41: antimycobacterial Flashcards

1
Q

KatG gene mutation results in resistance to?

A

isoniazid

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2
Q

mycolic acid synthesis inhibition is MoA of?

A

isoniazid

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3
Q

1st line drugs for M TB? (4)

A

isoniazid
rifampin
pyrazinamide
ethambutol

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4
Q

RoA of Isoniazid

A

oral or parenteral (IM)

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5
Q

If isoniazid resistance is observed what can we use?

A

rifampin

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6
Q

which 1st line mycobacterial drugs has bacteriostatic action?

A

ethambutol

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7
Q

INH prophylaxis is given to?

A

in person with positive tuberculin skin test who meets the criteria:

  1. HIV +
  2. recently infected
  3. X ray shows nonprogressive TB
  4. illicit injected drug use
  5. DM
  6. immunosuppression
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8
Q

which drug is activated by mycobacterial catalase-peroxidase

A

isoniazid

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9
Q

isoniazid is active against which mycobacteria?

A

M tb

M kansasii

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10
Q

which antimycobacterial drugs are metabolized by acetylation? (2)

A

isoniazid

dapsone

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11
Q

vitamin B6 deficiency is observed as adverse effect of ? (2)

A

isoniazid

dapsone

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12
Q

peripheral neuritis in isoniazid is more likely seen in which phenotype ?

A

slow acetylators

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13
Q

to prevent peripheral neuritis we can supplement?

A

vitamin B6 - pyridoxine

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14
Q

RoA of rifampin

A

oral , IV

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15
Q

MoA of ethambutol

A

Inhibit arabinosyl transferase and synthesis of arabinogalactan for cell wall.

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16
Q

resistance to ethambutol is gained by mutations in:

A

arabinosyl transferase.

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17
Q

adverse effect of ethambutol?

A

Optic neuritis, Impaired red-green color discrimination.
Hyperuricemia; GOUT.
Hepatitis and thrombocytopenia.

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18
Q

contraindication for ethambutol?

A

children too young to asses visual acuity

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19
Q

ethambutol is active against which mycobacteria?

A

M tb

MAI

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20
Q

treatment regimen for MAI?

A

Treatment: azithro/clarithromycin + ethambutol +/- rifabutin

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21
Q

incase if resistance to rifampin we use?

A

rifabutin

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22
Q

which antimycobacterial agent is more rapidly bactericidal than others, and has sterilizing effect?

A

pyrazinamide

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23
Q

which agent is a nicotinamide derivative?

A

pyrazinamide

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24
Q

2 known mechanisms of action of pyrazinamide

A
  1. inhibition of fatty acid syntesis

2. inhibits ribosomal translation of mRNA

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25
Q

inhibition of ribosomal mRNA , mechanism of pyrazinamide helps it to kill _____ TB?

A

dormant (nongrowing)

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26
Q

RoA of pyrazinamide

A

oral

27
Q

mutation of which enzyme results in resistance to pyrazinamide?

A

pyrazinamidase

28
Q

adverse effects of pyrazinamide

A
Arthralgia.
Hyperuricemia
gout.
Hematologic toxicity.
Hepatitis 
increase in serum iron concentration.
29
Q

pyrazinamide is bactericidal or bacteriostatic?

A

bactericidal

30
Q

which first line mycobacterial is broad spectrum?

A

rifampin

31
Q

rifampin is active against which Mycobacteria?

A

M tb
MAI
M kansasii
M leprae

32
Q

MoA of rifampin

A

: binds to B-subunit (of DNA dependent RNA polymerase) → inhibits DNA transcription and RNA synthesis

33
Q

clinical indications of rifampin? (

A
  1. TB
  2. leprosy
  3. TB meningitis
  4. prophylaxis (INH alternative, exposure to H influenza , prevent meningococcal disease)
  5. eliminate staphylococcal carriage
  6. treat staph infections: endocarditis
  7. occasionally: legionella pneumophila
34
Q

which drug is used in treatment of lepromatous leprosy but not for tuberculoid leprosy?

A

clofazimine

35
Q

regimen for leprosy? (3)

A

dapsone + clofazimine + rifampin

36
Q

resistance to rifampin is gained by which mechanism?

A

decreased affinity of RNA polymerase to drug

37
Q

reddish orange to brown discoloration of saliva, tears, urine is adverse effect of?

A

rifampin

- also causes permenant staining of contact lenses

38
Q

which 1st line antimycobacterial agent causes hepatotoxicity and nephrotoxicity?

A

rifampin

  • hepatitis
  • cholestatic jaundice
  • acute intersitial nephritis
  • light-chain proteinuria
39
Q

rifampins drug interactions are:

A

Macrolides - Benzodiazepines - Calcium channel blocker
Digoxin - Estrogens - Sulfonylureas - Theophylline
Warfarin

40
Q

long acting rifamycin derivative is called?

A

rifapentine

41
Q

highly lipophillic derivative of rifamycin? (take with food to avoid irritation)

A

rifabutin

42
Q

if HIV patient is on protease inhibitor, which drug is preffered to use in MTB regiment?

A

rifabutin

43
Q

TB aminoglycosides are?

A

amikacin
kanamycin
streptomycin

44
Q

which aminoglycoside for M TB treatment is contraindicated in pregnant women?

A

streptomycin

45
Q

ROA of M tb aminoglycosides?

A

parenteral

46
Q

which aminoglycoside is more active than streptomycin?

A

amikacin

47
Q

MoA of Bedaquiline?

A

acts by blocking proton pump for ATP synthase in M tb

48
Q

bedaquiline is approved for treating?

A

MDR TB

49
Q

which antimycobacterial agent prolongs QT interval? and what should u consider doing before taking drug?

A

bedaquiline

perform ECG before taking drug

50
Q

sulfones MoA?

A

same as sulfonazmide: inhibit dehydropteorate synthase –> inhibits folic acid synthesis

51
Q

dapsone belongs to which class of drugs?

A

sulfones

52
Q

in patient with G6PDH deficiency which drug can cause an adverse effect?

A

dapsone, can cause hemolytic anemia

53
Q

adverse effects of dapsone ? (7)

A
  1. gi disturbance
  2. peripheral neuropathy
  3. optic neuritis, blurred vision
  4. proteinuria, nephrotic syndrome
  5. lupus erythematous-like syndrome
  6. hematologic toxicity
  7. G6PDH def –> hemolytic anemia
54
Q

which antibiotic has antimycobacterial and antiinflammatory effects?

A

clofazimine

55
Q

clofazimine is bacteriostatic against which mycobacteria and bacteriocidal against which?

A

bacteriostatic –> M leprae
bactericidal –> M tb

remember: is also acitive against MAI

56
Q

half life of clodazimine?

A

70 days

57
Q

if i say phenazine dye, what comes to ur mind?

A

clofazimine

58
Q

photosensitivity and hepatitis, also discoloration of body secretions are adverse effects of?

A

clofazimine

59
Q

clinical indications of clofazmine?

A
  1. lepromatous leprosy (used with dapsone and rifampin)

2. erythema nodosum leprosum - due to its inflammatory effects

60
Q

which drug was banned due to phocomelia in offsprings of women who took drug during pregnancy?

A

thalidomide

61
Q

which drug has orphan status?

A

thalidomide

62
Q

which antimycobacterial drug is also used for legionella pneumophila ?

A

rifampin

63
Q

for treatment of prosthetic valve endocarditis we use rifampin in combination with?

A

gentamicin / vancomycin

64
Q

rifampin is used in prevention of meningococcal disease , but the preffered drugs for this are?

A

ceftriaxone / ciprofloxacin