Cephalosporins third generation

CEPHALOSPORINS, THIRD GENERATION Cefdinir (Omnicef) Cefpodoxime (Vantin)... 

Disulfiram Cephalosporins, third-generation Rifampin Vitamin ... 

Neonate Group streptococcus, E coli, Listeria Ampicillin + cephalosporin (third-generation) Ampicillin + aminoglycoside, chloramphenicol, meropenem... 

Peritonitis due to ruptured viscus Conforms, fragilis Metronidazole + cephalosporin (third-generation), piperacillin/tazobactam Carbapenem, tigecycline... 

Neisseria meningitidis Penicillin G Chloramphenicol, cephalosporin (third-generation)3... 

Salmonella TMP-SMZ, quinolone, cephalosporin (third-generation) Chloramphenicol, ampicillin... 

Low molecular weight heparins Extended spectmm penicillins First-generation cephalosporins Second-generation cephalosporins Third-generation cephalosporins Proton pump inhibitors blockers 5HT3 inhibitors Fluroquinolones Oxazolidinones/streptagramins Parenteral amino acids Sedative hypnotics Enteral feedings Insulins... 

Cephalosporins - third generation Chloramphenicol Penicillin G Corticosteroids ( ) [13]... 

It should be noted that the classification iato generations is not chronological, and so some second-generation compounds came to the market relatively recendy, after the third-generation was firmly estabUshed. Within each class there is also a further classification as to whether the compounds are administered orally or parenteraHy. A contemporary variation of the generation classification has been proposed, but has not found widespread use (85). Another proposal groups cephalosporins according to clinical indication or appHcation (86). 

The antibacterial spectmm of moxalactam (Table 9) is similar in breadth and potency to that of cefotaxime (36). Hence, moxalactam (48) is classified with the third-generation cephalosporins. In general 1-oxacephalosporins are considerably more susceptible to P-lactamases than their sulfur counterparts... 

Cephalosporins first entered the marketplace in 1964, when cephalothin (27) and cephaloridine (51), which are both injectable, were launched. By the late 1970s, the injectable cephalosporins had become important therapeutic agents in the hospitals. Also in 1964 the first oral cephalosporin, cephaloglycin [3577-01 -3] C gH N OgS, was launched only to be displaced by the end of the year by cephalexin (12). For years cephalexin was the leading oral cephalosporin on the market. It has since been displaced by cefaclor (13). With the advent of the more -lactamase stable cephalosporins such as cefoxitin (23) and cefuroxime (35), and the more potent agents such as cefotaxime (36) and other third-generation compounds, cephalosporins now dominate the antibiotic market worldwide. 

Cefsulodin (60) has a sulfonic acid nx)iety on the C-7 acyl side chain. This moiety conveys antipseudomonal activity to certain penicillins, and it is interesting to note that this artifice works with cefsulodin as well. It is also interesting that, in contrast to the other so-called third-generation cephalosporins, the spectrum of cefsulodin is rather narrow and its clinical success will place a premium upon accurate diagnosis. Its synthesis begins by acylation of... 

Cefmenoxime (61) is a third generation parenteral cephalosporin whose in vitro antimicrobial spectrum approximates that of cefotaxime. Its side chains consist of the common methyltetrazo lylthio group at C-3 and the familiar oximinoether aminothiazole moiety at C-7. It is synthesized... 

Cefpiramide (64) is a third generation cephalosporin with a l-methyl-[lH)-tetra2ol-5-ylthio-methyl moiety at C-3 and an acylated -hydroxyphenylglycine moiety at C-7. It includes in its activity spectrum reasonable potency in vitro against many strains of Pseudomonas. It can be synthesized in a variety of ways including condensation of cephalosporin antibiotic 63 with 6-methyl-4-(l-H)-pyridone-3-carboxylic acid in the form of its active N-hydroxysuccinimide ester (62) to produce cefpiramide (64) [20,21],... 

Cefoperazone (66) is a third generation parenteral antipseudomonal cephalosporin containing an acylated C-7 side chain reminiscent of that of piperacillin. One of the simplest syntheses... 

Class A Serine p-lactamases SHV-1 penicillinase in K. pneumoniae, and Koxy with activity against certain third generation cephalosporins in K. oxytoca BlaZ staphylococcal penicillinase TEM, SHV, VEB, PER and CTX-M penicillinases and ESBLs (P-lactamases with activity against third generation cephalosporins and aztreo-nam) KPC, IMI/NMC and SME carbapenemases... 

Explain the difference between the first-, second-, and third-generation cephalosporins. 

DISPLAY 8-1 Examples of First-, Second-, and Third-Generation Cephalosporins... 

Uncomplicated exacerbation Not requiring hospitalization Less than 3 exacerbations per year No comorbid illness I I V, greater than 50% predicted No recent antibiotic therapy Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis Oral Macrolide (azithromycin, clarithromycin) Second- or third-generation cephalosporin (cefuroxime, cefpodoxime, cefdinir, cefprozil) Doxycycline Ketolide (telithromycin) P-Lactam/P-Iactamase inhibitor (amoxicillin-clavulanate) Intravenous Not recommended... 

Complicated exacerbation FEV, less than 50% predicted Comorbid cardiac disease Greater than or equal to 3 exacerbations per year Antibiotic therapy in the previous 3 months Above organisms plus drug-resistant pneumococci, P-lactamase-producing H. influenzae and M. catarrhalis, Escherichia coli, Proteus spp., Enterobacter spp., Klebsiella pneumoniae Oral P-Lactam/P-Iactamase inhibitor (amoxicil 1 i n-clavulanate) Fluoroquinolone with enhanced pneumococcal activity (levofloxacin, gemifloxacin, moxifloxacin) Intravenous P-Iactam/P-Iactamase inhibitor (ampicillin-sulbactam) Second- or third-generation cephalosporin (cefuroxime, ceftriaxone) Fluoroquinolone with enhanced pneumococcal activity (levofloxacin, moxifloxacin)... 

Initiation of prophylactic antibiotics is recommended during acute variceal bleeding this is typically done with an oral fluoroquinolone (e.g., ciprofloxacin 500 mg twice daily x 7 days) or an IV third-generation cephalosporin. Prophylactic antibiotic therapy reduces in-hospital infections and mortality in patients hospitalized for variceal bleeding.44... 

Traditionally, high-dose penicillin G was the treatment standard for meningococcal disease. However, increasing penicillin resistance requires that third-generation cephalosporins now be used for empirical treatment until in vitro susceptibilities are known.23 Patients with a history of type I penicillin allergy or cephalosporin allergy may be treated with vancomycin. Treatment should be continued for 7 days, after which no further treatment is necessary. 

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