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Pharm Exam V > Antibacterials > Flashcards

Antibacterials Flashcards

1
Q

Functions of beta lactams?

Bacteriostatic or bacterocidal?

Beta lactam drug classes?

A

Beta lactams inhibit cell wall synthesis. Irreversibly inhibit transpeptidase and prevent cross links of peptidoglycan leading to autolysis.

ALL are bacteriocidal

Penicillins, Carbapenems, Monobactams, and Cephalosporins

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2
Q
  1. First generation penecillin drugs?
  2. Antistaphylococcal penecillins?
  3. Amino penecillins?
  4. Carboxy penecillins?
  5. Ureido penecillin?
A
  1. 1st gen: penicillin G and penecillin V
  2. Antistaph: Dicloxacillin, Nafcillin, and Oxacillin
  3. Amino: amoxacillin and ampicillin
  4. Carboxy: Ticarcillin
  5. Ureido: piperacillin
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3
Q

Penecillin G:

  1. Oral administration is used for?
  2. IV is used for?
  3. Not used for?
A

Penecillin G:

  1. Oral is for aerobic and anaerobic infections of the head and neck, recurrent streptococcal cellulitis in those with lymphedema, and prevention of recurrent rheumatic fever
  2. IV: aerobic GPC (pneumococcus, strep. pyogenes/pneumoniae), aerobic GPR (b. anthracis), aerobic/faculative anaerobe GNC (nisseria), anaerobic GPR (clostridium), anaerobes (EXCEPT_ bacteroides_), and spirochetes (Treponema, boriella, and leptospira)
  3. Not used for staph infections - resistant.
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4
Q

Anti-staphylococcal penecillins:

(Dicloxacillin, Nafcillin, and Oxacillin)

Use?

A

Anti-staphylococcal penecillins:

Used for METHACILLIN sensitive staph aureus (MSSA) as they are resistant to Staph Beta lactamase, ineffective against MRSA

Also used for skin and soft tissue infections

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5
Q

Aminopenecillins (amoxicillin/ampicillin):

  1. Resistance?
  2. Benefit of positive charge? Benefit of acid resistance?
  3. Amoxicillin is DOC for?
  4. Also used for?
A

Aminopenecillins:

  1. NO resistance to beta-lactamases
  2. Positive charge enhances diffusion; acid resistance so can give orally
  3. Amoxicillin is DOC for Otitis media/H influenza
  4. Used for high risk patients to prevent endocarditis, a variety of GPCs (enterococcus), GNCs (N. gonorrheae/meningitidis), and GNRs (E. coli, Salmonella, and proeus mirabilis)
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6
Q

Carboxypenecillin/Ticarcillin:

  1. Similar spectrum as? With the addition of?
  2. Used to treat?
A

Carboxypenecillin/Ticarcillin:

  1. Similar spectrum as the amino penecillins with the addition of activity against several GN organisms in the family of enterobacteriaceae
  2. Used to treat Enterobacter and pseudomonas
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7
Q

Ureido/Piperacillin:

  1. Resistance?
  2. Spectrum of action is similar to? It also has what additional activity?
A

Ureido/Piperacillin:

  1. Not resistant to beta-lactamases
  2. Spectrum is similar to carboxypenecillins (so amino penecillins + enterobacterieae) as well as activity against Klebsiella and enterococci
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8
Q

What drug has exrection that is hepatic and not renal (like all the rest)?

Penecillin antagonism?

A

Nafcillin has hepatic excretion

Antagonism:

a. Bacteriostatic abx (chloramphenicol, macrolides, tetracyclines) interfere wtih their activity
b. Ampicillin, amoxicillin, and penicillin v lowers estrogen levels (recudes effectiveness of oral contraceptives)
c. Low pH, dextrose/aminoglycoside solutions: inactivate B-lactams in solution but are synergistic in vivo

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9
Q

Penecillin synergy/potentiation?

A

Synergy

Piperacillin and Ticarcillin - can inhibit platelet aggregation (potentiates effects of anticoagulants)

probenecid blocks renal excretion - keeps active b-lactam in blood longer

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10
Q

Types of adverse reactions?

A

Adverse reactions:

a. allergy
b. GI
c. Hematologic reactions
d. CNS toxicity
e. Phlebitis
f. Interstitial nephritis

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11
Q

Penecillins: Adverse Reactions:

Allergies?

