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Pharm Cephalosporins

cephalosporin MOA Bind covalently to active site of transpeptidase enzyme which catalyzes the cross-linking reaction of peptidoglycan polymers in bacterial cell wall synthesis. Bacteria is lysed by osmotic pressure.
cephalosporins are penicillinase resistant
cephalosporins Work only in actively growing cells.
cephalosporins are drugs of 1st choice in Klebsiella infxns
Cephalosporins are used in UTI, Klebsiella infxns, Staph infxns(in patients allergic to penicillins..caution due to cross allerginicity), Gram neg sepsis(+gentamicin or tobramycin)
Drug of 1st choice in H. influenzae inf is Ceftriaxone
Cephalosporins MOA Bactericidal, they inhibit cell wall synthesis.
Cephalosporins have higher beta-lactimase resistance due to different side chain than beta lactam ring.
Cephalosporin Distribution Good in soft tissue and relatively good in bone.
Cephalosporin toxicity GI disturbances after oral administration, Reversible renal impairment requiring dose reduction. Hypersensitivity reactions.
Cephalosporin metabolism and excretion Mainly excreted via kidney, w/tubular secretion mechanism like penicillin, cefoperazone(3rg Gen) excreted mainly in bile, cephapirin(1st Gen) and cefotaxime(2nd Gen) biotransformed to less active metabolites.
Cephalosporin progression from 1st to 3r Gen broadening in activity against gram-negative bacteria and anaerobes, Decreased activity against gram positive bacteria, increased resistance to inactivation by B-lactamase enzymes
Cephalosporin chemistry very similar to penicillin G, Structurally and pharmacalogically similar to penicillins, 10-15% cross sensitivity w/ penicillin so be careful with pts allergic to penicillin
Gen 1 Cephalosporins Cephalexin(1), Cephradine, Cephapirin, Cefazolin, Cefadroxil
Gen 2 Cephalosporins Cefaclor(1), Cefuroxime Axetil, Cefprozil, Cefoxitin Na, Cefonicid Na, Cefotaxime Na, Cefotetan Disodium
Gen 3 Cephalosporins Ceftriaxone Na(1), Ceftazidime, Ceftizoxime, Cefoperazone Na, Cefepime
Gen 1 Cephalosporins to know Cephalexin (PO and acid stable), Cefazolin (IM)
Gen 2 Cephalosporins to know Cefaclor(PO), Cefotaxime Na(IM)
Gen 3 Cephalosporins to know Ceftriaxone Na (H. Influnzae, IM) Ceftazidime (gram neg. sepsis, IM)
Carbapanems Imipenem/Cilistatin, Meropenem
Carbapanems MOA Bind to penicillin binding protein-2 (PBP-2) + transpeptidase: remarkable degree of penicillinase resistant(by b-lactimase enzymes)
Carbapanems spectrum BROADEST of any B lactam (even 3rd gen Cephalosporins): Gram neg and pos (including Pseudomonas), anaerobes (incl. bacteroides
Carbapanems used in Mixed infections (abdominal and pelvic wounds...GSW)
Carbapanems administered IM
Carbapanems side effects NV, C. diff diarrhea, cross allergenicity w/penicillin, phlelbitis GI problems(pseudomembranous colitis)
Carbapanems Pharmacokinetics Parenteral use, good tissue distribution except CSF, Excreted in urine, Degradeted by dehydropeptidase in renal tubule. Administered together w/ cilastatin, an inhibitor of dehydropeptidase-1, increases its urinary concentration.
Cephalosporin resistance development In US 2% of S. aureus (clinically isolated) are resistant, Definate cross resistance exhibied by staph which are resistant to methicillin-type antibiotics.
Cephalosporin Drug interactions probenecid increases blood levels of cephalosporins, esp those excreted primarily by tubular secretions.
Created by: Garzilla