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IP3 exam #2 > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

Aminoglycosides

A
  • Binds to 30s ribosome
  • Are bactericidal
  • NO anaerobic activity
  • Concentration dependent
  • Combined with beta lactams can treat sepsis (gram - )
  • Combined with beta lactams or vancomycin can treat endocarditis (enterococus, gram +)
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2
Q

3 Mechanisms of Aminoglycosides

A

1) blocks formation of ribosome complex
2) blocks proof reading- leading to misreads so the wrong amino acids are made
3) blocks ribosomal translocation on mRNA (Bactericidal/irreversible)

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3
Q

Streptomycin

A

-Aminoglycoside

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4
Q

Kanamycin

A

-Aminoglycoside

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5
Q

Gentamicin

A

-Aminoglycoside

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6
Q

Tobramycin

A

-Aminoglycoside

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7
Q

Amikacin

A

-Aminoglycoside

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8
Q

Neomycin

A

-Aminoglycoside

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9
Q

Aminoglycoside warnings

A
  • Nephrotoxicity (reversible)

- Ototoxicity (irreversible)

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10
Q

Tetracyclines

A
  • Bind to 30s ribosome
  • Prevents binding of incoming tRNA
  • Bacteriostatic
  • Effective against; gram+, gram-, and atypicals
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11
Q

Tetracycline

A
  • Tetracycline
  • Short acting
  • Don’t use in children 6 to 12, will mess up their teeth
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12
Q

Doxycycline

A
  • Long acting tetracycline
  • Eliminated in the Bile
  • Covers CAP and MRSA
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13
Q

Minocycline

A
  • Minocin
  • Long acting tetracycline
  • Covers P. acnes, meningitis, gonorrhea, Chlamydia, and MRSA
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14
Q

Tigecycline

A

-Longest acting tetracycline

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15
Q

Tetracycline Interactions

A
  • Take on an empty stomach
  • Dairy
  • Antacids
  • Iron
  • Zinc
  • All lower absorption
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16
Q

Doxycycline

A
  • Doryx

- Tetracycline

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17
Q

Macrolides

ACE

A
  • Bind reversibly to the 50s
  • Mainly covers Atypicals (STDs) and mycobacteria
  • Orally absorbed
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18
Q

Azithromycin

A
  • Zithromax
  • Macrolide antibiotic
  • Long half life
  • Does NOT use CYP450
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19
Q

Clarithromycin

A
  • Biaxin
  • Macrolide antibiotic
  • Short half life
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20
Q

Erythromycin

A

-Makes you poop (in low doses)

21
Q

Fidaxomicin

A
  • New Macrolide antibiotic
  • Stays localized in the gut
  • Covers C. diff
22
Q

Lincosamide

A
  • Binds reversibly to 50s ribosome to block exit of polypeptide
  • Spectrum= gram +(MRSA) and anaerobes (B. fragilis)
  • Box warning: May cause C. diff
23
Q

Clindamycin

A
  • Cleocin
  • Lincosamide
  • Covers B. fragilis (anaerobe)
  • Covers gram + (MRSA)
  • Black box warning-C.diff
24
Q

Streptogramins

A
  • Bind reversibly to the 50s ribosome
  • Blocks the exit of the polypeptide
  • Active against gram + cocci (Except for E. faecalis)
25
Q

Dalfopristin + Quinupristin

A
  • Streptogramins
  • Dalfopristin increases the binding affinity of Quinupristin
  • When used together they are bactericidal
  • May cause prolonged QT interval
  • CYP3A4 metabolized
26
Q

Streptogramins

A
  • Binds to 23s rRNA to prevent the assembly of ribosome
  • 100% orally bioavailable
  • Bacteriostatic in general
  • Bactericidal for streptococcus
  • Covers gram + (MRSA and E. faecium)
  • Used for serious vancomycin resistant infections
27
Q

Linezolid

A
  • Zyvox

- 1st generation Oxazolidinone

28
Q

Tedlizolid

A

-2nd generation Oxazolidinone

29
Q

Synercid

A
  • Dalfopristin + Quinupristin

- Streptogramin

30
Q

Drugs that cover P. aeruginosa

A

1) Ceftriaxone (3rd gen cephalosporin)
2) Cefepime (4th gen cephalosporin)
3) Aztreonam (Monobactam)

31
Q

Drugs that cover MRSA

A

1) Ceftaroline (5th gen cephalosporin)
2) Doxycycline (tetracycline)
3) Minocycline (tetracylcine)
4) Clindamycin (Lincosamide)

32
Q

Drug of choice for S. pnumoniae

A

-Ceftazidime + Avibactam (3rd gen cephalosporin)

33
Q

Which drug covers E. faecalis

A
  • Quinupristin + Dalfopristin

- Streptogramins

34
Q

What covers E. faecium

A
  • Linezolid

- Oxazolidinones

35
Q

Moxifloxacin

A
  • Avelox

- Fluoroquine antibiotic

36
Q

What drives ototoxicity in Aminoglycosides

A
  • Mitochondria have similar ribosomes to bugs
  • So abx may attack the hosts mitochondria
  • This damage leads to ototoxicity
37
Q

Name some aminoglycosides

-ycin,-icin

A
  • Neomycin
  • Kanamycin
  • Gentamicin
  • Amikacin
  • Plazomicin (zemdri)
38
Q

If a drug follows the rule of five then..

A
  • It is orally bioavailable

- If not try IV or inhalation

39
Q

Tobraycin Inhalation

A

-Can be used for cystic fibrosis patients

40
Q

Plazomicin (Zemdri)

A
  • New Aminoglycoside

- Administered IV

41
Q

MoA of Macrolides

A
  • Bind to 50s subunit
  • Inhibit the translocation of tRNA
  • 14 or 15 membered rings
42
Q

Azithromycin

A
  • Macrolide
  • Long half life
  • No potential for ketal
  • Acid stable
43
Q

Lincosaindes structure

A

-Contain thiomethyl aminooctoside, amide linked to Nmethly derivaive

44
Q

Tetracycline structure

A
  • Contains 4 fused six member rings
  • Act on 30s ribosomal subunit
  • Inhibits elongation of protein chain
45
Q

Purpose of adding amines

A
  • Adds on a bit of lipophilicity

- Increasing half life of the drug

46
Q

Tigecycline

A
  • Tetracycline
  • Half life > 24hrs
  • Resistant to efflux pumps
  • Can overcome some resistance
47
Q

Tedizolid strength

A
  • Has the ability to be given IV or orally

- Good for patients trying to get out of the hospital

48
Q

Why is Chloramphenicol not used

A
  • Due to toxicities
  • Binds to 50s subunit
  • Can see in medical tourists

IP3 exam #2 (12 decks)

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