Flashcards in Antimycobacterial Drugs Deck (91):
1
treatment of active TB
4 drugs-
isoniazid
rifampin
pyrazinamide
ethambutol
2
treatment of MDR-TB
5-6 drugs
3
latent TB treatment
isoniazid or rifampin alone for 9 months
4
locations of TB drugs
intracellular
extracellular
cavities
5
speed of intracellular replication
slow
6
speed of extracellular replication
fast
7
speed of cavitary replication
slow
8
mycolic acid
long chain branched fatty acids in the wall
9
mycelia acid benefits
resist dehdyration, disinfectants, antibiotics, hide from macrophages
10
isoniazid works at
extra
intra
cavity
11
isoniazid is cidal or static
either- depends on location
12
isoniazid MOA
prodrug activated to nicotinoyl radical by Katg which inhibits mycolic acid synthesis by blocking InhA and KasA
13
KatG
mycobacterium enzyme that activates isoniazid to nicotinoyl radical
14
nicotinoyl radical
active form of isoniazid
15
InhA
acyl carrier protein reductase
16
KasA
acyl carrier protein synthetase
17
isoniazid resistance mechanisms
spontaneous resistance
KatG mutation
InhA overexpression
resistance to oxidative stress
18
isoniazid clearance
NAT2 aceylation in liver which is then either excreted by kidney oR converted to hydrazine by cops
acetylated and excreted
19
what increases isoniazid toxicity
slow acetylators
cyp inducers
20
isoniazid side effects
hepatotoxicity
neurotoxicity- PNS and CNS
21
prevention of isoniazid side effects
B6 supplements
22
isoniazid interactions
inhibits MAO- do not give with tyramine foods, excessive caffeine, MAOI
cyp inhibitors
alcohol
23
extracellular acting first line tb drugs
isoniazid
rifampin
ethambutol
streptomycin
24
intracellular acting first line tb drugs
isoniazid
rifampin
pyrazinamide
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