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Block 3 Pharm > Antiparasitics > Flashcards

Antiparasitics Flashcards

1
Q

Random US parasites

A 
Helminth infections in over 1 million
Toxocara (roundworms) from dogs and cas are 14%pop
malaria~2000 year
trichonomas vag~ 3 million
Giardia: 10% population
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2
Q

Infection of parasites associated with

A

poor economic conditions

encysted tapes in 25% inner city children and leading cause of seizures in kinds in hispanice

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3
Q

Cure vs control

A

have to eradicate several staes of parasite in host

-enZ unique to host and indespendible only to parasite

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4
Q

Nematode (roundworm) cycle

A

see eggs in feces–> then will hatch into a filiraform to pentrate skin and hang in our small intestine

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5
Q

Damages microtulbes
inhibits glycogen uptake
can’t move or get E… DEATH you nasty roundworm!

A

Mebendazole

mictrotubule destruction… now they can get glycogen and they can’t move!

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6
Q

effective for many intestinal roundworms and kills some ova… damages microtubules

A

Mebendazole

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7
Q

Use of Mebendazole

A

kills intestinal roundworms and some ova

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8
Q

Absorption of Mebendazole

A

low systemic bioavailability = low systemic toxicity

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9
Q

Albendazole uses

A

Echinococcus or cuteanous larval migrans and neurocystocerosis d/t Taenia solium

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10
Q

Used for echinoccosus or cutaneous larval migrans or neurocysticercosis due to Taenia solium

A

Albendazole

EICK.. they’re all bendy under my skin and in my BRAIN!

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11
Q

same as mebendazole, liver –>albendazole sulfoxide (active)
good systemic distribution

A

Albendaozle

EICK.. they’re all bendy uder my skin and in my BRAIN!

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12
Q

How is albendazole differenet from mebendazole

A

converted quickly be liver to active form for better distribution which is why is

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13
Q

Mech of Albendazole in depth

A

fuck with microtubules
inhibits glucose uptake
can’t get food or move = die

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14
Q

What is special about albendazole metabolite

A

more activated by liver and great distribution

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15
Q

Side effects of Albendazole

A

duh.. elevates hepatic enZ bc converted in liver… and makes tummy hurt

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16
Q

affects energy metabolism via inhibition of mitochondrial fumarate reductase in HOOKWORMS

A

Thiabendazole

tHiabendazole has an H… hookworms

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17
Q

MEch of Thiabendazole for HOOKWORMS

I’d be FUMING if i had hookworms

A

affects E metabolism
inhibiting mitochondiral fumarate reductase in hookworms
(I’ld be FUMING if i had hookworms)

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18
Q

Mech of Thiabendazole for Strongyloidesl

A

inhibits assembly of parasitic microtubules.

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19
Q

Thiabendazole uses:

A

Strongyoids

cuteanous larva migrans from dog or cat hookworms

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20
Q

Strongyloides

cuteanous larva migrans from dog or cat hookworms

A

Thiabendazole

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21
Q

absorption of Thiabendazole

A

oral form rapidly absorbed

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22
Q

side effects of thiabendazole

A

nauseua, vomit, dizzy

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23
Q

Pyrantel Pamoate mechanism

A

depolarizing neuromuscular blocker, causing spastic paralysis of worm
Pyrantel Pamoate causes dePPPPPolarization and PPPPParalysis

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24
Q

uses of Pyrantel Pamoate

A

hookworm, pinworm, roundworm

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25
Q

increase Ca++ permeability.. causes muslce cnx… spastic paralysis

A

Praziquantel causes PPPPPPermeability

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26
Q

Mech of Praziquantel

A

increase Ca++ permeability.. causes muslce cnx… spastic paralysis
(PPPPPraziquantel… increase PPPPermeability)

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27
Q

drug of choice for Schisotosoma

A

Praziquantel

I pray this Schits over soon”

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28
Q

Use of Praziquantel

A

Schistosomiasis (also for taneia solium to prevent neurocysteriocorcosis)

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29
Q

Tape worm drugs

A

Praziquantel, Albendazole, Paromomycin sulfate

30
Q

good activity for schistosomiasis but also for tania solium bc kills eggs to you can avoid cysticercosis

A

Praziquantel

31
Q

Used to treat neurocysticercosis

A

Albendazole (be careful in poeople with seizures)

32
Q

Used as 3rd choice for those that don’t tolerate Praziquantel or Albendazole for tapeworms

A

Paromomycin sulfate

“MOM.. i have tape worms”

33
Q

Key with anti-malarials

A

don’t prevent infection.. they only prevent progression to symptomatic malaira

34
Q

____ in mosquito salivary gland are injected into human blood

A

Sporozoites

35
Q

Exoerythrocytic stage—

A

sporozoites multiply in liver to form tissue schizonts

36
Q

Escape from liver into bloodstream as_____, which begins the erythrocytic stage; the merozoites invade red blood cells and multiply in them to form

A

merozoites

blood schizonts

37
Q

Infected erythrocytes eventually rupture releasing a new crop of ______ this erythrocytic cycle may be repeated several times

A

merozoites;

38
Q

What form are we always going to target with anti-malarial drugs

A

always the blood schizonts

39
Q

• have only one cycle of liver cell invasion and multiplication (liver infection ceases
spontaneously in

A

P. falciparum and P. malariae

40
Q

have dormant hepatic stage (hypnozoite) that can cause relapses
• treatment requires elimination from both the liver and blood

A

P. vivax and P. ovale •

Liver has 5 letters and so do these malaria

41
Q

Blood schizonticide:

parazitized erythrocytes concentrate the drug 25 fold by pH dependent mechanism into acidic vacuoles

A

Chloroquine

(think chloride because its negatve and will go to low pH

42
Q

which trophozoites are suspeptible to Chloroquine (quine sounds like 4… all are suspetible and stops heme quads!)

