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PHRM 865 Therapeutics > Exam 5 - Antimycobacterials Medchem LaCount > Flashcards

Exam 5 - Antimycobacterials Medchem LaCount Flashcards

(51 cards)

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1
Q

most common infection in the world

A

tuberculosis

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2
Q

4 layers of mycobacterium cell walls

A

-mycolic acid rich layer
-arabinogalactan
-peptidoglycan
-lipid bilayer

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3
Q

Isoniazid is a prodrug activated by which protein?

a. KatG
b. NAT2
c. pncA
d. panD

A

a. KatG

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4
Q

isoniazid MOA (3 steps; slide 9)

A
  1. Activation by KatG (catalase-peroxidase)
  2. Forms adducts with NAD+ and NADP+
  3. Inhibits enzymes that use NAD+ and
    NADP+
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5
Q

isoniazid is a component of

a. GDP
b. DHFR
c. FAS I
d. FAS II

A

d. FAS II

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6
Q

activated isoniazid inhibits ____

A

InhA

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7
Q

2 mechanisms of isoniazid resistance

A
  1. over-expression of InhA
  2. mutations in KatG so it is no longer active
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8
Q

isoniazid is metabolized via _______ by NAT2

a. hydroxylation
b. acetylation
c. oxidation
d. glucoronidation

A

b. acetylation

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9
Q

isoniazid competitively inhibits _______ _______ which can cause peripheral neuropathy

a. RNA polymerase
b. ATP synthase
c. pyridoxine phosphokinase
d. arabinosyl transferase

A

c. pyridoxine phosphokinase

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10
Q

isoniazid slow vs rapid metabolizer

A

slow = 3 hours
rapid = 1 hour

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11
Q

tx of active TB infections: what is the most common regimen (acronym)

A

RIPE
rifampin
isoniazid
pyrazinamide
ethambutol

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12
Q

isoniazid and ethionamide

a. inhibits mycolic acid synthesis
b. inhibits cell wall synthesis
c. inhibits cell memb synthesis and trans-translation
d. inhibits ATP synthesis

A

a. inhibits mycolic acid synthesis

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13
Q

ethambutol

a. inhibits mycolic acid synthesis
b. inhibits cell wall synthesis
c. inhibits cell memb synthesis and trans-translation
d. inhibits ATP synthesis

A

b. inhibits cell wall synthesis

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14
Q

pyrazinamide

a. inhibits mycolic acid synthesis
b. inhibits cell wall synthesis
c. inhibits cell memb synthesis and trans-translation
d. inhibits ATP synthesis

A

c. inhibits cell memb synthesis and trans-translation

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15
Q

bedaquiline

a. inhibits mycolic acid synthesis
b. inhibits cell wall synthesis
c. inhibits cell memb synthesis and trans-translation
d. inhibits ATP synthesis

A

d. inhibits ATP synthesis

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16
Q

_______ is a major toxicity of isoniazid and occurs in 1% of pts

A

hepatitis

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17
Q

isoniazid toxicity: can lead to drug-induced syndrome resembling systemic _______ _______

A

lupus erythematosus

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18
Q

T or F: vasculitis due to isoniazid is irreversible

A

F (disappears when the drug is stopped)

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19
Q

isoniazid toxicity mechanism: which CYP converts acetylhydrazine to hepatotoxic metabolites?

