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Antiparasitic drugs
antiparasitics
41
Veterinary Medicine
Professional
07/08/2020

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Term
What is Fipronil And what is it mechanism of action?
Definition

Synthetic insecticidal and acaricidal.

Phenylpyrazole family and acts as a gamma-aminobutyric acid (GABA) receptor agonist

Mech of action: binds to a site in the chloride channel of GABA receptors and inhibits GABA regulated chloride flux into nerve cells = hyperexcitability

Generally used as flea and tick prevention in dogs and cats, treats chewing lice

Term
GABA (gamma-aminobutyric acid)
Definition
A neurotransmitter that acts as a major inhibitor in the CNS and at neuromuscular junctions
Term
MOA of Isoxazolines
Definition
Inhibit c-aminobutyric acid (GABA) chloride channels and L-glutamate chloride channels

Romero et al. Vet Dermatol 2016; 27: 353–e88
Term
MOA of Fluralaner
Definition
Acts by antagonising the arthropod ligand-gated chloride channels
Fisara et al. Vet Dermatol 2015; 26: 417–e98
Term
Why doesn’t ivermectin work for trematodes and cestodes?
Definition
GABA is not involved in neurotransmission in these species.
Term
What is the MOA of Spinosad?
Definition

It’s activity occurs at the nicotinic acetylcholine receptor causing hyperexcitability, paralysis and death of insects

Used as a monthly flea treatment

do not use concurrently with ivermectin;

Term
Why does caution need to be taken when using spinosad in combination with high-dose ivermectin?
Definition

Spinal sad may act as a P-glycoprotein (think MDR1/ABCB1) inhibitor, that’s resulting in increased blood and CSF levels of ivermectin.

Your patient essentially turns into a Collie!

Term
What is the MOA of the neonicotinoids?
Definition

Act at the postsynaptic nicotinic acetylcholine receptor to produce hyperexcitability in insects.

Nitenpyram (Capstar) Has 100% efficacy on adult fleas within three hours but not effective after 48 hours.

Term
What species is doramectin used in?
Definition
This is an avermectin used to treat nematodes, lies and mites in pigs.
Term
What species can milbemycin be used in?
Definition
Milbemycin is an avermectin Used to target nematodes, microfilaria, sarcoptes, Notoedres, otodectes, demodex, Cheylitiella and intestinal parasites in dogs and cats.
Term
What can Moxidectin and treat and in which species?
Definition

Used to treat fleas and is also likely effective for lice, Otodectes, sarcoptes and Demodex in dogs, cats and ferrets.

Used in cattle to treat various nematodes, Hypoderma, mites, lice and horn flies.

Term
What is amitraz and what is it mechanism of action?
Definition

An anti-parasitic drug used topically to treat mites, including Demodex

Monoamine oxidase inhibitor, can act on alpha-2 and may cause sedation in animals animals

Term
What are the side effects and contra indications for amitraz?
Definition

Sedation, pruritus, PU/PD, bradycardia, hypertension, heart block, hypo thermia, hyperglycemia and rarely seizures

Do not use with other MAO’s like selegiline or alpha 2s, avoid in debilitated pets

Term
What is dichlorvos and what is it mechanism of action?
Definition

An anti-parasitic used to treat intestinal parasites

Anti-cholinesterase activity

Term
What are the side effects and contra indications associated with dichlorvos?
Definition

Overdose can cause organophosphate toxicity: salvation, diarrhea, difficulty breathing and muscle twitching

Do not use and animals with Heartworms, within two days of cholinesterase inhibiting drugs (* see below), can exacerbate the signs of respiratory disease

* Organophosphates: chlorpyrifos, dichlorvos, malathion, diazinon, phosmet, fenthion, chlorfenvinphos, and cythioate

*Carbamates: carbaryl and propoxur.

Term
what are the side effects and contra indications of diethylcarbanazine?
Definition

Vomiting, pulmonary reactions if microfilaria positive (should not be given to heartworm positive dogs)

Term

What is Doramectin and what is its mechanism of action?

Definition

An anti-parasitic drug approved for use in cattle to treat nematodes and arthropods

Macrocyclic lactone that is neurotoxic and potentiates glutamate gated chloride channels in parasites

Term
What are the contra indications and potential side effects of Doramectin?
Definition

Causes neurotoxicity at high doses, especially in MDR1 breeds, can cause tissue reactions in cattle from dead larvae

If using off label and small animals, check for microfilaremia

Term
What is fenbendazole and what is it mechanism of action?
Definition

A benzimidazole anti-parasitic drug that treats helminth intestinal parasites and lungworm

inhibits microtubules and blocks glucose uptake

No contraindications, may cause vomiting or diarrhea

Term
What is ivermectin used to treat and what is its mechanism of action?
Definition

Anti-parasitic macrocyclic lactone that is neurotoxic and potentiates glutamate and GABA gated chloride channels (present in invertebrate nerves and muscle cells) Leading to hyper polarization = paralysis and death

Treats many parasites in many species including heartworm and small animals and demodex/scabies

May have some anti-inflammatory properties in dogs

Term
What are the contraindications and potential side effects of ivermectin?
Definition

Do not use an animals <6 week old, caution with high doses in any breed but especially in MDR1 (no p glycoprotein) animals leads to neurotoxicity (ataxia, tremor, mydriasis, lethargy, blindness, hypersalivation) and even death

Avoid in animals with lots of microfilaria

Term
What is picrotoxin?
Definition
A GABA antagonist that can be considered in cases of ivermectin toxicity
Term
What is levamisole and what is its mechanism of action?
Definition

Imidazothiazole antiparasitic That is used to treat various worms in various animals, microfilaricidal in dogs

Causes neuromuscular toxicity in parasites and may also boost the host immune system(?)

