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222 Cards in this Set
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st. john's wort
plant name |
Hypericum Perforatum
|
|
st. john's wort
active ingredients |
hypericin & pseudohypericin
|
|
st. john's wort
use to tx |
mild-moderate depression
(hypericin) anti-viral agents- retroviruses |
|
st. john's wort
propossed mech |
unknown:
GABA agonist SSRI- block serotonin uptake |
|
st. john's wort
side effects |
phototoxicity
hypertention (d/t blockade of NE in addition to Ser) |
|
things to avoid with
st. john's wort |
aa's:
tryptophan / tyrosine tyramine: wine, smoked/pickled foods, cheese beta 2 agonists stimulants: amphetamines, coffee, decongestants, diet pills, cold meds |
|
ginseng
active ingredients: america = |
america = Panax Quinquefolius
active ingredient = panaxosides |
|
ginseng
active ingredients: asia = |
asia = Panax Ginseng
active ingredient = ginsenosides |
|
panax ginseng
tx: |
-- depression
axiolytic: GABA receptor modification --> similar to benzos decrease anxiety --> similar to diazepam --colds, influenza, respiratory problems |
|
T / F:
panax ginseng works immediately |
false:
takes 4-5 days for effects |
|
panax ginseng
side effects |
asthma attack
palpitations HTN no reported drug interactions |
|
ginkgo biloba
(ginkgobene) plant active ingredients |
plant = ginkgo biloba
alcohols, aldehydes, ketones, terpenes, steroids, flavonoids, glycosides |
|
ginkgo biloba
action |
dilates blood vessels
increases cerebral & peripheral blood flow decreases cerebral glucose levels neuroprotective - hypoxia & ischemia inhibits both MAO A & B (anxiolytic- synergistic action with antidepressants) |
|
ginkgo biloba
tx |
vasculare disorders:
phlebitis, leg ulcers, cerebral atherosclerosis, diabetic vasculature disease) mental/emotional fatigue clotting disorders: stoke / MI HA Raynaude's syndrome neuroprotectant: free radial scavenger |
|
ginkgo biloba
tox |
excessive bleeding or hemorrhage
increased cerebral bleeding in elderly |
|
Kava-Kava
bush active ingredients |
bush = piper methysticum
"intoxicating pepper" ingredients: kavain & dihydrokavain methysticin & dihydromethysticin |
|
kava-kava
action |
stimulator when CNS activity is low
inhibitory when CNS activity is high |
|
kava-kave
preparation uses |
capsules & teas
sedative, m. relaxant, diuretic, anxiolytic, analgesia |
|
kava-kava
side effects |
acute- unknown
chronic - many red eye, SOB, liver/kidney damage, decreased appetite, loss of m. control, m. weakness, dry skin, many more |
|
used to improve sleep
do NOT use with benzos |
valerian
|
|
red yeast fermented on rice
lowers cholesterol |
cholestin
|
|
from crab shells and cartilage
?? use |
glucosamine & chondroitin sulfates
|
|
boosts immune system by increaseing WBC activity
|
echinacea
|
|
antiseptic to tx sores in mouth
|
goldenseal
|
|
DHEA
precusor for what |
DHEA --> androstenediol --> testosterone
dehydroepinadrosterone |
|
DHEA
declines in what |
aging
lupus alzheimer's cancer diabetes obesity |
|
DHEA
low dose high dose |
low dose:
wt. loss, strength/endurance, improved CH and HDL/LDL, improved mental alertness or cognition high dose: liver dysfxn, decreased CO, masculinization of females |
|
melatonin
secreted by what tx |
secreted by pineal gland: circadian rhythm
sleep aid and jet-lag, not proven anti-aging |
|
melatonin
side effects |
infertility
loss of libido |
|
beta lactam antibiotics
|
beta lactam antibiotics:
inhibit cell wall synthesis --penicillins --B-lactamase inhibitors --cephalosporins --monobactams --carbapenems |
|
penicillins
narrow spectrum: penicillinase resistant: extended spectrum: |
narrow spectrum:
penicillin G penicillin V penicillinase resistant: dicloxacillin nafcillin extended spectrum: amoxicillin ampicillin piperacillin ticarcillin |
|
B-lactam antibiotic
mech |
block cell wall synthesis by inhibition of peptidoglycan cross-linking (irreversibly binds enzyme = transpeptidase)
PBP - penicillin-binding proteins |
|
which are acid-stable
|
acid-stable
(oral) penicillin V amoxicillin dicloxacillin nafcillin |
|
which are acid-labile
|
acid-labile
(parenteral) peperacillin ticarcillin |
|
where are penicillins NOT found
|
widely distributed, except NOT in:
--brain --prostatic secretions --intraocular sectretions therefore- not good for txing these |
|
what accounts for penicillin G's better absorption in the elderly?
