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Flashcards in 1-4 Gibson Deck (22)
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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
2
Q

Thiabendazole

A

A benzimidazole
Act against cellular integrity
Inhibitors of tubulin polymerisation
Slow

3
Q

Fenbendazole

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

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

6
Q

Praziquantel

A
Act against cellular integrity
Tegument disruption and vacuolisation
Ca2+ permeabilisers - cause Ca influx 
Spastic paralysis
Slow
7
Q

Proteinases

A

Act against cellular integrity
Tegument disruption
Maybe Ca2+ permeabilisers
Slow

8
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

9
Q

Imidazothiazoles (group)

A
eg levamisole
Affect NM coordination
Cholinergic agonist
Depolarisation, muscle contraction, spastic paralysis, rapid expulsion
GI helminths and lungworms
10
Q

Levamisole

A
An imidazothiazole
Affect NM coordination
Cholinergic agonist
Depolarisation, muscle contraction, spastic paralysis, rapid expulsion
GI helminths and lungworms
Water solube
11
Q

Tetrahydropyrimides (group)

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

Pyrantel

A
A tetrahydropyrimide
Affect NM coordination
Cholinergic agonist
Depolarisation, muscle contraction, spastic paralysis, rapid expulsion
GI helminths and lungworms
13
Q

Paraherquamide (PHQ)

A
Affect NM coordination
Cholinergic antagonist
Oxindole alkaloids
Flaccid paralysis
1000fold more active at parasitic nACHR than mammalian
14
Q

Piperazine

A
Affect NM coordination
Muscle hyperpolarisation
GABA agonist
Opens ligand gated Cl- channels
Flaccid paralysis
Also inhibits succinate production and depletes ATP
15
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

16
Q

Milbemycins

A

Affect NM coordination

Potentiation of inhibitory transmitters

17
Q

Emodepside

A
A cyclooctadepsipeptide
Affect NM coordination
Act on latrophilin-like receptor/K channels 
Hyperpolarisation and flaccid paralysis
Can form a pore/ionophore
18
Q

Amino-acetonitrile derivatives

A

Affect NM coordination

Novel AChR subunits

19
Q

Triclabendazole TCBZ

A

BZ selective against flukes

20
Q

Diamphenithide

A

Against flukes

Increase malate concentration, so inhibit glucose metabolism

21
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

22
Q

Carbamates

A

Cholinesterase inhibitor

Carbamylate active site serine residue