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Pharm > Antiparasitics > Flashcards

Antiparasitics Flashcards

1
Q

What is the most versatile antimalarial?

A

Chloroquine

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2
Q

What two malarial drugs are contraindicated by pregnancy?

A
  • quinine (also can generate resistance if used as prophylaxis)
  • primaquine
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3
Q

What is the indication for Mefloquine? Should this be used orally or IV?

A
  • first line therapy for chloroquine resistant malaria
  • prophylaxis for P. falciparum
  • erythrocyte schizonticidal activity
  • oral
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4
Q

What is the MOA of chloroquine?

A
  • kills blood schizont (inside RBC)
  • inhibition of heme biocrystallization
  • concentrate in parasite’s food vacuole, drug blocks heme to hemozoin, accumulating heme which is a toxin
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5
Q

What drug interaction is considered with anti-malarial drugs?

A

antacids decrease oral absorption

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6
Q

What are AEs of chloroquine?

A
  • prolonged use causes auditory dysfunction (tinnitis)
  • high dose causes retinopathy
  • resistance - parasite can develop membrane pumps to flush out the drugs
  • pts with glucose-6-phosphate dehydrogenase deficiency can get severe anemia
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7
Q

Which malarial drug can cross the BBB?

A

Mefloquine

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8
Q

What stage does chloroquine work against? Can it be a prophylactic? What can it not be used for?

A
  • erythrocytic stage
  • prophylaxis - yes
  • not effective for liver form
  • P. falciparum has developed resistance
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9
Q

What AEs apply to all malarial drugs?

A

rash, HA, dizziness, and ocular toxicity

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10
Q

What are AEs for Mefloquine?

A
  • high dose: cardiac arrest, cardiac conduction defects, neuro dysfunction (sz, hallucinations, psychosis) neuropsychiatric reactions
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11
Q

How and why would you use Quinine?

A
  • IV use for severe infections, including
  • cerebral malaria
  • erythrocytic stages of chloroquine resistant P. falciparum
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12
Q

What is the MOA of Mefloquine?

A
  • mefloquine is a weak base and accumulates in the parasites’ acidic lysosome
  • not active against hepatic or gametocyte form
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13
Q

What is the MOA of Primaquine? AE?

A
  • destroys parasite food vacuole
  • redox mediator
  • GI distress
  • leukopenia
  • hemolysis
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14
Q

What is the MOA of Atovaquone?

A
  • inhibition of mitochondrial ETC
  • blocking nucleic acid synthesis, inhibits replication
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15
Q

What is the indication for Primaquine?

A
  • hepatic stages
  • dormant forms of P. ovale and P. vivax
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16
Q

What is the indication for Proguanil?

A
  • works in hepatocytes, so is used in combination with chloroquine or another drug that works on erythrocytic stages
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17
Q

What is the indication for Atovaquone?

A
  • tissue and erythrocytic shizont
  • chloroquine resistant malaria
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18
Q

What is the MOA of Proguanil? Is this a fast or slow action? What are the AEs?

A
  • selectively inhibits dihydrofolate-reductase-thymidylase synthase enzyme, inhibiting DNA
  • slow action
  • flu like s/s, diarrhea, safe for pregnancy
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19
Q

What is the indication for Metronidazole? What kind of drug is this?

A
  • obligate anerobes
  • Amoebiasis, Giardiasis, Trichomoniasis
  • very affective against anaerobic abdominal or CNS infection
  • it is a prodrug
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20
Q

What drugs work against luminal amebicides?

A
  • Diloxanide furoate
  • iodoquinol
  • paromomycin
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21
Q

Besides malaria, what does chloroquine work agaisnt?

A

tissue amebicides

22
Q

The indication for tinidazole emetines is what?

A

both luminal and tissue amebicides

23
Q

What would you use to treat an amebic abscess of the liver or lung?

A

metronidazole or tinidazole plus one luminal agent

24
Q

What is the MOA of metronidazole?

A
  • selective toxicity
  • ferredoxin in anaerobes
  • reduces drug nitro group to produce reactive metabolite (enzyme PFOR)
  • reduced drug binds to DNA and damges it, disrupting helical structure, fragmenting DNA, and causing cell death
25
Q

How would you treat Trypanosoma bruceii?

What does this do to the parasite?

A
  • suramin and pentamidine
  • disrupts the membrane
26
Q

How would you administer metronidazole? Does this cross the BBB? Does hepatic function matter?

A
  • IV or PO, serum level same
  • does cross BBB
  • has reduced metabolism in pts with hepatic dysfunction
27
Q

What are the AEs of metronidazole?

