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pharm exam 2 > inhibitors of protein synthesis I > Flashcards

inhibitors of protein synthesis I Flashcards

1
Q

prokaryotic ribosomes are composed of what two subunits

A
  • 50S
  • 30S
  • combine to form 70S total
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2
Q

Eukaryotic ribosomes are composed of what two subunits

A
  • 60S
  • 40S
  • combine to form 80S
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3
Q

MOA of macrolides

A

targets 50S subunit of ribosome

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4
Q

Macrolides prototype

A

erythromycin

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5
Q

Name the three macrolides

A
  1. erythromycin
  2. clarithromycin
  3. azithromycin
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6
Q

route of administration of erythromycin

A

oral, IV

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7
Q

route of administration of Clarithromycin

A

oral

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8
Q

route of administration of azithromycin

A

oral, IV

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9
Q

are macrolides bacteriostatic or cidal

A

bacteriostatic; concentration/organism dependent- cidal activity

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10
Q

coverage of macrolides

A

G+

*majority of G- organisms are resistant

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11
Q

how do bacteria become resistance to macrolides

A
  • efflux pumps
  • methylation of drug binding site (ribosome)
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12
Q

toxicity of macrolides, particularly Erythromycin

A
  • diarrhea
    • erythromycin +++; Azithro ++; clarithromycin +: GI adverse effects
  • QT prolongation
    • erythro +++; Claritho ++; Azithro +
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13
Q

erythromycin is a potent inhibitor of what enzyme that leads to drug interactions

A

CYP3A4

  • therefore, can inhibit the hepatic metabolism of other drugs that require CYP3A4, increasing their serum concentrations and potentially causing toxicity
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14
Q

DOC for urogenital infections due to Chlamydia occuring during pregnancy

A

Erythromycin

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15
Q

DOC legionnaries’ disease

A

azithromycin

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16
Q

MOA of Ketolides

A

block bacterial protein synthesis; has 2 binding sites for the ribosomal RNA, 50S, which increases its affinity

17
Q

what group is Telithromycin in

A

Ketolides

18
Q

coverage of Telithromycin

A

broad spectrum

  • good against respiratory pathogens including erythromycin and penicillin resistant pneumococci: remains on market for community acquired PNA (not first choice)
19
Q

route of administration of Telithromycin

A

oral

20
Q

metabolism of Telithromycin

A

via CYP3A4

21
Q

toxicity of Telithromycin

A
  • diarrhea
  • hepatotoxicity
22
Q

MOA of Clindamycin

A

binds to 50S ribosomal subunit

23
Q

coverage of Clindamycin

A
  • aerobic G+
  • Anaerobic G- and G+ organisms
24
Q

is Clindamycin bacteriostatic or cidal

A

either, depends on

  • concentration at the site of action
  • specific susceptibility of the organism
25
Q

why is Clindamycin used to treat osteomyelitis

A

it obtains high concentration in bones

26
Q

which organisms are extremely susceptible to Clindamycin

A
  1. streptococci (except enterococci) and staphylococci (MRSA)
27
Q

what two Abx are used to treat toxic shock syndrome

A
  • clindamycin
  • vancomycin
28
Q

Clindamycin toxicity

A
  • Pseudomembranous colitis (overgrowth of clostridium difficile)
29
Q

is Clindamycin safe to use in nursing mothers

A

NO, crosses the placenta readily and is distributed into breast milk

30
Q

What two Abx does Streprogramins consist of

A
  • Dalfopristin
  • Quinupristin
  • Trade name (Synercid)
  • combination is bactericidal
31
Q

MOA of Dalfopristin; Quinupristin (Synercid)

A

both Abx bind to 50S particles but inhibit different stages of protein synthesis

32
Q

route of adminstration of Dalfopristin; Quinupristin (Synercid)

A

IV infusion

33
Q

Dalfopristin; Quinupristin (Synercid) has been approved for what uses

A
  • Aerobic G+
    • penicillin resistant S. pneumoniae
    • complicated skin infections due to staph aureus (MSSA and MRSA)
    • vancomycin resistant Enterococcus faecium
34
Q

adverse reactions of Dalfopristin; Quinupristin (Synercid)

A
  • hepatotoxicity
  • inhibit P450 drug metabolism system (CYP3A4), many metabolic interactions (warfarin, diazepam)
35
Q

what group does Linezolid belong to

A

Oxazolidinones

36
Q

coverage of Linezolid

A

aerobic G+ organisms

  • bacterial PNA
  • vancomycin-resistant enterococcal infections
  • MRSA

***new Abx; should be used as alternate agent bc overuse with hasten selection of resistant strains

37
Q

MOA of Linezolid

A
  • binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit
38
Q

Linezolid adverse reactions

A

reversible, non-selective inhibitor of monoamine oxidase (MAO)

*MAO inactivate neurotransmitters

39
Q

route of administration of Linezolid

A

IV or oral

*Oral bioavailability is 100%

pharm exam 2 (9 decks)

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