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Cephalosporins • First Generation Cephalosporins • Second Generation Cephalosporins • Third Generation Cephalosporins • Fourth Generation Cephalosporins Cephalothin (IV) G1 Spectrum Adverse Reactions Special Properties Pharmoco-kinetics Drug Clinical Reactions Uses Similar to ampicillin except effectPCNs); against:pain Common allergic rxn (less than Klebsiella Inadequate infections CSF penetration (80%) - notfor DOC meningitis • Klebsiella pneumoniae and absess at IM inj site (less with Can be usedfor with pts allergic to Alternative Possible potentiation penicillinase-resistant ofinnephrotoxicity staph. Elimination -caution primarily RTS • Penicillinase-producing staphylococci (not MRSA or cefazolin); NVD; + coombs test PRSP) and many gram + (proximal necrosis) with concurrent PCNs but(NOT nottubular those with immediate infection MRS or PRSP) • E. coli, P. mirabilis use of aminoglycosides, loop diuretics, or hypersensitivity rxn • Somewhat against H. Staph. infections ininfluenzae most PCN allergic pts • NOT for enterococci,probenecid listeria, or MRS NOT FOR MRS, PRSP, • Staphylococci (and other gram +) - cephalothin > cefazolin enterococcal/listeria/B. frag, or CNS • Gram - bacilli - cefazolin > cephalothin infections or meningitis Cefazolin (IV) G1 Adverse Drug Reactions Reactions Pharmoco-kinetics Special Properties Spectrum Clinical Uses Common allergic rxn except (less than Inadequate CSF penetration forPCNs); meningitis Similar- to ampicillin effect against: pain Klebsiella infections (80%) - notwith DOC and absess at IM inj site (less • Klebsiella pneumoniae Possible potentiation ofinnephrotoxicity Can be used with caution pts allergicstaph. to Alternative for penicillinase-resistant cefazolin);tubular NVD;necrosis) + coombswith test • (proximal Penicillinase-producing staphylococci (not concurrent MRSA or Cefazolin - gram elim. > RTS; longer t/2 PRSP) andnot many + GFimmediate PCNs but those with infection (NOT MRS or PRSP) use of aminoglycosides, loop diuretics, or • E. coli, P. mirabilis hypersensitivity rxn probenecid Staph. infections most PCN allergic pts • Somewhat against H.in influenzae •NOT NOTFOR for enterococci, or MRS - MRS,listeria, PRSP, • Staphylococci (and other gram +) - cephalothin > cefazolin enterococcal/listeria/B. frag, or CNS • Gram - bacilli - cefazolin > cephalothin infections or meningitis Cephalexin (PO) most used oral (Keflex) G1 Spectrum Adverse Pharmoco-kinetics Reactions Special Drug Clinical Reactions Properties Uses Similar to ampicillin except effect against: Common Inadequate -infections allergic CSF rxn penetration (less- than for PCNs); meningitis pain Klebsiella (80%) not DOC • Klebsiella pneumoniae and absess at IM inj site (less with Elimination primarily RTS Can Alternative Possible be usedfor potentiation with penicillinase-resistant caution ofinnephrotoxicity pts (not allergic staph. to • Penicillinase-producing staphylococci MRSA or cefazolin); NVD; + coombswith test concurrent PRSP) and many gram +necrosis) (proximal tubular PCNs infection but(NOT not those MRS with or PRSP) immediate • E. coli, P. mirabilis use of aminoglycosides, loop diuretics, or • Somewhat against H. influenzae hypersensitivity Staph. infectionsrxn in most PCN allergic pts • NOT for enterococci,probenecid listeria, or MRS NOT FOR MRS, PRSP, • Staphylococci (and other gram +) - cephalothin > cefazolin enterococcal/listeria/B. frag, or CNS • Gram - bacilli - cefazolin > cephalothin infections or meningitis Cefadroxil (PO) G1 Drug Reactions Special Adverse Properties Reactions Spectrum Pharmoco-kinetics Clinical Uses Similar to ampicillin except effect against:pain Common allergic rxn (less than PCNs); Inadequate CSF penetration for meningitis Klebsiella infections (80%) - not DOC • Klebsiella pneumoniae and absess at IM inj site (less with to Possible potentiation of nephrotoxicity Can be used with caution in pts allergic Elimination primarily RTS Alternative for penicillinase-resistant staph. • Penicillinase-producing staphylococci (not MRSA or cefazolin); NVD; + coombs test (proximal tubular necrosis) with concurrent PRSP) andnot many gram + t/2 PCNs but those with immediate Cefadroxil -MRS longer for less frequent infection (NOT or PRSP) aminoglycosides, loop diuretics, or • E.use coli,of P. mirabilis dosing hypersensitivity rxn Staph. infections inprobenecid most PCN allergic pts • Somewhat against H. influenzae • NOT for enterococci, NOT FOR - MRS,listeria, PRSP,or MRS • Staphylococci (and other gram +) - cephalothin > cefazolin enterococcal/listeria/B. frag, or CNS • Gram - bacilli - cefazolin > cephalothin infections or meningitis Cefadroxil (PO) G1 Spectrum Similar to ampicillin except effect against: Pharmoco-kinetics • Klebsiella pneumoniae • Penicillinase-producing staphylococci (not MRSA or Adverse Reactions Inadequate CSF penetration for meningitis PRSP) and many gram + Drug Reactions allergic rxn (less RTS than PCNs); pain •Common E. coli, P. mirabilis Elimination - primarily Special • Somewhat against and absess at H. IMinfluenzae injProperties site (less with • NOT for enterococci, listeria, or MRS test cefazolin); NVD; + coombs ClinicalofUses Possible potentiation nephrotoxicity • Staphylococci (and other gram +) - cephalothin > cefazolin (proximal tubular necrosis) concurrent Can be -used with caution in pts allergic to infections -with not DOC •Klebsiella Gram bacilli - cefazolin >(80%) cephalothin use of aminoglycosides, loop diuretics, or PCNs but not those with immediate Alternative for penicillinase-resistant staph. Second Generation Cephalosporins (Cefamandole-Like) Note some have MTT side chains Cefamandole (IV) prototype G2 Uses Clinical Special Properties Above the diaphragm drugs Pharmoco-kinetics Adverse Reactions Spectrum Drug Reactions stgeneration Similar toto first cephalosporins plus: "Day Care Similar 1Drugs" generation except: Two to 8X greater activity against H.allergic influenzae Can be used with caution in pts toto Primarily for ampicillin-resistant Cefamandole may cause bleeding (due Possible Elimination primarily RTS potentiation of nephrotoxicity (including ampicillin resistant) PCNs but not those with immediate H.influenzae infections (sinusitis, otitis (proximal tubular necrosis) with concurrent vit. K inhibition) and disulfuram-like rxn; More active against Klebsiella, E. coli, and indole + use of aminoglycosides, loop diuretics, or hypersensitivity media, URIs, these are due to rxn MTT side chain at R2 proteus probenecid NOT effective against enterococci, listeria, or MRS Cefuroxime (IV) Cefuroxime Axetil (PO) G2 Spectrum Special Pharmoco-kinetics Properties Drug Adverse Reactions Reactions Clinical Uses Similar to first generation cephalosporins plus: CSF penetration forthan meningitis Common allergic rxn (less PCNs); pain Above the diaphragm drugs Two to 8X greater activity against H. influenzae and absess at resistant) IM injwith site (less Cefuroxime - only adequate Possible Elimination - 2G primarily RTSwithCSF potentiation of nephrotoxicity "Day Care Drugs" (including ampicillin cefazolin); NVD; +t/2; coombs test penetration; longer side+chain More activefor against Klebsiella, E.no coli,MTT and indole (proximal tubular necrosis) with concurrent Primarily ampicillin-resistant H. influenzae proteus use of aminoglycosides, loopURIs, diuretics, or infections (sinusitis, otitis media, cefuroxime Cefuroxime also effective for PPNG probenecid for pneumonias) NOT effective enterococci, listeria, or DOC) MRS Cefuroxime foragainst H. influenzae meningitis (not Cefuroxime is alternative drug for PPNG Cefaclor (PO) oral equiv. of cefamandole G2 Adverse Reactions Drug Reactions Spectrum Pharmoco-kinetics Special Properties Clinical Uses Common - allergic rxncephalosporins (less than Similar to first generation plus: pain Inadequate CSF penetration for PCNs); meningitis Above the diaphragm drugs absess at IM inj site (less with Twoand to 8X greater activity against H. influenzae Possible potentiation of nephrotoxicity be Elimination -caution primarily RTS Can used with in pts allergic to "Day Care Drugs" cefazolin); NVD; + coombs test (including ampicillin (proximal tubularresistant) necrosis) with concurrent PCNs but for not those with immediate Primarily ampicillin-resistant H. More active against Klebsiella, coli,diuretics, and indoleor+ use of aminoglycosides,E. loop hypersensitivity rxnprobenecid influenzae infections (sinusitis, otitis proteus media, cefuroxime for listeria, pneumonias) Cefaclor -URIs, cheapest NOT effective against enterococci, or MRS Cefprozil and Loracarbef (PO) G2 Spectrum Drug Reactions Pharmoco-kinetics Special Properties Adverse Reactions Above the diaphragm drugs Similar to first generation cephalosporins plus: Inadequate CSF penetration for meningitis Common allergic rxn (less than PCNs); pain "Day Care Drugs" Two to 8X greater activity against H. influenzae Possible potentiation ofinRTS nephrotoxicity