Antibacterial Agents 3: Protein Synthesis Inhibitors Flashcards
What are the main Protein Synthesis inhibitors?
- Macrolides (-Thromycins)
- Tetracyiclines (including Doxycycline)
- Clindamycin
- Aminoglycosides (linezolid)
Are Protein Synthesis inhibitors more lipid soluble or water soluble? Why is this important?
Lipid
Lipid soluble drugs tend to be metabolized.
Which DQCRIMES drugs are Non renal eliminated (also non hepatotoxic)
Doxy and Clindamycin
Which Erythromycin like drug (from DQCRIMES) does not inhibit P450?
Azithromycin is A-OKAY
Which DQCRIMES inhibit P450?
Quinolones
Erythromycin like drugs (Macrolides)except Azithromycin
Protein Synthesis inhibitors generally target the __________ and are (bactericidal or bacteriostatic drugs)
Target Mitochondrial subunits (do not need to know 30 vs 50s)
They are bacteriostatic (except aminoglycosides)
Which of the following mechanisms of resistance is true of macrolides?
- Inc Efflux
- Dec entry
- Ezymatic inactivation
- Altered target
Altered Target
S. Pneumonia and H. Influenza change the 50s binding site.
How are macrolides administered?
Orally
T/F Azythromycin is metabolized in the liver.
False, It is NOT metabolized but instead excreted in the biliary pathway.
One large single dose of azithromycin can cover
Atypical Chlamydia.
What is the major advantage of Clarithromycin?
Greater duration of Activity.
What is the mechanism of resistance for Tetracyclines?
- Inc Efflux
- Dec entry
- Ezymatic inactivation
- Altered target
- Inc Efflux
MDR transporters move drug OUT OF CELL
True or False: Doxycycline is absorbed better than tetracycline AND may penetrate placental tissue.
True
T/F: All protein inhibitors can treat MSSA and MRSA.
False:
Macrolides, doxycycline and Clindamycin can.
Aminoglycosides CANT
Gonorrhea frequently “travels” with which other bacteria?
Atypical Chlamydia.
Which protein synthesis inhibitors treat Atypical Chlamydia and Mycoplasma?
Macrolides(-thromycins) and Doxycyclin.
Which drugs have a broad enough coverage to be able to cause superinfections (C. Diff)?
- Clindamycin** Important
has no action against C.diff - 3rd Gen Cephalo
- Amox/Clav
- Flouroquinones
Which drugs can treat C. Diff?
- Vancomycin
2. Metronidazole (DNA inhibitor)
Which drug class can cause a fungal (candida) overgrowth?
Tetracyclines
How does clindamycin work?
It is a static protein synthesis inhibitor (he said this was the answer to a TQ)
Which PSIs best treat B. Fragilis?
Clindamycin***most important
Tetracycline
What are some of the common adverse reactions for clindamycin?
Nausea, Diarrhea (c. diff), Skin rashes.
Aminoglycosides are ONLY effective against __________ (bacteria type)
Gram - Rods
E. Coli and Pseudomonas
T or F:
Amino glycosides bind reversibly to ribosomal subunits.
False
They bind IRREVERSIBLY to ribosomes. This is why they are bactericidal.
How are Aminoglycosides administered?
IM injection.
Where do aminoglycosides tend to accumulate in the body?
- Renal Cortex (nephrotoxicity)
2. Inner Ear (ototoxicity)
