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PHRM 865 Therapeutics > Lec 5 Aminoglycosides/Macrolides Cushman > Flashcards

Lec 5 Aminoglycosides/Macrolides Cushman Flashcards

1
Q

aminoglycoside 2 core structures

A

streptidine
2-deoxystreptamine

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2
Q

which of the following are NOT aminoglycosides? (2 of them)

a. tobramycin
b. erythromycin
c. plazomicin
d. amikacin A
e. clarithromycin
f. gentamicin C2
g. neomycin B
h. streptomycin

A

b. erythromycin
e. clarithromycin

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3
Q

4 main things for mechanism of aminoglycosides

A

-inhibits formation of initiation complex
-blocks further translation
-premature termination of transcription
-impairment of proofreading and formation of “nonsense proteins”

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4
Q

aminoglycosides bind to the ____ subunit of the ribosome

A

30S

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5
Q

what do the “nonsense proteins” formed by aminoglycosides do?

A

impair bacterial cell wall function

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6
Q

aminoglycoside antibiotics can affect the 30S ribosomal subunit to cause a _______ mutation

A

frameshift

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7
Q

which class of antibiotics affects normal codon-anticodon binding?

A

aminoglycosides

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8
Q

bacterial aminoglycoside uptake: passage through the cytoplasmic membrane is an _______ transport process

A

active

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9
Q

bacteria inactivate aminoglycosides by all of the following EXCEPT

a. acetylation
b. adenylation
c. phosphorylation
d. oxidation

A

d. oxidation

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10
Q

3 aminoglycoside resistance mechanisms

A
  1. metabolism
  2. altered ribosomes
  3. altered uptake
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11
Q

aminoglycoside resistance: the ___ rRNA binding site can be altered through point mutations, observed clinically with mycobacterium tuberculosis

a. 16S
b. 30S
c. 50S
d. 70S

A

a. 16S

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12
Q

which is TRUE about the toxicity of all aminoglycosides?

a. ototoxicity and nephrotoxicity are reversible
b. ototoxicity is reversible; nephrotoxicity is irrev
c. ototoxicity is irrev; nephrotoxicity is reversible
d. ototoxicity and nephrotoxicity are both reversible

A

c. ototoxicity is irrev; nephrotoxicity is reversible

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13
Q

T or F: serial audiograms are recommended with aminoglycosides

A

T

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14
Q

aminoglycosides concurrent use with _____ _____ or vanc can potentiate nephrotoxicity (answer is a drug class)

A

loop diuretics

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15
Q

respiratory paralysis from aminoglycosides can usually be reversed with _______ or calcium gluconate

a. probenecid
b. vancomycin
c. neostigmine
d. meclizine

A

c. neostigmine

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16
Q

aminoglycosides have broad spectrum activity, but in practice they are almost always reserved for gram _______

A

negative

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17
Q

how can penicillins and aminoglycosides be given together?

A

administered in different compartments (one in each arm) to avoid chemical rxn between the classes

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18
Q

penicillin/aminoglycoside combinations are used to treat

a. bacterial endocarditis
b. tuberculosis
c. UTIs, burns, some pneumonias, joint and bone infections

A

a. bacterial endocarditis

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19
Q

streptomycin is most often used to treat

a. bacterial endocarditis
b. tuberculosis
c. UTIs, burns, some pneumonias, joint and bone infections

A

b. tuberculosis

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20
Q

gentamicin use

a. bacterial endocarditis
b. tuberculosis
c. UTIs, burns, some pneumonias, joint and bone infections

A

c. UTIs, burns, some pneumonias, joint and bone infections

21
Q

most important aminoglycoside

A

gentamicin

22
Q

which aminoglycoside is used to treat nosocomial infections (hospital-acquired)?

a. tobramycin
b. plazomicin
c. amikacin
d. gentamicin
e. neomycin
f. streptomycin

A

c. amikacin

23
Q

Amikacin A’s important moiety that inhibits bacterial metabolism by R-factors

a. L-arginine
b. syn-methoxyether
c. L-hydroxyaminobuterylamide
d. C-6 hydroxyl

A

L-hydroxyaminobuteryl amide

24
Q

tobramycin is adenylated at ___ and acetylated at ___

A

C2; C3

25
Q

_______ has superior activity vs. Pseudomonas aeruginosa than Amikacin, it is widely used parenterally to treat gentamicin-resistant Pseudomonas aeruginosa infections

A

tobramycin

26
Q

2 orally used aminoglycosides

A

neomycin B
paromomycin

27
Q

two aminoglycosides used clinically to suppress gut flora in travelers diarrhea and prophylactically prior to GI surgery to dec the incidence of peritonitis

A

neomycin and paromomycin

28
Q

__________ is used to treat amoebic dysentery as well as dwarf tapeworm and beef tapeworm

a. paromomycin
b. gentamicin
c. streptomycin
d. erythromycin

A

a. paromomycin

29
Q

first antibiotic used to cure tuberculosis

A

streptomycin

30
Q

skipped plazomicin and streptomycin

A

ok

31
Q

macrolides are usually ___-membered lactone rings

A

14

32
Q

drugs ending in “mycin” comes from ?

a. streptomyces
b. micromonospora

A

a. streptomyces

33
Q

drugs ending in “micin” comes from ?

a. streptomyces
b. micromonospora

A

b. micromonospora

34
Q

which sugar of macrolides is most important for activity?

a. desosamine sugar
b. cladinose sugar
c. pentose sugar

A

a. desosamine sugar

(b. is less important, c. is not on the structure)

35
Q

Macrolides are polyketides because they are produced by sequential addition of _______ groups to a growing chain. This results in _______ groups on alternate carbon atoms in the macrolide ring.

A

propionate
methyl

36
Q

The pKa of the amine in erythromycin is ___. The amine can form salts that are more soluble

A

8.8

37
Q

Macrolide binding mainly involves the bacterial ___ RNA and not the protein

A

23S (part of 50S)

38
Q

4 resistance mechanisms for macrolides

A
  1. Lactone ester hydrolase induced to degrade the macrolides by hydrolysis of the macrocycle
  2. A2058 methylation
  3. Mutation of A to G in A2058
  4. An efflux pump ejects drugs from cell by an active transport process
39
Q

Certain organisms like Pseudomonas spp. and Enterobacter spp. exhibit _______ _______ by not allowing entry of macrolide antibiotics

A

intrinsic resistance

40
Q

erythromycin derivative that is stable in acid due to 6-OCH

A

clarithromycin

41
Q

amine analog, acid stable, N-methylated methyleneamino moiety replaces C-9 ketone

a. erythromycin
b. clarithromycin
c. azithromycin

A

c. azithromycin

42
Q

main route of erythromycin metabolism is _________ in the liver

A

demethylation

43
Q

erythromycins are primarily used for infections of skin and soft tissues primarily caused by gram ______ bacteria

A

positive

44
Q

clinical use of erythromycins look at that

A

okay

45
Q

long term use (10-20) days of macrolides can induce a reversible _______ _______

a. pseudomembranous colitis
b. cholestatic hepatitis
c. aplastic anemia
d. tendon rupture

A

b. cholestatic hepatitis

46
Q

how is clindamycin metabolized?

A

CYP P450

47
Q

erythromycin can inc the probability of _______ _______

a. pseudomembranous colitis
b. cholestatic hepatitis
c. aplastic anemia
d. pyloric stenosis

A

d. pyloric stenosis

48
Q

why is oral erythromycin given as enteric coated or as more stable salts or esters?

A

it is inactivated by gastric acids

PHRM 865 Therapeutics (8 decks)

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