A

ones actvely degrading hemaglobin… the chloroquine inhibits heme polymerization and the heme accumulate to toxic levels === death!

43
Q

Use of Chloroquine

A

all 4 species

will eradiate P. malariae and P. falciparum but wont cure P. vivax and ovale (still have liver form)

44
Q

Tx all 4 species

will eradiate P. malariae and P. falciparum but wont cure P. vivax and ovale (still have liver form)

A

Chloroquine

careful for P.falciparum resistance

45
Q

Side effect of chloroquine

A

visual impairment

chloroquine… 4 eyes!!!! b’c quine sounds like quad… also for all four… alsp think stops heme from going to 4

46
Q

Mech of Mefloquine

A

sim to chloroquine

47
Q

use to tx chloroquine resistant P.falciparum and P.vivax and as prophylaxsis in chloroquine resistant areas

A

Mefloquine

48
Q

What pts should not recieve mefloquine

A

pts with eplilepsy or pychiatric disorders

49
Q

Black box warning for Mefloquine

A

psychiatric effects like anxiety, paranoa and depression as well as vestibular effects
“Me-floquine will make ME crazy!”

50
Q

◊ ubiquinone analog
inhibits malarial mitochondrial election transport ~ cyt bc1
fucks up pyrimdine synthesis

A

atovaquone

51
Q

prodrug activated by hepatic CYP2C9 to inhibi malarial dihydrofolate reductase to block folate synthesis— pyrimidine synthesis

A

Proguanil

“pro as in prodrug”

52
Q

These two will inhibit protozoal pyrimidine synthesis

A

Atovaquone

Proguanil

53
Q

Mech of Atovaquone

think ABC’s~~~ goes A for atovaquone and BC for cyctochorm BC1

A

ubiquinone analog
inhibits malarial mitochondrial ETC by disrupting Cyt BC1
Fucks up their pyrimidine sythesis

54
Q

Mech of Proguanil

A

prodrug activated by hepatic CYP2C9

inhibits malarial dihydrofolate reductase block folate synthesis— pyrimidine synthesis

55
Q

Why do we use Proguanil and atovaquone together for chloroquine resistant P.falciparum

A

because synergistic effect on mitochondria when given together and fewer side effects

56
Q

Mech of quinine

A

similar to chloroquine
RBC infected with parasites…inside acidic vacuoles which concentrates the drug. The drug prevents the hemes that the trophazoites are degrading from polymerizing into a toxic free heme… build up toxic heme = death

57
Q

Uses of Quinine

A

Schizonticide for all four

alternative for P.Falciparum resistant to Chloroquine

58
Q

similar to chloroquine
RBC infected with parasites…inside acidic vacuoles which concentrates the drug. The drug prevents the hemes that the trophazoites are degrading from polymerizing into a toxic free heme… build up toxic heme = death

A

Quinine and Mefloquine

Diff side effects

59
Q

Both Quinine and Mefloquine are alt for Chloroquine reistant P. Falciparum, whats the differece

A

Mefloquine: black box on pyschiatric issues and epilepsy
Quinine: Cinchonism, cardiate effects simular to qunidine or nausea

60
Q

Side effects of quinine

A

cinchonism: headache, visual disturbance, dizziness, tinnitus
GI
cardiac effects similar to quinidine

61
Q

cinchonism: headache, visual disturbance, dizziness, tinnitus
gastric irritation, nausea, vomiting
cardiac effects similar to quinidine

A

sides for quinine

62
Q

Doxycycline mech

A

depress dihydroorotate
dehydrogenase activity,
can’t make pyrimidines

63
Q

fucks with dihydroorotate DH activity

then the malaria can’t make pyrimides

A

Mech of Doxycycline
“Doxy got all those D’s
Dihidroorotase DH”

64
Q

effective for multidrug-resistant P. falciparum, especially in combination with quinine
• also for malarial prophylaxis

A

Doxyclycine

65
Q

Drug to kill liver hypnoschizots

A

Primaquine

66
Q

Mechanism of Primaquine

A

act as oxidants will kill liver hypnozoites

67
Q

radical cure or terminal prophylaxis of P. vivax and P. ovale because it will kill dormant liver schizonts; usually given at end of therapy with chloroquine; for travelers to malarious regions, primaquine is usually given after return home

A

Primaquine

68
Q

radical cure for P. vivax and P. ovale and used with drugs to kill blood schizonts

A

Primaquine

69
Q

Drug can also be used to tx Pneumocystisi jiroveci pneumonia in AIDS pts

A

Primaquine

70
Q

uses of Primaquine

A

liver schizonts: P. vivax and P. ovale and pneumocystis jirovveci

71
Q

Side effects of primaquine

A

hemolytic rxns in those with G6P DH deficiency

72
Q

see hemolytic rnx in those with GP6 deficiency

A

Primaquine

Block 3 Pharm (19 decks)

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