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Pharma 2nd semester > C.3. Antiprotozoal and antihelminthic drugs > Flashcards

C.3. Antiprotozoal and antihelminthic drugs Flashcards

1
Q

list the drugs for Malaria (protoza)

A 
Chloroquine 
Mefloquine 
Quinine 
Artemether 
Lumefantrine 
primaquine 
Atovaquone/ Proguanil (Malarone)
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2
Q

what is pyrimethamine/sulfadoxine’s potential role in Malaria treatment?

A

treatment+prophylaxis of chloroquine resistant strains

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3
Q

what is the potential role of dapsone in malaria treatment?

A

prophylaxis use

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4
Q

what is the potential role of doxycycline in malaria treatment?

A

prophylaxis in areas with multidrug-resistant P. falciparum

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5
Q

where is the chloroquine prophylaxis regimen given?

A

in areas with no known resistant P. falciparum strains.

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6
Q

where is the Malarone prophylaxis regimen given?

A

in areas with chloroquine-resistant P. falciparum strains.

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7
Q

what is the mechanism of chloroquine?

A

inhibit heme polymerization into hemozoin–> intracellular accumulation of heme is toxic to the parasite

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8
Q

how are the antimalarial drugs given?

A

oral

quinine and Artemether–> IV in severe infections

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9
Q

pharmacokinetic property of chloroquine

A

antacids ↓ oral bioavailability

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10
Q

what are the uses of Chloroquine?

A
  1. treatment+ prophylaxis in areas without resistant P. falciparum strains. (1st line agent)
  2. treatment of P. vivax and P. ovale.
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11
Q

adverse effects of chloroquine

A

mild effects in low doses: GI distress, rash, headaches

high doses: retinal damage, auditory damage, QT prolongation

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12
Q

what additional use does hydroxychloroquine have other than being an anti-malaria agent?

A

used in autoimmune disorders: RA, SLE and Sjogren syndrome

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13
Q

what anti-malarial agents are blood schizonticide?

A 
chloroquine 
mefloquine
quinine
artemether
lumefantrine
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14
Q

which antimalarial agent is a tissue schizonticide?

A

primaquine

kills schizonts in the liver

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15
Q

which anti-malarial drugs have an unknown mechanism?

A

Mefloquine

Lumefantrine

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16
Q

what is the use of Mefloquine

A

treatment+ prophylaxis in areas with resistant P. falciparum strains. (1st line agent)

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17
Q

what is the mechanism of quinine?

A

inhibit protozoal DNA replication

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18
Q

what is the use of quinine?

A

treatment of multidrug-resistant malaria

*may be used in combination with doxycycline or clindamycin

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19
Q

side effects of mefloquine (4)

A
  1. GI distress
  2. skin rash
  3. conduction abnormalities
  4. neurotoxicity (seizures)
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20
Q

side effects of quinine (4)

A
  1. Cinchonism ( GI distress, headache, vertigo, blurred vision, tinnitus )
  2. acute hemolysis in G6PD deficient patients
  3. conduction abnormalities
  4. teratogenic
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21
Q

what is Quinidine and when is it used?

A

antiarrhythmic agent, an isomer of quinine

can be used IV in the treatment of severe complicated P. falciparum malaria

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22
Q

adverse effects of Quinidine

A

cinchonism, QRS an QT prolongation with risk of syncope

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23
Q

mechanism of Artemether and Artesunate

A

production of free radicals within the plasmodium food vacuoles

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24
Q

indications of Artemether and Artesunate

A

treatment of multidrug-resistant malaria

effective against quinine resistant strains

25
Q

side effects of Artemether and Artesunate

A

nausea, vomiting, diarrhea

26
Q

side effect of Lumefantrine

A

QT prolongation

27
Q

indication of Lumefantrine

A

in combination with artemether against P. falciparum

28
Q

why Artemether can’t be used for prophylaxis?

