protein synthesis inhibitors Flashcards

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
Q

macrolides used in respiratory tract infections

A

azithromycin is best if H. influenza is suspected

26
Q

mainstay treatment that macrocodes are used for

A

CA pneumonia together with ceftriaxone

27
Q

macrolide used to treat STIs

A

single, 1 g dose of azithromycin

28
Q

macrolide used for treatment of MAC

A

clarithromycin or azithromycin

29
Q

macrolide use for prophylaxis for MAC

A

azithromycin

30
Q

most important adverse effect of using macrolides

A

prolonged QT interval, contraindicated in patients already on anti arrhythmic medications

31
Q

drug drug interactions of macrolides

A

erythromycin and clarithromycin interact with CYP450 enzymes and alter the metabolism of drugs utilizing this system

32
Q

MOA streptogramins

A

both quinpristin and daltopristine bind the 50S subunit to inhibit bacterial protein synthesis

33
Q

MOR streptogramins

A

alteration of the ribosomal binding site (erm) and enzymatic inactivation

34
Q

spectrum of activity streptogramins

A

MRSA
PRSP
VRE

35
Q

streptogramins: bactericidal or bacteriostatic?

A

bacteriostatic

36
Q

streptogramins: time or concentration dependent?

A

time

37
Q

absorption of streptogramins PO

A

only available IV

38
Q

distribution streptogramins to the CSF

A

does not penetrate the CSF

39
Q

clinical uses streptogramins

A

VRE (faecium) only

40
Q

major adverse effect streptogramins

A

venous irritation when administered through peripheral vein.