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Pathophys/Pharm > Antibiotic Classes and MOA > Flashcards

Antibiotic Classes and MOA Flashcards

1
Q

What are the targets for killing a cancer cell?

A

DNA and Mitotic tubules

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2
Q

Do we want to target what we do in cancer cells when trying to kill bacteria?

A

NO. Because bacterial cells have things in them that our cells don’t and therefore we can target that

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3
Q

What are some things we target in bacterial cells?

A
  • Cell wall synthesis
  • Transcription and translation
  • DNA synthesis and integrity
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4
Q

What do bacteriostatic drugs do?

A
  • Inhibits cell growth, does NOT kill the cell

- They slow down the spreading of the bacteria and then the immune system takes over for the rest

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5
Q

What do bactericidal drugs do?

A

Kill bacteria

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6
Q

What do bacteriostatic drugs target?

A

Protein synthesis (except aminoglycosides)

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7
Q

What do bactericidal drugs target?

A

Cell wall synthesis

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8
Q

Who should get bacteriostatic drugs?

A
  • Non-immune compromised

- Uncomplicated infections

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9
Q

Who should get bactericidal drugs?

A

Immune compromised (particularly if life threatening infection)

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10
Q

How many drugs are bacterial infections usually treated with?

A

1 drug

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11
Q

What is antibiotic synergism and when would you use it?

A
  • Combination therapy (using 2+ antibiotics)
  • Can be critical for life-threatening infections
  • Infrequently would 2 antibiotics in the same class be used together
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12
Q

What is the MIC?

A
  • Minimal inhibitory concentration (minimal effective dose)
  • When the curve drops below the MIC you must redose
  • how much drug you need to stop the bacteria from growing
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13
Q

When are concentration dependent antibiotics most effective?

A

When they have a high peak concentration

  • Highest concentration kills
  • Aminoglycosides
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14
Q

When are time-dependent antibiotics most effective?

A

When there is a long exposure to a drug

  • Longest duration over MIC kills
  • Beta-lactams
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15
Q

What makes up the cell wall?

A

Peptidoglycan

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16
Q

Why is peptidoglycan a target for antibiotics?

A

Three enzymes are needed to build the polymer and all three are targets for antibiotics

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17
Q

What is peptidoglycan made of?

A

Two amino sugars in chain cross-linked to 5 amino acids

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18
Q

What are the two sugars in peptidoglycan and which has amino acids attached to it?

A

NAG and NAM

-NAM has the amino acids on it

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19
Q

How are the sugars connected?

A

They are cross-linked via 5 glycines and this is referred to as TRANSPEPTIDASE ENZYME

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20
Q

What is the target for beta lactam drugs?

A

Transpeptidase enzyme

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21
Q

What are three reasons for antibiotic resistance to penicillin?

A
  1. Bacteria developed “penicillinase enzymes”
  2. Bacteria have resistant transpeptidase enzymes
  3. Bacteria have multiple resistance patterns
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22
Q

What is the function of an OAT?

A

Secretes penicillin drugs into urine, enhancing elimination

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23
Q

What is probenicid?

A
  • OAT inhibitor
  • Using probenicid with penicillin helps prolong blood and tissue levels of the antibiotics, giving longer duration of efficacy
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24
Q

Why would you not want to give probenicid to a patient with a UTI?

A

Because probenicid keeps the drug away from the urine so its not excreted, but with a UTI we want the drug to go to the urine

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25
Q

______ have surpassed the use of oral amino and natural penicillins.

A

Oral Cephalosporins

26
Q

What are the two most common oral cephalosporins used currently?

A

Cefdinir and Cefpodoxime (both are 3rd generation)

27
Q

Unless a resistant organism has been previously identified, what two generations of cephalosporins can be started for broad empiric coverage?

A

3rd or 4th generation

28
Q

What generation are common pre-op antibiotics when viscera are not entered?

A

1st generation

29
Q

Why is it necessary to use a different beta lactam antibiotic when treating a strept throat infection vs an E. coli UTI?

A

Because even though all bacteria have the transpeptidase enzyme, different transpeptidase enzymes are found in different bacteria

30
Q

What are processes of the cell wall we target to kill the cell?

A
  1. Transpeptidase (BLs)
  2. Transglycosylation (binds NAG-NAM units together)
  3. Transamination (binds the peptides to NAM)
31
Q

What is the action of vancomycin?

A

Inhibits cell wall synthesis

  • Blocks transglycosylase (binding of NAM and NAG)
  • Blocks transpeptidase
  • Bactericidal
32
Q

Does vancomycin treat gram + or -?

