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Principles of Therapy Core Drugs > Antiprotozoals > Flashcards

Antiprotozoals Flashcards

1
Q

Name 2 Artemesinins

A

Artemether-lumefantrine and Artesunate

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2
Q

Name 2 Quinolines

A

Mefloquine and Quinine

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3
Q

Name the Biguanide combination

A

Atovaquone-proguanil

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4
Q

Which 3 drug groups are Antimalarials?

A

Artemesinins
Quinolines
Biguanide combination

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5
Q

What is the classification of Quinine?

A

Quinoline

Antimalarial

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6
Q

What is the mechanism of action of Quinine?

A

Inhibits the parasite’s haem polymerase and forms a hydrogen-bonded complex with double-stranded DNA. This leads to inhibition of strand separation, transcription and protein synthesis.

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7
Q

What are the therapeutic indications of Quinine? (4)

A
  • Malaria suppression and treatment
  • Erythrocytic forms of all 4 plasmodia
  • No effect on the dormant forms or on the gametocytes of P. falciparum
  • Main treatment of P. falciparum
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8
Q

How is Quinine administered?

A

Orally over 7 day course, or slow IV infusion

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9
Q

Describe the absorption of Quinine

A

well absorbed from GIT

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10
Q

Describe the metabolism of Quinine

A

metabolized in the liver

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11
Q

Describe the excretion of Quinine

A

Metabolites are excreted in the urine within 24 hours

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12
Q

What is the half-life of Quinine?

A

10 hours

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13
Q

What are the adverse effects of Quinine? (5)

A
  • irritant to the gastric mucosa and can cause nausea and vomiting and epigastric pain
  • “cinchonism” (nausea, dizziness, tinnitis, headache and blurring of vision)
  • hypotension
  • cardiac dysrhythmias
  • severe central nervous system disturbances
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14
Q

What is the classification of Mefloquine?

A

Quinoline

Antimalarial

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15
Q

What is the mechanism of action of Mefloquine?

A

Inhibits the haem polymerase

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16
Q

What are the therapeutic indications of Mefloquine?

A
  • P. falciparum
  • P. vivax
  • Prophylaxis and treatment of chloroquine- resistant and multidrug-resistant falciparum malaria
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17
Q

How is Mefloquine administered?

A

orally

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18
Q

Describe the absorption of Mefloquine

A

rapidly absorbed

19
Q

What is the half-life of Mefloquine?

A

up to 30 days

20
Q

What is the main adverse effect of Mefloquine?

A

GIT disturbances

21
Q

What is a contraindication of Mefloquine?

A

pregnancy

22
Q

What is the classification of Atovaquone and Proguanil?

A

Folate antagonists
Biguanide combination
Antimalarial

23
Q

What is the mechanism of action of Atovaquone?

A

Selectively inhibits the parasitic electron transport chain

24
Q

What is the mechanism of action of Proguanil?

A

Inhibits the enzyme dihydrofolate reductase in the parasite

25
Q

What are the therapeutic indication for Atovaquone and Proguanil?

A
  • chloroquine and multi-drug resistant strains of P. falciparum and P. vivax
  • prophylaxis
26
Q

How is Atovaquone and Proguanil administered?

A

orally (in combination with others)

27
Q

What is the half-life of Atovaquone?

A

2-3 days

28
Q

What is the half-life of Proguanil?

A

16 hours

29
Q

What are the adverse affects of Atovaquone and Proguanil?

A

very few in therapeutic doses

30
Q

What is the mechanism of action of Artemesinins?

A

Ativated by free or haem-bound iron causing the production of a reactive radical which leads to alkylation of proteins and haem in the parasite

31
Q

What are the therapeutic indications of Artesunate?

A

used intravenously for the management of severe malaria

32
Q

What are the therapeutic indications of Artemether and Lumefantrine?

A

used in combination for management of mild malaria (orally)

33
Q

What are the 2 adverse effects of Artemesinins?

A
  • Neurotoxicity: most common effect are headache and dizziness.
  • Cardiotoxicity: may cause elongated QT interval.
34
Q

What is the classification of Mebendazole?

A

Anthelmintic

Antinematodal

35
Q

What is the mechanism of action of Mebendazole?

A

Binds to free beta-tubulin, inhibiting its polymerization and thus interfering with microtubule-dependent glucose uptake in the worm

36
Q

What are the therapeutic indications of Mebendazole?

A

first choice agent against nematodes

37
Q

What is the spectrum of activity of Mebendazole?

A

broad

38
Q

What are the adverse effects Mebendazole? (2)

A
  • in children infested with large numbers of Ascaris worms: Nausea and vomiting, abdominal pain and diarrhoea
  • normal doses: few adverse effects
39
Q

What are the contraindications of Mebendazole?

A

Pregnancy: embryotoxic and teratogenic

40
Q

Describe the absorption of Mebendazole

A

Less than 10% of mebendazole is absorbed after oral administration, the absorbed agent is more than 90% bound to plasma proteins

41
Q

Describe the metabolism of Mebendazole

A

rapidly metabolized in the liver to inactive metabolites

42
Q

Describe the excretion of Mebendazole?

A

excreted in the urine and the bile within 24-48 hours

43
Q

How can the absorption of Mebendazole be increased?

A

when it is taken with a fatty meal

Principles of Therapy Core Drugs (8 decks)

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