Antimicrobials 7-8 Flashcards
WHAT ARE THE 50S INHIBITORS
Macrolides
Lincosamides
Chloramphenicol
“methylated ervthromycin”
Clarithromycin
What are the macrolides drugs
Clarithromycin
Azithromycin
Roxithromycin
Erythromycin
prototype, produced from S. erythraeus,
Erythromycin
use: for the treatment of ulcers caused by H. pylori
Clarithromycin
potent enzyme inhibitors
Clarithromycin & Erythromycin
14-16-membered macrocyclic lactone ring
Macrolides
Other term of Erythromycin
Ilotycin
a prodrug which is more lipophilic >- longer duration of action
ethylsuccinate
A type of pneumonia caused by legionella pneumop
Legionnaire’s disease
sulfur-containing antibiotic
Lincosamides
lipid-soluble, acid-stable prodrug with better oral absorption
estolate
motilin agonist
Erythromycin
isolated from Streptomyces lincolnensis
Lincomycin
from Streptomyces venezuelae
Chloramphenicol
70S Inhibitor
Oxazolidinone antibacterial
idiosyncratic reaction unrelated to dose
aplastic anemia:
old DOC for typhoid fever
Chloramphenicol
A/E C. difficile-induced pseudomembranous colitis
Clindamycin
Lincosamides drugs
Lincomycin
Clindamycin
DOC: VRSA
Linezolid
chlorine-substituted derivative of lincomycin
Clindamycin
rapidly absorbed and wel tolerated oraly but should not be administered with food and antacids
Azithromycin
a 15-membered lactone ring with N-methyl group
Azithromycin
Hydrate forms of azithromycin
dehydrate
monohydrate
extensive tissue distribution - allows once a day dosing
Azithromycin
weak enzyme inhibitor
Roxithromycin
NOT an enzyme inhibitor
Azithromycin
Brand name of hydrtae form of azithromycin
- dehydrate (Zithromax®)
- monohydrate (Azyth ®)
Remedy of a bitter taste of clarithromycin
Addition of palmitic acid (prodrug)
last-resort drug
Linezolid
DOC: Legionnaire’s disease
Erythromycin
patterned after nalidixic acid
Quinolones
SAR of Quinolones: addition of groups greatly reduces or abolishes activity
At 2
SAR of Quinolones: may be substituted with good effects
at 5, 6, 7, 8,
SAR of Quinolones: small alkyl substitution provides greater potency
at 1
SAR of Quinolones: increases antibacterial activity
At 6, + fluoroquinilines
SAR of Quinolones: provides activity against Pseudomonas aeruginosa
At 7, + Piperacillin
side effect is photosensitivity HIGHEST
Lomefloxacin
side effect is photosensitivity LOWEST in Quinolones
Sparfloxacin
DOC: prophylaxis and treatment of anthrax
Ciprofloxacin
SAR: nitro a t 5 t position is essential for antibacterial activity
Nitrofurans
What are the Nitrofurans Drugs
Nitrofurantoin
Nitrofurazone
Furazolidone
used topically in burns
Nitrofurazone
oral treatment used for bacterial and protozoal diarrhea
Furazolidone
used topically in burns
Nitrofurazone
inhibits DNA gyrase & Topoisomerase IV
MOA if quinolones
Nucleus of quinolones
1,4 dihydro-4-oxo-3 pyridine carboxylic acid
Retained G(-), G(+), and atypical bacteria activity: also has an activity against anaerobic bacteria
Trovafloxacin