Term
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Definition
1. 50 large ribosomal unit joins with 30s ribosomal unit
2. Initiation- tRNA goes onto P site with a Met group attached
3. Amino acid incorporation- tRNA w/ specific AA sits onto the A-site
4. Elongation: Petide bond forms via peptidyl transferase between AA groups
5. A site tRNA moves over to P site to move over for another tRNA to repeat the process
6. Termination |
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Term
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Definition
- Aminoglycosides (30s), Oxazoladinones (linezolid) (50s): blocks initiation complex
- Tetracyclines/glycylcycline (30s), dalfopristin/quinupristin (50s): blocks AA incorporation
- Cloramphenicol (50s): blocks peptide bond formation
- Macrolides/Clindamycin (lincosamides) (50s), type B streptogramins, ketolide: blocks elongation
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Term
What is the difference between human and bacterial translation ribosomal units? |
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Definition
Bacteria: 70s
Humans: 80s |
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Term
Which group of drugs inhibit the 30s ribosomal units? |
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Definition
A=Aminoglycosides
T= Tetracyclines |
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Term
Are protein synthesis inhibitors bacteriostatic or bacteriocidal? |
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Definition
Bacteriostatic except aminoglycosides |
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Term
Right off the bat, what does the name "aminoglycosides" tell you? |
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Definition
Seeing -"glycosides" tells you it's made up of sugar--> water soluble--> polar--> goes through kidney--> probably has kidney toxicities |
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Term
What are the 50s inhibitors? |
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Definition
Chloramphenicol, clindamycin
Erythromycin
Lincomycin
Linezolid |
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Term
"Buy AT 30, CCELL (sell) at 50"
What does this mean? |
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Definition
30s inhibitors:
Aminoglycosides
Tetracyclines
50s inhibitors:
Chloramphenicol, Clindamycin
Erythromycin
Lincomycin
Linezolid
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Term
What are examples of aminoglycosides? |
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Definition
"Mean" GNATS can NOT kill anaerobes
Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin |
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Term
What is the mechanism of action for aminoglycosides? |
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Definition
Blocks initiation of complex, causes misreading of codes upon tRNA trying to come in and bind to subunit and f***s it up
Requires O2 for uptake |
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Term
Aminoglycosides are best used on which organisms? |
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Definition
G- aerobic rods
Used in conjnction w/ cell wall inhibitors (β-lactams)
Neomycin for bowel surgery
Also for enterococci & P. aeruginosa
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Term
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Definition
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Term
What are the toxicities of aminoglycosides? |
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Definition
"Mean" GNATS canNOT kill anaerobes
Nephrotoicity (esp. w/ cephalosporins)
Ototoxicity (especially w/ loop diuretics)
Teratogen
Neuromuscular blockade, blocks acetylcholine release |
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Term
What is the most common drug associated w/ contact dermatitis?
What other agents can you find in neomycin/sporin? |
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Definition
Neomycin (neosporin)
Can find polymixin and bacitracin
*Boards love this question* |
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Term
A patient comes in with decreased acetylcholine release leading to muscle paralysis, dry eyes, etc., what should you be thinking about? |
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Definition
Botulism toxin or aminoglycoside SE
If botulin is not one of the answers, then look for a -mycin drug :)
Also a common board question |
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Term
What is the MOA of tetracyclines? |
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Definition
Bind to 30S and prevent attachment of aminoacyl tRNA; limited CNS penetration |
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Term
What can tetracyclines be used to treat? |
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Definition
Broad spectrum, but good with atypical bacteria like H. pylori, M. pneumonia, vibrio,
Rickettsia (typhus/spotted fever), Lyme disease, Chlamydia
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Term
What are some examples of tetracyclines? |
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Definition
- doxacycline
- minocycline
- democlocycline (Blocks ADH receptors, use for SIADH)
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Term
What are the side effects/toxicities of tetracycline? |
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Definition
- Tooth enamel dysplasia (discoloration)
- Dec bone growth in children
- Phototoxicity
- GI distress
- Vestibular dysfunction
- DO NOT give to children or pregnant women
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Term
What is the resistance that some bacteria have to aminoglycosides? |
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Definition
- Production of conjugating enzymes (transferase)
- Inactivate drugs by acetylation (of own ribosomes to prevent recognition by drug), phosphorylation, or adenylation
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Term
What do you know about cloramphenicol just by looking at its name? |
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Definition
Anytime you have -phen or phen sounding in a name, it means it is lipid soluble and can probably cross the BBB. Ex: acetominophen |
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Term
What is the MOA of cloramphenicol |
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Definition
- Blocks transpeptidation, 50s inhibitor
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Term
What is cloramphenicol usually used for? |
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Definition
- Meningitis (H. influenzae, N. miningitidis, S. pneumoniae)
- Conservative in states, used a lot still in developing countries
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Term
What are the toxicities of cloramphenicol? |
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Definition
- Bone marrow suppression
- "Gray baby"-> toxicity+lack UDP glucuronyl transferase= kernicterus
- Anemia (dose dependent
- aplastic anemia (dose independent)
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Term
What is the MOA of macrolides?
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Definition
Blocks translocation:
Binds to 23S rRNA of 50s ribosomal subunit |
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Term
What are some examples of marcolides? |
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Definition
- Erythromycin
- Azithromycin
- Clarithromycin
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Term
What can macrolides be used for? |
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Definition
- Atypical pneumonias (mycoplasma, chlamydia, legionella)
- URIs
- STDs
- G+ cocci
- Neisseria
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Term
What do macrolides have to do with cytochrome P450? |
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Definition
Macrolides block CY P450 EXCEPT azithromycin |
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Term
What are the side effects/toxicities of macrolides? |
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Definition
- Prolonged QT interval (esp erythromycin)
- GI discomfort (most common cause of noncompliance) by stimulating motilin
- Reversible deafness (ototoxic)
- Acute cholestatic hepatitis
- eosinophilia, skin rashes
- increases serum conc. of theophyllines
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Term
What is the MOA of clindamycin? |
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Definition
Blocks peptide bond formation at 50S ribosomal subunit |
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Term
What can clindamycin be used for? |
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Definition
Anaerobic infections (G+, S. aureus: osteomyelitis)
in aspiration pneumonia/lung abscesses
"Treats anaerobes above the diaphragm vs. metronidazole anaerobic infections below diaphragm" |
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Term
What are the toxicities of clindamycin? |
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Definition
- Pseudomembranous colitis (C. dif)
- fever
- diarrhea
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Term
What do you want to treat C. Dif infection with? |
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Definition
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Term
What is another name for Linezolid? |
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Definition
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Term
What is the MOA of linezolid? |
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Definition
Blocks formation of initiation complex by messing with 50s ribosomal subunit |
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Term
What is linezolid used for? |
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Definition
VRSA/VRE
drug resistant pneumococci |
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Term
What are the side effects of linezolid? |
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Definition
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Term
Is clindamycin an aminoglycoside? |
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Definition
No, this is an exception. Don't let the mycin fool you. They have different MOAs. |
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