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Antimycobacterial drugs Flashcards

(54 cards)

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1
Q

first line drugs for tuberculosis

A

rifampin
pyrazinamide
ethambutol
isoniazid

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2
Q

second line drugs for tuberculosis

A 
rifabutin
rifapentine
fluoroquinolone
capreomycine
ethionamide
amikacin
kanamycin
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3
Q

ISONIAZID ROA

A

oral

parenterally

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4
Q

isoniazid MOA

A

inhibit synthesis of mycolic acid

activated by catalase-peroxidase encoded by KatG gene

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5
Q

resistance to isoniazid

A

mutation of the KatG gene

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6
Q

isoniazid bactericidal or bacteriostatic?

A

bactericidal

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7
Q

isoniazid indication

A

bactericidal - M. tuberculosis and M.kansasii
M. avium-intracellulare
LATENT TB
prevent TB in neonates and children in close contact
prophylaxis: if + for tuberculin, HIV+ and recent exposure

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8
Q

AE isoniazid

A

Hepatitis (age dependent)
Peripheral neuritis: drug induced pyridoxine deficiency (B6) (paresthesia, numb finger and toe)
RARE: toxic encephalopathy and hematologic; granulocytosis, anemia, thrombocytopenia

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9
Q

ETHAMBUTOL bactericidal or bacteriostatic?

A

bacteriostatic

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10
Q

ethambutol roa

A

orally (w other drugs TB and M. AI

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11
Q

ethambutol moa

A

inhibit arabinosyl transferase and synthesis of arabinogalactan for cell wall

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12
Q

ethambutol resistance

A

mutation in arabinosyl transferase

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13
Q

AE ethambutol

A

Optic neuritis
impaired green-red color discrimination (retrobulbar neuritis)
CI in children to young to assess visual activity)
hyperuricemia, GOUT
hepatitis, thrombocytopenia

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14
Q

Pyrazinamide bactericidal or bacteriostatic?

A

bactericidal

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15
Q

pyrazinamide moa

A

orally given for M.TB, given in combination with isoniazid, ethambutol and rifampin

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16
Q

pyrazinamide MOA

A

nicotinamide derivative, converted in mycobacteria to active metabolite pyrazinoic acid by pyrazinamidase

inhibit fatty acid synthesis and translation

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17
Q

pyrazinamide resistance

A

mutation in pyrazinamidase

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18
Q

pyrazinamide AE

A

arthralgia
hyperuricemia and gout
hematologic toxicity
hepatitis and increase in serum ion concentration

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19
Q

pyrazinamide contraindicated

A

in pregnant women

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20
Q

Rifampin - broad or narrow spectrum?

A

broad

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21
Q

rifampin ROA

A

oral/IV

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22
Q

rifampin MET

Study These Flashcards
A

converted in the liver after oral administration to active desacetyl - rifampin. widely distributed to tissue and fluid.
enterohepatic cycling

23
Q

rifampin indications

Study These Flashcards
A

M.TB -> rifampin, isoniazid, ethambutol and pyrazinamide
M.kansasii
M.AI
M.leprae
Tubercular meningitis
Latent TB (alterative isoniazid)
Prevent; exposed to H.influenza, who can transmit to children under 4 unvaccinated
Meningococcal disease - in those close contact
treat - Legionella pneumophila with macrolide or fluoroquinolone

24
Q

Rifampin MOA

Study These Flashcards
A

binds to B subunit of DNA - dependent RNA polymerase, inhibit transcription

25
Rifampin resistance
decreased affinity of RNA polymerase. NEVER USE ALONE
26
rifampin AE
hepatitis (don't drink alcohol) hypersensitivity, fluelike illness w chills (large doses) nephrotoxicity (light chain proteinuria) discontinue if purpura develops reddish-orange-brown discoloration of SALIVA; TEAR; UriNE induces cytochrome P450; accelerate metabolism of other drugs -> macrolides, benzodiazepines, calcium blocker, digoxin, sulfonylureas, theophylline, warfarin, estrogen
27
Rifapentine - what is it derived from?
derived from rifamycin
28
rifapentine - indication
pulmonary TB by M.TB
29
2 phase regimens rifapentine
twice weekly rifapentine w isoniazid, ethambutol ad pyrazinamide for 2 months for 4 months rifapentine and isoniazid
30
rifabutin MOA
inhibit DNA dependent RNA polymerase
31
rifabutin indication
Treat TB in HIV infected (not rifampin, cannot use w protease inhibitor) prevent M.avium-intracellulare infection
32
rifabutin ROA
orally w food, to avoid irritation (lipophilic)
33
rifabutin AE
induce cytochrome P450
34
bedaquiline note
can be given orally one daily for 2w and 3 w for 22 weeks. should be given in common w at least 3 other drugs to which patients isolate is susceptible
35
bedaquiline MOA
blocking proton pump for ATP synthase in M.TB
36
bedaquiline indication
MDR-TB
37
bedaquiline ROA
orally
38
bedaquiline AE
electrocardiogram bf starting, and at regular intervals after prolonged QT; arrhythmia and sudden death: block of depolarizing K+ channels advese liver reaction interacts with cytochrome P450: mentoring!! e.g rifampin reduces bed aquiline, so montoring needed monitor electrocardiogram, liver reaction and CYP450
39
drugs for m. avian intracellular infection
ethambutol, rifampin, rifabutin azithromycin, clarithromycin ciprofloxacin
40
used to prevent MAC infections in HIV/ immunocompetent patients
azithromycin, clarithromycin and rifabutin | CAR
41
drugs combined to use for MAC
pulmonary and other MAC infections: azithromycin, ethambutol, rifabutin or rifampin (rifabutin if immunocompromised) 16-24 weeks
42
alternative for MAC in immunocompromised
clofazimine + streptomycin (contraindicated in pregnant women)/ amikacin
43
drugs for leprosy
MD therapy indicated
44
sulfones (dapsone) MOA
inhibit synthesis of folic acid by M.leprae (BACTERIOSTATIC)
45
sulfones (dapsone) ROA
orally w other drugs
46
sulfones (dapsone) AE
glucose 6 - phosphate deficiency - hemolytic anemia gastrointestinal disturbances peripheral neuropathy optic neuritis and blurred vision proteinuria, nephrotic syndrome, SLE like syndrome
47
sulfones (dapsone) MET
metabolized by acetylation. so people with high levels of acetyl-transferase activity have low level of drug
48
Rifampin
great bactericidal activity agains M.leprae combined w dapsone or dapsone+clofazimine
49
Clofazimine - facts
antimycobacterial and antiinflammatory effects enhances phagocytic activity of neutrons and macro penzydine dye
50
clofazimine - indications
bacteriocidal - M.TB bacteriostatic - M.leprae active - M.AI
51
Lepromatous leprosy
Clofazimine in combo w dapsone and rifampin antiinflammatory tuberculoid leprosy -> dapsone + rifampin
52
Clofazimine MET
slowly and incompletely absorbed from gut | highly lipophilic and widely distributed to tissues 70 days half-life
53
Clofazimine AE
Gi distress Photosensitivity Discoloration of body secretion and skin Hepatitis so contraindicated in hepatic disease
54
Thalidomide
phocomelia immunomodulating actions orphan drug - TB, leprosy, erythema nodosum leprosum ability to stimulate Tcells (CD8+)

test 1 (2 decks)

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