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3. Clin Pharm > Antiparasitics > Flashcards

Antiparasitics Flashcards

1
Q

Narrow-spectrum antiparasitics; broad calsses

A
  1. cestocides
  2. anti-coccidials
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2
Q

types of cestocides

A
  • praziquantel
  • epsiprantel
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3
Q

types of anti-coccidials

A
  • sulfonamides
  • amprolium
  • monensin
  • lasalocid
  • decoquinate
  • toltrazuril/ponazuril
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4
Q

drugs with limited cestocide activity, but not their main purpose, and what they treat

A
  • fenbendazole - Taenia sp. (dogs)
  • albendazole - Moniezia sp. (cattle)
  • pyrantel - Anoplocephala sp. (horses)
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5
Q

Drugs with only cestocide activity and what animals they are for

A
  • praziquantel - dogs, cats, horses
  • epsiprantel - dogs, cats
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6
Q

Praziquantel
class

A
  • isoquinolone
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7
Q

what is praziquantel licensed for?

A
  • Dogs, cats
    > Taenia spp, Dipylidium sp, Echinococcus spp
  • Horses
    > Anoplocephala sp
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8
Q

Mechanism of action of praziquantel

A
  • binds to parasite integument > rapid vacuolization
  • Influx of Ca2+ > muscle contraction (in seconds)
  • impaired function of scolex > paralysis, dislodgement, death
  • vulnerable to host digestion > tapeworm fragments may not be seen in feces
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9
Q

praziquantel pharmacokinetics

A
  • active as single dose via oral or parenteral administration
  • widely distributed to all tissues via either route
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10
Q

Praziquantel adverse effects:

A
  • wide margin of safety (therapeutic index >5)
  • oral - vomiting, lethargy/anorexia, transient diarrhea in dogs
  • excessive salivation in cats
  • injection site pain (transient)
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11
Q

availability of praziquantel

A

Available singly (Droncit) and in combination formulations:
* Drontal, Milbemax, Profender, NexGard COMBO (cats),
* Quest Plus, Eqvalan Gold (horses)
* Drontal Plus, Dolpac, Interceptor Plus (dogs)

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12
Q

Epsiprantel class

A

benzazepine

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13
Q

epsiprantel is licensed for what?

A

dogs & cats – Taenia spp, Dipylidium sp

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14
Q

mechanism of action of epsiprantel

A
  • thought to be similar to praziquantel
    > affects Ca2+ homeostasis within parasite
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15
Q

epsiprantel pharmacokinetics/treatment

A
  • active as single dose via oral administration
  • practically insoluble in water – minimal absorption from gastrointestinal tract
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16
Q

epsiprantel adverse effects

A
  • very wide margin of safety (therapeutic index >36)
  • vomiting, anorexia, transient diarrhea = occasional
  • side effects less common than with praziquantel

Note: cheaper than praziquantel

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17
Q

epsirantel availability

A

Only available as Cestex

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18
Q

coccidia life-cycle

A

Day 1: ingestion of oocysts
- Multiplication of the parasite in the small intestine without clinical signs
Day 14: Coccidia enter large intestine
Day 18-19:
>diarrhea +/- blood
> heavy infestation
> during stress
Day 18-25:
Excretion of oocysts

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19
Q

anti-coccidia drugs: coccidiocides

A

-sulfonamides
- amprolium (also coccidiostat)
- toltrazuril

20
Q

anti-coccidia drugs: coccidiostats

A
  • amprolium (also coccidiocide)
  • monensin
  • lasalocid
  • decoquinate
21
Q

sulfonamides are licensed for what animals? stat or cide? treat at what frequency and for how long?

A

Licensed: cattle, sheep, poultry (dogs & cats)
* coccidiocide
- first effective anti-coccidial agents
- treat daily until after > subclinical

22
Q

mechanism of action of sulfonamides? synergy?

A
  • interfere with protozoal folate synthesis:
  • decreased production of nucleotides
    > decreased DNA synthesis
  • sulfonamide + trimethoprim = synergistic
23
Q

sulfonamides adverse effects

A
  • gastrointestinal upsets (vomiting, anorexia, diarrhea)
  • precipitation in renal tubules in dehydrated animals
  • polyarthritis, especially Dobermans after >1 week therapy
  • keratoconjunctivitis sicca (“dry eye”) in dogs
24
Q

efficacy of sulfonamides?