GI?

Hematologic?

A

Penecillins: Adverse Reactions:

Allergy: skin rash (Ampicillin and amoxicillin induced skin rash may not be allergy related)

GI: D/N/V can occur with any b-lactam (most common with amoxicillin/clavulanate acid), oral candidiasis, and colitis (most common with Ampicillin or amoxicillin) and may lead to super infection with C. Difficile (treat with metronidazole)

Heme: both piperacillin and ticarcillin may inhibit platelet agg, and predispose very ill/malnourished patients to bleeding episodes

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12
Q

Penecillins: Adverse Reactions:

CNS toxicity?

What can cause phlebitis?

All penecillins can cause?

A

Penecillins: Adverse Reactions:

CNS: b-lactams are GABA antagonists: penecillin G in high concentrations may cause irritability, tremors, and seizures

Nafcillin can cause phlebitis at the injection site

ALL PENICILLINS can cause interstitial nephritis

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13
Q

Drugs that counter resistance to beta lactams?

A

Amoxicillin/Clavulinic acid and Ampicillin/sublactam (treat s. aureus, h. influenza, klebsiella, acinetobacter, and anaerobes)

Piperacillin/Tazobactam

Ticarcillin/clavulinic acid

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14
Q

What are the carbapenems?

Resistance?

A

Carbapenems:

a. Doripenem
b. Ertapenem
c. Imipenem
d. Meropenem

Extremely resistant to B-lactamases

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15
Q
  1. Doripenem uses?
  2. Ertapenem uses?
  3. Impenem/cilastin uses?
  4. Meropenem uses?
A
  1. Doripenem: complicated intra-abdominal infections and UTIs
  2. Ertapenem: mod-severe intra-abdominal infections, complicated UTIs, acute pelvic infections, and prophylaxis in colo-rectal surgery
  3. Impenem: serious intra-abdominal, UT, skin/skin structure, lower RT, gynecologic, bone, joint, and polymicrobic infections. Also septicemia and endocarditis
  4. Meropenem: complicated intra-abdominal infections, complicated skin/skin structure infections, and bacterial meningitis
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16
Q

Carbapenems:

  1. Bactericidal or bacteriostatic?
  2. Spectrum?
  3. Why is impenem co-administered with cilastin?
A

Carbapenem:

  1. Bactericidal
  2. Broad spectrum - GPC, GNR, anaerobic bacteria. NOT effective for MRSA
  3. Co-administer impenem with cilastin to prevent degradation by renal enzymes
17
Q

Carbapenems:

Interactions?

Adverse reactions/contraindications?

A

Carbapenem:

Interactions:

a. Probenecid - decreases secretion of carbapenem
b. Valproic acid (carbapenem causes decreased level of valproic acid)

Adverse reactions:

HA/N/D, anemia, seizures, rash, and cross-hyperreactivity in PCN allergic patients (contraindicatied in patients with anaphylaxis to beta-lactams)

18
Q

Aztreonam (monobactam)

  1. Particularly useful when?
  2. Uses?
  3. Spectrum?
A

Aztreonam (monobactam)

  1. Particularly useful with severe penecillin allergies (no cross reactivity) however, there is cross reactivity to ceftazadime
  2. Uses: UTI, lower RTI, skin/skin structure infections, intra-abdominal, gynecological, and surgical infections, and septicemia
  3. G- aerobes ONLY (pseudomonas). No activity against G+ or G- with extended spectrum beta lactamases
19
Q

Aztreonam (monobactam):

Drug interactions?

Adverse reactions? (parenteral vs. inhalation)

A

Atrezonam (monobactam):

Drug interactions:

a. Aminoglycosides - nephrotoxicity and ototoxiciy
b. Other B-lactam abx - antagonize aztreonam

Adverse reactions:

a. Parenteral: low incidence F/N/D, dyspnea, seizures, and rash
b. Inhalation: cough, wheezing, nasal congestion, fever, pharyngolaryngeal pain, chest discomfort, and ab. pain

20
Q

Cephalosporins:

  1. First generation drugs? Target?
  2. Second generation drugs? Target?
  3. Third generation drugs? Target?
  4. Fourth generation drugs? Target?
  5. Fifth generation drugs? Targets?
A

Cephalosporins:

  1. Cefazolin and Cephalexin - G+
  2. Cefuroxime and cefotetan - G-
  3. Cefdinir, Cefpodoxime, Ceftazidime, and Ceftriaxone - G-
  4. Cefepime - G-
  5. Ceftaroline - G+/G-/MRSA
21
Q

1st Generation Cephalosporins: Cefazolin/Cephalexin:

Spectrum?

