macrolides

Question 1

MOA

Answer 1

bind reversibly to 50S subunit

inhibit translocation + transpeptidation

Question 2

absorption

Answer 2

gastric acid inhibit + dec. - so enteric coated tab.
incomp. + adequate abs. - upper part of small intestine
high plasma lvls. - IV

Question 3

distribution

Answer 3

diffuse rapidly in ICFs

no activity in brain + CSF

Question 4

excretion

Answer 4

mainly met. in liver + bile
2-5% excreted in urine
not to be adjusted in renal patients

Question 5

low conc

Answer 5

bacteriostatic

Question 6

high con.

Answer 6

bacteriocidal

Question 7

aerobic
g+
cocci + bacilli

Answer 7

SCHooL Nahi jana
s. pyogenes
s. viridans
cornybacterium diphtheria
clostridium perfringes
h. influenza
listeria monocytognes
n. meningitis

Question 8

NP Bro CAL Bhi Mat jana

Answer 8

n. gonorrhea
pastruella multocida
borellia
bordetella pertussis
campylobacter jejuni
c. trochomatis
atypical mycobacterium - m. scrofulaceum
ligionella pneumophila
m kansassi + m. avium intracellare

Question 9

resistance

Answer 9

1- EFFLUX PUMPS
2- TARGET MODIFICATION - 
methylase enzyme
chromosomal mutations - campylobacter + g+ cocci +b. subtilis
3- DESTRUCTION - estrase enzyme 
enterobacterease

Question 10

therapeutic uses (same)

Answer 10

mycobacterial inf.
tetanus
prophylaxis - dental + benzyl penicillin allternative
campylobacter inf.
streptococcal inf.
staphylococcal inf.
legionella inf.

Question 11

uses (E)

Answer 11

chlamydial inf.
diphtheria
pertussis (DOC)

Question 12

clarithromycin

Answer 12

addition of methyl group
more acid stable
similar spec. to E
more active against - m. avium + m. laprae

Question 13

absorption (C)

Answer 13

absorbed well in GIT
bioavailability - dec. bcz 1st pass met 50-55%
inc. - given with food intake (extended release form _ 1g/day)
can be given with + without food (standard formulation)

Question 14

distribution (C)

Answer 14

widely distributed 
1st pass met. - 14 hydroxyclarithromycin
highly distributed
high IC conc.
serum level less than tissue conc. lvl

Question 15

excretion (C)

Answer 15

both renal and liver
1. liver 
highly metabolized 
many metabolites 
most significant -14 hydroxy
2- renal
unchanged + changed form
dose doesnt need to be adjusted

Question 16

advantage of C over E

Answer 16

less frequent dosing

lower GI intolerence

Question 17

therapeutic uses (C)

Answer 17

helicobacter pylori

syphilis

Question 18

azithromycin

Answer 18

more active against
h. influenza
campylobacter
NP Bro CAL Bhi Mat jana
advanced activity against m. avium intracellare + some protozoa; toxoplasmois + plasmodium

Question 19

absorption(A)

Answer 19

rapidly absorbed from GIT
dec. absorption with antiacids
250-500mg/once daily

Question 20

distribution(A)

Answer 20

widely distributed 
except CSF
tissue conc. more than serum con.
also present in phagosomes
fibroblast - drug reservoir
protein binding - low

Question 21

excretion(A)

Answer 21

HEPATIC MET
inactive metabolites
major route
RENAL - only 12% 
unchanged

Question 22

therapeutic uses (A)

Answer 22

diphtheria
mycobacterium inf. in AIDS
diarrhea - cryptosporidium

Question 23

toxicities

Answer 23

macrolide GRApES
GI disturbances
rashes
acute cholestatic hepatitis
ear toxicity/hearing loss + eosinophillia
hyperSensitivity

Question 24

contraindications

Answer 24

prolong QT interval - erythromycin

hepatic dysfunc.