protein synthesis inhibitors Flashcards

(40 cards)

1
Q

MOA clindamycin

A

inhibit protein synthesis by binding only to 50S

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2
Q

clindamycin: bacteriostatic or bactericidal?

A

bacteriostatic

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3
Q

MOR clindamycin

A

presence of erm gene, which alters the 50S binding site

no activity of mef gene against clindamycin

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4
Q

main area of use for clindamycin

A
anaerobic infections
peptostreptococcus
actinomyces
bacteriodes (use metronidazole instead)
prevotella
fusobacterium
clostridium spp. (excluding C. difficile)
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5
Q

best way to test for CA MRSA resistance to clindamycin?

A

SSSI infections due to MRSA, give clindamycin to see if theyre susceptible or not

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6
Q

clindomycin have to be givenIV or PO?

A

no, completely and rapidly absorbed (90%)

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7
Q

CSF distribution clindomycin?

A

poor distribution

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8
Q

clindomycin eliminated by hemodialysis?

A

no

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9
Q

elimination mechanism for clindomycin?

A

primarily by liver

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10
Q

primary clinical use clindomycin

A

anaerobic infections outside of the CNS, SSSI infections due to CA MRSA

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11
Q

the one major adverse effect clindomycin

A

one of the worst inducers of C. difficile colitis

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12
Q

3 macrolides in clinical use

A

erythromycin, clarithromycin, azithromycin

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13
Q

improvements due to purifying erythromycin into azithromycin and clarithromycin

A

better bioavailability
better tissue penetration
prolonged half lives
improved tolerability

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14
Q

MOA macrolides

A

inhibit protein synthesis by binding the 50S subunit to suppress protein synthesis

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15
Q

macrolides: bacteriostatic or bactericidal

A

bacteriostatic

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16
Q

MOR macrolides in the US

A

mef gene encoding active efflux which confers a low level of resistance to macrolides

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17
Q

MOR macrolides in Europe

A

erm gene encoding altered target sites on 50S which confers a high level of resistance to macrolides

18
Q

spectrum of activity for macrolides in G- aerobes (including macrolides rankings)

A

H. influenzae (not erythromycin)
M. catarrhalis
Neisseria
azithromycin > clarithromycin > erythromycin

19
Q

G- bacteria group that macrolides have NO activity against

A

enterobacteriacieae

20
Q

spectrum of activity for macrolides in G+ aerobes (including macrolides rankings)

A
MSSA
PSSP
Group and viridans streptococci
bacillus
corynebacteria
21
Q

activity macrolides against atypical bacteria

A

macrolides are the main mechanism of treatment for atypical bacteria
legionella pneumonia (water fountain infections)
chlamydia
mycoplasma

22
Q

Treatment of mycobacterium avid complex with these macrolides…

A

only azithromycin and clarithromycin

23
Q

absorption of erythromycin PO

A

variable absorption that is enhanced by giving with enteric coating or in ester salt formulations (destroyed by gastric acid)

24
Q

absorption of clarithromycin PO

A
well absorbed (55%) and acid tolerable
unchanged by the presence of food
25
macrolides used in respiratory tract infections
azithromycin is best if H. influenza is suspected
26
mainstay treatment that macrocodes are used for
CA pneumonia together with ceftriaxone
27
macrolide used to treat STIs
single, 1 g dose of azithromycin
28
macrolide used for treatment of MAC
clarithromycin or azithromycin
29
macrolide use for prophylaxis for MAC
azithromycin
30
most important adverse effect of using macrolides
prolonged QT interval, contraindicated in patients already on anti arrhythmic medications
31
drug drug interactions of macrolides
erythromycin and clarithromycin interact with CYP450 enzymes and alter the metabolism of drugs utilizing this system
32
MOA streptogramins
both quinpristin and daltopristine bind the 50S subunit to inhibit bacterial protein synthesis
33
MOR streptogramins
alteration of the ribosomal binding site (erm) and enzymatic inactivation
34
spectrum of activity streptogramins
MRSA PRSP VRE
35
streptogramins: bactericidal or bacteriostatic?
bacteriostatic
36
streptogramins: time or concentration dependent?
time
37
absorption of streptogramins PO
only available IV
38
distribution streptogramins to the CSF
does not penetrate the CSF
39
clinical uses streptogramins
VRE (faecium) only
40
major adverse effect streptogramins
venous irritation when administered through peripheral vein.