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Pharmacology > Exam 9: Antimalarial Drugs > Flashcards

Exam 9: Antimalarial Drugs Flashcards

1
Q

What is the most effective way to combat malaria?

A

Prevention

Killing the mosquitos

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2
Q

What is the difference between a clinical cure and a radical cure?

A

Clinical cure- erythrocytic forms of the parasite are eradicated and the patient has no symptoms.
Radical Cure- All forms of the parasite have been eradicated

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3
Q

What is the difference between Causal Prophylaxis and Suppressive Agents?

A

Causal prophylaxis targets the primary (hepatic) form of the parasite (less practical)
Suppressive Agents- Target erythrocytic forms and suppress symptoms

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4
Q

What forms do Chloroquine and Hydroxychloroquine act on?

A

Erythrocytic forms

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5
Q

Chloroquine and Hydroxychloroquine mechanism

A

Affect the pH of the parasite’s food vacuoles, interfering with their feeding

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6
Q

For what species are Chloroquine and Hydroxychloroquine clinical cures? Radical cures?

A

Clinical cures for all

Radical cures for P. falciparum and P. malariae (not vivax and ovale)

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7
Q

What is a problem with the use of Chloroquine and Hydroxychloroquine?

A

Resistance, especially with P. falciparum

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8
Q

What causes resistance to Chloroquine and Hydroxychloroquine?

A

A transport pump that removes the drug from the parasite

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9
Q

How are Chloroquine and Hydroxychloroquine metabolized?

A

Liver

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10
Q

What are adverse effects of Chloroquine and Hydroxychloroquine?

A

CNS- dizziness, headache, tinnitus
GI Upset
Retina and corneal toxicity
Immunological problems

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11
Q

In whom are Chloroquine and Hydroxychloroquine contraindicated?

A

Patients with psoriasis or porphyria

Due to immune effects

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12
Q

What is a special use of Hydroxychloroquine?

A

Rheumatoid Arthritis and SLE due to its anti-inflammatory actions at high doses
(potential for serious toxicity at these doses though…)

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13
Q

What is the mechanism of Quinine and Quinidine?

A

Interference with digestion of hemoglobin

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14
Q

What is a time when you’d use Quinine or Quinidine?

A

Chloroquine-resistant P. falciparum

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15
Q

How are Quinine and Quinidine taken?

A

Orally.

Also an IV preparation of Quinidine in the US

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16
Q

What are adverse effects of Quinine and Quinidine?

A 
GI irritation
Visual and auditory disturbances
Bradycardia
Teratogenic/abortion
Skeletal muscle relaxation
Cinchonism (headache, nausea, vomiting, dizziness, tinnitus, blurred vision)
17
Q

When might you use Mefloquine?

A

Chloroquine-resistant P. falciparum

18
Q

When shouldn’t you use Mefloquine?

A

Serious, life threatening infections.

It can only be taken orally.

19
Q

Adverse effects of Mefloquine?

A

Seizures
Activates latent psychosis
GI and cardiac problems

20
Q

When is Mefloquine contraindicated?

A

Patients with epilepsy, mental illness, or cardiovascular problems

21
Q

What are two inhibitors of folic acid synthesis that are used to treat Malaria?

A

Pyrimethamine and Proguanil

22
Q

What is the mechanism of Pyrimethamine and Proguanil?

A

Inhibition of DHFR

23
Q

When are Pyrimethamine and Proguanil mostly used?

A

Prophylaxis, especially against Chloroquine-resistant P. falciparum

24
Q

When might you use pyrimethamine plus sulfadoxine combination?

A

Presumptive treatment (person shows symptoms, but you haven’t diagnosed them for sure yet)

25
Q

What is the mechanism of Atovaquone?

A

Depolarizes the parasite’s mitochondria and inhibiting electron transport

26
Q

What is often used in combo with Atovaquone?

A

Proguanil (DHFR inhibitor)

27
Q

When might you use Atovaquine + Proguanil?

A

Prophylaxis against Chloroquine-resistant P. falciparum

28
Q

What are two downsides to Atovaquine + Proguanil?

A
  1. Expensive

2. Must be taken daily

29
Q

What is artemisinin?

A

An isolate of an herbal preparation that is part of Coartem.

30
Q

What is Coartem?

A

A product that contains an artemisinin derivative and is quickly becoming the primary drug used to treat most forms of malaria including Chloroquine-resistant P. falciparum

31
Q

What are a couple of regular antibiotics that have activity against plasmodium species?

A

Tetracycline//doxycycline

32
Q

What is Primaquine used for?

A

Follow up treatment when you think a person may have been infected with P. vivax or ovale

33
Q

What is the advantage of Primaquine? Disadvantage?

A

Can kill the plasmodium parasites in the liver (eradicate latent phase)
Disadvantage is that it has toxicities (CNS, GI, and can cause hemolytic anemia in patients with G6PD deficiency)

34
Q

Primaquine toxicity

A

Hemolytic anemia in patients with G6PD deficiency
GI upset
Headaches/dizziness

35
Q

What would you use for an acute, uncomplicated attack of malaria?

A 
Chloroquine
Quinine/Quinidine
Coartem (artemether/lumefantrine)
Mefloquine
Atovaquine + Proguanil
Doxycycline
36
Q

What is used for a radical cure of P. vivax/ovale?

A

Primaquine

37
Q

What are 5 drugs used for malaria prophylaxis?

A

Chloroquine (mostly)
Mefloquine (Chloroquine-resistant P. falciparum)
Doxycycline
Atovaquine + Proguanil
Primaquine (follow up therapy to eradicate P. vivix/ovale

Pharmacology (34 decks)

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