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BIIC Cancers and Pharmo > Anti-malarials > Flashcards

Anti-malarials Flashcards

(72 cards)

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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
Inhibitors of Electron Transport: ADRs (4)
- abdominal pain - nausea - hemolytic anemia - leukopenia
26
Inhibitors of Electron Transport: Considerations: Primaquine
inhibits hepatic stage caused by vivax and ovale--> DO NOT USE AS MONOTHERAPY==> coadminister w/ doxycycline or proguanil
27
Inhibitors of Translation: Names (3)
- doxycycline - tetracycline - clindamycin
28
Inhibitors of Translation: MOA
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
29
Inhibitors of Translation: Pharmacokinetics
D and T = daily dosing
30
Inhibitors of Translation: Pregnancy Category for Tetracyclines
D
31
Inhibitors of Translation: Tetracyclines: ADRs (3)
- photosensitivity - tooth discoloration and bone development in children - clostridium difficile diarrhea
32
Inhibitors of Translation: Clindamycin: ADR
diarrhea caused by Clostridium difficile
33
Inhibitors of Translation: Used in Combo w/
artesunate or quinine
34
Inhibitors of Folate Metabolism: Names (2)
- sulfadoxine-pyrimethamine | - proguanil
35
Inhibitors of Folate Metabolism: MOA
target dihydrofolate reductase(DHFR) and dihydropteroate synthase(DHPS) from the folate metabolic pathway - S = DHPS - P = DHFR
36
Inhibitors of Folate Metabolism: Pharmacokinetics
- S = single dose to treat, weekly/biweekly prophylactic | - P = once daily
37
Inhibitors of Folate Metabolism: Sulfadoxine-pyrimethamine: ADRs
- discontinue at appearance of rash - Stevens-Johnson Syndrome or toxic epidermal necrosis - pruritis, diarrhea, nausea, vomiting, headache
38
Inhibitors of Folate Metabolism: Proguanil: ADRs
- abdominal pain - diarrhea - nausea - vomiting - pruritis - hepatitis
39
Inhibitors of Folate Metabolism: Sulfadoxine-pyrimethamine: Consideration
highly effective against blood schizont stages of P. falciparum
40
Inhibitors of Folate Metabolism: Atovaquone-proguanil: Consideration
-blood schizonticides - effective against drug-resistant strains of P. falciparum and P. vivax
41
E. histolytica lacks ________.
fermentation enzymes - lactate dehydrogenase and pyruvate decarboxylase
42
E. histolytica is obtained by
ingesting contaminated food/water
43
Anaerobic organisms contain ___________ which metabolizes pyruvate to acetyl CoA
PFOR = pyruvate-ferredoxin oxidoreductase
44
Antibiotic: Metronidazole and Tinidazole: MOA
single-electron transfer forms a highly reactive nitro radical anion that kills susceptible organisms by radical-mediated mechanisms that target DNA
45
Antibiotic: Metronidazole and Tinidazole: Pharmacokinetics
``` M = dosed every 8 hrs T = dosed daily ```
46
Antibiotic: Metronidazole and Tinidazole: ADRs (4)
nausea, headaches, Candida vaginitis, hypersensitivity reaction
47
Antibiotic: Metronidazole and Tinidazole: Cosiderations
- useful against giardia - M treats ameba infections - H. pylori is resistant to M - T has a shorter treatment course
48
Antiprotozoal: Nitazoxanide: MOA
- activity against Giardia lamblia and Cryptosporidium parvum - inhibits PFOR
49
Antiprotozoal: Nitazoxanide: ADRs (3)
- abdominal pain - nausea - headache
50
Early Stage: African Sleeping Sickness Treatment: Pentamidine
MOA: inhibition of DNA, RNA, and protein synthesis ADR: fatigue, dizziness, hypotension, pancreatitis, kidney damage
51
Early Stage: African Sleeping Sickness Treatment: Suramin
MOA: inhibit energy metabolism and RNA polymerase ADR: pruritis, parethesia, vomiting, nausea
52
Late Stage: African Sleeping Sickness Treatment: Melarsoprol
MOA: inhibits trypanosomal pyruvate kinase--> inhibits glycolysis and decreases ATP production ADR: toxic to humans, phlebitis, brian inflammation
53
Late Stage: African Sleeping Sickness Treatment: Eflornthine
-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
Chaga's Treatment: Nifurtimox
MOA: toxic oxygen free radicals inside parasite ADR: anorexia, vomiting, memory loss, sleep disorders, seizures
55
Leishmania Treatments: Sodium stibogluconate and Meglumin antimonate
MOA: pentavalent antimony and inhibition of glycolytic pathway and fatty acid oxidation ADR: prolonged QT interval, pancreatitis, rash
56
Leishmania Treatments: Alternative
amphotericin and miltefosine
57
Anthelmintic: Ivermectin: MOA
activation of glutamate-gated chloride channels causes a blockade of neuromuscular transmission and paralysis of the worm
58
Anthelmintic: Ivermectin: Pharmacokinetics
single dose
59
Anthelmintic: Ivermectin: ADRs (2)
- inflammatory or allergic response | - seizures
60
Anthelmintic: Albendazole, Mebendazol, Triclabendazole: MOA
inhibits tubulin polymerization ---> disrupts nematodal motility and DNA replication--> immobilization and death
61
Anthelmintic: Albendazole, Mebendazol, Triclabendazole: Pharmacokinetics
A = dosed daily | M and T = every 12 hours
62
Anthelmintic: Albendazole, Mebendazol, Triclabendazole: ADRs (5)
- vomiting - nausea - diarrhea - increased liver enzymes - Stevens-Johnson Syndrome
63
Anthelmintic: Albendazole, Mebendazol, Triclabendazole: Consideration
used effective contraception during treatment and 3 days after final dose
64
Antifilarial Agent: Diethylcarbamazine: MOA
unknown
65
Antifilarial Agent: Diethylcarbamazine: Pharmacokinetics
dosed daily
66
Antifilarial Agent: Diethylcarbamazine: Pregnancy Category
X
67
Antifilarial Agent: Diethylcarbamazine: Indication
adult filariasis worms
68
Antifilarial Agent: Diethylcarbamazine: ADRs (3)
anorexia, headache, nausea
69
Anthelmintic: Praziquantel: MOA
contraction and paralysis of worm
70
Anthelmintic: Praziquantel: Pharmacokinetics
dosed every 8 hrs
71
Anthelmintic: Praziquantel: Indications
adult cestode(tapeworm) and trematode(fluke) infections
72
Anthelmintic: Praziquantel: ADRs (3)
nausea, headache, and abdominal discomfort

BIIC Cancers and Pharmo (10 decks)

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