anti-mycobacterial drugs Flashcards

1
Q

Which drugs are used to treat mycobacterial infections?

A
isoniazid
Pyrazinamide
ethambutol
rifampin/rifabutin
clofazimine
dapson
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2
Q

which drugs interfere with mycolic acid synthesis

A

isoniazid
pyrazinamide
ethambutol

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3
Q

which drugs interfere with DNA dependent RNA pol?

A

rifampin/rifabutin

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4
Q

which drug interferes with DNA template function

A

clofazimine

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5
Q

which drug inhibits DH synthase

A

dapsone

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6
Q

what is the treatment plan for M tuberculosis

A

6 month plan =
2 months isoniazid and rifampin, pyrazinamide
4 additional months isoniazid and rifampin

9 month plan =
isoniazid + rifampin

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7
Q

what is the treatment plan for M kansasii (pneumonia)

A

isoniazid + rifampin + ethambutol

treat until you have 12 months of negative sputum

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8
Q

what is the treatment plan for M avium complex (MAC) (pneumonia)

A

clarithromycin or azithromycin + ethambutanol +/- rifabutin

treat until six months after negative sputum

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9
Q

what is the treatment for M leprae

A

dapsone + rifampin +/- clofazimine

treatment for a min of 2 years

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10
Q

what is the treatment for M fortuitum

A

amikacin (aminoglycoside) + doxycycline (tetracycline)
4 months for cutaneous
6 months for bone
12 months for lungs

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11
Q

what is the treatment for M marinum

A

rifamin + ethambutol

3 months

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12
Q

isoniazid - mechanism

A

inhibits mycolic acid
bactericidal during long growth phase
bacteriostatic in resting organisms

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13
Q

what is mycolic acid?

A

a unique component of mycobacterial cell wall

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14
Q

isoniazid - side efects

A
hepatotoxicity (increases with age)
peripheral neuritis (B6 given for prevention)
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15
Q

pyrazinamide - mechanism

A

inhibits mycolic acid synthesis

bactericidal

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16
Q

proposed mechanism for inhibition of mycolic acid synthesis

A

target fatty acid synthase I gene

except ethambutol - inhibits use of mycolic acid in cell wall synth

17
Q

pyrazinamide - side effects

A

dose related hepatits

should only be used for short therapy; monitor liver function

18
Q

ethambutol - mechainsm

A

interferes with mycolic acid

  • inhibits incorporation of mycolic acid into cell wall
  • bacteriostatic
19
Q

ethambutol - side effect

A
optical neuritis (visual acuity and red/green discrimination)
-dont use in children under 5

also rare side effect is gout due to inhibition of excretion of uric acid

20
Q

ethambutol - excretion

A

renal

dose adjustment may be necessary - accumulation can happen in patients with impaired function

21
Q

rifampin/rifabutin - mechanism

A

DNA dep RNA polymerase - inhibits

eukaryotic RNA pol is less sensitive to rifampin because of binding affinity differences so it is safe to use

22
Q

rifampin/rifabutin - side effects

A

rifampin - substrate and inducer for CYP3A4
rifabutin is not as potent of an inducer

rifampin reduces HIV protease inhibitor levels by 80% - patients need to be switched to rifabutin (decreases by 20-40%)

also turns saliva, urine, tears orange-red

23
Q

clofazimine - mechanismm

A

inhibits template function of DNA

binds to DNA and inhibits function

24
Q

clofazimine - excretion

A

hepatic, to feces

little is excreted in the urine

25
Q

clofazimine - side effect

A

brownish pink coloring of skin, cornea, urine

26
Q

dapsone - mechanism

A
inhibits DH (dihydropterate) synthease
interferes in folic acid synthesis

dapsone is a sulfone so mechanism is like other sulfonamides

27
Q

dapsone - side effect

A

similar to sulfonamides

  • anorexia, nausea
  • hemolytic anemia is rare but more frequent in individuals with G6PDH deficiency
  • sulfone syndrome (rare)
28
Q

which drugs cause hepatotoxicity?

A

isoniazid

pyrazinamid

29
Q

which drug should you not use in pregnant patients?

A

clofazimine

30
Q

which drug can cause hemolytic anemia in G6PDH deficient patients

A

dapsone