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186 Cards in this Set

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bacterial cell wall synth. inhibitors (6)
pencillins, cephalos, imipinem/meropenem, aztreonam, vanco
bacterial protein synth. inhibitors (6)
aminos, chloramphenicol, macrolides, tetras, streptogramins, linezolid
nucleic synth. inhibitors (2)
fluoroquinolones, rifampin
folic acid synth. inhibitors (3)
sulfonamides, trimethoprim, pyrimethamine
moa penicillins/cephalosporins
interact w/ penicillin binding proteins in cytoplasm and inhibit transpeptidation reactions that cause X-LINKING
m.o. resistance for pens and cephalos?
-beta lactamase production
- pbp change
- porin changes
what bugs change their pbp structure?
what bug changes its porin channel?
staph aureus, pneumococci
- pseudomonas
spectrum of Pen-G / V?
-narrow spectrum
- SENStive to Beta-lactamase
Pen-G = doc in syphilis
- strepto, pneumo,meningococci
what is pen-V mainly used for?
only oral admin
- streptococci
- oral pathogens and dental infections
moa of "STAPHICILLIN?" (group of pens)
nafcillin, methicillin, oxacillin
- good against STAPH (not mrsa)
spectrum of aminopenicillins?
-broader spectrum
- beta-lactam senstive
- g+ cocci (not staph)
- e.coli, h.flu, listeria, borellia, h.pylori
which would u use ampicillin for?
listeria
what 2 specific bugs r reactive to amoxicillin?
- borrelia burg
- h.pylori
how is aminopenicillin activity enhanced?
-use in COMBINATION w/ beta-lactamase inhibitors --> clavulanic acid , sulbactam
clavulanic acid and sulbactam act as what for the penicillins?
bodyguards by protecting them against bacterial derived b-lactamase
how is ampicillin given?
oral / iv
aminopenicillins (ampicillin/amox) are synergistic with what other drug group against enterococci?
synergistic w/ AMINOS
these pencillins are the 4th variety of penicillins and are often called " antipseudomonal penicillins?"
ticarcillin, piperacillin
- extended spectrum, antipseudomonal, b-lactamase sensitive
ticarcillin/piperacillin activity against?
enhanced activity against G- RODS (pseudomonas)
- enhanced if used w/ b-lactamase inhibitors
- synergistic w/ aminos against pseudomonas
majority of pens are eliminated how?
renal elimination
- short half life of less than an hour
- dose reduction need in Rnl dysfunction
these 2 pens largely eliminated in bile
- nafcillin
- oxacillin
pen that undergoes enterohepatic cycling, but eventually excreted by kidney
ampicillin ; most likely to cause GI trouble
main side fx associated w/ pens?
hypersensitivities
- urticarial skin rash common
- anaphylaxis is possible
interstitial nephritis is seen w/ which pen?
methicillin
cephalosporins...moa?
same as pens--> interact w/ cytoplasmic PBP'S and inhibit transpeptidation reactions, thereby inhibiting cell wall synth
m.o. of resistance to cephalos?
- b-lactam production
- pbp change
- porin change
name the 2 main 1st generation cephalosporin drugs
-cefazolin
- cephalexin
spectrum of generation 1 cephs?
g+ cocci (not mrsa)
- e.coli, klebs and proteus
--> P.E.K. + G(+) bugs
main use for first gen cephs?
surgical prophylaxis b/c main infections in surgical wounds r caused by --> g+ strep/staph y g(-) e.coli
cns entry of 1st gen cephalos?
no cns entry
name 3, 2nd gen. ceph drugs
-cefotetan
-cefaclor
-cefuroxime
spectrum of 2nd gen?
increased g- coverage y partial anaerobic coverage
name of the only 2nd gen cephlo to enter cns?
cefuroxime
mnemonic for coverage of 2nd gen cephalos?
H-PEK
name 4, 3rd gen cephalos?
-ceftriaxone (im)
- cefotaxime (parenteral)
- cefdinir (oral)
- cefixime (oral)
spectrum of 3rd gen cephalos?
G+/G- COCCI
- many G- rods
cns entry?
all enter cns
what are 3rd gen cephs important for? (ceftriaxone, cefotaxime, cefdinir, cefixime)
- empiric rx of mengitis and sepsis
name the 1, 4th generation cephalosporin?
- cefepime (IV)
- not used much b/c held in reserve as a backup in case others fail
spectrum of cefepime IV?
wider spectrum
- resistant to most b-lactamases
- CNS entry :)
active tubular secretion of cephalos, and drug half lives are increased by using what drug in the kidney?
