Mata - antibiotics Flashcards

(55 cards)

1
Q

classes that inhibit DNA synthesis

A

Sulfonamides
Trimethoprim
Fluoroquinolones

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2
Q

classes that interfere with cell wall

A
Penicillins 
Cephalosporins 
Carbapenems 
Aztreonam 
Vancomycin
Daptomycin
Polymyxins 
Colistin
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3
Q

b-lactams

A

Penicillins
Cephalosporins
Carbapenems
Aztreonam

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4
Q

classes that inhibit protein synthesis

A
Macrolides 
Clindamycin
Chloramphenicol 
Streptogramins
Linezolid 
Tetracyclines 
Aminoglycosides 
Mupirocin
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5
Q

subgroups of Penicillins

A

Pen G
Pen V
Aminopenicillins (amoxicilin/ampicillin)
b-lactamase resistant (nafcillin/oxacillin)
extended spectrum (ticarcillin/pipercillin)

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6
Q

Penicillins

A

MOA: b-lactam
bactericidal
Gram + (some gram – cocci)
excretion: renal (except nafcililn)

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7
Q

Pen G limitations

A

short half-life
narrow spectrum (Gram +)
not acid stable (not orally)
susceptible to b-lactamases

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8
Q

Pen V improved ___ compared to Pen G

A

absorption

more acid stable, can be given orally

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9
Q

Aminopenicillins

A

semisynthetic
broader spectrum, includes some gram –
acid stable, used orally
rash more common

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10
Q

Ticarcillin and Pipercillin

A

extended spectrum
treat more serious gram –
aka anti-pseudomonal penicillins

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11
Q

3 ways to overcome b-lactamase

A

give more drug
inhibit b-lactamase directly
make changes to drug

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12
Q

nafcillin and oxacillin

A

b-lactamase resistant

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13
Q

naficillin excretion

A

biliary

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14
Q

Cephalosporins

A

MOA: b-lactam
bactericidal
Gram + and – (generations differ)
excretion: renal

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15
Q

1st gen cephalosporins

A

mainly gram + cocci
some gram –
ex: Cefazolin

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16
Q

Cefazoline used for

A

prophylactically before surgery, long half life, high protein binding

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17
Q

2nd gen cephalosporins

A

gram + and -

extended coverage of –

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18
Q

3rd gen cephalosporins

A

more gram – than +

ex: ceftriaxone

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19
Q

Ceftriaxone uses

A

bacterial meningitis - Strep pneumoniae and N. meningitidis
crosses BBB
hepatic/biliary elimination

