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132 Cards in this Set
- Front
- Back
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What are 6 lung worms that fenbendazole are effective against?
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1) Aelurostrongylus
2) Crenosoma vulpis 3) Paragominus 4) Capillaria 5) Filaroides 6) Angiostrongylus vasorum |
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What kind of drug is febantel?
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Prodrug-metabolized to fenbendazole and oxfendazole
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What is the only form that febantel is available in?
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Only available in combination with praziquantel and pyrantel= drontal plus
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What is the spectrum of activity of febantel? (3)
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1) Roundworms
2) Hookworms 3) Whipworms (dogs) |
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What is the mechanism of action of tetrahydropyrimidines?
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Nicotinic agonists
-Act selective on parasite Ach receptor -Causes depolarization--> contraction and tonic paralysis |
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How is pyrantel administered?
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Well absorbed orally
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When does the peak plasma concentration of pyrantel occur?
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3-6 hours
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What are the adverse effects of pyrantel in small animals?
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Well tolerated and safe
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What is the spectrum of activity of pyrantel? (3)
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1) Roundworms
2) Hookworms 3) Physaloptera |
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Pyrantel has synergistic activity with _______.
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Febantel
--> increased activity against hookworm and whipworm |
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What are the 2 advantages of piperazine? Disadvantage?
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Safe
Inexpensive -Only active against roundworms |
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What is the only arsenical anthelmintic approved in the US?
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Melarsomine
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What is the spectrum of activity of melarsomine?
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92-98% efficacy against adult heartworm in dogs
-Contraindicated in cats |
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How is melarsomine administered?
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Deep IM injection
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What are the 2 dosage intervals used to administer melarsomine? What's the advantage/disadvantage of each?
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1) 2 injections 24 hours apart
-Low risk of thromboembolism 2) 3 injections -Single injection followed by the 2 standard injections -High risk of thromboembolism |
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When are the peak concentrations of melarsomine established? Half life of melarsomine?
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Peak blood levels in 11 minutes
-Half life: 3 h |
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1/3 of dogs injected with melarsomine develop a _______ reaction.
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Local injection
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What are 7 adverse effects of melarsomine?
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1) Increased liver enzymes
2) Coughing 3) Gagging 4) Anorexia 5) Fever 6) Pulmonary congestion 7) Vomiting |
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What is the therapeutic index of melarsomine like?
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Very narrow therapeutic range
-Parasite removal by poisoning the patient just enough to kill the parasite... |
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What are 3 external parasiticides that are only used in dogs?
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1) Spinosad (Comfortis)
2) Amitraz + metaflumazone (Promeris) 3) Milbemycin + lefenuron (Sentinel) |
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What are the 2 groups of antiparasitic drugs that are macrolides?
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1) Avermectins
2) Milbemycins |
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What are 2 avermectins used in small animal medicine?
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1) Ivermectin
2) Selamectin |
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What are 2 milbemycins used in small animal medicine?
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1) Milbemycin
2) Moxidectin |
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What is the structure of ivermectin? Selamectin?
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Ivermectin: dissacharides
Selamectin: monosaccharides |
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How does the structure of milbemycins vary from avermectins?
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No sugar substituents
(Ivermectin-disaccharide, selamectin-monosacharide) |
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What are the 2 common mechanisms of action in avermectins and milbemycins?
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1) Agonists of glutamate-gated-Cl-channel-->
-Muscle hyperpolarization -Flaccid paralysis 2) Agonists of GABA-gated-Cl-channel--> -Muscle hyperpolarization -Flaccid paralysis |
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Why aren't the glutamate-gated-Cl-channels of mammalian cells affected by avermectins and milbemycins?
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The channel targeted isn't present in mammals
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Why aren't the GABA-gated-Cl-channels of mammalian cells affected by avermetins and milbemycins?
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Blood-brain barrier protects mammals
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What is the spectrum of activity of ivermectin in small animals? (3)
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1) Roundworm
2) Hookworm 3) Heartworm -Prevention -Microfilaricide (dogs -Adulticide (w/ doxycycline) |
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What is the spectrum of activity of selamectin in small animals? (3)
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1) Roundworm
2) Hookworm (cats) 3) Heartworm -Prevention |
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What is the spectrum of activity of milbemycin in small animals? (4)
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1) Roundworm
2) Hookworm 3) Whipworm (dogs) 4) Heartworm -Prevention -Microfilaricide (dogs) |
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What was the first commercially-available macrolide?
