What are the adverse effects of cephalosporins? How do they work, and what are the contraindications? Explore the toxicity and management strategies for cephalosporin therapy.

Understanding Cephalosporins: Mechanism of Action and Indications

Cephalosporins are a class of beta-lactam antimicrobials used to manage a wide range of infections caused by both gram-positive and gram-negative bacteria. These antibiotics are classified into five generations, each with a unique spectrum of coverage and clinical applications.

The mechanism of action of cephalosporins involves inhibiting the synthesis of the bacterial cell wall, which ultimately leads to cell death. The different generations of cephalosporins have varying degrees of activity against specific bacteria, with the later generations demonstrating extended coverage against resistant strains.

Contraindications and Adverse Effects of Cephalosporins

While cephalosporins are widely used, they can also be associated with various adverse effects. Contraindications for cephalosporin use include hypersensitivity to the drug or other beta-lactam antibiotics, as well as a history of severe allergic reactions (e.g., anaphylaxis) to penicillins or cephalosporins.

The adverse effects of cephalosporins can range from mild to severe, and may include:

• Gastrointestinal disturbances: Nausea, vomiting, diarrhea, and abdominal pain
• Hypersensitivity reactions: Rash, hives, angioedema, and anaphylaxis
• Nephrotoxicity: Kidney damage, especially with high-dose or prolonged use
• Neurotoxicity: Seizures, encephalopathy, and neuromuscular disorders
• Hematological effects: Neutropenia, thrombocytopenia, and hemolytic anemia
• Superinfections: Overgrowth of resistant organisms, such as Clostridioides difficile

Toxicity and Monitoring Strategies

The toxicity of cephalosporins can be influenced by several factors, including the specific cephalosporin used, the dose and duration of therapy, and the patient’s underlying medical conditions. Patients with renal impairment, for example, may be at a higher risk of developing nephrotoxicity due to the accumulation of the antibiotic in the body.

To mitigate the risk of adverse effects, healthcare providers should closely monitor patients receiving cephalosporin therapy. This may involve regular laboratory tests, such as complete blood counts, liver and kidney function tests, and therapeutic drug monitoring in some cases. Patients should also be closely observed for signs of hypersensitivity reactions or other adverse events.

Interprofessional Strategies for Improving Cephalosporin Therapy

Effective management of cephalosporin therapy requires a collaborative, interprofessional approach. Physicians, pharmacists, and nurses should work together to ensure the appropriate selection, dosing, administration, and monitoring of cephalosporin therapy. This may involve:

• Reviewing patient medical history and medication profile to identify potential contraindications or drug interactions
• Educating patients on the proper use of cephalosporins, potential adverse effects, and the importance of adherence
• Closely monitoring patients for signs of adverse events and promptly addressing any issues that arise
• Communicating effectively within the healthcare team to coordinate care and optimize patient outcomes

Cephalosporin Generations and Their Unique Characteristics

The five generations of cephalosporins each have their own distinctive features and applications:

1. First-generation cephalosporins: Effective against most gram-positive cocci and some gram-negative bacteria, such as E. coli and Klebsiella pneumoniae. Commonly used for skin and soft tissue infections, as well as surgical prophylaxis.
2. Second-generation cephalosporins: Improved coverage against gram-negative bacteria, including Haemophilus influenzae and Bacteroides species. Often used for respiratory tract, genitourinary tract, and biliary tract infections.
3. Third-generation cephalosporins: Expanded gram-negative coverage, including Enterobacteriaceae and Neisseria species. Useful for treating gram-negative infections resistant to other beta-lactams, as well as meningitis.
4. Fourth-generation cephalosporins: Similar coverage to third-generation, with additional activity against gram-negative bacteria with antimicrobial resistance, such as those producing extended-spectrum beta-lactamases (ESBLs).
5. Fifth-generation cephalosporins: Demonstrate activity against methicillin-resistant Staphylococcus aureus (MRSA) and penicillin-resistant Streptococcus pneumoniae.

Optimizing Cephalosporin Therapy: Considerations and Strategies

To ensure the safe and effective use of cephalosporins, healthcare providers should consider the following strategies:

• Carefully select the appropriate cephalosporin generation based on the suspected or confirmed pathogens, patient factors, and local resistance patterns
• Ensure appropriate dosing and administration, taking into account the patient’s renal function and other relevant clinical parameters
• Monitor patients closely for the development of adverse effects, and promptly address any issues that arise
• Promote antimicrobial stewardship by encouraging the judicious use of cephalosporins and other antibiotics, to minimize the development of resistance

Conclusion

Cephalosporins are a versatile class of antibiotics that play a crucial role in the management of various bacterial infections. Understanding the mechanism of action, contraindications, and potential adverse effects of cephalosporins is essential for healthcare providers to ensure safe and effective use of these medications. By implementing an interprofessional approach and following best practices, clinicians can optimize cephalosporin therapy and improve patient outcomes.

Cephalosporins – StatPearls – NCBI Bookshelf

Continuing Education Activity

Cephalosporins are beta-lactam antimicrobials used to manage a wide range of infections from gram-positive and gram-negative bacteria. The five generations of cephalosporins are useful against skin infection, resistant bacteria, meningitis, and other infections. This activity describes the indications, contraindications, and possible adverse effects of cephalosporins and will highlight the mechanism of action, adverse event profile, monitoring, route of administration, as well as other key factors.

Objectives:

• Identify the mechanism of action of cephalosporins.

• Describe the contraindications of cephalosporins.

• Review the toxicity of cephalosporins.

• Summarize interprofessional team strategies for improving care coordination and communication to advance cephalosporins and improve outcomes.

Access free multiple choice questions on this topic.

Indications

Cephalosporins are antimicrobials grouped into five generations based on their spectrum of coverage against gram-positive and gram-negative bacteria and their temporal discovery. First-generation cephalosporins have coverage against most gram-positive cocci as well as some gram-negative bacteria, e.g., Escherichia coli (E. coli), Proteus mirabilis, and Klebsiella pneumoniae. Second-generation cephalosporins have coverage against Haemophilus influenzae (H. influenzae), Moraxella catarrhalis, and Bacteroides spp. Third-generation cephalosporins have less coverage against most gram-positive organisms but have increased coverage against Enterobacteriaceae, Neisseria spp., and H. influenzae. Fourth-generation cephalosporins have similar coverage as third-generation cephalosporins but with additional coverage against gram-negative bacteria with antimicrobial resistance, e.g., beta-lactamase. Fifth-generation cephalosporins have coverage against methicillin-resistant staphylococci and penicillin-resistant pneumococci.    

