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Protein Synthesis Inhibitors
Board Review
12
Microbiology
Professional
10/19/2009

Additional Microbiology Flashcards

 


 

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Term
Protein Synthesis Inhibitors
Definition

1. 30 S inhibitors: Aminoglycosides (streptomycin, gentamicin, tobramycin, amikacin) and Tetracyclines

 

2. 50 S inhibitors: Chloramphenicol, Clindamycin, Erythromycin, Lincomycin, Linezolid

 

"Buy AT 30, CCELL AT 50"

 

Term
Aminoglycosides
Definition

1. Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin

2. MOA: bactericidal- inhibits formation of initiation complex and causes misreading of mRNA- requires O2 for uptake therefore it is ineffective against anaerobes

3. Clinical use: Severe gram-negative rod infections, synergistic with B-lactam antibiotics, neomycin for bowel surgery

4. Toxicity: Nephrotoxicity (especially when used with cephalosporins), Ototoxicity (especially when used with loop diuretics), Teratogen

5. Mg, Ca, acid ph block entry

6. Resistance by modification via acetylation, adenylation or phosphorylation

 

"Mean" GNATS canNOT kill anaerobes

Term
Tetracyclines
Definition

1.Tetracycline, Doxycycline, Demeclocycline, Minocycline

 

2. MOA- bacteriostatic, bind 30S and prevent attachment of aminoacyl-tRNA; limited CNS penetration

3. Doxycyline is fecally eliminated and can be used in patients with renal failure

4. must not take with milk, antacids, or iron-containing preparations bc divalent cations inhibit its absorption

5. Clinical use: Vibrio cholerae, Acne, Chlamydia, Ureaplasma, Urealyticum, Mycoplasma pneumoniae, Tularemia, H. pylori, Borrelia burgdorferi, Ricketssia

6. Toxicity: GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity.

 

7. Demeclocycline is an ADH antagonist and acts as a diuretic in SIADH

8. Resistance by decreased uptake or increased transport out of the cell

 

VACUUM THe BedRoom

 

 

2.Binds to 30S ribosome preventing access of tRNA to mRNA-ribosome complex

2. bacteriostatic- reversibly bound

3. Phototoxicity

4. treatment for SIADH

5. do not use in pregnancy or children- chelates in bone

6. Di- or trivalent cations impair absorption

7. mycoplasma, ureaplasma, tularemia, rickettsia

8. R is plasmid mediated via decreased cell entry

Term
Macrolides
Definition

1.Erythromycin, Azithromycin, Clarithromycin

 

2. MOA- inhibit protein synthesis by blocking translocation; bind to 23 rRNA of the 50S ribosomal subunit- Bacteriostatic

3. Clinical use- URIs, pneumonias, STDs, gram-positive cocci (strep infections in patients allergic to penicillin); Mycoplasma, Legionella, Chlamydia, Neisseria

4. Toxicity- GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rashes

5. Increases serum concentration of theophyllines and oral anticoagulants

 

6. Resistance by methylation of rRNA near erythromycin's ribosome-binding site

Term
Clindamycin
Definition

1. MOA- blocks peptide bond formation at 50S ribosomal subunit- bacteriostatic

2. Clinical Use- Treat anaerobic infections (B. fragilis, C. perfringens)

3. Toxicity- C. diff overgrowth, fever, diarrhea

4. Treats anaerobes above the diaphragm

Term
Quinupristin/Dalfopristin
Definition

1. streptogramins

2. bind separate 50s ribosome sites producing stable drug-ribosome complex which disallows extrusion of proteins

3. Should not be used for anything but Vancomycin resistant E. Faecium

4. phlebitis, arthralgias/myalgias, inc bilirubin

5. inh CYP3A4- cyclosporine, midazolam

6. Central line preferred

Term
Telithromycin
Definition

1. severe hepatotoxicity, visual disturbances, QT prolongation

2. substrate and inhibitor of CYP3A4- should not be given with simvastatin, lovastatin or atorvastatin

Term
Linezolid
Definition

1. Inhibits binding of mRNA to ribosome at initiation of translation (binds 50S ribosome preventing formation of 70S initiation complex)

2. Active v E. faecalis AND E. faecium, anaerobes

3. less active v gram - bacteria

4. Bacteriostatic

5. may not need dose reduction in renal failure

6. Time dependent killing

7. MAO inhibitors inc effects of decongestants

8. myelosuppression- weekly CBC

Term
Chloramphenicol
Definition

1.MOA- Inhibits 50S peptidyltransferase activity- Bacteriostatic

2. Clinical use- Meningitis (H. influenzae, N. meningitidis, S. pneumoniae)

3. Toxicity- anemia or aplastic anemia (dose dependent), gray baby syndrome in premature infants because they lack liver UDP-glucuronyl transferase- Toxicities limit use

 

4. Resistance by modification via acetylation

Term
Azithromycin/Clarithromycin
Definition

1. Azithromycin is more acid stabile

2. reduced incidence of GI effects and once daily dosing

3. strep infection in PCN allergic pts

4. Syphilis and gonorrhea in PCN allergic pts

Term
Pentamidine Isethionate
Definition

1. antitrypanosomal agent

2. MOA is not clear

3. extremely toxic- thrombophlebitis, hypotension, hypoglycemia

4. monitor crs daily, CBC 2x weekly, daily blood glucose, BP during infusion

Term
Metronidazole
Definition

1. inhibits H production by pyruvate phosphoroclastic rxn (electron sink)

2. aerobes don't have redox systems of sufficient neg potential to interact with MNDZ

3. anaerobic protozoa, giardia, trichomoas, B. fragilis, clostridium

4. Disulfiram reaction

5. inhibited warfarin metabolism

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