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120 Cards in this Set
- Front
- Back
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What are the six carbamate benzimidazoles?
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albendazole, fenbendazole, mebendazole, oxfendazole, oxibendazole, parbendazole
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What is the difference between thiazoles and carbamates?
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carbamates have a greater activity with a decreased dose requirement than thiazoles
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What are two thiazoles?
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thiabendazole and cambendazole
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What group of benzidazoles have larvicidal activity?
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thiazoles
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What are the probenzimidazoles? (3)
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netobimin, fenbantel and thiophanate
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What is Netobimin metabolically converted into?
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albendazole
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What is Fenbantel metabolically converted into?
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fenbendazole
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What kind of drugs are benzimidazoles?
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anti-nematodal
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What is the mechanism of action of benzimidazoles?
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bind to nematode microtubule causing a breakdown of structural units of many organelles and a cessation of numerous cellular processes
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What cellular processes are disrupted by benzimidazoles in nematodes as a result of irreversible binding of the microtubles?
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mitosis, protein assembly and energy metabolism
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Does benzinidazoles have side effects?
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No
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What three benzimidazoles have peak concentration in 2-7 hours?
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thiabendazole, flubendazole, and mebendazole
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How is thiabendazole excreted?
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urine and feces
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How long does it take thiabendazole to be metabolized?
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within 72 hours
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How effective is thiabendazole against nematode infestation in horses?
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Highly effective >90%
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What type of anthelmintic are benzimidazoles?
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Anti-nematodal
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How well is Mebendazole metabolized?
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poorly
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How long after administration is Mebendazole excreted?
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24-48 hours
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How is Mebendazole excreted?
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in feces
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What species has hydroxylation of phenol rings resulting in metabolites in mebendazole?
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ruminants
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What are substituted benzimidazoles effective against in ruminants?
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GI nematodes and lungworms
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What are substituted benzimidazoles effective against in swine?
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ALL SWINE PARASITES
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How is albendazole metabolized?
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hepatic metabolism
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What type of metabolite is produced once albendazole undergoes hepatic metabolism?
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active sulphoxide metabolite
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What two species have a higher capacity for metabolizing albendazole so a higher dose is required?
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cattle and goats
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How is albendazole excreted?
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urine
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How is albendazole administered to a sheep?
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intermittent-release bolus
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Why is it good to give fenbendazole on a full stomach in dogs?
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it increases the bioavailability
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What kind of metabolism does fenbendazole go through (hint: same as albendazole)?
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hepatic metabolism
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What metabolite is produced once fenbendazole is metabolized by the liver?
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active sulphoxide metabolite: oxfendazole
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What two species have a higher capacity for fenbendazole so a higher dose is required?
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cattle and sheep
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What two benzimidazoles do sheep and cattle have a higher capacity for so a higher dose is required?
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fenbendazole and albendazole
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How is fenbendazole administered to cattle?
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modified continuous release bolus
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How is oxfendazole administered to cattle?
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intermittent-release bolus or injection directly into rumen
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All benzimidazoles have limited GIT absorption except which three?
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thiabendazole, albendazole and oxfendazole
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Where should plasma levels always be for benzimidazoles regardless of dosage form?
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<1%
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Metabolism by the liver converts some benzimidazoles into what kind of metabolites?
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active
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As a general rule, how are benzimidazoles administered?
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orally
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Are worms resistant to other benzimidazoles susceptible or resistant to probenzimidazoles?
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resistant
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What kind of benzimidazoles are probenzimidazoles converted to?
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benzimidazole carbamates
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What BZD is netobimin converted to?
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albendazole
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What BZD is febantel converted to?
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fenbendazole
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When does febantel reach max plasma concentration in sheep?
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6-18 hours
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When does febantel reach max plasma concentration in cattle?
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12-24 hours
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What is the name of a the commercial drug that is febantel and praziquentel?
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Vercom
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What species is indicated for Vercom?
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dogs and cats
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What two drugs are in Vercom?
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febantel and praziquantel
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What commercial drug is a combination of febantel, pyrantal pamoate and praziquantel?
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Drontal plus
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What species is indicated for Drontal Plus?
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Dogs
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What three drugs are in Drontal Plus?
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febantel, pyrantal pamoate and praziquantel
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What is the withdrawal period for cattle and swine for Febantel?
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35 days
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what is the withdrawal period for sheep for Febantel?
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14 days
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What are the contraindications for Vercom and Drontal Plus and why?
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pregnant dogs and cats because the combination of febantel and praziquental increases the frequency of abortion
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What are three imidazothiazoles?
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butamisole hydrochloride, levamisole, tetramisole
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What isomer of levamisole is responsible for anthelmintic activity?
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l-isomer
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What kind of anthelmentics are imidazothiazoles?
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antinematodal
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What is the mode of action of Levamisole?
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ganglionic stimulant and direct cholinergic drug on nicotinic receptors causing paralysis of the nematode
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Besides an anthelmintic, what other property does levamisole hydrochloride have?
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immune stimulator
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When levamisole is used as a feed additive in ruminants, how much levamisole is used?
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50% levamisole
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What species can be administered levamisole parenterally in the SC?
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cattle
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What is the percent of levamisole in a topical pour-on?
