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Ectoparasiticides
N/A
71
Veterinary Medicine
Professional
10/26/2011

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Term
All of the following function as anti-cholinesterase agents and inhibiting the breakdown of acetylcholine EXCEPT:

a. Cabaryl
b. Dichlorvos
C. Cryomazine
d. Diazinon
e. Tetrachlorvinphos
Definition
C. Cryomazine

Cryomazine is an insect growth regulator (along with methoprene and pyriproxyfen)
Term
Which of the following classes of drugs functions by forming a covalent bond with acetylcholinesterase?

a. Carbamates
b. Neonicotinicides
c. Botanical ectoparasiticides
d. Macrocyclic lactones
e. Organophosphates
Definition
e. Organophosphates

Carbamates also inhibit acetylcholinesterase, but form a reversible, non-covalent bond.
Term
All of the following are effective when administered orally EXCEPT:

a. Diflubenzuron
b. Spinosad
c. Nitenpyram
d. Amitraz
e. Lufenuron
Definition
d. Amitraz--often used as a topical dip for the treatment of demodicosis and ticks.
Term
Which of the following is NOT a thiol organophosphate?

a. Coumaphos
b. Diazinon
c. Dichlorvos
d. Phosmet
e. Pirmiphos
Definition
c. Dichlorvos

Dichlorvos and Tetrachlorvinphos are both oxy compounds.

Note that for thiol organophosphates to work, they must first be metabolized to -oxy.
Term
_____________, trade name ____________, and _____________ are the carbamates discussed in class.
Definition
Cabaryl (trade name Sevin)

Propoxur
Term
Which of the following function by mimicking insect juvenile hormone, preventing molting and resulting in the persistence of larval stages of insects?

a. Cryomazine
b. Methoprene
c. Pyriproxyfen
d. A and B
e. A, B, and C
Definition
e. A, B, and C

All three of these are insect growth regulators.
Term
Diflubenzuron and Lufenuron are classified as ______________________________, and function how?
Definition
Diflubenzuron and lufenuron are classified as insect development inhibitors and function by inhibiting chitin synthesis in larvae and eggs.
Term
Which of the following functions by inhibiting electron transport, causing decreased cell respiration and oxidation of lactate/glutamate?

a. Pyriproxyfen
b. Rotenone
c. Permethrin
d. Ivermectin
e. Nitenpyram
Definition
b. Rotenone

Rotenone is a botanical ectoparasiticide that causes knockdown of arthropods by inhibition of electron transport.
Term
All of the following are in the classification of "pyrethroids" except:

a. Spinosad
b. Fenvalerate
c. Permethrin
d. Deltamethrin
e. Piperonyl butoxide
Definition
a. Spinosad
Term
T/F: Imidacloprid, Nitenpyram, Dinotefuran, and Spinosad are all classified as "neonicotinocides."
Definition
False: Imidacloprid, Nitenpyram, and Dinotefuran are all classified as neonicotinocides and function as nicotinic receptor agonists.

Spinosad is a nicotinic receptor agonist, but also activates GluCl channels, which hyperpolarizes.
Term
Anti-cholinesterase agents that inhibit the breakdown of Ach and cause resulting accumulation of Ach by covalent binding to serine.
Definition
Organophosphates

Thiol: Diazinon, Coumaphos, Phosmet, Pirmiphos

Oxy: Dichlorvos, Tetrachlorvinphos
Term
Inhibit acetylcholinesterase by forming reversible, non-covalent bonds.
Definition
Carbamates: Cabaryl, Propoxur
Term
Mimic insect juvenile hormone to prevent molting, resulting in the persistence of larval stages of insects.
Definition
Insect Growth Regulators: Cryomazine, Methoprene, Pyriproxyfen
Term
Inhibit chitin synthesis in the larvae and egg tooth. Only effective against immature stages of arthropods. Not adulticidal.
Definition
Insect Development Inhibitors: Diflubenzuron, Lufenuron
Term
Alkaloid. Causes knockdown by inhibition of electron transport, causing decreased cell respiration and oxidation of lactate/glutamate.
Definition
Rotenone
Term
Alkaloids of pyrethrum flowers that cause knockdown of arthropods by persistent opening of Na channels in arthropods.
Definition
Pyrethroids