|
G is destroyed by gastric fluid at pH2, so decrease in acid production with age accounts for better G absorption in the elderly
|
|
how are penicillins eliminated?
t 1/2? |
rapidly eliminated by glomerular filtration & renal tubular secretion
T 1/2 = 30-90 min |
|
which two penicillins are also excreted in the bile?
|
ampicillin
nafcillin |
|
what drug competes with the penicillins for the organic acid transporter in the proximal tuble and used to prolong T 1/2?
which penicillins are long-acting IM preps? |
probenecid (gout)
benzathine pen G procaine pen G |
|
DOC:
syhpilis meningitis pneumonia |
pen G
syhpilis (t. pallidum) meningitis (meningococci) pneumonia (pneumococci) gram + cocci note: until certain that pen-sensitive, a third gen cephalosporin or vancomycin is indicated |
|
DOC:
pharyngitis |
pen V
pharyngitis (strep pyogenes) |
|
used for penicillinase-producing staph
|
dicloxacillin (oral)
nafcillin (parenteral) "naf for staph" osteomyelitis endocarditis skin/tissue infections |
|
MRSA
DOC? |
methicillin resistant staphylococcus aureaus
DOC = vancomycin |
|
what extended spectrum pen include uses for some G-?
|
aminopenicillins:
amoxicillin ampicillin antipseudomonal: piperacillin |
|
DOC:
otitis, URT s. pneumo & h. influ |
amoxicillin
|
|
DOC:
meningitis d/t L. monocytogenes in immunocompromised |
ampicillin
|
|
emperic tx of suspected bacterial meningitis?
|
ampicillin + vancomycin + 3rd gen cephalosporin
|
|
DOC:
G- P. aeruginosa nosocomial pneumonia |
piperacillin (antipseudomonal)
|
|
hypersensitivity
|
IgE mediated
-rash -nephritis -serum sickness -anaphylactic shock degradation products of penicillin combine with protein to form antigenic compounds |
|
DOC:
strep pneumo |
strep pneumo
pen-sensitive: amoxicillin (kids) azithromycin ceftriaxone pen-resistant: levo/moxifloxacin |
|
DOC:
acute pharyngitis |
benzathine pen G
|
|
DOC:
scarlet fever strep |
benzathine pen G
|
|
DOC:
acute otitis media |
amoxicillin
|
|
DOC:
helicobacter pylori |
amozicillin
clarithromycin |
|
DOC:
impetigo |
staph:
dicloxacillin nafcillin mupirocin strep: amoxicillin mupirocin (topical) |
|
what class of Abs are more stable than penicillins (highly resistant to penicillinase) and less likely to cause hypersen. rxns?
|
cephalosporins
|
|
cephalosporins
excretion |
renal
except ceftiaxone = bile |
|
cephalosporins
which generation is primarily active against most G+ cocci, and which not covered? also some G- |
1st gen
not MRSA not enterococci |
|
cephalosporins
1st gens |
cephalexin (oral)
cefazolin (parenteral) |
|
cephalosporins
skin and soft tissue infections streptococci |
cephalexin
|
|
cephalosporins
sx prophylaxis against staph and G- enteric bacilli |
cefazolin
|
|
which 1st gen is preferred d/t longer T1/2
|
cefazolin
|
|
cephalosporins
2nd gen |
cefprozil (oral)
cefuraxime Na cefotetan cefoxitin |
|
cephalosporins 2nd gen
intra-ab, gyn, biiary infections |
cefotetan
|
|
cephalosporins 2nd gen
sx prophylaxis |
cefoxitin
|
|
cephalosporins
2nd gen otitis caused by amoxi-res H. influ |
cefprozil
|
|
cephalosporins 2nd gen
emperic therapy for community-acquired pneumonia |
cefotetan
|
|
only 2nd gen to enter CNS
|
cefuroxime Na
|
|
cephalosporins
3rd gen |
cefotaxime
ceftriaxone |
|
cephalosporin
gen that has wider range of activity against G- including: enterobacteriacae H. influ M. catarrhalis |
3rd gen
|
|
3rd gen tx's?
