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188 Cards in this Set
- Front
- Back
|
INH MOA
|
inhibits mycolic acid synthesis
(MTB and M kansasii) |
|
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INH interactions (2 drugs)
|
Phenytoin- inc conc, mental status change, nystagmus, ataxia
Theophylline- arrythmias, convulsions |
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Rifampin active against what organisms
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staph, meningococcus, Hflu, Atypical acid fast bacteria
|
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Rifampin on P450
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autoinduction (reduces conc of P450 drugs.....steroids, digoxin, anticonvulsants, ketoconazole, cyclosporine, methadone, coumadin, PI's, NNTI's)
|
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|
What drug works better against MAC?
|
Rifabutin
(also better to give if on PI's) |
|
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PZA
|
pyrazinamide
makes pyrazinoiic acid dec dose w/ renal insuff can cause hyperuricemia only treat MTB |
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Ethambutol MOA
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inhibit arabinosyl transferase
|
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Ethambutol adverse effects
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optic neuritis, colorblindness, hyperuricemia
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para-aminosalycylic acid (PAS) MOA and adverse
|
block folate synthesis
severe GI, drug induced lupus (only MDR and XDRTB) |
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cycloserine MOA
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inhib cell wall synthesis
last resort for resistant TB |
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treatment plan for latent TB
|
INH 5mg/kg/day x9mos
or rifampin 10mg/kg/day x4mos |
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treatment plan for active TB
|
2mos INH, rifampin+ PZA or ethambutol
4-7mos INH+rifampin if susceptible |
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Common Aminoglycosides
|
Gentamicin
Tobramycin Amikacin Streptomycin |
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Aminoglycoside MOA
|
bind 30S and inhibit protein synthesis
**postantibiotic effect** |
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What bugs aminoglycosides treat?
|
aerobic gm neg rods
(enterobactericeae, pseudomonas, hemophilus) |
|
|
Aminoglycosides resistance
|
modifying enzymes
acetyltransferases adenyltransferases phosphotransferases |
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Macrolides
|
erythromycin
clarithromycin azithromycin |
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Erythromycin
|
bind 50S
gm + bugs can cause transient hearing loss |
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Clarithromycin vs Erythromycin
|
2-4x more active against strep and staph than erythromycin
|
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Azithromycin
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less active vs strep and staph than erythromycin
|
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Clindamycin
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bind 50S
hit anaerobes and gm+ cocci |
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What antibiotic assoc with pseudomembranous colitis?
|
Clindamycin
|
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Chloramphenicol MOA
|
mostly bacteriostatic
bacteriocidal for Hflu, Spneumo, Nmeningitides |
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Chloramphenicol Tox
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myelosuppression
aplastic anemia gray baby syndrome (abd distension, flaccidity, cyanosis) optic neuritis |
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Chloramphenicol uses
|
brain abscess
meningitis if PCN allergic typhoid fever rocky mountain spotted fever |
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Linezolid MOA
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bind 50S
gm + bugs bacteriostatic for staph and enterococci bacteriocidal for strep |
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Linezolid tox
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not involved in P450 system
weak MAOI |
|
|
Linezolid uses
|
pcn resistant Spneumo
MRSA enterococci |
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Sulfonamides MOA
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structural analog of PABA
inhibit folic acid synthesis |
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|
Sulfonamides tox
|
crystalluria and sulfa stones
acute hemolytic anemia in G6PD def NOT FOR PREGGERS (kernicterus) Steven Johnson reaction |
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Sulfonamides interaction
|
displace warfarin, mtx, chlorpropamide (inc activity)
procaine dec sulfa activity |
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Sulfonamides uses
|
UTI
nocardia PJP malaria listeria aerobes |
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Quinolones
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nalidixic acid
ciprofloxacin levofloxacin |
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Ciprofloxacin
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fluoroquinolone
inhibit DNA gyrase very broad spectrum good for UTI and bacterial diarrhea |
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Levofloxacin
|
quinolones
better against strep than cipro |
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Cell wall synthesis inhibitors
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beta lactams (pcn, cephalosporins, carbepenems, monobactams)
vancomycin |
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protein synthesis inhibitors
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macrolides
tetracyclines aminoglycosides clindamycin chloramphenicol |
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nucleic acid synthesis
