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Pharmacology > Antiparasitics > Flashcards

Antiparasitics Flashcards

1
Q

Why is malaria difficult to target?

A

Undergoes gross changes in morphology, localisation and metabolic pathways.

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2
Q

Melarsen

A

Organic arsenical against trypanosomes. Inhibits lipoic-dependent and other dithiol containing Metallo-enzymes. Actively accumulated in trypanosoma.

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3
Q

Suramin

A

Anti-trypanosomal without toxic metal atom. Cannot cross BBB so only effective in early stages.

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4
Q

Chloroquine

A

Antimalarial. Inhibits the formation of hemozoin either by inhibiting polymerase or through complexation of heme.

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5
Q

Artemisinin

A

Anti malarial

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6
Q

Sulfadoxin

A

Anti malarial anti metabolite. Inhibits folate synthesis pathway. Inhibits DHPS.

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7
Q

Pyrimethamine

A

Anti malarial anti metabolite. Inhibits folate synthesis pathway. Inhibits DHFR.

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8
Q

Fansidar

A

Anti malarial anti metabolite. Inhibits folate synthesis pathway. Inhibits DHPS and DHFR. Combination drug.

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9
Q

What are helminths?

A

Multicellular eukaryotes such as nematodes (roundworms).

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10
Q

What are Protozoa?

A

Unicellular eukaryotes

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11
Q

What are the main targets of anti-helmintics?

A

Energy metabolism, neuromuscular coordination and micro tubule dynamics.

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12
Q

Closantel

A

Antihelmentic that targets energy metabolism. Uncoupled oxidative phosphorylation.

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13
Q

Clorsulon

A

Antihelmentic that targets energy metabolism. Inhibits glycolysis.

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14
Q

Thiobendazoles

A

Block microtubule dynamics in helminths. Bind to beta-tubulin in tubular dimer and cause depolymerisation. 300-400 fold lower affinity for mammalian beta-tubulin.

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15
Q

Invermectin and piperazine

A

Anti helminths that target neuromuscular coordination. Enhance inhibitory neurotransmission.

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16
Q

Levamisole

A

Anti helminths that target neuromuscular coordination. Nicotinic ACh receptor agonist that causes muscle contraction and spastic paralysis.

17
Q

Paraherquamide

A

Anti helminths that target neuromuscular coordination. Nicotinic antagonist - causes flaccid paralysis.

18
Q

Praziquantel

A

Broad spectrum anti helmintic that targets neuromuscular coordination. Binds to VGCa channels, causes Ca increase and sustained contraction - spastic paralysis. Also changes external surface structure facilitating antibody binding and sensitivity to immune response.

19
Q

How does trypanosomiasis differ in its early stage and late stage?

A

Early stage in blood stream. Late stage penetrates CNS.

Pharmacology (11 decks)

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