|
gonorrhea
UTI abdominal otitis media meningitis pneumonia lyme disease |
|
what gens enter CNS?
|
4th
most 3rds and cefurozime Na (only 2nd to enter CNS) |
|
cephalosporins
gen that is very resistant to BLM and targets G- |
4th gen
cefepime |
|
what do 4th gen tx?
|
cefepime
nosocomial paths: citrobacter freundii enterobacter cloacae |
|
which organisms are cephalosporins NOT effective against?
|
LAME
Listeria monocytogenes Atypicals: chlamydia & mycoplasma MSRA enterococci |
|
can someone with sever rxn to pens take cephs?
|
no
but mild pen rxn pts tend to be okay |
|
clavulanate
sulbactam tazobactam |
beta-lactamase inhibitors
|
|
b-lactamase inhibitors
|
clavulanate
sulbactam tazobactam irreversibly bind b-lactamase produced by wide range of bacteria |
|
what are b-lactamase inhibitors inactive against?
|
type I chromosomal BLMs
induced in enterobacter, acinetobacter, citrobacter by 2nd & 3rd gen cephalos |
|
aztreonam
class? |
monobactams
monocyclic b-lactam |
|
monobactams
use? |
aztreonam
aerobic G- enterobacter citrobacter Klebsiella Proteus P. aeruginosa esp. muti-drug resistant strains |
|
what are resistant to monobactams?
|
b-lactamase producing G-
anaerobes G+ |
|
carbapenems
|
imipenem
meropenem |
|
carbapenems
tx? |
systemic infections - esp. aer / anaer enteric bacilli
active against a wide range of G+ and G- including many aerobic and anaervobic G- bacilli |
|
what is given in conjunction with imipenem?
|
imipenem + cilastin
renal dehydropeptidase inhibitor |
|
what inhibits renal excretion of carbapenems?
|
probenecid (gout)
|
|
T / F
carbapenems are a good option for those allergic to pens |
NO
cross-sen with pens, cephalos, and other b-lactams avoid in allergic pts |
|
what are other key bacterial cell wall synthesis inhibitors?
|
vancomycin
bacitracin fosfomycin |
|
T / F
vancomycin is well absorbed from the gut |
false
|
|
vancomycin
|
active against several G+ cocci & bacilli
serious infections caused by pen-res orgs: --MRSA --enterococci |
|
what cell-wall inhibitor is a topical tx of minor skin and ocular infections
|
bacitracin
G+ staph & strep |
|
Fosfomycin
binds to? |
irreversibly inhibits enolyruvyl transferase in initial stages of cell wall peptidoglycan syn
|
|
fosfomycin
tx |
uncomplicated UTIs
single oral dose wich is excreted unchanged in urine and feces |
|
drug:
klebsiella pneumoniae |
imipenem
meropenem (carbapenems) |
|
cephalo drug:
strep pneumo |
ceftriaxone
|
|
cephalo drug:
impetigo staph |
cephalexin
|
|
meningococcemia
n. meningitidis |
cefotxime
ceftriaxone (3rd gen) |
|
Pseudomonas
lung |
piperacillin
|
|
Pseudomonas
CNS |
cefepime / ceftazidime + gentamicin
|
|
bacterial meningitis (H. influ) in 2 yo?
|
cefotaxime
3rd gen cross CNS and are effective against G- |
|
UTI baused by aerobe G- bacilli. allergic to penicillin
|
aztreonam
generally safe in those allergic to pens and cephs |
|
parenteraly administered against b-lactamase producing H. influ and N. gonorrhea
|
ceftriaxone
|
|
most active against Pseudomonas?