- probenicid prevents active tubular secretion of cephalos
which 2 drugs r eliminated in the BILE?
cefoperzone
- CEFTRIAXONE (largely eliminated in bile)
side fx of cephalos?
- hypersensitivities (2%)
- rashes most common
- assume x-allergenicity if allergic to pens
if patients are allergic to pen's and cephalos, which drugs can they consider?
G+ bug --> macrolides
G- bug --> aztreonam
which 3 antibiotics of cephalos do u want to AVOID drinking alcohol, due to the disulfiram fx?
- cefotetan
-cefoperazone
- cefamandole
*All 3 inhibit alcohol dehydrogenase and cause a build up acetaldehyde in the blood/body
These bugs make Cephalosporins, LAME!
LAME
L- listeria
A- atypicals (chalmydia/myco)
M- MRSA
E- enteroCOCCI
Imipinem and Meropenem moa?
same as pens
- gi distress
- imipenem = seizures w/ renal dysfunction
where are imipenem and meropenem used?
mainly used in hospitals b/c only given via IV
- empiric use for life threatening infections
imipenem / meropenem spectrum of action?
gram (+) cocci, gram (-) rods (enterobacter / pseudomonas) + anaerobes
imipinem is given w/ which drug to inhibit its metabolism?
imipenem is given with CILASTATIN to decrease its metabolism via RENAL DYHYDROPEPTIDASE
moa of Aztreonam?
-same as pens
- resistant to b-lactamases
uses of aztreonam?
- mainly GRAM (-) RODS IV
is Aztreonam x-allergenic with pens / cephs?
there is no x-allergenicity w/ aztreonam
moa of Vancomycin?
binds @ d-ala+d-ala muramyl pentapeptide and sterically hinders the transglycosylation reactions that are involved in the elongation of the peptidoglycan chains
- DO NOT INTERFERE W/ PBP's
vancomycin spectrum?
MRSA
Enterococci g+
c.dif (backup drug)
resistance to vanco occurs via?
change in muramyl peptide target; d-ala changes to d-lactate (terminal one)
in colitis how is vanco used? does it penetrate the cns?
IV b/c of low absorption in that condition
- no cns penetration
- penetrates tissues well, and can penetrate bone --> osteomyelitis use
elimination of vanco? length of half life?
- renally eliminated
- long half life
main side fx of vanco?
-red man syndrome due to histamine release (decrease rate of iv admin to lower red manism)
- permanent ototoxicity
- nephrotoxic
2 drug classes that bind to 30S
- tetras
- aminos
7 drug classes that bind to the 50S ribosome?
-linezolid
- dalfo/quinupristin
- chloramphenicol
- macrolides
- clindamycin
these drugs prevent the formation of the initiation complex...
aminoglycosides (30s)
linezolid (50s)
aminos cause what to happen to the protein synth?
aminos cause misreading of the genetic code and thus prevent proper protein formation...also incorporation of wrong amino acids in the chain --> CIDAL fx
this drug inhibits the activity of the bacterial peptidyl transferase?
chloramphenicol
these drugs prevent / block the attachment of aminoacyl TRNA to the acceptor site ...?
tetras (30s)
- dalfo/quinupristin (50s)
these drugs work on the 50S subunit; inhibit the translocation of PEPTIDYL TRNA from the ACCEPTOR to the DONOR site (static)
macrolides and clindamycin
y do aminos only work on aerobic bugs?
aminos need O2 to enter the cell of the bacteria b/c the uptake mechanism in the bacteria uses o2
--> thus causing an intrinsic resistance of ANAEROBIC bacteria
spectrum of aminos?
G- rods
3 main aminos ?
GENTAMYCIN , TOBRAMYCIN, amikacin
- used in combo
aminos + penG / ampicillin for which bugs?
enterococci
Aminos + extended spectrum penicillin or 3rd gen ceph (ceftriaxone,cefdinir, cefotaxime, cefixime) for which bug?
pseudomonas aeruginosa
streptomycin is used in which bugs?
TB
- doc --> bubonic plague and tularemia
y is neomycin only used topically?
b/c its too toxic systemically
what main aminoglycoside is used to treat gonorrhea?
SPECTINOMYCIN
y are aminos not absorbed orally or widely distributed into the tissues?
b/c aminos are POLAR COMPOUNDS
RENAl elimination is proprotional to what?
renal elimination of aminos is proportional to GFR
- need major dose reduction in renal dysfunctional states
what is the only class of abx that can be administered with ONCE DAILY DOSING?
