Agents Targeting Cellular Machinery Flashcards

1
Q

what drugs are aminoglycosides

A

Amikacin

Gentamicin

Kanamycin

Neomycin

Streptomycin

Tobramycin

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2
Q

what drug type is azithromycin, clarithromycin, erythromycin

A

Macrolides

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3
Q

what types of drugs are protein synthesis inhibitors

A

Tetracyclines

Aminoglycosides

Macrolides

Clindamycin, Chloramphenicol, Linezolid

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4
Q

what groups of drugs target DNA

A

Sulfonamides

Trimethoprim

Fluoquinolones

Metronidazole

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5
Q

what group is “-floxacin”?

A

Fluoroquinolones

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6
Q

what drugs are protein synthesis inhibitors

A

Aminoglycosides

Macrolides

Tetracycline

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7
Q

Do protein synthesis inhibitors exert a bacteriostatic or bacteriocidal effect?

A

Bacrteriostatic, some can be bactericidal

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8
Q

HOW do protein synthesis inhibitors work?

A

disrupt process of translation by targeting the molecular machinery needed to translate mRNA to protein

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9
Q

Name aminoglycosides (protein synthesis inhibitors)

A

streptomycin

gentamicin

kanamycin

amikacin

tobramycin

neomycin

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10
Q

Aminoglycosides are considered to have a 1 spectrum of activity resulting in a 2 (bacteriostatic/-cidal) effect

A
  1. broad

2. bactericidal

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11
Q

what organisms to aminoglycosides work against

A

aerobic organisms (uptake is oxygen dependent)

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12
Q

Aminoglycosides are 1 inhibitors. They are used in combo with 2 to treat serious gram 3 infections (penumonia, UTI) and are not absorbed will from the 4

A
  1. protein synthesis
  2. beta-lactams
  3. gut
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13
Q

MOA of aminoglycosides

A

binds to 30S and blocks formation of initiation complex

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14
Q

Key adverse effects of aminoglycosides

A

nephrotoxicity

ototoxicity

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15
Q

Macrolides mainly target gram + but some gram -. But overall narrow in spectrum. list the drugs in order from broadest to lowest spectrum

A

Azithromycin>Clarithromycin>Erythromycin

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16
Q

which macrolide has a long 1/2 life

A

Azithromyucin

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17
Q

where does azithromycin concentrate

A

Lungs
Tonsils
Cerivx

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18
Q

Key adverse effects of macrolides

A

GI issues

CV: prolong QT interval

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19
Q

drugs that are tetracyclines

A

tetracycline

minocycline

tigecycline

doxycycline

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20
Q

MOA of macrolides

A

Impairs translocation - blocking elongation or growing

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21
Q

MOA of tetracyclines

A

Binds to 30S subunit of ribosomes and prevents binding of tRNA

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22
Q

Tetracyclines are a 1 spectrum antibiotic that exerts a 2 effect

A
  1. broad

2. bacteriostatic

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23
Q

Key adverse effects of tetracyclines

A

Nutrient interactions: bind calcium which disrupts in growth of calcified tissue (bone, teeth) particularly during growth, discoloration of teeth

Ecological effect: disrupt normal flora

photosensitivity

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24
Q

whcih tetracyclines absorption is not affected by food

A

doxycycline

25
Q

which tetracycline undergoes urine excretion, so kidney function must be considered

A

tetracycline

minocycline

tigecycline

26
Q

which tetracycline undergoes liver excretion, so hepatic function must be considered

A

doxycycline

27
Q

what is clindamycins spectrum of activity? what is it used for

A

relatively narrow

soft tissue infections caused b streptococci and staphylococci

community acquired MRSA of skin and soft tissue

28
Q

MOA of clindamycin

A

prevents formation of initiation complex

29
Q

key adverse effects of clindamycin

A

GI

C. diff infection**

30
Q

Chloramphenicol is a 1 spectrum antibiotic that exerts a 2 effect

Rarely used except for serious infections such as 3 and 4. Can also be used to treat 5 infections

A
  1. broad
  2. bacteriostatic
  3. typhus
  4. rocky mountain spotted fever
  5. eye
31
Q

MOA of chloramphenicol

A

prevents transpeptidation or peptidyl bond formation

32
Q

key adverse effects of chloramphenicol

A

blood: suppression of RBC production

Gray baby syndrome: infants lack glucuronic acid conjugation

33
Q

Linezolid is effective against most gram 1 organisms.

A

positive

34
Q

because of its unique mechanism which protein synthesis inhibitor is effect against penicillin, methicillin, and vancomycin resistant organisms

A

Linezolid

35
Q

MOA of linezolid

A

inhibits formation of the ribosomal-fMet-tRNA complex

36
Q

Key adverse effect of linezolid

A

myelosuppression

37
Q

what protein synthesis inhibitor is good for hospital acquired MRSA and resistance strains

A

Linezolid

38
Q

what protein synthesis inhibitor has 100% bioavailability

A

Linezolid

39
Q

Sulfonamides are 1 agents that are 2 spectrum.

A
  1. antifolate

2. broad

40
Q

MOA of sulfonamides

A

structural similarity to PABA. Agents compete with PABA for the enzyme dihydropteroate synthase and block dihydrofolic acid synthesis and thus DNA synthesis

41
Q

key adverse effects of sulfonamides

A

photosensitivity

42
Q

what drug classes are folate synthesis inhibitors

A

sulfonamides

trimethroprim (and pyrimethamine)

43
Q

Trimethorpim and pyrimethamine spectrum of activity includes 1 bacteria. Used commonly to treat 2

A
  1. gram -

2. UTI

44
Q

MOA of trimethoprim and pyrimethamine

A

inhibitor of bacterial dihydrofolate reductase resuling in impaired DNA synthesis

45
Q

key SE of trimethoprim and pyrimethamine

A

blood: bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia

46
Q

Trimethoprim-sulfamethoxazole is a 1 agent that is commonly used to treat 2 and 3. MOA includes 4 activity when combining the 2 drugs

A
  1. antifolate
  2. UTI
  3. prostatitis
  4. synergistic
47
Q

what drug is a DNA gyrase inhibitor

A

fluoroquinolones

48
Q

Fluorquinolones are 1 spectrum antibiotics that work against gram 2 bacteria

A
  1. broad

2. + and -

49
Q

MOA of fluoroquinolones

A

dirsupt the winding of DNA and separation of DNA strands during transcription and replication

inhibit topoisomerase II (DNA gyrase) and IV

50
Q

key SE of fluorquinolones

A

GI

drug-nutrient interaction: bind divalent cations and prevent absorption

Cardio: QT elongation

51
Q

least active florquinolone

A

norflaxacin

52
Q

fluorquinolones that work well againsts gram - and some activity against +

A

group 2

  • ciprofloxacin
  • levofloxacin
  • ofloxacin
53
Q

fluoroquinolones that have best activity against gram +

A

group 3

  • gatifloxacin
  • gemifloxacin
  • moxifloxacin
54
Q

what type of drug is DNA damaging agents

A

Metronidazole

55
Q

Metronidazole is also effective against 1. Its spectrum of activity is limited to 2 bacteria. It is used in tx of 3

A
  1. protozoa
  2. anaerobic
  3. c. diff
56
Q

MOA of metronidazole

A

Prodrug - rxn metabolites bind to DNA and disrupt function causing damage

57
Q

key adverse effects of metronidazole

A

GI

metabolism: disulfiram-effect (avoid alcohol)

58
Q

what does ciprofloxacin treat

A

UTI

abdominal

respiratory

skin soft tissue

anthrax