Ribosomal Antibiotics Flashcards
Ribosomal Antibiotics
SAT C MLS L
Sprectinomycin
Aminoglycosides
Tetracyclines
Chloramphenocol
Macrolides
Lincomides
Stregogramins
Linezolid
Spectinomycin- MOA
binds to 30s subunit and prevents the formation of the initation complex
Spectinomycin- MOR
- Change in Binding Site
- Produce innactivating enzyme
Spectinomycin- admin
Parenteral
Spectinomycin- t 1/2
1-2 hours, 50 hrs in kidney failure
Spectinomycin- Use
- Single Dose Antibiotic tx for Gonorhea when resistant organisms are present and want to use a parenteral form
Aminoglycosides- MOA
Binds to 30s subunit –>
- inhibits 70s formation
- inhibits polyribosome formation
- misreading mRNA
Amigoclycosides- MOR
- Group transferases which innactivate the drug- Amino acetyl/aldenyl/Phospho- trasferases
- Normal inhibitory mechs
Aminoglycosides- Transport into cells
- passive diffusion through porins
- active transport across the cell membrane via O2 DEPENDENT MECHANISM, with energy from the E/C gradient, coupled to a protein pump
Therefore it only works on aerobes and is better with a cell wall destroying agent ie beta lactams
Aminoglycosides- AE
- Neprhotoxic
- Ototoxic- cochlear and vestibular
- Neurotoxic
What organ failure requires dose change of aminoglycosides
Renal
Aminoglycosides wide or narrow therapeutic range?
Narrow
Aminoglycosides- how is it dosed, what properties of aminoglycosides allow it to be dosed that way
dosed once a day for 3 reasons
- concentration dependent killing
- long post antibiotic effect
- nephrotoxicity is based on amount of time it spends at the trough, longer trough= more nephrotox, as does any dec RBF or underlying renal failure
Aminoglycosides- spectrum
Gram negative aerobes
- PSEUDOMONAS
- E.Coli
- Proteus
- klebsiella
- Enterobacter
- Serratia
Aminoglycosides- ROA
IV
Aminoglycosides- excretion
renal
Aminoglycosides- Drugs
- Streptomycin
- Gentomycin
- Tobramycin
- Neomycin
- Actinomycin
- Netilmicin
Streptomycin
- ROA: IV
- renal failure: huge t1/2 inc in renal failure
- use: in Tb
- AE: very nephrotoxic and vestibular toxic with minimal GI
Neomycin
- Admin- Topical (neosporin), Oral
- AE- highly nephroand choleartoxic-
- Absorption- not absorbed in bowel UNLESS there is damage
- Uses- bowel prep before surgery, with another drug for Gram +’s
Amikacin
- Resistance- resistance to most group transferases
- Use- use in the hospital if something is resistant to Gentimycin or Tobramycin
Tetracylines- MOA
- binds to 30s subunit–> blocks aminoacyl tRNA from binding to mRNA and the ribosome complex
Tetracyclines- MOR
- MOR- plasmid mediated efflux pump
Tetracycline- Specturm
- Staph/ Strep/ Enteric Anaerobes
- Resp infxn- H.Flu, penumococcus
- Pneumoia- Mycoplasma Pneumonia, Chlamydophila, Legionella (DOC in atypical penumonia)
Tetracyline- DOC
- atypical pneumonia
- STD- chalidmyia, PID, urea plasma, chancre
- Ricketsia
- Acne
- Lyme dz
Tetracycline- absorption
Oral absorption
Interfered with by any food with metal (Ca, Fe, Mg) or multivitamin b/c the metal will chelate the drug
Tetracyline- Drugs
- Tetracyline
- Doxycyline
- Minocyline
- Tigecycline
- Demeclocycline
Tetracyline- Length of action
Short acting
Doxycycline
excretion, AE, use
- Excretion- GI via bile
- AE= photosensitivity
- use= acne
Minocyline- AE, why?
AE= vertigo from CNS infiltration
Tigacycline- admin, spectum, clearance, t1/2, AE/ CI
- Admin= IV
- spectrum- very broad- PRSP, MRSA, NOT Pseudomonas or Proteus
- clearance- liver
- t1/2= 36 hr
- AE= N/V
- CI- during pregnancy through age 10
Demeclocylcline- AE
Causes nephrogenic Diabetes insipidus
Tetracyclines- AE
- Teeth and bone discoloration (CI during preg- age 8)
- hepatotoxicity
- photosensitivity- esp Doxycycline
Tetracycline- exceretion
All are renal except doxycycline
Macrolides- MOA
bind to 50s subunit and prevent translocation down the RNA
Macrolides- MOR
Plasmid mediated receptor site methylation
Marolides- absorption
Oral
Do Macrolides concentrate intra or extracellularly
Intra
Macrolies- Use and spectrum
Broad specturm
Used in Respiratory infxns
Macrolides- Drugs
Erythromycin
Clarithromycin
Azithromycin
Telithromycin
Erythromycin
- P450?
- Spectrum is similar to?
- Uses
- P450 inhitibor
- spectrum is similar to Penicillin
- Uses- gastroporesis b/c stimulates motilin receptor, SBE prophylaxis in dental surgery for those with a penicillin allergy
Calrithromycin
- Spectrum
- AE
- CI
- MAC, H.Pylori
- funny tasete in mouth but less GI tox than erythromycin
- CI in pregnancy
Azithromycin
- relative length of t1/2
- spectrum
- AE
- DOC
- common name
- long
- H.flu, Moraxella
- AE- tinnitus
- DOC in chalmydia
- Z-pack
Telithromycin- what charecteristics does it have that make it an important drug
Many Macrolide Resistant drugs are not resistant to this
- Binds more tightly to RNA
- poor substrate for efflux pump