AMINOS
- fx depend on peak drug level, and it has POST-ANTIBIOTIC FX --> bug killing continues long after it reaches below toxic levels in the blood
- "hit and run" fx
main side fx of aminos?
nephrotoxicity , acute tubular necrosis that is reversible
- potentiated via use of --> vanco, ampB, cisplat and cyclosporin
this side fx of aminos occurs roughly 2% of the time
ototoxicity , aminos are toxic to the hair cells in the ear
- irreversible deafness
- reversible vestibular dysfunction
- toxicity enhnaced by LOOP use
side fx of neomycin?
contact dermatitis
moa of tetras ?
bind to 30S subunit
- block association of aminoacyl trna to the acceptor site
spectrum of tetras?
broad spectrum
- good chlamydia/mycoplasma activity
- h.pylori
- rickets, borrelia, brucella and vibrio
what conditions are tetras used prophylactically for?
- acne
- chronic bronchitis in winter time for susceptible age groups
tetras are the doc for which bugs?
lyme disease
- cholera
name the 3 main drugs for class of tetracyclines?
- doxycycline
- minocycline
- demeclocycline
which 3 classes of drugs cause phototoxicity?
- tetras
- sulfonamides
- quinolones
tetras are the backup drug for which bug?
syphilis
- backup drug to pen-G
this drug is better than tetracycline hcl and can b used in prostatitis
-doxycycline
- reaches high levels in the prostatic fluid
- metabolized in the liver
this drug has high levels in the saliva and tears, and often used as prophylaxis for a patient who has the meningococcal carrier state?
minocycline
this tetracycline is used in the rx of SIADH due to its blockage of the ADH receptor in the collecting ducts?
demeclocycline
majority of tetras are eliminated how?
renally
doxy is eliminated through which organ?
liver
y cant u use chelators when giving tetras?
tetras bind to DIVALENT CATIONS (ca2+, Mg2+, Fe2+) --> causes decreased absorption
- also cannot use antacids during tetra rx
this drug is similar to tetras, is not affected by efflux pumps of bacteria, is a broad spectrum drug and is indicated for VANCOMYCIN RESISTANT organisms?
Tigecycline
y cant we use tetras in children?
- tetras decreases bone growth in kids
- tooth enamel dysplasia --> teeth turn gray/brown
these 2 tetras cause phototoxicity?
demeclo, doxy
these drugs can cause n,v,d and superinfections leading to which conditions in the upper and lower gi tracts?
- upper gi --> candidiasis superinfection
- lower gi --> staph aureus colitis
this tetra can rarely cause dizziness
minocycline
at high doses tetras cause what?
liver dysfunction in pregnancy
CONTRAINDICATED IN PREGNANT WOMEN
what is the clinical triad for Fanconi syndrome?
polyuria
polydypsia
low back pain
- caused by outdated tetras
chloramphenicol? moa?
works on the 50S ribosomal subunit... inhibits the activity of peptidyltransferase
- bacterioSTATIC
- basically prevents the making of a new peptide bond
is chloramphenicol a doc for any diseases?
nope
this drug is a backup drug for salmonella, b.fragile, rickettsia
chloramphenicol
tissue distribution of chloramph?
good, csf penetrance as well
how is chloramphenicol metabolized?
hepatic glucoronidation ; need dose reductions for liver dysfunction in neonates
how is gray baby caused?
neonates dont have enough glucoronosyl transferase
does chloramphenicol induce or inhbiit p450?
chloramphenicol INHIBITS P450
side fx of chloramp?
- dose dependent bone marrow suppression
- aplastic anemia (1/35k)
- gray baby syndrome
moa of macrolides?
inhibition of TRANSLOCATION of PEPTIDYl tRNA from acceptor site to the donor site
- 50S
3 examples of macrolides
erythromycin, azithromycin, clarithromycin
erythromycin is commonly used for ?
middle ear infections --> m.cat / H.flu
- strep/staph
- atypical bugs (chlam,mycoplsma, ureaplasma)
- legionella
- camp.jejuni
what type of pneumonia is macrolides a common use for?
community acquired pneumonia
- m.pneumoniae
- c.pneumoniae
- no action against viruses (other common cause of community acquired pneumonia)
what 2 macrolides are metabolized by liver and excreted in the poo? (bile)
- p450 fx?
erytho/clarithromycin
- INHIBIT P450
are erythro/clarithro safe in pregnancy?
NOOOO
how is azithromycin better than erythro/clarithromycin?
