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Pharmacology 2 > Anthelmintics > Flashcards

Anthelmintics Flashcards

1
Q

What is the MOA of Benzimidazoles?

A

Binds to parasite B-tubulin subunit (microtubules)

  • disrupts cell everything
  • binds to mammalian cell but dissolved very quickly
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2
Q

What is the PK of benzimidazoles?

A 
poor water solubility (pastes, suspensions, granules)
poor oral F
Distribution is high
hepatic metabolism (CYP enzymes)
- first pass effect
Other distribution: lung and intestines
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3
Q

What are benzimidazoles used for?

A

GI and lung nematodes

some cestodes and some trematodes

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4
Q

What is the most common benzimidazole?

A

Fenbendazole (safeguard, pancur)

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5
Q

What is Fenbendazole used for on label?

A

horses (suspensions, pastes, granules)
cattle (suspensiosn, feed)
swine/chicken (pancur, aquasol in water)
dogs (pancur, granules)

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6
Q

What is fenbendazole used to treat?

A

GI and lung nematodes

- strongyles, ascarides, whipworms, hookworms, pinworms

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7
Q

What is fenbendazole used for off label?

A

small ruminants, turkeys
cats (nematode, giardia, lung worms)
birds, exotics

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8
Q

What is Febental?

A

fenbendazole prodrug
“drontal plus” (fenbental+pyrantel+praziquantel)
- used for dogs

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9
Q

What is another benzimidazole used for cattle? what is it used to treat?

A

Albendazole (Valbazen)

  • adult flukes (not great choice)
  • tapeworms
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10
Q

What other benzimidazole can be used for adult and juv flukes and lung worm?

A

Triclabendazole

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11
Q

What is an emergency drug release?

A

a way for vets to access drugs approved in other areas of the world
- need documented evidence and safety
NO FOR:
- biologics, investigation drug, comparable drug here

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12
Q

What is the MOA of macrocyclic lactones (ML)?

A

opens glutamate gated Cl channels (opposite as isoxaolines)
- Cl entry into cell (hyperpolarization)
= flaccid paralysis of worm

may bind to GABA receptors at high concentrations

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13
Q

What are MLs used for?

A

nematodes and arthropods
Exception: demodex and some adult filaria(higher doses)
- heart worm preventative (low dose ivermec)
minimal against cest and trem

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14
Q

What is the PK of MLs?

A 
oral and transcuticular absorption from host
(oral, topical, injectable)
lipophilic with high VD
- hepatic metabolism
LONG withdrawal (most not for dairy)
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15
Q

What are some adverse effects of MLs?

A

toxicity with GABA stim in the CNS = neurosigns
-Tx: IV lipid emulsion
ABCB1 mutant dogs (white feed dont treat)
- decrease pgp increase distribution to brain

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16
Q

What are some Avomectin (ML) drugs? and what are they used for?

A

Ivermectin (ivomec)

  • oral drench (sheep)
  • oral paste (horses)
  • pour on cattle)
  • injectable (cattle, sheep, swine)
  • oral premix (swine)
  • tablets (dogs)

Eprinomectin

Eprinex - pour on
- license for dairy cows (no milk withholding)

Long-range (extended release SC)

  • rapid and slow absorption
  • 4-5m activity
  • 4m meat withdrawal
  • dont use for dairy

Doramectin (dectomax)

  • injectable (cattle/swine)
  • pour on (cattle)
  • similar to ivermectin

Salamectin (revolution)

  • monthly topical for dogs/cats
  • fleats, mites (not demodex), nematodes, HW prevention
  • safer than iver mec for ABCB1 mutants (still dont use)
  • fish
17
Q

What is a Milbemycin (ML) drug used?

A

Moxidectin
- cydectin pour on (beef and dairy), similar to
Ivermec/doramec
- Quest/Quest plus (oral gel horses), moxidectin +/- praziquantel, tapeworms + nematodes
- advantage multi (monthly topical, dogs, cats, ferrets), moxidectin +imidacloprid, HW prevention, fleas, ear mites, GI nematodes
- ProHeart (sustained release for dogs), HW prevention (6 months)

18
Q

What moxidectin monthly tablets do they have on the market? What do they all protect from, what unique parasite do each add?

A

all for HW prevention, hookworm, roundworm

milbemax (cats) - milbemycin + praziquantel, addition of tapeworm

interceptor tablets (dogs/cats) - milbemycin, addition of whipworm

Sentinel tablets (dogs) - milbemycin and lufenuron, addition of whipworm and fleas

Trifexis tablets (dogs) - milbemycin and spinosad, addition of whipworm and fleas

19
Q

What species is ML resistance most affecting/emerging? What parasites is it reported in?

A

SHEEP
emerging in cattle and horses
widely reported in cyathostomes and large strongyles

20
Q

What is the mechanism of ML resistance?

A

induction of parasite efflux pumps (p-gp)

changes in Glu gated Cl channels

21
Q

How do you test for resistance?

A

pre and post treatment FEC (if below 95% reduction = resistance)

22
Q

What are the ecological impacts of ML resistance?

A

avermectins persist in feces and kill feces degrading insects
evaluated part of drug approval (excretion in non-toxic form helps.

23
Q

What are some topical tips for ML?

A

skin not hair
watch for mud/feces
not low temps
flammable (branding)

24
Q

What is the very old dewormer called thats used for everything but ruminants?

A

piperazine

- over the counter

25
Q

What is the MOA, use and AE of piperazine?

A

MOA: anticholinergic activity in parasite muscular junction (hyperpolarization) and flaccid paralysis
USE: large round worms (ascarids)
AE: GI upset or neuro signs

26
Q

What are the drugs in the Pyrimidine class?

A

Pyrantel
Praziquantel

Emodepsite
nitroscanate (lopatol - tablets)
Melarsomine (immiticide)

27
Q

What is the MOA, use of pyrantel?

A

MOA: depolarizes NMJ, nicotinic receptor agonist, leads to spastic paralysis
USE: nematodes, some cestodes at higher doses

28
Q

What are the different labels for Pamoate salt (paste suspension)

A

Drontal (cats)/Drontal Plus (dogs)
- praziquantel +/- febantel

Dolpac
- pyrantel

Heart guard Plus
- pyrantel + Ivermec (invermec lasts longer and is lower dose for HW preven)

exodus (equine) - oral paste

Strongid (equine) -pate or suspension

  • large strongyles
  • EL in small animals
29
Q

What is the label for Tartrate salt (solution)?

A

Pro-Banminth Premix (swine)

- ascaris suum

30
Q

What is the MOA, use, and AE of Praziquantel?

A

MOA: increase in ICF Ca = spastic paralysis
Use: anti-cestode drugs for cat, dog, horses, cattle
- in combo with nematode or alone
AE: CYP drug interaction (inhibit Pgyp transporter)
grapefruit juice increses F

31
Q

What is the MOA, use and AE of Emodepside?

A

MOA: intracellular signal transduction = flaccid paralysis
Use: round, hook and tape
- safe for pregnany queens
AE: mild GI, watch for pgyp interaction

32
Q

What is the use and AE of Nitroscanate (lapotol)?

A

dogs for round, hook and tape
increased absorption with food
- safe in young puppies
AE: vomiting

33
Q

What is the use of Melarsomine?

A

dogs only
killed dirofilaria immitis adult
deep IM injection (epaxial muscles only)
NASTY DRUG

Pharmacology 2 (14 decks)

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