A

1st Gen Cephalosporins: Cefazolin/Cephalexin:

Spectrum:

a. G+ cocci: very active against strep. pyogenes (Group A strep), strep agalactiae (Group B strep), and viridans strep
b. Less G- activity: E. coli, proteus mirabilis, and klebsiella pneumoniae
c. Anaerobes: active against most penicillin-susceptible anaerobes found in the oral cavity, except bacteriodes fragilis

22
Q

1st Generation Cephalosporins: Cefazolin/Cephalexin:

Uses?

A

1st Generation Cephalosporins: Cefazolin/Cephalexin:

Uses:

a. Uncomplicated skin/soft tissue and urinary tract infections
b. Respiratory tract infections due to penecillin-sensitive Strep pneumoniae
c. Parenteral for surgical wound prophylaxis

BACTERIOCIDAL

23
Q

2nd Gen Cephalosporins: Cefuroxime:

Spectrum?

Uses?

A

2nd Gen Cephalosporins: Cefuroxime:

Spectrum:

a. G+: comparable to 1st gen against Strep and MSSA, otherwise slightly less active against G+
b. G-: H. influenzae, N. Meningitidis, and some Enterobacteriacaea (E.coli, klepsiella, and proteus)

Uses: community-acquired URTI and LRTI (h. influ, strep pneumoniae), sinusitis, otitis media, and uncomplicated UTIs (E. coli)

24
Q

Special 2nd Gen Cephalosporin: Cefotetan:

Spectrum?

Uses?

A

Special 2nd Gen Cephalosporin: Cefotetan:

Spectrum:

Less G+ than other second generations; G- improved activity against Enterobacteriaceae; Anaerobes - active against most anaerobes in the mouth and colon (Bacteroides)

Uses:

a. Mixed anaerobic/aerobic infections of skin/soft tissues, intra-abdominal/gynecological infections
b. Surgical prophylaxis

25
Q

3rd Gen Cephalosporins: Cefdinir/Cefpodoxime/Ceftazidime/Ceftriaxone:

Spectrum?

Uses?

A

3rd Gen Cephalosporins: Cefdinir/Cefpodoxime/Ceftazidime/Ceftriaxone:

Spectrum: Broad:

a. G+: decreased activity compared to 2nd gen - except Ceftriaxone: excellent against Strep pneumoniae (including those that are PCN resistant)
b. G-: DOC against N. gonorrhoeae (use Ceftriaxone), good activity against enterobacter and Serratia, most poor coverage of pseudomonas except Ceftazidime

Uses: broad including gonorrhea and pseudomonas

26
Q

4th Gen Cephalosporin: Cefepime:

Spectrum?

Uses?

A

4th Gen Cephalosporin: Cefpime:

Spectrum:

a. G+: better than 3rd gen. Active against Strep pneumoniae and Groups A/B streptococci; less active against MSSA than 1st/2nd gen- otherwise similar spectrum against G+ as 1st gen
b. G-: great for Enterobacteriaceae adn Pseudomonas aruginosa (similar to ceftazidime)

Uses: same as 3rd gen, though its suggested that use be limited to nosocomial sepsis and can cross BBB so effective for meningitis

27
Q

5th Gen Cephalosporin: Ceftaroline:

Spectrum?

Uses?

A

5th Gen Cephalosporin: Ceftaroline:

Spectrum: Anti-MRSA activity

a. G+: Strep pneumoniae/pyogenes/agalactiae and staph aureus
b. G-: H. influenzae, Klebsiella pneumoniae/oxytoca, and E. coli

Uses (limited to prevent resistance)

a. Community-acquired bacterial pneumonia (CABP) when S. aureus, MSSA only
b. Acute bacterial skin/skin structure infections when S. aureus, MRSA, and MSSA

28
Q

Cephalosporins are generally not active against?

What tends to become resistant?