- azithro is renally eliminated
- NO p450 actions
- SAFE IN KIDS AND PREGNANT WOMEN
what abx stimulate the motilin receptors and commonly cause g.i. distress?
macrolides
- erythro/azithro > clarithro
at high doses, what do macrolides do?
cause reversible deafness @ high doses
what drug works on macrolide resistant bacteria?
Telithromycin
what form of erythromycin is quickly absorbed, and causes cholestasis / jaundice in pregnancy and in the elderly?
erithromycin estolate
- elderly > 60 yoa
What type of drug is Clindamycin?
clindamycin is a LINCOSAMIDE
- inhibits translocation peptidyl tRNA from acceptor to the donor site on the 50S ribosomal subunit of the freaking bug
spectrum for clindamycin?
narrowwwww
- g+ cocci and anaerobes
- backup drug to b.fragilis
- can b used in toxo
this drug is the first known abx to cause what g.i. disease?
pseudomembranous colitis
why does clindamycin work in osteomyelitis ?
clinda has good bone penetration
- good for G+ cocci
name the 6 abx drugs that u dont want to use in a pregnant woman?
1.) aminos
2.) erythromycin estolate
3.) clarithromycin
4.) fluoroquinolones
5.) sulfonamides
6.) tetras
THIS drug prevents the formation of the initation complex in bacteria via the PREVENTION of N-FORMYLMETHIONYL- tRNA- ribosome -mRNA ternary complex?
Linezolid prevents the formation of the ternary complex :)
spectrum of action of linezolid?
used in VRSA, VRE and drug-RESISTANT Pneumococci
- basically, its used in bugs that are vancomycin resistant :(
side fx of linezolid?
bone marrow suppression
- observe via a depression in platelet levels
These 2 drugs act via --> a.) binds to 50 S ribosomal subunit and trna acceptor site and stimulates its dissociation from the ternary complex --> b.) dcreses the release of the completed polypeptide via blockage of its extrusion?
Quinupristin / Dalfopristin
spectrum of dalfo/quinupristin?
used PARENTERALLY in SEVERE infections caused -->
VRSA, VRE and other G+ cocci
what is... a substance that inhibits cell growth via competition or substitution of a natural substrate in an enzymatic process?
antimetabolite
these 2 abx classes act as antimetabolites as their moa?
- sulfonamides
- trimethoprim
inhibitors of folic acid synthesis are also by association inhibitors of what ?
nucleic acid synthesis
3 examples of folic acid synth. inhibitors?
- sulfonamides
- trimethoprim
- pyrimethamine
folic acid synth is via..
pteridine + PABA --> (dihydropterate synthetase) --> dihydropteric acid + glutamate --> dihydrofolic acid --> (dihydrofolate reductase) --> tetrahydrofolic acid (active folate form)
these drugs inhibit DIHYDROPTERATE SYNTHETASE
- sulfonamides
these drugs inhibit DIHYDROFOLATE REDUCTASE
- trimethoprim and pyrimethamine (works in toxo)
why do these drugs work?
b/c some bugs have to synthesize their own folic acid in order to survive...we dont have to, we get ours from our good vegetarian diet :)
this drug is a prodrug of salicylate and is used in what 2 conditions?
-ulcerative colitis
- rheumatoid arthritis
Ag Sulfadiazine is used when?
burn patients
combination of trimethoprim- sulfamethoxazole is used bc?
inhibition of both dihydropterate synthetase and dihydrofolate reductase --> makes it much harder for a bacteria to confer resistance to abx when getting hit from 2 directions... BYAAHHHH!!!
combination of trimethoprim/sulfamethoxazole is called what?
sequential blockade of folate synthesis
tmp/smx is co-doc for which infections?
- utis
- resp/ear/sinus infections
- h.flu/m.cat
- mrsa/vibrios (DOC)
- pcp pneumonia
tmp smx is doc for which bacteria?
NOCARDIA
TMP /smx is good for which other bugs?
- nocardia
- mycobacteria
- g (-) bugs --> (e.coli, salmona,shig,h.flu --> common causes of uti's)
- g(+) bugs --> staph,strep
which fungi and protozoans are tmp/smx good for?
- fungus --> pcp
- protozoa --> toxo (sulfadiazine + pyrimehtamine)
sulfonamdies conjuated how?
- hepatically acetylated
- renally excreted (drink lots of water batch!) otherwise u get CRYSTALLURIA
how do sulfonamides cause d-d interactions?
sulfas bind to albumin, which displaces other drugs and increases their activity in the body
what common drugs can be displaced by sulfonamides?
methotrexate
- phenytoin
warfarin
what trimester do you avoid sulfonamides ?
sulfas x-the placental barrier
- 3rd trimester
- can cause kernicterus in neonates
- hard to metabolize bilirubin and bilirubin deposits in the brain causing irreversible brain damage
sidefx of sulfonamides?
