What are cephalosporins and how do they work. Which generations of cephalosporins exist and what are their primary uses. How do cephalosporins differ from penicillins and what precautions should be taken when using them.

Understanding Cephalosporins: A Powerful Class of Antibiotics

Cephalosporins represent a significant group of beta-lactam antibiotics widely utilized in modern medicine. These drugs play a crucial role in combating various bacterial infections, offering healthcare providers a versatile arsenal against pathogens. Their development spans several decades, resulting in five distinct generations, each with unique characteristics and applications.

What exactly are cephalosporins?

Cephalosporins are antibiotics that belong to the beta-lactam family, sharing structural similarities with penicillins. They work by interfering with bacterial cell wall synthesis, ultimately leading to the destruction of the invading microorganisms. This mechanism of action makes them effective against a broad spectrum of bacteria, both gram-positive and gram-negative.

The Five Generations of Cephalosporins: Evolution in Antibiotic Therapy

The development of cephalosporins has progressed through five generations, each building upon the strengths of its predecessors while addressing emerging bacterial resistance patterns.

First-Generation Cephalosporins

First-generation cephalosporins, such as cefazolin and cephalexin, are primarily effective against gram-positive bacteria. They are commonly employed in treating skin and soft tissue infections, as well as certain respiratory, urinary, and bone infections. Their reliability and relative safety make them a go-to choice for many uncomplicated bacterial infections.

Second-Generation Cephalosporins

The second generation, including cefuroxime and cefoxitin, offers an expanded spectrum of activity against gram-negative bacteria while maintaining effectiveness against gram-positive organisms. These drugs are often prescribed for respiratory tract infections, urinary tract infections (UTIs), and Lyme disease. Other members of this generation, like cefaclor and cefprozil, are frequently used to treat sinus, lung, and ear infections.

Third-Generation Cephalosporins

Third-generation cephalosporins, such as ceftriaxone and ceftazidime, represent a significant advancement in the treatment of serious infections. These drugs exhibit enhanced activity against gram-negative bacteria and are capable of crossing the blood-brain barrier, making them valuable in treating meningitis and sepsis. Additionally, ceftriaxone has found use in treating gonorrhea and Lyme disease.

Fourth-Generation Cephalosporins

The fourth generation is represented by cefepime, which demonstrates broad-spectrum activity against both gram-positive and gram-negative bacteria. It is particularly useful in treating staphylococcal infections and has become an important tool in combating resistant strains of bacteria.

Fifth-Generation Cephalosporins

The latest addition to the cephalosporin family is the fifth generation, with ceftaroline as its primary representative. This drug was developed to address the growing concern of methicillin-resistant Staphylococcus aureus (MRSA) infections and has also shown efficacy in treating community-acquired pneumonia.

Clinical Applications: When and How Cephalosporins Are Used

Cephalosporins find application in a wide range of clinical scenarios, from common community-acquired infections to life-threatening hospital-associated pathogens.

• Skin and soft tissue infections
• Respiratory tract infections
• Urinary tract infections
• Bone and joint infections
• Meningitis
• Sepsis
• Surgical prophylaxis

The choice of cephalosporin depends on various factors, including the suspected pathogen, local resistance patterns, and patient-specific considerations such as allergies and kidney function.

Cephalosporins vs. Penicillins: Understanding the Relationship

While cephalosporins and penicillins share structural similarities, they are distinct classes of antibiotics. Both belong to the beta-lactam family, but cephalosporins offer several advantages in certain clinical situations.

Are cephalosporins safe for penicillin-allergic patients?

The cross-reactivity between cephalosporins and penicillins is a topic of ongoing research and clinical concern. Patients with a history of penicillin allergy may still be able to tolerate cephalosporins, particularly those of later generations. However, caution is warranted, especially with first- and second-generation cephalosporins, which have a higher likelihood of cross-reactivity.