First-generation cephalosporins include cefazolin, cephalothin, cephapirin, cephradine, cefadroxil, and cephalexin. First-generation cephalosporins have active coverage against most gram-positive cocci, such as staphylococci
spp. and streptococci
spp., while having minimal coverage against gram-negative bacteria. Gram-negative bacteria that are more susceptible to first-generation cephalosporins are Proteus mirabilis, E. coli, and Klebsiella pneumoniae. Oral first-generation cephalosporins are commonly prescribed to use against uncomplicated skin and soft tissue infections such as cellulitis and abscesses commonly due to a Staphylococci
spp. or Streptococci
spp. infection. Additionally, clinicians can use them for bone, respiratory tract, genitourinary tract, biliary tract, bloodstream infection, otitis media, and surgical prophylaxis. In fact, cefazolin is the cephalosporin of choice for surgical prophylaxis. One of the non-FDA-approved indications is to use first-generation cephalosporins for endocarditis prophylaxis for those who are susceptible and undergoing a dental or respiratory procedure.[1][2][3]

Second-generation cephalosporins divide into two subgroups: the second-generation and the cephamycin subgroup. Some of the second-generation subgroups include cefuroxime and cefprozil. The cephamycin subgroup includes cefmetazole, cefotetan, and cefoxitin. Within the first subgroup, cefuroxime has increased coverage against H. influenzae. Indications for cefuroxime also include Lyme disease in pregnant women and children. The cephamycin subgroup has increased coverage against Bacteroides species. Second-generation cephalosporins have less activity against gram-positive cocci than first-generation cephalosporins but have increased activity against gram-negative bacilli. They are often prescribed to treat respiratory infections such as bronchiolitis or pneumonia. Other indications for second-generation cephalosporins are similar to first-generation indications (bone, respiratory tract, genitourinary tract, biliary tract, bloodstream infection, otitis media, and surgical prophylaxis). In addition to the gram-negative bacteria covered by first-generation cephalosporins, second-generation cephalosporins also have coverage against H. influenzae, Enterobacter aerogenes, Neisseria species, and Serratia marcescens.[4]

Third-generation cephalosporins include cefotaxime, ceftazidime, cefdinir, ceftriaxone, cefpodoxime, cefoperazone, and cefixime. This generation has extended gram-negative bacteria coverage often used to treat gram-negative infections resistant to the first and second generation or other beta-lactam antimicrobials. When given IV, third-generation can penetrate the blood-brain barrier and cover bacteria in the cerebral spinal fluid, especially ceftriaxone and cefotaxime. Ceftriaxone can be given to treat meningitis caused by H. influenzae, Neisseria meningitidis, or Streptococcus pneumoniae. Ceftriaxone is also used to treat gonorrhea and disseminated Lyme disease. Ceftazidime, very importantly, has Pseudomonas
aeruginosa coverage. [5] 

Fourth-generation cephalosporin includes cefepime. Cefepime is a broad-spectrum antimicrobial that can penetrate the cerebral spinal fluid. Cefepime has an additional quaternary ammonium group, allowing them to better penetrate the outer membrane of gram-negative bacteria. Similar to the activity of cefotaxime and ceftriaxone, cefepime can cover Streptococcus pneumoniae and methicillin-sensitive Staphylococcus aureus (MSSA). Similar to ceftazidime, cefepime, very importantly, can cover for Pseudomonas
aeruginosa. In addition to the gram-negative bacteria that third-generation covers (Neisseria spp., H. influenzae, and Enterobacteriaceae), cefepime can provide coverage against beta-lactamase-producing gram-negative bacilli. Although effective against both gram-positive and gram-negative bacteria, cefepime is reserved for serious systemic infection in patients who are likely to have multi-resistance organisms.[6]

Fifth-generation cephalosporins include ceftaroline. Ceftaroline is also a broad-spectrum antimicrobial and thus can cover susceptible gram-positive and gram-negative organisms. However, what makes it unique from the rest of the cephalosporins is that it has coverage against methicillin-resistant Staphylococcus aureus (MRSA). Ceftaroline can also cover Listeria
monocytogenes and Enterococcus faecalis. However, ceftaroline does not cover Pseudomonas aeruginosa.[7]

Mechanism of Action

Bacteria synthesize a cell wall that is strengthened by cross-linking peptidoglycan units via penicillin-binding proteins (PBP, peptidoglycan transpeptidase). Initially derived from the fungus Cephalosporium sp., cephalosporins are a large group of bactericidal antimicrobials that work via their beta-lactam rings. The beta-lactam rings bind to the penicillin-binding protein and inhibit its normal activity. Unable to synthesize a cell wall, the bacteria die.

Staphylococcus aureus, which is initially susceptible to cephalosporins, can develop resistance by changing the structure of the penicillin-binding proteins.  S. aureus does this by having a gene that encodes a modified penicillin-binding protein; this prevents the cephalosporin’s beta-lactam rings from inactivating the protein. The bacterium that develops this mechanism of resistance is called methicillin-resistant Staphylococcus aureus (MRSA). As indicated above, out of the five generations of cephalosporin, only the fifth generation ceftaroline has coverage against methicillin-resistant Staphylococcus aureus. Another crucial resistance mechanism is producing the enzyme beta-lactamase, which cleaves the beta-lactam ring, preventing it from attaching to the penicillin-binding proteins, e.g., peptidoglycan transpeptidase. Beta-lactamase inhibitors can be co-formulated with cephalosporins to increase their spectrum of activity, e.g., ceftazidime/avibactam and ceftolozane/tazobactam.

Administration

First-generation: Cefazolin, cephalothin, and cephapirin are administered parenterally. The administration route for cefadroxil and cephalexin is oral. Cephradine administration can be parenteral or oral.  

