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219 Cards in this Set

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blocks cell wall synthesis by inhibition of peptidoglycan cross-linking
penicillin
ampicillin
tiracillin
piperacillin
imipenem
aztrenam
cephalosporins
block peptidoglycan synthesis
bacitracin, vancomycin, cycloserine
disrupt bacterial/fungal cell membranes
polymyxins
block nucleotide synthesis
sulfonamides, trimethoprim
block fungal cell memebranes
amphotericin B
nystatin
fluconazole/azoles
block nuecliotide synthesis
sulfonamides, trimethoprim
block DNA topoisomerases
quinolones
red orange body fluids
Rifampin
Block Protein synthesis at 50S ribosomal subunit
chlorophenicol, erythromycin/macrolides, lincomycin, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid
block protein synthesis at 30S ribosomal subunit
Aminoglycosides , tetracylins
bactericidal antibiotics
penicillin, cephalosporins, vancomycin, aminoglycosides, floroquines, metronidazole
penicillin G
IV form of penicillin
penicillin V
oral form of penicillin
MOA of penicillin
1. bind penicillin binding protein (aka tranpepsidase)
2. block transpepsidase cross-lining of cell wall
3. activate autolytic enzymes

(works on dividing bacteria)
clinical use of penicillin?
bactericidal
for gram-positive cocci/rods
gram-negative cocci
spirochetes
is penicillin penicillinase resistant?
no
toxisity of penicillin
hypersensitivity reactions, drug-induced coombs positive-hemolytic anemia
how do gram negative bacteria protect themselves from penicillin?
1.prvent peniciiln from penetrating cell layers by altering porins
2. beta-lactase enzyme
3.alter molecular structure of transpepsidase so beta-lactam antibiotic (penicillin) no bind to it
example of a bacteria that uses: altered molecular structure of transpepsidase so beta-lactam antibiotic (penicillin) no bind to it
MRSA
how do gram positive bacteria protect themselves from penicillin?
1. secrete beta-lactamase = penicillinase(S aureus) and try to intercept antibiotic outside the cell wall
name the penicillinase resistant penicillin?
methicillin, nafcillin,dicloxacillin
clinical use of penicillinase resistant penicillin?why such narrow spectrum?
s. Aureus - but not MRSA
B/C HAVE BULKIER r GROUP
TOXICITY of penicillinase resistant penicillin
HYPERSENSITIVITY reactions
which penicillinase resistant penicillin causes intersitial nephritis?
methicillin
aminopenicillins - names?
ampicillin, amoxicillin
MOA of aminopenicillins diff than penicillins?
wider specturm b/c better penitration through gram negative outer membrane and better binding to transpepsidase
are aminopenicillins penicillinase sensitive?
yes
clinical use of aminopenicillins?
extended-spectrum penicillin
gram-poitive and gram neg rods(H.influenza,E coli,listeria monocytes, proteus mirabilis, salmoella, enterococci

note: they are one of few drugs against gram-positive enterococcus
toxicity of aminopenicillins?
hypersensitivity reactions
ampicillin rash
psuedomembranous colitis
anti-pseudomonals?
ticarcillin, carbeicillin, pipercillin
diff in MOA of anti-pseudomonals and penicillin?
nothing but extensed spectrum
clinical use of anti-pseudomonals?
psudomonas spp. and gram negative rods
anerobes (bacteroides fragalis)
are anti-pseudomonals susceptible to penillinase? what can use to help with?
yes
give wiht clavulanic acid - which is a beta-lactamase inhibitor
toxicity of anti-pseudomonals?
hypersensitivity reactions
B lactamdrugs that inhibit cel wall synthesis but are less susceptible to penicilinase. and a bactericidal
cephalosprins
what are the first generation cephalosporins?
cefazolin, cephalexin

cef with lin xin
clinical use of 1st generation cephalosporins?
gram positive cocci, proteus mirabilis, ecoil, klebsiella pneumoniae

pek
what are the 2nd generation cephalosporins?
cefoxitin, cefaclor,cefuroxime

furry fox is fat
clinical use of 2nd generation cephalosporins?
gram positive cocci
h. influenza, enterobacter aerogenes, neiseseria spp,
proteus mirabilis, ecoil, klebsiella pneumoniae


