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MODA drugs > Anthelmintics > Flashcards

Anthelmintics Flashcards

1
Q

Benzimidazoles (group) BZ

A 
eg Thiabendazole and fenbendazole
Act against cellular integrity
Inhibitors of tubulin polymerisation
Bind beta-tubulin at growing end - prevent elongation
Deplete energy reserves
Inhibit excretion of waste
Slow starvation
Slow release boluses or prodrugs
Poorly soluble in water and given orally
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2
Q

Thiabendazole

A

A benzimidazole
Act against cellular integrity
Inhibitors of tubulin polymerisation
Slow

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3
Q

Fenbendazole

A 
A benzimidazole
Act against cellular integrity
Inhibitors of tubulin polymerisation
Febantel hydrolysed to active fenbendazole
Slow
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4
Q

Salicylanilides (group)

A

eg Closantel
Act against cellular integrity
Uncoupler of oxidative phosphorylation
Cause fall in tegument pH in liver fluke
Lipophilic H+ moiety allows to act as protonophores
Bind plasma proteins - ingested by blood sucking helminths
Lipophilic - can cross biological membranes
Similar effects on mammalian mitochondria
Slow

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5
Q

Clorsulon

A

Act against cellular integrity
Inhibit enzymes in glycolytic pathway
Inhibits phosphoglycerate kinase and mutase
Binds plasma proteins - blood ingesting helminths

Slow

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5
Q

Praziquantel

A 
Act against cellular integrity
Tegument disruption and vacuolisation
Ca2+ permeabilisers - cause Ca influx 
Spastic paralysis
Slow
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6
Q

Proteinases

A

Act against cellular integrity
Tegument disruption
Maybe Ca2+ permeabilisers
Slow

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7
Q

Organophosphates

A

Affect NM coordination
Cholinesterase inhibitors
Phosphorylate active site serine residue
Alkaline secretions of host GI tract hydrolyze and inhibit them
Fast and irreversible
Pralidoxime chloride antidote - reactivates AChEs by cleaving phosphate ester bond

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8
Q

Imidazothiazoles (group)

A 
eg levamisole
Affect NM coordination
Cholinergic agonist
Depolarisation, muscle contraction, spastic paralysis, rapid expulsion
GI helminths and lungworms
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9
Q

Levamisole

A 
An imidazothiazole
Affect NM coordination
Cholinergic agonist
Depolarisation, muscle contraction, spastic paralysis, rapid expulsion
GI helminths and lungworms
Water solube
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10
Q

Tetrahydropyrimides (group)

A 
eg pyrantel
Affect NM coordination
Cholinergic agonist
Depolarisation, muscle contraction, spastic paralysis, rapid expulsion
GI helminths and lungworms
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11
Q

Pyrantel

A 
A tetrahydropyrimide
Affect NM coordination
Cholinergic agonist
Depolarisation, muscle contraction, spastic paralysis, rapid expulsion
GI helminths and lungworms
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12
Q

Paraherquamide (PHQ)

A 
Affect NM coordination
Cholinergic antagonist
Oxindole alkaloids
Flaccid paralysis
1000fold more active at parasitic nACHR than mammalian
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13
Q

Piperazine

A 
Affect NM coordination
Muscle hyperpolarisation
GABA agonist
Opens ligand gated Cl- channels
Flaccid paralysis
Also inhibits succinate production and depletes ATP
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14
Q

Avermectins

A

-Macrocyclic lactones
Affect NM coordination
Potentiation of inhibitory transmitters
eg Ivermectin
Increase Cl- permeability -> hyperpolarisation and flaccid paralysis (of pharynx)
Glutamate gated Cl- channels - invertebrate specific

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15
Q

Milbemycins

A

Affect NM coordination

Potentiation of inhibitory transmitters

16
Q

Emodepside

A 
A cyclooctadepsipeptide
Affect MN coordination
Acto on latrophilin-like receptor/K channels 
Hyperpolarisation and flaccid paralysis
Can form a pore/ionophore
17
Q

Amino-acetonitrile derivatives

A

Affect NM coordination

Novel AChR subunits

18
Q

Triclabendazole TCBZ

A

BZ selective against flukes

19
Q

Triclabendazole TCBZ

A

BZ selective against flukes

20
Q

Diamphenithide

A

Against flukes

Increase malate concentration, so inhibit glucose metabolism

21
Q

Diamphenithide

A

Against flukes

Increase malate concentration, so inhibit glucose metabolism

22
Q

Cysteine proteinases

A

From plants - resistant to acid digestion
Attack cuticle and reduce egg production
Unlikely to become resistant
Cysteine residue hydrolyses peptide bonds in helminth proteins
Must be protected from oxidation for activity

23
Q

Cysteine proteinases

A

From plants - resistant to acid digestion
Attack cuticle and reduce egg production
Unlikely to become resistant
Cysteine residue hydrolyses peptide bonds in helminth proteins
Must be protected from oxidation for activity

24
Q

Carbamates

A

Cholinesterase inhibitor

Carbamylate active site serine residue

25
Q

Carbamates

A

Cholinesterase inhibitor

Carbamylate active site serine residue

MODA drugs (5 decks)

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