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Clinical Pharmacology > Antiprotozoal Agents (2) > Flashcards

Antiprotozoal Agents (2) Flashcards

1
Q

Imidazothiazole (Levamisole) acts at what receptor

A

Nicotonic Ach receptors on nematode muscle cells —> Spastic paralysis !!

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2
Q

Imidzothiazoles Spectrum

A

A variety of GIT and lung nematodes

NOT CESTODES OR TREMATODES

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3
Q

Imidazothiazoles- toxicity

A

Cholingeric activity -> MUSCARINIC AND NICOTONIC EFFECTS

i.e. SLUD, resp distress, bradycardia, asfixia, CNS depression

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4
Q

Imidazothiazoles — antidote

A

None

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5
Q

Imidazothiazoles— theraeutic margin

A

MOST TOXIC anthelmintic

Fairly narrow therapeutic margin (safety margin may be as low as THREE TIMES the therapeutic dose)

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6
Q

Imidazothiazoles sheep vs cattle; chicken

A

Sheep seem more sensitive than cattle

Chickens tolerate it well

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7
Q

Imidazothiazoles forms of usage

A

Tablet, oral solution, oral drench, feed additive, SQ, or TOPICAL POUR ON

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8
Q

Imidazothiazoles herd dosing

A

Use SQ or IM or Pour on for the cattle

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9
Q

Tetrahydropyrimidines (Pyrantel, Morantel) MOA

A

Agonist at Nicotinic Ach receptors (like Levamisole) —> spastic paralysis

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10
Q

Tetrahydropyrimidines spectrum of activity (horse)

A

Horses- GI NEMATODES

High doses- against ileocecal TAPEWORM OF HORSES

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11
Q

Tetrahydropyrimidines use in cattle, dogs, cats

A

GI nematodes

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12
Q

Tetrahydropyrimidines Toxicity

A

High margin of safety

Doses 7x greater than therapeutic dose —> no signs of toxicity

(Vs Levimasole) !!!!

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13
Q

What should you not combine with Tetrahydropyrimidines

A 
Other CHOLINERGIC agonists (Levamisole)
Or antagonists (piperazine)

**spastic paralysis!

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14
Q

Tetrahydropyrimidines

Pyrantel tartrate vs pamoate

A

Pyrantel tartrate for horses

Pamoate— horses and dogs

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15
Q

Pyrantel tartrate usage

A

HORSES: continues daily administration for prolonged periods of parasite exposure

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16
Q

Pyrantel pamoate uses in horses vs dogs

A

Horses- Suspension or paste, also mixing with feed

Dogs- Suspension and tablet forms, combined in a tablet
**with FEBANTEL and PRAZIQUANTEL

Combined with a chewable containing IVERMECTIN

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17
Q

Morantel tartrate usage

A

Only approved for cattle

*sustained release bolus for beef and dairy cattle

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18
Q

Heterocyclic compounds (piperazine) MOA

A

GABA agonists — induces FLACCID paralysis

Vs levimasole and Tetrahydropyrimidines— SPASTIC paralysis

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19
Q

Piperazine spectrum of activity

A

Narrow- primarily ASCARIDS

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20
Q

Piperazine toxicity

A

Wide margin of safety, even avail OTC

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21
Q

Piperazine toxicity

A

CNS depression (ataxia, weakness, muscle tremors)

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22
Q

name 2 heterocyclic compounds

A

Piperazine

Diethylcarbamazine

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23
Q

Piperazine usage

A

Dogs cats horses for ASCARIADS

24
Q

Diethylcarbamazine

A

First Heartworm preventive that has to be given daily

25
Q

When to use Diethylcarbamazine

A

Limited use- for dogs that do not tolerate MONTHLY heartworm preventatives

26
Q

Arsenicals

A

Melarsomine— heart worm adulticides

27
Q

Melarsomine MOA

A

Presumed to affect glycolysis (metabolism of parasite)

28
Q

Melarsomine spectrum of activity

A

Adult and 4 month old heartworms

29
Q

Melarsomine efficacy of a single regimen of 2 injections

What to do for second regimen

A

2 administrations, ONE MONTH APART —> efficacy of >90%

Second regimen —> 4months later —> efficacy to 98% (I think he is saying in class- do 1 month administrations, for 4 months??)