hen peks
what are the 3rd generation cephalosporins?
cetriaxone, cefotaxime, ceftazidime
clinical use of 3rd generation cephalosporins?
serious gram negative infections resistant to oteher B lactams
meningitis (most penetrate BBB)
ceftazidime used for what?
pseudomonas
ceftriaxone used for what?
gonorrhea
what are 4th generation cephs?
cefepime and cefpiramide

pime mide
clinical use of 4th generation cephalosporins?
increased activity against pseudomonas and gram positive organisms
toxicities of all cephs?
hypersensitivity reactions
cross hypersensitivity wiht penicillins
increased nephro tox of aminoglycosides
disuliram like reaciton w/ ethanol
what is aztreonam?
a monobactam resistan to Beta lactamase
what is the mOA of aztreonam?
inhibits cell wall synthesis ( binds to PBP3) synergistic with aminoglycosides
no cross-allergy with penicillin
what is the clinical use of aztreonam?
gram negative rods
klebiella spp,pseudomonas spp, serratia spp

NO activity against gram positive gram positives or anerobes
toxicity of aztreonam?
usually nontoxic, occasional GI upset
what drugs avoid during preg?
SAFE Moms Take Really Good Care
Sulfonamides
Aminoglycosides
Fluoroquinolone
Erythromycin
Metronidazole
Tetracyclins
Ribavirin
Griseoulvin
Chloamphenicol
what birth defect sulfonamides cause?
kernicterus
what birth defect aminoglycosides cause?
ototoxicity
what birth defect Fluoroquinolones cause?
Cartilage damage
what birth defect erthyromycin cause?
acute cholestatic hepatitis in mom
what birth defect clarithromycin cause?
embryotoxic
what birth defect metronidazole cause?
mutagenesis
what birth defect tetracylines cause?
discolored teeth, inhibition of bone growth
what birth defect ribavirin cause?
teratogenic
what birth defect griseofulvin cause?
teratogenic
what birth defect choloramphenicol cause?
gray baby
treat onchoceriasis
Ivermectin (rIVER blindness treated wiht IVERmectin)
treat nemaode/ roundworm (pinworm,whipform infections
mebendazole/thiabendazole
used to treat
giant worm - ascaris
Hookworm-nectar/ancylostoma
pinworm-enterobius
pyrantel pamoate
used to treat
trematode/fluke- schistosomes,paragonimus,clonochis
and
cyticercosis
praziquantel
treat cestode/tapeworm-diphyllobothrium latum,taenia
x-cept cysticercosis
Niclosamine
RX leishmaniasis
pentavalent antimony
Rx Malaria
Chloroquine,quinine,meloquine,atovaquone,proguanil
Rx Latent hypnozoite(liver) forms of malaria(P.vivax, P.Ovale)
primaquine
RX giardiasis
amebic dysentry(e. histolytica), bacterial vaginitis (gardnerella vavginalis, Trichomonas
Metronidazole
RX pneumocystis carnii pneumonia prophylaxis
TMP-SMX, pentamindine
RX chagas disease, american typanosomiasis (T. cruzi)
Nifurtimox
RX African trypanocomiasis (sleeping sickness)
Suramin
what is imipenem/cilastratin. meropenem?
broad spectrum , B lactamase resistant carbenem-always administered with cilastatin
what is cilastatin and why is it administered with imipenem?
it is a renal dihydropeptidase inhibitor to decease the inactivation of renal tubules
clinical use of imipenem/cilastatin, meropenem
gram poitive cocci, gram negative rods, and anerobes
enterobactor- drug of choice
drug of choice for enteobacter ?
imipenem/cilastatin, meropenem
what is tox of imipenem/cilastatin, meropenem?
GI distress , skin rash, CNS tox(seizures)@ high plasma levels
what drung inhibits cell wall mucopeptide formation by binding D-ala D ala of cell wall precursors.
vancomycin
how does vancomycin resistance occur?
D-ALA D-ALA TO D-ALA D-LAC
is vacomycin bactericidal or static?
bactericidal
what is the clinical use of vancomycin?
gram positive multidrug resistant organisms includ S. aureus and C. difficile
what causes nephrotox, ototox, thrombophlebitis and diffuse flusing
vancomycin
what causes red man syndrome
vancomycin
how prevent red man syndrom
pretraeat with antihistamines and slow inusion rate
30 s inhibitors
AT 30

