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Antimicrobial > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

Penicillin MOA

A

Time dependent killing
Bind to PBP during cross-linking of cell wall

Resistance: beta lactamases, modification of PBP, efflux, impaired penetration

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2
Q

Penicillin Spectrum

A 
- B-lactamase negative GPC
(S.pneumoniae, S.pyrogens, VGS)
- oral anaerobes (GPs) (actinomyces, peptococcus, petptostretococcus)
- N. meningitis (GN)
- syphilis 
* GRAM POSITIVES**
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3
Q

Penicillin Gaps

A
  • atypical organisms
  • B-lactamase (+) GPCs - Staph
  • aerobic GNB
  • anaerobic GN
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4
Q

Amoxicillin/Ampicillin MOA

A

PCN + more penetration into outer membrane and higher affinity for PBP so increase in GN

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5
Q

Amoxicillin/Ampicillin Spectrum

A

PCN + gram positives including enterococcus

some gram negatives

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6
Q

Amoxicillin/Ampicillin Gaps

A

susceptible to B-lactamases

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7
Q

Piperacillin Spectrum

A

more GN activity
- harder to treat GN  pseudomonas & enterococcus

Gaps in Coverage:
- susceptible to B-lactamases

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8
Q

Piperacillin + Tazobactam Spectrum

A

Useful for where there is resistance! LARGE spect.

  • oral anaerobes
  • GP in general (inc. MSSA)
  • GN in general
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9
Q

Cephalosporins 1st gen

A

cefazolin

cephalexin

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10
Q

Cephalosporins 1st gen spectrum

A 
Coverage: PCN PLUS
- easy to kill GN: E.coli, proteus spp., klebsiella spp
Retain:
- aerobic GPC
- oral anaerobes
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11
Q

Cephalosporins 2nd gen

A

cefoxitin
cefaclor
cefuroxime

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12
Q

Cephalosporins 2nd gen spectrum

A

Coverage: PCN + 1GC PLUS
- gut anaerobes: B. fragillis sp (but resistance high so not often used)

cefuroxime: H.influenza and Moraxella catarrhalis (respiratory organisms)

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13
Q

Cephalosporins 3rd gen

A

Ceftriaxone
Cefotaxime
Ceftazidime

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14
Q

Cephalosporins 3rd gen spectrum

A

Ceftriaxone: 1st GC PLUS broader GNB
Gaps in Coverage: LOSE: Staph activity & anaerobic coverage

Ceftazidime: PCN PLUS broader GNB than 2nd GC (b/c of sidechain which inc. penetration of GN membrane) and Pseudomonas
Gaps in Coverage: LOSE GP coverage** NO strep or staph coverage

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15
Q

Cephalosporins 4th gen

A

Cefepime

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16
Q

Cephalosporins 4th gen spectrum

A

Coverage: 3GC plus more GNs, AmpC

Retain:

  • GP similar to ceftriaxone (3GC)
  • PsA similar to ceftazidime (3Gc)

Gaps in Coverage:
- ESBL

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17
Q

Carbapenems: Meropenem and Imipenem

A

Coverage: added to Pip/tazo OR 3GC

  • oral & gut anaerobes
  • GP in general (inc. MSSA)
  • GN in general
  • ESBL
  • ampC
  • Pseudomonas (M&I)
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18
Q

Carbapenems: Ertapenem

A
  • less activity than mero/imipen against GN

- LOSE: pseudomonas, enterococci, acinetobacter

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19
Q

Vancomycin

A 
Coverage:
- GPs only (b/c too large & polar to cross GN CM)
- C. difficile (po)
- MSSA, MRSA
- PCN resistant strep meningitis 
- enterococcus
“drug of last choice” 
Use when:
- B-lactam allergy, B-lactam resistance (MRSA, CoNS)
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20
Q

Vancomycin AE

A
  • red man syndrome: pruritis, red rash of face, neck, upper torso w/ hypoT -> tx by slowing infusion rate (histamine release causes this)
  • hypotension, flushing, erythematous rash, chills (infusion related)
  • ototxicity (w/ other ototoxic drugs)
  • nephrotoxicity (risk ↑w/ high doses or other nephrotoxic drugs)
  • neutropenia
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21
Q

Daptomycin

A

Coverage:
- GPs (inc. MRSA, MRSE, VRE)

Gaps in Coverage:

  • no GNs
  • no anaerobes
22
Q

Daptomycin AE

A

myalgias, myopathies

23
Q

Ciprofloxacin (early fluroquinolone)

A

Spectrum:

  • aerobic GN activity
  • poor GP activity (no staph/strep)
24
Q

Respiratory Fluroquinolones (moxifloxacin, levofloxacin)

A

Spectrum:

- better” GP coverate + added gut anaerobe coverage (moxi is broader)

25
Q

Fluroquinolones AEs

A

AE: occur in ANY part of body

  • N/V/D
  • photosensitivity (cipro is WORST)
  • CNS: HA, dizziness, drowsiness
  • hepatic (transient risk in LFTs, jaundice)
  • renal (nephritis)
  • skin (rash, photosens)
  • MSK (arthopath, tendinitis, tendon rupture)
  • CVS (hypoT, tachy, QT prolongation)
  • endocrine (hypo or hyper glycemia)
26
Q

Metronidazole spectrum

A
  • gut anaerobes ONLY (C. diff & parasites)
27
Q

Sulfonamide-trimethoprim spectrum

A

Spectrum:

  • GP (inc MRSA)
  • GN (H. influ, enterobacter SPICA)

What does it lack?