For individuals with a severe penicillin allergy, including a history of anaphylaxis, the use of cephalosporins should be carefully evaluated by a healthcare provider. In some cases, skin testing or graded challenges may be necessary to determine the safety of cephalosporin administration.

Safety Considerations and Potential Side Effects

Like all medications, cephalosporins come with potential risks and side effects that patients and healthcare providers should be aware of.

Common side effects of cephalosporins

• Gastrointestinal disturbances (nausea, diarrhea)
• Skin rashes
• Headache
• Dizziness
• Candidiasis (yeast infection)

Serious but rare side effects

• Anaphylaxis
• Severe skin reactions (Stevens-Johnson syndrome)
• Clostridium difficile-associated diarrhea
• Blood disorders
• Kidney damage

Patients should be counseled to report any unusual symptoms to their healthcare provider promptly. Additionally, it’s crucial to complete the entire prescribed course of antibiotics, even if symptoms improve, to prevent the development of antibiotic-resistant bacteria.

Special Precautions and Contraindications

Certain patient populations require special consideration when prescribing cephalosporins:

Newborns and ceftriaxone

The use of ceftriaxone in newborns, particularly those with jaundice, requires careful evaluation due to the potential risk of kernicterus. Alternative antibiotics may be preferable in this population.

Patients with renal impairment

Cephalosporins are primarily excreted by the kidneys. Patients with impaired renal function may require dose adjustments to prevent drug accumulation and potential toxicity. Regular monitoring of kidney function is essential during cephalosporin therapy.

History of seizures

Some cephalosporins, particularly cefepime, have been associated with an increased risk of seizures, especially in patients with pre-existing seizure disorders or renal impairment. Close monitoring and possible dose adjustments may be necessary for these individuals.

The Future of Cephalosporins: Combating Antibiotic Resistance

As antibiotic resistance continues to pose a global health threat, the development of new cephalosporins and novel combinations with other antibiotics remains an active area of research. These efforts aim to address emerging resistant pathogens and preserve the effectiveness of this important class of antibiotics.

Combination therapies

Researchers are exploring combinations of cephalosporins with beta-lactamase inhibitors to overcome certain resistance mechanisms. These hybrid drugs show promise in treating infections caused by multi-drug resistant organisms.

New generation development

The potential for a sixth generation of cephalosporins is being investigated, with a focus on creating drugs with even broader spectrums of activity and improved stability against bacterial resistance mechanisms.

As we continue to rely on cephalosporins in clinical practice, it’s crucial to use them judiciously and in accordance with antimicrobial stewardship principles. This approach will help preserve their effectiveness for future generations and contribute to the global effort to combat antibiotic resistance.

What are Cephalosporins? Uses, Warnings, Side Effects, and More

Common Questions & Answers

What drugs are cephalosporins?

Cephalosporins are a large group of beta-lactam antibiotics. These drugs are used to treat a wide variety of bacterial infections. There are five generations of cephalosporins, grouped according to their range of coverage against bacteria and when the drugs were developed.

What are examples of cephalosporins?

Examples of cephalosporins include first-generation drugs cefazolin and cephalexin; second-generation drugs cefuroxime and cefoxitin; third-generation drugs ceftriaxone and ceftazidime; fourth-generation drug cefepime; and fifth-generation drug ceftaroline.

Is a cephalosporin a penicillin?

Cephalosporins are similar to penicillins on a molecular level, and as a result, they might lead to an allergic reaction in people who are allergic to penicillins. If your penicillin allergy is not severe, you may still be able to take cephalosporins, but probably not first- or second-generation drugs.

What are the most common cephalosporins?

The first-generation cephalosporins (such as cefazolin and cephalexin) are commonly used to treat skin and soft tissue infections. Second-generation cephalosporins, including cefaclor, cefprozil, loracarbef, and cefpodoxime, are commonly used to treat sinus, lung, and ear infections.

What are the five generations of cephalosporins?

