antibiotics for osteomyelitis and skin infections med chem Flashcards

1
Q

tetracycline drugs

A

tetracycline
monocycline
doxycycline
tigecycline

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2
Q

tetracycline MoA

A

interacts with 30S subunit of ribosome and sits in A site to prevent elongation (bacteriostatic)

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3
Q

tetracycline general pharmacophore

A

4 rings and dimethylamine pointing into the board

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4
Q

ways to inactivate tetracyclines

A
  • make dimethylamine come out of the board
  • dehydration of OH on north side
  • breaking C ring through intramolecular reaction
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5
Q

avoid taking tetracyclines with what

A

multivitamins and milk because of chelation with ions

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6
Q

tetracyclines clinical use

A
  • Gm+
  • MRSA
  • limited Gm-
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7
Q

tetracycline resistance

A

widespread in forms of

  • efflux
  • mutations in ribosome
  • cell wall variation
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8
Q

side effects of tetracyclines

A
  • light sensitivity
  • severe kidney damage
  • incorporation into bones and teeth
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9
Q

tigecycline unique structure feature

A

the claw on the tetracycline ring that prevents efflux based resistance

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10
Q

tigecycline clinical use

A

broad spectrum, typically saved for instances of resistance

hits basically everything but pseudomonas

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11
Q

clindamycin MoA

A

sits in 50S peptidyltransferase to inhibit the enzyme

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12
Q

clindamycin clinical use

A
  • Gm+ (staph, strep)
  • used w/ aminoglycosides for Gm-
  • some anaerobes
  • used if PCN allergy
  • PO/IV
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13
Q

clindamycin side effects

A
  • GI

- pseudomembranous colitis caused by C.difficile

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14
Q

linezolid MoA

A

prevents formation of 70S subunit complex by binding w/ 50S subunit

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15
Q

linezolid clinical use

A
  • Gm+
  • MRSA
  • VRE
  • IV/PO
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16
Q

linezolid resistance

A

still rare but can be seen as:

  • point mutation of ribosome
  • efflux pump in Gm-
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17
Q

linezolid side effects

A
  • monoamine oxidase inhibitor, so avoid w/ tyramine foods and serotonergic drugs
  • bone marrow suppression
18
Q

linezolid monitoring

A

weekly blood counts

19
Q

synercid

A
  • IV only
  • combo of dalfopristin and quinupristin
  • 30:70 ratio quinupristin:dalfopristin because dalfo binding first increases affinity for quinupristin
20
Q

synercid MoA

A

binds to A and P sites to interfere with tRNA binding and misalignment of P site

21
Q

mupirocin MoA

A

binds to Ile-tRNA synthetase to prevent incorporation of Ile into proteins

22
Q

mupirocin clinical use

A
  • used topically or nasally because it is hydrolyzed in vivo

- broad spectrum activity, good against staph and strep

23
Q

mupirocin resistance

A

mutations in synthetase enzyme prevents binding

24
Q

vancomycin MoA

A

“hugs” cross link area of peptidoglycan to prevent transpeptidase cross link AND prevents sugars from cross linking

25
Q

vancomycin clinical use

A
  • narrow spectrum Gm+
  • used for C.diff and enterococci
  • last resort for MRSA
  • PO/IV
26
Q

vancomycin resistance

A

D-Ala D-Ala becomes D-Ala D-Lactate to reduce hydrogen bonding

27
Q

vancomycin resistant enterococci background

A
  • 2nd most common Gm+ in hospitals

- high moretality

28
Q

treatments for VRE

A

synercid
linezolid
cubicin (daptomycin)

29
Q

linezolid route

A

oral and IV

30
Q

clindamycin route

A

oral

31
Q

tigecycline route

A

IV

32
Q

telavancin and dalbavancin MoA

A
  • disrupts peptidoglycan cross linking

- long FA chain anchors it in membrane helping with affinity

33
Q

telavancin route

A

IV

34
Q

dalbavancin route

A

IV

35
Q

telavancin and dalbavancin clinical use

A
  • MRSA

- some vancomycin resistant strains

36
Q

difference between telavancin and dalbavancin

A

half life

dalbavancin has once weekly dosing

37
Q

daptomycin MoA

A

creates a potassium ion channel leading to membrane depolarization

38
Q

daptomycin clinical use

A
Gm+
-resistant strep
-resistant staph
-resistant entero
MRSA
VRE
-IV
39
Q

daptomycin side effects

A
  • elevated serum creatinine phosphkinase

- rhabdomyolysis

40
Q

daptomycin monitoring

A

signs of muscle pain or weakness

41
Q

tetracyclines contraindications

A
  • pregnant females

- children under 8

42
Q

vancomycin IV side effects

A
  • GI

- red man syndrome