inhibitors of protein synthesis Flashcards
tetracyclines (doxy, minocy, tetra) are ___________________
inhibitors of protein synthesis
tetracyclines bind to ____ of bacterial ribosome and blocks tRNA from entering the acceptor site on the _____. It is _____
30S subunit
ribosome
reversible
tetracyclines have a high affinity to _______, binds to calcium, iron, mg. This happens before it binds to the ribosome
cations
tetracycline is able to bind to our 80S ribosomes. May inhibit _____
growth
tetracyclines diffuse through the porin channels of _________ and are lipophilic so can diffuse across the cytoplasmic membrane into _________
gram negative
gram positive
(broad spectrum)
tetracyclines inhibit proteases, making it ________
antiinflammatory
3 components of resistance:
- ______ export it
- Ribosomal production of proteins that interfere with tetra binding
- Enzymatic ______ of tetra
efflux pumps
inactivation
patient should ______ dairy products, food, and antacids
avoid
tetracyclines are eliminated in the ______ and excreted in the ______ and _____ at high concentrations in a _____ form
bile
urine and feces
________ is good against atypical bacteria, like ______ and _______ (obligate intracellular bacteria and mycoplasma), and _____ (H. pylori, B. burgdoferi)
tetracycline
chlamydia
rickettsia
spirochetes
tetracyclines cross the placenta and enter the _______
breast milk
you might use tetracycline for ______, ______, _________, UTIs, lyme disease, mycoplasma pneumonia
acne
rosacea
chlamydial infections
______ side effects include ______ of teeth in young children, photosensitivity, _______, suppression of vaginal lactobacillus, which can cause _____
brown staining
diarrhea
vaginitis
macrolides affect protein synthesis at the ______ level. Same resistance issues as tetra.
ribosomes
macrolides are good at targeting _______ pathogens
intracellular
erythromycin is not often used, but for ______
pertussis
azithrymycin is great against ________ (chlamydial infections, atypical infections)
atypical
________ is an alternative to penicillin
azithromycin
azithromycin does not inhibit _________ like all the other macrolides. It also has a really long ____ ____
cytochrome P450 enzymes
long half life
because azithromycin does not inhibit P450, it does not have _____ ______
drug interactions
the worst side effect of the macrolides is the ________ of the ____ interval, but ______ is the least worrisome
prolongation
QT interval
the prolonged QT interval can cause severe _______
arrthymias
Azithromycin 250 mg #6
2 tab PO x 1
then 1 tab PO daily x 4 days
prescription example
most common side effect of azithromycin is ______
GI disturbance, so take with food!
clindamycin is a ________. Also binds to 50S ribosome to suppress _____ ____
lincosamine
protein synthesis
mutation of the ribosomal receptor side, modification of the receptor, and enzymatic inactivation of clindamycin are all _______
forms of resistance
clindamycin is not a substrate for ________ efflux pumps, so strains resistant to macrolides are susceptible to clindamycin
macrolide
clindamycin is good against _______ anaerobes, S. progenies, and _________
plasmodium
________ is good alternative to penicillin and azirthromycin
clindamycin
clindamycin is notorious for causing ________
CDAD (clostridium difficile associated diarrhea)
amino glycosides are polar, so GI absorption is _______. Outside of topical applications, these won’t often be prescibred
poor
aminoglycosides bind ________ to the 30S ribosomal subunit
irreversibly! so bacteriocidal
______ takes care of aerobic gram negatives . Often paired with ______, which is excellent at gram positives
aminoglycosides
vancomycin
problem with amino glycosides is they are very _________ and _______
nephrotoxic
ototoxicity
toxicity of _______ will cause deafness
aminoglycosides (gentamycin)
chloramphenicol is _______ used because of its toxicity.
rarely
borrelia burgdoferi and H. Pylori are ______, so _________ would be a good drug for them
spirochetes
tetracyclines
macrolides inhibit _____ ______
protein synthesis