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USU Pharm lec 58
Antibiotics I
Question | Answer |
---|---|
Name the B-Lactams | Penicillins, Cephalasporins, Carbapenems, Monobactam |
B-lactam mechanism | inhibits transpeptidase from cross-linking the D-ala--D-ala substrates (Dala-Dala analogue) |
B-lactam mechanisms of resistance | increased penicillinases. decreased affinity of PBPs (mutation & recombination). decreased cell membrane permeability. energy-dependent efflux pumps. |
B-lactam adverse effects | Allergic, diarrhea, CV effects, CNS, Coagulation defects |
acid stable antibiotic, active against gram-positive (non-penicillinase), also Neisseria and some anaerobes | Penicillin V |
penicillinase-resistant penicillins | methicillin (also nafcillin, oxacillin, cloxacillin, dicloxacillin) |
Methicillin resistance (MRSA) | related to failure to bind PBPs |
1st penicillin for gram-neg. Active against E.coli, P. mirabilis, H.influenza, Salmonella, Shigella, Neisseria | ampicillin (also amoxicillin) |
Cephazolin (also cephalexin, cephadrine, cefadroxil) | 1st Gen cephalosporin. narrow spectr. surg prophylax. most gram +, moderate against gram -. |
Cefotetan | 2nd Gen ceph. B. fragilis, other anaerobes. intra-abdominal surg prophylaxis |
2nd Gen Cephalosporins | increased activity against Gram - (E.coli, P.mirabilis). |
3rd Gen cepalosporins | CNS, bone, lung, urinary tract penetration. Gram -, enteric bacteria |
Ceftazidime | 3rd Gen ceph. for multi-drug resistant Gram - like P. aeruginosa |
First drug approved for MRSA | ceftaroline (3rd Gen ceph) |
Cefepime | 4th Gen Ceph. like ceftazidime against P. aeruginosa & other Gram -. resistance to chromosomally-encoded B-lactamases |
Imipenem (also meropenem, ertapenem, doripenem) | Carbapenems. IV only. |
"may not always have cross-allergenicity with penicillin" vs "usually does not show cross-allergenicity" | may not: imipenem. usually does not: aztreonam |
Carbapenem with extremely broad spectr, B-lactamase reist, | imipenem |
Aztreonam | Monobactam. Gram -. |
Vancomycin | Glycopeptide Antibiotic. binds D-ala-D-ala terminus. |
no cross-resistance/allergenicity. used for serious staph/strep infection in B-lactam sensitive patients | vancomycin |
Daptomycin | inhibit cell membrane potential lipopeptide antibiotic. For complicated skin infections, endocarditis by gram +. |
clavulanate | "suicide inhibitor" of B-lactamase, given with a penicillin ie Augmentin(amoxicillin + clavulanate), Timentin (ticarcillin + clavulanate) |
cilastatin (in drugs to know list at cilastin) | dipeptidase inhibitor (given in combo with imipenem to preven renal tubule hydrolyzation) |
ticarcillin | carboxylated penicillin derivative. anti-pseudomonal |