphylococci, enterococci, streptococci, morganella, borrelia, clostridium, and many others. Resistance to cephalosporins is shown only by streptococci of group D, some enterococci. These bacteria do not secrete plasmid, but chromosomal lactamases, which destroy the drug molecules.

Basic indications for use

Indications for which drugs of any generation are prescribed are the same. In children, remedies are most often recommended for serious infections of the upper respiratory tract, the respiratory tract, which develop rapidly or threaten with various complications.

The most common indication of cephalosporins is bronchitis or pneumonia.

If with angina (acute tonsillitis), penicillin antibiotics are much more often recommended, then in case of acute purulent otitis, cephalosporins are prescribed for children. The same drugs are often prescribed in pill form or injections for purulent sinus in parallel with surgical treatment. Among intestinal infections in children and adults, cephalosporins are treated with:

Severe inflammatory-infectious diseases of the gastrointestinal tract, the abdominal cavity are also treated with these tools. The indications include peritonitis, cholangitis, complicated forms of appendicitis, gastroenteritis. From pulmonary pathologies, indications are abscess, pleural empyema. During the course they inject drugs for purulent wounds, soft tissue infections, kidney damage, bladder, septic meningitis, borreliosis. Cephalosporins are a popular destination after prophylactic operations.

Third generation drugs - list

There are a large number of drugs in this group. One of the most popular is ceftriaxone and medications based on this active ingredient:

The cost of one vial of Ceftriaxone does not exceed 25 rubles, while the imported analogues are much higher - 250-500 rubles per dose. The drug is administered at 0.5-2 g times / day intramuscularly, intravenously. Also known pharmaceutical agents of cephalosporins of the 3rd generation are Cefixime and Suprax. The last mentioned medicine is sold in the form of a suspension (700 rubles per bottle) and can be used in children from birth. At the age of 6 months, therapy is carried out under the supervision of a physician. Suprax is also produced in the form of water-soluble tablets, which are absorbed faster and are less irritating to the gastrointestinal tract. The list of other 3rd generation drugs is as follows:

  • Spectracef with cefditoren (1000-1400 rubles),
  • Pancef, Ixim Lupine with cefixime (700-1200 rubles),
  • Fortum, Ceftazidim with ceftadizim (500-900 rubles).

For kidney disease (with pyelonephritis), an antibiotic 3 generations of cefotaxime cephalosporins is often administered in the hospital. The same drug perfectly helps with gonorrhea, chlamydia, female diseases - adnexitis, endometritis. Cefuroxime in injections or tablets is most popular for abdominal infections, well helps against bacterial heart disease.

Fourth generation drugs

The 4th generation list of cephalosporins is not as extensive as their predecessors. A distinctive feature of these products is higher efficacy against bacteria that produce beta-lactamase. For example, the antibiotic in solution Cefepime belongs to the 4th generation and is resistant even to a number of chromosomal beta-lactamases. The drug is prescribed for pyelonephritis, bronchitis, pneumonia, gynecological infections, with neutropenic fever.

The cost of Cefepime is 140 rubles / 1 dose. Typically, the drug is administered at 1 g / time per day, with severe infections - 1 g / twice per day. In children, an individual dose is prescribed at the rate of 50 mg / kg of weight. The course of therapy is 7-10 days, in serious cases - up to 20 days. Other drugs are also produced based on the active substance cefepime:

  • Cefomax (160 rubles / dose),
  • Maxipim (380 rubles / dose).

The second drug of the 4th generation is Cefpyr. It has similar indications, it can be used for infections caused by bacteria emitting beta-lactamase. The drug destroys rare infections caused by bacterial associations. In pharmacies, it is rare, a medicine based on it, Cefanorm costs about 680 rubles.

Cephalosporins for children and pregnant women

During pregnancy, almost all cephalosporins of 3-4 generations are allowed. The exception is 1 trimester - during this period the development of the fetus occurs, and any drug can affect it negatively. Therefore, in the first trimester, according to the strictest indications, the following medicines are prescribed:

Children, if not shown the introduction of drugs in the injections, prescribed oral forms - suspensions. Perhaps the initial introduction of drugs in the injections for 3-5 days with the subsequent transition to the form of a suspension. Most often appointed Supraks, Zinnat, Pancef, Cephalexin. The price of drugs is 400-1000 rubles. Some of them are not recommended until 6 months of age in oral form, but can be administered to newborns and infants as injections.

Cephalosporins preparations of the 1st and 4th generation

The main difference between the drugs in question and their predecessors is that 4th generation cephalosporins act on more microorganisms, both gram-positive and gram-negative. In addition, they are effective against cocci, sticks and germ bacteria that are completely resistant to antibiotics of the 3rd generation.

Due to the listed features and benefits, cephalosporins of the described type are used in complex chemical therapy of acute and chronic inflammatory diseases of the skin, digestive, urinary system, pelvic organs, joints and bones.

Despite the relative safety of these antibiotics, they produce many side effects, among which are often observed allergic reactions, digestive disorders, reduced activity of the immune system. Therefore, 4th generation cephalosporins are rarely prescribed to women with hormonal disorders, including pregnant women, with dysbacteriosis, irritable bowel syndrome, autoimmune problems. Acceptance of the described antibiotic drugs can only aggravate the course of disease.

List of 4th generation cephalosporins

To date, there are about 10 varieties of these drugs, but most of them are still in the research stage, and only 2 types have been approved for mass production: cefpirome and cefepime. These antibiotics are active active substances in many names of medicines.

Names of cephalosporins 4th generation:

  • Izodepom
  • Kefsepim,
  • Maxipim,
  • Cefanorm,
  • Ladef,
  • Movizar,
  • Cefepime,
  • Maxicef
  • Cefomax,
  • Chaining
  • Cefepim Alkem,
  • Cefepim Jodas,
  • Cefepim Agio,
  • Efipim.

It should be noted that the 4th generation cephalosporin antibiotics are produced in ampoules with a solvent, supplied with a powder for the preparation of a medicinal suspension. The fact is that the drugs act only when administered intramuscularly, as much as possible absorbed into the blood and lymph. 4th generation cephalosporins are not produced in tablets, because their molecular structure does not allow active substances to penetrate into the cellular structures of the intestinal mucosa and the digestive tract, antibiotics are destroyed even when they enter the stomach due to high acidity of the stomach.

An important achievement in the production of the examined cephalosporins is that they can be stored for a long time even after dilution of the powder with a solvent. The resulting liquid sometimes darkens due to contact with air and ultraviolet radiation, but does not lose its therapeutic properties.

For a pronounced and sustained outcome of treatment, it is important to follow the correct regimen - enter the suspension every 12 hours (intramuscularly), preferably at the same specific time. You should also not exceed the recommended course duration, which usually ranges from 7 to 10 days. Otherwise, the organism may be intoxicated with antibiotics, hepatological lesions of the liver and kidney pathology.

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