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quinolones
trimethoprim sulfonamides |
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3 stages of cell wall synthesis
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stage 1- precursor formation (cycloserine inhibs)
stage 2- attachment to membrane (risocerin, bacitracin inhibs) stage 3- cross-linking of peptidoglycan strands (pcn, vancomycin, and cephalosporins) |
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transpeptidase
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a penicillin binding protein
cross links the glycopeptide |
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PCN resistance
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PBP w/ less affinity
MRSA pcn resistant pneumococci enterococcus Staph Aureus makes penicillinase |
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penicillinase resistant
|
oxacillin (only one metabolized by liver)
methicillin dicloxacin nafcillin |
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ampicillin and amoxicillin
|
inc oral absorption
treat hflu, e coli, proteus |
|
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suicide inhibitors of beta lactamase
|
clavulanic acid (+amoxicillin)
sulbactam (+ampicillin) tazobactam (+piperacillin) |
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Resistance to cephalosporins
|
MRSA
enterococci PBP w/ dec affinity |
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monobactams
|
aztreonoam
no cross allergenicity w/ pcn and cephalosporins |
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carbapenems
|
imipenem
has specific porin in gm neg bacilli can cause seizures |
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vancomycin
|
only IV
tx gm + cocci, C dif, MRSA |
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Polymyxins
|
polymyxin B, Colistin
cell membrane disruption tx MDR gm neg bacilli (eg- Actinebacter) in topical form too |
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Daptomycin
|
lipopeptide agent
doesn't act on cell wall post antibiotic effect alternative to vancomycin |
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Amphotericin B MOA and use
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polyene
binds ergosterol in fungal cell membrane candidia, crypto, aspergillus, zygo, dimorphics |
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Amphotericin B tox
|
renal tox
infusion tox |
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Nystatin
|
bind ergosterol in fungal cell membrane
topical |
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Flucytosine
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Antifungal antimetabolite
deaminated to 5FU synergistic w/ AmphoB |
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cryptococcal meningitis tx
|
AmphoB+ 5FC
|
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Azoles MOA
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imidazole and triazoles
inhibit lanosterol demethylase disrupts ergosterol synthesis |
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Azole tox
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inhibit P450
|
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Ketoconazole
|
imidazole
topical for tinea infections can treat prostate ca (inhibit testosterone) |
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Clotrimazole
|
imidazole
topical only and lozenges for thrush |
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Miconazole
|
imidazole
topical only |
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Fluconazole
|
triazole
skin, mucosal, systemic candida crypto meningitis coccidio candida krusei is resistant |
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Itraconazole
|
triazole
metab by liver DOC for histo, blasto, sporothrix |
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Voriconazole
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triazole
P450 interactions tox-photosensitivity, visual disturbances, hepatitis DOC-aspergillus |
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Posaconazole
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triazole
broadest spectrum only one with reliable activity against mucor and rhizopus |
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Echinocandins MOA
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inhibit synthesis of glucan in cell wall
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Capsofungin
|
echinocandin (inhibit glucan synthesis in cell wall)
IV only no CYP450 metabolism hit candida |
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Tolnaftate
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thiocarbamate
tinea infections not effective against candida |
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Fungal cell wall vs cell membrane
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Cell Wall - manin, chitan, glucan (endocandins)
Cell membrane (azoles) |
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AmphoB tox
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distal RTA w/ severe wasting of K and Mg
anemia (dec EPO) infusion tox |
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AmphoB+5FC treats...
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crypto meningitis
candida endocarditis |
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Flucytosine tox
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(5FU antifungal)
adjust for renal leukopenia, thrombocytopenia |
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antifungals that need gastric acid for absorption
|
ketoconazole
itraconazole posaconazole |
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Aminoglycosides bacteriocidal or static?
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bacteriocidal
|
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protein synthesis inhibitors bacteriocidal or static?
|
bacteriostatic
|
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nucleic acid synthesis inhibitors bacteriocidal or static?
