ISOQUINOLIN AND BENZAZEPIN DERIVATIVES

Question 1

SUBSTANCES

Answer 1

Praziquantel and Epsiprantel (closely related analogs)

Question 2

MECHANISM OF ACTION

Answer 2

Induction of spastic paralysis in the parasite. Primarily action is on neuromuscular coordination, by interfering with the regulation of intracellular Ca2+ concentrations, impairing both motility and function of the suckers of the cestode.

Question 3

ANTHELMINTIC SPECTRUM

Answer 3

• Anticestodal effect (against tapeworms).
• High efficacy against mature and larval stages including Echinococcus spp.* and against certain trematodes (blood flukes).
• No effect on nematodes, liver fluke

Question 4

PHARMACOKINETIC FEATURES

Answer 4

• Rapid and almost complete absorption from the GI
• Distribution to all organs (re-enter gut lumen via bile and mucosa)
• Rapid hydroxylation into inactive forms in the liver and secretion in bile.

SIDE-EFFECTS
- Wide safety margin, practically non-toxic (TI=50).

Question 5

APPLICATION

Answer 5

Praziquantel
Ru (eg. Moniezia spp., Stilesia ) PO 3.75 mg/kg
Horses (Anoplocephala perfoliata ) PO 1 mg/kg
Poultry (waterfowl) PO 5-10 mg/kg
Cats and Dogs PO (5 mg/kg) or SC (5.8 mg/kg) (10 mg/kg)

Epsiprantel
5 mg/kg (dog) Against Echinococcus spp

Question 6

PRAZIQUANTEL

Answer 6

+ IVERMECTIN

+ MOXIDECTIN