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Antiprotozoal Agents (1) Flashcards

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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
Sulfonamides — name 4
Sulfadimetoxine Sulfadimetoxine with ormetoprim Sulfadiazine with trimethoprim Sulfamethoxazole with trimethoprim
26
SEE CHART OF ANTIPROTOZOAL AGENTS
Memorize chart Compare Ponazuril vs Nitrazoxanide
27
Anthelmintic resistance — species
Horse sheep goats = most affected | Cattle in NZ and South America
28
Mechanisms of anthelmintics Resitance
Failure to reach SOA Altered target Inactivation of anthelmintic agent
29
Resistance to which drugs documented? Which two receive the most attention (although not “true”)
ALL DRUGS Benzimidazoles and ML “statistically” though
30
3 methods to reduce resistance
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
Name 6 antinematodal drugs
Benzimidazoles Levamisole Pyrantel, Morantel Heterocyclic compounds (Piperazine, Diethylcarbamazine) Arsenicals (Melarsomine — heartworm adulticide) Cyclic Octadepsipeptides (Emodepside)
32
Benzimidazoles examples
Albendazole, Fenbendazole, others
33
Benzimidazoles MOA
..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
Benzimidazoles spectrum of activity
..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
Therapeutic margin of benzimidazoles
Wide
36
Albendazole toxicity in cats
Weight loss Neutropenia Mental dullness
37
Albendazole toxicity in dogs
Lethargy and anorexia BM suppression Liver toxicity (high dose or chronic) Last two- unknown mechs
38
Which drug has BM suppression
Albendazole, dogs
39
When is albendazole contraindicated
Pregnant animals- do not sue in female cattle in first 45 days pregnancy TERATOGENIC EFFECTS POSSIBLE
40
Fenbendazole has efficacy against what
BROAD spectrum agent with efficacy against...
41
Benzimidazoles — herd dosing
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
Clinical use of Benzimidazoles in SA
Hookworms, whipworms, tapeworms, TAENIA but not Echinococcus, GIARDIA
43
Benzimidazoles - clinical use in horses
Fenbendazole- Large and small strongyles Pin worms At higher doses- ascarids
44
FEBANTEL
Pro drug of Fenbendazole (active metabolite) IMPT- don’t forget because it doesn’t end in “azole”
45
Benazimadoles- name two really important ones
Thiabendazole (ineffective against cestodes and trematodes) FEBANTEL (Pro Drug of fenbendazole!!) only one that doesn’’t end in azole
46
Benzimidazoles clinical use— WITHDRAWL times I.e. fenbendazole in cattle vs pigs
Variable, dep on species and formulation Cattle- 27 days for albendazole, 8 days for fenbendazole Pigs- 0 days for Fenbendazole
47
Name 8 Antiprotozal Agents
``` Pirimethamine Amprolium Clindamycin Metronidazole Triazines (Ponazuril, Diclazuril) Nitrothiazoles (Nitrazoxanide = Navigator ) Sulfonamides/trimetropim Benzimadoles ```
48
Pyrimethamine MOA
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
Folic acid synthesis is important for what
DNA and RNA synthesis
50
Pyrimethamine spectrum of activity
Toxoplasmosis (dogs and cats) Neospora (dogs) Sarcocystis (EPM in horses)
51
Pyrimethamine toxicity
BM suppression
52
Pyrimethamine and sulfas
Used in combination with sulfas (sulfadiazine) for 30-180 days
53
Amprolium MOA
It is a structural analog of thiamine —> competes for thiamine uptake into Protozoal organisms
54
Amprolium Spectrum of activity
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
Amprolium toxicity
Thiamine deficiency (uncommon)
56
Thiamine deficiency — PEM in what species
Cattle, goat, sheep Camelids Deer
57
Polioencephalomalacia signs
Star gazing Anorexia Loss of motor control Coma, death
58
Thiamine deficiency — polyneuritis in what species
Chicken, turkey, pigeons
59
Polyneuritic clinical signs
Star gazing Anorexia, paralysis Death
60
Amprolium pharmaceutical considerations- labeled for what animals
Labeled for food animals ELDU in dogs, cats, other animals has occurred

Clinical Pharmacology (7 decks)

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