E2L19: Chemical Methods - Inhibit Protein Synth + Nucleic Acid Synth Flashcards
What do agents that inhibit protein synth do?
affect translation, effects ribosomes, toxic b/c we make proteins
Name some groups of agents that inhibit protein synth.
- aminoglycosides, tetracyclines, nitrobenzene, macrolide, linezolid
What are aminoglycosides? Examples?
- glycosides common in plants
- add sugar to chemical so it can go into soln
- broad spectrum, but clinically typ for G-
- 2 toxicities: OTO (ears) and Nephro (kidneys), severe infections
- ex: streptomycin, neomycin, gentamycin, capreomycin, kanamycin, amikacin
Streptomycin?
- aminoglycoside - inhibit protein synth
- DOC for severe infections of TB (MDR/XDR) and for Black Plague (Yersinia pestis)
Neomycin?
- aminoglycoside - inhibit protein synth
- broad spectrum
- in triple ointments
- DON’T USE for LARGE BURNS –> can go systemic and cause HEARING LOSS
Gentamycin?
- aminoglycoside - inhibit protein synth
- replacing streptomycin, esp for G- infections (esp. if nosocomial)
- typ w/ ticarcillin
- for Pseudomonas aeruginosa Other infection, typ in combo with ticarcillin
Capreomycin, Kanamycin, Amikacin
- aminoglycosides - inhibit protein synth
- MDR or XDR TB
Tetracyclines? Example?
- ex: Doxycycline
- -> common for most infections:
- > Substitute for Penicillin for G+
- > Borrelia (Lyme, spirochete)
- > Chlamydia trachomatis UTI (STD, adult form)
- > Mycoplasma pneumo (CAP)
- > Rocky Mountain Spotted Fever (Rickettsia)
Nitrobenzene Derivative? Example?
- toxic
- inhibits protein synth
- causes aplastic anemia (prevents bone marrow from making RBC/WBC)
- ex: chloramphenicol - LAST CHOICE
- -> for VRE (vancomycin resistant entereococci)
- -> for typhoid fever (salmonella typhii)
- -> meningitis (haemophilus influ.)
Macrolides? Examples?
- ex: Azithromycin (Zithromax)
- -> DOC for many infections:
- > N. gonorrhea in pregnant women allergic to beta-lactam antibiotics (ex: cephalosporins, penicillins, carbetalactams)
- > Chlamydia trach. UTI, Myco. pneumo. (CAP), Bordetella Pertussis, Legionella Pneumophila
- ex: Erythromycin
- -> DOC for:
- > ophthalmia neonatorum + Chlamydia trachomatis + N. gonorrhea in babies
- > Myco. pneumo.
- > Bordetella pertussis
- > Corynebacterium diphtheria
Linezolid? Aka?
- inhibits protein synth
- aka Zyvox
- toxic, blocks 1st ternary complex during translation
- DOC for systemic MRSA serious infections
What do agents that inhibit nucleic acid synthesis do? Some interfere with RNA synthesis! Some DNA synthesis!
- they’re structural analogues -> fit into DNA and are mutations, organism dies
- toxic to humans, all eukaryotes, prokary, and viral DNA
What are some examples of agents that inhibit RNA synthesis?
rifampin, ethambutol
Rifampin?
- inhibits RNA synthesis
- DOC for TB
- blocks RNA polymerase
Ethambutol?
- inhibits RNA synthesis
- DOC for TB
- might interfere w/ RNA polymerase?
- definitely blocks mycolic acid in TB tho
Name some examples that interfere w/ DNA synth.
acyclovir, AZT (azidothymidine), griseofulvin, fluoroquinolones (ciprofloxacin, moxifloxacin), metronidazole (aka Flagyl), mebendazole
Acyclovir?
- inhibits DNA synth
- purine analogue (adenine, guanine)
- DOC for Herpes (cold sores, genital)
AZT? aka?
- aka azidothymidine
- inhibits DNA synth
- pyrimidine analogue for thymine
- in past, used for long term AIDS patients
- -> formally #1 DOC for AIDS
- now used to prevent pregnant mom passing AIDS to baby
Griseofulvin?
- inhibits DNA synth
- from penicillium
- antifungal
- affects microtubules, blocks mitosis, toxic!!!
- DOC for severe athlete’s foot (trichophyton sp) oral
- -> trichophyton can get into hair and very difficult to get rid of
- blocks mitosis (cell division) by affecting cytoskeleton
Fluoroquinolones? Examples?
- ex: ciprofloxacin and moxifloxacin
- lots of side effects
- inhibits DNA synth
- blocks DNA gyrase from coiling DNA
- -> CIPROFLOXACIN DOC for Pseudo. aeruginosa UTIs and Bacillus anthracis
Metronidazole? aka?
- aka Flagyl
- inhibits DNA synth
- gets reduced in anaerobic conditions, acts as structural analogue in DNA –> for anaerobic infections
- DOC for: amoebic dysentery, trichomonas vaginalis, antibiotic colitis (get after use of broad spectrum antibiotics like ampicillin, caused by Clostridium difficile)
Mebendazole?
- inhibits DNA synth
- binds to microtubules, affects ATP synthase
- antihelminthic (worm infections)
All of the following antibiotics inhibit protein synth except:
a) chloramphenicol
b) tetracycline
c) erythromycin
d) streptomycin
e) rifampin
e) rifampin
rifampin inhibits nucleic acid synth, blocks RNA synthesis
Which of the following descriptions of antiviral chemotherapeutic agents are mismatched?
a) acyclovir - herpes simplex virus
b) ribavirin - respiratory syncytial virus (RSV)
c) azidothymidine - AIDS
d) interferon - produced naturally by infected animals
e) none of these
e) none
iunno what ribavirin or interferon are, but w/e
Uses of antiparasitic drugs includes all of the following except?
a) mebendazole - malaria
b) quinine - malaria
c) chloroquine - malaria
d) metronidazole - amebicide
e) metronidazole - trichomonas
a) mebendazole - malaria
mebendazole is an antihelminth