Antiparasitics Flashcards by Meghan May

Random US parasites

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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Infection of parasites associated with

poor economic conditions

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

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Cure vs control

have to eradicate several staes of parasite in host

-enZ unique to host and indespendible only to parasite

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Nematode (roundworm) cycle

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

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

Mebendazole

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

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

Mebendazole

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Use of Mebendazole

kills intestinal roundworms and some ova

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Absorption of Mebendazole

low systemic bioavailability = low systemic toxicity

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Albendazole uses

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

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

Albendazole

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

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

Albendaozle

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

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How is albendazole differenet from mebendazole

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

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Mech of Albendazole in depth

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

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What is special about albendazole metabolite

more activated by liver and great distribution

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Side effects of Albendazole

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

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affects energy metabolism via inhibition of mitochondrial fumarate reductase in HOOKWORMS

Thiabendazole

tHiabendazole has an H… hookworms

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MEch of Thiabendazole for HOOKWORMS

I’d be FUMING if i had hookworms

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

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Mech of Thiabendazole for Strongyloidesl

inhibits assembly of parasitic microtubules.

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Thiabendazole uses:

Strongyoids

cuteanous larva migrans from dog or cat hookworms

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Strongyloides

cuteanous larva migrans from dog or cat hookworms

Thiabendazole

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absorption of Thiabendazole

oral form rapidly absorbed

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side effects of thiabendazole

nauseua, vomit, dizzy

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Pyrantel Pamoate mechanism

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

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uses of Pyrantel Pamoate

hookworm, pinworm, roundworm

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

Praziquantel causes PPPPPPermeability

Mech of Praziquantel

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

drug of choice for Schisotosoma

Praziquantel | I pray this Schits over soon"

Use of Praziquantel

Schistosomiasis (also for taneia solium to prevent neurocysteriocorcosis)

Tape worm drugs

Praziquantel, Albendazole, Paromomycin sulfate

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

Praziquantel

Used to treat neurocysticercosis

Albendazole (be careful in poeople with seizures)

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

Paromomycin sulfate | "MOM.. i have tape worms"

Key with anti-malarials

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

____ in mosquito salivary gland are injected into human blood

Sporozoites

Exoerythrocytic stage—

sporozoites multiply in liver to form tissue schizonts

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

merozoites | blood schizonts

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

merozoites;

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

always the blood schizonts

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

P. falciparum and P. malariae

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

P. vivax and P. ovale • | Liver has 5 letters and so do these malaria

Blood schizonticide: | parazitized erythrocytes concentrate the drug 25 fold by pH dependent mechanism into acidic vacuoles

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

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

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

Use of Chloroquine

all 4 species | will eradiate P. malariae and P. falciparum but wont cure P. vivax and ovale (still have liver form)

Tx all 4 species | will eradiate P. malariae and P. falciparum but wont cure P. vivax and ovale (still have liver form)

Chloroquine | careful for P.falciparum resistance

Side effect of chloroquine

visual impairment | chloroquine... 4 eyes!!!! b'c quine sounds like quad... also for all four... alsp think stops heme from going to 4

Mech of Mefloquine

sim to chloroquine

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

Mefloquine

What pts should not recieve mefloquine

pts with eplilepsy or pychiatric disorders

Black box warning for Mefloquine

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

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

atovaquone

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

Proguanil | "pro as in prodrug"

These two will inhibit protozoal pyrimidine synthesis

Atovaquone | Proguanil

Mech of Atovaquone | think ABC's~~~ goes A for atovaquone and BC for cyctochorm BC1

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

Mech of Proguanil

prodrug activated by hepatic CYP2C9 | inhibits malarial dihydrofolate reductase block folate synthesis--- pyrimidine synthesis

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

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

Mech of quinine

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

Uses of Quinine

Schizonticide for all four | alternative for P.Falciparum resistant to Chloroquine

Quinine and Mefloquine | Diff side effects

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

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

Side effects of quinine

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

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

sides for quinine

Doxycycline mech

depress dihydroorotate dehydrogenase activity, can't make pyrimidines

fucks with dihydroorotate DH activity | then the malaria can't make pyrimides

Mech of Doxycycline "Doxy got all those D's Dihidroorotase DH"

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

Doxyclycine

Drug to kill liver hypnoschizots

Primaquine

Mechanism of Primaquine

act as oxidants will kill liver hypnozoites

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

Primaquine

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

Primaquine

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

Primaquine

uses of Primaquine

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

Side effects of primaquine

hemolytic rxns in those with G6P DH deficiency

see hemolytic rnx in those with GP6 deficiency

Primaquine