Second-generation: Cefuroxime can be administered parenterally or orally. Cefprozil administration is oral. Cefmetazole, cefotetan, and cefoxitin are administered parenterally.

Third-generation: Cefotaxime, ceftazidime, and ceftriaxone administration is via the parenteral route. Cefdinir, cefixime, and cefpodoxime are administered orally. A single intramuscular shot of 125 or 250 mg of ceftriaxone effectively treats uncomplicated gonococcal infection or its complications, such as pelvic inflammatory disease or epididymo-orchitis.[8][9][10]

Fourth-generation: Cefepime is administered parenterally.

Fifth-generation: Ceftaroline is administered parenterally.

Many of the parenterally administered cephalosporins have short half-lives and need to be given more frequently in patients with normal renal function. Cefazolin and ceftriaxone have a longer half-life; thus, they do not need to be dosed as often. Ceftriaxone is the only cephalosporin that does not need to have its dose modified in the presence of renal failure. However, in patients with both renal and hepatic impairment, the recommended daily dose should not exceed 2 g.[11] 

Adverse Effects

Cephalosporins have low toxicity and are generally safe. The most common adverse reactions from cephalosporins are nausea, vomiting, lack of appetite, and abdominal pain.

The less common adverse reaction includes:

Hypersensitivity Reaction

A hypersensitivity reaction to cephalosporin is infrequent and is more common in first and second-generation cephalosporins. Common allergic reaction to cephalosporin includes rash, hives, and swelling. Rarely will the hypersensitivity reaction result in anaphylaxis. Patients who are allergic to penicillin might show a hypersensitive reaction to cephalosporins as well. This cross-reactivity is more common in first and second-generation cephalosporins because they have R-groups more similar to penicillin G. Third generation and beyond show minimal cross-reactivity.[12][13]

Drug-induce Immune Hemolytic Anemia (DIIHA)

The proposed mechanism of action of DIIHA is that the drug binds to the red blood cell membrane; this causes no harm to the red blood cell itself or the patient. However, if the patient starts making IgG antibodies against the drug, the antibody will bind to the red blood cell. The immune system will react with the abnormal red blood cell resulting in hemolysis. Cefotetan and ceftriaxone are the two cephalosporins most likely to cause DIIHA.[14] 

Disulfiram-like Reaction 

Cephalosporins containing a methyltetrazolethiol side chain can inhibit the aldehyde dehydrogenase enzyme resulting in the accumulation of acetaldehyde. Cefamandole, cefoperazone, and moxalactam are the most common cephalosporin to present with this reaction.[15]

Vitamin K Deficiency 

Certain cephalosporins can inhibit vitamin K epoxide reductase, preventing the production of the reduced(active) vitamin K. Therefore, there is a decreased synthesis of coagulation factors, and the patient is predisposed to hypoprothrombinemia.[16] 

Increase Nephrotoxicity of Aminoglycosides 

There are reported cases of drug-induced nephrotoxicity when patients take cephalosporin and aminoglycosides in combination, but other factors often cloud the evidence. Therefore, the synergistic nephrotoxicity of cephalosporin and aminoglycoside is not to be completely understood.[17][18]

Pseudomembranous Colitis

Pseudomembranous colitis is often associated with the use of clindamycin and ampicillin. Cephalosporin use is also a common cause of pseudomembranous colitis, especially third-generation cephalosporins.[19][17] 

Contraindications

One of the contraindications of cephalosporin is if patients are allergic to them or have had an anaphylactic reaction to penicillin or other beta-lactam antimicrobials. 

Ceftriaxone is contraindicated in neonates with hyperbilirubinemia because of reports that ceftriaxone displaces bilirubin from albumin, increasing the free bilirubin concentrations and increasing the risk of jaundice in neonates.[20][21] Ceftriaxone reacts to a calcium-containing solution, and it can precipitate in the lungs and kidneys of infants less than 28 days old, which could be life-threatening. Therefore, ceftriaxone is also contraindicated in infants less than 28 days old if they are expected to receive any calcium-containing products. [22] 

Monitoring

It is essential to monitor for possible signs of anaphylactic reaction as well as allergic reactions such as hives, itching, and swelling. Physicians and pharmacists also need to monitor renal function periodically because that could potentially warrant a change in the dose and/or dosing frequency of the cephalosporin (except for ceftriaxone).[23] With other possible adverse reactions listed above, monitor CBC for possible signs of drug-induced immune hemolytic anemia or hypoprothrombinemia from vitamin K deficiency. Also, monitor for possible signs of a disulfiram-like reaction or pseudomembranous colitis. 

Toxicity

Testing the effects of high dosage cephalosporin in rabbits, there is new evidence of nephrotoxicity due to its effect on the mitochondria system of the kidney.[24] Cefepime overdose can result in seizures and encephalopathy. Studies show it to potentially result from cefepime crossing the blood-brain barrier and displaying concentration-dependent ϒ-aminobutyric acid (GABA) antagonism, which can also occur with toxic doses of penicillin G. Other studies show altered mental status and a triphasic wave discharge on electroencephalogram (EEG). Discontinuation of cefepime demonstrates normalization of mental status.[25][26]

Exercise caution with cephalosporin treatment in patients with a history of seizures, especially with poor renal function.

Enhancing Healthcare Team Outcomes

Effective interprofessional teamwork and coordination by clinicians, nurses, pharmacists, and other healthcare professionals are required to provide the best care for the patient. One of the principles that enhance healthcare team outcomes is having a shared goal for everyone, including the patient. Having clear roles between the different interprofessional team members and trusting each other can increase the team’s efficiency. Crucial for team success is having effective communication skills. A clinician needs to be able to accurately diagnose a disease and prescribe the proper medication and inform possible adverse effects to the patients. Nurses also need to know possible adverse effects so that they can inform the physician if they notice any adverse effects developing. A pharmacist can educate the patient on how to properly administer the drug and the other potential adverse effects, as well as verify agent selection and coverage and report any potential interactions to the ordering clinician. The patient also must tell the clinician and nurse what they are experiencing, anything unusual, so that everyone is informed about the patient’s well-being. Through effective interprofessional healthcare teamwork, appropriate management of cephalosporin adverse drug reactions can occur, resulting in better patient outcomes. [Level 5]

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References

1.

