pharm exam 3 Flashcards

(94 cards)

1
Q

dopamine blockade at mesolimbic-mesocortical pathway

A

antipsychotic efficacy

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2
Q

DA blockade at nigrostriatal pathway

A

parkinsonian side effects

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3
Q

DA blockade at tuberoinfundibular pathway

A

hyperprolactinemia (weight gain, sexual dysfunction)

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4
Q

DA blockade at medullary-periventricular pathway

A

anti-emetic effects

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5
Q

DA hypothesis

A

excess DA @ mesolimbic –> + symptoms

deficit DA @ mesocortical –> - symptoms

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6
Q

antipsychotics mechanism

A

DA D2 receptor antagonists!!

EXCEPT atypical higher affinity for 5-HT2A than D2 (why it’s better at treating - symptoms)

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7
Q

what is the neuroleptic malignant syndrome tetrad?

A
  1. mental status change (confusion, stupor)
  2. hyperthermia
  3. extreme muscle rigidity (increase CK)
  4. autonomic dysfunction (tachycardia, HTN, sweating)
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8
Q

high potency antipsychotic characteristics

A

higher risk EPSE but less sedating

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9
Q

high potency antipsychotic prototype

A

haloperidol

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10
Q

low potency antipsychotic characteristics

A

lower risk of EPSE but more sedating

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11
Q

low potency antipsychotic prototype

A

chlorpromazine

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12
Q

second generation antipsychotic protoype

A

clozapine

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13
Q

what’s unique about clozapine?

A

efficacy for recalcitrant schizophrenia & suicidal behavior; reserved for cases where other antipsychotics have failed due to agranulocytosis; nearly absent risk of EPSE/TD

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14
Q

list the four 5-HT2A > D2 antagonists

A

risperidone
olanzapine
quetiapine
ziprasidone

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15
Q

the partial D2 receptor agonist

A

aripiprazole (abilify); its partial agonism of D2 receptors blocks full agonist effect of DA

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16
Q

atypical vs typical antipsychotics

A

atypical better at treating NEGATIVE symptoms, have lower risk EPSE/TD, but higher risk of weight gain & more expensive

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17
Q

MIC definition

A

lowest conc. of an agent that PREVENTS VISIBLE BACTERIAL GROWTH in 24 hrs

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18
Q

what are innately resistant to aminoglycosides?

A

anaerobes

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19
Q

what are innately resistant to metronidazole?

A

aerobes

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20
Q

what are gram negative innately resistant to?

A

LIPOPHILIC– standard penicillins & high MW hydrophilic– vancomycin

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21
Q

ways a bug can ACQUIRE resistance?

A
  1. inactivation of the antibiotic
  2. decreased uptake of the antibiotic
  3. increased efflux of the antibiotic
  4. altered target site (so it can’t bind)
  5. bypass target process
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22
Q

mechanisms of acquiring resistance

A

enzyme induction (increasing expression of existing resistance genes), vertical transfer (spontaneous mutation), horizontal transfer (conjugation)

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23
Q

do abx cause mutations?

A

NO! they promote resistance by exerting selective pressure

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24
Q

classic mech. of MDR

A

gram neg. doing horizontal transfer (conjugation, plasmid transferring R factor)

