pharm exam 3 Flashcards

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
Q

highest risk for c dif

A

clindamycin, cephalosporins (broad spectrum), fluoroquinolones, carbapenems

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26
Q

tx c dif

A

NOT antidiarrheal agents. abx: metronidazole, vancomycin, fidaxomicin)

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27
Q

downside of bacteriostatics

A

reliant on competent host immune system (so don’t use in immunocompromised)

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28
Q

what agent would you use for locations that are difficult for abx to penetrate?

A

bactericidal! esp. in endocarditis, meningitis, osteomyelitis

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29
Q

ideal or actual body weight for aminoglycosides

A

ideal! bc hydrophilic

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30
Q

abx whose dose should be reduced in pts with decreased kidney fxn

A
Cephalosporins (1 & 2 gen)
Aminoglycosides
Vancomycin
Ethambutol
Sulfonamides/trimethoprim
Carbapenems
Extended spectrum penicillins
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31
Q

abx whose dose should be reduced in pts with decreased liver fxn

A
Clindamycin
Chloramphenicol
Metronidazole
Macrolides
Rifampin
Isoniazid
Tetracylclines
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32
Q

category D abx

A

DON’T USE IN PREGNANT! Aminoglycosides & tetracyclines (and sulfonamide-induced kernicterus during nursing)

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33
Q

most common abx that provoke sensitivity rxn’s

A

beta lactams
sulfonamides
trimethoprim
erythromycin

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34
Q

significance of gram neg. OM

A

hinders transport of many abx; small hydrophilic drugs can cross via transport through porins

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35
Q

list the bactericidal agents

A

aminoglycosides, beta-lactams, daptomycin, fluoroquinolones, isoniazid, metronidazole, polymyxins, pyrazinamide, rifampin, vancomycin

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36
Q

list the bacteriostatic agents

A

(the CCEMOSTT ones!)

chloramphenicol, clindamycin, ethambutol, macrolides, oxazolidinones, sulfonamides, tetracyclines, trimethoprim

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37
Q

what class inhibits cell wall synthesis?

A

beta lactams! & glycopeptides (vancomycin), fosfomycin (treats uncomplicated UTIs in women)

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38
Q

beta lactam subclasses

A

penicillins, cephalosporins, carbapenems, monobactams

39
Q

which bugs are innately resistant to B lactams and why?

A

chlamydia, mycoplasma, & legionella! bc they lack a peptidoglycan-based cell wall (b lactam mech. binds PBPs & inhibits cross linking of peptidoglycan)

40
Q

beta lactam mechanism

A

irreversibly inhibits PBPs –> inhibits cross-linking of cell wall NAM-NAG polymers & peptidoglycan buildup activates autolysins –> mediate cell wall disassembly

41
Q

penicillin structure

A

B-lactam ring fused to a FIVE member thiazolidine ring

42
Q

4 classifications penicillin

A
  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
Q

which penicillin is orally effective?

A

pen V! it is acid-stable in stomach (unlike G)

44
Q

clavulanic acid use?

A

B-lactamase inhibitor so combine with aminopenicillins & anti-pseudomonals (i.e. amoxicillin, ticarcillin, piperacillin)

45
Q

what is pen G benzathine used for?

A

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
Q

least toxic of all abx?

A

penicillins

47
Q

standard penicillin clinical uses

A

syphilis–benzathine, group A strep (pharyngitis, endocarditis), oral infections

48
Q

antistaph penicillins clinical uses

A

pen G resistant MSSA (endocarditis, skin & soft tissue infections), osteomyelitis; superior to vancomycin

49
Q

aminopenicillins clinical uses

A

URI (strep pharyngitis, otitis media); enterococcal infections

50
Q

antipseudomonal penicillin uses

A

empiric treatment nosocomial infections, mixed infections, URI with suspected beta lactamase resistance

51
Q

cephalosporin structure

A

b lactam ring fused to SIX membered ring

52
Q

progression of 5 cephalosporin generations

A

increasing activity against gram negative bacteria, decreasing inactivation by beta lactamases, increasing CNS penetration

53
Q

first generation cephalosporin

A

cefazolin–commonly used to prevent surgical site infections

54
Q

second generation cephalosporin

A

cefoxitin–prophylaxis in abdominal surgery

55
Q

third glass cephalosporin

A

ceftriaxone–widely used; treats gram - meningitis & gonorrhea

56
Q

fourth generation cephalosporin

A

cefepime–empiric treatment nosocomial infections

57
Q

fifth generation cephalosporin

A

ceftaroline–only cephalosporin active against MRSA

58
Q

what is imipenem-cilastatin?