and absess at IM inj site with H. be used with caution pts allergic to Can Elimination primarily (including ampicillin resistant) (less Primarily for ampicillin-resistant (proximal tubular necrosis) with concurrent cefazolin); NVD; + coombs test PCNs Cefprozil but not andthose Loracarbef with immediate -(sinusitis, PO indole More active against Klebsiella, E.better coli, and influenzae infections otitis + use of aminoglycosides, loop diuretics, or absorption proteus media, rxn URIs, cefuroxime for hypersensitivity probenecid NOT effective against enterococci, listeria, or MRS pneumonias) Cefprozil - may be more stable against beta lactamase producing strains of staph, H. flu, and Morazella Second Generation Cephalosporins (Cefoxitin-Like) Note some have MTT side chains Cefoxitin (IV) prototype G2 Spectrum Pharmoco-kinetics Adverse Reactions Special Drug Clinical Reactions Properties Uses Similar to first generation cephalosporins but with Inadequate CSF penetration forPCNs); meningitis enhanced activity against: Common allergic rxndrugs (less than pain Below the -diaphragm Bacteroides fragilis and absess at IM inj site (less Elimination -Expensive primarily RTSwith PPNG Possible potentiation of nephrotoxicity Other bacteroides species -anaerobes (cefoxitin > cefazolin); NVD; + coombs test cefotetan) (proximal tubular withinfections concurrent Tx of abdominal andnecrosis) gynecologic N. Gonorrhoeae (including PPNG) loop diuretics, or use of aminoglycosides, where B. fragilis suspected Gram - enteric aerobicis bacilli (Klebsiella, E. coli, probenecid some serratia) cefotetan cefoxitin Urinary tract, lower>respiratory tract, soft NOT effective against enterococci, listeria, or MRS tissue infections (cefotetan) < active against H. flu and enterobacter than cefamandole Cefotetan (IV) G2 Spectrum Special Drug Reactions Properties Adverse Pharmoco-kinetics Reactions Clinical Uses Similar to first generation cephalosporins but with enhanced Common Inadequate - allergic CSFrxn penetration (less PCNs); meningitis pain Below the diaphragm drugsthanfor activity against: Bacteroides fragilis and absess at IM- primarily inj may siteof(less with Expensive; Possible cefotetan potentiation have nephrotoxicity cost advantage PPNG Elimination RTS Other bacteroides species -anaerobes - (cefoxitin > cefotetan) cefazolin); NVD; + coombs test (proximal since it can tubular be administered necrosis) with less concurrent frequently Cefotetan - has and long t/2 (4.5 hrs) infections N. (including PPNG) TxGonorrhoeae of abdominal gynecologic use of aminoglycosides, loop diuretics, Gram - enteric aerobic bacilli (Klebsiella, E. coli, some Cefotetanmay cause bleeding (due to serratia) vit.or K– where >B. fragilis is suspected cefotetan cefoxitin probenecid inhibition) and disulfuram-like rxn; these NOT effective against enterococci, listeria, or MRS Urinary tract, lower respiratory tract, soft are due to MTT side chain at R2 Less active against H. flu and enterobacter than cefamandole tissue infections (cefotetan) Cefmetazole (IV) G2 Spectrum Clinical Uses Adverse Reactions Pharmoco-kinetics Special Properties Similar to first generation cephalosporins but with enhanced Below the diaphragm drugs Common - allergic rxn (less than PCNs); pain activity against: Inadequate CSF penetration for meningitis Bacteroides fragilis PPNG andElimination absessspecies at IM inj site (less cefazolin); --anaerobes primarily RTS>with Other bacteroides - (cefoxitin cefotetan) Expensive Gonorrhoeae PPNG) NVD; +(including coombs test TxN. of abdominal and gynecologic Drug Reactions Gram - enteric aerobic bacilli (Klebsiella, E. coli, some serratia) – Cefmetazole - may cause bleeding (due to vit. cefotetan > cefoxitin infections where B. fragilis is suspected Possible potentiation of nephrotoxicity NOTK effective against enterococci, listeria, or MRS inhibition) and disulfuram-like rxn; these Less active tract, against tubular H.lower flu and enterobacter thanwith cefamandole (proximal necrosis) concurrent Urinary respiratory tract, soft are due to MTT side chain at R2 use of aminoglycosides, loop diuretics, or tissue infections (cefotetan) infections or probenecid meningitis Third Generation Cephalosporins • • • • • • • Ceftriaxone (IV) - Rocephin Cefotaxime sodium (IV) Ceftizoxime sodium (IV) Ceftazidime pentahydrate (IV) Cefoperazone (IV) Moxalactam disodium (IV) Cefixime (PO) Ceftriaxone (IV) Rocephin G3 Spectrum Pharmoco-kinetics Adverse Clinical Reactions Uses More active