Hsieh WC, Ho SW. Evaluation of antibacterial activities of cephalosporin antibiotics: cefazolin, cephaloridine, cephalothin, and cephalexin. Zhonghua Min Guo Wei Sheng Wu Xue Za Zhi. 1975 Mar;8(1):1-11. [PubMed: 1097210]

2.

Griffith RS. The pharmacology of cephalexin. Postgrad Med J. 1983;59 Suppl 5:16-27. [PubMed: 6364086]

3.

Bergeron MG, Brusch JL, Barza M, Weinstein L. Bactericidal activity and pharmacology of cefazolin. Antimicrob Agents Chemother. 1973 Oct;4(4):396-401. [PMC free article: PMC444566] [PubMed: 4598612]

4.

Tartaglione TA, Polk RE. Review of the new second-generation cephalosporins: cefonicid, ceforanide, and cefuroxime. Drug Intell Clin Pharm. 1985 Mar;19(3):188-98. [PubMed: 3884304]

5.

Klein NC, Cunha BA. Third-generation cephalosporins. Med Clin North Am. 1995 Jul;79(4):705-19. [PubMed: 7791418]

6.

Okamoto MP, Nakahiro RK, Chin A, Bedikian A, Gill MA. Cefepime: a new fourth-generation cephalosporin. Am J Hosp Pharm. 1994 Feb 15;51(4):463-77; quiz 541-2. [PubMed: 8017411]

7.

Zhanel GG, Sniezek G, Schweizer F, Zelenitsky S, Lagacé-Wiens PR, Rubinstein E, Gin AS, Hoban DJ, Karlowsky JA. Ceftaroline: a novel broad-spectrum cephalosporin with activity against meticillin-resistant Staphylococcus aureus. Drugs. 2009;69(7):809-31. [PubMed: 19441869]

8.

Judson FN. Treatment of uncomplicated gonorrhea with ceftriaxone: a review. Sex Transm Dis. 1986 Jul-Sep;13(3 Suppl):199-202. [PubMed: 3094173]

9.

Jennings LK, Krywko DM. StatPearls [Internet]. StatPearls Publishing; Treasure Island (FL): Mar 13, 2023. Pelvic Inflammatory Disease. [PubMed: 29763134]

10.

Rupp TJ, Leslie SW. StatPearls [Internet]. StatPearls Publishing; Treasure Island (FL): Nov 28, 2022. Epididymitis. [PubMed: 28613565]

11.

Andriole VT. Pharmacokinetics of cephalosporins in patients with normal or reduced renal function. J Infect Dis. 1978 May;137 Suppl:S88-S99. [PubMed: 349098]

12.

Moreno E, Macías E, Dávila I, Laffond E, Ruiz A, Lorente F. Hypersensitivity reactions to cephalosporins. Expert Opin Drug Saf. 2008 May;7(3):295-304. [PubMed: 18462187]

13.

Dickson SD, Salazar KC. Diagnosis and management of immediate hypersensitivity reactions to cephalosporins. Clin Rev Allergy Immunol. 2013 Aug;45(1):131-42. [PubMed: 23546989]

14.

Garratty G. Drug-induced immune hemolytic anemia. Hematology Am Soc Hematol Educ Program. 2009:73-9. [PubMed: 20008184]

15.

Uri JV, Parks DB. Disulfiram-like reaction to certain cephalosporins. Ther Drug Monit. 1983 Jun;5(2):219-24. [PubMed: 6224316]

16.

Shearer MJ, Bechtold H, Andrassy K, Koderisch J, McCarthy PT, Trenk D, Jähnchen E, Ritz E. Mechanism of cephalosporin-induced hypoprothrombinemia: relation to cephalosporin side chain, vitamin K metabolism, and vitamin K status. J Clin Pharmacol. 1988 Jan;28(1):88-95. [PubMed: 3350995]

17.

Rankin GO, Sutherland CH. Nephrotoxicity of aminoglycosides and cephalosporins in combination. Adverse Drug React Acute Poisoning Rev. 1989 Summer;8(2):73-88. [PubMed: 2672726]

18.

Silverblatt F. Pathogenesis of nephrotoxicity of cephalosporins and aminoglycosides: a review of current concepts. Rev Infect Dis. 1982 Sep-Oct;4 Suppl:S360-5. [PubMed: 7178755]

19.

de Lalla F, Privitera G, Ortisi G, Rizzardini G, Santoro D, Pagano A, Rinaldi E, Scarpellini P. Third generation cephalosporins as a risk factor for Clostridium difficile-associated disease: a four-year survey in a general hospital. J Antimicrob Chemother. 1989 Apr;23(4):623-31. [PubMed: 2663814]

20.

Gulian JM, Gonard V, Dalmasso C, Palix C. Bilirubin displacement by ceftriaxone in neonates: evaluation by determination of ‘free’ bilirubin and erythrocyte-bound bilirubin. J Antimicrob Chemother. 1987 Jun;19(6):823-9. [PubMed: 3610909]

21.

Bickford CL, Spencer AP. Biliary sludge and hyperbilirubinemia associated with ceftriaxone in an adult: case report and review of the literature. Pharmacotherapy. 2005 Oct;25(10):1389-95. [PubMed: 16185184]

22.

Bradley JS, Wassel RT, Lee L, Nambiar S. Intravenous ceftriaxone and calcium in the neonate: assessing the risk for cardiopulmonary adverse events. Pediatrics. 2009 Apr;123(4):e609-13. [PubMed: 19289450]

23.

Spyker DA, Thomas BL, Sande MA, Bolton WK. Pharmacokinetics of cefaclor and cephalexin: dosage nomograms for impaired renal function. Antimicrob Agents Chemother. 1978 Aug;14(2):172-7. [PMC free article: PMC352429] [PubMed: 697345]

24.

Tune BM, Fravert D. Cephalosporin nephrotoxicity. Transport, cytotoxicity and mitochondrial toxicity of cephaloglycin. J Pharmacol Exp Ther. 1980 Oct;215(1):186-90. [PubMed: 7452482]

25.

