AntiParasitic drugs Flashcards
5 characteristics of the ideal parasiticide?
• selective toxicity
• economical to purchase
& apply
(small vs. large animal)
- hits all stages of parasite development disrupting the entire life cycle
- safe for use in “at risk” animals
- does NOT induce resistance in the parasite** no such thing!
Food animal production
vs
small animal/equine medical care
• Economics of anti parasitic
- food animal production
- -> economic return on entire herd health
- pets & horses
= control of zoonotic disease & health of individual pet
4 categories of “at risk” patients (concerning anti-parasitics)?
- old
- young
- pregnant
- debilitated
Why is it difficult to prove the presence of parasite resistance in animals?
- Hard to separate out drug administration errors vs actual drug failure
- Can’t culture them
How does selective pressure result in emergence of resistant populations?
- allows resistance to emerge by killing all susceptible & allowing resistant forms to remain
What is refugia?
How does it ↓ the # of resistant organisms in a population?
Does refugia try to reduce resistant organisms to zero?
Refugia
- a portion of a population of parasites that survives or avoids exposure to an antiparasitic drug treatment
- subset population of population is NOT subjected to drug
- -> allows susceptible parasites to compete w/ resistant forms
- -> keeps resistant forms low
- -> slows resistance development w/ low worm burden present
5 methods to reduce development of parasite resistance to antiparasiticides?
• Refugia = good management practice
• Use only drugs known to be effective against
the target species of parasite
• Target only health threatening parasite
species; reduce population to safe level
• Drugs that work by different mechanisms
- if combine drug
• Rotate type of drugs used over time (equine)
EPA vs. FDA
• regulatory fxns?
• What drugs or compounds would fall under each?
How does this translate to availability as OTC products?
EPA
• controls pesticides
• available OTC
• applied topically
FDA
• regulates internal drugs
• Legend drugs
legend drugs
• what are they?
• who regulates them?
- given internally (PO or by injection)
- prescription only
- on or by order of vet
- must have valid VCPR
- FDA regulated
ectoparasiticides
-External antiparasitics
endoparasiticides
-Internal antiparasitics
endectocides
-Compounds that do both internal and external parasites
Term that describes drugs against any internal worm parasite
-anthelmintics
Term used to describe drug against roundworms
Vermicide VS Vermifuge?
-antinematodals
Vermicide
• Kills
Vermifuge
• paralyzes –> expulsion
Term used to describe drug against tapeworms
• what are the specific types?
-anticestodals
Cestocides
Taeniacides
Taeniafuge
Term used to describe drug against Flukes
-antitrematodals
2 groups of macrolides or macrocyclic lactones?
members of each of these groups?
1 - Avermectins • Ivermectin • Selamectin • Doramectin • Eprinomectin
2- Milbemycins
• Milbemycin oxime
• Moxidectin
Are avermectins & milbemycins lipophilic or hydrophilic type drugs?
How does this translate to the ability of the drug to reach many target sites?
- Lipophilic
Wide distribution
• GI mucosa
• Lungs
• Dermis
** able to target migrating larvae
what receptor do macrocyclic lactones work on?
• MOA?
How does this actually kill the parasite?
Bind to glutamate receptor sites on chloride channels
- -> open channel
- -> Cl- enters cells
- -> ↑ threshold
- -> pharyngeal muscle paralysis
- -> starve & can’t hold on
- -> flushed out
Why are macrolides NOT effective against cestodes & trematodes?
- Flukes & Tapes do NOT have glutamate receptors
= not susceptible
Mammalian receptor macrocyclic lactones combine with to produce toxicity?
- Why are these still safe drugs for most animals?
- Mammals don’t have PERIPHERAL glutamate receptors
• Cl- gated GABA receptors in CNS
- macrolides can activate - BBB protects most
What keeps Macrocyclic Lactones out of the brain?
- P-glycoprotein
P-glycoprotein
- Cell membrane pump
- -> transports selected drugs from INTRA to Extracellular
Where is P-gp found
- endothelial cells of BBB
- GI epithelial cells
- bile canaliculi
- renal PCT