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Pharm 2 - Antihelminthics 3

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drraythe's version from 2015-11-22 17:56

Anticestodal drugs (TAPEWORMS)

Question Answer
Taeniacides do what?Kill the tapeworm
Taeniafuges do what?Induce tapeworm expulsion
Dichlorophen is for what?Tx cestode & nematode infxn in SM ANIMALS!
MOA of Dichlorophen?Acts by uncoupling oxidative phosphorylation - inhibiting ATP production
Resorantel is used for Txing what in who?RUMINANTS w/ cestodes & ALSO RUMEN FLUKES (Trematodes)!
Which drug Tx RUMNANT FLUKES & cestodes in rumis?Resorantel
What is Praziquantel effective against?Wide spectrum of activity - adult & 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 ↑ in size & burst open (then eosinophilic granules get in & lyse the parasite)
Praziquantel absorption (admin) & distribution?Rapid/complete absorption into systemic circ from oral admin. Widely distributed so good against adult & larval cestodes
Metabolism/excretion of Praziquantel?Rapid metabolism in liver, excretion in urine
Spectrum of Praziquantel, in who?Safe for ALL ANIMALS, kills adult & larval cestodes, & trematodes
Epsiprantel MOA?Similar to Praziquantel, Ca++ ion induced tetanic contraction.....Dmgs the tegument of the tapeworm –lysis & 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) & is excreted in the feces (since it wasnt absorbed)
Can BZDs help w/ cestodes/trematodes?Yes, the substituted 1s → Fenbendazole, Oxfendazole, Albendazole, Mebendazole (FOAM)
What is Anaplocephala perfoliata? Who does it affect? What is the best Tx?Ileocecal tapeworm in horses! Pyrantel Pamoate is the most effective Tx
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Anti-trematodal drugs

Question Answer
What is Fasciolicidal?Kills flukes (trematodes)
Bithionol Sulfoxide is used for what?Rumen flukes & liver flukes of ruminants
*Nitroxynil is used in who? For what?Sheep & cattle. Trematodes (liver flukes) & ****Ivermectin & BZD resistant Haemonchus contortus of sheep
Rafoxanide is for Txing what? In who?For ADULT & IMMATURE FLUKES in sheep & cattle
MOA of Rafoxanide?Proton ionophore - transports cation across cell membranes (changes ion conc). Uncoupling oxidative phosphorylation in 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 & immature trematodes
Closantel MOA?Proton ionophore; uncoupling of oxidative phosphorylation inhibits ATP production
Use Closantel against what, in who?Liver flukes & ********Effective against resistant strain of H. contortus*****
Which is the MOST EFFECTIVE DRUG (preferred) against resistant strains of H. contortus?Closantel
Pharmacokinetics of Closantel? (What it does in body, binding, half-life, excretion)99% plasma protein bound! → long half-life (~14days) Excreted in feces
Oxyclozanide is for what?RUMEN 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 deprived of energy
Contraindication for Clorsulon?OCCURS IN TISSUES & MILK! So need withdrawal period for food producing animals
What is in IvomecPlus?Clorsulon & Ivermectin
Which Benzimidazoles are Fasciolicidal?Albendazole/Netobimin
Fenbendazole/Fenbantel
Triclabendazole
Which BZD does prophylactic Tx against liver flukes?Albendazole
**Which BZD is ONLY for trematodes????Triclabendazole
In what 2 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 ↑ 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 & is in the liver! (Affects their integument)
What would be the ideal Fasciolocide (for acute fasciolosis) against liver flukes?Diamphenethide for flukes 1day-10wks & also Rafoxanide for 4wks-adult
What is Paramphistomosis?The Dz in ruminants czd by stomach (RUMEN) fluke infestation
Which stage of the rumen fluke is the worst?Immature stages
How can you Tx Paramphistomosis?Resorantel
Bithionol
Combination of Oxyclozanide & Oxfendazole
What is Paragonimiasis?Lung fluke infxn
How do you Tx Paragonimiasis?Albendazole (cats & dogs) & Fenbendazole (dogs) (also Bithionol & Praziquantel)
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Question for the rest

Question Answer
MOA of heartworm adulticides (name drugs too)HAVE ARSENIC! (Thiacetarsamide sodium & Melarsomine)
MOA of Dichlorophen? (What drug category?)Acts by uncoupling oxidative phosphorylation – inhibiting ATP production (anti-cestodal = tapeworms)
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 ↑ in size & burst open (then eosinophilic granules get in & lyse the parasite)
MOA of Rafoxanide? (What drug category?)(Anti-trematodal) Proton ionophore – Transports cation across cell membranes (changes ion conc). Uncoupling oxidative phosphorylation in parasitic mitochondria ATP production is inhibited
MOA of most of the Antitrematodals?Inhibit ATP production
Drug acting on immature flukes, MOA?Diamphenathide!
Liver metabolism → amine metabolite (liver) → this is ACTIVE against the flukes & is in the liver! (Affects their integument)
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