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219 Cards in this Set
- Front
- Back
blocks cell wall synthesis by inhibition of peptidoglycan cross-linking
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penicillin
ampicillin tiracillin piperacillin imipenem aztrenam cephalosporins |
|
block peptidoglycan synthesis
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bacitracin, vancomycin, cycloserine
|
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disrupt bacterial/fungal cell membranes
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polymyxins
|
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block nucleotide synthesis
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sulfonamides, trimethoprim
|
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block fungal cell memebranes
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amphotericin B
nystatin fluconazole/azoles |
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block nuecliotide synthesis
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sulfonamides, trimethoprim
|
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block DNA topoisomerases
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quinolones
|
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red orange body fluids
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Rifampin
|
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Block Protein synthesis at 50S ribosomal subunit
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chlorophenicol, erythromycin/macrolides, lincomycin, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid
|
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block protein synthesis at 30S ribosomal subunit
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Aminoglycosides , tetracylins
|
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bactericidal antibiotics
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penicillin, cephalosporins, vancomycin, aminoglycosides, floroquines, metronidazole
|
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penicillin G
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IV form of penicillin
|
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penicillin V
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oral form of penicillin
|
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MOA of penicillin
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1. bind penicillin binding protein (aka tranpepsidase)
2. block transpepsidase cross-lining of cell wall 3. activate autolytic enzymes (works on dividing bacteria) |
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clinical use of penicillin?
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bactericidal
for gram-positive cocci/rods gram-negative cocci spirochetes |
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is penicillin penicillinase resistant?
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no
|
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toxisity of penicillin
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hypersensitivity reactions, drug-induced coombs positive-hemolytic anemia
|
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how do gram negative bacteria protect themselves from penicillin?
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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
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MRSA
|
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how do gram positive bacteria protect themselves from penicillin?
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1. secrete beta-lactamase = penicillinase(S aureus) and try to intercept antibiotic outside the cell wall
|
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name the penicillinase resistant penicillin?
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methicillin, nafcillin,dicloxacillin
|
|
clinical use of penicillinase resistant penicillin?why such narrow spectrum?
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s. Aureus - but not MRSA
B/C HAVE BULKIER r GROUP |
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TOXICITY of penicillinase resistant penicillin
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HYPERSENSITIVITY reactions
|
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which penicillinase resistant penicillin causes intersitial nephritis?
|
methicillin
|
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aminopenicillins - names?
|
ampicillin, amoxicillin
|
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MOA of aminopenicillins diff than penicillins?
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wider specturm b/c better penitration through gram negative outer membrane and better binding to transpepsidase
|
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are aminopenicillins penicillinase sensitive?
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yes
|
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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?
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hypersensitivity reactions
ampicillin rash psuedomembranous colitis |
|
anti-pseudomonals?
|
ticarcillin, carbeicillin, pipercillin
|
|
diff in MOA of anti-pseudomonals and penicillin?
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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?
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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
|