Flashcards in protein synthesis inhibitors Deck (38)
what are the protein synthesis inhibitors?
30s: tetracyclines, aminoglycosides
50s: Macrolides, Clindamycin, Streptogramins, Oxazolidinones
doxycycline excretion: renal?
not renal - hepatic and fecal
Tetracycline: MOA, Spectrum, bactericidal or static?
MOA: 30s subunit (protein)
spectrum: BROAD (+ and -).
-atypicals: ricksettsia (ticks, mites, fleas, lice), chlamydia, mycoplasmic pneumoniae
-spirochete: lyme disease
3 possible ways:
-efflux pump (bacteria expels drug out of cell)
-bacteria proteins that prevent binding of drug to ribosome
*resistance to one tetracycline DOES NOT mean to resistance to all
Additions to spectrum of tetracyclines: doxycycline and minocycline
doxy: atypical: CAP, malaria, prophylaxis
mino: P. Acnes
PK of tetracyclines
Absorption decreased by:
Divalent cations ( Ca, Fe, Mg or Al)
Antacids (don't take with these)
=reduced bioavailability when with foods
poor CNS penetration
super infection can occur with what type of antibiotic?
any broad spectrum (most often cause is candida or Cdiff)
serious adverse effects of tetracycline
Staining of teeth
Bind to calcium deposited in newly formed bone or teeth in young children and fetal teeth during pregnancy
Fetal bone deformities
Deposit in bone leading to deformity or growth inhibition
CONTRAINDICATED in pregnant women, infants, children < 8 years or younger
"TETRAcycline = TERATogenic"
Glycycline --> tigecycline
Tetracycline derivative (semisynthetic of minocycline)
MOA: 30s subunit
Spectrum: BROAD (+ and -) including MRSA, VRE
atypical- legionella (CAP)
clinical uses: CAP, infections of deep tissue and intra-abdominal
"GNATS" - all "mycin" except Amikacin
post antibiotic effect is most common in what type of abx?
those that inhibit protein/DNA/RNA.
PAE- suppression of bacterial growth after brief drug exposure
PK of aminoglycosides: Absorption, distribution, elimination
abs: only IV (occassional IM) or topical (conjunctivitis)
distribution: good, no CSF or eye (unless topical) but can use for meningitis with other drugs if inflamed and synergistic (beta lactams)
elimination: renal, MUST make dose adjustment w/ kidney failure. (monitor serum drug levels )
aminoglycosides are good to treat what?
gram neg serious infections: bacterial meningitis, sepsis, (endocarditis), osteomyelitis, etc)
aminoglycosides adverse effects
ototoxic, nephrotoxic, neuromuscular blockade
triple antibiotic ointment
neomycin (gram- and gram +, too nephrotoxic for oral or IV- hence ointment)
polymixin (gram -)
bacitracin (gram +)
"mean GNATS caNNOT kill anaerobes"
GNATS: gentamycin, neomycin, amikacin, tobramycin, streptomycin
NNOT: nephrotoxicity, neuromuscular blockade, ototoxic, teratogen (oto and nephro for fetus too)
erythromycin is used mostly for what?
acne (only macrolide that is bacteriostatic instead of cidal
fidaxomicin use for?
MOA, spectrum, adverse
Cdiff but VERY expensive
MOA: thought of as macrolide but binds to RNA polymerase and stops protein binding
Spectrum: NARROW- CDiff (gram +)
Adverse: bowel obstruction or GI hemorrhage
"FACE" fidaxomycin, azithromycin, clarithromycin, erythromycin
..or girls names - "FrIDA, AZI, CLARe, ERYn"
macrolide MOA and spectrum
MOA: 50s subunit
spectrum: gram + cocci
chlamydia, mycoplasma, legionella(CAP)
macrolides- drug resistance patterns
primarily why we dont use erythromicin anymore
1. target modification- prevent abx to ribosome bind
3. drug inactivation
axithromycin: - LONG half life- different Dosing - “Zpack” - pt only takes for 5 days but actually stays in system for 10 days - increases pt compliance
EASIER IS BETTER -
bile and feces
generally use macrolides for what clinical uses?
STIs and CAP
adverse effects of MACROlides
GI Motility (usual stomach upset)
acute Cholestatic hepatitis
-erythro and clindo are worst for these, Azithromycin is best to use to limit adverse effects
-first 2 most important
Erythromycin and Clarithromycin have what significant danger?
drug interaction- inhibit CYP34A - increases serum levels of other drugs (esp. statins and warfarin)
treatment of anerobes above and below diaphram
abx most common cause of superinfection Cdiff
Clindamycin and fluoroquinolones