Term
What are the contraindications and potential side effects of levamisole?
Definition

Can cause cholinergic toxicity and vomiting; Do you not use with pyrantel as they have overlapping toxicities

Avoid and animals with high microfilaria burden

Term
What is Lufenuron and what is it mechanism of action?
Definition

A benzolurea insecticide That inhibits kite and synthesis and prevents flea eggs from hatching (Insect growth inhibitor)

Used to prevent flea infestation’s and is generally combined with other meds like milbemycin

Term
What is mebendazole and what is its mechanism of action?
Definition

A benzimidazole anti-parasitic that inhibits microtubules and blocks glucose uptake (similar to fenbendaxole)

Treats intestinal parasites

associated with occasional V/D

Term
What is a milbemycin oxime and what is its mechanism of action?
Definition

Macrocyclic lactone antiparasitic that is neurotoxic to parasites by potentiation of glutamate gated chloride channels

Used as a heartworm preventative, miticide, microfilaricidal and can treat demodex/scabies

Term
What are the contra indications and potential side effects of milbemycin oxime?
Definition

Can cause neurotoxicity at high doses

Caution in ivermectin sensitive breeds, do not use with drugs and increase penetration a cross the blood brain barrier

Term
What is selamectin and what is it mechanism of action?
Definition

A semi synthetic avermectin/macrocyclic lactone used for heartworm prevention, fleas, mites, text, intestinal parasites, ear mites and scabies

Neurotoxic through potentiation of glutamate gated chloride channels

Term
What are the contra indications and potential side effects of selamectin?
Definition

Do not use in puppies <6 weeks old

Do not use in kittens <8 weeks old

Can cause hair loss at the site of application, rarely nausea, lethargy, salivation, tachypnea and muscle tremors

Check heartworm status before administration

Term
What is thiobendazole and in what animals is it used in?
Definition

Benzimidazole Antiparasitic drug that inhibits microtubules and blocks glucose uptake

Used in horse and ruminant intestinal parasite infections

Side effects are uncommon

Term
What is metronidazole and what is it generally used to treat?
Definition

A nitroimidizole antiparasitic and Antiprotozoal Used to treat diarrhea/intestinal parasites/anaerobes and protozoa

Disrupts DNA in the parasitic organism the nitrogen free radicals

Can cause neurological effects, caution with pregnancy

Toxicity may be worse and cats

Term
What is pyrethrin/permethrin and what is it mechanism of action?
Definition

Pyrethroid insecticide used to kill and repel fleas and ticks as well as mosquitoes biting flies and lice

Finds to sodium channels leading to hyperexcitability and death

Term
What are the contraindications and potential side effects of pyrethrin/permethrin?
Definition

Do not use in cats! Do not use in dogs <7 weeks

can cause skin irritation V/D; Lethargy, seizures/neurotoxicity in cats

Term
What is Moxidectin and what is its mechanism of action?
Definition

Milbemycin a antiparasitic that potentiates glutimate gated chloride channels, hyper polarizing nerve cells

Used to treat intestinal parasites in horses and cattle, heartworm prevention

Term
What are the potential side effects in contra indications of moxidectin?
Definition

Can be neurotoxic at high doses, caution with ivermectin sensitive breeds

avoid in dogs <8 weeks old

don’t use with drugs I could increase the penetration across the blood brain barrier (Ketoconazole, cyclosporine)

Term
What is metaflumizone a.k.a. promaris known for?
Definition
Associated with pemphigus drug reactions in dogs, no longer on the market
Term
What is chloropyrifos?
Definition

Organophosphates pesticide that inhibits acetylcholinesterase

Commonly used in agriculture

Can cause a cute toxicity to people/Animals at high doses

Term
What is phosmet?
Definition

Organophosphates pesticide that inhibits acetylcholinesterase

Used on apple trees to control aphids, suckers, fruit flies and mites

Can be used on pigs, cattle and dogs for fleas ticks and lice

Term
Why might an owner be using tea tree oil?
Definition

Some believe that it will repel fleas by soaking into the insect exoskeleton and suffocating them

Can cause burns and toxicity as well as drooling, vomiting and trouble breathing

DO NOT use

Term
What is limonene?
Definition

Derived from oil of citrus fruit peels, has limited insecticidal properties

Avoid due to adverse effects, especially in cats

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