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Pharm > Malaria Drugs > Flashcards

Malaria Drugs Flashcards

1
Q

Quinine (Qualaquin)

A

Class: Quinolone derivitive
Mech: Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
Thera: Prophylaxis, treatment of acute malarial attacks
Important SE’s: Cinchonism, hypotension, hypoglycemia, abortion, arrhythmias
Misc: Also called quinidine (used in anti-arrhythmias)

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2
Q

Chloroquine (Aralen)

A

Class: Quinolone derivitive
Mech: Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
Thera: Prophylaxis, treatment of acute malarial attacks
Important SE’s: Itching (Africans), retinitis (rare)

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3
Q

Hydroxychloroquine (Plaquenil)

A

Class: Quinolone derivitive
Mech: Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
Thera: Prophylaxis, treatment of acute malarial attacks

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4
Q

Mefloquine (Lariam)

A

Class: Quinolone derivitive
Mech: Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
Thera: Prophylaxis, treatment of acute malarial attacks

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5
Q

Primaquine (Primaryl)

A

Class: Quinolone derivitive
Mech: Forms quinolone-quinone intermediates that oxidize schizont membranes
Thera: Prophylaxis, treatment of acute malarial attacks, also prevent relapses
Important SE’s: Hemolysis (G6PD deficiency), methemoglobinemia
Other SE’s: Fever, nausea, vomiting
Misc: Only drug that inhibits exoerythrocytic schyzogony

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6
Q

Amantadine (Symmetrel)

A

Mech: Positive charge helps chloroquine overcome chloroquine-resistant malaria vacuoles; point mutations against amantadine return bacteria to chloroquine-sensitivity

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7
Q

Artesunate

A

Class: Artemisinin compound
Mech: Specifically and selectively inhibit SERCA of P. falciparum
Important SE’s: Neurotoxicity, prolongation of QT interval
Misc: can use IV form for severe cases of malaria

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8
Q

Artemether

A

Class: Artemisinin compound
Mech: Specifically and selectively inhibit SERCA of P. falciparum

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9
Q

Lumefantrine

A

Class: Aminoalcohol
Thera: Used in combination w/artemether (called Coartem); want to avoid resistance!!
Misc: Also called benflumentol

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10
Q

Atovaquone (Mepron)

A

Class: Napthalene
Mech: Depolarizes parasitic mitochondria and inhibits their electron transport
Thera: Used in combination w/proguanil
Misc: use for prophylaxis and treatment of malaria due to P. falciparum, including chloroquine-resistant strains

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11
Q

Chloroguanide (Malarone)

A

Class: Antifolates
Mech: Dihydrofolate reductase inhibitors (human and parasite pathway)
Important SE’s: Rare
Misc: Also called proguanil

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12
Q

Tetracycline (Tetracyn)

A

Class: Antibiotic
Thera: Severe malaria & chloroquine-resistant uncomplicated malaria

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13
Q

Clindamycin (Cleocin)

A

Class: Antibiotic
Thera: Severe malaria & chloroquine-resistant uncomplicated malaria

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14
Q

Doxycycline (Adoxa)

A

Class: Antibiotic
Thera: Severe malaria & chloroquine-resistant uncomplicated malaria
Important SE’s: Photosensitivity

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15
Q

Characteristics of the five human forms of malaria?

A
  1. P vivax: wide distribution, often involved in relapses
  2. P falciparum: most lethal and common, much resistance to major drugs
  3. P malariae: less common, could cause asymptomatic infections that can last for decades
  4. P ovale: less common, involved in relapses
  5. P knowlesi: thought to be just monkeys, but now some cases in humans
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16
Q

Clinical signs of malaria

A
  1. Periodic episodes of chills and fevers
  2. Usually enlarged liver and spleen
  3. Identified parasites in blood smears
17
Q

Frequency of febrile paroxysms:

A

Vivax: 2 days;
Malariae: 3 days;
Falciparum: irregular

18
Q

Quinoline derivatives include

A

quinine/quinidine, chloroquine, mefloquine, primaquine

19
Q

What is the only parenteral antimalarial available in the US?

A

Quinine/quinidine (latter with gluconate)

20
Q

Chloroquine’s uses and where is there sensitivity and resistance?

A

Prophylaxis and acute attacks;

sens: Central America, Saudi Arabia and Egypt;
resistance: a lot of Africa, Asia, South America

21
Q

List how chloroquine works on cells with parasites (mechanism):

A
  1. Chloroquine can’t leave digestive vacuoles if there is a point mutation preventing chloroquine release
  2. Chloroquine can be released if there is a mutation in that positive charge
  3. Give amantadine (an antiviral) that can prevent CQ from exiting again, allowing for toxic complexes of chloroquine and heme to accumulate
  4. If there’s a mutation such that the channel is resistant to the amantadine, it becomes CQ sensitive again!!
22
Q

SE’s of mefloquine

A

Affects nervous system and causes psychotic effects

23
Q

What does a drug take advantage of to get into a digestive vacuole?

A

Uses a pH gradient (going from 7.4 to 4.8 from the plasma, RBC cytoplasm, parasite cytoplasm, to food vacuole

24
Q

Chemoprophylaxis: what do you use in four different areas

A

CQ-sens zone: chloroquine;
CQ-resistant zone: mefloquine, doxycycline, atovaquone/proguanil;
mefloquine-resistant zone: doxycycline, atovaquone/proguanil;
terminal prophylaxis: primaquine

25
Q

For treatment of severe malaria, what protocol can you follow?

A
  1. IV quinidine gluconate plus tetracycline, doxycycline, or clindamycin (ICU, cardiac function, parasitemia, glucose, Hb, electrolytes)
  2. IV artesunate followed by atovaquone-proguanil, doxycycline (dlindamycin in pregnant women), or mefloquine
  3. Exchange blood transfusion (if altered mental status, pulmonary edema, renal complications)
26
Q

How to treat chloroquine sens strains?

A
  1. P falciparum, malariae, or knowlesi by chloroquine phosphate with alternative hydroxychloroquine
  2. P vivax, ovale: chloroquine phosphate and primaquine phosphate (with alternative hydroxychloroquine and primaquine phosphate)
27
Q

How to treat CQ-resistant strains?

A
  1. P falciparum: atovaquone-proguanil (alternatives artemether-lumefantrine, quinine sulfate plus either doxy, tetra, or clindo for children younger than 8 or preg, and mefloquine)
  2. P. vivax: quinine sulfate and doxy or tetra, and primaquine phosphate, with alternatives atovaquone-proguanil + primaquine phosphate, or mefloquine and primaquine phosphate
28
Q

To eradicate persistent exoerythrocytic parasites after clinical cure of acute attack by _____ or _____, what is the drug of choice?

A

Vivax or ovale; Primaquine phosphate

Pharm (23 decks)

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