Antimycobacterial Drugs Flashcards Preview

Block 5 > Antimycobacterial Drugs > Flashcards

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

length of MAC treatment

12 months after first negative culture