|
piperacillin
antipsuedomonal drug |
|
endocarditis penicillinase-producing staph. parenteral
|
nafcillin
penicillinase-resistant |
|
drugs that affect 30S ribosomal subunit
|
aminoglycosides
tetracyclines |
|
amikacin
gentamicin neomycin striptomycin tobramycin |
aminoglycosides
|
|
aminoglycosides
mech |
block initiation of protein syn by fixing the 30S/50S complex at the start codon
causes misreading of mRNA leading to --premature termination of translation --incorporation of incorrect aa. (abnormal proteins) |
|
aminoglycosides
bacter___? |
rapidly bactericidal
poorly absorbed from gut conc dependent postantibiotic effect not-metabolized (renal) |
|
how are aminoglycosides administered?
|
parenterally for systemic infections
topical for skin, m. mem, eye |
|
T / F aminoglycosides are highly basic and do not readily nter host cells or cross BBB
|
true
|
|
what inactivate aminoglycosides?
|
acetylase
adenylase phosphorylase |
|
aminoglycoside
tox |
nephrotox
prox. tube ototox labyrinth hair cells |
|
aminoglycosides
tx? |
aerobic G- bacilli
|
|
aminoglycoside
multi-drug-resistant TB plague (yersinia pestis) tularemia (franacisella tularensis) |
streptomycin
|
|
aminoglycoside
most active against enterobacteriaceae species |
gentamicin
|
|
aminoglycoside
most active against P. aeruginosa |
tobramycin
|
|
aminoglycoside
used when res to other aminos resistant to enzyme inactivation |
amikacin
|
|
aminoglycoside
topical most nephrotox |
neomycin
|
|
tetracyclines
|
tetracycline
doxycycline minocycline |
|
tetracyclines
mech |
bind to 30S
prevent access of aminoacyl-tRNA to the A site |
|
T / F
tetracyclines are broad spectrum and bacteriostatic |
true
|
|
what is oral bioavailablility of tetracyclines
|
70%
|
|
what can you NOT take with tetracyclines
|
antacids
iron supplements |
|
which tetracycline is not dependnent upon renal elimination
|
doxycycline
|
|
which tetracycline reaches CNS and penetrates skin more effectively
|
minocycline
|
|
tetracyclines
adverse effects |
discoloration of teeth
photosensitivity --accumulates under skin and absorbs UV-- sunburn-like |
|
DOC:
RMSF |
tetracyclines
|
|
DOC:
lyme disease |
tetracyclines
|
|
drug for:
acne vulgaris |
tetracyclines
|
|
drug for:
chlamydia |
doxycyclines
|
|
drug for:
PUD H. pylori |
tetracyclines
|
|
DOC:
borrelia burgorferi |
doxy
|
|
alt drug for:
treponema pallidum |
pen G
doxy! alt drug |
|
drugs that affect 50S subunit
|
macrolides
chloramphenicol clindamycin quinupristin-dalfopristin linezolid mupirocin |
|
azithromycin
clarithromycin erythromycin |
macrolides
|
|
macrolides
mech |
bind 50S and prevent translocation of nascent peptide from the A side to the P site
inhibits binding of the next aminoacyl tRNA |
|
how are macrolides given?
|
orally
absorption and activity of erythromycin is redused by gastic acid |
|
which are more readily absorbed (less GI distress), have longer T1/2, and achieve highter tissue conc
|
azythromycin
clarithromycin |
|
macrolides
excretion |
urine
bile |
|
which macrolides have CYP activity and can cause tox of other drugs?
|
erythromycin
clarithromycin |
|
macrolides
tx |
URI & pneumonia
streptococci pneumococci chlamydiae H. influ --otitis --sinusitis M. pneumoniae L. pneumophila H. pylori |
|
azithro very active against..
|
chlamydiae
H. influ --otitis --sinusitis M. pneumoniae L. pneumophila |
|
which macrolide is most active agianst H. pylori?
|
clarithromycin
|
|
50S Abs
|
macrolides
chloramphenicol clindamycin quinupristin-dalfopristin linezolid mupirocin |
|
clindamycin is similar to
|
erythromycin
|
|
does clindamycin readily enter CNS?