Payne LE, Gagnon DJ, Riker RR, Seder DB, Glisic EK, Morris JG, Fraser GL. Cefepime-induced neurotoxicity: a systematic review. Crit Care. 2017 Nov 14;21(1):276. [PMC free article: PMC5686900] [PubMed: 29137682]

26.

Tchapyjnikov D, Luedke MW. Cefepime-Induced Encephalopathy and Nonconvulsive Status Epilepticus: Dispelling an Artificial Dichotomy. Neurohospitalist. 2019 Apr;9(2):100-104. [PMC free article: PMC6429673] [PubMed: 30915188]

Disclosure: Toai Bui declares no relevant financial relationships with ineligible companies.

Disclosure: Charles Preuss declares no relevant financial relationships with ineligible companies.

Uses, List of Generations, Side Effects, and More

Cephalosporins are a type of antibiotic that can treat a range of simple infections. People can take them orally or doctors can inject them into a vein.

Cephalosporins are a type of antibiotic. Antibiotics are medications that treat bacterial infections. There are many types, often called classes, of antibiotics available. Cephalosporins are a type of beta-lactam antibiotic.

They can be taken orally or injected into a vein (intravenous injection), depending on the infection.

Read on to learn more about cephalosporins, including what they treat and the side effects they can cause.

Healthcare providers use cephalosporins to treat a variety of bacterial infections, especially for people who are allergic to penicillin, another common antibiotic.

Some examples of infections that cephalosporins can treat include:

• skin or soft tissue infections
• urinary tract infections (UTIs)
• strep throat
• ear infections
• pneumonia
• sinus infections
• meningitis
• gonorrhea

Oral cephalosporins are generally used for simple infections that are easy to treat. For example, a routine case of strep throat might be treated with a course of oral cephalosporins.

Intravenous (IV) cephalosporins are used for more severe infections. This is because IV antibiotics reach your tissues faster, which can make a big difference if you have a serious infection, such as meningitis.

Cephalosporins are grouped together based on the type of bacteria that they’re most effective against. These groups are referred to as generations. There are five generations of cephalosporins.

To understand the differences between the generations, it’s important to understand the difference between Gram-positive and Gram-negative bacteria.

One of the main distinctions between the two is their cell wall structure:

• Gram-positive bacteria have thicker membranes that are easier to penetrate. Think of their cell wall as a chunky, loose-knit sweater.
• Gram-negative bacteria have thinner membranes that are harder to penetrate, making them more resistant to some antibiotics. Think of their wall as a piece of fine chain mail.

First-generation cephalosporins

First-generation cephalosporins are very effective against Gram-positive bacteria. But they’re only somewhat effective against Gram-negative bacteria.

First-generation cephalosporins might be used to treat:

• skin and soft tissue infections
• UTIS
• strep throat
• ear infections
• pneumonia

Some first-generation cephalosporins are used as prophylactic antibiotics for surgery involving the chest, abdomen, or pelvis.

Examples of first-generation cephalosporins include:

• cephalexin (Keflex)
• cefadroxil (Duricef)
• cephradine (Velosef)

summary

First-generation cephalosporins are more effective against Gram-positive bacteria, though they also work against some Gram-negative bacteria.

Second-generation cephalosporins

Second-generation cephalosporins also target some types of Gram-positive and Gram-negative bacteria. But they’re less effective against certain Gram-positive bacteria than first-generation cephalosporins are.

They’re often used to treat respiratory infections, such as bronchitis or pneumonia.

Other infections sometimes treated with second-generation cephalosporins include:

• ear infections
• sinus infections
• UTIs
• gonorrhea
• meningitis
• sepsis

Examples of second-generation cephalosporins include:

• cefaclor (Ceclor)
• cefuroxime (Ceftin)
• cefprozil (Cefzil)

summary

Second-generation cephalosporins target both Gram-positive and Gram-negative bacteria. But they’re a little less effective against Gram-positive bacteria compared to first-generation cephalosporins

Third-generation cephalosporins

Third-generation cephalosporins are more effective against Gram-negative bacteria compared to both the first and second generations. They’re also more active against bacteria that may be resistant to previous generations of cephalosporins.

The third generation also tend to be less active than previous generations against Gram-positive bacteria, including Streptococcus and Staphylococcus species.

One third-generation cephalosporin, ceftazidime (Fortaz), is often used to treat pseudomonas infections, including hot tub folliculitis.

Third-generation cephalosporins may also be used to treat:

• skin and soft tissue infections
• pneumonia
• UTIs
• gonorrhea
• menigitis
• Lyme disease
• sepsis

A few examples of third-generation cephalosporins include:

• cefixime (Suprax)
• ceftibuten (Cedax)
• cefpodoxime (Vantin)

Summary

Third-generation cephalosporins are effective against many Gram-negative bacteria and bacteria that haven’t responded to first- or second-generation cephalosporins.

Fourth-generation cephalosporins

Cefepime (Maxipime) is the only fourth-generation cephalosporin that’s available in the United States. While effective against a variety of Gram-positive and Gram-negative bacteria, it’s usually reserved for more severe infections.

Cefepime can be used to treat the following types of infections:

• skin and soft tissue infections
• pneumonia
• UTIs
• abdominal infections
• meningitis
• sepsis

Cefepime can be administered intravenously or with an intramuscular injection. It may also be given to people with a low white blood cell count, which can increase the risk of developing a severe infection.

Summary

Fourth-generation cephalosporins work against both Gram-positive and Gram-negative bacteria. They’re generally used for more severe infections or for those with weakened immune systems.

Fifth-generation cephalosporins

You may hear fifth-generation cephalosporins referred to as advanced- generation cephalosporins. There’s one fifth-generation cephalosporin, ceftaroline (Teflaro), available in the United States.

This cephalosporin can be used to treat bacteria, including resistant Staphylococcus aureus (MRSA) and Streptococcus species, that are resistant to penicillin antibiotics.

Otherwise, ceftaroline’s activity is similar to that of third-generation cephalosporins, although it isn’t effective against Pseudomonas aeruginosa.

Summary

Ceftaroline is the only fifth-generation cephalosporin available in the United States. It’s often used to treat infections, including MRSA infections, that are resistant to other antibiotics.

As with any kind of medication, you can be allergic to cephalosporins. The most common sign of an allergic reaction to cephalosproins is a skin rash.