Fenvalerate, permethrin, Piperonyl butoxide (MGK 264), deltamethrin
Term
Derived from antibiotics. Interrups feeding and laying of eggs by opening GluCl channels and causing flaccid paralysis.
Definition
Macrocyclic lactones (ivermectin)
Term
Activates octopamine receptors.
Definition
Amitraz
Term
Nicotinic receptor agonists that are highly selective for insect receptors Da1, Da2, Da3.
Definition
Neonicotinicides

Imidacloprid, Dinotefuran, Nitenpyram
Term
Macrocyclic lactone isolated from Saccharopolyspora spinosa. A nicotinic receptor agonist with affinity for the Da6 receptor. Also activated GluCl channels, inducing hyperpolarization.
Definition
Spinosad
Term
Closes chloride channels of all arthropods.
Definition
Fipronil
Term
Blocks Na channels in insect neurons, causing hyperpolarization.
Definition
Metaflumazone
Term
T/F: it is ok to use concurrently a drug that causes depolarization and a drug that causes hyperpolarization when treating for ectoparasites.
Definition
False.

This is why Dr. Hsu does NOT recommend Spinosad, as it causes concurrent depolarization and hyperpolarization.
Term
Which of the following does NOT have action against ticks or mites (when used alone, not in combination with other products)?

a. Amitraz
b. Coumaphos
c. Permethrin
d. Nitenpyram
e. Rotenone
Definition
d. Nitenpyram--only indicated for fleas
Term
Give the class of ectoparasiticide for the following drugs:

Diazinon
Coumaphos
Lufenuron/Diflubenzuron
Pyriproxyfen
Methoprene
Cabaryl/Propoxur
Metaflumazone
Spinosad
Dichlorvos
Imidacloprid/Nitenpyram
Tetrachlorvinphos
Permethrin/Fenvalerate
Rotenone
Amitraz
Fipronil
Definition
Diazinon: organophosphate

Coumaphos: organophosphate

Lufenuron/Diflubenzuron: Insect Development Inhibitors

Pyriproxyfen: Insect Growth Regulator

Methoprene: Insect Growth Regulator

Cabaryl/Propoxur: Carbamates

Metaflumazone: Other

Spinosad: Other

Dichlorvos: organophosphate

Imidacloprid/Nitenpyram: Neonicotinicides

Permethrin/Fenvalerate: Botanical Ectoparasiticides (Pyrethroids)

Rotenone: Botanical ectoparasiticide

Amitraz: Other

Fipronil: Other
Term
For each of the following classes of ectoparasiticides, list the ectoparasites for which they are effective:

Organophosphates
Carbamates
Insect Growth Regulators
Insect Development Inhibitors
Rotenone
Pyrethroids
Macrocyclic Lactones
Amitraz
Neonicotinicides
Spinosad
Fipronil
Metaflumazone
Definition
Organophosphates: all arthropods
Carbamates: all arthropods (used vs. fleas, ticks)
Insect Growth Regulators: Fleas, bed bugs
Insect Development Inhibitors: flies, fleas, bed bugs
Rotenone: all arthropods
Pyrethroids: all arthropods
Macrocyclic lactones: grubs, mites, lice, ticks, flies
Amitraz: ticks, mites
Neonicotinicides: Fleas, bed bugs
Spinosad: fleas
Fipronil: fleas, ticks
Metaflumazone: Fleas, ticks (if ProMeris Duo)
Term
Which fleacidal drug is considered the safest with the shortest duration?

a. Nitenpyram
b. Imidacloprid
c. Dinotefuran
d. Spinosad
e. Fenvalerate
Definition
a. Nitenpyram

Nitenpyram kill 95% of fleas in 5 hours, only lasts 1-2 days, and has rapid GI absorption, hydroxylation, conjugation, and urinary excretion, resulting in NO accumulation in body tissues.
Term
Which species should not be administered organophosphates due to severe toxicity problems?

a. Horses
b. Cats
c. Ruminants
d. A and B
e. B and C
Definition
e. B and C

Ruminants have about half the number of acetylcholinesterase of other species, so anti-cholinesterase drugs should be avoided.

