Antifungals, Antiprotozoals, Antivirals, Paraciticides Flashcards

1
Q

What are the mechanisms of action of the antifungal agents?

A
  • Amphotericin B binds ergosterol to form pores
  • Azoles inhibit ergosterol synthesis
  • Griseofulvin and Fenbendazole bind microtubules to inhibit mitosis
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2
Q

What are the mechanisms of action of the antiprotozoal agents?

A
  • Folate acid synthesis inhibitors: Blocks successive steps in folate synthesis of protozoa needed for protein/NA metabolism
  • Metronidazole: reduced metabolite causes breakage of DNA
  • Clindimycin: binds 50s ribosome to disrupt protein synthesis
  • Amprolium: Thiamine analog
  • Ponazuril: Activity against important organelles
  • Nitazoxanide: Interferes with pyruvate:ferrodoxin oxidoreductase enzyme (PFOR) essential for anaerobic energy reactions (same pathway that metronidazole requires)
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3
Q

What are the mechanisms of action of the antiviral agents?

A
  • AZT: inhibits reverse transcriptase
  • Purine nucleoside analogs: Analogue of guanosine- inhibits viral DNA polymerase
  • L-lysine: competes with arginine, herpesvirus needs to make proteins
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4
Q

What are the most important side effects of the antifungal agents?

A
  • Amphotericin B- Very Nephrotoxic, acute anaphylactic reactions
  • Azoles- GI (mild) and rare hepatotoxicity
  • Griseofulvin- Common, Cats most serious side effects: neutropenia,
    anemia, neurotoxicosis
  • Fenbendazole- OFF LABEL use for dermatophytes in LA
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5
Q

What are the most important side effects of the antiprotozoal agents?

A
  • Folic Acid Synthesis Inhibitors: Bone marrow suppression, Keratoconjunctivitis sicca, teratogenic
  • Metronidazole: Carcinogenic/mutagenic! BANNED FOOD ANIMALS!
  • Clindimycin: DO NOT USE IN HORSES,RUMINANTS, RODENTS,
    LAGOMORPHS- Serious GI side effects that can cause death
  • Amprolium: Thiamine deficiency Polioencephalomalacia high doses
  • Ponazuril: Few
  • Nitazoxanide: disrupts normal GI flora, some deaths caused by
    enterocolitis reported, laminitis
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6
Q

What are the most important side effects of the antiviral agents?

A

AZT:cats–anemia

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7
Q

What are the distinguishing differences in the pharmacokinetics of the antifungal agents?

A
  • Amphotericin B not water soluble- IV or topical only
  • Azoles- oral or topical
  • Griseofulvin accumulates in keratin (skin, nails, etc), need to administer for extended lengths for effect
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8
Q

What are the spectrum of activity of the anti fungals?

A

Amphotericin B is most effective against all EXCEPT ringoworm (dermatophytes), Azoles have wide spectrum, Griseofulvin DERMATOPHYTES ONLY, Fenbendazole OFF LABEL for dermatophytes in Large Animals

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9
Q

What are the major indications for use for the anti-protozoal agents?

A
  • Folic acid inhibitors: aerobic organisms
  • Metronidazole: anaerobic only, Entamoeba, Trichomonas, Giardia
  • Clindimycin: Toxoplasmosis
  • Amprolium: Coccidiosis in food animals
  • Ponazuril: Sarcocystis neurona horses (EPM), off label SA coccidiosis
  • Nitazoxanide: EPM in horses
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10
Q

What are the indications for use of antivirals?

A
  • AZT: retroviruses (FIV, FeLV)
  • Purine analogs: Herpesviruses
  • L-lysine: cats with Herpes conjunctivitis
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11
Q

Which antiviral agent is not a drug?

A

L-lysine is a nutritional supplement

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12
Q

What drug should you use to treat a nematode infection?

A

Fenbendazole (Benzimidazole), Pyrantel (nicotinic anthelmintic), Ivermectin (Macrocyclic Lactone)

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13
Q

What drug should you use to treat a trematode infection?

A

Fenbendazole (Benzimidazole)

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14
Q

What drug should you use to treat a cestode infection?

A

Praziaquantel (Isoquinolone)

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15
Q

What drug should you use to treat a flea infestation?

A

Permethrin (Synthetic pyrethroids), Fluralaner (Isoxazolines)

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16
Q

What drug should you use to treat a tick infestation?

A

Permethrin (Synthetic pyrethroids), Fluralaner (Isoxazolines)

17
Q

What drug should you use to treat a mite infestation?

A

Ivermectin (Macrocyclic Lactones), Permethrin (Synthetic pyrethroids)

18
Q

What should you use to treat a bot infestation?

A

Ivermectin (macrocyclic lactone)

19
Q

What is the MOA of the Benzimidazoles?

A
  1. Bind to and inhibit tubulin
  2. Inhibit mitochondrial enzyme function
20
Q

What is the MOA of the Macrocyclic lactones?

A

Causes FLACCID PARALYSIS in 2 ways:
1.Hyperpolarize parasite neurons
2.At synapses enhance release of GABA

21
Q

What is the MOA of the Nicotinic anthelmintics?

A

Cause ACh release, Continued depolarization
RIGID paralysis

22
Q

What is the MOA of the Isoxazolines?

A

Acts at neuron chloride channels
RIGID paralysis

23
Q

What is the MOA of the Isoquinolones?

A

Isoquinolones 2 MOAs:
1- Destroy cestode tegument
Exposes parasite antigens so Host’s GI/immune system destroy worm
2- Paralyze the parasite- RIGID paralysis

24
Q

What is the MOA of the Synthetic pyrethroids?

A

Acts @ presynaptic sodium channels
RIGID paralysis

25
Q

What are the parmacokinetic factors to consider when using Parasiticides?

A

Fluralaner Long 1/2 life- longer duration between oral treatments-~12 wks

26
Q

What are the major adverse effects, contraindications and safety features of the Benzimidazoles?

A

Adverse effects uncommon- high margin of safety
Safe for use during pregnancy
Hypersensitivity reaction
Antigens released by dying parasites

27
Q

What are the major adverse effects, contraindications and safety features of the Macrocyclic lactones?

A

Hypersensitivity reaction- Antigens released by dying parasites
Neurologic signs if crosses blood brain barrier
Sensitivity in collie & herding breeds- p-glycoprotein

28
Q

What are the major adverse effects, contraindications and safety features of the Nicotinic anthelmintics?

A

Adverse effects uncommon- good safety margin
Poorly absorbed from GI tract (Added safety)
Possible vomiting

29
Q

What are the major adverse effects, contraindications and safety features of the Isoxazolines?

A

Neurologic including Seizures*
*Do not use in patients with history of seizures

Gastrointestinal

30
Q

What are the major adverse effects, contraindications and safety features of the Isoquinolones?

A

Adverse effects uncommon- Wide margin of safety
Possible gastrointestinal upset
Injectable formulation: pain with injection

31
Q

What are the major adverse effects, contraindications and safety features of the synthetic pyrethroids?

A

Relatively safe for most mammals
EXCEPTION: TOXIC for CATS Metabolized via glucuronidation in liver
Note: OK to use products specifically labeled for cats
Toxicity - Neurological signs