*(also key note)what are the routes of dermal absorption, and which is most common?
Transcellular, Intercellular (most drugs are absorbed this way), Transfollicular, Sweat pores, Lateral diffusion
Mechanisms of insect resistance include
↓ penetration of the drug, ↑ activity of detoxifying enzymes (cross resistance between classes of drugs), ↓ sensitivity of the target site (changes in Na channels lead to diminished binding of pyrethroids)
Key note: Mechanism of action of ectoparasiticides: (3 things, some have subtypes)
(1) Ectoparasite nervous system: AChE-inhibitors, Na+ channel blockers, nAChR inhibitors, GABA and Cl- channel inhibitors (2) Ectoparasite repellents (3) Insect growth and development inhibitors
Mechanism of insect resistance include (3)
(1) Decreased penetration of the drug (2) Increased activity of detoxifying enzymes (the cause of cross resistance between classes of drugs) (3) Decreased sensitivity of the target site (changes in Na+ channels lead to diminished binding of pyrethroids)
Macrocyclic Lactones (also antinematodal with ectoparasite activity)
MOA of Avermectins?
Targets ~glutamate, GABA, and glycine gated ion channels (Good Going God, for making MyDumbRetard)<--as much as I don't like using that word, I will do whatever it takes to learn this shit
contraindications of avermectins?
NOT USED be used in collies, bobtails, shelties---> *toxicity in collies, bobtails, shelties (have the MDR1 mutation) because they target the GABA receptor (mydumbretarded1---> stupid collies, shelties and bobtails)
which drugs are in the oil pour-on preparations?
erpinomectin and moxidectin (primo milk on the skin and the moxi to go on any way it wants)
spectrum of activity of macrocyclic lactones?
broad (mac and his broad shoulders)
which drugs have no withdrawal for milk?
eprinomectin and moxidectin (the same ones as oil pour on...and primo milk, moxie to do what it wants with no concenquences)
which animal/breed is very susceptible to macrocyclic lactones?
Interacts with the Na+ channels---- Targets voltage gated Na channels in axonal membrane; GABA gated Cl channels; mitochondrial ATPase and nicotinic receptors (put salt on a python it will shrivel up like a gabbing nicotine addict)
how does resistance occur in the pyrethrins and pyrethroids?
Resistance --> mutations in Na channels = ↓ binding of the ectoparasiticide to the Na channel
what is the safety like for pyrethrins and pyrethroids, and why is it like that?
Minimal systemic absorption after dermal application --> NO food and milk withdrawal time (pythons arent going to be in your milk and meat)
admin? why benifit is related to it's PK and the admin?
topical/dermal-- Minimal dermal uptake - minimal withdrawal time
DO NOT use in cats --> grooming --> ingestion. Also Aquatic animals= highly sensitive. (pythons will eat cats and fishes easily)
fleas, lice, mites, and ticks (repellent effect on flies) (pythons will eat anything)
Allethrin and Phenothrin are used for what?
Used as a spot-in formulation against fleas and ticks in dogs (Dogs get ALL the PHEN)
Resmethrin and Permethrin... note about these?
Short withdrawal time (The Res is Permanant....unless we withdrawal it, which would give it a short time)
Fenvalerate...note about these?
used in ear tags for cattle (FEN for VAL to put earrings on cows)
Flumethrin and Cypermethrin...note about these?
Used as fly repellent spray in horses (horse flew pass the cypresses, repelled by the fire)
what is the drug in the isoxazoline exctoparasitisets?
fluralaner (FLURNER ERH MER SERKS)
MOA of fluralaner
Selective inhibition of arthropod GABA and Lglutamate- gated chloride channels--> Binding within the chloride channel lumen-->Similar effects as fipronil but different class of drugs (Fi like fluras-- flur same as fipronil MOA)
Oclacitinib is used for what? MOA?
new anti-itch drug--> Mechanism of action: inhibition of JAK-1 (Janus kinase-1)--> Inhibits activation of nerve cells and immune cells by cytokines (Janus lacktit)
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