Test 3: 41 anthelminitics part 1 Flashcards

1
Q

what two systems do anti parasite drugs effect

A

neurotransmission

cellular integrity

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2
Q

Macrocyclic lactones have Broad-spectrum activity against most —

A

nematodes (including immature forms - hypobiotic larvae) and arthropods

not effective against adult heartworm, but works for immature worms

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3
Q

macrocyclic lactones are ineffective against —

A

cestodes and trematodes and adult heartworm (D. immitis)

broad spectrum anti parasite for nematodes and arthropods

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4
Q

dosing of macrocyclic lactones

A

monthly - persistent efficacy

well absorbed into GI, lungs and skin regardless of route of administration

effective against nematodes, arthropods and immature heartworm

not effective against cestodes and trematodes and adult heartworm

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5
Q

how do macrocyclic lactones work

A

Bind with high affinity to a glutamate-gated chloride channel

MLs bind to glutamate receptors that trigger chloride influx

Prevents initiation or propagation of normal action potentials

The net effect is paralysis and death of the target parasite!!

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6
Q

side effects of macrocyclic lactones

A

toxic: collies with MDR1 (ABCB1) gene: vomting, lethargy, tachycardia

excreted as active drug- may have environmental effect- toxic to aquatic animals

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7
Q

what are some macrocyclic lactones

A

ivermectin (heart worm)
moxidectin (proheart)
milbemyxin oxime (interceptor)
Doramectin
selamectin (revolution)
eprinomectin

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8
Q

ivermectin

A

macrocyclic lactone

Safe in Collies and in all breeds, even dogs with mutant MDR1

used in Cattle, sheep, swine, horses, bison, reindeer, dogs, and cats

withdrawal 35 d dairy, 14 d meat

heartgard

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9
Q

moxidectin

A

macrocyclic lactone

Cattle, sheep, horses, dogs, cats, and ferrets(heartworm)

Moxidectin pour-on is approved for use in beef and dairy cattle

100% efficacy in preventing Ancylostoma caninum in dams and pups when given on pregnancy day 55

Wider margin of safety than IVM for Collies (30X)

proheart

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10
Q

milbemyxin oxime

A
  • Dogs and cats
  • Considered safe for pregnant and nursing animals
  • It is nontoxic to rough-coated Collies at up to 20X the recommended dose

macrocylic lactone- interceptor

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11
Q

doramectin

A

macrocyclic lactone
Cattle and swine
It is NOT RECOMMENDED for use in dogs and cats
Withdrawal interval of 35d (milk) and 14d (meat) (same as ivermectin)

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12
Q

selamectin

A

Dogs and cat
safe in MDR1 mutant
dogs when given at 40 mg/kg topically
oral doses of 15 mg/kg, MDR1 mutant dogs have only mild signs of neurologic toxicity

revolution

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13
Q

eprinomectin

A

Approved in a topical and injectable formulation for use in cattle only
* Combination product of EPM and praziquantel is approved for cats
* Extralabel: sheep, donkeys, rabbits

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14
Q

two types of tetrahydropyrimidine anti-parasite

A

pyrantel (dog, horse, swine)

morantel tartrate (ruminants)

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15
Q

Tetrahydropyrimidine anti parasites are broad spectrum for —

A

adult GI nematodes

except for whipworms (trichuris)

pyrantel
morantel tartrate

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16
Q

how do tetrahydropyrimidines work

A
  • Act as nicotinic agonists that disturb the neuromuscular junction
  • Nicotinic acetylcholine receptors are essential for neurofunction
  • Depolarization of the muscle membrane, contraction and subsequent paralysis

antiparasite: pyrantel, morantel tartrate

17
Q

pyrantel

A

Horses, swine, and dogs

It is NOT APPROVED for use in ruminants but has been recommended/considered effective for GI nematodes

Resistance to pyrantel is common in equine parasites

simparica trio
heartgard

18
Q

— can prevent the apperance of “ milk spots” in the liver from the migration of Ascaris suum

A

pyrantel tartrate

horse and swine
white powder, soluble in water

19
Q

pyrantel tartrate vs pyrantel pamoate

A

pyrantel tartrate: white powder, soluble in water, horses and swine, prevent milk spots from Ascaris suum

Pyrantel pamoate: yellow, insoluble in water, horses and dogs, safe in pups and pregnant animals

20
Q

benzimidazoles are effective against

A

nematodes, most cestodes, and some trematodes in horses and ruminants

Can not treat trematodes in dogs and cats

poorly soluble in water- give before food, slow acting compound

21
Q

how do benzimidazole work

A

Disrupt parasite cell division
* Bind to parasite β-tubulin molecules and inhibit formation of microtubules
* Microtubules provide structure and shape to eukaryotic cells
* Higher affinity for nematode tubulin than mammal tubulin

Blocks mitochondrial function
* Can inhibit fumarate reductase
* Deprive the parasite of energy and result in death

treat nematodes, most cestodes and some trematodes in horses and ruminants

may need to redose at BID, poorly absorded and slow acting

give on empty stomach, more effective at lower pH

22
Q

side effects of benximidazole

A

teratogenicity- congenital malformation, embryo lethal effects

Withholding period after anthelmintic treatment for food-producing animals
* 8-14 days before slaughtering for meat * 3-5 days before milking for human consumption

albendazole, febendazole

23
Q

albendazole

A

benzimidazole antiparasite

Cattle, sheep and goats
* GI nematodes
* Lung nematodes, including larval forms
* Cestodes
* Lung and liver trematodes

NOT APPROVED for use in dogs and cats

24
Q

febendazole

A

Ruminants, horses, swine, dogs, and zoo animals
* Considered safe to use in pregnancy
* Have been used off label (US) to treat giardiasis

treat Gi nematodes, lung nematodes, cestodes

does not treat trematodes like albendazole

panacur, safeguard

25
Q

OXIBENDAZOLE

A

benzimidazole antiparasite

horses

Apparently effective against small strongyles that are resistant to BZs

26
Q

isoquinolones are effective for

A

cestodes and tramatodes of genus schistomsoma

cattle and people

should not be used in puppies or kittens younger than 7 weeks

27
Q

what are some isoquinolones

A

praziquantel and epsirprantel

safe and effective against cestode and trematodes of schistosoma

28
Q

how does isoquinolone work

A

exact mechanism unknown

Attack the parasite neuromuscular junction and the tegument

cause contraction and paralysis of the parasite

Vacuolization and destruction of the protective tegument

attack cestodes and Schistosoma trematodes

29
Q

praziquantel

A

should not be used in puppies and kittens younger than 7 weeks
of age

kills adult and larval cestodes and Schistosoma sp. trematodes

FDA-approved for dogs and cats

  • Available for horses in combination with MLs only

isoquinolones: praziquantel, epsiprantel

30
Q

epsiprantel

A

Cestodes
* Dogs and cats - Cestex (Zoetis)

31
Q

Arsenicals treat —

A

adult heartworms ( Dirofilaria immitis)

NOT SAFE for cats - toxicity problems
Dogs with moderate risk of thromboembolism: AHS treatment protocol

melasormine

32
Q

how to treat heartworm in dogs and cats

A

cats no treatment

dogs: arsenical antiparasities such as melasormine

kills adult heartworm- D. immitis

33
Q

clorsulon

A

Very effective in cattle against all stages of Fasciola hepatica (liver fluke/trematodes)

NOT EFFECTIVE against Paramphistomum sp. (rumen fluke)

Limitation: withdrawal has not been established - avoid lactating cattle