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bacteriocidal
(fluoroquinolones, rifampin) |
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Antifolates
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sulfonamides
trimethoprim pyrimethamine |
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resistance to macrolides
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formation of methlytransferases that alter binding site on 50S
active transport out of cell |
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resistance to tetracyclines
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inc activity of transport systems to pump drug out of cell
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resistance to sulfonamides
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change target enzyme
inc PABA formation use of exogenous folic acid |
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resistance to fluoroquinolones
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change target enzymes
increased drug efflux |
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resistance to chloramphenicol
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form inactivating acetyltransferases
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tx for pseudomonas
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ciprofloxacin
AG+beta lactam imipenem |
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Bugs that ceftriaxone doesn't work on
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LAME
listeria (amoxicillin) atypical (tetrcycline) MRSA (vancomycin) enterococci (amox or amp+AG) |
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What antibiotic can cause seizures?
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imipenem
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Vancomycin MOA
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bind D-ala D-ala
sterically hinder transglycosylation (MRSA, enterococci, C dif) |
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Why are anaerobes resistant to aminoglycosides?
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uses oxygen-dependent uptake
|
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tetracycline that treats gingivitis
|
minocycline
|
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What antibiotics prevent formation of the initiation complex for protein synthesis?
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Aminoglycosides (30S)
Linezolid (50S) |
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What antibiotics prevent tRNA binding to A site (elongation)?
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Tetracyclines (30S)
|
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What antibiotics inhibit peptidyl transferase and formation of the peptide bond?
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Chloramphenicol (50S)
|
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What antibiotics prevent translocation (last step of elongation)?
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macrolides (50S)
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antibiotics that can cause ototoxicity
|
ethacrinide
macrolides vancomycin tetracyclines |
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Which antibiotic is attracted to bone but remains active there (can treat osteomyelitis)?
|
clindamycin
|
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Drugs that inhibit dihydrofolate reductase
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MTX
trimethoprim pyrimethamine |
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Direct inhibitors of nucleic acid synthesis (not analogs)
|
Quinolones (ciprofloxacin)
|
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Ciprofloxacin MOA
|
block topo2 (DNA gyrase) and topo4
|
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Long term use of this drug can cause tendonitis and potential rupture (achilles), long QT, photosensitivity, rash
|
Ciprofloxacin
|
|
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Metronidazole is DOC for....
|
giardia
trichomonas entamoeba |
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What drugs do you have to coadminister with pyridoxine?
|
Cycloserine
INH |
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|
azoles inhibit what step of ergosterol synthesis
|
14 a demethylase (takes lanosterol to ergosterol)
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|
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What drugs bind ergosterol?
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amphoB and nystatin (makes cell leaky)
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adamantanes
|
amantadine
|
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neuraminidase inhibitors
|
zanmivir/oseltamivir
|
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nucleotide analogs
|
cidofovir
adefovir dipivoxil |
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pyrophosphate analogue
|
foscarnet
|
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Treat influenza
|
amantadine (adamantane)
zanamivir/oseltamivir (neuraminidase inhibitors) |
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Treat HSV/VZV
|
cidofovir
foscarnet |
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drugs for ganciclovir resistant CMV
|
foscarnet
cidofovir |
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treat Hep B
|
entecavir
telbivudine tenofovir adefovir dipovoxil interferon |
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treat Hep C
|
ribavirin
interferon |
|
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amantadine MOA
|
block M2 protein H+ ion channel
no activity against influenza B |
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amantadine interaction and adverse
|
CNS- insomnia, confusion, anxiety/depression, hallucinations
antihistamines may inc CNS effects |
|
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What flu drug may cause bronchospasm in asthma patients?
|
zanamivir
|
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Acyclovir activation
|
triphophorylated intracellularly
1st = viral thymidine kinase 2 and 3rd = cellular thymidine kinase now can inhibit viral DNA pol |
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Valacyclovir
|
prodrug of acyclovir
treat HSV and VZV |
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Dec Valacyclovir and Acyclovir dose in what circumstance?
|
decreased renal function
|
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Famciclovir
|
tx HSV, VZV
prodrug of penciclovir di-deacetylated in blood, intestine, liver, then oxidized to PCV then monophospho'd by viral thymidine kinase |
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|
What antiviral increases the peak level of digoxin?