30
Q

Melarsomine- margin of safety and toxicity

A

Low margin of safety

Liver toxicity, Nephrotoxicity, adulticide induced thromboembolic pneumonia

31
Q

See orange chart— side effects

**know first five effects

A 
Injection site reactions
Coughing and gagging 
Depression / Leth
Anorexia /Inappetance
Pyrexia

Also Lung congestion, V/D , dyspnea, hypersalivation, panting, hemoptysis followed

32
Q

See second orange chart of onset times

A

Know that it isn’t immediate

But usually like a week later or so

33
Q

Dimercaprol

A

Possible Antidote

34
Q

Dimercaprol— when efficacious

A

If given within 3 hours of melarsomine administration (but reduces the effects of melarsomine)

35
Q

Melarsomine is contraindicated for what class

A

Dogs with Class 4 (very severe HW diease)

MAY DIE

36
Q

Melarasomine in cats

A

NO. Not indicated !!!!!

37
Q

Where to inject immiticide

A

GIVE IN LUMBAR AREA ONLY (deep IM injection into epaxialmuscle group between L3-L5)

NOT SQ! If formulation stays in between skin and muscle will lead to inflammation and abscess

38
Q

Melarsomine IV or IM

A

IM ONLY
NOT IV

AVOID SUPERFICIAL INJECTION OR LEAKAGE

39
Q

Melarsomine monitoring

A

MONITOR DURING TX AND FOR UP TO 24 HOURS AFTER LAST INJECTION

Keep the patient in your care at LEAST 8 hours (ideal 24 hours to see adverse effects)

40
Q

Melarsomine goal

A

Eliminate ALL ADULT heartworms with min post TX complications

41
Q

Melarsomine— what stage effective

A

ADULTS ONLY

42
Q

Emodepside MOA

A

Binds to a G protein coupled receptor (GPCR) which is a LATROPHILIN like receptor —> secondary messengers system —> releases an INHIBITORY NEUROPEPTIDE (possible GABA) —> FLACCID PARALYSIS

43
Q

Emodepside spectrum of activity

A

Broad NEMATODAL ACTIVITY (larval and adult forms— including those resistance to other drugs)

Activity against TAPEWORMS

44
Q

Emodepside toxicity, margin of safety

A

High margin of safety

45
Q

Emodepside clinical use— dogs or cats

A

Cats as a spot on formulation (Profender)

Dogs— ORAL ONLY

46
Q

Emodepside - kittens

A

Do not use in kittens under two months

47
Q

Emodepside- Collies

A

If ivermectin sensitive copies, the therapeutic margin is a LOT LOWER

Treatment at 2x the therapeutic dose can cause —> discomfort, uncertain gait

48
Q

Anticestodal drugs

A

Praziquantel and esiprantel

Also Pyrantel and Morantel

49
Q

Name 2 important cestodes

A

Anoplocephala perfoliata— causes erosions around ileocecal valve —> intussuusception

Ecchinococcus granulosus (dogs)

50
Q

Praziquantel and epsiprantel MOA (name 2 main MOA)

A

1) damage tegument of parasites

2) Interferes with Ca2+ homeostasis —> causes muscular contraction and paralysis

51
Q

Praziquantel SOA (farm animals vs dogs)

A

Targets adults stages of ALL SPECIES OF TAPEWORMS of FARM AND COMPANION ANIMALS

100% activity against E granulosus in dogs, TREATMENT OF CHOICE

Some activity against trematodes

52
Q

Epsiprantel SOA

A

labeled for TX of common tapeworms in dogs and cats

53
Q

Praziquantel toxicity

A 
GI toxicity (vomiting ) with high doses
Safe in pregnant animals
54
Q

Epsiprantel (Castex)

A

GI toxicity (vomiting) can occur with large overdoses (40x in cats) !!

No signs of toxicity with 36x in dogs

55
Q

Take home message of toxicity of Praziquantel and epsiprantel

A

“Both drugs are relatively safe”

Clinical Pharmacology (7 decks)

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