against many enteric gram - aerobes; Ceftriaxone longest t/2 of all Ceftriaxone Common -coli, -allergic DOC for rxn PPNG (less proteus, than but does PCNs); not pain DOC for E. Indole positive cephalosporins (8inj hrs); excreted in bile (OK and absess at IM site (less with cover chlymadia; PRSP; H. ducreyi and Providencia, Serratia for CRF) NVD; + coombs test cefazolin); Generally lessAmpicillin-resistant active against gram + H. organisms than Salmonella; flu st generation 1 meningitis (good CSF penetration); pts in Very effective against H. influenzae and N. renal failure gonorrhoeae (including PPNG), NOT effective against enterococci, listeria, or MRS Cefotaxime sodium (IV) & Ceftizoxime sodium (IV G3 Spectrum Pharmoco-kinetics Clinical Uses More active against many enteric gram - aerobes; DOC for E. better CSF- DOC penetration for meningitis Ceftriaxone for PPNG but does not coli, Indole positive proteus, Providencia, Serratia cover Elimination - PRSP; primarily chlymadia; H. RTS ducreyi and Generally less active against gram + organisms than 1st Salmonella; generation Ampicillin-resistant H. flu Very effective against H. influenzae and N. gonorrhoeae meningitis (good CSF penetration); pts in (including PPNG) renal failure NOT effective against enterococci, listeria, or MRS Ceftazidime pentahydrate (IV) G3 CeftriaxoneAdverse -Drug DOC Reactions for Reactions PPNG but does not Spectrum More active-chlymadia; against manyrxn enteric gram - aerobes; cover PRSP; H. ducreyipain and Common allergic (less than PCNs); DOCSalmonella; for E. coli, Indole positive proteus, Ampicillin-resistant H. flu and absess at IM inj site (less with Pharmoco-kinetics Possible potentiation of nephrotoxicity Providencia, Serratia meningitis (good CSF penetration); pts in cefazolin); NVD; + coombs test (proximal tubular necrosis) with concurrent Generally less active against gram + organisms than G1 Same as G1 renal failure Veryuse effective against H. influenzae N. diuretics, or of aminoglycosides, and loop gonorrhoeae (including PPNG), NOT effective probenecid against enterococci, listeria, or MRS Ceftazidime - most active cephalosporin against P. aeruginosa (cefoperazone also good but not given alone) Cefoperazone (IV) G3 Pharmoco-kinetics Spectrum Adverse Reactions Clinical Uses More active against manyMTT enteric gram - aerobes; Cefoperazone -have excreted in bile (OK for Cefoperazone side chain and may Cefoperazone Pseudomonas infection that is DOC for E. coli, Indole positive proteus, CRF); poor CNSbleeding penetration than other G3s have increased and disulfuram-like not in the CNS and pt has renal failure Providencia, Serratia rxn less active against gram + organisms than Generally 1st generation Very effective against H. influenzae and N. gonorrhoeae (including PPNG), NOT effective against enterococci, listeria, or MRS Moxalactam disodium (IV) G3 Pharmoco-kinetics Adverse Reactions Spectrum Clinical Uses More active against enteric gram - may aerobes; moxalactam havemany MTTPPNG side chain and Ceftriaxone - -DOC for but does not DOC for E. coli, Indoleand positive proteus, have increased bleeding disulfuram-like chlymadia; PRSP;Serratia H. ducreyi and cover Elimination - primarily RTS Providencia, rxn Salmonella; Ampicillin-resistant H. flu than Generally less active against gram + organisms meningitis (good1stCSF penetration); pts in generation renal Veryfailure effective against H. influenzae and N. gonorrhoeae (including PPNG), NOT effective against enterococci, listeria, or MRS Cefixime (PO) G3 Spectrum Adverse Reactions Pharmoco-kinetics Clinical Uses More active against many enteric gram - aerobes; Cefixime - diarrhea Cefixime PPNG single dose Serratia DOC for E. -coli, Indolevia positive proteus,oral Providencia, less active against gram + organisms than Generally Elimination - primarily RTS 1st generation Very effective against H. influenzae and N. gonorrhoeae (including PPNG), NOT effective against enterococci, listeria, or MRS • Cefixime - poor activity against staph Cefepime (IV) G4 Parenteral only “Broadest” Gram neg and Gram Pos Spectrum of cephalosporins Low affinity for gram Neg blases, does not induce blases 100% renal excretion T1/2 – 2.2 hrs Cephalosporins with MTT Side Chain • G2 Cephalosporins – Cefamandole – Cefotetan – Cefmetazole • G3 Cephalosporins – Moxalactam – Cefoperazone Cephalosporin activity against Gram Positives G1> G2>G3>G4 Cephalosporin activity against Gram Negatives/Stability to GN Blases G4> G3>G2>G1