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Block 5 > Antimycobacterial Drugs > Flashcards

Antimycobacterial Drugs Flashcards

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
Q

cavity acting first line tb drugs

A

isoniazid
rifampin
ethambutol

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26
Q

rifampin acts in

A

intracellular
extracellular
cavity

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27
Q

rifampin cidal or static

A

cidal

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28
Q

rifampin MOA

A

inhibits bacterial RNA polymerase

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29
Q

rifampin resistance

A

RNA polymerase mutations

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30
Q

rifampin clearance

A

deacetylation in liver

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31
Q

specific isoniazid CNS effects

A

memory loss
psychosis
seizures

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32
Q

specific isoniazid PNS effects

A

paresthesia of hands/feet

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33
Q

rifampin ADR

A

elevated AFT- rare hepatotoxicity
turns secretions red
thrombocytopenia
hypersensitivity rxn

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34
Q

rifampin interactions

A

cyp inducer- MANY drug interactions
oral contraceptives
warfarin
protease inhibitors

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35
Q

rifapentine

A

same as rifampin but longer half life and fewer drug interactions

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36
Q

pyrazinamide acts where

A

intracellular

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37
Q

pyrazinamide cidal or static

38
Q

pyrazinamide MOA

A

prodrug- converted by pyrazinamidase (bacterial deaminase) to pyrazinoic acid
disrupts membrane function and transport

39
Q

pyrazinamidase

A

enzyme that activates pyrazinamide

40
Q

pyrazinoic acid

A

active form of pyrazinamide

41
Q

resistance mechanism for pyrazinamide

A

pyrazinmidase mutation

42
Q

elimination of pyrazinamide

43
Q

pyrazinamide ADR

A

hepatotoxicity

hyperurecemia

44
Q

most hepatotoxic first line tb

A

pyraziamide

45
Q

pyramidamide interactions

46
Q

ethambutol acts

A

extracellular

cavities

47
Q

ethambutol MOA

A

inhibits arabinagalactan synthesis

48
Q

arabinagalactan synthesis

A

anchor for mycolic acid

49
Q

ethambutol resistance

A

mutation in target enzyme

50
Q

ethambutol clearance

51
Q

ethambutol ADR

A

optic neuritis

hyperuricemia

52
Q

hepatotoxic first line tb drugs

A

isoniazid

pyrazinaide

53
Q

hyperurecemia is in what first line tb drugs

A

pyrazinamide

ethambutol

54
Q

optic neuritis is in what first line tb drug

A

ethambutol

55
Q

streptomycin acts wehre

A

extracellular

56
Q

streptomycin cidal or static

57
Q

streptomycin MOA

A

binds 30S subunit and causes mRNA misreading

58
Q

streptomycin resistance

A

rRNA and protein mutations

59
Q

streptomycin elimination

60
Q

streptomycin ADR

A

ototoxicity- vestibular and auditory

nephrotoxicity

61
Q

ototoxic first line tb

A

streptomycin

62
Q

nephrotoxic first line tb

A

streptomycin

63
Q

weakest first line tb

A

ethambutol

64
Q

neurotoxic tb drugs

A

isoniazid
cycloserine
ethioamide

65
Q

what is given to prevent neurotoxicity

A

pyridoxine

66
Q

what drugs is pyridoxine given with

A

isoniazid

cycloserine

67
Q

cycloserine cidal or static

68
Q

cycloserine MOA

A

inhibits peptidoglycan synthesis

69
Q

cycloserine clearance

70
Q

cycloserine side effects

A

neurotoxicity
peripheral neuropathy
CNS- anxiety, depression, psychosis, memory loss, seizures

71
Q

cycloserine contraindicated in

A

psychosis
alcoholism
epilepsy
renal impairment

72
Q

ethionamide cidal or static

73
Q

ethionamide MOA

A

prodrug- inhibits InhA (mycolic acid synthesis)

74
Q

ethionamide ADR

A

GI upset
CNS toxicity- depression, sensory disturbances
hepatitis

75
Q

amino salicylic acid static or cidal

76
Q

amino salicylic acid MOA

A

inhibits thymine nucleotide synthesis

77
Q

aminosalicylic ADR

A

GI upset

hypersensitivity

78
Q

drugs causing GI upset

A

Ethambumide

aminosalicylic acid

79
Q

bedaquiline use

A

MDR only- with 3 other drugs known to work

80
Q

bedaquiline moa

A

inhibits ATP synthase

81
Q

bedaquiline elimi

A

cyp metabolism

plasma bound

82
Q

bedaquiline ADR

A

QT prolongation
elevated AFT
headache
arthalgia

83
Q

QT prolongation

A

bedaquiline

84
Q

drugs that inhibit InhA

A

isoniazid

ethionamide

85
Q

leprosy drugs

A

rifampin

dapsone

86
Q

length leprosy treatment

A

6-12 months

87
Q

dapsone MOA

A

static, concentrated in infected skin
inhibits folate synthesis
inhibits neutrophil functioning
antioxidant

88
Q

dapsone ADR

A

hemolysis- severe in G6PD deficiency

methemoglobinemia

89
Q

drug affected by G6PD decifiency

90
Q

drugs for MAC

A

rifampin
ethambutol
aminoglycoside

91
Q

length of MAC treatment

A

12 months after first negative culture

Block 5 (27 decks)

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