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Pharmacology II > Anti-parasitic Agents IV > Flashcards

Anti-parasitic Agents IV Flashcards

1
Q

Ectoparasites include?

A
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2
Q
  • Ectoparasites can transmit ________
  • Ectoparasites can cause ________ ________
A

diseases, allergy dermatitis

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3
Q

The ideal ectoparasiticide should be?

A
  • An effective repellent and adulticide
  • Persistent in the blood or skin surface
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4
Q

The formulation of an insecticide must be stable to _______ and _______/__________.
Provide an example.

A

sunlight, water/shampooing
Example:
Imidacloprid→ photostable and persistent after shampooing
Early generation of pyrethroids

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5
Q

A good ectoparasiticide has a high __________ against the ectoparasite and is not ____ to the host

A

efficacy, toxic

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6
Q
  • Fleas engorge with a blood meal from the host 5 min to 1 hour of infestation
    → female fleas 25 min
    → male fleas 11 min
A
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7
Q

Ticks feed on a blood meal for a longer period

A
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8
Q

Ectoparasiticides act on what parts of the nervous system?

A
  • Acetylcholinesterase (AChE) inhibitors
  • Na+ channel blockers
  • Nicotinic acetylcholine receptor (nAChR) inhibitors
  • GABA/glutamate receptor Cl- channel inhibitors
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9
Q

Other than the nervous system, ectoparasiticides act as?

A
  1. Repellants
  2. Attack insect growth and development
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10
Q

Antiparasitics are available as:

A
  • Sprays
  • Powders
  • Shampoo
  • Foams
  • Spot-ons
  • Dips
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11
Q

Sprays may have residual effect depending
on the active compound and concentration

A
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12
Q

Shampoos have a ____ residual effect and must stay on the skin at least ___ minutes (to kill fleas and ticks)

A

little, 10

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13
Q

Spot-on products → ___ of use and _____

A

ease, efficacy

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14
Q

Powders are _______ formulation but must be _______ applied

A

safest, frequently

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15
Q

Fipronil (Frontline®) is
* Effective against _____ fleas
* All stages of ______ dog ticks, _____ dog ticks, _____ ____ ticks, and _____ ticks
* Treatment and control of _____ lice (Trichodectes canis)
* Effective against flea ___ and flea ____ (Frontline® Plus)

A

adult
brown, american, lone store, deer

biting

eggs, larvae

Drugs with same formulation are effective against flea eggs, not just the specific drug frontline???

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16
Q

Fipronil is not effective in preventing fleas from ?

A

preventing fleas from biting and feeding

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17
Q

Fipronil is approved for ?

A

dogs and cats (> 8 weeks)

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18
Q

What is the MOA of Frontline?

A
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19
Q

Describe Fipronil’s safety and toxicity.

  • _____ margin of safety
  • No adverse effect at ___-times the doses in dogs and cats
  • It is not _______
    ➢ At toxic doses it can cause?
A
  • Wide margin of safety
  • No adverse effect at 5-times the doses in dogs and cats
  • It is not teratogenic
    ➢ At toxic doses it can cause:
  • Hyperactivity
  • Hyperexcitability
  • Convulsions
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20
Q

What is the MOA of Neonicotinoids: Imidacloprid (Advantage®) and Spinosad (Comfortis®) Nitenpyram (CapstarTM)?

A

Competitive inhibition at the postsynaptic nicotinic acetylcholine receptors (nAChR)

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21
Q

Neonicotinoids cause a ________ response

A

bi-phasic

Increased frequency of spontaneous discharge followed by a complete block to nerve propagation

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22
Q

Neonicotinoids do not bind to NR in ________ effectively

A

mammals

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23
Q

Describe the efficacy of Imidacloprid (Advantage®).

  • Imidacloprid is indicated for the treatment of ____ and ____ stage ____ in dogs and cats
  • kills ____ and _____ within 1 hour of exposure
  • It has limited activity against ____
A
  • Imidacloprid is indicated for the treatment of adult and larval stage fleas in dogs and cats
  • kills larvae and adult fleas within 1 hour of exposure
  • It has limited activity against ticks
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24
Q

Describe the safety and toxicity of Imidacloprid.

  • Imidacloprid is not a _________
  • The available products should not be given to patients younger than ?
A
  • Imidacloprid is not a teratogen
  • The available products should not be given to patients younger than 4 months
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25
Q

Imidacloprid (Advantage®) Formulations:

A
  • Imidacloprid → Advantage®
  • Imidacloprid + pyriproxyfen → Advantage® II (for dogs and cats)
  • Imidacloprid + permethrin → K9 Advantix®
  • Imidacloprid + moxidectin → Advantage Multi® (for dogs and cats)
26
Q

Imidacloprid + moxidectin → Advantage Multi® (for dogs and cats) is a spot-on formulation used to treat ?

A

fleas, heartworm prevention, intestinal worm, and ear mites (moxidectin)

27
Q

Spinosad (Comfortis®) Formulations

A
  • Spinosad → Comfortis® (chewable tablets, for dogs and cats)
  • Spinosad + milbemycin oxime → Triflexis®(chewable tablets, for dogs)
28
Q

The bioavailability of spinosad is greater than 70% after ____ administration

A

oral

29
Q

Describe the efficacy of Spinosad.