|
Famciclovir
|
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Ganciclovir/Valganciclovir MOA
|
nucleoside analog of guanine
(VGCV is prodrug of GCV and VACV) |
|
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Ganciclovir activation
|
Triphosphorylated intracellularly
(CMV viral encoded TK for all 3) GCVTP= inhib viral DNA pol |
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Indications for Ganciclovir
|
CMV (x10 more active than acyclovir)
tx HHV6 |
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Ganciclovir complications
|
myelosuppression
potential teratogen |
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Foscarnet MOA
|
pyrophosphate analog
inhibit viral DNA pol (doesn't need phosphorylation) |
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Cidovir MOA
|
nucleotide analog
diphosphorylated by cellular enzymes |
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Cidovir indications
|
CMV retinitis from AIDS
acyclovir and foscarnet resistant HSV and VZV |
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Cidovir interactions
|
rifampin
ketoprofen chloropropamide dapsone MTX TMP-SMX DDC NSAIDs |
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Adenovir Dipivoxil
|
nucleotide analog of adenosine
treat chronic Hep B |
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Entecavir
|
nucleoside analog of guanasine
treat chronic Hep B |
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Entecavir activation
|
triphosphorylated by cellular enzymes
|
|
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Telbivudine
|
nucleoside analog of thymidine
treat chronic Hep B |
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|
Telbivudine adverse
|
(thymidine analog, treat Hep B)
myopathy peripheral myopathy lactic acidosis |
|
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Ribavirin
|
nucleoside analog of guanosine
treat Hep C (+interferon) severe RSV (can cause hemolytic anemia) |
|
|
Interferon
|
recombinant alpha 2a, 2b
pegylated recombinant 2a, 2b |
|
|
indications for recombinant alpha 2a and 2b interferons
|
genital HPV
hepB and C VZV, HSV, CMV, juvenile laryngeal papillomatosis, west nile |
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resistance to interferon
|
HIV+ HCV
|
|
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initial treatment of HIV
|
2 NRTI's + 3rd drug (efavirenz, atanivir/ritonavir, darunivir, raltevir)
|
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Drugs that inhibit HIV entry
|
maraviroc- block CCR5
enfuviritide- binds heptad repeat (HR1), interferes w/zipping |
|
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Maraviroc metabolism
|
CYP3A4 substrate
(St Johns wort and rifampentine= inducer) |
|
|
Tenofovir in HIV tx
|
only nucleotide analog
only one that doesn't need to be triphosphorylated can cause renal insufficiency |
|
|
NRTIs combos to avoid in HIV tx
|
zidovudine antagonizes phosphorylation of stavudine
tenofovir+didanosine w/ food |
|
|
NRTI class complications
|
mitochondrial tox-->lactic acidosis
lipodystrophy (STAVUDINE>zidovudine) hepatotox |
|
|
Important HIV mutations that cause resistance
q151M complex |
only tenofovir active
|
|
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Important HIV mutations that cause resistance
69 insertion complex |
all nucleosides inactive
|
|
|
Important HIV mutations that cause resistance
K65R |
only zidovudine active
|
|
|
Important HIV mutations that cause resistance
thymidine analog mutations |
wipe out zidovudine, stavudine, tenofovir
|
|
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NNRTI's MOA
|
block RNA and DNA dependent polymerases
|
|
|
Avoid coadministration of NNRTI's and....