  • GAS
  • PsA
  • anaerobes
  • enterococcia
28
Q

Fidaxomicin Spectrum

A

Spectrum:

  • C. diff
  • less effect on the fecal microbial (vs vanco)
29
Q

Fidaxomicin MOA

A

RNA polymerase inhibitor – binds to DNA template – RNA polymerase (RNAP) complex prior to RNAP-DNA complex formation

30
Q

Sulfonamide-Trimethoprim MOA

A

Block enzyme in bacteria required for synthesis of tetrahydrofolic acid (a cofactor needed for bacteria to make the nucleotide bases T, U, G, A)

31
Q

Metronidazole MOA

A
  • activated by microbial proteins flavodxin & feredoxin

- when activated puts nicks in the microbial DNA strands

32
Q

Fluroquinolones MOA

A

Inhibit bact. DNA synthesis by interacting w/ DNA gyrase & topoisomerase IV

33
Q

Aminoglycosides

A

Gentamicin
Tobramycin
Amikacin

34
Q

Aminoglycosides MOA

A
  • IRreversably bind 30S ribosomal subunit
  • may have some activity on cell membrane causing leakage
  • uptake enhanced w/ exposure of cell-wall active agents (ie PCN)
35
Q

Aminoglycosides Spectrum

A

What do they add:

  • GNB: Pseudomonas
  • MRSA
  • GN aerobic bacilli

What do they lose:
NOT good for GPs or anerobes -> only GP if given synergistically with beta lactams

36
Q

Aminoglycosides AE

A

AE:

  • nephrotoxicity (reversible) – in elderly + on other nephrotoxic drugs
  • ototoxicity (irreversible)
37
Q

Linezolid (oxazolidinones) MOA

A
  • bind to 50S ribosomal subunit near interface w/ 30S s/u preventing formation of 70S initiation complex
  • different from other “protein synthesis” inhibitors which inhibit peptidyl transferase or translation-termination rxn
38
Q

Linezolid (oxazolidinones) Spectrum

A
  • only GP organisms including resistant ones
  • MRSA, VRE

Where does it fit?

  • alt to vanco for MRSA
  • VRE
39
Q

Linezolid AE

A
  • reversible inhibitor of monamine oxidase
  • thrombocytopenia
  • leukopenia
  • bone marrow suppression w/ prolonged use or other RFs
  • N.V.D
  • rash
40
Q

Macrolides

A

Erythromycin
Clarithromycin
Azithromycin

41
Q

Macrolides MOA

A
  • reversibly binds to 50S ribosomal subunit

- prevents translocation of peptidyl-RNA (incoming tRNA c/n be added & pro synthesis stops)

42
Q

Macrolides AE

A
  • N/V/D (worst for Erythro)
  • QT-prolongation* (drug interations)
  • seizures
  • jaundice
  • hepatitis
  • rash (uncommon)
  • hearing loss (transient)*
43
Q

Macrolides Spectrum

A
  • PCN spectrum PLUS
  • gram negatives
  • S. pneumo *30% R in CAN
  • atypical pneumo organisms (ie legionella)
  • C & A -> H. influenza

Where do they fit? Used if need atypical organism coverage or for STIs/travel

44
Q

Macrolides DI

A

DI: (macrolides are P45O inhibitor) theophylline, cyclosporine

  • ERY > CLARI w/ CYP P450 but NONE w/ AZITHRO*
45
Q

Clindamycin MOA

A

MOA: similar to macrolides

  • binds to 50S subunit
  • prevents translocation of pepridyl tRNA from the acceptor site to donor site
46
Q

Clindamycin Spectrum

A

Coverage: (adds to PCN)

  • anaerobes
  • aerobic GPs
  • most GPs (EXCEPT enterococcus)
  • PCPs, MRSA
  • some parasites

Gaps in Coverage:

  • no gram negatives (b/c c/n cross the outer CM)
  • enterococcus
47
Q

Clindamycin AE

A
  • diarrhea* -> C. difficile
  • transient ↑ of liver enz
  • neuromuscular blockade
  • N/V
48
Q

Tetracyclines

A
  • passively diffuse through pores in CW (GNs) & through inner mem of GPs w/ nrg dependent pump
  • Reversably binds 30S subunit
  • binds at site that blocks binding of some AA-charged tRNA to the acceptor site or mRNA comples
  • chelates cations essential to protein synthesis (Ca, Mg*)
49
Q

Tetracyclines spectrum

A

Coverage: PCN spec PLUS

  • GP & GN (similar to macrolides)
  • atypical organisms (Mycoplasma, chlamydia, rickettsiae)
50
Q

Tetracyclines AE

A
  • GI
  • photosensitivity (doxy)
  • brownish discolouration of teeth
  • hepatotoxicity
  • hypersensitivity rxns
  • drug induced lupus (mino, doxy)
  • CNS_ dizziness, ataxia, vertigo
  • fanconi-like syndrome (renal tubular dysfxn) -> w/ outdated product
51
Q

Tigecycline (a tetracycline) spectrum

A

Coverage:

  • GPs (inc. MRSA & VRE) - activity vs resistant organisms, b/c bacteriostatic and no bacteremia action so use is limited
  • atypicals
  • anaerobes
  • most GNs
  • ESBL – E.coli/K.pneumo

Gaps in Coverage:

  • morganella
  • Pseudomonas
  • proteus
  • providencia

Antimicrobial (2 decks)

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