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54 Cards in this Set
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- Back
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Beta-Lactams |
(PACC) Penicillins, cephalosporins, aztreonam, carbapenems |
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Beta-Lactams MOA |
Bactericidal and Time-Dependent *Bind to penicillin binding proteins that are responsible for formatino of peptidoglycan cell wall. Inhibit cell wall synthesis Activate endogenous autolytic system |
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Beta-Lactam Resistance |
*Inactivation by B-Lactamase enzymes, hydrolyse B-lactam ring (staph) Alteration of PBP (strep, MRSA) Decrease in cell wall permeability (psudomonas) |
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Natural Penicillins |
Parenteral: Penicillin G (IV), Penicillin G Procaine (IM), Penicillin G Benzathine (IM) Oral: Penicillin VK |
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Natural Penicillins - Spectrum |
G(+): Streptococci (B & G), Staphylococci, Enterococci, Listeria G(-): Neisseria meningitidis Anaerobic: Fair, used in dental infections (G(+) Anaerobes); not B. fragilis Other: Treponema pallidum |
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Penicillinase Resistant Penicillins |
Parenteral: Methicillin, Oxacillin, Nafcillin Oral: Dicloxacillin, Cloxacillin |
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Penicillinase Resistant - Spectrum |
G(+): Staph and Strep (not S. pneumoniae) G(-): None Anaerobes: None |
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Aminopenicillins |
Parenteral: Ampicillin Oral: Amoxicillin & Ampicillin |
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Aminopenicillin - Spectrum |
G(+): Strep, enterococci, listeria G(-): non-beta-lactamase producing enterobacteria (H. influenzae and pylori) Anaerobes: None, especially G(-) anaerobes |
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Carboxypenicillins |
Parenteral: Ticarcillin Oral: carbenicillin |
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Carboxypenicillins - Spectrum |
G(+): Lower than aminopenicillin and ureidopenicillins G(-): Enterobacteraceae (more than aminopenicillins) and P. aeruginosa Anaerobes: not reliable |
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Ureidopenicillins |
Parenteral: *piperacillin, mezlocillin |
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Ureidopenicillins - Spectrum |
G(+): Enterococci, streptococci (no staph) G(-): Enterobacteracae, *psuedomonas (good against) Anaerobes: not reliable |
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B-lactam/b-lactamase Inhibitors |
Parenteral: Ampicillin/sulbactam, ticarcillin/cavulanate, pipracillin/tazobactam Oral: Amoxicillin/clavulanate |
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B-lactam/b-lactamase inhibitor - spectrum |
G(+): Same as parent, improved staph protection G(-): B-lactamase producing organisms Anaerobes: Good,, including B. fragilis Better for G(-) aerobes and anaerobes |
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Beta-Lactams Absorbtion |
Oral: most destroyed by gastric acid. Acid Stable: dicloxacillin, amoxicillin, ampicillin. Food delays absorbtion IM: Treat syphilis. Benzathine below, procaine peaks |
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Beta-Lactam Distribution |
Good tissue penetration [- eyes, prostate, and CNS (CNS penetration increased with inflammation)] Protein binding highly variable |
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Beta-Lactam Metabolism |
Minimal/no metabolism Short half-life: requires multiple daily dosing |
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Beta-Lactam Elimination |
Majority is renal, requires renal dose adjustment Exceptions: Nafcillin and oxacillin are liver |
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Cephalosporin Classes |
1st Gen: Good G+, some G- 2nd: less G+, more G- 3rd: Some G+, even more G- 4th: Good G+ and good G- |
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Cephalosporins do NOT cover |
MRSA - not true anymore Enterococci |
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Cephalosporin absorption |
oral tends to be good, some food restrictions |
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Cephalosporin distribution |
Similar to penicillin 3rd and 4th penetrate CSF |
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Cephalosporin Metabolism |
Ceftriaxone and cefoperazone are partially metabolized, no renal dose adjustment necessary
Cefotaxime deaceylated by liver to active metabolite, which is renally excreted |
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Cephalosporin Elimination |
Most elimated via kidneys, require renal dose adjustment Longer T1/2 than penicillin, so less frequent dosing |
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Cephalosporin 1st Gen Agents |
Parenteral: Cefazolin Oral: Cephalexin, cefadroxil, cefaclor |
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Cephalosporin 1st Gen Spectrum |
G(+): Staph and strep (not strep pneumoniae) G(-): some E. coli, Klebsiella Anaerobes: none |
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Cephalosporin 2nd gen agents |
Parenternal: Cefuroxime, cefotetan, cefoxitin, cefonicid, cefmetazole Oral: Cefuroxime, cefpodoxime, cefprozil, loracarbef |