Aminoglycosides - bacteriocidal
Tetracyclines - bacteristatic
50 s inhibitors
cell at 50
Chloamphenicol
erythromycin
lincomycin
cLindamycin

all bacterio static
examples of aminoglycosides
streptomycin, gentamycin,
tobramycin, amikacin
they are bactericidal
inhibit ormaltion of initiation complex and cause misrading of mrna
require o2 for uptake
therfore ineffective angainst anaerobes
aminoglycosides
severe gram negative infections
synergistic with B -lactam antibiotics
aminoglycosides
used for bowel surgery
neomycin
cause neph tox-es used wiht cephalosporins
ototox -espec with loop diuretics
teratogen
aminoglycosides
B lactamase clevage of B lactam ring
resistance against what?
penicillins/cepalosporins
Modification via acetylation, adenylation, or phosporylation
resistance against what
aminoglycosides
terminal D alla of cell wall component with D LAC decreased affinity of drug
resistance against what
vancomcin
mod via acetylaion
resistance against what
choloramphenicol
aminoglycosides
methylation of rRNA near erythromycin's ribosome-binding site
resistance against what
macrolides
increased transport out of cell
resistance against what
tetracyclin
altered enzyme (bacterial dihydropteroate synthetase) or resistance against what
sulfonamides
increased paba synthesis
sulfonamides
decreased uptake
tetracyclin and sulfonamides
antimirobial prophylaxis
meningococcal
riampin(drug o choice)
minocyclin
antimirobial prophylaxis
gonorrhea
ceftriaxone
antimirobial prophylaxis
syphillis
Benzathine penicillin G
antimirobial prophylaxis
history recurrent UTI's
TMP-SMX
antimirobial prophylaxis
pneumocytis carinii pneumonia
TMP-SMX (drug of choice)
aerosolized pentamidine
antimirobial prophylaxis
endocarditis with surgical or dental procedures
penicillins
inhibits cell wall synthesis
used for fungus
caspofungin
clinical use invasive aspergillos
caspofugin
GI upset and flushing
caspofugin
inhibits fungal enzyme squalene epoxidase
terbinafine
used to treat dermatophytoses
escecially onychomycosis
terbinafine
inhibits DNA synthesis by conversion to luorouracil, which completes wiht uracil
flucytosine
used in systemic fungal infections (candida, cryptococcus)
flucytosine
causes nausea, vomiting, diarrhea, bone marrow suppression
flucytosine
interferes wiht micotubule funtion, disrupts mitosis
griseofulvin
deposits in keratin-containing tissues (nails)
griseofulvin
used for oral treatmetn of superficial infections
griseofulvin
inhibits growth of dermatophytes (tinea and ringworm)
griseofulvin
is a teratogenic, carcinogenic, causes confusion, headaches, increased p-450 and warfarin metabolism
griseofulvin
binds to ergosterol
disrupting ungal membranes
too toxic for systemic use
nystatin
forms membrane pores that allow leakage of electrolyrtes and distrupts homeostatis
bind ergosterol
amphotericin B
causes fever/chills (shake and bake) , hypotention, neph tox, arrythmias, anemia, IV phlebiis (amphoterrible)
hydration reduces nephrotox
amphotericin B
used for wide specturm of systemic mycosis
cryptococcus, blastomyces, coccidiodies, aspergillus, histoplasma, candida, mucor(systemic mycoses)
intathecally for fungal memingitis, no cross BBB
amphotericin B
swish and swallow or oral candidiasis(thrush)
topical or diaper rash or vaginal candidiasis
nystatin
inhibit fungal steroid ergosterol synthesis
fluconazol, kepconazole, clotrimazole, itaconazole, voricconazole
systemic mycosis
fluconazol, kepconazole, clotrimazole, itaconazole, voricconazole
used ofr cytptococcial meningitis in AIDS patinets and candidal infections of all types -yeast infections
fluconazol
blastomyces, coccidiodies, histoplasma, candida albicans ,
ketoconazole,
hormone inhibition (gynecomastia), liver disfunciton (inhibit cytochrome p-450) fever and chills
fluconazol, kepconazole, clotrimazole, itaconazole, voricconazole
inhibits bacterial dihydrofolate reductase
bacteriostatic
trimethoprim
causes megaloblastic anemia, leukopenia, granulocytopenia
(may alleviate wiht supplimental folinic acid)
trimethoprim
used in combination wiht sulfonamides (TMP-SMX) causeing sequential block o folate sntheiss
-combo used in for what organisms?
trimethoprim
used or UTI'S shegella, salmoella, pneumocystis carinii pneumonia
What are the Macrolides:
Erythromycin, azithromycin, clarithromycin
Inhibit protein synthesis by blocking translocation, bind to the 23S rRNA of the 50S ribosomal subunit, bacteriostatic
Macrolides
Clinical use of macrolides
URIs, pneumonias, STDs-- gram positive cocci (streptococcal infections in patients allegic to penicillin), Mycoplasma, Legionella, Chlamydia, Neisseria
GI discomfort (most common cause of noncompliance), acute cholestatic hepatitis, eosinophilia, skin rashes.
Macrolides toxicity
Increases serum concentration of theophyllines, oral anticoagulants
Macrolides toxicity
Chloamphenicol mechanism
Inhibits 50S peptidyltransferase, bacteriostatic
Meningitis (Haemophilus influenzae,Neisseria meningitidis, Streptococcus pneumoniae
clinical use of chlorophenicol
