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Principles of Science BVetMed 3 > Anthelmintics > Flashcards

Anthelmintics Flashcards

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1
Q

Define anthemintic

A

Chemotherapeutic agent to control helminth infections

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2
Q

Define chemotherapy

A

Use of drugs to injure an invading organism without injury to the host (i.e. selective toxicity)

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3
Q

2 spectrums of activity

A

Broad or narrow

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4
Q

Chemical groups of anthelmintics - examples 3

A

Benzimidazoles (BZ) - fenbendazole
Imidaothiazoles (LM) - levamisole
Macrocyclic lactones (ML) - ivermectin

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5
Q

Classification of anthelmintics by target parasite

A

Nematodicide (roundworms)
Cestodicide (tapeworms)
Trematodicide/flukicide (trematodes/flukes)

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6
Q

How can anthelmintics be delivered? 3

A

Orally (drench, tablet, oral bolus)
Parentally (injection)
Topically (pour-on)

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7
Q

Overall classifications of anthelmintics -4

A
  • spectrum of activity
  • chemical group/mode of action
  • target parasites
  • method of delivery/formulation
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8
Q

Another name for group 1 benzimidazoles

A

White drenches

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9
Q

Another name for group 2 LM/imidazothiazoles

A

Yellow drenches

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10
Q

Another name for group 3 ML

A

Clear drenches

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11
Q

What are the 2 new groups of broad-spectrum anthelmintic

A 
4 = AD = amino acetonitrile derivatives
5 = SI = spiroindoles
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12
Q

What are some examples of narrow spectrum anthelmintics

A

Fluke drenches, tapewormers, heartworms

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13
Q

Examples of benzimidazoles

A

Albendazole, Fenbendazole, Flubendazole, Mebendazole, Oxfendazole, Triclabendazole

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14
Q

Mode of action - BZ

A

Bind to parasite B-tubulin leading to inhibition of glucose uptake, glycogen depletion and death

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15
Q

Administration - BZ

A

Low water solubility - oral products only. Resuspend prior to administration

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16
Q

What determines BZ potency?

A

Duration of exposure (BZs kill worms very quickly)

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17
Q

3 ways to increase BZ potency?

A
  1. ) multiple low doses more potent than one single dose
  2. ) potency greater in ruminant/horse than dog (rumen/caecum acts as a reservoir)
  3. ) potency greater in ruminants if starved 12-24hr (slows rate of passage of ingesta)
18
Q

Another name for Imidazothiazoles/yellow drenches

A

Tetrahydropyrimidines

19
Q

Examples of Imidazothiazoles and Tetrahydropyrimidines

A

Imidazothiazoles - levamisole

Tetrahydropyrimidines - pyrantel

20
Q

How do yellow drenches work?

A

Cholinergic agonists - cause a rapid and reversible spastic paralysis

21
Q

Administration - yellow drenches

A

Only available as oral drenches.

22
Q

What does levamisole act on?

A

Nematodes - especially adult gutworms, less so mucosal larvae and hypobiotic larvae. Also lungworms. NOT trematodes, cestodes, arthropods or protozoa.

23
Q

Administration - levamisole? 3 How does this affect its pharmacokinetics?

A

Injection - rapid and high peak in plasma concentration, shorter duration of action
Oral - middle peak/duration
Pour-on longer half life, lowest plasma concentration

24
Q

Examples of ML calsses - 2

A

Avermectins and Milbemycins

25
Q

Mechanism of action - ML

A

Open invertebrate specific glutamate-chloride channels in post-synaptic membrane leading to flaccid paralysis

26
Q

Spectrum of ML

A

Broad spectrum - targets all nematode gutworm and lungworm stages. Variable effects on arthropods. Not trematodes, cestodes or protozoa.

27
Q

Pharmacokinetics of MLs

A

Oral/injection (highest peak) or pour-on.
Persistent effect provides period of protection against re-infection. Presistent activity used to design prophylactic worm control strategies.

28
Q

Define metaphylaxis

A

Protection of animals grazing contaminated pasture

29
Q

Define prophylaxis

A

preventing pasture infection (i.e. prevents autoinfection peak)

30
Q

Name the roundwormers - 9

A

BROAD SPECTRUM:

  • Benzimidazoles
  • ML
  • Imidazothiazoles/tetrahydropyrimidines
  • Aminoacetile derivatives (new)
  • spiroindoles (new)

NARROW SPECTRUM:

  • desipeptides
  • salicylanilides
  • piperazines
  • phenylisothiocyanates
31
Q

What are monepantel and derquantel?

A

Examples of new broad spectrum anthelmintics

32
Q

Name the roundwormers

A

BROAD SPECTRUM:

  • benzimidazoles
  • Tetrahydropyrimidines

NARROW SPECTRUM:

  • isoquinolines
  • phenylisothiocyanates
33
Q

How does praziquantel (PZQ) work?

A

Tegument destruction (especially at the proliferation zone) –> increased membrane permeability for calcium ions, loss of intracellular calcium –> spastic paralysis and malabsorption. Ultimately the tapeworm is digested.

34
Q

Flukicide - spectrum of action

A

Narrow spectrum target fluke and blood feeding nematodes. Some activity against blood sucking nematodes.

35
Q

How do flukicides (salicylanilides and substituted phenols) work?

A

uncouple oxidative phosphorylation decreasing the availability of high energy phosphate compounds

36
Q

Phamacokinetics - salicylanilides

A

Binds to plasma proteins –> prolonged plasma half life, not used in milking cattle or sheep.

37
Q

What is the flukicide of choice for treating acute fasciolosis?

A

Triclabendazole (for treating flukes down to 2d old)

38
Q

Define RDR

A

Recommended Daily Dose

39
Q

What is fenbendazole (FBZ) active against?

A

(LS and SS) mucosal larvae

40
Q

Define excipient

A

Other ingredients (as opposed to the acitve compound) that alter physical attributes and/or biological properties (e.g help transport drug through skin and into circulation)

41
Q

3 main ways althelmintics can be delivered

A

By mouth (oral) - drench, paste, tablet, in feed, bolus
PN (injection) s/c, i/m
Topical (trans-dermal) - pour on

Principles of Science BVetMed 3 (110 decks)

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