L25: Aminoglycosides Flashcards

1
Q

Which five drugs are aminoglycosides (hint: ST GAP)?

A

S - Streptomycin
T - Tobramycin

G - Gentamycin
A - Amikacin
P - Plazomicin

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2
Q

The bacteria 70S ribosomes (composed of 2 main subunits: 30S and 16S RNA subunit + 21 proteins) is targeted by which two drug classes?

A

1) Tetracyclines
2) Aminoglycosides

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3
Q
A
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4
Q

Aminoglycosides bind irreversibly to ___S to block protein synthesis. They are also ____, especially in combination
A. 30S, bacteristatic
B. 50S, bactericidal
C. 30S, bactericidal
D. 50S, bacteristatic

A

C. 30S, bactericidal

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5
Q

To enter into the bacterial cell, aminoglycosides diffuse through the porin channels in the outer membrane
of gram __ bacteria. Also
cross the plasma membrane of the bacteria by an
___-dependent, active transport process

A. Gram (-) ; O2 dependent
B. Gram (+) ; O2 dependent
C. Gram (+) ; CO2 dependent

A

A. Gram (-) ; O2 dependent

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6
Q

This active transport by which aminoglycosides crosses the plasma membrane of the bacteria is inhibited by __ pH and by
____ conditions

A

low ; anaerobic

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7
Q

True or False: Aminoglycosides are not effective against anaerobic
bacteria or in the acidic pH of an abscess

A

True

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8
Q

Antibiotics that inhibit bacterial cell wall synthesis ___
the transport of aminoglycosides into the bacteria

A. diminish
B. enhance

A

B. enhance

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9
Q

What type of effect is seen with an aminoglycoside + beta-lactam?
A. Additive
B. Synergistic
C. Antagonistic
D. Nihilistic

A

A. Synergistic

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10
Q

Aminoglycosides have best activity against?
A. Gram (-) Aerobic
B. Gram (-) Anaerobic
C. Gram (+) Aerobic
D. Gram (+) Anaerobic

A

A. Gram (-) Aerobic

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11
Q

Although Gentamicin and Tobramycin have some activity against S. aureus/ S.epidermidis, you should not use ____ alone for serious
Staph

A

aminoglycosides

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12
Q

Aminoglycosides are often used with a ____ antibiotic
for better coverage against gram (+)

A

beta-lactam

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13
Q

True or False: Gentamicin/
Streptomycin are used with a beta-lactam
(Penicillin G) to get a synergistic effect against Entercocci spp

A

True

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14
Q

Aminoglycosides are combined with β-lactams or vancomycin for ____

A

Gram-positive
endocarditis

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15
Q

What are the 5 clinical uses of aminoglycosides?

A
  1. Gram (-) Enteric Infections
  2. Tb
  3. P. aeru
  4. Opthalamic - ocular bacterial infections, conjunctivitis, corneal ulcers
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16
Q

True or False: Aminoglycosides are effective for abscesses or anaerobes

A

False - ineffective for abscesses or anaerobes

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17
Q

Aminoglycosides are very polar – therefore: found in high concentrations in
___ but not so much other tissues

A

kidney

18
Q

True or False: Ceftriaxone preferred for meningitis

A

True

19
Q

True or False: Aminoglycosides use concentration-dependent killing

A

True

20
Q

____: ~3 hr period after drug below MIC
where effect still present – allows for less frequent dosing
with no lapse in killing + higher efficacy with less toxicity
(as seen in aminoglycosides)

A

Postantibiotic effect

21
Q

For aminoglycosides, high [drug] in renal cortex and inner ear – leads to ____ and ____

A

nephrotoxicity and ototoxicity

22
Q

Why is nephrotoxicity so common with aminoglycoside use?

A
  • PCT selectively take up
    drug via megalin
23
Q

Decreased renal function is so common
with aminoglycosides that oral dosing regimens take this into account by doing what?

A

Lower the dose to compensate
for lowered drug elimination

24
Q

Ototoxicity is an irreversible side effect of ____ use

A

aminoglycoside

25
Q

What is the most important mechanism for drug resistance?

A. Enzymatic inactivation of drug
B. Impaired drug influx
C. Loss or mutation of ribosomal target protein
(streptomycin)

A

A. Enzymatic inactivation of drug

  • Phosphorylation
    (aminoglycoside kinases)

-Adenylation acetylation
(mediated by transferases)”

26
Q

____ is most resistant to these enzymes used to inactivate drugs in aminoglycosides

A

Amikacin

27
Q

Permanent vertigo/loss of balance is common with use of which drug?
A. Tobramycin
B. Staphylomycin
C. Streptomycin
D. Gentomycin

A

C. Streptomycin

28
Q

___ is second line drug for Tb and use in pregnancy can lead to fetus that is deaf
A. Tobramycin
B. Staphylomycin
C. Streptomycin
D. Gentamycin

A

C. Streptomycin

29
Q

____ is a mix of C1, C1a, C2 and is used to treat resistant streptococci/enterococci via: combo
with cell wall agents
A. Tobramycin
B. Staphylomycin
C. Streptomycin
D. Gentamycin

A

D. Gentamycin

30
Q

True or False: While gentamycin given IV can be used to treat meningitis, the condition is usually treated with 3rd gen cephs

A

True

31
Q

Which of the following
can treat gram (-) hospital-acquired UTIs and P. aeruginosa sepsis?
A. Tobramycin
B. Staphylomycin
C. Streptomycin
D. Gentamycin

A

D. Gentamycin

32
Q

____: Similar spectrum to gentamycin; cross-resistance
possible but not guaranteed
A. Tobramycin
B. Staphylomycin
C. Streptomycin
D. Gentamycin

A

A. Tobramycin

33
Q

Tobramycin a little better for _____

____ resistant to tobramycin

A

P. aeruginosa

E. faecium

34
Q

Which is more nephrotoxic: gentamicin or tobramycin?

A

gentamicin

35
Q

Which of the following is inhaled in fixed dose for P.aeruginosa in cystic fibrosis??
A. Tobramycin
B. Staphylomycin
C. Streptomycin
D. Gentamycin

A

A. Tobramycin

36
Q

____: Kanamycin derivative, less toxic but
may be cross-resistance to kanamycin.

Generally used for bugs resistant to gentamicin/tobramycin

A. Tobramycin
B. Staphylomycin
C. Streptomycin
D. Gentamycin
E. Amikacin

A

E. Amikacin

37
Q

Amikacin treats Gram (-) microbes, such as…

A

Pseudomonas

38
Q

____ is composed of A, B, C, and small proportion of others; ____ is neomycin E

In both cases, hypersensitivity is common

A

Neomycin; Paromomycin

39
Q

True or False:
Neomycin is NOT used
parenterally but Paromomycin can be used parenterally/
topically (parasitic infections)

A

True

40
Q

_____ is the newest aminoglycoside to be approved. It is resistant to inactivating enzymes and used to treat complicated UTI’s.

A