|
no
high risk of GI superinfection C. Diff sever diarrhea can be fatal |
|
tx of C. diff
|
metronidazole or vancomycin
|
|
clindamycin excretion
|
urine
bile |
|
clindamycin
tx |
pen-res strep
anaerobic -bacteroides fragilis -clostridium perfringens |
|
chloramphenicol
mech |
50S at peptidyltransferase site and inhibits transpeptidation
|
|
chloramphenicol is highly lipophilic
|
true
readily enters the CNS |
|
chloramphenicol
excretion |
urine
metab'd by glucuronate conjugation --adjust for neonate to prevent sever tox |
|
chloramphenicol
side effect |
anemia d/t inhibition of iron incorporation into heme
|
|
chloramphenicol
tx |
broad spctrum
meningitis - pneumococci - menigococci - H. influ |
|
newer class of Ab's called streptogramins
|
quinupristin-dalfopristin
|
|
quinupristin-dalfopristin
administration |
IV
wide distribution (NOT CNS) |
|
quinupristin-dalfopristin cross into CNS
|
no
|
|
quinupristin-dalfopristin
mech |
similar to macrolides-
prevent addition of new aa. |
|
dalfopristin inhibits __
|
peptidyl transferase
synergistically enhances binding of quinupristin blocks formation of the peptide bond |
|
quinupristin-dalfopristin
tx |
vancomycin-resistant organisms
|
|
newer class of dugs called oxazolidinediones
|
linezolid
|
|
linezolid
admin |
IV or oral
oral bio = 100% |
|
linezolid
mech |
binds 50S (23S RNA)
prevents form of fxnal 70S complex |
|
T / F
cross-resistance is more likely d/t linezolid's unique mech |
false
unlikely!! |
|
linezolid
tx |
aerobic G+
vancomycin-res E. faecium MRSA |
|
mupirocin
structure / mech |
sturucture is unrelated to other Abs
side chain = like isoleucine competes for bacterial isoleucine tRNA synthetase |
|
mupirocin
cross-rxn? |
no
|
|
mupirocin
tx |
active against most staph
fist effective topical for impetigo (strep & staph) |
|
DOC:
bordetella pertussis |
azithromycin
|
|
acne vulgaris
|
tretinoin
erythromycin clindamycin |
|
kid pharyngitis by chlamydia pneumoniae. adverse rsxn to amoxi
|
azithromycin
macrolide-- very effective against otitis and URI |
|
acts at 50S subunit to inhibit translocation of peptidyl-mRNA from accepter to donor site?
|
azithromycin
macrolide others: chlarithromycin & erythromycin |
|
requires a 7 day course of tx in order to be effective against uncomplicated gonorrhea/
|
doxycyclin
compliance is an issue |
|
H. influ, M. cat, N. gonorrh are all B-lactamase producers. effective against ALL?
|
ceftriaxone
IM DOC Cefepime (4th) is also efective |
|
antifolate drugs
|
sulfonamides
trimethoprim |
|
sulfonamides
|
sulfamethoxazole
sulfacetamide - topical ocular silver sulfadiazine - burns |
|
sulfamethoxazole
|
rapidly absorbed
T1/2 11hrs |
|
sulfamethoxazole
tx |
UTI
|
|
T / F
water should be restricted while taking sulfamethoxazole |
false
hydration is mandatory drug is inactivated by N-acetylation metabolite can precipitate in renal tubles causeing crystalluria |
|
trimethoprim
tx |
synthetic aminopyrimidine drug
weak base-- concentrates is tissues that are more acidic: -prostatitis -vaginitis |
|
TMP-SMX
|
UTI & prostate infections
-e. coli -k. pneumonia -proteus -enterobacter |
|
DOC:
pulmonary by pneumo. jiroveci |
TMP-SMX
immunocompromised pts |
|
T / F
TMP-SMX is active against psudo. aeruginosa, which is ofter hospital UTI |
false!!
