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Pharm 2- Anthelmintics 3

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kelseyfmeyer's version from 2015-05-10 01:45

Anticestodal drugs (TAPEWORMS)

Question Answer
Taeniacides do what?kill the tapeworm
Taeniafuges do what?induce tapeworm expulsion
Dichlorophen is for what?tx cestode AND nematode infection in SM ANIMALS!
MOA of dichlorphen?acts by uncoupling oxidative phosphorylation–inhibiting ATP production
Resorantel is used for treating what in who?RUMINANTS with cestodes and ALSO RUMEN FLUKES(trematodes)!
which drug tx RUMNANT FLUKES and cestodes in rumis?Resorantel
what is praziquantel effective against?wide spectrum of activity-- adult and larval cestodes & trematodes
MOA of praziquantel? influences Ca++ion flux across the parasite surface membrane--> effects cell membrane integrity...cell surface swelling--->leads to formation of several sm vacuoles, which inc in size and burst open (then eosinophilic granules get in and lyse the parasite)
Praziquantel absorption (admin) and distribution?rapid/complete absorpton into systemic circ from oral admin. widely distributed so good against adult AND larval cestodes
metabolism/excretion of praziquantel?rapid metabolism in liver, excretion in urine
spectrum of praziquantel, in who?safe for ALL ANIMALS, kills adult AND larval cestodes, and trematodes
Epsiprantel MOA?similar to praziquantel, Ca++ ion induced tetanic contraction.....damages the tegument of the tapeworm –lysis and digestion by the host
epsiprantel kills what in who?ONLY CESTODES in SMALL ANIMALS
how is the absorption of epsiprantel? where is it excreted?LOW absorption from GIT (unlike prazi), and is excreted in the feces (since it wasnt absorbed)
can BZDs help with cestodes/trematodes?yes, the substituted ones--> mebendazole, fenbendazole, oxfendazole, albendazole
what is Anaplocephala perfoliata? who does it affect? what is the best treatment?Ileocecal tapeworm in horses! pyrantel pamoate is the most effective tx
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anti-trematodal drugs

Question Answer
what is Fasciolicidal?effective against flukes (trematodes)
Bithionol sulfoxide is used for what?Rumen flukes & liver flukes of ruminants
*Nitroxynil is used in who? for what?sheep and cattle. Trematodes (liver flukes), and ****Ivermectin and BZD resistant Haemonchus contortus of sheep
Rafoxanide is for treating what? in who?sheep and cattle....for ADULT AND IMMATURE FLUKES
MOA of rafoxanide?Proton ionophore–transports cationacross cell membranes (changes ion conc). Uncoupling oxidative phosphorylationin parasitic mitochondria ATP production is inhibited
unique pharmacokinetics of rafoxanide?NO metabolism, 99% plasma protein bound so there is a LONG HALF LIFE- 16days- BROAD SPECTRUM ACTION against mature and immature trematodes
Closantel MOA?Proton ionophore; uncoupling of oxidative phosphorylation inhibits ATP production
use closantel agaist what, in who?liver flukes and ********Effective against resistant strain of H. contortus*****
which is the MOST EFFECTIVE DRUG against resistant strains of H. contorus?closantel
pharmacokinetics of closantel? (what it does in body, binding, half life, excretion)99% plasma protein bound!--> super long half life (~14days.) excreted in feces
Oxyclozanide is for what?RUMAN flukes
Clorsulon is used for what (whats unique about it)FDA approved for liver fluke infestations
MOA of clorsulon?affects glycolytic enzymes of F. hepatica –blocks glycolytic pathway fluke deprives of energy
contraindication for clorsulon?OCCURS IN TISSUES AND MILK! so need withdrawal period
what is in IvomecPlus?clorsulon and ivermectin
which benzimidazoles are fasciolicidal?Albendazole, Fenbendazole, Triclabendazole, Netobimin (prodrug for albendazole)
which BZD does prophylactic tx against liver flukes?Albendazole
**which BZD is ONLY for antitrematodes????Triclabendazole
in what two ways is Triclabendazole extra good against flukes?(1) Active metabolite (Triclabendazole sulfoxide) is bound to plasma protein for 7 days (2) excreted in BILE which inc exposure of flukes to the drug
**which drug is 100% effective against IMMATURE (liver) flukes?Diamphenethide
MOA of diamphenethide?liver metabolism--> amine metabolite (liver)--> this is ACTIVE against the flukes, and is in the liver! (affects their integument)
what would be the ideal fasciolocide ( for acute fasciolosis) against liver flukes?diamphenethide for flukes 1day-10wk old, and also rafoxanide for 4wk old-adult
what is Paramphistomosis?the disease caused by infestation of ruminants with stomach (RUMEN) flukes.
which stage of the rumen fluke is the worst?immature stages
how can you treat Paramphistomosis?Resorantel, bithionol, combination of oxyclozanideand oxfendazole
what is Paragonimiasis?lung fluke infection
how do you treat Paragonimiasis?Albendazole(cats and dogs) and fenbendazole(dogs) (also Bithionol and Praziquantel)
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Question for the rest

Question Answer
MOA of heartworm adulticides (name drugs too)HAVE ARSENIC! (Thiacetarsamide sodium and melarsomine)
MOA of dichlorphen? ( what drug category?)acts by uncoupling oxidative phosphorylation–inhibiting ATP production (anti cestodal- aka tapeworm)
MOA of praziquantel? (what drug category?)(anti cestodal- tapeworm) influences Ca++ion flux across the parasite surface membrane--> effects cell membrane integrity...cell surface swelling--->leads to formation of several sm vacuoles, which inc in size and burst open (then eosinophilic granules get in and lyse the parasite)
MOA of rafoxanide? (what drug category?)(anti trematodal) Proton ionophore–transports cationacross cell membranes (changes ion conc). Uncoupling oxidative phosphorylationin parasitic mitochondria ATP production is inhibited
MOA of most of the antitrematodals?inhibit ATP production
Drugs acting on immature flukes, MOA?diamphenathide! liver metabolism--> amine metabolite (liver)--> this is ACTIVE against the flukes, and is in the liver! (affects their integument)
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