Cats are easy to get excited, have a drug metabolism problem, and are sensitive to synthetic pyrethroids and anti-cholinesterase drugs.
Term
Cats should not be administered:

a. Organophosphates
b. Pyrethroids
c. Nitenpyram
d. A and B
e. B and C
Definition
d. A and B

Organophosphates and pyrethroids are bad news for cats.
Term
T/F: most ectoparasiticides are highly lipid soluble, and therefore may cause CNS disturbances.
Definition
True
Term
Horses tend to get what type of toxicity to ectoparasiticides?
Definition
Horses have sensitive skin, so they are more likely to get urticaria or hyperemia.
Term
List the toxic signs produced by organophosphates:
Definition
SLUDD
Cardiac arrhythmias
Fasciculations
Ataxia
Convulsions

Chronic toxicity leads to paralysis
Term
Treatment of acute organophosphate toxicity involves:

a. Atropine
b. 2-PAM
c. Yohimbine
d. A and B
e. A, B, and C
Definition
d. A and B

2-PAM must be given with atropine within 24 hours of OP exposure, as it cannot cross the BBB
Term
Treatment of carbamate toxicity includes:

a. Atropine
b. 2-PAM
c. Yohimbine
d. A and B
e. A, B, and C
Definition
a. Atropine

2-PAM is not needed for carbamate toxicity because AchE does not need to be reactivated, since the binding of AchE is REVERSIBLE.
Term
Why does it take such a long time for animals to fully recover from organophosphate poisoning if no treatment is given?
Definition
The signs of OP toxicity are so long-lived because organophosphates form a covalent bond with AchE, which cannot be readily broken down. When this bonding occurs, AchE is inhibited. Treatment is aimed at re-activating AchE
Term
_________________ works by reactivating acetylcholinesterase and cannot cross the BBB, so must be given in conjunction with atropine.
Definition
Pralidoxime (2-PAM)
Term
T/F: Pralidoxime is the treatment of choice for chronic organophosphate toxicity.
Definition
False: there is nor treatment for chronic OP toxicity
Term
What three classes of drugs should be avoided when using organophosphates?
Definition
Any drugs that affect Ach receptors or the CNS should be avoided:

1. Cholinergic agonists
2. Skeletal muscle relaxants
3. CNS stimulants/depressants
Term
_____________, _________________, and ______________ are insect growth regulators.
Definition
Cryomazine
Methoprene
Pyriproxyfen
Term
_______________ and _________________ are insect development inhibitors.
Definition
Diflubenzuron
Lufenuron
Term
________________ is an inhibitor of microsomal enzymes that is used synergistically with pyrethroids to increase insecticidal activity.
Definition
Piperonyl butoxide (MGK 264)
Term
_________________ and _______________ are two classes of insecticides that cause rapid knockdown.
Definition
Rotenone
Pyrethroids
Term
________________ and ______________ are two ectoparasiticides that are used to control demodicosis.
Definition
Ivermectin (Macrocyclic lactone)
Amitraz
Term
List 5 ectoparasiticides that can be given orally to be effective:
Definition
Diflubenzuron
Lufenuron
Nitenpyram
Ivermectin
Organophosphates
Term
Amitraz activates ________________ receptors in animals and _____________ receptors in arachnids. Because of this, what side effects would we see in animals?
Definition
Alpha-2 adrenergic receptors: animals

Octopamine receptors: arachnids (inhibits neurotransmission-->flaccid paralysis)

Side effects similar to xylazine: sedation, bradycardia, hyperglycemia, GI stasis
Term
Amitraz should not be used in horses due to the risk of what?
Definition
Fatal impaction colic
Term
_____________, ____________, _____________, and ________________ are all nicotinic receptor agonists. Of these, ______________ and ____________ are administered orally, while _____________ and ________________ are administered topically. _______________ has the most rapid onset and shortest duration of action, making it safe and effective and a good choice for quick treatment of fleas before boarding or going to an area with a lot of other animals.
Definition
Imidacloprid
Dinotefuran
Nitenpyram
Spinosad

Spinosad and Nitenpyram are administered orally

Imidacloprid and Dinotefuran are administered topically

Nitenpyram has the quickest onset and shortest duration of action
Term
You are working in an animal shelter and received a litter of 2 week old kittens that are infested with fleas very badly. Which fleacide would you use to take care of the bad flea infestation in these kittens and why?
Definition
Nitenpyram--nitenpyram is the safest fleacide with the shortest duration. It is rapidly absorbed, hydroxylated, conjugated, and excreted with no accumulation in body tissues.

