Antimalarial Flashcards

1
Q

what are the 4 Plasmodium that infect humans

A
  • P. falciparum
  • P. Vivaz
  • P. Ovale
  • P. Malariae
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2
Q

Malaria has what two stages

A
  • human liver stage: dormant
    • hypnozoite
  • human blood stage
    • merozoite
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3
Q

which plasmodium species have secondary tissue forms?

A

P. Ovale and P. vivax

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4
Q

what is a “clinical cure”

A
  • therapy that is used to suppress symptoms
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5
Q

function of blood schizonticides

A

act on erythrocytic forms of the parasite

  • ***Do NOT affect the secondary tissue forms of P. vivax and P. Ovale
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6
Q

function of tissue schizonticides

A
  • act on hepatic stages
  • prevent relapses
  • do not suppress symtpoms once erythrocytic stages have been established
  • can prevent initial development of malaria (Prophylaxis), but generally too toxic
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7
Q

function of gametocidal agents

A
  • act on gametocytes
  • may slow spread of the disease
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8
Q

DOC: sensitive plasmodium organisms

A

Chloroquine

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9
Q

function of Chloroquine

A

active against asexual erythrocytic forms

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10
Q

problem with treating with Chloroquine

A

resistant forms (particularly P. Falciparum) are a serious problem

  • transport pump removes drug from parasite
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11
Q

MOA: Chloroquine

A
  • exact MOA not fully elucidated
  • may interfere with lysosomal degradation of hemoglobin
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12
Q

route of administration: Chloroquine

A

oral or parenteral

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13
Q

accumulation of Chloroquine

A

melanin-rich tissues: skin, retina

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14
Q

toxicity of Chloroquine

A
  • retinal and corneal toxicity
  • ototoxicity
  • hemolysis - G6PD deficiency
  • QT prolongation
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15
Q

DOC: plasmodium infections that are chloroquine-resistant

A

Mefloquine

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16
Q

DOC: prophylaxis against all chloroquine-resistant plasmodia

A

Mefloquine

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17
Q

route of administration of Mefloquine

A

oral

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18
Q

toxicity of Mefloquine

A
  • depression of myocardium
  • seizures
  • may aggravate latent psychoses
  • vivid dreams
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19
Q

contraindications for Mefloquine

A
  • patients with a history of mental illness or epilepsy
  • pregnant women: teratogenicity
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20
Q

function of Quinine and Quinidine Gluconate

A
  • acts on erythrocytic forms
21
Q

Quinine and Quinidine Gluconate is Gametocidal against which plasmodium organisms

A
  • P. vivax
  • P. ovale
22
Q

which therapys are found in cinchona bark

A

Quinine and Quinidine Gluconate

23
Q

DOC: treatment of complicated, chloroquine-resistant plasmodia

A

Quinine and Quinidine Gluconate

24
Q

DOC: unconscious patient

A

Quinine and Quinidine Gluconate combined with doxycycline or clindamycin

25
Q

route of administration of quinine

A

oral

26
Q

route of administration of Quinidine Gluconate

A

IV

27
Q

toxicity of Quinine and Quinidine Gluconate

A
  • Cinchonism: overdose: tinnitus, HA, dizziness, flushing, visual disturbances
  • antiarrhythmic agent: class 1A
  • QT elongation
  • hemolysis in G6PD
28
Q

Use of doxycycline with quinidine gluconate (or quinine sulfate)

A

another option for treatment of complicated chloroquine-resistant malaria

29
Q

Use of clindamycin with quinidine gluconate (or quinine sulfate)

A

another option for treatment of complicated chloroquine-resistant malaria in children/pregnant women

30
Q

Name the 4 folate metabolism inhibitors

A
  • Pyrimethamine
  • Proguanil
  • Trimethoprim
  • pyrimethamine + sulfadoxine (not available in US)
31
Q

folate metabolism inhibitors target what malaria forms

A

main effect on erythrocytic forms

32
Q

how does malaria become resistant to folate metabolism inhibitors?

A

create mutations in dihydrofolic acid

33
Q

specific MOA of sulfadoxine

A
  • **sulfonamide
  • inhibits incorporation of PABA into folic acid
34
Q

specific MOA of pyrimethamine and proguanil

A

inhibit dihydrofolate reductase, blocking conversion of dihydrofolic acid to tetrahydrofolic acid

35
Q

Function of atovaquone + proguanil

A
  • synergistic combination
  • active against tissue and erythrocytic forms
36
Q

Is Artemisinin used as monotherapy

A

No!

  • artemisinin combination treatment (ACT)
37
Q

use of Artemether/Lumefantrine

A
  • chloroquine resistant P. falciparum and P. vivax
38
Q

contraindications Artemether/Lumefantrine

A

patients with a h/o cardiac disease or prolonged QT interval

39
Q

what is the therapy for tissue schizonticide

A

Primaquine

40
Q

List the Blood Schizonticides

A
  • Choloquine
  • Mefloquine
  • Quinine sulfate and Quinidine gluconate
  • doxycycline
  • pyrimethamine + sulfadoxine
  • trimethoprim
  • proguanil
  • atovaquone + proguanil
  • artemisinin
41
Q

“radical cure”

A
  • of P. vivax and P.ovale
  • used for terminal prophylaxis
42
Q

route of administration of Primaquine

A

oral

43
Q

toxicity of Primaquine

A
  • hemolytic anemia: G6PD deficiency
44
Q

contraindications of Primaquine

A
  1. G6PD deficiency: treat relapse
  2. SLE or RA
  3. pregnant females
45
Q

treatment options for chloroquine-resistant P. falciparum

A
  • quinine sulfate + doxycycline/clindamycin/tetracycline
  • mefloquine
  • atovaquone with proguanil
  • artemether-lumefantrine
46
Q

treatment for severe malaria

A
  • Quinidine + doxycycline/clindamycin/tetracycline
47
Q

treatment for prevention of relapse from P. vivax and P. ovale

A

Primaquine

48
Q

treatment of P. vivax or P. ovale

A
  • chloroquine
  • quinine sulfate + doxycycline
  • mefloquine
  • atovaquone with proguanil