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BIIC Cancers and Pharmo > Anti-malarials > Flashcards

Anti-malarials Flashcards

1
Q

P. falciparum malaria has acquired resistance to ________

A

chloroquine

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2
Q

Inhibitors of Heme Metabolism: Quinolines

A
  • chloroquine
  • quinine
  • quinidine
  • mefloquine
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3
Q

Inhibitors of Heme Metabolism: Artemisinin Derivatives

A
  • artemisinin
  • artesunate
  • artemether
  • sihydroartemisinin
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4
Q

Inhibitors of Electron Transport

A
  • primaquine

- atovaquone

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5
Q

Inhibitors of Translocation

A
  • doxycycline
  • tetracycline
  • clindamycin
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6
Q

Inhibitors of Folate Metabolism

A
  • sulfadoxine-pyrimethamine

- proguanil

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7
Q

Which drugs work on the liver stages of malaria?

A
  • atovaquone/proguanil

- primaquine

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8
Q

Quinolines: Names (4)

A

chloroquine, quinine, quinidine, mefloquine

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9
Q

Quinolines: MOA

A

inhibits polymerization of Ferriprotoporphyrin IX (heme) to Hemozoin(polymerized heme)–> accumulation of unpolymerized heme leads to oxidative membrane damage that is toxic

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10
Q

Quinolines: Which are taken once a week? (2)

A

chloroquine and mefloquine

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11
Q

Quinolines: Which are taken every 8 hours? (2)

A

quinine and quinidine

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12
Q

Quinolines: ADRs: Common (4)

A
  • tinnitus
  • headaches
  • nausea
  • vomiting
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13
Q

Quinolines: ADRs: Serious (3)

A
  1. prolonged QT interval
  2. mefloquine neuropsychiatric effects
  3. chloroquine toxic at high doses in kids
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14
Q

Quinolines: Chloroquine is a first-line treatment and prophylactic for? (5)

A
  • vivax
  • ovale
  • malariae
  • knowlesi
  • senstive strains of falciparum
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15
Q

Quinolines: where is an alternative place to find quinine?

A

tonic water and can be used prophylactically

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16
Q

Artemisinins: Names

A
  • artemisinin
  • artesunate
  • artemether
  • dihydroartemisinin
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17
Q

Artemisinins: MOA

A
  • forms free radical after activation by iron

- adducts that are toxic to plasmodia

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18
Q

Artemisinins: Pharmacokinetics

A

co-administration w/ ketoconazole decreases metabolism of artemisinins b/c it is a potent CYP3A4 inhibitor

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19
Q

Artemisinins: ADRs (5)

A
  • nausea
  • vomiting
  • dizziness
  • tinnitus
  • type 1 hypersensitivity
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20
Q

Artemisinins: First-line treatment for?

A

P. falciparum

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21
Q

Artemisinins: USE IN COMBINATION

A

USE IN COMBINATION

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22
Q

Inhibitors of Electron Transport: Names (2)

A

primaquine and atovaquone

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23
Q

Inhibitors of Electron Transport: MOA

A

selectively interrupts the plasmodial ETC

  • P = ubiquinone
  • A = cytochrome bc1 complex
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24
Q

Inhibitors of Electron Transport: Pharmacokinetics

A
  • metabolized to quinone–> acitve metabolite
  • BAD for G6PD pts
  • daily dosing for both
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25
Q

Inhibitors of Electron Transport: ADRs (4)

A
  • abdominal pain
  • nausea
  • hemolytic anemia
  • leukopenia
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26
Q

Inhibitors of Electron Transport: Considerations: Primaquine

A

inhibits hepatic stage caused by vivax and ovale–> DO NOT USE AS MONOTHERAPY==> coadminister w/ doxycycline or proguanil

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27
Q

Inhibitors of Translation: Names (3)

A
  • doxycycline
  • tetracycline
  • clindamycin
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28
Q

Inhibitors of Translation: MOA

A

D and T = bind to 30S subunit and blocks binding of tRNA to the A site of mRNA
C = binds to 50S subunit and prevents the transfer of amino acids to the A site

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29
Q

Inhibitors of Translation: Pharmacokinetics

A

D and T = daily dosing

30
Q

Inhibitors of Translation: Pregnancy Category for Tetracyclines

A

D

31
Q

Inhibitors of Translation: Tetracyclines: ADRs (3)

A
  • photosensitivity
  • tooth discoloration and bone development in children
  • clostridium difficile diarrhea
32
Q

Inhibitors of Translation: Clindamycin: ADR

A

diarrhea caused by Clostridium difficile

33
Q

Inhibitors of Translation: Used in Combo w/

A

artesunate or quinine

34
Q

Inhibitors of Folate Metabolism: Names (2)

A
  • sulfadoxine-pyrimethamine

- proguanil

35
Q

Inhibitors of Folate Metabolism: MOA

A

target dihydrofolate reductase(DHFR) and dihydropteroate synthase(DHPS) from the folate metabolic pathway

  • S = DHPS
  • P = DHFR
36
Q

Inhibitors of Folate Metabolism: Pharmacokinetics

A
  • S = single dose to treat, weekly/biweekly prophylactic

- P = once daily

37
Q

Inhibitors of Folate Metabolism: Sulfadoxine-pyrimethamine: ADRs

A
  • discontinue at appearance of rash
  • Stevens-Johnson Syndrome or toxic epidermal necrosis
  • pruritis, diarrhea, nausea, vomiting, headache
38
Q