You could potentially also use Program (lufenuron + nitenpyram) to be sure to kill the flea larvae as well. Lufenuron is also safe for very young animals (though not labeled for kittens as young as 2 weeks).
Term
What are the active ingredients in Frontline Plus?
Definition
Fipronil + methoprene
Term
When would Frontline Plus be a better choice than frontline?
Definition
Frontline Plus kills fleas for up to 3 months, ticks for 1 month, and is effective against flea eggs. The effectiveness against flea eggs is due to the methoprene. Frontline Plus, then, would be a better choice when trying to rid an animal from all the stages of the flea life cycle.
Term
List the physiological mechanisms by which arthropods become resistant to ectoparasiticides:
Definition
1. decreased penetration into target organism or increased efflux of ectoparasiticide glycoprotein
2. increased metabolism of ectoparasiticides
3. decreased sensitivity of the target site or receptor
Term
Which of the following ectoparasiticides should not be used in combination with metaflumazone?

a. Pyrethroids
b. Spinosad
c. Fipronil
d. Neonicotinocides
e. all of the above should not be used w/ metaflumazone
Definition
e. All of the above should not be used with metaflumazone

Drugs that cause hyperpolarization and depolarization should not be used concurrently.

Pyrethroids cause persistent opening of Na channels: depolarization

Spinosad causes concurrent hyperpolarization (GluCl) and depolarization (nicotinic agonist)

Neonicotinicides cause depolarization (nicotinic agonists)

Fipronil blocks Cl channels: depolarization

Since metaflumazone is a Na channel blocker and causes hyperpolarization, it should not be used with anything that causes depolarization.
Term
Thiol organophosphates
Definition
Diazinon
Coumaphos
Phosmet
Pirimphos
Term
Oxy Organophosphates
Definition
Dichlorvos
Tetrachlorvinphos
Term
Carbamates
Definition
Carbaryl
Propoxfur
Term
Insect Growth Inhibitors
Definition
Cryomazine
Methoprene
Pyriproxyfen
Term
Insect Development Inhibitors
Definition
Diflubenzuron
Lufenuron
Term
Pyrethroids
Definition
Fenvalerate
Permethrin
Deltamethrin
Term
Just know rotenone is a botanical ectoparasiticide
Definition
Term
Macrocyclic Lactones
Definition
Ivermectin
Spinosad
Term
Just know amitraz (not in a class of ectoparasiticides)
Definition
Term
Neonicotinicides
Definition
Imidacloprid
Dinotefuran
Nitenpyram
Term
Just know fipronil (not in class of ectoparasiticides).
Definition
Term
Just know metaflumazone (not in class of ectoparasiticides).
Definition
Term
T/F: most macrocyclic lactones effectively kill fleas at a clinical dose.
Definition
False: ivermectin is useful vs. mites, lice, ticks, and flies, but DO NOT kill fleas at clinical doses

Take a long time to work
Term
Dosing for lufenuron is __________ in dogs and ___________ in cats and is administered how often?
Definition
10 mg/kg PO in dogs
30 mg/kg PO in cats
Administered every 30 days
Term
What types of side effects can pyrethroids cause in cats?
Definition
CNS disturbances: tremors, rigidity, ataxia, seizures, hypersalivation, mydriasis
Term
How is pyrethroid toxicity treated?
Definition
Muscle relaxants: methocarbamol

Anti-convulsants: diazepam
Term
What are the side effects that can occur with lufenuron administration?
Definition
Anorexia
Vomiting
Lethargy
Term
T/F: spinosad should not be used concurrently with other macrocyclic lactones.
Definition
True
Term
How long does capstar last?
Definition
1-2 days
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