not effective for P. aeruginosa |
|
Fluoroquinolones
|
ciprofloxacin G-
levofloxacin Norfloxacin |
|
Fluoroquinolones
absorption |
well absorbed and widely distributed
lungs, kidneys, prostate, endometrium, ovaries |
|
T / F Fluoroquinolones have short postantibiotic effect
|
false
long- bactericidal conc. dependent killing |
|
Fluoroquinolones inhibit the metab of __ and so it should be limited
|
caffeine
|
|
Fluoroquinolones
mech |
inhibits bact DNA topoisomerase
type II (gyrase): G- induce neg supercoils in cirular DNA eliminate the positive supercoils present ahead of the DNA rep fork type IV: G+ separates the DNA once replication is complete (decatenation) |
|
Fluoroquinolones
UTI |
norfloxacin
-enterobacteria -P. aeruginosa |
|
Fluoroquinolones
tx |
UTI - norfloxacin
diarrhea - camp, salm, e. coli RTI - pneumococci, H. influ, M. cat levofloxacin ocular - levofloxacin |
|
rapidly excreted in urine
turns urive brown |
nitrofurantoin
|
|
nitrofurantoin
mech |
bact enzymes reduce to active drug which damge DNA
|
|
how does fxn of nitrofurantoin coorespond to urine pH
|
pH > 5 = decreases activity
pH < 5 = increases activity remember: likes acid |
|
nitrofurantoin
tx |
UTI
acute infections localized to bladder many stains of E. coli & enterococci |
|
unique lipopeptide Ab for skin infcetions
|
daptomycin
|
|
daptomycin
|
plasma mem fxn without entering the cyto
|
|
daptomycin
tx |
G+
MRSA VRSA VR enterococci |
|
topical polypeptide Ab
|
polymyxin B
|
|
polymyxin B
mech |
phospholipid component of cell wall to disrupt integrity
--leakage of cyto G- |
|
polymyxin B
tx |
most G- bacilli
(except proteus) |
|
nonabsorbed Ab for traveler's diarrhea
|
rifaximin
trav diarrhea non-invasive E. coli |
|
rifaximin
mech |
inhibits bact RNA synthesis by inhibiting DNA-dependent RNA polymerase
|
|
cause cough, dyspnea, pulmonary infiltrates, neutropenia, paresthesia
|
nitrofurantoin
used to tx UTI GI effects are MC |
|
crystalluria is most likely to occur after __ with inadequate fluid intake
|
sulfamethoxazole
|
|
obligate aerobes
thrive in oxygen rich tissue (lung) intracellular (macrophage) |
mycobacterial infections
|
|
T / F
mycobacterium are hydophobic with high lipid content in cell wall |
true
mycolic acid |
|
mycobacterial infections
|
TB:
M. tuberculosis atypical: M. kansasii M. avium (MAC) leprosy: M. leprae |
|
1st line TB drugs
|
isoniazid (or fluoroquinolone)
ethambutol pyrazinamide rifampin (or fluoroquinolone) |
|
2nd line TB drugs
|
rifabutin
fluoroquinolones cycloserine capreomycin ethionamide aminosalicylic acid |
|
Isoniazid
inhibits __ |
inhibits mycolic acid syn
|
|
Isoniazid
resistance d/t __ deletion |
katG deletion (no catalase)
|
|
Isoniazid
side effects |
hepatitis
peripheral neuritis hemolysis in G6PD def |
|
Rifampin
inhibits __ |
DNA-dep RNA pol
|
|
Rifampin
resistance d/t __ |
decreased affinity of enzyme for drug
|
|
Rifampin
side effects |
hepatitis
flu-like induction of P450 red-orange discoloration of fluids |
|
ethambutol
inhibits __ |
arebinosyl transferase
|
|
ethambutol
side effects |
vision abnormalities
|
|
pyrazinamide
mech |
disrupts mem energetics and transport fxn
|
|
pyrazinamide
side effects |
hepatitis
myalgia rash hyperuricemia phototox |
|
tx
M. tuberculosis |
isoniazid
+ rifampin + pyrazinamide + ethambutol |
|
M. avium-intracellular
prophylaxis tx |
prophylaxis:
azithromycin tx: azithromycin + ethambutol + rifabutin |
|
M. leprae
tuberculoid lepromatous |
tuberculoid:
dapsone + rifampin lepromatous: dapsone + rifampin + clofazimine |