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132 Cards in this Set
- Front
- Back
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"We're ECSTaTiC about bacteriostatics."
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Erythromycin
Clindamycin Sulfamethoxazole TMP Tetracyclines Chloramphenicol Bactericidal antibiotics |
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"Very Finely Proficient At Cell Murder"
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Vancomycin
Fluoroquinolones Penicillin Aminoglycosides Cephalosporins Metronidazole |
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PCN G is given by this route
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IV
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PCN V is given by this route
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oral
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Give 3 mechs of PCN
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1. blocks PBP
2. blocks crosslinking of cell wall 3. activates autolytic enzymes |
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Spectrum of 1st gen PCNs? (x2)
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G+ organisms and syphilis
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Toxicity of PCNs?
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-hypersensitivity reaction
-hemolytic anemia |
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Name the PCN-ase resistant PCNs (x3)
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methicillin
nafthacillin dicloxacillin |
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Spectrum of pcnase resistant pcns?
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Naf for staph --> use for Staph aureus, except MRSA
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methicillin has this unusual toxicity
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interstitial nephritis
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Name the 2x aminopcns
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-ampicillin
-amoxicillin |
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Which of the aminopcns has greater oral bioavailability?
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amOxicillin for ORAL
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Aminopcns are given with this drug to enhance spectrum
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clavulanic acid (B-lactamase inhibitor)
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Coverage of aminopcns?
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-HELPS kill enterococci:
Haemophilus influenzae E coli Listeria monocytogenes Proteus mirabilis Salmonella enterococci |
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Name the 3x antipseudomonals
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ticaricillin, carbenicillin, piperacillin
"James Bond uses pipe bomb, car, and explosive tick to kill Pseudomonas" |
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Coverage of ticaricillin/carbenicillin/piperacillin? (x2)
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Pseudomonas spp. and G- rods
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Must give this drug with antipseudomonal pcns
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clavulanic acid (B-lactamase inhibitor)
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Name 3x B-lactamase inhibitors ("CAST")
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Clavulanic Acid
Sulbactam Tazobactam |
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Give the spectrum of 1st gen cephalosporins ("PEcK" + ___)
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PEcK =
Proteus mirabilis E. coli Klebsiella pneumoniae G+ cocci |
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("HENS PEcK")
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Haemophilus influenzae
Enterobacter Neisseria Serratia marcescens Proteus mirabilis E coli Klebsiella |
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Give the spectrum of 3rd gen cephalosporins
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serious G- infections resistant to other B-lactam abx
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Give the spectrum of 4th gen cephalosporins
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Pseudomonas, G+ organisms, G- organisms
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Which antibiotic is associated with VitK deficiency?
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cephalosporins
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Which antibiotic is associated with a disulfuram-like reaction when used with alcohol?
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cephalosporins
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Monobactam that is resistant to B-lactamases and inhibits cell wall synthesis?
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Aztreonam
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Spectrum of Aztreonam
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G-RODS only
Used in (1) pcn-allergic patients and (2) pts with renal insufficiency who can't tolerate AG's |
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Name the 2x carbapenem drugs
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-imipenem/cilastatin
-meropenem |
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why must imipenem be given with cilastatin?
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Cilastatin = inhibitor of renal dihydropeptidase I
renal DHP I inactivates the drug, so want to block this enzyme |
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Coverage of carbapenems? (x3)
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G+ cocci
G- rods Anaerobes (however, many sfx, so limited to life-threatening infxns) |
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3x side effects of carbapenems?
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-GI distress
-skin rash -CNS (seizures) |
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Protein synthesis inhibitors specifically target this bacterial structure
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ribosome (70S; eukaryote ribosome is 80S)
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Explain the acronym "Buy AT 30, CCELL at 50"
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Acronym to remember protein synthesis inhibitors
30S inhibitors: A - AG T - tetracyclines 50S inhibitors C-chloramphenocil C-clindamycin E-erythromycin L-lincomycin L-linezolid |
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AG's:
Mean GNATS canNOT kill anaerobes Explain |
GNATS = drugs
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin ----- NOT = toxicities -N: nephrotoxic -O: ototoxic -T: teratogenic |
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Coverage of AG's?
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Severe gram negative rod infections
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AG's are synergistic with this class of abx
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B-lactams
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mechanism of AG's
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inhibits formation of initiation complex, causes misreading of mRNA
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mech of tetracyclines?
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bind to 30s subunit and prevent attachment of aminoacyl trna
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how can you tell that a drug is a tetracycline?
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all end in -cycline
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why can doxycycline in particular be used in pts with renal failure?
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fecally eliminated
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why must patients taking tetracyclines avoid milk, antacids, or iron-containing products during drug administration?
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divalent cations bind drug in the gut --> inactivates
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why are tetracyclines so effective against Rickettsia and Chlamydia?
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These are both obligate intracellular parasites, and tetracyclines accumulate intracellularly
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3x toxicities of tetracyclines?
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-GI discomfort
-discoloration of teeth and inhibition of bone growth in kids -gray baby syndrome |
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resistance to tetracyclines x2?
