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The discovery of cephalosporins is credited to Italian pharmacologist and politician Giuseppe Brotzu. He was the first one to isolate cultures of Cephalosporium acremonium in sewer water off the coast of Sardinia in 1948.The initial isolate was then modified to create the cephalosporins that were first introduced into clinical use in 1964 and are still being used today.

The cephalosporin antibiotics are most similar to the penicillins in both structure and mechanism of action. Like penicillins, cephalosporins are bactericidal (kill bacteria) and disrupt the bacteria from building a strong cell wall. Without this critical, outer protective covering of the bacteria, the bacteria ruptures and dies.

Cephalosporins are most commonly and effectively used to treat outpatient indications of pneumonia, skin and soft tissue infections, sinusitis, urinary tract infections, and ear infections. The specific indication dictates which of the cephalosporins will be prescribed, as it is critical for the doctor to select a drug with the appropriate spectrum of activity.

The most commonly used classification system categorizes cephalosporins using the term "generations." Like penicillins that are categorized into groups, cephalosporins are divided into generations based on their chemical structure, pharmacologic activities, and antimicrobial coverage. To date, there are four well-known generations of cephalosporins, plus only one FDA-approved advanced and/or fifth-generation cephalosporin.

The first-generation cephalosporins (ex. Cephalexin and Cefadroxil) are often used for skin infections caused by S. aureus and Streptococcus. The second-generation cephalosporins (ex. Cefprozil and Cefuroxime) are used primarily for respiratory tract infections because they are more effective against H. influenza. The third-generation cephalosporins (ex. Cefdinir and Cefixime) are useful for more severe community-acquired respiratory tract infections, resistant infections, and nosocomial or hospital-acquired infections.

Cefepime is the only agent classed as a fourth-generation cephalosporin and is generally prescribed for intra-abdominal infections, respiratory tract infections, and skin infections. Finally, Ceftaroline fosamil is the only agent FDA approved and classed as a fifth-generation cephalosporin, but it has yet to be studied for pediatric use.

Across all generations, cephalosporins are relatively well tolerated. Still, the most common complaints are gastrointestinal upset, resulting in nausea, vomiting, or diarrhea. Should the patient experience any unusual bleeding, especially severe diarrhea with blood, the doctor should be contacted immediately. Similarly the doctor should be contacted if the patient experiences rash, hives, or difficulty breathing, as these may be signs of hypersensitivity.

This is a good time to mention that there is potential cephalosporin cross-sensitivity in patients with a true penicillin allergy (4% to 10% of cases) that has been observed predominantly with first-generation cephalosporins. Depending on the condition being treated and the severity of the underlying penicillin allergy, the doctor may or may not choose to use a cephalosporin.

Lastly with regards to administering cephalosporins to children, taking the medication with food may alleviate some of the commonly reported GI symptoms.

Depending on which medication is being used, refrigeration may or may not be recommended. For instance, cephalexin recommends refrigerating the suspension, while cefdinir recommends storing the suspension at room temperature. That is why it is extremely important to follow the Instructions as indicated on the prescription bottle or by the pharmacist.

Regardless of which agent is prescribed, it is of utmost importance to complete the full course of the drug, even if the child feels better before the course of treatment is over. Discontinuing therapy can lead to persistent infection, spread of disease, complications, and future resistance. These consequences are avoidable if the medication is taken exactly as directed, so aid your child in proper medication adherence.

By Ursula Chizhik, PharmD

Ursula Chizhik, PharmD earned her Pharmacy Doctorate degree at the University of Maryland School of Pharmacy. She was a retail pharmacist for 11 years before making the switch to join the FLAVORx team. FLAVORx has been helping children take their medicine since 1994. She is now the resident pharmacist and Director of Pharmacy Programs at FLAVORx, Inc. Ursula lives in Marriottsville, Maryland with her husband and two sons. She welcomes you to contact her via email at
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Author:Chizhik, Ursula
Publication:Pediatrics for Parents
Article Type:Report
Geographic Code:1USA
Date:Jul 1, 2014
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