Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
186 Cards in this Set
- Front
- Back
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 |