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Drugs - Smith > deck_5727627 > Flashcards

deck_5727627 Flashcards

1
Q

what makes up the 70S ribosome complex?

A

30 S subunit + 50 S subunit

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2
Q

what makes up the 80S ribosome complex?

A

40S subunit + 60S subunit

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3
Q

describe the 3 ribosomal binding sites for tRNA

A

A site holds AA to be added P site holds growing polypeptide chain E site
exit site for tRNA

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4
Q

once the initiation complex is in place, the ___ assembles onto the ___ and the initiate proteins disassociate.

A
  • large ribosomal subunit

* small subunit

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5
Q

after the large ribosomal subunit assembles onto the small ribosomal subunit and the initiation proteins disassociate, what happens?

A

the ribosome is now ready to begin translation

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6
Q

prokaryotic translation occurs on ___ ribosomes

A

70S

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7
Q

eukaryotic translation occurs on ___ ribosomes

A

80S

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8
Q

describe the main steps of translation after the initiation complex is in place and the large and small ribosomal subunits are assembled

A
  • codon recognition
  • peptide bond formation
  • translocation
  • ribosome is ready for the next aminoacyl tRNA
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9
Q

what are the 4 functional targets of antimicrobial PSIs?

A
  • chloramphenicol
  • erythromycin (macrolides)
  • tetracyclines
  • streptomycin (aminoglycoside)
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10
Q

___ binds to the 50S ribosomal subunit portion and inhibits formation of the peptide bond

A

chloramphenicol

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11
Q

___ binds to the 50S ribosomal subunit portion, preventing translocation/movement of the ribosome along mRNA

A

erythromycin (macrolide)

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12
Q

___ interfere with attachment of tRNA to the mRNA-ribosome complex

A

tetracyclines

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13
Q

___ changes shape to the 30S ribosomal subunit portion, causing the code on mRNA to be read incorrectly

A

streptomycin (aminoglycoside)

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14
Q

what are the 5 aminoglycosides?

A
  • gentamycin
  • amikacin
  • tobramycin
  • streptomycin
  • neomycin
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15
Q

what class of antimicrobials has the following mechanism of action?binds to the 30S ribosomal subunit changing its shape, which can have the following three consequences: (1) blocked initiation of mRNA translation, (2) premature termination of mRNA translation, and (3) misreading of the mRNA and incorporation of incorrect amino acids

A

aminoglycosides

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16
Q

describe streptomycin

A
  • aminoglycoside drug
  • IM, IV administration
  • oldes of the family
  • high level of bacterial resistance
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17
Q

describe gentramycin

A
  • aminoglycoside drug
  • IV preffered administration
  • most commonly prescribed aminoglycoside
  • used in combination with penicillins
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18
Q

describe amikacin

A
  • aminoglycoside drug
  • IM, IV administration
  • broadest spectrum of all aminoglycosides
  • used for hospital acquired infections
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19
Q

describe tobramycin

A
  • aminoglycoside drug
  • IM, IV administration
  • excellent activity against pseudomonas aeruginosa
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20
Q

describe neomycin

A
  • aminoglycoside drug
  • topical administration only
  • used primarily as topical for skin infections
  • neomycin enema
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21
Q

what is a neomycin enema?

A

to flush and detoxify the colon and lower bowel before bowel surgery

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22
Q

aminoglycosides are used primarily to treat infections caused by what class of bacteria?

A

aerobic gram negative

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23
Q

the utility of aminoglycosides is limited by the occurrence of ___

A

serious toxicities

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24
Q

describe the bactericidal effect of aminoglycosides

A
  • concentration-dependent killing (type 1)
  • mild post-antibiotic effect (PAE) once-daily dosing
  • effective, reduces risk of toxicity
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25
Q

describe the exceptions to daily dosing of aminoglycosides

A

administered every 8 hours for:

  • pregnancy
  • neonatal infections
  • bacterial endocarditis
  • monitor creatinine clearance and BUN
26
Q

aminoglycosides are generally given via IV or IM. the exception is neomycin, which is given topically. why?

A

due to nephrotoxicity

27
Q

in anuric patients, the 1/2 life of aminoglycosides can increase by how much?

A

20-40x

28
Q

with aminoglycosides, since the risk of nephrotoxicity and ototoxicity is concentration-dependent, it is crucial to do what?

A

reduce dosages, especially in patients with impaired renal function

29
Q

aminoglycosides synergize with ___ or ___

A

beta-lactams or vancomycin (when used in combination)

30
Q

all aminoglycosides have the potential to produce ___ toxicity

A

vestibular/cochlear and renal toxicity(major limitation to the clinical utility of aminoglycosides)

31
Q

ototoxicity caused by aminoglycosides may become irreversible rapidly. the toxicity correlates with what?