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Cephalosporin 2nd Gen Spectrum |
G(+): Staph and Strep (S. Pneumoniae unreliable) G(-): Same as 1st, but also H. influenzae and M. catarrhalis Anaerobes: none Exception: Cefoxitin and cefotetan same as 1st gen, and enhanced anaerobic coverage |
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Cephalosporin 3rd gen agents |
Parenteral agents: ceftriaxone, cefotaxime, ceftizoxime, ceftazidime, cefoperazone Oral: Ceftibuten, cefdinir, cefditoren |
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Cephalosporin 3rd gen spectrum |
Ceftriazone and cefotaxime: G(+): Staph and strep (inluding PCN Resistant pneumonococci) G(-): same as 2nd gen, with N. gonorrheae and enterobacteriacease Anaerobic: none Exceptions: Ceftizoxime -same as above but less penumonococcal; Ceftazidime - poor G+, G- same but covers P. aeruginosa |
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Cephalosporin 4rd Gen |
Cefepime G(+): Strep and Staph G(-): e. coli, klebsiella, h. influenzae, m. catarrhalis, n. gonorrhoeae, enterobacteriacae, p. areuginosa Anaerobes: none |
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Cephalosporin 5th Gen |
Ceftaroline Enhanced affinity to PBP G(+): Staph, including *MRSA, oral anaerobes, s.pneumoniae G(-): H. influenzae, M. catarrhalis, E. coli, K. pneumoniae |
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Cephalosporin ADR |
Hypoprothrombinemia and bleeding: Agents with MTT side chain (cefamandole, moxalactam, cefmetazole, cefotetan, and cefoperazone); inhibit vitamin k clotting factors Disulfram reactions with alcohol |
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Carbapenems |
Last line of defense against G(-) Inc: imipenem, meopenem, doripenem, ertapenem |
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Carbapenem absorption/distribution |
Absorption: poor, all available are IV Distribution: good in most tissues |
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Carbapenem metabolism/elimination
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Metabolism: Imipenem is metabolized by dehydropeptidase in brush border of kidney, cilastatin prevents this degredation Elimination: Renal, requires dose adjustment |
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Carbapenem Spectrum |
Broad Imipenem/meropenem/doripenem: Very good G+, MRSA; Great G- and anaerobic Ertapenem: same, but no activity against p. aeruginosa or enterococcus |
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Carbapenem ADR |
Cross RXN with penicillin Seizures |
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Monobactams |
Aztreonam Aerobic gram negative only No beta-lactam ring - use in G(-) pts. who are allergic |
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Aztreonam PK |
Absorption: Poor, only IV Distribution: Good Metabolism: none Elimation: Renal, dose adjust |
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Aztreonam ADR |
Hypersensitivty uncommon - no cross reactivity with PCN allergy |
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Bacterial Folate Antagonists |
Benzene ring Bacteriostatic |
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Bacterial Folate Antagonist Resistance |
Overproduction of PABA Alternate pathways/use of exogenous FA intake Mutations in dihydropteroate synthase (target enzyme) Loss of cell wall permeability |
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Short Acting Folate Antagonists |
Sulfamethizole: UTI, not systemic Sulfisoxazole: UTI, combine with erythromycin for otitis media |
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Intermediate acting Folate Antagonists |
Sulfadiazine: with pyrmethamine for toxoplasmosis and malaria Sulfamethoxazole: UTI, and above |
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Long Acting Folate Antagonists |
Sulfadoxine: Malaria Tx |
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Poorly absorbed folate antagonists |
Sulfasalazine: Ulcerative colitis or crohn's disease |
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Co-trimoxazole |
Trimethoprim-sulfamethoxazole aka bactrim, TMP-SMX Good synergist, 20 SMX:1 TMP *Dose based on trimethoprim |
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TMP-SMX Absorption/Distribution |
Absorbed well Distribution: TMP more lipid soluble, larger Vd. Protein binding is good (40% TMP, 65% SMX) Distributes well in most tissues, including lung, CSF, urine |
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TMP-SMX Metabolism/Elimination |
TMP not metabolized, SMX is acetylated with active metaboltes TMP Excreted unchanged in urine, 3-% SMX is excreted unchanged Renal Dose Adjustment Necessary |
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TMP-SMX Spectrum |
G(+): Staph (not MRSA), Strep (not S. pneumoniae), Listeria G(-): Haemophilus, moraxella, enterobacteriacae Misc: pneumocystis carinii, nocardia, GI pathogens |
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TMP-SMX ADRs |
Rashes, SJS syndrome Crystalluria Hemolytic Anemia (G6PD Deficiency) |
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TMP-SMX Interaction |
Increases Warfarin effects, bleeding risk Displaces protein bound drugs - phenytoin Risk of kernicterus in pregnancy - causes encephalopathy in neoborns |
