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Medical Pharmacology > Pharmacology of Antimycobacterial/Antiprotozoal Agents > Flashcards

Pharmacology of Antimycobacterial/Antiprotozoal Agents Flashcards

1
Q

what is RIPE for TB?

A

rifampin, isoniazid, pyrazinamide/streptomycin, ethambutol

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2
Q

MOA of rifampin

A

inhibits transcription by binding to the Beta subunit of RNA polymerase, stopping phosphodiester bone formation in RNA

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3
Q

what are the rifamycins?

A

rifampin, rifabutin, rifapentine

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4
Q

MOA of rifamycins

A

form very stable complex with RNA polymerase to prevent elongation

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5
Q

spectrum of rifamycins

A

love to kill bacteria in the phagosome, very broad including mycobacteria, not enterobacteraceae

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6
Q

resistance against rifamycins

A

spontaneous mutation of rpoB gene (rapid and predictable)

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7
Q

use of rifamycins

A

monotherapy only for prophylaxis for neisseria meningitis or h influenzae meningitis, combination therapy for TB, leprosy, bone infections, endocarditis

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8
Q

ADE rifamycins

A

potent enzyme inducer so has many drug interactions, stains body fluids red/orange

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9
Q

what is izoniazid used for

A

used only for TB

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10
Q

what activates isoniazid

A

mycobacterial catalase-peroxidase

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11
Q

how does resistance occur against isoniazid

A

inactivation of catalase peroxidase via mutation of KatG gene

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12
Q

kinetics of isoniazid

A

N acetylation and hydroxylation, food decreases absorption

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13
Q

ADE of isoniazid

A
  1. hepatitis
  2. peripheral neuropathy (prevent with B6)
  3. lupus like syndrome (because slow acetylator)
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14
Q

which drugs are N acetylators

A

dapsone (sulfonamides), hydralazine, isoniazid, procainamide
(SHIP)

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15
Q

what is SLE like syndrome

A

when N acetylators are acetylated too slow and it looks like lupus

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16
Q

what is pyrazinamide

A

TB drug that inhibits bacterial FA synthetase I and reduce pH

rapidly cidal

ADE: hepatitis, gout, hematologic toxicity

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17
Q

what is streptomycin

A

aminoglycoside inhibition of protein via binding to 30S, misreading

ADE: nephrotoxic, ototoxic, neuromuscular blockade (not hepato!)

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18
Q

what is ethambutol

A

for TB and mycobacterium avium intracellulare (MAC)

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19
Q

MOA ethambutol

A

inhibits arabinosyl transferase, interfering with cell wall synthesis

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20
Q

ADE ethambutol

A

check to see colorblindness BEFORE, optic neuritis, colorblindness, hepatitis

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21
Q

what is used for intensive TB tx

A

2 months of RIPE

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22
Q

what is used for continuation phase for TB tx

A

4 months of INH plus rifampin

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23
Q

when to treat for TB

A
  1. 5mm induration with HIV, recent contact, old TB, organ transplant, immunocompromised
  2. 10mm induration IV drug user, recent immigrants, residents and employees of nursing homes, hospitals, correctional facility etc
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24
Q

what to use to treat latent TB?

