26 – Ecto-parasiticides Flashcards
Many ectoparastiticide formulations
- ear tags
- collars
- immersion baths
- topical dusts
- shampoos
- premise application (fleas!)
- pour-on
What are the different acetylcholinesterase inhibitors?
- Organophosphates
- Carbamates
Acetylcholinesterase inhibitors: organophosphates
- mechanism: IRREVERSIBLE binding to AChE
- HIGHLY toxic to mammals
- Environmental concerns
What are the different compounds and formulations of acetylcholinesterase inhibitors: organophosphates?
- Diazinon ear tags (control horn flies and face flies in cattle)
- Many other compounds
Acetylcholinesterase inhibitors: carbamates
- Mechanism: competitive inhibitor of AChE (reversible)
- Less toxic than organophosphates, still toxic though
o Given small amount for a large animal
What are the different compounds and formulations of acetylcholinesterase inhibitors: carbamates?
- Carbaryl dusting powder for control of mites, fleas, lice, ticks, and flies in various food animal species
(Amitraz)
- Inhibits monamine oxidase
- Toxicity: activation of alpha2 receptors
- Prevention of ticks
- NOT in Canada
Pyrethrins (basic from chrysanthemum flower)/Pyrethroids (synthetically modified compounds)
- ‘natural’
- Highly LIPIDLY soluble
- Topical formulations stay in stratum corneum
o NO systemic absorption
o Considered pesticides - *TOXIC IN CATS
Examples of drugs that are pyrethins/pyrethroids
- Permethrin (ex. vetolice)
- Cypermethrin
- Cyfluthrin (CyLence)
What is the mechanism of pyrethrins/pyrethroids?
- Most act on Na+ channels (stuck in OPEN state) or other NT functions
What are the formulations of pyrethrins/pyrethroids?
- Shampoos
- Sprays
- Dips
- Dusts
- Ear-tags
What are pyrethrins/pyrethroids active against?
- Fleas
- Ticks
- Flies: probably the best fly control
- Lice
- (Mites: not as good)
- *ENVIRONMENTAL CONTAMINATION
Pyrethins/pyrethroids is toxic in cats
- Due to grooming of topical products?
- Poor hepatic glucuronidation?
- *especially in environmental decontamination
o ALSO TOXIC FOR FISH! - *persist in environment for a long time
Neonicotinoids
- Like nicotine, but more stable
- Non-ionized at physiological pH (so crosses BBB)
- Minimal environmental impact (but it is what is killing bees, due to using it on plants to kill bugs)
What is the mechanism of neonicotinoids?
- Activates INSECT nicotinic receptors
- No effect on vertebrate nicotinic or muscarinic receptors
- First depolarizes neuron (Na channels open), but eventually STOPS neural transmission