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Heme Pharm > Anti-Malarials > Flashcards

Anti-Malarials Flashcards

1
Q

Drugs for the prevention of malaria in travelers in areas without resistant P. falciparum

A

Chloroquine

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2
Q

Drugs for the prevention of malaria in travelers in areas with chloroquine resistant P. falciparum

A

Atovaquone + Proguanil (Malarone) Mefloquine

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3
Q

Drugs for the prevention of malaria in travelers in areas with multidrug resistant P. falciparum

A

Doxycycline

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4
Q

Terminal prophylaxis of P. vivid and P. ovale infections; alternative for primary prevention

A

Primaquine

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5
Q

4 species of plasmodium which cause malaria

A

– Plasmodium falciparum – Plasmodium vivax – Plasmodium malariae – Plasmodium ovale

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6
Q

Most virulent species of plasmodium; responsible for most of serious complications & deaths

A

Plasmodium falciparum

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7
Q

Drug resistance (important therapeutic problem is most notable with this virulent species)

A

Plasmodium falciparum

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8
Q

primarily pathogenic to monkeys; now known to cause illness to humans in Asia

A

P. knowlesi

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9
Q

Stage 1 of lifecycle: Transmission of (1) by Plasmodium-infected Anopheles into the bloodstream

A
  1. sporozoites
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10
Q

Stages 2&3 of lifecycle: (1) invade (2); divide forming (3)

A
  1. Sporozoites 2. Liver 3. multinucleated schizonts (pre-erythrocytic stage)
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11
Q

Active against hepatic-stage schizonts (stages 2 and 3)

A

Atovaquone-proguanil and primaquine

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12
Q

Stage 4: (1) rupture & release (2) to blood; invade RBC, forming (3) & later (4)

A
  1. Schizonts 2. merozoites 3. trophozoites 4. multinucleated schizonts (erythrocytic stage)
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13
Q

Blood-stage schizonticides (stage 4)

A

Quinoline derivatives (Chloroquine, amodiaquine, quinine, quinidine, mefloquine, primaquine, lumefantrine & halofantrine) Antifolates (sulfadoxine-pyrimethamine, atovaquone-proguanil) Antimicrobials (tetracycline, doxycycline and clindamycin) Artemisinin derivatives interrupt schizogony within red cells

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14
Q

Quinoline derivatives (Chloroquine, amodiaquine, quinine, quinidine, mefloquine, primaquine, lumefantrine & halofantrine)

A

stages 2, 3, 4, 5 Active against hepatic-stage schizonts Active against blood-stage schizonticides gametocidal drug (primaquine)

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15
Q

Antifolates (sulfadoxine-pyrimethamine, atovaquone-proguanil)

A

stages 2, 3, 4 Active against hepatic-stage schizonts Active against blood-stage schizonticides

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16
Q

Antimicrobials (doxycycline)

A

Active against Blood-stage schizonticides (stage 4)

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17
Q

Artemisinin derivatives interrupt schizogony within red cells

A

Active against Blood-stage schizonticides (stage 4) gametocidal drugs (Stage 5)

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18
Q

Stage 5. Some merozoites differentiate into ♂ or ♀ (1); ingested by the Anopheles mosquito & mature in the mid-gut to (2) (migrate to the salivary glands of the mosquito)

A
  1. gametocytes 2. sporozoites
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19
Q

gametocidal drugs

A

Artemisinin derivatives and Primaquine

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20
Q

Tissue schizonticides

A

drugs that eliminate developing or dormant liver forms

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21
Q

Blood schizonticides

A

drugs that act on erythrocytic forms of the parasites

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22
Q

Gametocidal drugs

A

drugs that kill sexual stages & prevent transmission to mosquitoes

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23
Q

Causal prophylactic drugs

A

prevent erythrocytic infection

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24
Q

Treatment & chemoprophylaxis of infection with sensitive parasites

A

Chloroquine

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25
Q

Treatment of severe P. falciparum infections, especially cerebral malaria

26
Q

Chemoprophylaxis and Treatment of infections with P. falciparum

A

Mefloquine

27
Q

Treatment of infections with some chloroquine‐resistant P. falciparum; could be combined with artesunate; preventive therapy in endemic areas

