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antibiotics
antibiotcs
41
Biology
2nd Grade
10/07/2011

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Term
penicillin
Definition
g=parenteral, v=oral
active against G+
susceptible to B lacatamases
Term
nafcillin
Definition
penicillin resistant, narrow spectrum
protected against B lactamases
Used only against pen-G resistan staphylocci
not effective against G-
Term
amoxicillin
Definition
broad-spectrum (aminopenicillins)
additional activity against G-
susceptible to B lactamases
Term
ticarcillin
Definition
carboxypenicillin
pseudomonas aeurginosa
other G- infections
susceptible to B lactamase
large doses cause sodium overload
Term
piperacillin
Definition
ureidopenicillin
pseudomonas aeurginosa
other G- infections
susceptible to B lactamase
Term
penicillin allergy
Definition
most common drug allergy
due to breakdown into peniccoyl which binds proteins
cross reactive to beta lactams
hypersensitivity can be fatal
Term
cefazolin
Definition
high against G+
alternative if mild penicillin allergy
prophylaxis in surgery
Term
cefoxitin
Definition
more active against G-
resistance to B lactamases
less active than 1st gen to G+
poor CNS penetration
Term
cefotaxime
Definition
good CNS penetration and good against G-
meningitis and gonorrhea
Term
cefepime
Definition
broad spectrum, good CNS,
useful in empirical treatment
Term
cephalosporins
Definition
cleared by kidney
poor absorption of many of them
hypersensitivity, diarrhea, potentially nephrotoxic
Term
carbapenems (imipenem)
Definition
B lactam w/ broad spectrum
binds PBP1 and PBP 2
primarily kidney elimination
cilastatin prevents renal inactivation
nausea, diarhhea, seizures
Term
aztreonam
Definition
Monobactam
binds PB3 to inhibit cell wall synth.
active toward G- only
IV due to poor absorption
excreted by kidneys
resistant to B lactamases
safe in patients with penicillin allergy
Term
vancomycin
Definition
tricyclic glycopeptied
prevents polymerization of cell wall precursors
only works in G+
excreted by kidneys
treats MRSA, severe CDAD
Ok for penicillin allergies
ototoxic, red man syndrom, thrombophlebiits
Term
fosfomycin
Definition
phosphoenol pyruvate analogue for G- UTI
inhibits production of murein monomers
enters bacteria via glycerophosphate monomer
Term
bacitracin
Definition
works on G+
cyclic polypeptide
inhibits bactoprenol dephosphorylation
bactoprenol trans murein monomers into periplasmic space
used topically with other agents
nephrotoxic in high concentrations
Term
aminoglycosides
Definition
interfere with protein synthesis
streptomycin, gentamicin, amikacin, neomycin (SANG)
HIGHLY POLAR--not well distributed
attract LPS
bactericidal against G-
passive diffusion through porins then active transport into cytosol (O2 dependent)
binds 30S and causes RNA misreading
blockade of translocation
LONG post antibiotic effect
Term
streptomycin
Definition
aminoglycoside
2nd line for tuberculosis
Term
gentamicin
Definition
combine with B lactam to fight G+ cocci and also effective in combo againsst G- organisms
Term
amikacin
Definition
aminoglycoside
least susceptible into inactivation
Term
neomycin
Definition
aminoglycoside
topical therapy
Term
aminoglycosides (adverse reactions)
Definition
ototoxicity if long exposure
nephrotoxicity
neuromuscular blockade
Term
tetracycline
Definition
transported by active transport
binds 30S, inhibits binding of tRNAs to A site of mRNA ribosomal complex
resistance due to production of interfering proteins or efflux transporters
orally effective, forms chelates, distributed widely in CNS, bone teeth, placent, breast milk
Term
tetracycline (uses and adverse rxns)
Definition
G+ and G- organisms
tigecycline--new and effective
rickettsia, chlamydia, lyme disaese, anthrax, mycoplasma pneumonia
acne and periodontal disease
treat peptic ulcer with metronidazole combo
prophylaxis of malaria

