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Pharmacology Exam 2 > Inhibitors of Protein Synthesis > Flashcards

Inhibitors of Protein Synthesis Flashcards

1
Q

Macrolide Drugs

A

Erythromycin, Clarithromycin, Azithromycin

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2
Q

Macrolide Key Notes

A

G+ (similar to Pen G)
Binds 50S
Bacteriostatic typically, but concentration/organism dependent
Oral absorption, biliary excretion, fecal elimination

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3
Q

Treating H. Pylori

A

Clarithromycin + Omeprazole + Ampicillin

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4
Q

Macrolide Resistance

A 
Efflux Pumps (main resistance)
Methylation of drug binding site (50S)
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5
Q

Macrolide Toxicity

A

GI disturbances- nausea, vomiting, diarrhea, etc. (E>A>C)
QT prolongation (A>E=C)
Drug interactions - CYP3A4 inhibitor (E=C>A)
IV erythro - Ototoxicity
Hepatic changes

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6
Q

Ketolide Drugs

A

Telithromycin (Ketek)

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7
Q

Telithromycin key notes

A

Broad Spectrum
Binds 50S at TWO sites
Bacteriostatic
Oral

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8
Q

Telithromycin Use

A

CAP (Good against respiratory pathogens, ie. erythromycin- and penicillin-resistant pneumococci)

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9
Q

Telithromycin Toxicity

A

Diarrhea, N/V, Dizziness
Contraindicated in patients with Myasthenia Gravis
Drug interactions - Metabolized by CYP3A4

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10
Q

Clindamycin Key Notes

A

Spectrum: aerobic G+ cocci and some anaerobic G- and G+ organisms. G- aerobes and enterococci are resistant.
Binds 50S
Bacteriostatic OR Bactericidal (concentration/organism dependent)
Metabolized by liver, minimally excreted by kidneys
Oral, Parenteral, and Topical

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11
Q

Clindamycin Use

A

OSTEOMYELITIS
Streptococci and staphylococci are extremely susceptible (MRSA).
Toxoplasma Encephalitis (NOT good for Meningitis)
Gram+ anaerobes
NOT for enterococci

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12
Q

Clindamycin Toxicity

A

CDAD (C. Diff Associated Diarrhea) - Well-known cause of pseudomembranous colitis (overgrowth of c. diff)
Rashes, GI disturbances

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13
Q

CDAD Treatment

A

STOP Clindamycin and START Metronidazole (DOC for c diff)

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14
Q

Clindamycin Contraindications

A

Pregnant and Nursing - Crosses placenta and distributed into breast milk

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15
Q

Streptogramin Drugs

A

Dalfopristin; Quinupristin (Synercid)

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16
Q

Streptogramin MOA

A

Dalfopristin - Binds 50S and inhibits EARLY phase

Quinupristin - Binds 50S and inhibits LATE phase

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17
Q

Two drugs that act synergestically

A

Dalfopristin & Quinipristin (Synercid) - Bactericidal

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18
Q

Synercid Use

A

Aerobic G+ including: PCNR S. pneumonia, MDR-streptococci
MSSA and MRSA
Vancomycin resistant enterococcus faecium

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19
Q

Synercid Administration

A

IV

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20
Q

Synercid Adverse Reactions

A

Hepatotoxicity, N/V, pain, pruritus, rash

Drug reactions - Inhibits CYP3A4

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21
Q

Synercid Contraindications

A 
Breast-feeding
Children
Hepatic Disease
Pregnancy
Streptogramin hypersensitivity
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22
Q

Ozazolidinone Drugs

A

Linezolid

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23
Q

Linezolid Spectrum

A

Aerobic G+ organisms

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24
Q

Linezolid MOA

A

Binds 23S RNA of the 50S subunit - unique to this drug
Prevents formation of a functional 70S
Bacteriostatic; except for streptococci (bactericidal)

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25
Q

Inhibitor of MAO (monoamine oxidase)

A

Linezolid

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26
Q

Linezolid Use

A 
G+ Infections:
Pneumonia
Skin infections
Vanco-resistant enterococcal (VRE) infections
MRSA
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27
Q

Linezolid Administration

A

IV or Oral

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28
Q

Oral admin is 100%

A

Linezolid

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29
Q

Linezolid Adverse Reactions

A

Diarrhea, HA, n/v

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30
Q

Linezolid Contraindications

A

Hypersensitivity
Pheochromocytoma
Drug interactions (ie. MAO inhibitors)
Tyramine rich food interactions (aged cheese, pork, smoked or pickled food)

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31
Q

Aminoglycoside Drugs

A

Streptomycin, Gentamicin, Tobramycin, Amikacin, Neomycin

32
Q

Which aminoglycoside is NOT topical?

A

Amikacin

33
Q

Which aminoglycoside is NOT IV/IM?

A

Neomycin

34
Q

Which aminoglycoside can be given orally?

A

Neomycin

35
Q

TB treatment

A

Isoniazid; Streptomycin is 2nd line; Ofloxacin 3rd

36
Q

Gentamicin, Tobramycin, Amikacin Spectrum

A

G-

37
Q

Aminoglycoside MOA

A

Binds 30S

BACTERICIDAL

38
Q

Which drugs require oxygen to be transported into the cell?

A

Aminoglycosides - Therefore they are only effective against aerobic organisms. Anaerobic are not susceptible.