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Ivermectin
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What is oral absorption of ivermectin like?
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Rapid oral absorption
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When are peak plasma concentrations of Ivermectin established?
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Peak: 4-10 h
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What is the half life of ivermectin?
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1.8 days
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What are 6 adverse effects of ivermectin?
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1) Mydriasis (>2.5 mg/kg)
2) Tremors (>5 mg/kg) 3) Stupor to coma 4) Ataxis 5) Seizures 6) Death (>40 mg/kg) |
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What is the LD50 of ivermectin?
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80 mg/kg
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Why are some dogs sensitive to ivermectin?
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MDR gene mutation interferes with metabolism and allows drug to get through BBB to CNS
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What are 5 breeds of dogs that have the MDR gene mutation and ivermectin should not be used in?
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1) Collies (70%)
2) Longhaired whippet (65%) 3) Australian shepherd (50%) 4) Shetland sheepdog (15%) 5) German shepherd (15%) |
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Compare the dose of ivermectin needed for prevention and microfilaricide compared to killing worms.
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Prevention and microfilaricide: 0.05 mg/kg
Worms: 0.2-0.6mg/kg |
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Compare the dose of ivermectin neded for heartworm prevention compared to lung worms (Aelurostrongylus).
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Prevention: 0.024 mg/kg once monthly
Aelurostrongylus: 0.4 mg/kg once |
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What is the only macrolide approved for internal and external parasites?
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Selamectin
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What is the heartworm prevention of choice in collies?
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Selamectin
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True or false. Selamectin is effective against Aelurostrongylus in cats.
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True
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What is the bioavailability of selamectin in dogs? cats?
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Dogs: 4%
Cats: 74% |
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What is the half life of topical selamectin administration in dogs & cats?
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Dogs: 11 d
Cats: 8 d |
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What are the pharmacokinetics of milbemycin (absorption, peak, half life)?
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Similar to ivermectin
-Rapid oral absorption -Peak concentration: 4-10 h -Half life: 1.8 d |
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What are 5 uses of milbemycin at 0.5mg/kg in dogs?
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1) Heartworm prevention (cats too) & microfilaricide
2) Roundworms, hookworms, whipworms 3) Baylisascaris procyonis (raccoon roundworm) in dogs 4) Pneumonyssoides caninum (nose mites) 5) Demodicosis |
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What is a use of milbemycin at 2 mg/kg?
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Sarcoptes scabiei
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What dose of milbemycin is well tolerated? in collies?
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200 mg/kg
Collies: 10 mg/kg |
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In small animals, moxidectin is formulated with _______.
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Imidacloprid
-ProHeart 6 is available only through a restricted distribution program |
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What is the oral absorption of moxidectin like? Peak concentrations? Half-life?
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-Rapid oral absorption
-Tmax at 2-3 hours -Elimination half-life: 19 days |
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What are 2 isoquinolones that are closely-related cesticides?
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1) Praziquantels
2) Epsiprantel |
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What is the mechanism of action of isoquinolones?
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-Increases cell membrane permeability to calcium-->
Loss of intracellular calcium--> Contraction and paralysis -vacuolization and destruction of protective tegument |
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Praziquantel has marked activity against what 3 parasites?
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1) Dipylidium
2) Taenia 3) Echinococcus |
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What is oral absorption of praziquantel like?
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High oral bioavailability, but marked first pass effect
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True or false. Praziquantel is highly protein bound.
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True
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What is the oral half-life of praziquantel?
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30 m to 3 h
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True or false. Praziquantel has a narrow therapeutic index.
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False, very safe drug
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Epsiprantel is similar to which drug?
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Praziquantel
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What is the oral absorption of epsiprantel like?
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Poorly absorbed orally
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What is the spectrum of activity of epsiprantel?
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Active against Dipylidium & taenia
-Potentially against Echinococcus: data insufficient to recommend a dosage that will clear the infection |
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How is epsiprantel administered?
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Oral film-coated tablet
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What are the 3 advantages of broad spectrum combinations of antiparasitics?
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1) Increased spectrum
2) Easier administration 3) Client satisfaction |
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What animal is emodepside + praziquantel used in?
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Spot-on product for use in cats that comes in prefilled applicators
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What animals is Emodepside + praziquantel used in?