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10%
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What parasites are covered by levamisole in cattle and sheep?
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parasites of the abomasum, mature and immature GI parasites, mature and immature lungworms and eyeworm
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What specific worm is tetramisole indicated for in poultry?
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gapeworm
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Which is safer levamisole or tetramisole?
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levamisole
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At what dose is tetramisole lethal to sheep?
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90mg/kg
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What species is more tolerable to parenteral administration of levamisole: sheep or cattle?
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cattle
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simultaneous administration of what drug with levamisole increases toxicity by lowering LD50?
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pyrantel tartarte
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Which route of administration should levamisole be given to dogs and cats?
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oral
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How long should lactating animals milk not be used for human consumption after treatment with levamisole?
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48 hours
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What is important for the VET to do when administering levamisole?
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wear gloves to prevent percutaneous absorption
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What two drugs are tetrahydropyrimidines?
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pyrantal and morantel
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What kind of anthelmintic are tetrahydropyrimidines?
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antinematodal
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What is the mode of action of pyrantel?
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depolarizing neuromuscular blocking agent and produces sustained muscle contraction followed by paralysis
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What species does not tolerate oral administration of pyrantel?
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cattle
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What route do dogs excrete pyrantel?
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urine
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Besides in dogs, how is pyrantel excreted?
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feces
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Why is pamoate salt given with pyrantel?
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it is poorly absorped so it allows drug to reach lower intestine and act against pinworms
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What two drugs are in Heartgard 30 Plus?
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pyrantel pamoate and ivermectin
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What species is less tolerant of pyrantel tartrate than the pamoate salts?
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horses
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What is the contraindication of pyrantel?
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severely debilitated animals
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What is the difference between morantel and pyrantel?
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morantel is safer and has greater anthelmintic effects
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What is the premix for a sustained release bolus of morantel?
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morantel premix 88
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What is special about morantel in food animals?
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no withdrawel period
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What is the important drug of organophosphates?
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dichlorvos
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What type of anthelmintics are dichlorvos?
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antinematodal
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What is the mode of action of organophosphates?
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irreversible inhibition of acetylcholinesterase causing accumulation of Ach which interferes with neuromuscular transmission and causes sustained muscular contraction and paralysis
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What area of infestation does organophosphates NOT treat in ruminants?
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large intestine
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What is the safety margin for organophosphates?
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narrow
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What should animals not be treated simultaneously with when on organophosphates?
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other AchE inhibiting drugs
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What type of animal is not approved to take organophosphates?
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lactating dairy cattle
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What do you use to treat toxicity of organophosphates?
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atropine and pralidoxime
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What is dichlorvos incorporated into when feeding to monogastric species?
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polyvinyl chloride resin pellets to avoid rapid degradation in proximal alimentary tract
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What is the specific parasite that dichlorvos is effective against that is advantageous?
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whipworms
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What are two major groups of marcocyclic lactones?
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avermectins and milbemycins
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What are macrocyclic lactones active against?
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nematodes and arthropods
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What is the mode of action of macrolide endectocides?
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bind to glutamate-gated Cl channels leading to ion imbalance that is lethal to parasite. acts by increasing release of GABE from synaptosomes and creating a lower affinity reverible binding to GABE related Cl channels leading to flaccid paralysis
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Where is the primary site of action of macrolide endectocides in nematodes?
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synapses between inhibitory and excitatory neurons
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What is the primary site of action of macrolide endectocides in arthropodes?
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myoneural junction
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How does macrolide endectocides interfere with reproduction?
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causes abnormal egg formation and sterility
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What bacteria is milbemycins based on?
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streptomyces avermitilis
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What bacteria are avermectins based on?
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streptomyces avermitilis
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Why do macrolides have a wide margin of safety in mammals?
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because mammalian GABA-mediated neurotransmission occurs in the CNS and macrolides do not cross the BBB in mammals
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what two dog breeds have been known to have macrocyclic sensitivities?
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collies and australian shepherds
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What are two milbemycin drugs?
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milbemycine oxime and moxidectin
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How is milbemycin oxime excreted?
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bile and fecse
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What is a commercially used drug of milbemycin oxime used in cats?
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interceptor flavor tabs
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How are adverse reactions of milbemycine oxime treated?
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with corticosteroids and IV fluids
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How is moxidectin excreted?
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feces
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What is a commercially used moxidectin that is save for ivermectin senstitive collies?
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moxidec
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Can moxidectin be used in pregnant animals?
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yes
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What are the five avermectins?
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ivermectin, abamectin, doramectin, eprinomectin, selamectin
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What administration has the best bioavailability when using ivermectin?
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SC
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what is the main rout of elimination of ivermectin?
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feces- a little in urine
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Is ivermectin transmitted to milk in lactating females?
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yes up to 5%
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What is the withdrawal period for cows lactating or calving once given a controlled-release bolus of ivermectin?
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180 days
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How does toxicity to ivermectin manifest in collies?
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neurological effects to oral administration
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What breed of cattle show toxic effects to ivermectin?
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Murrah gray cattle
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What two species is ivermectin contraindicated in?
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crocodiles and chelonians
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What is a commercially used form of abamectin that is administered subcutaneously?
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avomec
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What is the max dose of abamectin that cows tolerate?
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1mg/kg
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