A

Gram + ONLY

33
Q

What route is vancomycin given?

A
  • Poorly absorbed orally

- IV requires monitoring to prevent renal and ototoxcitiy

34
Q

What are the chemical properties of vancomycin?

A
  • Glycopeptide
  • BIG molecule
  • Polar
  • Water soluble
35
Q

What is vancomycin used for?

A

BIG GUN

  • Only used for severe or resistant gram positive infections
  • Sepsis due to strep. pneumo or MRSA
36
Q

What are potential side effects of vancomycin?

A
  • Red man syndrome

- Renal and Oto toxic (too high blood levels of vancomycin can cause dead kidneys and deafness)

37
Q

Is vancomycin a concentration-dependent or time-dependent drug?

A

Time-dependent

  • Its efficacy is primarily dependent on Duration of time above the MIC, not the Cpeak
  • Too high Cpeak is toxic!!!
38
Q

What drug class is daptomycin?

A

Lipopeptide

39
Q

What is the action of daptomycin?

A

Toxic to the cell wall and cell membrane

  • Binds to the membranes and disrupts non-polar permeability
  • Bactericidal
  • Won’t use unless consulted with infectious disease
40
Q

What is the action of fosfomycin?

A

It blocks an early step in cell wall synthesis

41
Q

What is fosfomycin a good choice to treat?

A

Uncomplicated UTI

*Beta-lactam allergies

42
Q

How can we target protein synthesis in bacterial cells without it hurting our own cells?

A

Human ribosomes (which are responsible for protein synthesis) have 40s and 60s subunits while bacterial ribosomes have 30s and 50s ribosomes

43
Q

What drug classes are protein synthesis inhibitors?

A
  • Tetracyclines (30s bacteriostatic)
  • Macrolides (50s bacteriostatic)
  • Aminoglycosides (30s bactericidal)
  • Lincosamides & Oxazolidinones (50s bacteriostatic)
44
Q

What two drugs in the tetracycline class do we most often use?

A
  • Doxycycline

- Minocycline

45
Q

What is Tigecycline?

A

A new tetracycline

  • Only indication is Gram + resistant organisms like MRSA
  • Never use for UTI
  • Restricted drug
  • Not able to order this for uncomplicated cellulitis
46
Q

What is the tetracycline class good for?

A

-Well distributed in water/urine (UTIs, urethritis)

47
Q

What are tetracyclines not good for?

A
  • Not good for CNS infections as they are too large/polar to cross into CNS (not for meningitis)
  • Drugs chelate calcium which discolors teeth (don’t take with dairy products)
48
Q

What is the most often used macrolide?

A

Azithromycin (Z-pak)

49
Q

What macrolide is infrequently used?

A

Erythromycin because it has many drug/drug interactions

50
Q

What are the common aminoglycosides that are used?

A
  • Gentamicin

- Tobramycin

51
Q

What is the action of aminoglycosides?

A
  • Irreversible inhibitors of protein synthesis
  • Moves into cells via porin channels
  • Actively transported into cytoplasm
  • Binds to 30s subunit of ribosome
52
Q

What should you not use aminoglycosides for?

A

Meningitis (poor CNS penetration)

53
Q

Are aminoglycosides concentration dependent or time dependent?

A

Concentration, higher concentration = higher kill rate

  • But higher concentration enhances toxicity risk
  • Blood levels and kinetics need to be obtained
  • Oto and nephrotoxic (best to get patient off of these and onto less toxic drugs)
54
Q

What two drugs are sulfonamides (anti folate drugs)

A

-Trimethoprim
-Sulfamethoxazole
(if these two are given together its bactrim)

55
Q

What can you NOT use sulfonamides for?

A

Streptococcus

56
Q

What is the most common use for sulfonamides?

A

UTI (e. coli)

57
Q

What three drugs are fluoroquinolones?

A
  • Ciprofloxacin
  • Levofloxacin
  • Moxifloxacin
58
Q

What is the action of fluoroquinolones?

A

Inhibit bacterial topoisomerase II

59
Q

What are known complications of fluoroquinolones?

A

Tendon rupture, skeletal muscle injury, peripheral neuropathy

60
Q

What drug is a nitroimidazole?

A

Metronidazole

61
Q

What is metronidazole good to treat?

A

ANAEROBES

-Pelvic, vaginal, and intra-abdominal infections (including STDs, post-operative, perforations)

Pathophys/Pharm (9 decks)

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