First and second generation cephalosporins (such as cefazolin and cefuroxime) treat skin and soft tissue infections. Cefuroxime also treats respiratory infections and UTIs. Third-generation cephalosporins (ceftriaxone and ceftazidime) are typically for serious infections. Fourth-generation cefepime treats staphylococcal infections. Fifth-generation ceftaroline is effective against MRSA and pneumonia.

Because of their long history of development, there are numerous cephalosporins on the market. According to the Nelson Textbook of Pediatrics, the five generations of cephalosporins break down as follows:

• First-generation cephalosporins are commonly used to treat skin and soft tissue infections. Examples include cefazolin and cephalexin. Doctors also use these drugs to treat bone, respiratory, urinary, genital, biliary tract, ear, and bloodstream infections, per StatPearls.
• Second-generation cephalosporins are used to treat respiratory tract infections, UTIs, skin and soft tissue infections, and Lyme disease. Examples include cefuroxime and cefoxitin. Other second-generation cephalosporins (cefaclor, cefprozil, loracarbef, cefpodoxime) are commonly used to treat sinus, lung, and ear infections.
• Third-generation cephalosporins are typically used for serious infections, including meningitis and sepsis. Examples include ceftriaxone and ceftazidime. Ceftriaxone is also used to treat gonorrhea and Lyme disease, per StatPearls.
• A fourth-generation cephalosporin called cefepime is used to treat staphylococcal infections.
• A fifth-generation cephalosporin called ceftaroline is effective against MRSA (methicillin-resistant Staphylococcus aureus) and community-acquired pneumonia.

Precautions and Warnings

People who are allergic to cephalosporins, or any inactive ingredients found in these drugs, shouldn’t take them.

Cephalosporins share a molecular similarity with penicillins, and so might lead to an allergic reaction in people who are allergic to penicillins. Depending on the severity of your penicillin allergy, you may still be able to take cephalosporins, but most likely not first- or second-generation drugs, notes StatPearls.

You should also avoid cephalosporins if you’ve had an anaphylactic reaction to other beta-lactams.

The third-generation cephalosporin ceftriaxone is contraindicated in some newborns, because it could increase the risk of jaundice.

Make sure your doctor or pharmacist is monitoring your kidney function when you are taking cephalosporins, because that could potentially warrant a change in the dose or dosing frequency of your medication.

An overdose of the fourth-generation cephalosporin cefepime can lead to seizures and encephalopathy (brain disease). If you have a history of seizures, especially with poor kidney function, use caution when taking cephalosporins.

As with all antibiotics, it’s important that you finish the entire course you were prescribed — even if you feel better. This is the only way to ensure that the infection is completely gone. Otherwise, the infection could return and be much more difficult to treat the second time around.

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List of Cephalosporins + Uses, Types & Side Effects

Cephalosporins are a large group of antibiotics derived from the mold Acremonium (previously called Cephalosporium). Cephalosporins are bactericidal (kill bacteria) and work in a similar way to penicillins. They bind to and block the activity of enzymes responsible for making peptidoglycan, an important component of the bacterial cell wall. They are called broad-spectrum antibiotics because they are effective against a wide range of bacteria.

After the first cephalosporin was discovered in 1945, scientists improved the structure of cephalosporins to make them more effective against a wider range of bacteria. Each time the structure changed, a new “generation” of cephalosporins were made. There are five generations of cephalosporins. Most cephalosporins start with cef, ceph, or kef. Note that this classification system is not used consistently from country to country.

What are cephalosporins used for?

Cephalosporins may be used to treat infections caused by susceptible bacteria, such as:

• Bone infections
• Ear infections (eg, otitis media)
• Skin infections
• Upper respiratory tract infections
• Urinary tract infections.

What are the differences between cephalosporins?

There are five “generations” of cephalosporins, with each generation differing slightly in their antibacterial spectrum (ie, how effective they are at killing certain types of bacteria). Within each generation, there are differences in terms of administration (such as oral or intravenous administration), absorption, excretion, and how long the activity of the cephalosporin lasts in the body.

