Lecture 2

Question 1

Vancomycin is a _____

Answer 1

glycopeptide

Question 2

Vancomycin inhibits cell wall _____ formation by binding to the _____ side chain of cell wall precursors

Answer 2

Peptidoglycan;

D-ala D-ala

Question 3

Vancomycin treats gram __ bacteria only, and is bacterio____

Answer 3

+, cidal

Question 4

VRE’s appeared after the use of ____, a glycopeptide antibiotic, was used as a feed additive in live stock

Answer 4

avoparcin

Question 5

Mechanism of VRE resistance:

Answer 5

mutation of PG cell wall precursor from D-ala D ala to D-ala-D-lactate

Question 6

Side effects of vancomycin: NOT

Answer 6

Nephrotoxicity,
Ototoxicity,
Thrombophlebitis

Question 7

Vancomycin can cause ___ man syndrome, which is diffuse flushing of the skin due to ____

Answer 7

red;

histamine

Question 8

Macrolides are macrocylic ____, usually __-membered rings

Answer 8

lactones; 14

Question 9

Macrolides are poly____, because they are produced by sequential addition of ____ groups to a growing chain

Answer 9

ketides;

proprionate

Question 10

Mechanism of Macrolides:

bind reversible to the __ site of the ribosome, inhibiting ____ of the peptidyl-tRAN from the __ to the ___ site

Answer 10

P; translocation;

A; P

Question 11

Macrolides typically bind the ___ RNA of the ___ ribosomal subunit

Answer 11

23S; 50S

Question 12

Mechanisms of macrolide resistance:
____ is induced to degrade the macrolides
efflux pump ejects the drugs via ____ transport

Answer 12

lactone ethyl hydrolase

active

Question 13

Mechanisms of macrolide resistance:
Drug induced production of an RNA _____. A specific adenine base on the ___ RNA molecule of the 50s ribosomal subunit is ____

Answer 13

methylase
23s
methylated

Question 14

Mechanisms of macrolide resistance:

mutation of ___ to ____ at the specific site A2058

Answer 14

Adenine to guanine;

reduces affinity

Question 15

Macrolides can be inactivated under ____ conditions by a process involving the ___ group

Answer 15

acidic

6-OH

Question 16

Acidic conditions cause ___ formation in macrolides, inactivating them and causing GI ____

Answer 16

ketal, cramping

Question 17

Clarithromycin is more acid ____ due to blocking ketal formation via a 6-____ derivative

Answer 17

stable

6-OCH3

Question 18

Azithromycin is acid ____ due to it being an ____ analog

Answer 18

stable

amine

Question 19

The main route of erythromycin metabolism is ____ in the liver. It is eliminated mainly via ____

Answer 19

demethylation

bile

Question 20

Erythromycin and clarithromycin bind and _____ _____ and related P450 encymes

Answer 20

inhibit CYP3A

Question 21

Inhibition of CYP450 causes an _____ in activity of other drugs, besides ____, which is a CYP inducer

Answer 21

increase

Rifampicin

Question 22

Side effects of macrolides can be remembered by: _____

Answer 22

MACRO

Question 23

The M in MACRO stands for _____

Answer 23

Motility (GI issues)

Question 24

The A in MACRO stands for ____ caused by long _____ interval

Answer 24

arrhythmia; QT

Question 25

The C in macro stands for _____. It is reversible/irreversible

Answer 25

cholestatic hepatitis; reversible

Question 26

The R in MACRO stands for ____. Serious side effects related to this term include ____ and _____

Answer 26

Rash;
stevens-johnson syndrome;
toxic epidermal necrolysis 0_0

Question 27

the O in MACRO stands for ____

Answer 27

eOsinophilia

Question 28

There is an increased risk of ____ ____ in children whose mothers took erythromycin

Answer 28

pyloric stenosis

Question 29

Erythromycin reaches high concentrations in _____, which transport it to the site of the infection

Answer 29

phagocytes

Question 30

Erythromycin ____ ____ is the ester prodrug of erythromycin. It is more ____ and thus has increased absorption following oral administration

Answer 30

ethyl succinate;

lipophillic

Question 31

_____ is the C6 methyl ether of erythromycin. This blocks ____ formation and increases oral stability

Answer 31

clarithromycin;

ketal

Question 32

The 14-R-hydroxy metabolite of _____ has greater antibiotic activity than the drug itself, especially against _____

Answer 32

clarithromycin;

H Influenzae

Question 33

Azithromycin is a __-membered ring due to an added ____ group

Answer 33

15;

N-CH3

Question 34

____ AND ____ present in some antiacids form coordination complexes with ____ and prevent absorption

Answer 34

Magnesium, aluminum;

azithromycin

Question 35

______ has greater activity against Gram - bacteria than the other macrolides

Answer 35

Azithromycin