A

T1/2 is too short

29
Q

side effects of Malarone (atovaquone+Proguanil)

A

GI distress, fever, rash

30
Q

indication of Malarone

A

treatment+ prophylaxis of multidrug-resistant P. falciparum malaria

31
Q

mechanism of Atovaquone

A

disrupts mitochondrial metabolism

32
Q

mechanism of Proguanil

A

antimetabolite (↓folate synthesis)

33
Q

MoA of Primaquine

A

generates metabolites that act as oxidants

34
Q

side effects of Primaquine

A
  1. GI distress
  2. rash, headache
  3. acute hemolysis in G6PD deficient patients
  4. teratogenic
35
Q

what are the antibacterial and antiprotozoal indications of metronidazole?

A

antibacterial–> anaerobic gram - (mostly)

antiprotozal–> giardia lamblia, trichomonas vaginalis, antamoeba histolytica

36
Q

is metronidazole an inhibitor of the CYP450 enzyme?

A

yes

37
Q

mechanism of metronidazole

A

it undergoes reductive bioactivation of its nitro group –> form reactive free radicals –> interfere with nucleic acid synthesis

38
Q

how is metronidazole given?

A

oral and parenteral

39
Q

matabolism of metronidazole

A

hepatic

40
Q

side effects of metronidazole

A
  1. GI distress
  2. leukopenia
  3. CNS effects (neuropathy)
  4. dark discoloration of urine
  5. metallic taste
  6. Disulfiram like reaction with ethanol (nausea, vomiting, headache, hypotension)
41
Q

treatment of toxoplasmosis?

A

pyrimethamine/sulfadiazine

42
Q

what is the treatment of Leishmaniasis?

A

Stibogluconate

43
Q

what is the treatment of Trypanosoma Cruzi (Chagas disease)?

A

Nifurtimox

44
Q

what is the treatment of Trypanosoma brucei (sleeping sickness)?

A

“PMS”
Pentamidine- early infection stage
Melarsoprol- advanced infection–> CNS involvement
Suramin- early infection stage

45
Q

what are the drugs for helminthic infections?

A

“NIV”
Niclosamide
Ivermectin
Mebendazole

46
Q

how are helminthic drugs given?

A

orally

47
Q

what is the mechanism of action of Mebendazole?

A

inhibits microtubule synthesis

inhibits glucose uptake

48
Q

indications for Mebendazole (4)

A
  1. Ascaris lumbricoides
  2. Enterobius vermicularis (Pinworm infection)
  3. Trichuris Trichuria (whipworm infection)
  4. Visceral larva migrans
49
Q

side effects of mebendazole

A
  1. GI distress
  2. Granulocytopenia. alopecia (in high doses)
  3. teratogenic
50
Q

treatment of amebiasis (Entamoeba histolytica infection)

A

may require co-administration of metronidazole with luminal active agents (Paromomycin or Diloxanide)

51
Q

what does it mean that Mebendazole is a luminal active agent?

A

it means that 90% of the given dose is not absorbed –> stays in the lumen of the intestine

52
Q

does Ivermectin cross the BBB?

A

no

53
Q

what is the mechanism of Ivermectin?

A

facilitates GABA-mediated transmission in nematodes and causes immobilization of parasites

54
Q

mechanism of Niclosamide

A

Uncoupling oxidative phosphorylation

55
Q

indications of Ivermectin

A
  1. intestinal nematodes–> Strongyloids stercoralis

2. tissue/ blood nematodes–> cutaneous lrava migrans, oncocerca volvulus

56
Q

side effects of Ivermectin

A 
reaction to the dying worms (can be managed with antihistamine and NSAIDS's) :
fever, headache
rash, pruritis
joint and muscle pain
hypotension 
lymphadenopathy

*TERATOGENIC

57
Q

Indications of Niclosamide

A

TAPEWORMS:

  1. Taenia saginata (beef tapeworm)
  2. Taenia solium (pork tapeworm)
  3. Diphyllobothrium latum (fish tapeworm)
58
Q

side effects of Niclosamide

A

GI distress, fever, rash

*generally well tolerated

Pharma 2nd semester (49 decks)

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