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25
highest risk for c dif
clindamycin, cephalosporins (broad spectrum), fluoroquinolones, carbapenems
26
tx c dif
NOT antidiarrheal agents. abx: metronidazole, vancomycin, fidaxomicin)
27
downside of bacteriostatics
reliant on competent host immune system (so don't use in immunocompromised)
28
what agent would you use for locations that are difficult for abx to penetrate?
bactericidal! esp. in endocarditis, meningitis, osteomyelitis
29
ideal or actual body weight for aminoglycosides
ideal! bc hydrophilic
30
abx whose dose should be reduced in pts with decreased kidney fxn
``` Cephalosporins (1 & 2 gen) Aminoglycosides Vancomycin Ethambutol Sulfonamides/trimethoprim Carbapenems Extended spectrum penicillins ```
31
abx whose dose should be reduced in pts with decreased liver fxn
``` Clindamycin Chloramphenicol Metronidazole Macrolides Rifampin Isoniazid Tetracylclines ```
32
category D abx
DON'T USE IN PREGNANT! Aminoglycosides & tetracyclines (and sulfonamide-induced kernicterus during nursing)
33
most common abx that provoke sensitivity rxn's
beta lactams sulfonamides trimethoprim erythromycin
34
significance of gram neg. OM
hinders transport of many abx; small hydrophilic drugs can cross via transport through porins
35
list the bactericidal agents
aminoglycosides, beta-lactams, daptomycin, fluoroquinolones, isoniazid, metronidazole, polymyxins, pyrazinamide, rifampin, vancomycin
36
list the bacteriostatic agents
(the CCEMOSTT ones!) | chloramphenicol, clindamycin, ethambutol, macrolides, oxazolidinones, sulfonamides, tetracyclines, trimethoprim
37
what class inhibits cell wall synthesis?
beta lactams! & glycopeptides (vancomycin), fosfomycin (treats uncomplicated UTIs in women)
38
beta lactam subclasses
penicillins, cephalosporins, carbapenems, monobactams
39
which bugs are innately resistant to B lactams and why?
chlamydia, mycoplasma, & legionella! bc they lack a peptidoglycan-based cell wall (b lactam mech. binds PBPs & inhibits cross linking of peptidoglycan)
40
beta lactam mechanism
irreversibly inhibits PBPs --> inhibits cross-linking of cell wall NAM-NAG polymers & peptidoglycan buildup activates autolysins --> mediate cell wall disassembly
41
penicillin structure
B-lactam ring fused to a FIVE member thiazolidine ring
42
4 classifications penicillin
1. standard (penicillin G, penicillin V): g + 2. anti-staph (nafcillin): protects against B lactamase; MSSA 3. aminopenicillins (amoxicillin): adds activity against g - bc + charged R group allows it to get through porins 4. anti-pseudomonal (ticarcillin, piperacillin)
43
which penicillin is orally effective?
pen V! it is acid-stable in stomach (unlike G)
44
clavulanic acid use?
B-lactamase inhibitor so combine with aminopenicillins & anti-pseudomonals (i.e. amoxicillin, ticarcillin, piperacillin)
45
what is pen G benzathine used for?
repository preparation; single dose given IM for treatment of syphilis & prevention of rheumatic fever. example of time dependence (absorbed for several weeks & produces persistent but low blood levels)
46
least toxic of all abx?
penicillins
47
standard penicillin clinical uses
syphilis--benzathine, group A strep (pharyngitis, endocarditis), oral infections
48
antistaph penicillins clinical uses
pen G resistant MSSA (endocarditis, skin & soft tissue infections), osteomyelitis; superior to vancomycin
49
aminopenicillins clinical uses
URI (strep pharyngitis, otitis media); enterococcal infections
50
antipseudomonal penicillin uses
empiric treatment nosocomial infections, mixed infections, URI with suspected beta lactamase resistance
51
cephalosporin structure
b lactam ring fused to SIX membered ring
52
progression of 5 cephalosporin generations
increasing activity against gram negative bacteria, decreasing inactivation by beta lactamases, increasing CNS penetration
53
first generation cephalosporin
cefazolin--commonly used to prevent surgical site infections
54
second generation cephalosporin