A
  • acquired drug resistance, especially in poultry
    *still an effective anti-coccidial in small animals and ruminants
  • no clinical evidence that one sulfonamide more/less toxic or efficacious than another
25
Q

Amprolium in licensed for what animals? cide or stat? administered how?

A

Licensed: cattle, poultry (sheep, dogs, cats)
* coccidiocide + coccidiostat
* administered orally - food, water, capsules

26
Q

mechanism of action of amprolium?

A

competitively inhibits thiamine uptake

27
Q

adverse effects of amprolium?

A
  • anorexia, depression
  • prolonged use can > development of thiamine deficiency > CNS dysfunction
  • clinical signs may be reversed by adding thiamine to diet
  • not recommended for use in puppies >12 days
28
Q

Ionophore antibiotics? origin?

A
  • monensin
  • lasalocid

> streptomyces products

29
Q

ionophore antibiotics are coccidiostats or cides? other effects?

A

Both: (a) coccidiostats (b) increase weight gain

30
Q

mechanism of action of ionophore antibiotics

A

Action:
- Facilitate transport of cations across cell membrane:
> intracellular accumulation of cations (e.g. Ca2+ )
* selectively affect Gram +ve organisms – rumen microflora shifts to Gram –ve organisms:
> influences production of volatile fatty acids
> increased feed efficiency + increased weight gain

31
Q

Ionophore antibiotics
Pharmacokinetics:

A
  • administered orally
  • absorbed: monogastrics > ruminants
32
Q

monensin toxicity

A
  • cattle, sheep (horses, dogs) – skeletal/cardiac muscle
  • dose errors in mixing with feed
  • accidental ingestion by susceptible species
  • accidental feedmill contamination of feed
  • regurgitated bolus - potentially lethal for dogs if chewed
33
Q

momensin license and admin

A

Licensed: cattle, sheep, goats, poultry
* coccidiostat
- administered daily in feed (premix) for at risk period

34
Q

monensin admin in cattle, and advantages of use

A
  • feed premix / controlled release bolus
  • promotes increased feed efficiency and weight gain
  • helps prevent :
    >bloat in beef cattle on pasture
    > subclinical ketosis in dairy cattle
  • promotes increased milk production efficiency
35
Q

lasalocid license and admin

A

Licensed: cattle, sheep, poultry
* coccidiostat
– administered daily in feed (premix) for at risk period
– incorporated into mineral block

36
Q

lasalocid admin and advantages in cattle

A
  • feed premix
  • promotes increased feed efficiency and increased weight gain
37
Q

Decoquinate license and admin

A

Licensed: cattle, sheep, poultry
* coccidiostat (quinolone)
* administered orally - in milk replacer, feed, mineral block

38
Q

action of decoquinate

A
  • inhibits cytochrome-mediated electron transport in parasite mitochondrion
39
Q

safery of decoquinate? when is it most effective?

A
  • practically insoluble in water – very safe
  • most effective in calves when fed continuously in feed
40
Q

effectiveness comparison between monensin, lasalocid, and decoquinate

A

Note: monensin, lasalocid and decoquinate at manufacturers’ recommended levels = equally effective coccidiostats

41
Q

Triazine derivatives

A
  • toltrazuril
  • ponazuril
42
Q

Triazine derivatives act how?

A
  • act on apicoplast - present in apicomplexan parasites (e.g. coccidia) – exact action unknown
  • coccidiocides – typically act on all intracellular stages
43
Q

Toltrazuril; when to use for strong immunity

A

treatment in prepatent period > strong immunity

44
Q

Toltrazuril is approved for treatment of:

A

(i) preclinical coccidiosis in neonatal pigs:
- single dose at 3-4 days of age
- 70-day meat withdrawal

(ii) preclinical coccidiosis in lambs:
- single dose ~1 week before onset of diarrhea
- 48-day meat withdrawal

(iii) preclinical coccidiosis in dairy and beef calves:
- single dose ~1 week before onset of diarrhea
- 63-day meat withdrawal

45
Q

Ponazuril; what is it? what is its use and admin strategy? how effective?

A
  • active metabolite of toltrazuril
  • “aid in reducing clinical severity of Equine Protozoal Myeloencephalitis due to Sarcocystis neurona”
  • daily for 28 days
  • “approximately 2 horses out of 3 will respond favourably to treatment”

3. Clin Pharm (11 decks)

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