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Antinematodals Flashcards

1
Q

What are examples of Avermectins?

A

Ivermectin
Selamectin
Doramectin
Eprinomectin

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2
Q

What are examples of Milbemycins?

A

Milbemycin oxime

Moxidectin

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3
Q

What gives rise to the collective name for Macrolides?

A

The macrocyclic ring

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4
Q

What is the mechanism of action of Avermectins and Milbemycins inside the insect or parasite?

A

Through the stimulation of a receptor site for glutamate

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5
Q

What does stimulation of the glutamate receptor cause?

A

Muscle paralysis that causes starvation or move away from their infection site and die

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6
Q

What parasites are macrolides are ineffective against because they do not have glutamate receptors?

A

Tapeworms and flukes

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7
Q

Do Macrolides produce a well-documented toxicity?

A

Yes

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8
Q

Because macrolides are lipophilic, they can readily diffuse through and potentially gain access to the GABA receptors causing toxicity. Why does toxicity not occur every time a macrolide is administered?

A

Because of a special protein pump P-glycoprotein (P-gp) that moves drugs from the brain side back into the blood

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9
Q

Where else are P-glycoprotein pumps located?

A

Liver and GI tract

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10
Q

What affects the P-gp pump and allows macrolides to accumulate within the brain, increasing the risk for toxicity?

A

Inhibited by other drugs

P-gp can be defective

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11
Q

What drugs can inhibit the P-gp?

A

Calcium channel blocker antiarrhythmics
Cyclosporine immunosuppressant
Antifungal agents Ketoconazole or itraconazole

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12
Q

What breeds of dog have a genetic defect in the gene that codes for their P-gp?

A

Collies and other related breeds

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13
Q

What is the gene that codes for P-gp known as?

A

Multiple drug resistance 1 genes (MDR1)

ATP-binding cassette-type B1 genes (ABCB1)

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14
Q

What are the clinical signs of animals with a defective P-gp pump?

A 
CNS depression
Hypersalivation
Vomit
Become ataxic
Stagger
Progress to depression
Unresponsiveness
Bradycardia
Mydriasis
Loss of menace response
Coma
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15
Q

Is there an antidote for avermectin or milbemycin toxicosis?

A

No. Recovery requires the animal be kept alive in a comatose or severely depressed state for days to weeks before the effects of the drug wear off

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16
Q

What explains how avermectins and milbemycins readily penetrate many tissues and persist at low, but still effective concentrations for a long period of time?

A

Lipophilic nature of macrolides

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17
Q

What else are macrolides effective against when administered by oral or injection because they can penetrate into the tissues and the tissue fluid?

A

Mites
Sucking lice
Feeding ticks

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18
Q

What can macrolides contaminate for an extended period of time?

A

Milk

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19
Q

What are macrolides excreted by?

A

Liver into the feces

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20
Q

What explains the long-lasting effect of macrolides in the body?

A

The enterohepatic circulation in conjunction with the persistence in the tissues

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21
Q

What is the first macrolide to be available for use in vet med?

A

Ivermectin

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22
Q

What does Ivermectin treat?

A

Heartworms

Intestinal & external parasites

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23
Q

Ivermectin is combined with what to produce parasiticides with a wider spectrum of activity?

A

Other anthelmintics

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24
Q

Heartgard Plus is combined with what and what does it treat?

A

Ivermectin & Pyrantel pamoate

Control intestinal ascarids

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25
Q

Iverhart Max is combined with what and is used to treat what?

A

Ivermectin + Pyrantel pamoate + Praziquantel

Tapeworms, intestinal ascarids

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26
Q

Small animal toxicity is associated with waht?

A

Accidental exposure to large animal products and not with small animal products

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27
Q

What does Ivermectin require to be effective against parasites?

A

Small concentrations

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28
Q

What is the normal dose of Ivermectin to prevent heartworm?

A

0.006 mg/kg

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29
Q

What dose of Ivermectin is toxic to Collies?

A

0.1 mg/kg

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30
Q

What medication is on the shelves as Revolution and is a broad-spectrum endectocide?

A

Selamectin

31
Q

What is Selamectin primarily used as?

A

Heartworm preventative

Also effective against GI parasites & external parasites?

32
Q

What external parasites is Selamectin effective against?

A

Fleas
Ear mites
Sarcoptic manage
One tick species

33
Q

Selamectin is approved as what kind of medication?

A

Monthly topical application in dogs and cats

34
Q

How much of the topically applied drug do dogs absorb systemically?

35
Q

How much of the topically applied drug do cats absorb systemically?

36
Q

Because of the high absorption rate what else is topically applied selamectin approved to treat in cats?

A

Ancylostoma tubaeforme and Toxocara cati

37
Q

Why is toxicity in breeds with MDR1 gene mutation rare?

A

Because of the route of administration and the relatively low amount of drug absorbed in dogs

38
Q

Is topical application still effective as a heartworm preventative even after the pet is bathed?

