Pharmacology Flashcards
Describe the mechanism of action for Benzimidazoles ?
Mechanism of action Benzimidazoles
- affects parasite eneergy metabolism preventing nutrient uptake
- Drug binds to nematode tubulin (higher affinity than in mammals)
- inhibits polymerisation of beta subunits of tubulin
- results in mitotic arrest (lethal in rapidly dividing cells)
- or disrupted homeostasis
- worm expulsion
- A high concentraion may inhibit fumerate reductase a nessary enzyme for anerobic respiration.
Provide examples of Benzimidazoles and clinical application in horses ?
Benzimidazoles
Example
Albendazole, triclabendazole, fenbendazole, oxfendazole, oxibendazole, parbendazole and mebendazole
Horse = useful large strongles, small pinworm, ascarids, lung worm,
BZDs combined with other drugs eg piperazine for oxyuris.
Describe the clinical applications of Benzimidazoles in ruminants and pigs ?
Benzimidazoles in ruminants and pigs
- adult and larvae of lung worms
- GI nematodes
- limited activity against whip worms
diposition in these species is affected by oesophageal groove, fasting/ starvation and diet type.
Identify five antinematodal drugs (4) ?
Febantel how does it work ?
Febantel undergoes heptaic metabolism to active fen and oxfendazole.
Describe the clinical application of Benzimidazoles in horses ?
Benzimidazoles in horses
- usefule against adult large strongles
- small pin worm
- ascarids
- lung worm
BZDS combined with other drugs , eg piperazine for immature oxyuris
Describe the pharmacokinetics of binzimidazoles ?
Pharmacokinetics of binzimidazole ?
- poor absorption from the GI tract and variable bioavailability
- a full stomach or fatty meal is reccomened for fenbenzol in dogs
- efficiancy is time dependant (dependant on duration of exposure and this class has minimal residual activity.)
- toxicity is rare - ParBDZ and camBDZ are contraindicated in pregnant animals especially ewes. Withdrawl periods of two weeks for food animals.
Know the effectiveness of Benzimidazoles (table) in dogs and cats ?
Name a benzimidazole which that only has approval as a flukacide ?
Triclabendazole
Describe the mechanism of action of nicontenic anthelminitics and imidazothiazoles ?
Mechanism of action
These drugs selectively bind to and stimulate parasite nicotinic cholingeris (nAChR)
These are L or N type receptors that cause spastic paralysis when stimulated
Exposure to high doses over time may be associated with resistance
Provide examples of Nictinic anthelmintics and imidazothiazoles ?
This group of drugs includes
Tetrahydrppyrimidines = pyrantel and oxantel
Imidazothiazoles = levamisole
Describe the general pharmokinetics of Levamisole ?
Pharmakokinetics of Levamisole
- Aministrated as a drench, bolus, pour on or SC injection.
- rapidly absorbed
- undergoes metabolism
- excreted primarily by the kidneys
Describe the general pharmakokinetics of Pyrantel and Oxantel ?
Pharmakokinetics pyrantel and oxantel
- Embonate salts have low solubility and low systemic availability esp. ruminants
- this may contribute to increased efficacy for GIT nematodes
Describe the clinical applications of Levamisole ?
Clinical application of Levamisole
Levamisole is generally less effective against immature and arrested forms
Ruminant
- abomasal abomasal haemonchus and ostertagia
- small intestine cooperia, trichostrongylus, bunostonum
- large intestine oesophagastomum
- lung worms (mature and immature) dictocaulus
Swine
- ascaris, strongyloides, metastrongylus, stephanurus and oesphagostomum
Poultry
- ascaridia, heterakis, capillaria and oxyspiruria
Dogs and cats
- rarely used low therapeutic index
- Toxocara, Toxoscaris
- vomiting and anemia
Describe the clinical application of Pyrantel and Oxantel ?
Clinical application Pyrantel and Oxantel
Horses
- GI parasites Parascaris, equorum, strongylus
- not effective against strongles Edentates
- ileo caecal tape worm, anoplocephala
Dog
- Not effective against canine whipworm and tapeworm or heart worm
Anthelmentic spectrum in cats dogs and swin is very similar to Levamisole.