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

B3-046 - Parasite Drugs Flashcards

(56 cards)

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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

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A

May alter heme metabolism, still largely unclear

24
Q

Quinine Pharmacokinetics

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A

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

25
Quinine is used best for
Chloroquine resistant P. falciparum
26
Quinine symptoms
Cinchonism (headache, sweating, nausea, tinnitus, dizziness, blurred vision), QT prolongation
27
Atovaquone/Proguanil combo is also called
Malarone
28
Atovaquone mechanism
Inhibits ETC, decreased mitochondrial, leading to loss of pyrimidine production
29
Atovaquone absorption
oral, but poorly high protein binding, 2-3 day half life
30
Proguanil mechanism
Inhibits protozoal dihydrofolate reductase
31
Proguanil absorption
well absorbed CYP metabolism Active metabolite is Cycloquanil 12hr t-1/2
32
Proguanil uses
PPx or treatment for chloroquine resistant P. falciparum
33
Proguanil adverse effects
GI, headache, anorexia, dizziness, Steven Johnson (rash)
34
Fansidar mechanism
Anti-folate combination Blocks synthesis/utilization of folic acid
35
Fansidar adverse effects
GI, cutaneous reactions (sometimes severe), headache, vomiting, diarrhea
36
Fansidar Pharmacokinetics
Well absorbed and distributed, excreted in urine
37
Fansidar clinical use
Effective blood schizonticide for P. falciparum Chloroquine-resistant P. falciparum Slow acting - cannot be used alone for acute attacks
38
Metronidazole mechanism
Tissue amebicide Nitroimidazole - activated by electron donation Affective for anaerobic/hypoxic sites
39
Metronidazole pharmacokinetics
Oral/IV Well absorbed and dist. including CNS and bone Cleared in urine following hepatic metabolism.
40
Metronidazole clinical uses
Intestinal, extra intestinal, and urogenital protozoal infections -Trichomoniasis, giardiasis, amebiasis Anaerobic infections
41
Metronidazole adverse effects
Many and common - nausea, headache, dry mouth, leukopenia Disulfiram effect - no drinking while on this drug
42
Pentamidine Mechanism
Unknown
43
Pentamidine pharmacokinetics
IV, IM, or aerosol Concentrates in liver, spleen, kidneys
44
Pentamidine clinical uses
Aerosol used for PPx or treatment against Pneumocystis pneumonia IV against Leishmaniasis, sleeping sickness, and more
45
Pentamidine adverse effects
Respiratory stimulation followed by depression, hypotension, anemia These effects are less common with aerosol administration
46
Mebendazole mechanism
Blocks microtubule synthesis, blocks vesicle and organelle movement Wide-spread anti helminthic
47
Mebendazole pharmacokinetics
Given orally, less than 10% absorbed Rapidly metabolized, excreted in urine Dose limited by GI effects
48
Mebendazole uses
Effective against pinworm, hookworm, ascaris
49
Mebendazole is possibly _______
embryotoxic
50
Albendazole mechanism
Interferes with microtubule aggregation (beta-tubulin), alters glucose uptake (starves worm) Wide spectrum anti-helminthic
51
Albendazole metabolism
Rapid and completely metabolized in liver Fairly safe due to low absorption
52
Ivermectin mechanism
Binds glutamate gated chloride channels and causes hyper-polarization of nerve -> paralysis
53
Ivermectin uses
Oral treatment for Stronguloidasis and Onchocerciasias (subcutaneous nodules, corneal and anterior chamber) head lice, scabes
54
Ivermectin absorption
Well absorbed and distributed t-1/2 16-18 hr metabolized by CYPs
55
Ivermectin ____ cross the blood brain barrier
does not very minor effect on GABA receptors
56
Ivermectin adverse effects
Neuropathy, headache, dizziness

IBI Test 2 (5 decks)

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