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20
Q

Ceftriaxone precaution

A

incompatible with calcium containing products

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21
Q

4th gen cephalosporins

A

gram + and -, for b-lactamase producing bacteria

ex: cefepime

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22
Q

Ceftaroline

A

advanced generation/newer cephalosporin
bactericidal
for MRSA

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23
Q

patients with history of anaphylaxis to penicillins should not get ___

A

cephalosporins

24
Q

________ enter breast milk and may alter bowel flora of the infant

A

Cephalosporins

25
___ should not be given to hyperbilirubinemic and preterm neonates because in vitro, can displace bilirubin from serum albumin, potentially triggering kernicterus
Ceftriaxone
26
Aztreonam
MOA: b-lactam Gram + (no anaerobes) does not cross react with penicillin
27
Carbapenems
``` MOA: b-lactam resistant to b-lactamases very broad spectrum given IV excretion: renal ```
28
Vancomycin
MOA: inhibits cell wall synthesis, high affinity binding to D-Alanyl-D-alanine terminus of cell wall precursor units, no cross bridges formed Gram + important for MRSA
29
oral vancomycin
not orally bioavailable, used to treat C. diff
30
adverse effects of vancomycin
ototoxicity nephrotoxicity hypersensitivity reactions red man syndrome
31
Daptomycin
MOA: disruption of bacterial membrane through formation of transmembrane channels cause leakage of intracellular ions --> depolarizing cell membrane and inhibiting macromolecular synthesis Gram + only concentration dependent killing serious infections, but not in lungs IV only excretion: renal
32
Polymyxins
MOA: bind to and disrupt action of LPS, neutralizing bacteria's toxicity Gram --
33
Colistin
a polymyxin orally for bowel decontamination inhaled therapy for CF patients
34
Macrolides include
azithromycin clarithromycin erythromycin
35
Macrolides
``` MOA: reversibly bind to 50S subunit at tRNA binding site, inhibit protein synthesis usually bacteriostatic narrow spectrum (gram + and --) oral or IV good for lung infections excretion: bile ```
36
erythromycin causes...
dose limiting GI disturbances | used a prokinetic
37
Adverse effects of macrolides
``` C. diff colitis hepatitis, hepatic dysfunction QR prolongation torsades de pointes drug interactions through P450 interactions ```
38
advantage of azithromycin
``` not a substrate of CYP3A4 ○ lowers risk of drug interactions ○ less risk of hepatotoxicity - reduced risk of cardiotoxicity - longer half-life - ability to reduce inflammation, changes gene expression in anti-inflammatory way ```
39
Clindamycin
``` MOA: binds to 50S subunit, inhibits protein synthesis at tRNA binding site bacteriostatic cross resistance with macrolides narrow spectrum (for anaerobic) accumulates in bone penetrates will into abscesses ```
40
Chloramphenicol
first successful treatment for typhoid fever | broad spectrum
41
Streptogramins
MOA: type A: ribosomal initiation complexes assembled normally but functionally inactive. type B: inhibit first two of three elongation steps, do not affect 3rd step Gram + (MRSA) excretion: biliary/fecal
42
Linezolid
MOA: binds in the A site pocket at the peptidyltransferase center of the ribosome overlapping the aminoacyl moiety of an A-site bound tRNA preventing formation of the larger ribosomal-fMet-tRNA complex that initiates protein synthesis Gram +
43
advantages of linezolid
oral preparation with 100% bioavailability (without regard to food) extensive volume of distribution 100% serum concentrations in lung, bronchi neither substrate nor inhibitor of CYPs activity against most gram + bacteria and mycobacteria
44
drug interactions with linezolid
with SSRIs --> serotonin syndrome
45
Tetracyclines
MOA: binding reversibly to receptors of the 30S ribosomal subunit, prevent addition of new AA to peptide chain broad spectrum bacteriostatic
46
side effects of tetracyclines
nausea on empty stomach
47
doxycyline
longer acting tetracycline 95% absorbed, even with food fecal excretion
48
adverse effects of tetracyclines
brown discoloration of teeth photosensitivity Fanconi-like syndrome from expired
49
Tigecycline
MOA: similar to tetracycline but avoid efflux pumps | overcomes 2 major mechanisms of tetracycline resistance: efflux pump acquisition and ribosomal protection
50
advantages of tigecycline
○ Extremely broad range (activity against drug resistant strains and vancomycin-resistant bacteria and mycobacteria) ○ Long half-life (100 mg initial dose followed by 50 mg injection every 12 hours). ○ Resistance is less likely. Good safety profile.
51
Aminoglycosides
MOA: enter susceptible bacteria by oxygen-dependent active transport (not anaerobes) and passive diffusion. Bind to 30s subunit of 70s ribosome. enable binding of incorrect tRNAs Gram -- , aerobic some Gram +, mycobacteria, mycoplasma, spirochetes synergize with b-lactams and vancomycin excretion: renal high accumulation in kidneys
52
Adverse effects of aminoglycosides
toxicities in kidneys and auditory system nephrotoxicity - reversible ototoxicity - irreversible
53
Amikacin
aminoglycoside use against Mycobacterium tuberculosis strains that are multi drug resistant IM or IV renally cleared
54
Neomycin
aminoglycoside used orally for bowel prep in topicals
55
Mupirocin
``` MOA: bind reversibly to isoleucyl tRNA synthetase. prevents incorporation of isoleucine into growing protein chains. arrests protein synthesis. Gram + cocci topical eliminated S. aureus i nose not effective systemically ```