First generation cephalosporins

First generation cephalosporins refer to the first group of cephalosporins discovered. Their optimum activity is against gram-positive bacteria such as staphylococci and streptococci. They have little activity against gram-negative bacteria.

Cephalexin and cefadroxil can be given by mouth, whereas cefazolin can only be given by injection (IV/IM). There are also differences with regards to how frequently the different first-generation cephalosporins need to be dosed.

Second generation cephalosporins

Second-generation cephalosporins are more active against gram-negative bacteria, with less activity against gram-positive bacteria.

Third generation cephalosporins

Third generation cephalosporins followed the second-generation cephalosporins. No single third-generation cephalosporin treats all infectious disease scenarios.

Cefotaxime and ceftizoxime (discontinued) offer the best gram-positive coverage out of all the third-generation agents; ceftazidime and cefoperazone (discontinued) are unique in that they provide antipseudomonal coverage.

Ceftriaxone has a long half-life which allows for once daily dosing and may be used for the treatment of gonorrhea, pelvic inflammatory disease, and epididymo-orchitis. It is also an alternative to penicillins for suspected meningitis.

All the third-generation cephalosporins except for cefoperazone (discontinued) penetrate cerebrospinal fluid.

Fourth generation cephalosporins

Fourth generation cephalosporins are structurally related to third-generation cephalosporins but possess an extra ammonium group, which allows them to rapidly penetrate through the outer membrane of gram-negative bacteria, enhancing their activity. They are also active against β-lactamase producing Enterobacteriaceae which may inactivate third-generation cephalosporins.

Some fourth-generation cephalosporins have excellent activity against gram-positive bacteria such as methicillin-susceptible staphylococci, penicillin-resistant pneumococci, and viridans group streptococci.

Cefepime is the only fourth generation cephalosporin available in the United States. Cefpirome is available overseas.

Next (fifth) generation cephalosporins

Ceftaroline is currently the only next-generation cephalosporin available in the United States. It is active against methicillin-resistant Staphylococcus aureus (MRSA) and gram-positive bacteria. It also retains the activity of the later-generation cephalosporins and is effective against susceptible gram-negative bacteria.

Are cephalosporins safe?

Cephalosporins are generally safe, with low toxicity and good efficacy against susceptible bacteria.

Allergic reactions have been reported with cephalosporins and symptoms may include a rash, hives (urticaria), swelling, or rarely, anaphylaxis. Up to 10% of people with a history of penicillin allergy will also be allergic to cephalosporins.

Rarely, seizures have been reported with some cephalosporins; the risk is greatest in those with kidney disease.

Cephalosporins have also been associated with a reduced ability of the blood to clot leading to prolonged bleeding times. People with kidney or liver disease, nutritionally deprived, taking cephalosporins long-term, or concurrently receiving anticoagulant therapy are more at risk.

For a complete list of severe side effects, please refer to the individual drug monographs.

What are the side effects of cephalosporins?

Cephalosporins generally cause few side effects. The most common side effects reported include abdominal pain, diarrhea, dyspepsia, headache, gastritis, and nausea and vomiting. Transient liver problems have also been reported.

Rarely, some people may develop a super-infection due to overgrowth of a naturally occurring bacterium called Clostridium difficile, following use of any antibiotic, including cephalosporins. Symptoms may include severe diarrhea.

Uncommonly, an overgrowth of the yeast, Candida albicans, may occur following cephalosporin use, resulting in the symptoms of thrush.

For a complete list of side effects, please refer to the individual drug monographs.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Asthma

Bronchial asthma is a chronic inflammatory disease of the upper respiratory tract, which is accompanied by characteristic symptoms: shortness of breath, wheezing, chest tightness, cough, especially in the early morning and at night. It is believed that asthma is largely the result of an allergic reaction, an unfavorable environmental condition. There is also a hereditary factor.

