Mata - antibiotics Flashcards

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
Q

___ should not be given to hyperbilirubinemic and preterm neonates because in vitro, can displace bilirubin from serum albumin, potentially triggering kernicterus

A

Ceftriaxone

26
Q

Aztreonam

A

MOA: b-lactam
Gram + (no anaerobes)
does not cross react with penicillin

27
Q

Carbapenems

A
MOA: b-lactam
resistant to b-lactamases
very broad spectrum 
given IV
excretion: renal
28
Q

Vancomycin

A

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
Q

oral vancomycin

A

not orally bioavailable, used to treat C. diff

30
Q

adverse effects of vancomycin

A

ototoxicity
nephrotoxicity
hypersensitivity reactions
red man syndrome

31
Q

Daptomycin

A

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
Q

Polymyxins

A

MOA: bind to and disrupt action of LPS, neutralizing bacteria’s toxicity
Gram –

33
Q

Colistin

A

a polymyxin
orally for bowel decontamination
inhaled therapy for CF patients

34
Q

Macrolides include

A

azithromycin
clarithromycin
erythromycin

35
Q

Macrolides

A
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
Q

erythromycin causes…

A

dose limiting GI disturbances

used a prokinetic

37
Q

Adverse effects of macrolides

A
C. diff colitis
hepatitis, hepatic dysfunction
QR prolongation 
torsades de pointes 
drug interactions through P450 interactions
38
Q

advantage of azithromycin

A
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
Q

Clindamycin

A
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
Q

Chloramphenicol

A

first successful treatment for typhoid fever

broad spectrum

41
Q

Streptogramins

A

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
Q

Linezolid

A

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
Q

advantages of linezolid

A

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
Q

drug interactions with linezolid

A

with SSRIs –> serotonin syndrome

45
Q

Tetracyclines

A

MOA: binding reversibly to receptors of the 30S ribosomal subunit, prevent addition of new AA to peptide chain
broad spectrum
bacteriostatic

46
Q

side effects of tetracyclines

A

nausea on empty stomach

47
Q

doxycyline

A

longer acting tetracycline
95% absorbed, even with food
fecal excretion

48
Q

adverse effects of tetracyclines

A

brown discoloration of teeth
photosensitivity
Fanconi-like syndrome from expired

49
Q

Tigecycline

A

MOA: similar to tetracycline but avoid efflux pumps

overcomes 2 major mechanisms of tetracycline resistance: efflux pump acquisition and ribosomal protection

50
Q

advantages of tigecycline

A

○ 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
Q

Aminoglycosides

A

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
Q

Adverse effects of aminoglycosides

A

toxicities in kidneys and auditory system
nephrotoxicity - reversible
ototoxicity - irreversible

53
Q

Amikacin

A

aminoglycoside
use against Mycobacterium tuberculosis strains that are multi drug resistant
IM or IV
renally cleared

54
Q

Neomycin

A

aminoglycoside
used orally for bowel prep
in topicals

55
Q

Mupirocin

A
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