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-decreased uptake
-increased efflux 2ry to plasmid-encoded transport pumps |
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macrolides bind to this aspect of the ribosome
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23S rRNA of the 50S subunit
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mechanism of macrolides?
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inhibit protein synthesis by blocking translocation
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spectrum of macrolides?
(one big one) |
-ATYPICAL PNEUMONIAS (mycoplasma, chlamydia, legionella)
-URI, STD, G+ cocci, Neisseria |
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resistance to macrolides
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methylation of 23S rRNA binding site
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mechanism of chloramphenicol?
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inhibits 50S peptidyltransferase activity
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how to tell that a drug is a macrolide?
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-thromycin is the suffix
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spectrum of chloramphenicol?
(one big disease) |
MENINGITIS (H flu, N meningitidis, Strep pneumo)
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Why does chloramphenicol cause gray baby syndrome?
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Toxicity:
infants lack UDP-glucuronyl transferase, required to eliminate the drug |
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mechanism of clinda?
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-binds 50S subunit
-blocks peptide bond formation |
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spectrum of clindamycin?
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ANAEROBIC INFECTIONS in aspiration pneumonia or lung abscesses
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drug used to treat anaerobes ABOVE the diaphragm
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clindamycin
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drug used to treat anaerobes BELOW the diaphragm
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metronidazole
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sulfonamides inhibit this enzyme
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dihydropteroate synthetase
(competitive inhibitor) |
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TMP inhibits this enzyme
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dihydrofolate reductase
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in what way are TMP and SMX synergistic?
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inhibition of different steps in the bacterial folate synthesis pathway
thus blocks bacterial DNA synthesis |
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3x mechs for resistance to sulfonamides?
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- altered dihydropteroate synthetase
-dec. uptake -inc PABA synthesis (overcomes competitive inhibition) |
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toxicity of TMP?
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TMP = treats marrow poorly
megaloblastic anemia leukopenia granulocytopenia Occurs because inhibition of DHFR --> decreased nucleotides for DNA synthesis |
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a. What compound can be used to treat TMP toxicity?
b. what is this treatment called? |
a. folinic acid (bypasses step catalyzed by DHFR)
b. leukovorin rescue |
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quinolone mechanism?
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inhibits DNA gyrase (TOPO II)
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spectrum of quinolones?
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G- rods of urinary and GI tracts
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what unique toxicity is seen with quinolones?
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FluoroquinoLONES hurt attachments to your BONES
-Tendonitis and tendon rupture |
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resistance to fluoroquinolones?
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mutated topo II (DNA gyrase)
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mechanism of metronidazole?
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forms free radical toxic metabolites in bacterial cells that damage DNA
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mechanism of polymyxins?
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Detergent - MYXIN up the membrane
binds to bacterial cell membranes and disrupts osmotic properties |
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use of polymixins?
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resistant G- infections
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four drugs used in M. tuberculosis therapy
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RIPE for tx:
Rifampin Isoniazid Pyrazinamide Ethambutol |
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TB prophylaxis?
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INH
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How is pyrazinamide useful in tx of TB?
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works well in acidic pH of phagolysosome where TB engulfed by macrophage is found
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ethambutol mechanism?
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decreased carbohydrate polymerization of mycobacterial cell wall
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important ethambutol sfx?
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optic neuropathy --> red/green color blindness
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most important sfx (x1) of most drugs for TB other than ethambutol?
hint: can't drink and take TB drugs |
hepatotoxicity
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mech of INH?
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inhibits synth of mycolic acids
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toxicity of INH x2?
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INH = injures neurons and hepatocytes
neurotoxicity hepatotoxicity lupus |
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how can INH toxicity be prevented?
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give with vit B6 (pyridoxine)
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4 R's of Rifampin:
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RNA pol inhibitor
Revs up P450 system (inducer) Red/orange body fluids (nonhazardous) Rapid resistance with monotherapy |
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Give the best abx to use for:
Meningococcus |
rifampin
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Give the best abx to use for:
Gonorrhea |
ceftriaxone
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Give the best abx to use for:
syphilis |
PCN G
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Give the best abx to use for:
recurrent UTI |
TMP-SMX
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Give the best abx to use for:
Pneumocystis jirovecii pneumonia (AIDS) |
TMP-SMX
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Give the best abx to use for:
endocarditis with surgical or dental procedure |
PCNs
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Give the best abx to use for:
Mycobacterium avium intracellulare |
azithromycin
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Give the best abx to use for:
MRSA |
Vancomycin
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Give the best abx to use for:
VRE |
linezolid + streptogramins
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What fatty compound is unique to the membrane of fungi?
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ergosterol
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give the synthesis pathway for ergosterol (two steps)
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squalene --> lanosterol --> ergosterol
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mechanism of amphoteracin B?
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binds ergosterol --> pore in membrane allows leakage of electrolytes
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uses of amphoteracin B?
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-SERIOUS, SYSTEMIC mycoses
-intrathecal for fungal meningitis |
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review toxicity of ampho B?
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everything - "amphoterrible"
fever/chills, hypoTN, nephrotoxicity, arrythmias, anemia, IV phlebitis -hydration reduces nephrotox -liposomal ampho B (form of the drug) reduces other toxicity |
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nystatin mech?
