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Nursing Margaret Scofield 280-2245 Criss III rm 577 Chemistry: beta-lactam ring: Unique properties of the cephalosporins are determined by the additions to the ring, R1, R2, R3.
Mechanism of Action: Similar to the penicillins. These agents bind to penicillin-binding proteins and both disrupt cell wall synthesis and activate autolysins (enzymes that cleave bonds in the cell wall).
Resistance: The principal cause of cephalosporin resistance is production of beta-lactamases, the enzymes that cleave the beta-lactam ring of cephalosporins, and occasionally these same enzymes can also cleave penicillin beta-lactam rings. The cephalosporins are grouped according to when they were discovered, first generation through fourth generation. The first-generation are most easily destroyed by beta-lactamases and the third- through fifth-generation are most highly resistant. In general as you progress from first-generation agents to fifth-generation agents, there is: (a) increasing activity against gram-negative bacteria and anaerobes (b) increasing resistance to destruction by beta-lactamases (c) increasing ability to reach the cerebrospinal fluid.
The exception is ceftriaxone which is eliminated by the liver. VRSA Higher Higher Good Higher Higher Poor PO & IV IV IV Abdominal surgery prophylaxis. febrile neutropenia.Major Differences Between Cephalosporin Generations Class Activity Against GramNegative Bacteria Resistance to BetaLactamases Distribution to Cerebrospinal Fluid Administration Important Indications First Generation: cefazolin Low cephalexin Low Poor IV PO Surgical prophylaxis Non-serious soft tissue or UTI infections Second Generation cefuroxime cefoxitin cefotetan (VitK & disulfuram effects) Third Generation cefdinir ceftriaxone ceftazidime Fourth Generation cefepime Fifth Generation Higher ceftaroline Highest Good IV MRSA. IM IV. . IM Gram negative meningitis Highest Highest Good IV. pneumonia Pharmacokinetics: Distribution to the spinal fluid is only good for the third. Elimination occurs through the kidney and the excretion of most cephalosporins is decreased with probenecids (similar to penicillins) and thus toxicity can increase. IM & Pseudomonas aeruginosa Meningitis.and fourth-generations. hence the first. upper respiratory infections PO IV.and second-generations should not be used to treat meningitis.
Third-Generation cephalosporins have a high activity against gram-negative organisms and can penetrate the CSF and so are the drug of choice for treating meningitis. Instead the third and fourth-generation agents with their very broad antimicrobial spectra. Ceftriaxone forms precipitates with calcium depositing in lungs and kidneys Clinical uses: Cephalosporins are broad-spectrum. especially Clostridium difficile.Adverse Effects: Allergic reactions Bleeding with second generation cephalosporins (cefotetan) and third generations (cefoperazone). ceftazidime). Alcohol interactions: the same drugs mentioned above will induce a state of alcohol intolerance by the build up of acetaldehyde. cefdinir (Omnicef) widely prescribed this season However these drugs should not be used routinely or resistant organisms will develop. They can be useful alternatives for patients with mild penicillin allergies. First-Generation cephalosporins are alternatives to mild penicillin allergies and are used as a prophylaxis against infection in surgical patients. bactericidal drugs.g. Second Generation cephalosporins are limited in use: Cefuroxime has been used against pneumonia caused by Haemophilus influenza. Ceftazidime is the only one that can treat Pseudomonas aueruginosa.e. penicillin or first or second-generation cephalosporin) . should be avoided in situations where a narrower spectrum drug would suffice (i. In addition ceftriaxone and cefotaxime are drugs of choice for treating gonorrhea. Impairment of Vitamin K synthesis and impairment of platelet aggregation. (e.
a dipeptidase inhibitor. aerobic and anerobic Pharmacokinetics: Must be given with cilastatin.Other Beta-Lactam Drugs Carbapenems Imipenem (Primaxin) IV. Side effects: GI. eliminated renally. hypersensitivity. IM Spectrum: Very broad spectrum parenteral drug that is a beta-lactam antibiotic Important for Pseudomonas aeruginosa and Enterococcus species (not MRSA) Mechanism of action: Binds to penicillin binding proteins and penetrates all tissues including CSF Penetrates Gram negative and gram positive cell walls. suprainfections . to prevent degradation of imipenem.