In rare cases, cephalosprins may cause a serious allergic reaction known as anaphylaxis.

Symptoms of anaphylaxis include:

• hives
• flushed skin
• swollen tongue and throat
• breathing difficulties
• low blood pressure
• rapid or weak pulse
• nausea or vomiting
• diarrhea
• dizziness
• fainting

get help

Anaphylaxis can be life-threatening. Seek immediate medical treatment if you’re taking a cephalosporin and experience symptoms of anaphylaxis.

What if I’m allergic to penicillin?

It’s rare to be allergic to both penicillin and cephalosporins. But if you’ve had a serious anaphylactic reaction to penicillin antibiotics in the past, you shouldn’t take cephalosporins.

It’s uncommon to have an allergy to both penicillin antibiotics and cephalosporins, so cephalosporins can be used cautiously in people with a penicillin allergy.

However, people who’ve had a serious anaphylactic reaction to penicillin antibiotics shouldn’t take cephalosporins.

In addition, some cephalosporins are more likely to cause a reaction in people with a penicillin allergy. These include:

• cephalothin
• cephalexin
• cefadroxil
• cefazolin

Cephalosporins can cause a range of side effects, including:

• stomach upset
• nausea
• vomiting
• diarrhea
• yeast infection or oral thrush
• dizziness

One of the more serious side effects that can occur is a C. difficile infection. This infection typically occurs after a long course of antibiotics and can be potentially life-threatening.

Symptoms to watch out for include:

• watery diarrhea
• abdominal pain
• fever
• nausea
• decreased appetite

You can help to prevent stomach upset and diarrhea by:

• taking probiotics, which can help to add good bacteria to your digestive tract
• following the instructions that come with your medication, as some antibiotics should be taken with food, while others should be taken on an empty stomach
• avoiding foods that can contribute to stomach upset, such as spicy or greasy foods

Cephalosporins are generally safe for most people, including those who are pregnant. In fact, some first-generation cephalosporins are commonly used to treat UTIs in pregnant people.

However, you shouldn’t take cephalosporins if you’re breastfeeding.

Cephalosporins can sometimes interact with other medications you’re taking. Make sure to tell your healthcare provider about all other medications you take, including supplements, vitamins, and over-the-counter medications.

Cephalosporins are a type of antibiotic used to treat a range of bacterial infections. There are different generations of cephalosporins, and some are better suited to treat certain infections than others.

If you have to take antibiotics, make sure to tell your doctor about all other medications you take, as well as any previous allergic reactions to antibiotics.

Remember

Make sure you take the full course of antibiotics as prescribed by your doctor, even if you start to feel better before finishing them. Otherwise, you may not kill all of the bacteria, which can make them resistant to antibiotics.

Side effects of cephalosporins

Allergic reactions (in 1-4% of patients):
urticaria, transient eosinophilia,
rarely bronchospasm, anphylactic
shock. Precursive allergy to penicillins
rare (2% of cases).

When using high doses –
reversible hematopoiesis suppression
(leukopenia, neutropenia), bleeding.
Hypoprothrombinemia and hemorrhagic
syndrome is most characteristic of
cefamandole, cefotetan, cefoperazone,
cefmetazole, moxalactam. These same
drugs cause intolerance
alcohol.

Transient increase in activity
aminotransferases and alkaline phosphatase.

When using high doses of cephalosporins
possibly increased nephrotoxicity
combination of cephalosporins with
loop diuretics and aminoclicosides.

Dyspeptic disorders in
the use of cephalosporins that produce
bile (cefoperazone, ceftriaxone).

Monobactams

Aztreonam.
The basis of molecular structure
aztreonam, as well as other beta-lactam
antibiotics is represented by beta –
lactam ring. Mechanism: inhibition
transpeptidase enzyme followed by
disruption of the cell wall
microorganisms and their death.

Manifests
high activity towards
Gram-negative microorganisms
(Escherichia, Klebsiella, Proteus, Morganella,
sinengnoy stick, serations, neisseria,
Haemophilus influenzae, Citrobacter), and
resistance to beta-lactamases. TO
resistant staphylococci,
streptococci, pneumococci, bacteroids.
Unlike cephalosporins and carbapenems
does not stimulate the production of beta-lactamase
gram-negative bacteria.

Can
apply for intolerance
penicillins, cephalosporins or
restrictions on the use of aminoclicosides
(impaired kidney function, elderly
age

Carbapenems.

First time
have been isolated from Streptomuces
cattleya. Distinguish
1st generation: imepenem, tienam, primaxin:
2nd generation: meropenem.

This
highly active antibiotics. Their STK
approaching the IPC. They take first
place in terms of activity in relation to
Gram-positive microorganisms, and
for Gram-negative
microorganisms are second only to
fluoroquinolones. Carbapenems have
the broadest spectrum of action among
all currently in use
antibacterial agents: gram-positive
cocci (strepto-, pneumococci),
Gram-negative bacteria (intestinal
coli, Pseudomonas aeruginosa, meningococci,
gonococci, legionella): anaerobic
flora, including B.
Fragilis:
actinomycetes. Moderately active in
against enterococci, Pseudomonas aeruginosa
sticks, listeria. Not valid on
chlamydia, mycoplasma, tuberculosis.

Readings
for use
are severe infections
association of pathogens: infections
urinary tract, pelvis and
abdominal cavity, pneumonia, septicemia,
infections in immunocompromised patients
and agranulocytosis, etc.

From
side effects are possible dyspeptic
disorders, thrombophlebitis, eosinophilia,
pseudomembranous colitis, arterial
hypotension, increased activity
hepatic transaminases.

