Renal: 9. Bridges : Protein Synthesis Inhibitors Ii & Iii

Front 1

where do tetracyclines prevent protein synthesis?

Back 1

30S ribosome

Front 2

Tigecycline is used for what

Back 2

MRSA

and really bad resistant stuff

Front 3

tetracyclines are ___ spectrum

Back 3

broad

wide range of aerobic and anaerobic G+ & G- bacteria

Front 4

Chlamydia, Rickettsia, mycoplasma p. can be readily treated with this broad spectrum drug

Back 4

Tetracycline

Front 5

2 most widely prescribed tetracyclines?

Back 5

Doxycycline & minocycline

Front 6

if a pt has poor renal function, what would be your tetracycline of choice?

Back 6

Doxycycline

Front 7

what tetracycline can enter the CSF?

Back 7

minocycline

for meningococcal carrier state

Front 8

DOC or alternative for
Mycoplasma p

Back 8

Tetracyclines

Front 9

DOC or alternative for chlamydia

Back 9

Tetracyclines

Front 10

DOC or alternative for Rickettsiae

Back 10

Tetracyclines

Front 11

DOC or alternative for Lyme Disease

Back 11

Tetracyclines

Front 12

DOC or alternative for Anthrax

Back 12

Tetracyclines

Front 13

Tetracyclines are bacterio____

Back 13

STATIC

Front 14

tetracycline MOA

Back 14

Tetracyclines bind reversibly on 30S to interfere with charged tRNA and keep from binding to acceptor site

Front 15

what is the resistance to tetracycline at the ribosomal level?

Back 15

bug produces a protein to protect itself. this protein competes with the drug for binding and kick it off

Front 16

what are the 2 mechanisms of resistance to teteracyclines

Back 16

1. efflux pumps

2. ribosome protection

proteins that interfere with tetracycline binding
they dislodge drug from the ribosome & increase the apparent kd of drug binding to the ribosome

Front 17

what are the bacteriocidals and statics?

Back 17

Bacteriocidals: Very Finely Proficient At Cell Murder- Vancomycin, Fluoroquinolones, Penecillins, Aminoglycosides, Cephalosporins, Metronidazole

Bacteriostatics: We're ECSTaTiC about bacteriostatics!- Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol

Front 18

what drug chelates and messes with absorption of certain vitamins and the drug itself

Back 18

Tetracyclines

Front 19

pt says their stomach gets upset when they take this drug. So they want to take milk, or antacids with it. You know that this drug forms stable chelates, which messes with absorption. What is the drug?

Back 19

Tetracyclines

Front 20

pt has taken tetracycline since they were 3. what might this do to the mouth

Back 20

staining of mandiublar teeth

Chelates with calcium
concentrates in bone & teeth

Front 21

what tetracyclines are less dependent on kidneys for elimination?

Back 21

Doxycycline and minocycline are less dependent on kidneys for elimination

no dosage adjustment with compromised renal function
excreted in bile

Front 22

MRSA, Staph epidermis, penicillin-resistant streptococcus pneumoniae (PRSP), vancomycin-resistant enterococcus (VRE)... consider using

Back 22

Tigecycline

Front 23

how is tigecycline administered?

Back 23

IV

Front 24

why is tigecycline not useful for UTIs?

Back 24

biliary excretion!!

Front 25

tetracyclines should not be used in what populations due to tooth affects?

Back 25

Children (Readily bind in newly formed bone or teeth in young children)

preggo women, it can cross the placenta

Front 26

just note that tetracyclines can cause

Liver Toxicity
Rare but can be fatal
Occurs more commonly with tetracycline and minocycline and less often with doxycycline

Local Tissue Toxicity
Directly irritating to tissues …
IV: thrombophlebitis (frequent w/ prolonged use)
IM: painful (avoid route)

Back 26

had to say this...it was just a rando slide that I couldn't think of a question

Front 27

pt comes in and has very bad sunburn from limited exposure to the sun..what caused this

Back 27

tetracyclines

photosensitive

Front 28

Pt grabs an old bottle of tetracycline. They feel like they have an infection so they start popping it even though the expiration date is well past due. What can this cause?

Back 28

Fanconi syndrome

kidney tox!

Front 29

Chloramphenicol acts where?

Back 29

Protein Synthesis Inhibitors acting at the 50S ribosome

Front 30

this is a drug of last resort, for life-threatening infections.

Back 30

Chloramphenicol

Front 31

what is the biggest tox of Chloramphenicol?

Back 31

bone marrow suppression

Anemia, leukopenia, thrombocytopenia
Dose-dependent
Reversible

Front 32

what is an idiosyncratic response?

what drug has a tox that can act like this?

Back 32

just pops up out of nowhere

Chloramphenicol

(remember it can wipe out bone marrow, so it could kill someone)

Front 33

newborn baby was given a drug that causes Gray color, shock, hypothermia, vomiting, flaccidity
Can be fatal within 2 days of initial symptoms
40% mortality rate

what was the drug?

Back 33

Chloramphenicol

Front 34

Erythromycin
Clarithromycin
Azithromycin

are what kind of drugs?

Back 34

macrolides

Front 35

what is a good substitute for penicillins?

Back 35

macrolides

Front 36

DOC for Campylobacter jejuni

Back 36

Macrolides

Front 37

DOC for H pylori

Back 37

Macrolides

Front 38

DOC for Shigella spp.