A

Cephalosporins generally not active against: MRSA (ex-ceftaroline), enterococcus, penicillin resistant s. pneumoniae, listeria, legionella, clostridium, campylobacter, or acinetobacter

Enterobacter tend to become resistant

29
Q

Carbapenems, Monobactams, and Cephalosporins:

  1. Distribution?
  2. Increased toxicity?
  3. Antagonism?
A

Carbapenems, Monobactams, and Cephalosporins:

  1. Distribution: generally high renal levels and low CSF (except Ceftriaxone and Cefepime)
  2. Alcohol may induce disullfiram effects (flushing, cramps, nausea, sweating) in conjunction with NMTT cephalosporins (Cefotetan)
  3. Antacids/H2 blockers interfere with absorption of oral cephalosporins; bacteriostatic abx interfere with all B-lactams; and Low pH, dextros/aminoglycosie solutions inactivate B-lactams
30
Q

Carbapenems, Monobactams, and Cephalosporins:

  1. Potentiation?
  2. Cephalosporin adverse reactions?
A

Carbapenems, Monobactams, and Cephalosporins:

  1. Probenecid blocks renal excretion of B-lactams and thus they stay in blood longer
  2. Cephalosporin AE:
    a. may receive ceph. even if PCN allergy as lont as NO anaphylaxis history
    b. colitis (in broad spectrum)
    c. directly toxic to renal tubular epithelium
    d. Prolonged use of Ceftriaxone causes biliary sludging
    e. Cefotetan) may cause bleeding disorders; admin with Vit K
31
Q

Carbapenems, Monobactams, and Cephalosporins:

  1. Carbapenem adverse reactions?
  2. Adverse reactions of all B-lactams?
A

Carbapenems, Monobactams, and Cephalosporins:

  1. Carbapenem AE:
    a. Impenem: super infections
    b. Impenem/Meropenem: dizziness or headache
  2. ALL B-lactam AE:
    a. D/N/V
    b. Oral candidiasis in prolonged therapy
    c. GABA antagonists: in [high] - irritability, tremor, seizures
    d. Phlebitis at injection site
32
Q

Resistance to all B-lactams:

  1. Chromosomal?
  2. Acquired?
  3. Resistance between B-lactam groups?
A

Resistance to all B-lactams:

  1. Chromosomal: efflux pumps, G+ can mutate transpeptidase encoding gene (eg. S. aureus and pneumococci)
  2. Acquired__ by plasmid: B-lactamases (easily transferred) and G- make less but concentrat more in the periplasmic space and are more resistant to penicillins (eg. C. perfringes)
  3. Resistance to one does NOT = resistance to another. EG:
    a. S. aureus, Haemophilus, and E. coli - B-lactamases hydrolyze penicllins but not cephalosporins BUT:
    b. pseudomonas A. and enterobacter: hydrolyze both
33
Q

Inhibitors of Murein monomer synthesis:

Drug?

MOA?

Uses?

A

Inhibitor of murein monomer synthesis:

Bacitracin

MOA: interferes with bactoprenol pyrophosphate, rendering this lipid carrier useless for further rounds of monomer translocation; ONLY cell wall agent with a LIPID target

Uses: topical for skin/ophthalmologic infections; oral for C. difficile or VRE (vancomycin resistant enterococci) infections in GI (not primary though); too toxic for systemic use

34
Q

Inhibitors of murein polymer synthesis:

Drug?

MOA?

Use? IV vs PO?

A

Inhibitor of murein polymer synthesis:

Vancomycin:

MOA: inhibits transglycosidase and thereby blocks the addition of murein units to polymer chain (binds terminus of monomer peptide unit) BACTERICIDAL

Use__s: Exclusively GPR and GPC that are resistant to other abx (limited use due to toxicity)

IV - MRSA and MRSE (multi-drug resistant staph epidermidis), penicillin resistant strep pneumoniae, enterococci (not VRE)

PO - C. difficile entercolitis (if metronidazole resistant)

35
Q

Vancomycin:

  1. Route of administration?
  2. Serious adverse reactions?
  3. Common Adverse reactions?
  4. Resistance?
A

Vancomycin:

  1. Poor absorption GI, IV for systemic infections, NO IM
  2. Serious AE: nephrotox and ototox (esp used with other drugs that cause this), neutropenia, and anaphylaxis
  3. Common AE: red man syndrome due to histamine release from rapid IV infusion, drug fever, hypersensitivity rash, and drug induced neutropenia

4 Resistance: starting to be seen (VRSA = vancomycin resistant staph aureus), plasmid mediated

Pharm Exam V (6 decks)

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