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WRAP UP > PHARM_ANTIPARASITICS > Flashcards

PHARM_ANTIPARASITICS Flashcards

1
Q

MOA chloroquine?

A

intracellular heme accumulation; toxic

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2
Q

moa quinine

A

DNA complexer; prevents strand separation

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3
Q

MOA primaquine

A

free radical generators in plasmodium

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4
Q

MOA pyrimethamine, proguanil

A

pyrimethamine, proguanil = DHFR inhibitors

sulfadoxine = dihydropteroate synthase inhibitor

combo of pyrimethamine w/ sulfadoxine sequentially blocks folic acid synth.

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5
Q

MOA atovaquone-proguanil

A

inhibits mitochondrial ETC

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6
Q

MOA artesunate, artemether

A

free radical generators in plasmodium

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7
Q

MOA atovaquone

A

inhibits ETC

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8
Q

what is the target for chloroquine?

A

blood schizonticide

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9
Q

what is the target for mefloquine?

A

blood schizonticide

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10
Q

what is the target for quinine?

A

blood schizonticide

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11
Q

what is the only antimalarial drug that has activity against liver schizonts (vivax & ovale)?

A

primaquine

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12
Q

what is the target of atovaquone-proguanil therapy?

A

blood schizonticide (falciparum)

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13
Q

what is the target of artesunate, artemether?

A

blood schizonticide (falciparum) including multidrug resistant strains

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14
Q

what is the target of proguanil?

A

slow acting blood schizonticide + prevents sporogeny in mosquito

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15
Q

what is the target of pyrimethamine?

A

blood schizonticide

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16
Q

what is the mechanism of resistance to chloroquine?

A

decreased intracellular &/or decreased intravacuolar drug accumulation

17
Q

describe the pharmacokinetic properties of chloroquine?

A

orally active high Vd-long persistance some hepatic metab., renal elimination

18
Q

describe the PK properties and metabolism of artesunate and artemether

A

oral; poorly water soluble, but levels achieved exceed cytotoxic requirement short half-lives wide TI

19
Q

explain the mechanism of hemolytic anemia induced by primaquine in african american males with G6PD deficiency

A

G6PD protects rbc from ROS, antimalarial causes buildup of ROS that is toxic

20
Q

describe the toxic adverse effect of chloroquine

A

Irreversible retinopathy, maculopathy, and macular degeneration

  • most often after long-term or high-dose therapy
  • regular opthalm. exam should be done for all pts getting long-term therapy & drug discontinued at 1st sign of any adverse rxn Abnormal ECG; prlonged QT interval
21
Q

which drug causes cinchonism?

A

quinine

22
Q

what are the most common symptoms occurring from long-term exposure to quinine?

A

Cinchonism: repeated headaches Nausea blurred vision tinnitus hearing impairment-deafness

23
Q

what are the drugs of choice for treating uncomplicated malaria/P. falciparum in a region of chloroquine resistance or unknown resistance?

A

atovaquone-proguanil artemether-lumefantrine quinine + doxy or tetracycline or clindamycin Melfoquine *if species not identified is subseq. diagnosed as P. Vivax or P. ovale then retreat with primaquine

24
Q

what are drugs of choice for all regions in treating p. malariae?

A

chloroquine or hydroxychloroquine

25
Q

what are the drugs of choice in all regions for treating P. vivax or ovale?

A

chloroquine or HC + primaquine

26
Q

what are the drugs of choice in treating P. ovale in regions with chloroquine resistance?

A

quinine + doxy or tetracycline atovaquone-proguanil + primaquine

27
Q

what are the drugs of choice for treating pregnant women with malaria?

A

chloroquine or hydroxychloroquine quinine + clindamycine OR mefloquine

28
Q

what are the drugs of choice for treating P. falciparum in all regions?

A

quinidine + one of the following: doxy, tetracycline, clindamycin contact CDC for artesunate followed by atovaquone-proguaanil, doxy, or mefloquine (clindamycin in pregn.)

29
Q

which antimalarial drug requires a loading dose to achieve effective plasma concentration?

A

chloroquine (has a large volume of distribution)

30
Q

which antimalarial drug most likely produces hemolytic anemia in a pt with G6PD deficiency?

A

primiquine but also: quinine

31
Q

which antimalarial drug is combined with proguanil (folate antagonist) to form an effective treatment for chemoprophylaxis of falciparum malaria?

A

atovaquone

32
Q

If you have a pt taking a drug for malaria with headache, vertigo, blurred vision, and tinnitus, what drug were they taking?

A

quinine (this is cinchonism)

33
Q

name the 4 sets of drugs that are used to treat uncomplicated chloroquine-resistant P. falciparum?

A

Atovaquone-proguanil Artemether-lumefantrine Quinine-doxycycline Mefloquine

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