cefoxitin--prophylaxis in abdominal surgery
55
third glass cephalosporin
ceftriaxone--widely used; treats gram - meningitis & gonorrhea
56
fourth generation cephalosporin
cefepime--empiric treatment nosocomial infections
57
fifth generation cephalosporin
ceftaroline--only cephalosporin active against MRSA
58
what is imipenem-cilastatin?
beta lactam, very broad spectrum; used in MDR infections, anaerobic & mixed infection
59
aztreonam structure
beta lactam ring NOT fused with a second ring
60
aztreonam:
beta lactam, narrow spectrum, GRAM NEGATIVE AEROBES (including pseudomonas); inhaled by CF patients w/ p. aeruginosa
61
glycopeptide prototype
vancomycin
62
glycopeptide mech
(vancomycin)--prevents polymerization of cell wall precursors; only active against gram + (strep & staph); reserved for serious resistant infections
63
vancomycin adverse rxn's
ototoxic, nephrotoxic, "red man syndrome"
64
fosfomycin use
cytosol (prevents NAG to NAM); uncomplicated UTIs in females
65
aminoglycoside required drugs
gentamicin, amikacin
66
aminoglycoside MOA
bactericidal, conc. dependent; binds to 30s ribosomal subunit which causes misreading of mRNA
67
aminoglycoside uses
combine w/ beta lactam for serious gram negative infections (septicemia), w/ beta lactam or vancomycin for endocarditis, & plague, TB
68
adverse rxn aminoglycosides
ototoxicity, nephrotoxicity, neuromuscular blockade (why it's contraindicated in pts with myasthenia gravis)
69
how is gentamicin given?
once-daily high doses! bc conc. dependent
70
tetracyclines required drugs
doxycycline, tigecycline
71
abx that inhibit protein synthesis
aminoglycosides (gentamicin, amikacin), tetracyclines (doxycycline, tigecycline), macrolides (azithromycin, clarithromycin), clindamycin, chloramphenicol, linezolid, quinupristin-dalfopristin
72
how are tetracyclines given?
lipid soluble so orally; except tigecycline is given parenterally
73
tetracyclines form what?
chelates with multivalent cations (don't administer w/ dairy, pepto bismol, iron supplements)
74
doxycycline uses
broad spectrum against gram + & -
75
tigecycline use
IV for highly resistant gram - infections
76
macrolide required drugs
azithromycin, clarithromycin
77
macrolide MOA
bacteriostatic; binds 50S subunit & inhibits translocation
78
COMBO TO AVOID
macrolide w/ clindamycin or chloramphenicol (binding sites overlap so would result in abx antagonism)
79
macrolide uses
upper & lower respiratory tract infections (pertussis, pneumonias, diphtheria, sinusitis, bronchitis, pharyngitis), atypicals (chlamydia, myco. avium) & PUD (H pylori)
80
clindamycin MOA & use
binds 50S subunit, most effective against g + & anaerobe; used for skin & soft tissue infections (i.e. gas gangrene)
81
major concern for clindamycin?
CDAD!
82
chloramphenicol use
broad spectrum used mainly outside US due to toxicity
83
isoniazid MOA
prodrug that inhibits synthesis of mycolic acid by inhibiting InhA and KasA enzymes
84
what would reduce risk of peripheral neuropathy while being treated for TB?
taking vitamin B6!!
85
what TB drug doesn't have an effect on the liver?
ethambutol
86
what can be used as second line for TB treatment?
streptomycin
87
what would give someone with active TB?
INH + rifampin + pyrazinamide + ethambutol
88
active TB treatment phases include:
induction: 2 months of INH, rifampin, pyrazinamide, ethambutol continuation: next 4 months or longer of INH and rifampin
89
prophylaxis for latent TB consists of:
1st line = daily monotherapy for 9 months with INH | 2nd line = daily monotherapy for 4 months with rifampin
90
drug that can cause unpredictable aplastic anemia
chloramphenicol
91
what is an adverse effect of fluoroquinolones?
tendon rupture in kids
92
three drugs that can be used to treat c dif?
metronidazole, vancomycin, fidaxomicin
93
#1 drug for UTI
SMX-TMP
94
what are the 2 formulations of colistin and how are they given?
1. colistin sulfate--topical & oral (GI) | 2. colistimethate--parenteral (prodrug)