A

beta lactam, very broad spectrum; used in MDR infections, anaerobic & mixed infection

59
Q

aztreonam structure

A

beta lactam ring NOT fused with a second ring

60
Q

aztreonam:

A

beta lactam, narrow spectrum, GRAM NEGATIVE AEROBES (including pseudomonas); inhaled by CF patients w/ p. aeruginosa

61
Q

glycopeptide prototype

A

vancomycin

62
Q

glycopeptide mech

A

(vancomycin)–prevents polymerization of cell wall precursors; only active against gram + (strep & staph); reserved for serious resistant infections

63
Q

vancomycin adverse rxn’s

A

ototoxic, nephrotoxic, “red man syndrome”

64
Q

fosfomycin use

A

cytosol (prevents NAG to NAM); uncomplicated UTIs in females

65
Q

aminoglycoside required drugs

A

gentamicin, amikacin

66
Q

aminoglycoside MOA

A

bactericidal, conc. dependent; binds to 30s ribosomal subunit which causes misreading of mRNA

67
Q

aminoglycoside uses

A

combine w/ beta lactam for serious gram negative infections (septicemia), w/ beta lactam or vancomycin for endocarditis, & plague, TB

68
Q

adverse rxn aminoglycosides

A

ototoxicity, nephrotoxicity, neuromuscular blockade (why it’s contraindicated in pts with myasthenia gravis)

69
Q

how is gentamicin given?

A

once-daily high doses! bc conc. dependent

70
Q

tetracyclines required drugs

A

doxycycline, tigecycline

71
Q

abx that inhibit protein synthesis

A

aminoglycosides (gentamicin, amikacin), tetracyclines (doxycycline, tigecycline), macrolides (azithromycin, clarithromycin), clindamycin, chloramphenicol, linezolid, quinupristin-dalfopristin

72
Q

how are tetracyclines given?

A

lipid soluble so orally; except tigecycline is given parenterally

73
Q

tetracyclines form what?

A

chelates with multivalent cations (don’t administer w/ dairy, pepto bismol, iron supplements)

74
Q

doxycycline uses

A

broad spectrum against gram + & -

75
Q

tigecycline use

A

IV for highly resistant gram - infections

76
Q

macrolide required drugs

A

azithromycin, clarithromycin

77
Q

macrolide MOA

A

bacteriostatic; binds 50S subunit & inhibits translocation

78
Q

COMBO TO AVOID

A

macrolide w/ clindamycin or chloramphenicol (binding sites overlap so would result in abx antagonism)

79
Q

macrolide uses

A

upper & lower respiratory tract infections (pertussis, pneumonias, diphtheria, sinusitis, bronchitis, pharyngitis), atypicals (chlamydia, myco. avium) & PUD (H pylori)

80
Q

clindamycin MOA & use

A

binds 50S subunit, most effective against g + & anaerobe; used for skin & soft tissue infections (i.e. gas gangrene)

81
Q

major concern for clindamycin?

A

CDAD!

82
Q

chloramphenicol use

A

broad spectrum used mainly outside US due to toxicity

83
Q

isoniazid MOA

A

prodrug that inhibits synthesis of mycolic acid by inhibiting InhA and KasA enzymes

84
Q

what would reduce risk of peripheral neuropathy while being treated for TB?

A

taking vitamin B6!!

85
Q

what TB drug doesn’t have an effect on the liver?

A

ethambutol

86
Q

what can be used as second line for TB treatment?

A

streptomycin

87
Q

what would give someone with active TB?

A

INH + rifampin + pyrazinamide + ethambutol

88
Q

active TB treatment phases include:

A

induction: 2 months of INH, rifampin, pyrazinamide, ethambutol
continuation: next 4 months or longer of INH and rifampin

89
Q

prophylaxis for latent TB consists of:

A

1st line = daily monotherapy for 9 months with INH

2nd line = daily monotherapy for 4 months with rifampin

90
Q

drug that can cause unpredictable aplastic anemia

A

chloramphenicol

91
Q

what is an adverse effect of fluoroquinolones?

A

tendon rupture in kids

92
Q

three drugs that can be used to treat c dif?

A

metronidazole, vancomycin, fidaxomicin

93
Q

1 drug for UTI

A

SMX-TMP

94
Q

what are the 2 formulations of colistin and how are they given?

A
  1. colistin sulfate–topical & oral (GI)

2. colistimethate–parenteral (prodrug)