Ceftolozane (ceftolozane): description, use, side effects

Contents

• 1 Description of ceftolozane
  • 1.1 Description of ceftolosan
  • 1.2 Medical uses of ceftolozane
  • 1.3 Side effects of cef tolosan
  • 1.4 How to use ceftolosan
  • 1.5 Interactions of ceftolosan with other drugs
  • 1.6 Special instructions for the use of ceftolosan
  • 1. 7 Related videos:
  • 1.8 Q&A:
    • • 1.8.0.1 What is ceftolosan?
      • 1.8.0.2 How is ceftolosan used?
      • 1.8.0.3 Which infections can be treated with ceftolosan?
      • 1.8.0.4 What side effects can ceftolosan cause?
      • 1.8.0.5 Can ceftolosan be used during pregnancy?
      • 1.8.0.6 Are there any contraindications to the use of ceftolosan?
      • 1.8.0.7 Can ceftolosan be used to treat children?
  • 1.9 Special precautions when using ceftolosan
  • 1.10 Preventing side effects of ceftolozane

Ceftolozane is an antibiotic from the cephalosporin group used to treat infections caused by certain types of bacteria. It has a wide spectrum of activity and is effective against a variety of pathogens. Ceftolosan is one of the key drugs in the fight against infections, especially in the hospital environment. In this article you will find a detailed description of the drug, its mechanism of action, indications for use, dosage and side effects.

Ceftolosan is a cephalosporin antibiotic used to treat various infections caused by bacteria. It is a strong and effective antimicrobial agent that is used in hospitals and other healthcare facilities.

The drug ceftolosan is widely used to treat urinary tract, lung, skin and soft tissue infections. It has a broad spectrum of activity and is effective against many types of bacteria, including Gram-negative and some Gram-positive.

However, like any antibiotic, ceftolosan can cause some side effects. Some of these include allergic reactions, diarrhea, nausea and vomiting. In some cases, serious side effects may occur, such as anemia, increased sensitivity to sunlight, and impaired liver function.

Ceftolosan is an important drug in the treatment of infections caused by bacteria, especially in immunocompromised patients. However, before starting treatment, it is necessary to consult a doctor in order to avoid possible side effects and get the maximum benefit from this drug.

Product description ceftolosan

Ceftolosan is an antibiotic belonging to the fourth generation cephalosporin class. It is active against a wide range of bacteria, including gram-negative and gram-positive microorganisms.

Ceftolosan is often used in combination with tazobactam, which is a beta-lactamase inhibitor. This combination provides a wider spectrum of action and increases the effectiveness of the drug.

Ceftolosan is used to treat infections of the respiratory tract, urinary tract, skin and soft tissues, and infections caused by certain types of bacteria, including Pseudomonas.

Ceftolosan is usually taken intravenously by infusion into a vein. The dosage and duration of taking the drug depend on the type of infection and the recommendations of the doctor. It is necessary to strictly follow the instructions of the doctor and not stop taking the drug without his permission.

It is important to note that ceftolosan may cause side effects including diarrhea, nausea, vomiting, headache, increased sensitivity to sunlight and others. If you experience any unusual symptoms or side effects after taking the drug, you should contact your doctor.

Before you start taking ceftolosan, tell your doctor about all the medicines you are taking, including over-the-counter medicines and nutritional supplements. Any allergic reactions to antibiotics or other drugs should also be reported.

Medical use of ceftolosan

Ceftolozane is an antibiotic used in medicine to treat various infections. It belongs to the class of cephalosporins and has a wide spectrum of action, which allows it to be used to combat various pathogenic microorganisms.

Ceftolosan is used to treat urinary tract infections, including acute pyelonephritis and acute cystitis. It can also be used to treat bronchial and lung infections, including those complicated by chronic obstructive pulmonary disease (COPD) or cystic fibrosis.

Ceftolosan is often used in combination with another antibiotic, such as tazobactam, to enhance its effectiveness and broaden its spectrum of action. Combination therapy may be necessary to treat infections caused by multidrug-resistant organisms.

Ceftolosan is available as an injection solution that is injected into a vein or muscle. The dosage and duration of treatment depend on the type and severity of the infection, as well as on the condition of the patient. Before using ceftolosan, it is necessary to evaluate the sensitivity of the microorganism to the drug.

It is important to note that ceftolosan is a prescription drug and should only be used with a doctor’s prescription. Patients should follow the instructions of the doctor and not stop treatment without his consent, even if the symptoms of the infection have disappeared.

Side effects of ceftolozane

Ceftolozane is a cephalosporin antibiotic used to treat various infections caused by bacteria resistant to other antibiotics. However, like all medicines, ceftolosan can cause side effects in some patients.

A list of possible side effects from taking ceftolosan includes:

• Diarrhea
• Taste changes
• Headache
• Possible allergic reactions such as skin rash or itching
• Possible increase in certain liver enzymes
• Possible decrease in certain blood cells such as platelets or white blood cells

If you experience any side effects from taking ceftolosan, it is important to see a doctor so that he can assess their severity and decide whether to continue treatment with this drug. In some cases, it may be necessary to change the dosage or change the drug to another antibiotic.

Please note that this list of side effects is not exhaustive and other side effects may occur. Always follow your doctor’s instructions and check with your doctor if you experience any new symptoms or sensations while taking ceftolosan.

How to use ceftolosan

Ceftolosan is an antibiotic used to treat infections caused by certain types of bacteria. It is used only on prescription and is available in powder form for solution for injection.

Before you start using ceftolosan, it is important to consult your doctor and read the instructions for use. The following are general guidelines for using ceftolosan:

1. Ceftolosan is usually given intravenously (into a vein) as an injection. The dosage and mode of administration are determined by the physician depending on the type of infection, the condition of the patient and other factors.
2. The solution for injection must be prepared according to the instructions. Ceftolosan powder is usually dissolved in a special solvent, which must also be provided with the drug.
3. The resulting solution should be clear or slightly yellowish. If the solution has a different color or contains visible particles, its use should be discontinued and a doctor should be consulted.
4. Ceftolosan is usually given intravenously over a period of time. The duration of the course of treatment depends on the characteristics of the infection and the recommendations of the doctor.
5. It is important to observe the regularity and accuracy of taking ceftolosan. Do not skip prescribed doses or change dosage without your doctor’s instructions.
6. If you experience side effects while taking ceftolosan, tell your doctor right away. Some of them may require medical attention.

It is important to remember that these recommendations are general and may be modified by the clinician depending on the individual patient and infection characteristics. Therefore, always follow the doctor’s instructions and do not self-medicate.

Ceftolosan is a powerful antibiotic that may be effective in treating certain infections. However, it should only be used as prescribed by a doctor, in compliance with all recommendations and instructions.