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Cats & kittens > 8 weeks of age
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What is the spectrum of activity of Emodepside + praziquantel? (3)
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1) Roundworms
2) Hookworms 3) Tapeworms |
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What are the active ingredients of Virbantel and Drontal?
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Pyrantel + praziquantel
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What is the spectrum of activity of virbantel and drontal (pyrantel + praziquantel)? (3)
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1) Tapeworms (Taenia, dipyllidium, echinococcus)
2) Roundworms 3) Hookworms |
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What is different about feline and canine drontal dosing?
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Dogs get 5 mg/kg of both pyrantel and praziquantel
Cats get 5mg/kg of pyrantel and 20mg/kg of praziquantel |
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What are 2 situations where Drontal should not be administered to a cat?
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Cats weighing less than 0.8 kg
Kittens younger than 4 weeks of age |
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What are the 3 active ingredients of Drontal Plus?
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1) Pyrantel
2) Praziquantel 3) Febantel |
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What is the spectrum of activity of Drontal plus? (4)
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1) Tapeworms (including Echinococcus)
2) Roundworms 3) Hookworms 4) Whipworms |
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What are 3 contraindications for Drontal Plus?
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1) Pregnant dogs
2) Dogs weighing less than 1 kg 3) Puppies younger than 3 weeks of age |
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Why is pyrantel combined with Ivermectin?
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To provide activity against hookworms and roundworms
-Ivermectin dose=heartworms |
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True or false. Ivermectin + pyrantel is safe to use in collies.
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True
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Why can't ivermectin + pyrantel kill GI parasites?
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Ivermectin is too low of a dose for GI parasites
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How often is Ivermectin + pyrantel administered?
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Given at monthly intervals during heartworm season
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Why is praziquantel added to ivermectin + pyrantel?
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To provide activity against tapeworms
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What are 5 external parasiticides used in small animals?
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1) Macrolides
2) Phenylpyrazoles 3) Neonicontinoids 4) Spinosads 5) Insect-growth regulators (IGR) |
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Macrolides are potent _________, but are also active against _______.
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Potent anthelmintics
Active against arthropods: insects, mites, ticks |
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What are 3 macrolides that are effective against external parasites?
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1) Ivermectin
2) Selamectin 3) Milbemycin |
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What are the 4 external parasites that ivermectin is effective against?
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1) Canine & feline scabies
2) Demodicosis 3) Cheyletiellosis (type of mite) 4) Ear mites |
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What are 2 external parasites that milbemycin is effective against?
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1) Canine & feline scabies
2) Demodicosis |
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What are 5 external parasites that selamectin is effective against?
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1) Canine & feline scabies
2) Ear mites 3) Ticks 4) Fleas 5) Lice |
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All 3 macrolides (Ivermectin, selamectin, milbemycin) have activity against what external parasite?
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Canine & feline scabies
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What is the mechanism of action of Fipronil?
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Inhibits GABA-regulated chloride flux
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What is the spectrum of activity of fipronil (Frontline)?
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-Flea adulticide
-Activity against ticks & lice |
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What are the 2 routes of administration available for fipronil?
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1) Spray
2) Spot-on (frontline) |
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What is the mechanism of action of neonicotinoids?
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Act selectively on insect acetylcholine receptor (nAChR)
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What are 2 anti-parasitics that have a mechamism of action that acts on parasite Ach receptor (nAChR)?
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1) Tetrahydropyrimidines (nicotinic agonist=nematodicide)
2) Neonicotinoids |
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What are 2 neonicotinoids?
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1) Imidacloprid
2) Nitenpyram |
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How is Imidacloprid administered?
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Spot-on application for dogs and cats
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What is the spectrum of activity of imidacloprid (Advantage)?
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Adulticidal activity against fleas
-Lasts up to 4 weeks |
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Imidacloprid has a therapeutic margin of at least ____-fold.
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20 fold
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How is Nitenpyram administered?
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Oral product for dogs & cats
-Rapid absorption |
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What is the half life of Nitenpyram in dogs? Cats?
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Dogs: 2 hours
Cats: 16 hours |
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What is the spectrum of activity of nitenpyram?
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100% activity against adult fleas
for 24 hours |
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How is Spinosad administered? What's its spectrum of activity?
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Oral product to control fleas in dogs only
-No activity against ticks |
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Spinosad is not to be used in combination with _______.
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Ivermectin
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How old do dogs have to be to use Spinosad?