tox chloroamphenicol
anemia(doe dependent), aplastic anemia(does independnet), gray abby syndrome (in premature infants b/c they lack liver udp-glycuronyl transferase
clocks peptide bond formation at 50s ribosomal subunit . bacteriostatic
clindamycin
treats anaerobes above the diaphram
clindamycin
treat anaerobic infections (Bacteroides fragalis, clostridium perfringens)
clindamycin
pseudomembranous colitis (C. difficile overgrowth. fever , diarrhea
clindamycin
types of sulfonamides
sulfamethoxazole (SMX) sulfisoxazole, triple sulfas, sulfadiazine
PABA antimetabolites inhibit dihydropteroate synthase. bacteriostatic
sulfonamides MOA
clinical use of sulfonamides
gram-positive, gram-negative, Nocaria, Chlamydia. Triple sulfas or SMX for simple UTI
Hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity (tubulointerstitial nephritis)
Sulfonamides
kernicterus in infacnts
Sulfonamides
displace other drugs from albumin (e.g. warfarin)
Sulfonamides
What are the fluoroquinolones
ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin, nalidixic acid (a quinolone)
inhibit DNA gyrase (topoisomerase II), bacericidal
fluoroquinolones' mechanism
clinical use of fluoroquinolones
gram-negative rods or urinary and GI tracts (including Pesudonomas), Neisseria, some gram-positive organisms
GI upset, superinfections, skin rashes, headache, dizziness.
fluoroquinolones tox
Contradicted in pregnant women and children because animal studies show damage to cartilage.
fluoroquinolones tox
Tendonitis and tendon rupture in adults, leg cramps and myalgias in kids.
fluoroquinolones tox
Metronidazole mechanism
forms metabolites in the bacterial cell, bactericidal
Antiprotozoal
Metronidazole clinical use
Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, anaerobes (bacteriodes, clostridium)
Metronidazole clinical use
used with bismuth and amoxicillim (or tetracycline) for "triple therapy" against H. pylori
Metronidazole clinical use
polymixin B and polymixin E are examples of what?
polymixins!duh
bind to cell membranes of bacteria and distrupt their osmotic properties
care cationic
basic
act like detergents
polymixins
-myxins mix up membranes
resistant to grm negative infections
polymixins
neurotox, acute renal tubular necrosis
polymixins
streptomycin
pyrazinamide
isoniazid(INH)
rifampin
ethambutol
cycloserine (2nd line therapy)
ANTI-TB DRUGS
tb prophylazxis?
INH isoniazid
deacerased synthesis of mycolic acid
isoniazid
hemolysis if G6PD deficincy , enurotox, hepatotox, SLE ,
INH
what can prevent neurotox in INH
pyridoxine vit b6
common tox to all anti-tb drugs
all hepatotoxic
inhibits DNA- dependent RNA polymerase
Rifampin
used against TB delays reasistance to dapsone when used for leprosy
used for meningococcal prophylaxis in contacts of childeren with H. influenza type B
Rifampin
causes minor heptotox and drug interaction (increased P 450)
Rifampin
inhibits influenza neuroaminidase. so release of progeny virus is decreased
Zanamivir, oseltamivir
influeza A and B
Zanamivir, oseltamivir
inhibits synthesos o guanine nucleotides by competivitly inhibiting IMP dehydrogenase
Ribavirin MOA
RSV, chronic hepatitis C
Clinical use of ribavirin
hemolytic anemia, sever teratogen
ribavirin
preferentially inhibits viral DNA polymerase when phosphorylates by viral thymidine kinase
acyclovir
HSV,VZV,EBV,mucocutaneous and genital herpes lesions. prophylaxis in immunocompromised patients
acyclovir
delirium, tremor, nephrotox
acyclovir
lack of thymidine kinase
acyclovir
phosphorylation by viral kinas preferentially inhibits CMV DNA polymerase
Ganciclovir
CMV , esecially in immunocompromised patients
Ganciclovir
leukopenia, neutropenia, thrombocytopenia, renal tox. MOre tox to host enzymes than acyclovir
Ganciclovir
Mutated CMV DNA polymerase or lack of thymidine kinase
Ganciclovir
blocks viral penetration/uncoating(M2 protein) may buffer pH o endosome. also caus the release of dopamine rom intact nerve terminals
Amantadine
prophylaxis and treatmetn for influenza A; parkinson's disease
Clinical use of amantadine
ataxia, dizziness, slurred speech
tox of amantadine
Mutated M2 protein. In 2006 , 90% of influenza A were resistant to amantadine
amantadine
is a derivative with fewer Cns side effects . does not cross the BBB
rimantidine
Viral DNA polymerase inhibitor that binds to the pyroposphate binding site o the enzyme . does not require activatiation by viral kinase
foscarnet
nephrotox
foscarnet tox
mutated DNA Polymerase
mechanism of resistance of foscarnet
glycoproteins from human leukocytes that block various various stages of RNA and DNA syntheiss. Induce ribonuclease that degrades viral mRNA
Intererons
pyrofosphate analog
foscarnet
IFN alpha used for what
chronic hep B and C
KAPOSi's sarcoma
IFN b
MS
IFN gamma
NADPH, OXIDASE DEFICIENCY
NEUTROPENIA
tox or interferone
plioconanl
for poliovirus inhibits penetration of picornavirus into cell
saquinavir , ritonavir , indinavir nelfinacir amprenavir used for what?are what>
HIV THERAPY
are protease inhibitors

