Pharm Cephalosporins
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| 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.
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| cephalosporins are | penicillinase resistant
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| cephalosporins Work | only in actively growing cells.
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| cephalosporins are drugs of 1st choice in | Klebsiella infxns
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| 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)
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| Drug of 1st choice in H. influenzae inf is | Ceftriaxone
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| Cephalosporins MOA | Bactericidal, they inhibit cell wall synthesis.
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| Cephalosporins have higher beta-lactimase resistance due to | different side chain than beta lactam ring.
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| Cephalosporin Distribution | Good in soft tissue and relatively good in bone.
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| Cephalosporin toxicity | GI disturbances after oral administration, Reversible renal impairment requiring dose reduction. Hypersensitivity reactions.
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| 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.
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| 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
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| 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
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| Gen 1 Cephalosporins | Cephalexin(1), Cephradine, Cephapirin, Cefazolin, Cefadroxil
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| Gen 2 Cephalosporins | Cefaclor(1), Cefuroxime Axetil, Cefprozil, Cefoxitin Na, Cefonicid Na, Cefotaxime Na, Cefotetan Disodium
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| Gen 3 Cephalosporins | Ceftriaxone Na(1), Ceftazidime, Ceftizoxime, Cefoperazone Na, Cefepime
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| Gen 1 Cephalosporins to know | Cephalexin (PO and acid stable), Cefazolin (IM)
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| Gen 2 Cephalosporins to know | Cefaclor(PO), Cefotaxime Na(IM)
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| Gen 3 Cephalosporins to know | Ceftriaxone Na (H. Influnzae, IM) Ceftazidime (gram neg. sepsis, IM)
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| Carbapanems | Imipenem/Cilistatin, Meropenem
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| Carbapanems MOA | Bind to penicillin binding protein-2 (PBP-2) + transpeptidase: remarkable degree of penicillinase resistant(by b-lactimase enzymes)
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| Carbapanems spectrum | BROADEST of any B lactam (even 3rd gen Cephalosporins): Gram neg and pos (including Pseudomonas), anaerobes (incl. bacteroides
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| Carbapanems used in | Mixed infections (abdominal and pelvic wounds...GSW)
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| Carbapanems administered | IM
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| Carbapanems side effects | NV, C. diff diarrhea, cross allergenicity w/penicillin, phlelbitis GI problems(pseudomembranous colitis)
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| 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.
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| 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.
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| Cephalosporin Drug interactions | probenecid increases blood levels of cephalosporins, esp those excreted primarily by tubular secretions.
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