Lecture 73

Question 1

Chloroquine: 1) Drug class 2) Target species/stage 3) Mode of action

Answer 1

Class: Antimalarial

Target species/stage: Erythrocytic forms of plasmodium spp.

MOA: Prevents Plasmodium from detoxifying heme to hemozoin

Question 2

Quinine: 1) Drug class 2) Target species/stage 3) Mode of action

Answer 2

Class: Antimalarial

Target species: Erythrocytic stage of Plasmodium spp.

MOA: Prevents plasmodium from detoxifying heme to hemozin

Question 3

Mefloquine: 1) Drug class 2) Target species/stage 3) Mode of action 4) Should be followed by _______ to eradicate hypnozoites for P. ______. 5) Has very long ______ and is contraindicated in _______ women bc it is ________.

Answer 3

Class: Antimalarial

Target species: Erythrocytic stage of Plasmodium spp. –> schizonticidal

MOA: Prevents plasmodium from detoxifying hemozoin

Should be followed by Primaquine for P. vivax

Has very long Half-life and is contraindicated in pregnant women bc it is Teratogenic.

Question 4

Halofantrine 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 4

Class: antimalarial

Target: erythrocytic stage

MOA: Prevents heme detox

Notes: SEVERE heart problems. Contraindicated in pregnancy

Question 5

Lumefantrine + Artemether (Coartem) 1) Drug class 2) Target species/stage 3) mechanism of action 4) Related to ______, but lesser side effects.

Answer 5

Class: Antimalarial

Target: Resistant P. falciparum

MOA: Prevents heme detoxification

Notes: Related to halofantrine, but does not cause the same toxicity (mild side effects)

Question 6

Pyrimethamine and Proganil 1) Drug class 2) Target species/stage 3) mechanism of action

Answer 6

Class: Antimalarial

Target: Erythrocytic Plasmodium spp

MOA: Inhibits DHFR (just like trimethoprim)

Question 7

What is Fansidar? Side effects?

Answer 7

Sulfadoxine + Pyrimethamine

Side effects: may cause skin problems and allergy. Megaloblastic anemia from Pyrimethamine in high dose.

Question 8

Primaquine 1) Drug class 2) Target species/stage 3) mechanism of action 4) Usage Notes: Why is primaquine contraindicated in those with a G6PD deficiency?

Answer 8

Class: antimalarial

Target: Liver hypnozoites (P. vivax and ovale) and gametocytes (all spp)

MOA: Prevents pickup by mosquitoes by possibly generating ROS

Usage Notes: High doeses causes metHbemia and cyanosis. Because the drug causes ROS development, which those with the condition cannot tolerate.

Question 9

Atovaquone 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 9

Class: Antimalarial

Target: Tissue and erythrocytic schizonts

MOA: inhibits CytBC1 -> blocks mito’s ETC; blocks dihydroorotate DH (pyrimidine synth)

Notes: contraindicated in pregnancy

Question 10

Benznidazole 1) Drug class 2) Target species/stage 3) mechanism of action

Answer 10

Class: Antitrypanosomal

Target: T cruzi / Chaga’s disease

MOA: inhibits protein and RNA synthesis

Question 11

Pentamidine 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 11

Class: Antitrypanosomal

Target: T. gambiense/West african sleeping sickness

MOA: Unknown

Usage: Early infection only because it does not penetrate the CNS well.

Question 12

Eflornithine 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 12

Class: antitrypanosomal

Target: T. gambiense/ W. African sleeping sickness

MOA: Inhibits ornithine decarboxylase -> no polyamines

Usage: Late stage sickness, because it has good CNS penetration.

Question 13

Suramin 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 13

Class: Antitrypanosomal

Target: T rhodesiense/ E. African sleeping sickness

MOA: unknown

Use: Early stages only due to poor CNS penetration

Question 14

Melarsoprol 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 14

Class: Antitrypanosomal

Target: T rhodesiense

MOA: Prodrug that is activated into melarsen oxide to irreversibly bind to sulfhydryl groups on small molecules, proteins and enzymes.

Use: Late stage only; contraindicated in pregnancy; reactive encephalopathy.

Question 15

Albendazole and Mebendazole 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 15

Class: Benzimidazoles; Antihelminthic

Target: Motility, division, and glucose uptake

MOA: binds to tubulin, blocking microtuble formation, causing paralysis and energy depletion (microtubulin dependent glucose uptake)

Notes: Broad spectrum

Question 16

Praziquantel 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 16

Class: Anti-tapeworm and anti trematodes (schitosomiasis)

Target: mobility

MOA: increases Ca influx, causing prolonged contraction/paralysis

Notes: Azoles increase side effects; anticonvulsants are antagonists.

Question 17

Diethylcarbamazine 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 17

Class: Antihelminthic

Target: lymphatic filariasis by Wuchereria

MOA: uncertain, but may involve sensitizing microfilariae to phagocytosis

Notes: Contraindicated in pregnancy.

Question 18

Ivermectin 1) Drug class 2) Target species/stage 3) mechanism of action 4) usage notes

Answer 18

Class: Antihelminthic

Target: Strongyloidiasis, Onchocerciasis

MOA: Binds to Glutamate-gated Cl channels to hyperpolarize cells and cause paralysis

Notes: can cause blindness