39
Q

What does oral contact with the compound produce?

A

Hypersalivation and vomiting

40
Q

Does topical application overdoses of 10x the prescribed produce significant signs in dogs and cats?

A

No other than hypersalivation

41
Q

What macrolides are approved for use in cattle?

A

Doramectin and Eprinomectin

42
Q

What macrolide is on the market as Dectomax, is available as an injectable and topical “Pour-on” and approved for use in cattle and swine?

A

Doramectin

43
Q

What macrolide is on the market as Eprinex, approved for use as a topical application in cattle, subcutaneous injection in beef cattle and is effective against internal parasites, grubs and mange?

A

Eprinomectin

44
Q

How many days does the subcutaneous Eprinomectin injection in beef cattle (LongRange) provide antiparasitic activity?

A

100 to 150 days

45
Q

What antinematodal was originally used against agricultural insects?

A

Milbemycin Oxime

46
Q

Milbemycin Oxime orally administered tablets are FDA approved to treat what?

A

heartworm prevention in dogs & cats
Treatment/control for hookworms & roundworms in dogs and cats
Whipworms in dogs
Topically applied treatment of ear mites in cats

47
Q

What products contain Milbemycin Oxime?

A

Interceptor
Sentinel
Trifexis

48
Q

What does Milbemycin Oxime show some promise in treating?

A

Demodectic mange

49
Q

Milbemycin Oxime is nontoxic to what breed when doses 20x the regular dose?

50
Q

What products contain Moxidectin?

A

Cydectin
Quest
Advantage Multi
ProHeart 6

51
Q

Does ProHeart 6 clear the adult heartworms or the circulating microfilariae?

A

No. It is just used as a heartworm preventative

52
Q

Does ProHeart 6 prevent hookworm reinfection?

A

No it just kills the adults and migrating larvae

53
Q

Moxidectin is used in cattle and horses as what drug forms?

A

Pour on for cattle

Oral gels in horses

54
Q

What does Moxidectin products prevent in cattle and horses?

A 
Intestinal parasites
Mites
Cattle grubs
Horse Stomach bots
Lice
Flies
Nematodes
55
Q

What product comes as a combination of Moxidectin and Imidacloprid?

A

Advantage multi

56
Q

What is Advantage multi used for?

A

Approved for heartworm prevention
Treatment & control of roundworms, hookworms, whipworms
Treatment of sarcoptic mange & fleas

57
Q

Advantage Multi is the only FDA approved product for what?

A

eliminating the circulating microfilariae in dogs

58
Q

What is the mechanism of action of Benzimidazoles?

A

Attack Beta-tubulin proteins

59
Q

What are Beta-tubulin proteins involved in?

A 
Cell division
Maintaining cell shape
Cell motility
Cell secretion
Intracellular transport
60
Q

What does attacking the Beta-tubulin proteins accomplish?

A

Disrupts the normal cellular function & eventually kill the parasite

61
Q

How long does it take for benzimidazoles to work?

A

Up to 24 hours

Multiple exposures to the drug over 3 or more days

62
Q

What have been noted at very high doses of selected benzimidazoles?

A

Teratogenic effects

63
Q

Benzimidazoles are recognized by what?

A

Azole suffix

64
Q

What are examples of benzimidazoles?

A 
Thiabendazole 
Fenbendazole (Panacur, Safe-Guard)
Oxibendazole (Anthelcide EQ)
Albendazole (Valbazen)
Fabantel (Drontel Plus)
65
Q

What is considered the prototype drug for the benzimidazoles?

A

Thiabendazole

66
Q

Which benzimidazole has a wide range of activity against ascarids & strongyles, and some antiinflammatory and antifungal activity?

A

Thiabendazole

67
Q

Thiabendazole has been used for a long time, and because of this what has been documented with this drug?

A

Parasitic resistance

68
Q

What has a wide spectrum of activity against nematodes, effective against a limited number of tapeworms and is used as an oral paste/solution in horses, granules in small animals and exotics?

A

Fenbendazole

69
Q

What has been used for a long as an equine dewormer to control large and small strongyles, large roundworms, pinworms, and threadworms?

A

Oxibendazole

70
Q

What is used to treat intestinal nematodes, lungworms, trematodes, cestodes and protozoa in livestock?

A

Albendazole

71
Q

What has been linked to teratogenic effects and bone marrow suppression?

A

Albendazole

72
Q

Which benzimidazole is a “Prodrug”?

73
Q

What is a “prodrug”?

A

It must be converted by the metabolism to the active form of the drug

In the case of Febantel this means fenbendazole & oxibendazole

74
Q

Febantel is not available as a stand alone antiparasitic. What is it combined with and what is the name of the drug it is used in?

A

Combined with pyrantel and praziquantel to form Drontal Plus

Pharmacology (21 decks)

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