39
Q

Aminoglycoside spectrum

A

Almost exclusively for Aerobic G- enteric bacteria (rods), or when there is suspicion of sepsis or endocarditis

40
Q

Streptomycin Uses

A

Tularemia (rabbit fever)
Bubonic plague
TB
Endocarditis when it is given along with other agents

41
Q

Gentamicin/Tobramycin/Amikacin Use

A

P. aeruginosa (DOC w/ antipseudomonal PCN)

42
Q

Neomycin and gentamicin use

A

Topical application of wounds and burns caused by G- organisms

43
Q

DOC for Enterococci infections

A

Streptomycin or Gentamicin + Pen G or Vancomycin

44
Q

Aminoglycoside toxicity

A

Ototoxicity and Nephrotoxicity dependent on duration of time the conc of drug is above threshold

45
Q

Which drugs have concentration dependent killing?

A

Aminoglycosides - Increasing concentrations kill an increasing population of bacteria, and at a more rapid rate

46
Q

Benefit of aminoglycosides

A

PAE (post antibiotic effect).
Single, large dose has better efficacy than multiple smaller doses by reducing the toxic side effects. This also helps with concentration dependent killing

47
Q

Downside of aminoglycosides

A

None is absorbed orally (only IM/IV and topical)
None penetrate CSF readily
Normal kidney rapidly excretes all.

48
Q

Aminoglycoside use should be…

A

In combination with other antibiotics

49
Q

Broad Spectrum IPS Abx

A

Chloramphenicol, Tetracyclines, Glycylcyclines

50
Q

Chloramphenicol Spectrum

A

BROAD SPECTRUM

One of the BEST synthetic abx we have, but very toxic. Used for life threatening infections.

51
Q

Chloramphenicol Toxicity

A

Fatal aplastic anemia (dose-INDEPENDENT)
Bone marrow suppression (dose-DEPENDENT)
“Gray baby” syndrome - inadequate glucuronyl transferase: can’t METABOLIZE

52
Q

Chloramphenicol Uses

A

RESTRICTED TO LIFE THREATENING CONDITIONS:
Typhoid Fever
Meningitis (Crosses CNS 100%) - Penicillin is DOC unless allergic
Rikettsia, Brucellosis, Rocky Mountain Spotted Fever, Melioidosis
Bacterial Conjunctivitis (topical)

53
Q

Chloramphenicol MOA

A

Binds 50S

Bacteriostatic (can be cidal against certain organisms)

54
Q

Reason for Chloramphenicol Toxicity

A

Inhibits mitochondrial protein synthesis in host cells!

55
Q

Distribution of Chloramphenicol

A

Distrubted WIDELY to all tissues, including EYES and CNS - Best CNS penetration of any medication.

56
Q

Metabolism of Chloramphenicol

A

Metabolized in liver (90%)
Conjugated with GLUCURONIC ACID
Metabolite excreted in the kidney
Potent inhibitor of CYP3A4 and CYP2C19

57
Q

Chloramphenicol Resistance

A

Acetyl Transferase - Acetylates and inactivates drug
Binding site modified
Efflux pumps

58
Q

Tetracycline Drugs

A

Tetracycline (oral/topical)
Doxycycline (oral)
Minocycline (oral)

59
Q

Tetracycline MOA

A

Binds 30S

Bacteriostatic

60
Q

Tetracycline Spectrum

A

BROAD SPECTRUM

61
Q

Tetracycline Resistant Organisms

A

B. fragilis
Proteus
Pseudomonas

62
Q

Tetracycline Uses

A 
H. Pylori (w/ Metronidazol and Bismuth)
Cholera (DOC)
Mycoplasma pneumonia (DOC, erythro)
Chlamydia (DOC, azithro/erythro)
Rickettsia (DOC for rocky mountain spotted fever)
Lyme Disease (early DOC, amoxicillin)
Vibrio species (DOC)
Amebiasis, acne, and gonorrhea (acute)
Brucellosis
Plague (in combo with aminoglycoside)
63
Q

Tetracycline Resistance

A

Tetracycline is susceptible to Efflux Pumps, but…

Tetracycline resistant strains can be treated with doxy, mino, and tigecycline which are resistant to efflux pumps

64
Q

Which tetracyclines have better oral absorption?

A

Doxy and Minocycline

65
Q

Chelating drugs

A

Tetracyclines chelate with Ca, Fe, and Al:
DON’T TAKE WITH VITAMINS
Can cause dental discoloration and inhibit bone growth

66
Q

Tetracycline Metabolism

A

Most are metabolized by liver and excreted in urine.
Doxycycline is EXCEPTION - Not hepatically metabolized and is excreted in feces.
Doxy –> Deuce

67
Q

Long acting tetracyclines

A

Doxycycline and Minocycline - Require less frequent administration

68
Q

Tetracycline Adverse Reactions

A 
GI disturbances
Bone growth inhibition/Dental discoloration
Liver damage
Fanconi syndrome (kidney damage)
Photosensitivity
Hypersensitivity is UNCOMMON
69
Q

Tetracycline Contraindications

A

Children <8 yrs old
Pregnant women
Nursing women

70
Q

Glycylcycline Drug

A

Tigecycline (Tigacil) - Synthetic derivative of minocycline

71
Q

Synthetic derivative of minocycline

A

Tigecycline

72
Q

Tigecycline administration

A

IV only!

73
Q

Tigecycline MOA

A

Binds 30S

Bacteriostatic

74
Q

Tigecycline Spectrum

A

BROAD Spectrum

Similar to tetracyclines, but shows activity against tetracycline-resistant organisms

75
Q

Tigecycline Uses

A

MRSA
S. epidermidis (MRSE)
PCN-resistant S. pneumoniae (PRSP)
Vancomycin-resistant enterococci (VRE)

76
Q

Tigecycline Adverse Reactions

A

Similar to tetracyclines.

Main adverse effect is n/v

Pharmacology Exam 2 (4 decks)

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