a. CYP2C9
b. CYP2D6
c. CYP2D9
e. CYP2E1

A

e. CYP2E1

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20
Q

pyrazinamide:
inactive at _____ pH
activated at _____ pH

A

neutral; low

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21
Q

pyrazinamide is a prodrug requiring conversion to pyrazinoic acid by _____

a. KatG
b. NAT2
c. pncA
d. panD

22
Q

pyrazinamide inhibits _____, leading to inhibition of CoA synthesis

a. KatG
b. NAT2
c. pncA
d. panD

23
Q

panD converts L-aspartate to _______

a. alanine
b. valine
c. serine
d. tryptophan

24
Q

pyrazinamide resistance is PRIMARILY due to mutations in ____

a. KatG
b. NAT2
c. pncA
d. panD

25
what is the most common SE of pyrazinamide? what is the most dangerous?
most common = joint pain (arthalgia) most dangerous = hepatitis
26
ethambutol inhibits which enzyme? a. RNA polymerase b. ATP synthase c. pyridoxine phosphokinase d. arabinosyl transferase
d. arabinosyl transferase
27
mycobacterial arabinosyl transferases are involved in the polymerization of a. mycolic acid b. arabinogalactan c. peptidoglycan d. lipid bilayer
b. arabinogalactan
28
ethambutol resistance is due to mutations in which enzyme?
due to mutations in arabinosyl transferase
29
T or F: ethambutol is primarily used alone
F (synergistic with rifampin; not used alone due to resistance)
30
most important toxicity of ethambutol a. headaches b. hepatitis c. urine discoloration d. optic neuritis
d. optic neuritis (can be irrev if tx not d/c)
31
most effective first line agent for TB
rifampin
32
rifampin is most effective when _____ _____ is occurring
cell division
33
biggest difference between rifampin and rifapentine
rifapentine has longer half life (13.5 hrs vs 2-5 hrs)
34
rifampin binds to _______ _______ to block the path of elongating RNA a. RNA polymerase b. ATP synthase c. pyridoxine phosphokinase d. arabinosyl transferase
a. RNA polymerase
35
does rifampin bind to the active site or away from the active site?
away from active site
36
rifampin's main adverse reaction
colors urine, tears, and sweat orange
37
preferred FQ for TB regimen a. levofloxacin b. moxifloxacin c. gatifloxacin d. ciprofloxacin
b. moxifloxacin
38
which 3 anti-TB drugs have hepatitis as a toxicity?
rifampin, isoniazid, pyrazinamide RIP
39
what 3 drugs are in the BPaL regimen approved in 2019?
bedaquiline pretomanid linezolid
40
the BPaL Regimen is used in tx of what 2 things?
XDR-TB tx-intolerant or non-responsive MDR-TB
41
which of the following is FALSE about bedaquiline? a. first in class diarylquinoline b. inhibits ATP synthase c. IV only d. resistance is due to mutations in atpE
c. IV only (oral)
42
bedaquiline inhibts which enzyme? a. RNA polymerase b. ATP synthase c. pyridoxine phosphokinase d. arabinosyl transferase
b. ATP synthase
43
bedaquiline resistance is due to mutations in a. pncA b. atpE c. LAM d. NAT2
b. atpE
44
nitroimidazole used in BPaL regimen a. bedaquiline b. pretomanid c. linezolid d. fluconazole
b. pretomanid
45
pretomanid is a prodrug activated by ____ a. Ddn b. PanD c. KatG d. InhA
a. Ddn (deazaflavin-dependent nitroreductase)
46
pretomanid mechanism: which of the following occurs in AEROBIC conditions? a. Forms reactive intermediate metabolite that inhibits mycolic acid production b. Generates reactive nitrogen species such as NO c. Direct poisoning of the respiratory complex -> ATP depletion d. Increases killing by innate immune system
a. Forms reactive intermediate metabolite that inhibits mycolic acid production (the others occur in anaerobic, nonreplicating, persistent bacilli)
47
second line agents: aminoglycoside, protein synthesis inhibitor a. streptomycin b. ethionamide c. para-aminosalicylic acid d. cycloserine e. capreomycin
a. streptomycin
48
second line agents: chemically related to isoniazid a. streptomycin b. ethionamide c. para-aminosalicylic acid d. cycloserine e. capreomycin
b. ethionamide
49
second line agents: -antimetabolite -folate synthesis antagonist a. streptomycin b. ethionamide c. para-aminosalicylic acid d. cycloserine e. capreomycin
c. para-aminosalicylic acid
50
second line agents: -analog of D-alanine -cell wall synthesis inhibitor a. streptomycin b. ethionamide c. para-aminosalicylic acid d. cycloserine e. capreomycin
d. cycloserine
51
second line agents: peptide protein synthesis inhibitor a. streptomycin b. ethionamide c. para-aminosalicylic acid d. cycloserine e. capreomycin
e. capreomycin

PHRM 865 Therapeutics (32 decks)

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