Macrolides And Telithromycin

Front 1

moa of macrolides

Back 1

Inhibits protein synthesis by binding -reversibly to 50 S ribosomal subunit
-Interfere with binding of other antibiotics – clindamycin and chloramphenicol

Front 2

macrolides are statis or cidal

Back 2

static,
cidal vs c. jejni

Front 3

t/f macrolides cover gram +: strep and staph but has no clinical evidence vs staph and is only tested in the club

Back 3

true,

Front 4

erythromycin covers

Back 4

gram +
-strep
-staph (not really)

gram -:
-campylobacter jejuni
-moraxella catarrhalis
-bordetella pertussis
-n. gonorrhea

other
-atypicals + hb
Legionella pneumophilia
Mycoplasma pneumoniae
Chalamydia pneumoniae
Chlamydia trachomatis
Treponema pallidum
H. pylori
Borrelia burgdorferi

Front 5

clarithyromycin covers

Back 5

gram +
-strep
-staph (not really)

gram -:
gram -:
-campylobacter jejuni
-moraxella catarrhalis
-bordetella pertussis
-n. gonorrhea
-hemophilus influenza

other
-atypicals + hb+ mt
Legionella pneumophilia
Mycoplasma pneumoniae
Chalamydia pneumoniae
Chlamydia trachomatis
H. pylori
Borrelia burgdorferi
Mycobacteria spp.
Toxoplasma gondii
Mycobacteria spp.

Front 6

how does gram - coverage differ b/t ery and clarith

Back 6

- clarithyro covers ery gram - + hemophillus influenza

Front 7

how does clarithy other coverage comp to erythy

Back 7

- ery box (- treponema pallidum)
- + mycobacteria spp. , toxoplasma gondii

Front 8

azith spectrum of coverage

Back 8

gram +
-strep
-staph (not really)

gram -:
-campylobacter jejuni
-moraxella catarrhalis
-bordetella pertussis
-n. gonorrhea
-hemophilus influenza
-ecoli
-salmonella
-shigella
(clarith box + hess)

other
-atypicals + hb+ mt
Legionella pneumophilia
Mycoplasma pneumoniae
Chalamydia pneumoniae
Chlamydia trachomatis
H. pylori
Borrelia burgdorferi
Mycobacteria spp.
Toxoplasma gondii
Mycobacteria spp.
-treponema pallidum

Front 9

which abx covers treponema pallidum: ery, clarith, azith

Back 9

covers: ery and azith
not: clarith

Front 10

macrolides cover gram + bacillus?

Back 10

no

Front 11

Macrolides are the doc for staph aures?

Back 11

no, not 1st or 2nd line

Front 12

macrolides are the doc for staph epi

Back 12

no

Hint 12

remember staph coverage only dx tool

Front 13

macrolides cover saprophyticus?

Back 13

- no

Front 14

macrolides cover strep pneumonia?

Back 14

- yes

Front 15

ery absorption

Back 15

- Erratic, inactivated by gastric
acid (EC formulations)
- better with salt form than base:
(estolate>ethylsuccinate>stearat
e)
- F = low

Front 16

clarith absorption

Back 16

Rapid absorption
- Acid stable

Front 17

azith absorption

Back 17

- rapid absorption
- acid stable
- f dec by food ( newly formulated tabs, may be taken w/out regard to food)

Front 18

macrolide distribution

Back 18

distributes widely, except CSF
 intracellular (phagocytes & macrophages)/tissue concentration >> plasma
concentration
(azithromycin [tissue] 10 -100 X > [plasma])

Front 19

macrolide distribution in the blood?

Back 19

- very little goes into the blood
- dnt give in bug is in the blood

Front 20

ery,clar and azith are eliminated by?

Back 20

hepatic and renal

Front 21

ery, clarith, azith
half life

Back 21

ery: 1.6 hrs
clar: 5-7 hrs
azith: 68 hrs

Front 22

clarith elimination needs dosage adj?

Back 22

yes, crcl <30 ml/min
- avoid use in severe hepatic impairment

Front 23

ery dosage frequency ?

Back 23

q 6 hrs

Front 24

clarith admin: biaxin xl w/ or w/out food

Back 24

with food

Front 25

clarith dosage frequency

Back 25

po q 24 hrs

Front 26

ery adr

Back 26

- gi
-cholestatic hepatitis
- otoxtoxicity
-phlebitis

Front 27

clarith adr

Back 27

- n/d/abd cramps
- metallic taste
- inc liver enzymes

Front 28

azith adr

Back 28

- n/d/adb cramps
- inc liver enzymes

Front 29

pregnancy categories
ery, clarith, azith

Back 29

- preg B: ery, azith
- preg C: clarith

Front 30

drug interactions of ery,clarith,azith

Back 30

-Inhibition of CYP450 1A2 & 3A4
o Theophylline, cyclosporine, carbamazepine, warfarin, astemizole ...etc. (potential
interaction with other substrates of these enzymes)

- Inhibition of gut flora responsible for digoxin digestion (documented with E, caution with
C & A)

-Increased digoxin level

-Competitive binding to 50 S ribosomal subunit
o Antagonizes effects of clindamycin and chloramphenicol

Front 31

clarith covers community aquired pneumonia

Back 31

yes

Front 32

telithromycin moa

Back 32

-Inhibits protein synthesis by binding to 23S ribosomal RNA of 50S ribosomal subunit
- 23S has 5 domains (I-V)
- Clarithromycin and telithromycin binds to II and V

Front 33

telithromycin is static or cidal

Back 33

static

Front 34

telithromycin spectrum of activity

Back 34

gram +
-staph aures
-streptococcus: pneu, pyogenes

gram -
haemophilus influ
moraxella catarrhalis

inactive vs
-enterobacteriaceae
-psa aeruginosa

other (atypicals)
-chlamydophilia pneumoniae
-legionella pneumophila
-mycoplasma pneumoniae

anaerobes
-clostridium
-peptostreptococcus
-proprionibacterium
-provetella

Hint 34

gram -: hm
other: clm

anaerobes 3p + c

Front 35

clinical indications for telithyromycin, explain the change

Back 35

Before February 2007
-Community-acquired pneumonia (CAP)
- Acute exacerbation of chronic
bronchitis (AECB)
- Acute bacterial sinusitis (ABS)

After feb 12, 2007
Community-acquired pneumonia (CAP)

Front 36

absorption of telithy

Back 36

- 90% absorption

Front 37

metabolism of telith

Back 37

- cyp 3a4 inhibitor

Front 38

adr of telithromycin

Back 38

- myasthenia gravis
- hepatotoxicity
- visual disturbances
- gi
- cardiac: qtc prolongation
-

Front 39

contraindications of telithromycin

Back 39

- hepatotoxicity

Front 40

bbw of telithromycin

Back 40

- myasthenia gravis

Front 41

telithromycin pregnancy category

Back 41

preg cat c

Front 42

inc telithromycin levels

Back 42

- itraconazole
-ketoconazole

Front 43

dec telithromycin levels

Back 43

-CRaPP

-carbamezapine
-rifampin
-phenobarbital
-phenytoin