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33 Cards in this Set

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Spectinomycin- Class, MOA, Resistance
Class: related to aminoglycosides
MOA: bacterioSTATIC, binds to 30S subunits and inhibits initiation complex
Res: binding site alteration or drug inactivating enzymes
Spectinomycin- Use, PK
- gonorrhea, though not DOC
PK: poorly absorbed by GI
Aminoglycosides- MOA, Use,
MOA: bind to 30S subunit and inhibit initiation complex, cause misreading of genetic code on mRNA template, are bacteriCIDAL, transported across the membrane by O2 DEPENDENT process, very highly polar, acidic environment limits absorption
Aminoglycosides- Use, PK
Use: aerobic gram negatives, often used w/ beta lactam antibiotics, good for pseudomonas
PK excreted UNCHANGED in urine, 1x/day dosing b/c ototox related to trough levels
Aminoglycosides- AE, Resistance
AE: nephrotoxic (acute tubular necrosis), neurotoxic (neuromuscular blockade), OTOTOXIC
Res: group transferases-- transfer of groups, such as acetylation to the drug itself
Aminoglycoside drugs
- streptomycin, gentamycin, tobramycin, neomycin, and amikacin
- Streptomycin, Gentamycin, Tobramycin, Neomycin, and AMikacin- Class
Aminoglycosides
Streptomycin- Special use
Amikacin- special use
Streptomycin: TB
Amikacin: resistant to inactivating enzymes, used when widespread ressistance to gentamycin/tobramycin in the hospital.
Would aminoglycosides be able to be transported across the cell wall of an anaerobic bacteria? Does low extracellular pH help in transport of aminoglycosides?
1. NO
2. NO
- anaerobic and acidic conditions inhibit aminoglycoside transport
What is one very unique mechanism of resistance for aminoglycosides?
Which aminoglycoside is resistnat to many inactivating enzymes?
- plasmid mediated production of group transferases which inactivate the drug
- Amikacin
Aminoglycosides- PK, AE
PK: not absorbed by GI tract, usually require IV or IM
AE: ototox, nephrotox, NM blockade, and skin rxns
Aminoglycoside- Use, what drugs are often used synergistically?
Use- aerobic gram (-) organisms, strict anaerobes are resistant
- often used w/ beta lactam drugs synergistically
Tetracyclines- MOA
- inhibit binding of aminoacyl t RNA to the mRNA ribosomal complex
- bind to 30S subunit, are bacterioSTATIC
Tetracyclines- MOR
- efflux of drugs by plasmid coded efflux protein pump= TEST Q
- altered drug permeability/enzymatic inactivation of the drug
Tetracyclines- PK, AE, Use, CI
PK: oral, does not absorb well into the CNS
AE: hepatotoxicitiy, teeth discoloration
CI: preggers, young children
Use: BROAD spectrum- both gram - and gram +
- also works of rricketsiae, chlamydiae, and mycoplasma infections, borrelia bergdorfiri (lyme dz)
Chloramphenicol- MOA
- bind ot 50 S subunit and inhibit the peptidyl transferase- in transpeptidation
- bacterioSTATIC
Chloramphenicol- MOR
- production of plasmid coded drug inactivating enzyme-- chloramphenicol acetyltransferase
Chloramphenicol- PK(absorption)
- GI tract absorption, well distributed in body including the CSF
- hepatic inactivation
Chloramphenicol- AE
- Grey baby syndrome
- dose dependent bone marrow suppression- inhibition of mitochondrial ribosomes
- dose independent aplastic anemia
Chloramphenicol- Use
- BROAD spectrum, typhoid fever, (big 3) meningitis, children and pregnant women w/ rocky mt spotted fever
Macrolides- MOA, Drugs
- erythromycin, clarithromycin, azithromycin, and telithromycin
- MOA: bind to 50S, prevent the ribosome form translocating down the mRNA
Macrolides(thromycins)- MOR
- methylation of receptor on the 50 S ribosome results in decreased affinity for the drug
- production of drug inactivating enzymes
- reduced permeability of the drug
Macrolides- Absorption/Distribution, Use
- GI tract absorption, wide distribution, concentration INSIDE cells
Use: broad spectrum, respiratory infections (even severe atypicals- legionairres, mycoplasma, corny dip, bordatella pertussis)
Lincosamides- Drugs, MOA
- LIncosamide, Clindomycin
- MOA: bind to 50S subunit, prevents ribosome from translocating down the mRNA
Lincosamide- MOR
- methylaiton of ribosomal receptor site
- production of drug inactivating enzymes
- reduced permeability to the drug
Lincosamides- Absorption/PK, Use
- concentrated INSIDE cells
- excreted in urine and BILE
Use: ANaerobic infection above diaphragm, aerobic gram + cocci infections
Streptogramins- MOA
- bind to different sites on 50 S ribosomal subunit and work to prevent ribosom from translocating down the mRNA
- bacteriaCIDAL
Streptogramins- MOR
- methylation of quiniupristin binding site
- production of drug inactivating enzyme
- active transport efflux
Streptogramins- Use
- penicillin resistant pneumococci- PRSP
- methicillin resistant stap aureus- MRSA
- vanc resistant staph aurus
- vanc resistant enterococci
Linezolid- MOA
- bacteriaCIDAL- binds to a unique site on 50S subunit and inhibits formation of 70S ribosome
- inhibits initiation complex
- inhibits translocation of peptidyl tRNA
LInezolid- MOR
- mutation of binding site rRNA
- no cross resistance w/ other drugs
LInezolids- USe
- PRSP
- MRSA
- VRSA
- VRE
Macrolides, LIncosamides, and streptogramins share what type of resistance mechanism?
- constitutive methylase production which confers resistance b/c they share the same ribosomal binding site-- called MLS type B resistance