  • It is indicated for the prevention and treatment of _____ flea in dogs and cats
    (≥ __ weeks of age)
  • It starts working in __ min of exposure
  • Spinosad is not labeled for use against ___ (not effective)
A
  • It is indicated for the prevention and treatment of adult flea in dogs and cats
    (≥ 14 weeks of age)
  • It starts working in 30 min of exposure
  • Spinosad is not labeled for use against ticks (not effective)
30
Q

Spinosad (Comfortis®)
Safety/Toxicity

A
  • Adverse reactions are rare in dogs and cats
  • The oral LD50 in rats is 3600 mg/Kg → very safe
31
Q
A
32
Q

Ivermectin treats what ectoparasites in all of the following animals:
1. Swine
2. Cattle
3. Dogs
4. Cats

A

See below

33
Q
A
34
Q
A
35
Q
A
36
Q

What is the MOA of Isoxazolines: Sarolaner, afoxolaner, fluralaner, and lotilaner?

A
  • These drugs inhibit GABA-gated and glutamate-gated chloride ion channels (blockade). This
    results in an irreversible hyperexcitation in targeted parasites
  • Isoxazolines are more selective for GABA receptors in insects and ticks than those receptors
    in mammals
37
Q

T/F: MLs are called broad spectrum drugs because they are effective even against cestodes.

A

False, they do not act on cestodes

38
Q

T/F: The main MOA of MLs is caused by acting on GABA gated chloride channels.

A

False
The main MOA is the glutamate gated chloride channels

39
Q

Isoxazolines: Sarolaner, afoxolaner, fluralaner, and lotilaner are effective against?

A
  • Effective against fleas (Ctenocephalides felis and C. canis)
  • Effective against ticks → Dermacentor reticulatus, D. variabilis, Ixodes ricinus, Rhipicephalus
    sanguineus, Amblyomma Americanum (lone star tick), A. maculatum, and I. scapularis )
40
Q

Name the ticks that are common vectors of dz in the USA?

A

Rickettsia rickettsii (Rocky Mountain spotted fever) is transmitted by Dermacentor ticks,
Borrelia burgdorferi (Lyme disease) by Ixodes ticks, and Ehrlichia and Babesia by
several tick species including those of the genera Dermacentor, Amblyomma, and
Rhipicephalu

41
Q

Isoxazolines: Sarolaner, afoxolaner, fluralaner, and lotilaner
Pharmacokinetics
* Good absorption following ____ administration
* They have a _____ distribution
* Low ________ clearance
* ____ metabolism
* _____ and ______ excretion

A

oral, wide, systemic, Liver, Billiary, urinary

42
Q

Isoxazolines: Safety/Toxicity
* These drugs are very selective for ____ and ___ nervous system
* ____ adverse effects have been observed in dogs receiving doses five time the label dose

A

fleas, tick, No

43
Q

Pyrethrins are extracts from ?

A

chrysanthemum flower

44
Q

What is the MOA of Pyrethrins?

A

Mode of action
They disrupt neurologic function by prolonging the opening of Na+ channels→ It results in repetitive membrane depolarization
* Pyrethrins rapidly kill fleas, flies, lice, cheyletiella, otodectes, and mosquitoes

45
Q

Insect sodium channels can be as much as ____ times more sensitive than mammalian channels

A

100

46
Q
  • Pyrethroids are synthetic analogs of _______ (same MOA). They are more _____ to
    breakdown
  • Pyrethroids are extremely selective for ______
  • Pyrethroids are grouped into 4 generation
  • The ____ generation include the ever-popular pyrethroids
A

pyrethrins, resistant

insects

third

47
Q

________ is probably the most widely used pyrethroid in veterinary medicine

A

Permethrin

48
Q

Both pyrethrin and permethrin have ______ properties

A

repellent

49
Q

Most of the spot-on products are at high concentrations of __________ (up to 65%) and are allowed only FOR ____ and NOT ___

  • The (3?) are formulated at lower concentration (0.05%)
    → approved for both dogs and cats
A

Permethrin, DOGS, CATS

sprays, shampoos, and dusts

50
Q

Permethrin is also widely used in food animal as ____ and ____-on to treat ectoparasites
➢ Require ____ withdrawal times provided the product is correctly applied!!!

A

sprays, pour
short

51
Q

Dermal absorption of pyrethrins and pyrethroids is very limited (<1%) across the ____ of domestic
animals and humans. They are very ________ and have _____ molecular weights.

A

skin, lipophilic, large

52
Q

Toxicity can follow _________ (grooming) or
__________ absorption
→ Consider all the factors that may contribute to this effect

A

ingestion, percutaneous

53
Q

Clinical signs of pyrethroid toxicity may be confused with ____ or _______ toxicity
* Toxicity is manifest as ?
There is no specific ________ for pyrethroid toxicity
➢ Treatment is ________ → include _______

A

OP, carbamate

salivation, tremors, and seizures

antidote, symptomatic, bathing

54
Q

The IGRs can be grouped as?

A

Juvenile-hormone analogs (JHAs)
Insect development inhibitors (IDIs)

55
Q

Juvenile-hormone analogs (JHAs) falsely signal the organism such as (3?) to remain in its immature egg or larval stage

A

ticks, fleas, and flies

56
Q

List the approved JHAs.

A
57
Q
  • Methoprene is used mainly to control ?
A

horn flies in cattle

58
Q
  • Pyriproxyfen is often applied as ?
A

sprays, spot-ons, and/or collar for dogs and cats

59
Q

Insect development inhibitors (IDIs): Benzoylphenyl urea compounds interfere with the development of the ?

A

exoskeleton by inhibiting chitin synthesis
or deposition pathways

60
Q

Chitin is an essential constituent of ?

A

flea eggshells and exoskeleton of immature fleas
→ Diflubenzuron
→ Lufenuron

Pharmacology II (27 decks)

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