French Inhibitors of Protein Synth

Question 1

antibiotics that inhibiting protein synthesis?

Answer 1

Macrolides , Tetrocyclines, Lincomycins, Aminoglycosides, chloramphenicol, oxazolidinones, streptogamins

Question 2

antibiotics that inhibiting INITIATION of protein synthesis?

Answer 2

AGs,TCNs

Question 3

antibiotics that inhibiting ELONGATION of protein synthesis?

Answer 3

Chloramphenicol, MACs (Erythro), clindamycin

Question 4

Mech of action of MACs (Azithromycin)?

Answer 4

static - inhibit protein synthesis at same site as Cindamycin

Question 5

How do bacteria become resistant to MACs?

Answer 5

alter target (50S ribosome), efflux drug, inactivate drug

Question 6

How to administer Azithromycin?

Answer 6

PO on empty stomach

Question 7

MAC absorption?

Answer 7

good PO (some IV avilable)

Question 8

MAC distribution?

Answer 8

wide - goes to fetu. Accumultes in macs, skin, lungs, tonsils, cervix, sputum

Question 9

Azithromycin metabolism?

Answer 9

not metabolized - biliary excretion

Question 10

Dosing for Azithromycin?

Answer 10

QD - high tissue penetration & slow release

Question 11

MOST common clinical use for MACs?

Answer 11

G+ cocci (Strep & Staph), Atypicals (Chlamydia & mycoplasma)

Question 12

Adverse reactions caused by MACs?

Answer 12

GI disturbance, hepatotoxicity, prolonged QT interval

Question 13

DDI with MACs?

Answer 13

Erythromicin & clarithromycin can inhibit CYP450

Question 14

How do MACs cause GI upset?

Answer 14

drug (especially erythro) binds motilin receptor

Question 15

Do all MACs cause DDIs?

Answer 15

no! remember ACE (Azithro is A-ok, but Clarithro & Erythro Cause Effect)

Question 16

Mech of action for TCNs?

Answer 16

static - binds 30S ribosome

Question 17

How are TCNs selective?

Answer 17

host cells have efflux protein

Question 18

resistance to TCNs?

Answer 18

MDR receptors (efflux), proteins that bind TCN

Question 19

TCN absorption?

Answer 19

PO (impaired by milk products)

Question 20

TCN distribution?

Answer 20

Fetus!

Question 21

TCN elimination?

Answer 21

Doxy/mino = hepatic, other TCNs = renal

Question 22

Spectrum of use for TCN?

Answer 22

Broad

Question 23

common clinical use for TCNs?

Answer 23

MRSA, Atypicals (chlamydia, mycoplasma)

Question 24

ADRs to TCNs?

Answer 24

Teeth & bones, Super infections (fungal), yeast overgrowth, photosensitivity, liver/kidney toxicity, GI disturbance

Question 25

DDIs with TCNs?

Answer 25

Antacids & Iron supplements (decrease bioavailability)

Question 26

Mechanism of action for Clindamycin (lincomycins)?

Answer 26

statos - binds 50S ribosome

Question 27

Route of absorption for Clindamycin?

Answer 27

PO (also IV)

Question 28

Clindamycin distribution?

Answer 28

especially into bone

Question 29

Clindamycin elimination?

Answer 29

heptaobiliary elimination & breast milk

Question 30

Spectrum for Clindamycin?

Answer 30

narrow (G+ cocci & Anaerobes) choice in MRSA

Question 31

ADRs to Clindamycin?

Answer 31

Superinfection (CDAD, pseudomembranous colitis), diarrhea

Question 32

Mechanism of action for Aminoglycosides?

Answer 32

CIDAL - irreversibly binds 30S, requires O2

Question 33

Resistance to AGs?

Answer 33

chemically modify AGs, decrease drug influx, change ribosomal target

Question 34

AGs absorption? Route?

Answer 34

poor oral absorption, route: IV/IM

Question 35

AGs distribution?

Answer 35

ECF, especially: renal cortex & inner ear

Question 36

AGs elimination?

Answer 36

renal

Question 37

AGs dosing?

Answer 37

once daily, narrow Therapeutic Index so requires Cp monitoring

Question 38

AGs spectrum?

Answer 38

narrow (G- aerobes: pseudomonas & E coli, M. tuberculosis, enterococci)

Question 39

ADR to AGs?

Answer 39

ototoxicity, nephrotoxicity (requires regular Cp monitoring)

Question 40

AGs DDI?

Answer 40

PCNs irreversibly binds and inhibits AGs

Question 41

Mech of action for Chloramphenicol?

Answer 41

statis - inhibits 50S ribosome (including mitochondrial ribosomes in bone marrow)

Question 42

Resistance to Chloramphenicols?

Answer 42

impermeability, inactivation by bacterial enzymes

Question 43

Chloramphenicol Absorption?

Answer 43

PO (also IV)

Question 44

Chloramphenicol distribution?

Answer 44

wide - including CSF

Question 45

Chloramphenicol elimination?

Answer 45

liver (glucouronidation) - neonates cannot process

Question 46

Chloramphenicol Spectrum?

Answer 46

broad (G+/- cocci, anaerobes including Bacteroides, Atypicals)

Question 47

ADR to chloramphenicol?

Answer 47

bone marrow toxicity (aplastic anemia), Gray baby syndrome (hepatotoxicity), GI

Question 48

Mech of action for Oxazolidinones?

Answer 48

static - binds 50S, inhibits formation of 70S complex

Question 49

Oxazolidinones absorption?

Answer 49

excellent PO (also IV)

Question 50

Oxazolidinones elimination?

Answer 50

nonenzymatic oxidation & renal

Question 51

Oxazolidinones Spectrum?

Answer 51

last resort - G+ (multi resistant)

Question 52

ADRs to Oxazolidinones?

Answer 52

thrombocytopenia

Question 53

DDI to Oxazolidinones?

Answer 53

inhibits MAO (hypertensive response, serotonin syndrome)

Question 54

Mech of action for Streptogamins?

Answer 54

CIDAL - binds 50S & inhibits elongation

Question 55

Streptogamin absorption?

Answer 55

IV only

Question 56

Streptogamin elimination?

Answer 56

hepatic conjugation, biliary excretion

Question 57

Streptogamin Spectrum?

Answer 57

last resort G+ & atypicals

Question 58

ADRs to Streptogamin?

Answer 58

infusion related, inhibits CYP3A4