ADVERSE: GI irritation, bone and teeth deposition (don't give to kids), renal toxicity, superinfection (CDAD), hepatotoxicity, photosensitivity
Term
Macrolides (erythromycin)
Definition
bacteriostatic
bind reversibly to P site on 50S, inhibiting translocation
Resistance--efflux or methylation of 50S subunit via erm ghepatic metabolism via cyp3A4--interacts with other drugs
Legionnaire's, whooping cough, diptherica, chlamydia
ADVERSE: GI irritation chestatic hepatitis, prolonged Q-T
Term
Clindamycin
Definition
Lincosamide
binds at 50S to block peptide bond formation
G+ aerobes
Group A strep, gas gangrene, abdominal and pelvic bacteroides fragilis
diarrhea and CAD--adverse
Term
chloramphenical
Definition
binds peptidyl transferase to prevent attachment of incoming tRNA to A site
MRSA, G- anaerobes
widely distributed and liver metabolism
resistance--acetyltransferase
only for life threatening situations
ADVERSE--grey baby, bone marrow suppression, aplastic anemia
Term
linzeolid
Definition
oxazolidinone
binds at unique site of 23S rRNA of 50S subunite--blocks fomration of initiation complex
use--MDR G+--VRE and MRSA
ADVERSE--myelosuppression (anemia, leucopenia, thrombocytopenia)
interacts w/ MAOIs and SSRIs
Term
quinupristin-dalfopristin
Definition
synergistic combo
bind to peptidyl transferase of 23S rRNA to block initiation
dalfopristin--inhibits peptidyl transferase
Quinupristin binds at macrolide ssite
mainly for G+
ADVERSE--hyperbilirubinemia and myalgia/arthralgia
Term
Fluoroquinolones
Definition
(ciprofloxacin)
inhibit one of two topoisomerase II enzymes
prophylaxis of anthrax
urogenital tions
ADVERSE--tendon rupture, confusion, prolonged Q-T interval
CDAD
inc. plasma levels of warfarin and theophylline
reduced absorption with cations
Term
Metronidazole
Definition
anaerobic bacteria and protozoa
prodrug--PFOR or nitroreductase in anaerobes produces cytotoxic intermediates that destray DNA!
use for CDAD
Use with tetracycline to fight H. pylori
ADVERSE--headache, GI disturbances, weird colored urine, metallic taste
CYP3A4 substrate
Term
Sulfamethoxazole
Definition
sulfonamide
inhibits dihydropteroate synthase (folic acid synthesis)--prevents DNA replication
board spectrum G+/G-
E coli UTI
ADVERSE
Kernictus, hypersensitivity, hemolytic anemia, renal damage
Term
Trimethoprim
Definition
inhibitor of dihydrofolate reductase
use against G- and G+
UTIs
bone marrow suppression
Term
Co-trimoazole
Definition
synergistic TMP/SMX
broad spectrum of G+/G-
ADVERSE: myelosuppression
UTIs, pneumocystis jirovici pneumonia
otitis media infections
Term
daptomycin
Definition
cycli lipopetide
Ca++ dependent insertion into membrane
only active against G+
skin infections by MRSA or VRSA
ADVERSE-myopathy
Term
colistin
Definition
polymyxin E
binds plasma membrane and disrupts bilayer
two forms--sulfate (dermal, oculare, GI) and methate (parenteral)
MDR G-
ADVERSE--neuro/nephro toxic
Term
Isoniazid
Definition
inhibits mycolic acid synthesis
passively diffuses into mycobacteria
activated by KatG
resistance--change in KatG gene
inactivated by liver acetylatin
treats TB
peripheral neuropathy due to loss of B6
Hepatotoxicity--potentially fatal necrosis
Term
Rifampin
Definition
Rifamycin
binds to B subunit of RNA polymerase
resistance--muation of rpoB
treats TB, leprosy, H influenzae, S aureus, Legionalla, Neisseria meningitidis
ADVERSE--hepatotoxic (jaundice and hepatitis)
discoloration of body fluids
induces many CYP forms
Term
Ethambutol
Definition
Inhibits mycolic acid syntehsis via arabinosyl transferase III
resistance--embAB gene
use to treat TB in combo
ADVERSE--optic neuritis
Term
Pyrazinamide
Definition
prodrug--converted to pyrazinoic acid by mycobacterial pyrazinamidase
treat TB
ADVERSE--hepatotoxic, hyperuricemia(gout)
Term
Streptomycin
Definition
Second line TB treatment
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