|
Rifampin
Midazolam PPI's and rilpivirine |
|
|
NNRTI class complication
|
skin rash 1-3 wks
|
|
|
Efavirenz
|
NNRTI
CNS side effects avoid in 1st trimester of pregnancy |
|
|
Important HIV mutations that cause resistance
K103N |
renders 1st generation NNRTIs ineffective
(etravirine and rilpivirine OK) |
|
|
Integrase inhibitor
|
Raltegravir
(inhibit HIV-1 integrase) rifampin can lower drug levels |
|
|
Class complications of PI's
|
increased bleeding in hemophilia
hepatotox lipodystrophy (protease paunch) CV hyperlipidemia type 2 DM osteonecrosis |
|
|
drugs that inhibit viral DNA pol
|
acyclovir
foscarnet ganciclovir |
|
|
drugs that inhibit viral RNA pol
|
foscarnet
ribavirin |
|
|
inhibit viral reverse transcriptase
|
zidovudine
didanosine lamivudine stavudine nevirapine efavirenz |
|
|
inhibit viral aspartate protease
|
indinavir
ritonavir saquinavir nelfinavir |
|
|
inhibit viral neuraminidase
|
zanamivir
oseltamivir |
|
|
What do acyclovir and ganciclovir treat HSV and VZV?
|
because those are the 2 viruses that have a thymidine kinase
|
|
|
How treat herpes encephalitis?
|
Acyclovir IV
|
|
|
Why want to maintain hydration in a pt on Ganciclovir?
|
because it can cause nephrotoxicity
|
|
|
dose limiting tox for ganciclovir
|
myelosuppression
mucositis |
|
|
If a patient on ganciclovir develops myelosuppression, what is an alternative drug?
|
foscarnet
|
|
|
Which are prodrugs? NRTI's or NNRTI's?
|
NRTI's
|
|
|
Drug to prevent vertical transmission of HIV
|
Nevirapine- NNRTI, single dose at delivery decreases vertical transmission by 50%
|
|
|
What HIV drug is the most hematotoxic?
|
AZT (zidovudine,T analog)
|
|
|
Why not give Stavudine and AZT together?
|
both T analogs
|
|
|
Emtricitabine
|
new form of lamivudine (analog of cytidine)
|
|
|
Abacavir
|
analog of guanosine
(NRTI to treat HIV) |
|
|
PI toxicity
|
indinavir- crystalluria
ritonavir- interactions! induce 1A2, inhibit 3A4 saquinavir- most HIV resistant |
|
|
Quinoline derivatives MOA
|
inhibit parasitic heme polymerase
(which normally protects parasite from toxic heme biproduct- Ferriprotoporphyrin9) |
|
|
Cinchonism
|
quinine and quinidine tox
tinnitus, headache, nausea, blurred vision can also cause hypotension and hypoglycemia |
|
|
Chloroquine treats...
|
vivax, ovale, malariae, knowlesi
|
|
|
Mefloquine
|
treat falciparum, vivax, ovale, malariae
prophylaxis for travellers dont give w/ quinine, beta blockers |
|
|
Primaquine
|
only drug to kill hypnozoites in liver (radical cure vivax and ovale)
also tx for toxoplasmosis |
|
|
Artemisinin derivatives
|
Most potent drug in the arsenal to treat falciparum
|
|
|
Dihydrofolate reductase inhibitors to treat malaria
|
proguanil
pyrimethamine |
|
|
Atovaquone MOA
|
inhibit mitochondrial electron transport
tx PJP, toxoplasmosis, malaria, babesiosis |
|
|
Malarone
|
proguanil+atovaquone
(block dihydrofolate reductase and mitochondrial electron transport chain) prophylaxis and therapy for malaria |
|
|
PJP treatment
|
bactrim
atovaquone is sulfa allergic also--- pentamidine, dapsone |
|
|
Dapsone MOA
|
inhibit dihydropteroate synthase
|
|
|
Babesiosis tx
|
atovaquone + azithromycin
|
|
|
Giardia DOC
|
tinidazole (long acting form of metronidazole, 1 dose)
|
|
|
Nitroimidazoles (metronidazole, tinidazole) MOA
|
reduce electron transport proteins
dont drink etOH! |
|
|
metronidazole treats
|
entamoeba histolytica
giardia trichomonas dracunuclus medinensis |
|
|
tx for most Helminths (round worms, including pin worms)
|
mebendazole
albendazole (inhibit microtubule formation) |
|
|
Filariasis and strongyloides tx
|
ivermectin
|
|
|
Praziquantel
|
inc Ca uptake, ^ vacuolaization damages tegument of parasite
treat flukes |
|
|
malaria prophylaxis
|
chloroquine +/- primaquine
mefloquine if in resistant area |
