Antimycobacterial Drugs Flashcards

(91 cards)

1
Q

treatment of active TB

A
4 drugs- 
isoniazid
rifampin
pyrazinamide
ethambutol
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2
Q

treatment of MDR-TB

A

5-6 drugs

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3
Q

latent TB treatment

A

isoniazid or rifampin alone for 9 months

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4
Q

locations of TB drugs

A

intracellular
extracellular
cavities

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5
Q

speed of intracellular replication

A

slow

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6
Q

speed of extracellular replication

A

fast

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7
Q

speed of cavitary replication

A

slow

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8
Q

mycolic acid

A

long chain branched fatty acids in the wall

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9
Q

mycelia acid benefits

A

resist dehdyration, disinfectants, antibiotics, hide from macrophages

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10
Q

isoniazid works at

A

extra
intra
cavity

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11
Q

isoniazid is cidal or static

A

either- depends on location

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12
Q

isoniazid MOA

A

prodrug activated to nicotinoyl radical by Katg which inhibits mycolic acid synthesis by blocking InhA and KasA

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13
Q

KatG

A

mycobacterium enzyme that activates isoniazid to nicotinoyl radical

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14
Q

nicotinoyl radical

A

active form of isoniazid

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15
Q

InhA

A

acyl carrier protein reductase

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16
Q

KasA

A

acyl carrier protein synthetase

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17
Q

isoniazid resistance mechanisms

A

spontaneous resistance
KatG mutation
InhA overexpression
resistance to oxidative stress

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18
Q

isoniazid clearance

A

NAT2 aceylation in liver which is then either excreted by kidney oR converted to hydrazine by cops
acetylated and excreted

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19
Q

what increases isoniazid toxicity

A

slow acetylators

cyp inducers

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20
Q

isoniazid side effects

A

hepatotoxicity

neurotoxicity- PNS and CNS

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21
Q

prevention of isoniazid side effects

A

B6 supplements

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22
Q

isoniazid interactions

A

inhibits MAO- do not give with tyramine foods, excessive caffeine, MAOI

cyp inhibitors
alcohol

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23
Q

extracellular acting first line tb drugs

A

isoniazid
rifampin
ethambutol
streptomycin

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24
Q

intracellular acting first line tb drugs

A

isoniazid
rifampin
pyrazinamide

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25
cavity acting first line tb drugs
isoniazid rifampin ethambutol
26
rifampin acts in
intracellular extracellular cavity
27
rifampin cidal or static
cidal
28
rifampin MOA
inhibits bacterial RNA polymerase
29
rifampin resistance
RNA polymerase mutations
30
rifampin clearance
deacetylation in liver
31
specific isoniazid CNS effects
memory loss psychosis seizures
32
specific isoniazid PNS effects
paresthesia of hands/feet
33
rifampin ADR
elevated AFT- rare hepatotoxicity turns secretions red thrombocytopenia hypersensitivity rxn
34
rifampin interactions
cyp inducer- MANY drug interactions oral contraceptives warfarin protease inhibitors
35
rifapentine
same as rifampin but longer half life and fewer drug interactions
36
pyrazinamide acts where
intracellular
37
pyrazinamide cidal or static
cidal
38
pyrazinamide MOA
prodrug- converted by pyrazinamidase (bacterial deaminase) to pyrazinoic acid disrupts membrane function and transport
39
pyrazinamidase
enzyme that activates pyrazinamide
40
pyrazinoic acid
active form of pyrazinamide
41
resistance mechanism for pyrazinamide
pyrazinmidase mutation
42
elimination of pyrazinamide
kidney
43
pyrazinamide ADR
hepatotoxicity | hyperurecemia
44
most hepatotoxic first line tb
pyraziamide
45
pyramidamide interactions
none
46
ethambutol acts
extracellular | cavities
47
ethambutol MOA
inhibits arabinagalactan synthesis
48
arabinagalactan synthesis
anchor for mycolic acid
49
ethambutol resistance
mutation in target enzyme
50
ethambutol clearance
renal
51
ethambutol ADR
optic neuritis | hyperuricemia
52
hepatotoxic first line tb drugs
isoniazid | pyrazinaide
53
hyperurecemia is in what first line tb drugs
pyrazinamide | ethambutol
54
optic neuritis is in what first line tb drug
ethambutol
55
streptomycin acts wehre
extracellular
56
streptomycin cidal or static
cidal
57
streptomycin MOA
binds 30S subunit and causes mRNA misreading
58
streptomycin resistance
rRNA and protein mutations
59
streptomycin elimination
renal
60
streptomycin ADR
ototoxicity- vestibular and auditory | nephrotoxicity
61
ototoxic first line tb
streptomycin
62
nephrotoxic first line tb
streptomycin
63
weakest first line tb
ethambutol
64
neurotoxic tb drugs
isoniazid cycloserine ethioamide
65
what is given to prevent neurotoxicity
pyridoxine
66
what drugs is pyridoxine given with
isoniazid | cycloserine
67
cycloserine cidal or static
both
68
cycloserine MOA
inhibits peptidoglycan synthesis
69
cycloserine clearance
renal
70
cycloserine side effects
neurotoxicity peripheral neuropathy CNS- anxiety, depression, psychosis, memory loss, seizures
71
cycloserine contraindicated in
psychosis alcoholism epilepsy renal impairment
72
ethionamide cidal or static
both
73
ethionamide MOA
prodrug- inhibits InhA (mycolic acid synthesis)
74
ethionamide ADR
GI upset CNS toxicity- depression, sensory disturbances hepatitis
75
amino salicylic acid static or cidal
static
76
amino salicylic acid MOA
inhibits thymine nucleotide synthesis
77
aminosalicylic ADR
GI upset | hypersensitivity
78
drugs causing GI upset
Ethambumide | aminosalicylic acid
79
bedaquiline use
MDR only- with 3 other drugs known to work
80
bedaquiline moa
inhibits ATP synthase
81
bedaquiline elimi
cyp metabolism | plasma bound
82
bedaquiline ADR
QT prolongation elevated AFT headache arthalgia
83
QT prolongation
bedaquiline
84
drugs that inhibit InhA
isoniazid | ethionamide
85
leprosy drugs
rifampin | dapsone
86
length leprosy treatment
6-12 months
87
dapsone MOA
static, concentrated in infected skin inhibits folate synthesis inhibits neutrophil functioning antioxidant
88
dapsone ADR
hemolysis- severe in G6PD deficiency | methemoglobinemia
89
drug affected by G6PD decifiency
dapsone
90
drugs for MAC
rifampin ethambutol aminoglycoside
91
length of MAC treatment
12 months after first negative culture