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IBI Test 2 > B3-046 - Parasite Drugs > Flashcards

B3-046 - Parasite Drugs Flashcards

1
Q

Antimalarials

A

Chloroquine
Primaquine
Mefloquine
Quinine
Atovaquone/Proguanil
Pyrimethamine-Sulfadoxine

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2
Q

Anti-helminths

A

Ivermectin
Mebendazole
Albendazole

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3
Q

Antiprotozoal drugs

A

Metronidazole
Pentamidine

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4
Q

Chloroquine Mechanism

A

Alters metabolism and detoxification of heme by parasite.

Prevents free heme conversion into hemozoin. Build up of free heme damages parasite and kills the parasite.

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5
Q

Chloroquine is administered _____

A

orally or parenterally (via injection or infusion)

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6
Q

Chloroquine is excreted in

A

Urine

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7
Q

Loading dose

A

Giving a higher dose initially before dropping to the lower maintenance dose. This is used in Chloroquine therapy

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8
Q

Clinical Uses of Chloroquine

A

Very good a killing blood pathogens
Acute - clears parasitemia from all for Plasmodia

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9
Q

Chloroquine is curative for

A

P. malaria and P. knowlesi and sensitive P. falciparum

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10
Q

Chloroquine is used with _____ for P. ovale and sensitive p. vivax

A

Primaquine

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11
Q

Chloroquine as a PPX

A

Begin 1 week before travel (loading dose) and continue 4 weeks after return

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12
Q

Adverse effects of Chloroquine

A

Generally well tolerated
Symptoms: puritis, GI, mild headache; psoriasis exacerbation

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13
Q

Chloroquine resistance

A

Widespread in South America, Africa, Asia
Most common in P. falciparum, increasing in P. vivax
P-glycoprotein pumping mech

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14
Q

Primaquine mechanism

A

Unsure - works on DNA, maybe ROS

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15
Q

Primaquine Pharmacokinetics

A

only TISSUE schizonticide
Oral, well absorbed and distributed

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16
Q

Primaquine: metabolites are _________

A

intracellular oxidants

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17
Q

Used in combination with chloroquine to PPx or cure of P. vivax and P. ovale

A

Primaquine

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18
Q

Symptoms of Primaquine

A

GI, hemolytic anemia in G6PDH deficiency

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19
Q

Mefloquine mechanism

A

Unknown - potentially similar to chloroquine

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20
Q

Mefloquine Pharmacokinetics

A

Only oral
Well absorbed
Metabolized in liver
Excreted in feces

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21
Q

Mefloquine symptoms

A

GI, CNS, psychotropic effects (1:250 doses)

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22
Q

Clinical use of Mefloquine

A

PPx or treatment of Chloroquine-resistant malaria

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23
Q

Quinine Mechanism

A

May alter heme metabolism, still largely unclear

24
Q

Quinine Pharmacokinetics

A

Oral, well absorbed
Doesn’t cross blood brain barrier
Metabolized by CYP3A4

25
Q

Quinine is used best for

A

Chloroquine resistant P. falciparum

26
Q

Quinine symptoms

A

Cinchonism (headache, sweating, nausea, tinnitus, dizziness, blurred vision), QT prolongation

27
Q

Atovaquone/Proguanil combo is also called

A

Malarone

28
Q

Atovaquone mechanism

A

Inhibits ETC, decreased mitochondrial, leading to loss of pyrimidine production

29
Q

Atovaquone absorption

A

oral, but poorly
high protein binding, 2-3 day half life

30
Q

Proguanil mechanism

A

Inhibits protozoal dihydrofolate reductase

31
Q

Proguanil absorption

A

well absorbed
CYP metabolism
Active metabolite is Cycloquanil
12hr t-1/2

32
Q

Proguanil uses

A

PPx or treatment for chloroquine resistant P. falciparum

33
Q

Proguanil adverse effects

A

GI, headache, anorexia, dizziness, Steven Johnson (rash)

34
Q

Fansidar mechanism

A

Anti-folate combination
Blocks synthesis/utilization of folic acid

35
Q

Fansidar adverse effects

A

GI, cutaneous reactions (sometimes severe), headache, vomiting, diarrhea

36
Q

Fansidar Pharmacokinetics

A

Well absorbed and distributed, excreted in urine

37
Q

Fansidar clinical use

A

Effective blood schizonticide for P. falciparum
Chloroquine-resistant P. falciparum
Slow acting - cannot be used alone for acute attacks

38
Q

Metronidazole mechanism

A

Tissue amebicide
Nitroimidazole - activated by electron donation
Affective for anaerobic/hypoxic sites

39
Q

Metronidazole pharmacokinetics

A

Oral/IV
Well absorbed and dist. including CNS and bone
Cleared in urine following hepatic metabolism.

40
Q

Metronidazole clinical uses

A

Intestinal, extra intestinal, and urogenital protozoal infections
-Trichomoniasis, giardiasis, amebiasis
Anaerobic infections

41
Q

Metronidazole adverse effects

A

Many and common - nausea, headache, dry mouth, leukopenia
Disulfiram effect - no drinking while on this drug

42
Q

Pentamidine Mechanism

A

Unknown

43
Q

Pentamidine pharmacokinetics

A

IV, IM, or aerosol
Concentrates in liver, spleen, kidneys

44
Q

Pentamidine clinical uses

A

Aerosol used for PPx or treatment against Pneumocystis pneumonia
IV against Leishmaniasis, sleeping sickness, and more

45
Q

Pentamidine adverse effects

A

Respiratory stimulation followed by depression, hypotension, anemia
These effects are less common with aerosol administration

46
Q

Mebendazole mechanism

A

Blocks microtubule synthesis, blocks vesicle and organelle movement
Wide-spread anti helminthic

47
Q

Mebendazole pharmacokinetics

A

Given orally, less than 10% absorbed
Rapidly metabolized, excreted in urine
Dose limited by GI effects

48
Q

Mebendazole uses

A

Effective against pinworm, hookworm, ascaris

49
Q

Mebendazole is possibly _______

A

embryotoxic

50
Q

Albendazole mechanism

A

Interferes with microtubule aggregation (beta-tubulin), alters glucose uptake (starves worm)
Wide spectrum anti-helminthic

51
Q

Albendazole metabolism

A

Rapid and completely metabolized in liver
Fairly safe due to low absorption

52
Q

Ivermectin mechanism

A

Binds glutamate gated chloride channels and causes hyper-polarization of nerve -> paralysis

53
Q

Ivermectin uses

A

Oral treatment for Stronguloidasis and Onchocerciasias (subcutaneous nodules, corneal and anterior chamber) head lice, scabes

54
Q

Ivermectin absorption

A

Well absorbed and distributed
t-1/2 16-18 hr
metabolized by CYPs

55
Q

Ivermectin ____ cross the blood brain barrier

A

does not
very minor effect on GABA receptors

56
Q

Ivermectin adverse effects

A

Neuropathy, headache, dizziness

IBI Test 2 (5 decks)

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