Back 38

Macrolides

Front 39

Macrolides are a go to for what groups (alt to tetra)

Back 39

children & pregnant females (alternative to tetracyclines)

Front 40

what drug class is best used for URIs

Back 40

macrolides

Front 41

DOC for Mycoplasma pneumoniae

Back 41

Macrolides

Front 42

DOC for Chlamydia

Back 42

Macrolides

Front 43

DOC for Bordetella p. (Whooping cough)

Back 43

Macrolides

Front 44

DOC for Campylobacter (enteritis)

Back 44

Macrolides

Front 45

Macrolides are bacterio____

Back 45

static

Front 46

MOA for Macrolides

Back 46

reversibly binds 50 ribosome
inhibits peptide chain elongation
inhibits translocation of peptidyl tRNA from A to P site

Front 47

2 resistance against Macrolides

Back 47

efflux pump

ribosome modification

Front 48

what is the ribosome modification in macrolides that provide resistance?

Back 48

Methylation alters the macrolide binding site on bacterial ribosome

(note this is different than the tetracyclines!)

Front 49

erythromycin is less ____ than the newer macrolides?

Back 49

acid-stable

aka it has worse oral absorption

Front 50

this marcolide is taken once a day and has a long half-life. good for pt compliance

Back 50

Azithromycin

Front 51

macrolides can inhibit what?

Back 51

CYP3A4

Front 52

what GI effects do macrolides have?

**

Back 52

Directly stimulates GI motility

can cause anorexia, NVD, epigastric distress

Front 53

number one reason for stopping erythromycin?

Back 53

Directly stimulates GI motility-->epigastric distress

Front 54

Cholestatic hepatitis can be a side effect of?

Back 54

erythromycin

Front 55

Clindamycin acts where

Back 55

Protein Synthesis Inhibitors acting at the 50S ribosome

Front 56

Clindamycin is bacterio_____

Back 56

static

Front 57

spectrum of use for Clindamycin

Back 57

Treatment of anaerobic and streptococcal & staphylococcal infections (skin/soft tissue)

Front 58

DOC for C. perfringens

Back 58

Clindamycin

Front 59

primary resistance to clindamycin?

Back 59

Alteration of ribosomal binding site
primarily by methylation (like the macrolides)
Cross resistance may be seen with erythromycin

Front 60

what drug can penetrate well into bones?

Back 60

Clindamycin

Front 61

what drug can be actively transported into polymorphonuclear leukocytes and macrophages?

Back 61

Clindamycin

Front 62

diarrhea and pseudomembranous colitis can be adverse effects of?

Back 62

Clindamycin

Front 63

what drug is most likely to cause pseudomembranous colitis (not based on % of time the drug is used, just by how it works)

Back 63

Clindamycin

Front 64

where do quinupristin + dalfopristin
work?

Back 64

Protein Synthesis Inhibitors acting at the 50S ribosome

Front 65

effective against G+ bacteria
staphylococci resistant to
Methicillin (MRSA) (alt)
Quinolones
Vancomycin

you would use?

Back 65

quinupristin + dalfopristin

Front 66

DOC for Vancomycin-resistant Enterococcus faecium (VRE)

Back 66

quinupristin + dalfopristin

Front 67

principle use of quinupristin + dalfopristin?

Back 67

drug resistant G+ cocci infections

bacteremia and soft tissue infections

Front 68

quinupristin + dalfopristin are bacteri_____

Back 68

cidal

Front 69

MOA for quinupristin + dalfopristin

Back 69

Quinupristin:
binds at same site as macrolides (prevent peptide chain elongation, can't move A to P)

Dalfopristin
directly interferes with polypeptide chain formation
binds near quinupristin; synergistically enhances binding of quinupristin

Front 70

resistance to dalfopristin?

Back 70

Enzymatic inactivation
Efflux pump

Front 71

resistance to quinupristin??

Back 71

Binding site modification by methylase
Enzymatic inactivation

Front 72

Quinupristin & dalfopristin do what to P450 enzymes?
**

Back 72

Potent CYP3A4 inhibitor
Appropriate caution and monitoring recommended for drugs in which the therapeutic index is narrow

Front 73

what can cause severe arthralgias and myalgias?

Back 73

Quinupristin & dalfopristin

Front 74

Linezolid works where

Back 74

Protein Synthesis Inhibitors acting at the 50S ribosome

Front 75

spectrum of Linezolid?

Back 75

Similar to quinupristin & dalfopristin (G+ bacteria) plus E. faecalis

Should be reserved for MDR G+ bacteria

Front 76

DOC for pen resistant strep pneumo, and MRSA?

Back 76

Linezolid

Front 77

DOC for enterococcus faecium AND faecalis

Back 77

Linezolid

Front 78

MOA for Linezolid

Back 78

Binds to 50S to block formation of initiation complex
Mostly ‘static’ (cidal for streptococci)

Front 79

resistance to Linezolid

Back 79

Mutation of rRNA binding site

Front 80

you should avoid tyramine rich food with use of what?

Back 80

Linezolid

Front 81

this drug should be avoided with use of adrenergic or serotonergic drugs (SSRIs)

Back 81

Linezolid

Front 82

VRE, MRSA, serious G+... use?

Back 82

Daptomycin

Front 83

MOA for Daptomycin

Back 83

causes loss of gradient of the ions needed for DNA and RNA for protein synthesis

pokes holes in the membrane

Front 84

Daptomycin is bacteri_____

time or conc depend?

Back 84

cidal

conc dependet

Front 85

clearance of daptomycin?

Back 85

renal

Front 86

one thing daptomycin doesn't really work for?

Back 86

pneumonia

Front 87

this drug can cause Skeletal muscle damage (myopathy)

Back 87

Daptomycin