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Clinical Pharmacology > Antiprotozoal Agents (1) > Flashcards

Antiprotozoal Agents (1) Flashcards

1
Q

Name 8 antiprotozoal agents

A

See list

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2
Q

What is the agent of choice for toxoplasma

A

Clindamycin

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3
Q

Clindamycin MOA

A

Long term exposure to low levels —> decrease T gondii replication

Affects PR synthesis of free parasites

Impairs tachyzoite infecting host cell

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4
Q

Clidamycin dose

A

10-20 mg per kg BID or PO

IM 3-6 weeks

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5
Q

Caution with what for Clindamycin

A

Treating cats with pulmonary TP

Unexplained feline deaths in experimental trial

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6
Q

Clindamycin toxicity

A

Oral or IM doses at HIGHER doses than for anaerobic infections, for 2-4 weeks

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7
Q

What is FIRST LINE drug of choice for giardiasis

A

Metronidazole

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8
Q

Metronidazole and cattle

A

Not allowed!

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9
Q

Metronidazole and trichomonas

A

Effective! But Not to be used in cattle

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10
Q

Metronidazole MOA

A

Intermediate metabolites —> affect DNA

Alters Metabolic pathways that are needed for Protozoa survival

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11
Q

Metro toxicity

A

Dose dependent vestibular toxicity - slowly reversible

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12
Q

Metro use in Food animals

A

PROHIBITED
No tritrichmonas to in cattle

ELDU in all veterinary species

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13
Q

Triazines (name 2)

A

Ponazuril

Diclazuril

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14
Q

Ponazuril

A

Marquis

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15
Q

Diclazuril

A

Protazil

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16
Q

Triazines MOA

A

Damages apicoplast of Protozoa organisms (downstream effects unclear)

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17
Q

Triazines — use in poultry

A

Used as coccidiostat

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18
Q

Triazines- FDA approved treatment and prevention of what

A

Sarcocystis neurona, horses, PO for 30 days

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19
Q

Triazines toxicity

A

Horses- blisters (nose, mouth), Rash and hives, Colic, Diarrhea

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20
Q

Is Ponazuril or Diclazuril safer

A

Literature says P is safer

But not nec true (on market longer)

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21
Q

Nitrothiazoles

A

Nitrazoxanide= navigator

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22
Q

Nitrothiazoles MOA

A

Compound —> reduced to FR—> interferes with cellular respiration of TARGET organism

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23
Q

Nitrothiazoles spectrum of activity

A

FDA approved TREATMENT for s neurona — not prevention though

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24
Q

Nitrothiazoles toxicity

A

Severe and fatal enterocolitis (can kill normal flora)

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25
Q

Sulfonamides — name 4

A

Sulfadimetoxine
Sulfadimetoxine with ormetoprim

Sulfadiazine with trimethoprim

Sulfamethoxazole with trimethoprim

26
Q

SEE CHART OF ANTIPROTOZOAL AGENTS

A

Memorize chart

Compare Ponazuril vs Nitrazoxanide

27
Q

Anthelmintic resistance — species

A

Horse sheep goats = most affected

Cattle in NZ and South America

28
Q

Mechanisms of anthelmintics Resitance

A

Failure to reach SOA
Altered target
Inactivation of anthelmintic agent

29
Q

Resistance to which drugs documented? Which two receive the most attention (although not “true”)

A

ALL DRUGS

Benzimidazoles and ML “statistically” though

30
Q

3 methods to reduce resistance

A

Combine or rotate drugs with diff MOA

Using as few treatments as possible

Use appropriate doses (overestimate the dose if you do not have exact weight???)

31
Q

Name 6 antinematodal drugs

A

Benzimidazoles
Levamisole
Pyrantel, Morantel
Heterocyclic compounds (Piperazine, Diethylcarbamazine)
Arsenicals (Melarsomine — heartworm adulticide)
Cyclic Octadepsipeptides (Emodepside)

32
Q

Benzimidazoles examples

A

Albendazole, Fenbendazole, others

33
Q

Benzimidazoles MOA

A

..see diagram too

Binds to parasite free Beta-tubulin molecules —> affects tubulin polymerization and interfering with cell division, motility , and transport

Inhibits enzymes —> DECREASED energy production in parasites

34
Q

Benzimidazoles spectrum of activity

A

..BROAD spectrum (newer agents)