A

isoniazid

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25
what is MAC (mycobacterium avius intracellulare)
opportunistic pathogen in HIV most commonly seen when CD4 less than 50.
26
prophylaxis for MAC
azithromycin or clarithromycin
27
treatment for MAC
azithromycin or clarithromycin plus ethambutol and rifabutin
28
how to treat mycobacterium leprae
dapsone rifampin clofazimine thalidomide
29
what does dapsone do
inhibits dihydropterate synthetase (loss mycobacterial folate)
30
ADE dapsone
hemolysis in G6PD
31
what is clofazimine
phenazine dye that reduces the risk of erythema nodosum leprosum
32
what is thalidomide
treats erythema nodosum leprosum, multiple myeloma and mycobacterial infections -- also teratogenic
33
what is metronidazole used for
extraluminal amebiasis (kills trophozoites of enteramoeba histolytica . also trichomoniasis also giardia also c diff but not anymore
34
what activates metronidazole
pyruvate ferredoxin oxireductase (PFOR) to its active reduced form, bind DNA and proteins, leading to microbial death
35
ade metronidazole
disulfram reaction
36
what is most responsible for complications for malaria?
p falciparum (complications, death and drug resistance_
37
malaria prophylaxis
prevent mosquito bites! increasing resistance means no chemoprophylactics are completely protective.
38
what eradicates the hypnozoites from p vivax and ovale?
primaquine
39
what do tissue schizonticides do
eliminate developing or dormant liver forms
40
what do blood schizonticides do
act on erythrocytic parasites
41
what do gametocides do
kill sexual stages to prevent transmission to mosquitos
42
what does primaquine do
prevents relapses of vivax and ovale by killing hypnozoites -- does not work on eyrthrocytic form
43
when does primaquine reach peak?
1-2 hours
44
ADE of primaquine
causes hemolytic anemia in G6PD , cannot be used in pregnancy
45
which drugs cannot be used with G6PD
sulfonamides (dapsone) primaquine nitrofurantoin
46
benefits of primaquine
good for last minute travelers bc started 1-2days before. also most effective for vivax so good for travel where there is 90%+ vivax
47
drawback of primaquine
no G6PD, not used for pregnant women | take it every day
48
effectiveness of chloroquine
highly effective blood schizonticide, moderate against gametocyte of vivax, ovale, malariae, NOT falciparum
49
drawback of chloroquine
resistance is common in falciparum
50
advantage of chloroquine
taken weekly, can take if pregnant, good for long trips bc taken weekly
51
disadvantage of chloroquine
cannot be used in areas with chloroquine or mefloquine resistance, may exacerbate psoriasis, must be started 1-2weeks before travel and taken 4 weeks after
52
action of atovaquone and proguanil
atovaquone: disrupts mitochondrial electron transport proguanil: converted to active metabolite that inhibits plasmodial dihydrofolate reductase ARE ACTIVE AGAINST TISSUE AND ERYTHROCYTIC SCHIZONTS allowing chemo to be stopped 1 week after end of exposure
53
benefit of atovaquone and proguanil
good for last min bc take 1-2days before, good for shorter trips bc taking only 1 week after traveling.
54
drawback of atovaquone and proguanil
expensive, cannot be used by pregnant
55
what is mefloquine
effective single agent for prophylaxis and treatment of infections caused by multidrug resistant forms of p falciparum strong blood schizonticidal but not hepatic or gametocytes
56
half life of mefloquine
20 days -- weekly dosing, steady state over a number of WEEKS
57
ade mefloquine
boxed warning of neuro and pyschiatric toxicities (appear in 50%) don't use with hx of epilepsy, psych disorders, arrythmia, cardiac conduction defects
58
benefit of mefloquine
good for long trips because 1 weekly, can be used in pregnancy
59
drawback mefloquine
not good for last minute, needs to be started at least 2 weeks before. must take 4 weeks after so not good for short trips.
60
what is quinine
gametocidal against vivax and ovale not falciparum
61
ADE quinine
tinnitus, HA, nausea, dizziness, flushing, visual disturbances == called cinchonism
62
when is primethamine used
not widely used because of frequent resistance and toxicity
63
what antibiotics are used for erythrocytic schizonts?
tetracycline and doxycycline, doxy has become standard chemoprophylactic esp in areas with high rates of resistance
64
why is doxycycline good for travelers
last minute is good bc only 1-2 days before leaving, least expensive
65
drawback of doxycycline
cannot use when pregnant
66
what is nitazoxanide used for
giardia and cryptosporidium parvum

Medical Pharmacology (13 decks)

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