A
  • psychosis
  • disulfiram - like reaction - blocking acetaldehyde dehydrogenase which develop aldehyde toxicity - hangover effect
28
Q

What are drug interactions and contraindications to metronidazole?

A
  • pregnancy
  • warfarin - disrupts the intestinal flora/Vit K synthesis, increasing bleeding
  • etoh in last 12 hours or future 24 hours
29
Q

For advanced stages of sleeping sickness, what drug should be used?

What is the MOA?

A
  • melarsoprol
  • is an organic arsenic compound that can enter the CNS
30
Q

What would you use to treat Toxoplasma gondii, the infection in pregnant women? Why would you use these drugs?

A
  • pyrimethamine and sulfonamides
  • can pass through the placenta, encyst and destroy tissue
31
Q

What are the overall AE to anti-helminth drugs?

A
  • HA
  • rash
  • fever
  • oral drugs
    • GI distress
  • systemic toxicity - due to antigens from disintegrating parasites
  • Mazzotti reaction - groups of s/s when lysis of the parasite releases its contents into the hosts that cause sepsis like syndrome
32
Q

What is the indication for Praziquantel?

A
  • broad spectrum, trematode and cestode infection
33
Q

What is the indication for Niclosamide? What does it not work for?

A
  • cestodes, for beef and fish tapeworms, intestinal flukes
  • not effective for cysts (hydatid, cysticercosis)
34
Q

What would you use to treat a wide spectrum of worm infections, including eggs, larvae, and adult forms of nematodes and cestodes (cysticercosis and hydatid cysts)?

A
  • Albendazole
35
Q

What is the indication for Mebendazole?

A
  • pinworm and roundworms
  • localized helminthic infections
  • larval nematodes
36
Q

What is the MOA of Mebendazole?

A
  • first, selectively inhibit microtubules (preventing polymerization)
  • second, inhibit glucose uptake through tegument (depletion of glycogen)
37
Q

What are AEs of Mebendazole?

A
  • alopecia (balding)
  • GI distress
38
Q

What anti-helminthic drugs are contraindicated by pregnancy?

A
  • mebendazole
  • piperazine
  • ivermectin
39
Q

What is the MOA of Piperzine? Can it cross the BBB? What are the AEs?

A
  • selectively bind onto the parasite’s GABA receptors, inducing paralysis;
  • can cross the BBB
  • minor GI disturbance, human GABA system can be affected
40
Q

What are the contraindications to Piperazine?

A

hepatic or renal dysfunction, seizures, pregnancy

41
Q

What is the drug of choice for onchocerciasis? What else will this drug treat?

A
  • ivermectin
  • some forms of filariasis and head lice
42
Q

What will treat eye worms? microfilariae? What is this drug’s AE?

A
  • DimethylCarbamazine
  • Mazzotti reaction
43
Q

What is the drug of choice against lice? Second line?

A
  • Permethrin
  • Malathion
44
Q

What is the MOA of Permethrin?

A
  • induce Na+ flux, thus reducing action potential
45
Q

What is the MOA of Malathion?

A
  • inhibits insect cholinesterases
  • blocks acetylcholine hydrolysis at synapse
46
Q

What is the MOA of Ivermectin? What is an AE of ivermectin?

A
  • first, binds to glutamate gate chloride channels in nerve and muscles
  • second, intensifies GABA mediated neurotransmission in nematodes
  • both result in paralysis and immobilization
  • AE: fatal neurotoxicity
47
Q

Does ivermectin cross the BBB?

A

no - has selective toxicity because cannot cross BBB and human GABA only in CNS

48
Q

What is the MOA of Pyrantel pamoate?

A
  • selectively binds on the parasite’s nicotinic receptors at NMJ
  • depolarization induced paralysis
  • expelled by peristalsis
49
Q

What drug treats hookworms and round worms?

A
  • Pyrantel pamoate
50
Q

What is the MOA of Albendazole?

What are some AEs?

A
  • blocks microtubules. inhibits glucose uptake
  • alopecia
  • recent cases of hepatotoxicity in children
51
Q

What is the MOA of Niclosamide and what is a common drug interaction?

A
  • uncoupling oxidative phosphorylation
  • avoid etoh for 24-48 hours
52
Q

What is the MOA of Praziquantal?

A
  • increases the tegmental permeability of schistosomes for Ca+ ions, cause vacuolization, paralysis, and death
  • tetanic muscular contractions

Pharm (3 decks)

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