GI nematodes, lung nematodes, some cestodes and treamtodes

Protozoa (giardiasis) (Fenbendazole and albendazole treats giardia in dogs and cats)

Fungi (thiabendazole aka Tresaderm)

Mites

35
Q

Therapeutic margin of benzimidazoles

A

Wide

36
Q

Albendazole toxicity in cats

A

Weight loss
Neutropenia
Mental dullness

37
Q

Albendazole toxicity in dogs

A

Lethargy and anorexia
BM suppression

Liver toxicity (high dose or chronic)

Last two- unknown mechs

38
Q

Which drug has BM suppression

A

Albendazole, dogs

39
Q

When is albendazole contraindicated

A

Pregnant animals- do not sue in female cattle in first 45 days pregnancy

TERATOGENIC EFFECTS POSSIBLE

40
Q

Fenbendazole has efficacy against what

A

BROAD spectrum agent with efficacy against…

41
Q

Benzimidazoles — herd dosing

A

Incorporation into water or feed blocks (no direct control!)

Drenching/tubing = time consuming, $

Ruminants devices- special devices that release constant rate of drug, for up to 4 month (animal can be constantly exposed to the drug)

42
Q

Clinical use of Benzimidazoles in SA

A

Hookworms, whipworms, tapeworms, TAENIA but not Echinococcus, GIARDIA

43
Q

Benzimidazoles - clinical use in horses

A

Fenbendazole-

Large and small strongyles
Pin worms

At higher doses- ascarids

44
Q

FEBANTEL

A

Pro drug of Fenbendazole (active metabolite)

IMPT- don’t forget because it doesn’t end in “azole”

45
Q

Benazimadoles- name two really important ones

A

Thiabendazole (ineffective against cestodes and trematodes)

FEBANTEL (Pro Drug of fenbendazole!!) only one that doesn’’t end in azole

46
Q

Benzimidazoles clinical use— WITHDRAWL times

I.e. fenbendazole in cattle vs pigs

A

Variable, dep on species and formulation

Cattle- 27 days for albendazole, 8 days for fenbendazole

Pigs- 0 days for Fenbendazole

47
Q

Name 8 Antiprotozal Agents

A 
Pirimethamine 
Amprolium
Clindamycin
Metronidazole
Triazines (Ponazuril, Diclazuril)
Nitrothiazoles (Nitrazoxanide = Navigator )
Sulfonamides/trimetropim
Benzimadoles
48
Q

Pyrimethamine MOA

A

Normally, Para-aminiobenzoic acid (PABA) is converted by Dihydropteroate synthase into Dihydropteric acid—> Dihydrofolic acid —> via Dihydrofolate reductive —> Tetrahydrofolic acid

Basically Pyrimethamine inhibits Dihydrofolate Reductase —> Less Tetrahydrofolic acid (active form of folic acid)

LESS folic acid synthesis

49
Q

Folic acid synthesis is important for what

A

DNA and RNA synthesis

50
Q

Pyrimethamine spectrum of activity

A

Toxoplasmosis (dogs and cats)
Neospora (dogs)
Sarcocystis (EPM in horses)

51
Q

Pyrimethamine toxicity

A

BM suppression

52
Q

Pyrimethamine and sulfas

A

Used in combination with sulfas (sulfadiazine) for 30-180 days

53
Q

Amprolium MOA

A

It is a structural analog of thiamine —> competes for thiamine uptake into Protozoal organisms

54
Q

Amprolium Spectrum of activity

A

A PREVENTATIVE (vs therapeutic) medication, greatest effect against FIRST generation schizonts

Used in drinking water of poultry and cattle for prevention/treatment of coccidia

55
Q

Amprolium toxicity

A

Thiamine deficiency (uncommon)

56
Q

Thiamine deficiency — PEM in what species

A

Cattle, goat, sheep
Camelids
Deer

57
Q

Polioencephalomalacia signs

A

Star gazing
Anorexia
Loss of motor control
Coma, death

58
Q

Thiamine deficiency — polyneuritis in what species

A

Chicken, turkey, pigeons

59
Q

Polyneuritic clinical signs

A

Star gazing
Anorexia, paralysis
Death

60
Q

Amprolium pharmaceutical considerations- labeled for what animals

A

Labeled for food animals

ELDU in dogs, cats, other animals has occurred

Clinical Pharmacology (7 decks)

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