03a: Antibacterial Agents Flashcards
List the four sites of antibiotic action.
- Cell wall synthesis
- Protein synthesis
- Nucleic acid synthesis
- Folic acid synthesis
List the classes of antibiotics that target cell wall synthesis. Star the beta lactams
- Penicillins*
- Vancomycin
- Beta-Lactamase Inhibitors
- Cephalosporins*
- Carbapenems*
Penicillin is (bactericidal/bacteriostatic) and (time/conc)-dependent.
Bactericidal; time-dependent
Mechanism of action of beta lactams is (stim/inhib) of (X), followed by bacterial cell (Y).
Inhibition;
X = PBPs (cross link peptide chains of peptidoglycan)
Y = lysis (via osmotic P or autolysins)
Natural penicillins, such as (X), primarily target gram (pos/neg) (aerobes/anaerobes) and is treatment of choice for which situations/infections?
X = penicillin G
Gram-pos aerobes (strep);
- Strep (GAS pharyngitis)
- Syphilis
Extended spectrum penicillins differ from natural penicillins in that they have greater:
access/ability to penetrate through O.M. of gram negatives
Aminopenicillins, such as (X), have coverage similar to penicillin G with (more/less) coverage for:
X = ampicillin; more
- Enterococcus
- Listeria
- Enterobacteriaceae
T/F: Aminopenicillins have very broad range of coverage for gram positives.
False
T/F: Penicillinase-resistant penicillins have very broad range of coverage for gram positives.
True
Drug of choice for endocarditis prophylaxis (i.e. via enterococcus).
Aminopenicillins (ex: ampicillin)
T/F: Most penicillins must be given by IV or IM to achieve adequate levels.
True (degraded by gastric acid)
T/F: Penicillins distribute well into most tissues, particularly bone/CSF.
False - less so in bone/CSF, though CSF levels are 5-20% of serum levels
Penicillins are mainly excreted (changed/unchanged) via which route?
Unchanged;
Renal (rapid)
Most common adverse effect of penicillins.
Hypersensitivity (3-10%), though anaphylaxis is rare
T/F: There may be cross-reactivity between penicillins and cephalosporins, but not other beta-lactams.
False - can be cross-reactivity between any of those
Beta-Lactamase Inhibitor example.
Clavulanic acid
Cephalosporins have which mechanism of action?
They’re beta-lactams! Similar to penicillins (inhibit PBPs)
(X) is a first-generation cephalosporin that acts primarily on which type of bacteria?
X = cefazolin
Gram-positive aerobes (ex: strep, MSSA)
(X) is a second-generation cephalosporin that acts primarily on which type of bacteria? (Y) is also a second-gen drug, but with additional activity against (Z).
X = cefuroxime
Gram-pos (mainly Strep, less Staph) and Gram-neg aerobes;
Y = cefoxitin
Z = gram-neg anaerobes
Which cephalosporin would you likely use to treat respiratory infections and community acquired pneumonia?
Cefuroxime (second generation)
(X) is a third-generation cephalosporin that acts primarily on which type of bacteria?
X = ceftriaxone Gram pos (mainly Strep, less Staph) and gram neg aerobes (less than fourth gen)
Which cephalosporin would you likely use to treat strep pneumo and gram negative infections?
Gen 3 (ceftriaxone)
Which cephalosporin would you likely use to treat hospital-acquired Pseudomonas?
Gen 4 (cefepime)
T/F: Gen 4 cephalosporins have no gram-positive acitivty.
False - similar to Gen 1 activity
T/F: Cephalosporins have no activity against anaerobes.
False - Cefoxitin(a gen 2) does against gram-neg anaerobes
Aside from (X), the pharmacokinetics of cephalosporins are similar to (Y) drugs.
X = ceftriaxone (longer half-life and biliary excretion) Y = penicillins
T/F: Cephalosporins have adverse effects/toxicity overall similar to penicillins.
True
Carbapenems have which mechanism of action?
They’re beta-lactams! Similar to penicillins (inhibit PBPs)
Carbapenems: (X) is combined with (Y) to prevent:
X = imipenem Y = cilastatin
Imipenem brakdown to nephrotoxic product
List the three mechanisms that pathogens use for antimicrobial resistance.
- Efflux of drug
- Alteration of drug
- Degradation of drug
(X) are broad-spectrum agents, generally reserved for documented resistance activity. These agents work on gram (pos/neg) (aerobes/anaerobes).
X = carbapenems
Gram pos and neg aerobes and anaerobes
Most common adverse effect of carbapenems are:
GI disturbances
T/F: Vancomycin is a beta-lactam that’s bactericidal and time-dependent.
Partly false - it’s a glycopeptide (not beta-lactam)