2nd to pens in causing hypersensitivity rxns
- phototoxicity
- stephen johnson syndrome
trimethoprim/ pyrimethamine side fx to the bone?
bone marrow suppression due to decreased folic acid production
- enterocolitis
this class of abx are direct inhibitors of nucleic acid synth?
quinolones!
name 3 drugs of quinolone family
- norfloxacin
- ciprofloxacin
- ofloxacin
--oxacins
quinolones can also be used to treat this bug, which can also be treated with pens and tetras ?
anthrax
moa of fluoros?
inhibits topo2 and topo 4
resistance is building to fluoros b/c of what?
G(+) cocci --> via topo4 --> MRSA
G(-) rods --> topo 2
narrow or wide spectrum of action of flouros?
WIDE SPECTRUm
- utis
- stds, pid's
fluoro used for chlamydia?
ofloxacin
fluoro used for gonorrhea?
cipro/ ofloxacin
fluoros can also be used in skin, tissue infections as well as where else?
-bone infections --> used in OSTEOMYELITIS
any quinolone can be used for diarrhea caused by ?
shigella
salmonella
e.coli
campy. jejuni
levofloxacin is used for?
drug resistant pneumococci
active secretion of fluoros in the kidney can be inhibited by which medication?
probenicid
why cant u drink milk when taking fluoros?
iron and calcium inhibit absorption
what are the 4 main side fx of fluoros?
-tendonitis rupture in young adults
- QT INTERVAL PROLONGATION
- CONTRAINDICATED IN PREGNANCY :)
- no use in children due to disruption of chondrogenesis in the epiphyseal plates
these are the antibiotics for h.pylori in g.i. ulcers? BMT REGIMEN
BMT regimen
B = bismuth
M= metronidazole
T= tetracycline
or --> clarithro/amox/omeprazole
moa of METRONIDAZOLE?
unknown...
produces FREE RADICALS and is BACTERICIDAL
METRO is the DOC for which condition caused by overuse of antibiotics?
pseudomembranous colitis
Metro is DOC for these 3 PROTOZOANS!
GET!
G= giardia
E= entamoeba
T= trichomonas
metro is used for the majority of Gram (-) bacteroides and which other species?
Clostridium
metro is also used in what 2 other infections?
- g.vaginalis (overactive vagina)
- h.pylori (stomach ulcers)
side fx of metronidazole... do u take it while drinking alcohol? do u like the taste of metal?
- stomatitis, metallic taste, cystitis, glossitis
- n,drrha
-dont drink w/ alcohol due to its disulfiram fx
- reversible p.neuropathy
What Rx regiment is used for Tb?
STRIPE therapy
St= streptomycin
R= rifampin
I= isoniazid
P= pyrazinamide
E= ethambutol
what drug is used prophylactically for tb?
isoniazid...but rifampin if patient is intolerant
moa of isoniazid?
inhibits mycolic acid synthesis
- must be converted by catalase to active form
how does high level resistance form in the use of Isoniazid?
high level resistance --> deletions in the katG GENE
- encodes catalase needed for bioactivation in the bacteria
Low level resistance in INH rx?
inhA gene deletions --> encodes the acyl protein in the mycolic acid target
side fx of INH?
-hepatitis (depends on age)
-peripheral neuritis (use b6 to prvnt)
- sideroblastic anemia (b6 to prevent)
-hemolysis in g6pd
- sle in slow acetylators
Rifabutin is the preferred form of rifampin...but how does it work?
rifampin inhibits dna-dependnt rna polymerase --> inhibits nucleic acid synth
side fx of rifampin?
- syndrome of flu-like symptoms that really isnt the flu
- p450 INDUCTION
- RED/ORANGE PEE
moa of EthambutoL?
- inhibits ARABINGALACTAN synthesis
side fx of ethambutol?
retrobulbar neuritis
- dcrsed visual acuity
- red/green color discrimination changes
moa of pyrazinamide?
not known
- activated by bacteria
- strains that are resistant lack the bioactivating enzyme
sidefx of pyrazinamide?
- polyarthralgia
- hepatitis
- hyperuricemia --> increases risk of gout
- phototoxicity
- increased porphyrin synth
what condition would pyrazinamide be contraindicated in?
porphyrias
rx for MAC?
prophylaxis --> azithromycin once a week or clarithromycin daily
rx --> clarithromycin + ethambutol +/- rifabutin