A

the number of destroyed hair cells

32
Q

the frequent monitoring of what is essential during nephrotoxicity caused by aminoglycosides?

A

plasma concentrationex. BUN and serum creatinine levels

33
Q

name the 4 major adverse effects of aminoglycosides

A
  • ototoxicity
  • nephrotoxicity
  • neuromuscular paralysis
  • contact dermatitis
  • accumulation in fetal plasma and amniotic fluid in utero (teratogenic)
34
Q

what 4 groups are most at risk for aminoglycoside adverse effects?

A
  • elderly
  • impaired renal function septic patients
  • must adjust dose previous exposure to aminoglycosides
  • “functional accumulation”
35
Q

name the 4 types of tetracyclines

A
  • tetracycline
  • doxycycline
  • minocycline
  • tigecycline
36
Q

describe the spectrum of tetracyclines

A
  • broad spectrum against gram positive and negative, and atypical intracellular organisms
37
Q

which class of antimicrobials has the following mechanism of action?binds reversibly to 30S subunit of bacterial ribosome blocking access of the amino acyl-tRNA to the mRNA-ribosome complex’s acceptor site

A

tetracyclines

38
Q

the mechanism of action of tetracyclines inhibits the ___ subunit to prevent attachment of the ___

A
  • 30S

* aminoacyl-tRNA

39
Q

tetracyclines have a ___ action

A

bacteriostatic

40
Q

___ is often used for the treatment of acne vulgaris

A

tetracycline

41
Q

describe the cross-resistance of tetracyclines, and the exception

A
  • if resistant to one TTC (tetracycline), then resistant to all TTCs
  • exception: tigecycline
42
Q

the oral absorption of tetracyclines is altered by what 3 things?

A
  • dairy
  • iron supplements
  • antacids
43
Q

where in the body does tetracycline tend to concentrate?

A
  • Caclium-hydroxyapatite teeth/bones, or tumore with high calcium content
44
Q

what are the 11main adverse effects of tetracyclines?

A
  • GI upset
  • disulfuram-like effect (avoid alcohol)
  • hepatotoxicity
  • headache
  • metallic taste
  • phototoxicity
  • vestibular problems
  • benign intracranial hypertension
  • itching in anal and genital areas
  • superinfections
  • don’t give to pregnant patients
45
Q

describe superinfections as an adverse effect of tetracyclines

A
  • candida pseudomonas colitis

* diarrhea due to overgrowth of c. difficile

46
Q

what are the two main oral adverse effects of tetracyclines?

A
  • hairy tongue

* deposition in bone and primary dentition

47
Q

what are the contraindications for tetracyclines?

A
  • pregnant patients
  • breastfeeding patients
  • children <8 yrs
  • inpatients with liver and renal disease
48
Q

describe the spectrum of bacteria tigecycline acts against

A

same as doxycyline and other TTCs plus activity against:

  • MRSA
  • multidrug resistant s. pneumoniae
  • vancomycin resistant enterococci
  • some anaerobes
49
Q

___ was developed to overcome TTC-resistance in complicated skin, soft tissue, and intra-abdominal infections

A

tigecycline

50
Q

how is tigecycline administered?

A

IV

51
Q

what are the adverse effects of tigecycline?

A

similar to other TTCs, including teeth and bones

52
Q

what are the 3 macrolides?

A

erythromycin, clarithromycin, azithromycin

53
Q

which antimicrobials has the following mechanism of action?binds irreversibly to 50S subunit of bacterial ribosome to inhibit the translocation step of protein synthesis

A

macrolides (ketolides)

54
Q

describe the spectrum of action of macrolides

A

gram positive and negative, and atypical bacteria (cross resistance within class)

55
Q

what are considered the safest antimicrobials?

A

macrolides

56
Q

the following clinical uses describe what antimicrobial?2nd line agents for skin and soft tissue infections not due to MRSA; frequently used for URIs and community acquired pneumonia

A

macrolides

57
Q

which macrolide is often used in patients allergic to penicillin?

A

erythromycin

58
Q

erythromycin has largely been replaced by ___ and ___ for community acquired penumonia

A

clarithromycin and azithromycin

59
Q

describe the clinical uses of azythromycin

A
  • “z-pak”

* azithromycin is preferred therapy for urethritis caused by chlamydia

60
Q

which of the macrolides has the longest 1/2 life and volume of distribution in its class?

A

azithromycin

Drugs - Smith (9 decks)

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