A

Sulfadoxine-pyrimethamine

28
Q

Treatment and chemoprophylaxis of P. falciparum infections

A

Atovaquone + Proguanil (Malarone)

29
Q

Radical cure and terminal prophylaxis of infections with P. vivax and P. ovale; alternative chemoprophylaxis for all species

A

Primaquine

30
Q

Drug of choice for treatment of P. falciparum-sensitive malaria & chemoprophylaxis of malaria

A

Chloroquine

31
Q

Mutations in a (1) correlates with P. falciparum resistance

A
  1. putative transporter (PfCRT)
32
Q

Terminate fever in 24-48 hours; Clears parasitemia in 48-72 hours

A

Chloroquine

33
Q

Almost complete GIT absorption

A

Chloroquine

34
Q

mechanism of action: concentrates in parasite food vacuoles; increases (1) and toxicity to parasite

A
  1. free heme Chloroquine; Amodiaquine
35
Q

Amodiaquine a/e

A

Agranulocytosis, aplastic anemia and hepatotoxicity are common adverse effects

36
Q

Chloroquine a/e

A

Pruritus Nausea, abdominal pain, blurring of vision Hemolysis in persons deficient in G6PD Hypotension ECG changes: QRS widening; T wave abnormalities

37
Q

First line therapies for P. falciparum malaria, especially cerebral malaria

38
Q

Alkaloid from bark of cinchona tree

39
Q

Rapid-acting, highly effective schizonticide against all four human malaria parasites

40
Q

Quinine: gametocidal against (1) but not (2)

A
  1. P. vivax and P. ovale 2. P. falciparum
41
Q

Quinine versus quinidine - which has shorter half life

42
Q

Quinine a/e

A

Cinchonism: Tinnitus; Headache; Visual disturbances; Nausea; Dizziness; Flushing Hypersensitivity reactions Hemolytic abnormalities Hypoglycemia ECG abnormalities

43
Q

Contraindicated with quinine

A

Mefloquine Al3+ containing antacids warfarin and digoxin

44
Q

Strong blood schizonticidal activity against P. falciparum and P. vivax

A

Mefloquine

45
Q

Disrupts plasmodia mitochondria electron transport

A

Atovaquone + Proguanil (Malarone)

46
Q

Acts against Tissue/Erythrocytic schizonts

A

Atovaquone + Proguanil (Malarone)

47
Q

Atovaquone + Proguanil (Malarone) a/e

A

Abdominal pain, nausea, vomiting, diarrhea, rash

48
Q

Contraindication Atovaquone + Proguanil (Malarone)

A

Co-administration with tetracycline or rifampin

50
Q

Active drug = Cycloguanil, a
triazine metabolite

51
Q

Folate synthesis blockade ‐ selec􀆟􀆟ve ↓ of
plasmodial dihydrofolate reductase
activity)

52
Q

Erythrocytic forms of all four human
malarial species

A

Pyrimethamine

Proguanil

53
Q

↓Bacterial protein synthesis (also ↓Protein synthesis in plasmodial species)

A

Doxycyclin and Tetracyclin

54
Q

a/e of doxycyclin and tetracyclin

A

GI symptoms; photosensitivity

55
Q

standard prophylactic drug in SE
Asia

A

Doxycyclin (in combination with Mefloquine)

56
Q

Available as a fixed dose combination with Artemether – 1st line therapy for
uncomplicated malaria in most of Africa

A

Lumefantrine

57
Q

a/e of Halofantrine

A

Dose-related QT and PR intervals prolongation
Embryo-toxic, thus contraindicated in pregnancy

58
Q

production of free radicals following iron catalyzed cleavage of artemisinin endoperoxide bridge in the parasite’s food vacuole

A

Artemisinin

59
Q

inhibition of parasite’s calcium ATPase

A

Artemisinin

60
Q

Artemisinin a/e

A

N/V

diarrhea, dizziness

Rare:

neutropenia, anemia, hemolysis, allergic reactions

Heme Pharm (13 decks)

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