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> 14 weeks of age
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What is the spectrum of activity of IGR? Mechanism of action?
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Controls early stages of flea metabolism, morphogenesis and reproduction
-NO direct adulticidal activity -Interrupt environmental stage of flea life cycle |
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IGR is usually combined with an ______.
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Adulticide
e.g. Advantage=pyriproxifen + imidacloprid |
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What are 3 IGRs?
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1) Lufenuron
2) Methoprene 3) Pyriproxifen |
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What is the mechanism of action of lufenuron?
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Inhibits synthesis and deposition of chitin within the ova and larval exoskeleton of developing fleas
-Taken up by the feeding flea and incorporated into the developing egg |
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What is the mechanism of action of methoprene?
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Flea juvenile hormone analog
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What is the mechanism of action of pyriproxifen?
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Juvenile hormone mimetic for fleas
-In advantage with Imidacloprid |
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How is amitraz + metaflumazone administered? What animal?
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Spot-on product for dogs > 8 weeks of age
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What are the 3 uses of amitraz + metafluazone?
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1) demodicosis
2) fleas 3) ticks -Market name=Promeris |
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Milbemycin + lufenuron is approved for use in _______.
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Dogs
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What is the spectrum of activity of milbemycin + Lufenuron in dogs? (5)
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1) Heartworm prevention
2) Hookworms 3) Roundworms 4) Whipworms 5) Controls fleas |
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Why is imidacloprid added to moxidectin?
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Imidacloprid is added for flea control
-All together covers: round worms, hook worms, whip worms, heart worms, ear mites, fleas |
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True or false. Imdacloprid + moxidectin is a product only approved for use in dogs.
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False, there is a feline product, but the canine product CANNOT be used in cats.
Marketed as: Advantage-multi |
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What is the spectrum of activity of Imidacloprid + moxidectin? (6)
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1) Heartworm prevention
2) Roundworms 3) Hookworms 4) Whipworms (dogs) 5) Fleas 6) Ear mites (cats) -Marketed as: Advantage-multi |
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What is a very common cause of large bowel diarrhea in adult dogs?
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Whipworms
-So deworm a dog with diarrhea before performing endoscopy |
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What are 4 nematicides used in small animal medicine?
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1) Macrolides
2) Benzimidazoles 3) Tetrahydropyrimidines 4) Arsenicals |
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What is 1 cestocide used in small animal medicine?
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Isoquinolones
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What are 2 reasons that parasites are important in veterinary medicine?
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Zoonosis
Disease e.g. whipworms cause diarrhea in adult dogs |
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Benzimidazoles are a large family of _____ spectrum agents.
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Broad
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What is the mechanism of action of benzimidazoles?
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Bind to beta-tubulin--->
inhibits tubulin polymerization in susceptible helminths (nematicide) |
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Why are benzimidazoles so safe to use in mammals?
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25-400 fold lower inhibition constant for mammalian tubulin
-So takes HIGH dose to damage mammal tubulin |
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How are benzimidazoles administered in small animals? How often?
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Poorly soluble, given by mouth
-Faster GI transit in SAs, so requires multiple dosing (3 or more days) |
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True or false. Benzimidazoles are commonly used in small animal medicine.
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False, except still use albendazole, but causes GI issues so only use when really needed
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True or false. Albendazole in small animals is extra label use.
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True
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What is oral absorption of albendazole like?
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Well absorbed orally
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What are 4 adverse effects of albendazole?
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1) Teratogenic
2) Myelosuppression 3) Ataxis 4) *Vomiting & diarrhea |
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What is the spectrum of activity of albendazole? (4)
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1) Roundworms
2) Hookworms 3) Lungworms 4) Capillaria plica |
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What is the spectrum of activity of fenbendazole? (5)
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1) Roundworms
2) Hookworms 3) Whipworms (Dogs) 4) Lungworms 5) Giardia |
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What age does a dog have to be in order to use fenbendazole?
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Approved for use in dogs 6 weeks of age or older
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What are the adverse effects of fenbendazole?
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Rare cases of bone marrow hypoplasia
-Very safe drug |
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How long does fenbendazole have to be given to kill intestinal worms in dogs & cats? For giardia
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Dogs: 3 days
Cats: 5 days Giardia: 5 days |
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What drug can be used to treat Baylisascaris procyonis infection in a dog?
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Milbemycin (0.5 mg/kg)
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