B-25. Anthelmintics (salicylanilides, substituted phenols, isoquinolines, clorsulon, monepantel, emodepside) Flashcards
Must know drugs isoquinolones
Praziquantel
Drugs salicylamides
Closantel
Oxyclosanide
Niclosamide
Drugs of substituted phenols
Nitroxinil
diamphenethide
Mode of action of salicylamides
Vermicidal, allows H+leakage into mitochondria
Mode of action of substituted phenols
Vermicidal, allows H+ into mitochondria
Diamphenetide spectrum
Unique high activity against youngest immature fluke stages
Salicylamides & substitute phenols spectrum
For sheep & cattle against : fasciolosis & haemonchosis
For 6 week old fluckes
AC & AN
Salicylamides & substituted phenols drugs acting as AN
Closantel
Oxyclosanide
Nitroxinil
Salicylamides & substituted phenols having AC activity
Nitroscanate
Dichlorophen
Nicliosamide
Pk of Closantel
Long half life
Excr: bile & faeces
Residues detected in liver for WEEKS
PK of Oxyclozanide
Long half life
Excr: bile & faeces
Residues detected in liver for WEEKS
Nitroxinil PK
Destroyed by rumen bact, has to be given SC
Metabolism of diamphenetide
Gut & liver
Toxicity of salicylamides & substituted phenols
Not safe (low ti)
Normal dose: anorexia, unformed faeces
High dose: blindness, hyperthermia, convulsions, death
Administration route of salicylamides & substituted phenols
All PO except Nitroxinil (SC)
Isoquinolone drugs
Praziquantel & Epsiprantel
Mode of action of isoquinolones
Interfere with IC calcium —> spastic paralysis
Spectrum of isoquinolones
AC & AT (not liver flukes)
High efficacy against matur & larval stages
Resistance of isoquinolones
Liver flukes
ADME of isoquinolones
A: rapid & complète from GI
D: all organs
M: hydroxyl action into inactive form in liver
E: bile
Administration routes of praziquantel
PO: Ru, Eq, poultry, Ca, Fe
SC: Ca, Fe
Administration route of epsiprantel
SC: Ca
Indication of Epsiprantel
Echinococcus
Clorsulon
Mode of action, pk, administration
Inhibition of glycosidic pathway in LIVER FLUKES
safe, plasma bound
PO: Sheep ; SC: bovine (combined with ivermectin)
NOT FOR DAIRY CATTLE
Monepantel
Mode of action
Toxicity
Spectrum
PK
Agonist nAch receptor
Safe
Narrow, GI nematodes (includes hypobiotic larvae)
Abs: Good ; excr: faeces
Emodepside:
Mode of action
Spectrum
Combination
Inhibition of synaptic transmission
GI nematodes, roundworm, hookworms
Cats: combo Praziquantel (topical)
Dogs: combo Praziquantel (PO)
Puppies: Toltrazuril