Inhibitors of Folate Metabolism: Proguanil: ADRs

A
  • abdominal pain
  • diarrhea
  • nausea
  • vomiting
  • pruritis
  • hepatitis
39
Q

Inhibitors of Folate Metabolism: Sulfadoxine-pyrimethamine: Consideration

A

highly effective against blood schizont stages of P. falciparum

40
Q

Inhibitors of Folate Metabolism: Atovaquone-proguanil: Consideration

A

-blood schizonticides - effective against drug-resistant strains of P. falciparum and P. vivax

41
Q

E. histolytica lacks ________.

A

fermentation enzymes - lactate dehydrogenase and pyruvate decarboxylase

42
Q

E. histolytica is obtained by

A

ingesting contaminated food/water

43
Q

Anaerobic organisms contain ___________ which metabolizes pyruvate to acetyl CoA

A

PFOR = pyruvate-ferredoxin oxidoreductase

44
Q

Antibiotic: Metronidazole and Tinidazole: MOA

A

single-electron transfer forms a highly reactive nitro radical anion that kills susceptible organisms by radical-mediated mechanisms that target DNA

45
Q

Antibiotic: Metronidazole and Tinidazole: Pharmacokinetics

A 
M = dosed every 8 hrs
T = dosed daily
46
Q

Antibiotic: Metronidazole and Tinidazole: ADRs (4)

A

nausea, headaches, Candida vaginitis, hypersensitivity reaction

47
Q

Antibiotic: Metronidazole and Tinidazole: Cosiderations

A
  • useful against giardia
  • M treats ameba infections
  • H. pylori is resistant to M
  • T has a shorter treatment course
48
Q

Antiprotozoal: Nitazoxanide: MOA

A
  • activity against Giardia lamblia and Cryptosporidium parvum
  • inhibits PFOR
49
Q

Antiprotozoal: Nitazoxanide: ADRs (3)

A
  • abdominal pain
  • nausea
  • headache
50
Q

Early Stage: African Sleeping Sickness Treatment: Pentamidine

A

MOA: inhibition of DNA, RNA, and protein synthesis
ADR: fatigue, dizziness, hypotension, pancreatitis, kidney damage

51
Q

Early Stage: African Sleeping Sickness Treatment: Suramin

A

MOA: inhibit energy metabolism and RNA polymerase
ADR: pruritis, parethesia, vomiting, nausea

52
Q

Late Stage: African Sleeping Sickness Treatment: Melarsoprol

A

MOA: inhibits trypanosomal pyruvate kinase–> inhibits glycolysis and decreases ATP production
ADR: toxic to humans, phlebitis, brian inflammation

53
Q

Late Stage: African Sleeping Sickness Treatment: Eflornthine

A

-early and late stage West NOT East
MOA: irrerversible inhibitor of ornithine decarboxylase and inhibits polyamine synthesis–> inhibits nucleic acid and protein synthesis
ADR: less toxic that melasoprol, acne

54
Q

Chaga’s Treatment: Nifurtimox

A

MOA: toxic oxygen free radicals inside parasite
ADR: anorexia, vomiting, memory loss, sleep disorders, seizures

55
Q

Leishmania Treatments: Sodium stibogluconate and Meglumin antimonate

A

MOA: pentavalent antimony and inhibition of glycolytic pathway and fatty acid oxidation
ADR: prolonged QT interval, pancreatitis, rash

56
Q

Leishmania Treatments: Alternative

A

amphotericin and miltefosine

57
Q

Anthelmintic: Ivermectin: MOA

A

activation of glutamate-gated chloride channels causes a blockade of neuromuscular transmission and paralysis of the worm

58
Q

Anthelmintic: Ivermectin: Pharmacokinetics

A

single dose

59
Q

Anthelmintic: Ivermectin: ADRs (2)

A
  • inflammatory or allergic response

- seizures

60
Q

Anthelmintic: Albendazole, Mebendazol, Triclabendazole: MOA

A

inhibits tubulin polymerization —> disrupts nematodal motility and DNA replication–> immobilization and death

61
Q

Anthelmintic: Albendazole, Mebendazol, Triclabendazole: Pharmacokinetics

A

A = dosed daily

M and T = every 12 hours

62
Q

Anthelmintic: Albendazole, Mebendazol, Triclabendazole: ADRs (5)

A
  • vomiting
  • nausea
  • diarrhea
  • increased liver enzymes
  • Stevens-Johnson Syndrome
63
Q

Anthelmintic: Albendazole, Mebendazol, Triclabendazole: Consideration

A

used effective contraception during treatment and 3 days after final dose

64
Q

Antifilarial Agent: Diethylcarbamazine: MOA

A

unknown

65
Q

Antifilarial Agent: Diethylcarbamazine: Pharmacokinetics

A

dosed daily

66
Q

Antifilarial Agent: Diethylcarbamazine: Pregnancy Category

A

X

67
Q

Antifilarial Agent: Diethylcarbamazine: Indication

A

adult filariasis worms

68
Q

Antifilarial Agent: Diethylcarbamazine: ADRs (3)

A

anorexia, headache, nausea

69
Q

Anthelmintic: Praziquantel: MOA

A

contraction and paralysis of worm

70
Q

Anthelmintic: Praziquantel: Pharmacokinetics

A

dosed every 8 hrs

71
Q

Anthelmintic: Praziquantel: Indications

A

adult cestode(tapeworm) and trematode(fluke) infections

72
Q

Anthelmintic: Praziquantel: ADRs (3)

A

nausea, headache, and abdominal discomfort

BIIC Cancers and Pharmo (10 decks)

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