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binds ergosterol to create pores in fungal cell membrane
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why is nystatin use always topical?
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too toxic for systemic use
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"Swish and swallow" nystatin for this infection
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oral/esophageal candidiasis
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Topical nystatin for these 2x conditions
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-diaper rash
-vaginal candidiasis |
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mechanism of azoles?
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squalene --> lanosterol --||--> ergosterol
azoles block P450 system that converts lanosterol to ergosterol |
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Indications for azoles (x2)?
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1. cryptococcal meningitis in AIDS (crosses BBB)
2. candidial infections |
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this drug is used in tx of invasive aspergillosis
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capsofungin
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this drug is used to treat onchyomycosis
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terbafine
mech: inhibits ergosterol synthesis: [squalene -||-> lanosterol --> ergosterol] |
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this drug is used to inhibit the growth of dermatophytes (all the tineas)
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griseofulvin
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what is the mechanism of amantidine?
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blocks viral penetration/uncoating
influenza A must acidify its core via an ion channel (M2 protein) to uncoat the viral core and liberate the genome. amantidine blocks this channel. |
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amantidine is useful for the treatment of this neurological disease
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Parkinson's disease
causes release of DA from intact nerve terminals --> can cause cerebellar problems in normal individuals due to inc DA |
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amantidine can be used to treat this virus
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influenza A only
Note that 90% of influenza is resistant to amantadine, so not used anymore |
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Name the drug class:
zanamavir, oseltamavir |
neuraminidase inhibitors
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What is the mechanism of the drug(s) below?
zanamavir, oseltamavir |
Neuraminidase inhibitors - prevent virus from cleaving sialic acid residues and thus prevents virions from being released from an infected cell
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mechanism of ribavarin?
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inhibits synthesis of guanine nucleotides
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uses of ribavarin x2?
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-RSV
-chronic hepatitis C |
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toxicity of ribavarin
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-hemolytic anemia
-SEVERE teratogen |
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viral nucleic acid synthesis can be blocked by these two drug classes
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-purine/pyrimidine analogs
-reverse transcriptase inhibitors |
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acyclovir mechanism?
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guanosine analog
-inhibits viral DNA pol -phosphorylated by VIRAL thymidine kinase only, so no effect on host cells |
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ganciclovir mechanism?
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guanosine analog
-inhibits viral DNA pol -phosphorylated by VIRAL thymidine kinase only, so no effect on host cells |
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acyclovir coverage?
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-HSV
-VZV -EBV HHV 1-4 |
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ganciclovir coverage?
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CMV (HHV5)
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acyclovir resistance (x1)
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lack of viral thymidine kinase
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ganciclovir resistance? (x2)
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-mutated CMV DNA pol
-lack of viral TK |
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foscarnet mechanism?
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FOScarnet = pyroFOSphate analog
inhibits viral DNA pol |
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two *very specific* uses of foscarnet?
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-CMV retinitis in immunocompromised pts when ganciclovir fails
-acyclovir resistant HSV |
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foscarnet resistance x1?
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mutated DNA pol
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HAART therapy requires at least (#) drugs to prevent development of resistance
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3 drugs:
2 NTRI's + 1 protease inhibitor 2 NTRI's + 1 NNRTI |
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How can a reader tell that a drug is an HIV protease inhibitor?
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ends with -navir
NAVIR tease a protease |
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mechanism of HIV protease inhibitors?
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inhibits HIV protease, whose function is to cleave HIV polypeptide into functional proteins
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a. NRTI's and NNRTI's have similar mechanisms - describe it
b. what is different about their mechanism? |
a. both competitively inhibit nucleotide binding to RT and terminate the DNA chain
b. NRTI's must be PHOSPHORYLATED before they are active; NNRTI's do not require this step |
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identify the class of the drugs below:
-nevirapine -efavirenz -declaviridine |
NNRTI
= non-nucleoside reverse transcriptase inhibitors |
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identify the class of the drugs below:
-zidovudine -didanosine -zalcitabine -stavudine |
NRTI
nucleoside reverse transcriptase inhibitor |
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identify the class of the drug below:
-enfuvirtide |
enFUvirtide = fusion inhibitor
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what is the mechanism of enFUvirtide, a fusion inhibitor?
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binds viral gp41 --> inhibits conformational change required for fusion with CD4 cells, blocking entry and replication
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what is the mechanism of IFNs as related to viral therapy?
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in virally infected cells, induce formation of glycoproteins that block replication of both RNA and DNA viruses
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IFN-B is used to treat this condition
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MS
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IFN-y is used to treat this condition
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NADPH oxidase deficiency
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Review abx to avoid in pregnancy
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SAFE Moms Take Really Good Care:
Sulfonamides Aminoglycosides Fluoroquinolones Erythromycin Metronidazole Tetracyclines Ribavarin Griseofulvin Chloramphenicol FA 198 |
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antimicrobial chemotherapy for toxoplasma gondii?
(2x agents used together) |
-sulfadiazine
-pyrimethamine |