The quality of life of a person suffering from bronchial asthma strongly depends on how ready he is to comply with a number of specific measures: the use of drugs for basic and symptomatic therapy, the maximum possible elimination of risk factors, the use of a specially designed set of exercises.

Symptomatic drugs relieve spasm of the muscles of the bronchi, thereby facilitating the attack. Salbutamol, Berotek – help to stop an asthma attack, salmeterol allows you to prevent, and formoterol (Atimos, Oxys turbuhaler) – to prevent and stop an attack that has begun.

Basic therapy drugs include drugs that help control an asthmatic attack. The first group – cromones – Intal, Tailed Mint – drugs that help with relatively mild forms of bronchial asthma. Glucocorticosteroids in the form of inhaled forms have a more serious effect: Pulmicort, Beclazone, Klenil, Flixotide. Now there are drugs that allow you to combine the properties of symptomatic and basic therapy drugs: Seretide, Seretide Multidisk, Symbicort Turbuhaler. The third group of anti-asthma drugs includes antileukotriene drugs that quickly eliminate the basal tone of the airways, which is especially important for the treatment of aspirin bronchial asthma – Singulair. The fourth group – xanthines – was previously widely used for emergency relief of an attack: Eufillin or long-term control of the course of the disease – theophylline (Teotard). However, with the advent of more effective drugs, this group is now more often used as an auxiliary or in the absence of other drugs.

In the treatment of bronchial asthma, it is advisable to use expectorants that facilitate the removal of sputum from the bronchi: Lazolvan, ACC. The action of expectorants is especially effective when using nebulizers – special devices that allow the delivery of drugs directly to the focus of inflammation in the bronchi. In this case, drugs are used in the form of solutions.

In the course of the disease complicated by infections, antibiotics of the tetracycline and erythromycin groups, as well as penicillins and cephalosporins, are used.

In addition to traditional medical methods of treatment, the following are used: the Buteyko method – a specially developed set of breathing exercises aimed at eliminating the clinical symptoms of the disease; halotherapy – exposure to highly dispersed salt aerosol while staying in artificially created salt caves; speleotherapy is a method of treatment by prolonged stay in a peculiar microclimate of natural karst caves, grottoes, salt mines, artificially traversed mine workings of metal, salt and potash mines.

Pankratova Evgenia Igorevna

The material is informational. Medicinal products, biologically active supplements and other products are indicated as an example of their possible use and / or application, which in no way constitutes a recommendation for their use. Before using drugs, dietary supplements and medical equipment and other products, be sure to consult a specialist.

21.10.54.170 OKPD code 2 – interpretation, procurement examples and restrictions

Cephalosporins

Main

OKPD classifier 2

C

21

90 028 21.1

21.10

21.10.5

21.10.54

21.10 .54.170

Classifier OKPD 2

Code 21.10.54.170

Explanation: Cephalosporins

Comments: the classifier does not contain comments on this code at

Old code: 24.41.54.180

The entry in the OKPD 2 classifier with code 21.10.54.170 does not contain clarifying (child) codes.

No. 0517100000218000025

541,524₽

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Supply of veterinary preparations for the needs of Federal State Unitary Enterprise PZ “Komsomolskoye” 900 03

Found in documents | Cefapirin. An antibacterial drug of the first generation cephalosporin group. In 19 g, 500 mg of cefapirin in the form of benzathine salt as an active ingredient. — 300 pieces

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Altai Territory | FSUE PZ “KOMSOMOLSKOE”

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No. 31806591972

745 357₽

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Supply of drugs 72-ЗК)

Found in documents | Cephalosporins – 700 vials

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Zabaikalsky Krai | city ​​of Krasnokamensk | GAUZ “KB No. 4”

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No. 31806609478

184 256₽

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9 0002 Found in documents | Cephalosporins – 100 vials

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