NAVIR tease a pro-tease inhibitor
what inhibits assembly of new virus by blocking protease in progency virons
protease inhibitors for HIV therapy
saquinavir , ritonavir , indinavir nelfinacir amprenavir
cause GI intolerance (N, dia), hyperglycemia, lipodystrophy, thrombocytopenia(indinavir)
HIV therapy
ZIDOVUDINE(AZT), didanosine (ddI), zalcitabine(ddC), stavudine(d4T), lamivudine(3TC),abacavir
nucleosides - reverse transcriptase inhibitores for HIV
nin nucleoside reverse transcriptase inhibitors for HIV
Nevirapine, efavirenz,delavirdine
prefeentially inhibit reverse transcriptase of HIV, incorporation of viral genome into ost DNA
reverse transcriptase inhibitors both types
cause bone marrow suppression (neutropenia and anemia), peripheral neuropathy, lactic ascisoiss(neucleosides) rash (non-nucleaosides), megaloblastic anemia(AZT)
TOX of reverse transcriptase inhibitors both types
highly active antiretroviral therapy
HAART
what is HAART
combo therapy o protease inhibitos reverse transcriptase inhibitors
at what cell count is HAART INDICATED
<500cells/mm3 of CD4, or high viral load
is AZT USED during preg why?
yes - to reduce risk o etal transmission
Clinical use of tetracyclines:
Vibrio cholerae, Acne, Chlamydia, Ureaplasma, Urealyticum, Mycoplasma pneumoniae, Tularemia, H. pylori, Borrelia burgdorferi (Lyme Disease), Rickettsia

Vaccum the Bedroom
GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity, contradiction in pregnancy
Tetracycline toxicity
Tetracyclines
Bacteriostatic, bind to 30S and prevent attachment of aminoacyl-tRNA, limited to CNS penetration
This is fecally eliminated and can be used in patients with renal failure
Doxycycline

(must not take with milk, antacids, or iron-containtaing preparations because divalent cations inhibit its absorbtion in the gut)
What are the tetracyclines?
Tetracyclines, doxycycline, demeclocycline, minocycline
block mRNA synthesis
rifampin