Interactions of ceftolosan with other drugs

Ceftolosan may interact with some other drugs, which may lead to changes in their effectiveness and side effects. Before starting treatment with ceftolozane, it is important to tell your doctor about all medications you are taking, including prescribed prescription drugs, over-the-counter drugs, as well as vitamins and nutritional supplements.

The following is a list of some medicines that may interact with ceftolosan:

• Probenicide: Probenicide may increase the concentration of ceftolosan in the blood, which may increase its action and cause side effects. With the simultaneous use of ceftolosan with probenicide, it is necessary to carefully monitor the patient’s condition and, if necessary, adjust the dosage.
• Antiepileptic drugs: Some antiepileptic drugs, such as carbamazepine, phenytoin and phenobarbital, may reduce the concentration of ceftolosan in the blood. With the simultaneous use of ceftolosan with these drugs, it may be necessary to adjust the dosage of ceftolosan.
• Drugs that reduce gastric acidity: Drugs such as antacids, proton pump inhibitors and histamine receptor antagonists may reduce the absorption of ceftolosan in the stomach. With the simultaneous use of ceftolosan with these drugs, it is recommended to take them at least 2 hours before or after taking ceftolosan.

This is not a complete list of medicines that may interact with ceftolosan. It is important to consult your doctor or pharmacist before starting treatment with ceftolosan and to inform you of all medications you are taking.

Special instructions for the use of ceftolosan

1. Individual intolerance

Before starting treatment with ceftolosan, it is necessary to establish the absence of individual intolerance to this drug. To do this, allergic tests are carried out, which allow you to identify possible reactions of the body to the substance.

2. Diseases of the kidneys and liver

In the presence of diseases of the kidneys and liver, it is necessary to take ceftolosan with caution. In such cases, it is recommended to regularly monitor the function of these organs.

3. Pregnancy and lactation

Ceftolosan can cross the placental barrier and be excreted in breast milk. Therefore, its use during pregnancy and lactation is possible only under strict medical indications and under the supervision of a physician.

4. Influence on the ability to drive vehicles and work with mechanisms

Ceftolosan may cause dizziness and drowsiness. Therefore, during treatment, you should refrain from driving vehicles and working with dangerous mechanisms that require increased concentration.

5. Interactions with other medicinal products

Ceftolosan may interact with some other medicinal products, which may change their effectiveness or cause side effects. Before starting treatment with ceftolozane, you should consult your doctor about possible interactions with other drugs.

6. Compliance with the dosage and mode of administration

To achieve maximum effectiveness and prevent the development of bacterial resistance, it is necessary to strictly adhere to the dosage and mode of administration of ceftolosan, indicated in the instructions for use or prescribed by a doctor.

7. Shelf life and storage conditions

Ceftolosan should be stored in its original packaging at a temperature not exceeding 25°C. The expiration date of the drug is indicated on the package. After the expiration date, the drug should be discarded.

Related videos:

Q&A:

What is ceftolosan?

Ceftolozane is an antibiotic that belongs to the group of cephalosporins. It is used to treat infections caused by various bacteria.

How is ceftolosan used?

Ceftolosan is usually administered intravenously, that is, injected into a vein. The dosage and duration of treatment depend on the type and severity of the infection, as well as on the individual characteristics of the patient.

Which infections can be treated with ceftolosan?

Ceftolosan is used to treat urinary tract infections, including complicated kidney infections. It can also be used to treat infections of the gastrointestinal tract, lungs, and skin.

What side effects can ceftolosan cause?

Various side effects may occur with the use of ceftolosan, including diarrhea, nausea, vomiting, headache, elevated liver enzymes, and others. If you experience any side effects, you should contact your doctor.

Can ceftolosan be used during pregnancy?

Ceftolosan should only be used during pregnancy if the benefit outweighs the potential risk to the fetus. It is necessary to consult a doctor.

Are there any contraindications to the use of ceftolosan?

Ceftolosan is contraindicated in case of allergy to antibiotics of the cephalosporin group or to any of the components of the drug. It is also not recommended for use in severe renal impairment.

Can ceftolosan be used to treat children?

Ceftolosan is not recommended for the treatment of children under 18 years of age, as its safety and efficacy in this age group have not been established.

Special precautions when using ceftolosan

Ceftolosan is an antibiotic indicated for the treatment of various infections. However, before using it, a few special precautions must be taken into account:

1. Before starting treatment with ceftolosan, it is necessary to conduct a sensitivity test to this drug. This will help to avoid possible allergic reactions and unwanted side effects.
2. It is important to consider that ceftolosan may interact with other drugs. Before using it, you should consult your doctor or pharmacist to avoid unwanted effects.
3. Ceftolosan may cause diarrhea. If you have a gastrointestinal problem while taking this drug, call your doctor right away.
4. In the event of an allergic reaction such as hives, swelling of the throat or difficulty breathing, seek immediate medical attention. This may be a sign of a serious allergic reaction to ceftolosan.
5. Ceftolosan may adversely affect kidney function. If you have kidney problems, talk to your doctor before taking this drug.
6. It is recommended to refrain from drinking alcohol while taking ceftolosan. Alcohol can increase the side effects of the drug and reduce its effectiveness.
7. Ceftolosan is not recommended during pregnancy and breastfeeding, as its effects on the fetus and infant have not been adequately studied. If you are planning a pregnancy or are breastfeeding, please consult your doctor before starting treatment.

With all the above warnings, the use of ceftolosan should be under medical supervision. In case of unwanted side effects or other problems, you should immediately seek medical help.

Prevention of side effects of ceftolosan

To reduce the risk of side effects when using ceftolosan, the following precautions are recommended:

1. Compliance with the dosage and regimen. It is necessary to strictly follow the instructions of the doctor and not to exceed the recommended dose of the drug. It is also important to take ceftolosan at the indicated time.
2. Avoidance of alcohol. When taking ceftolosan, it is not recommended to drink alcohol, as this may increase the undesirable effects of the drug and increase the risk of adverse reactions.
3. Compliance with hygiene rules. Hygiene practices, including regular hand washing and body cleanliness, are essential to prevent infections and superinfection.
4. Taking the drug with food. Ceftolosan can be taken with or without food, however, taking it with food may help reduce possible stomach side effects.