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Helminths

Parasitic worms
Inhabit GI tract and other tissues and organs
of livestock
Classified into:
Roundworms (Nematodes)
Tapeworms (Cestodes)
Flatworms (Trematodes)

Helminth infection
Emaciation/debilitation
Anemia
Reduced productivity (milk, egg and meat
production)
Poor weight gain despite good appetite
Damage to vital organs
Intestinal or lymphatic obstruction

Chronic diarrhea, progressive emaciation and weight


loss despite good appetite

Fasciola hepatica (Liver fluke) invades liver


and bile duct

Anthelmintics or De-wormers
Available formulations:
Suspensions (meant for drenching)
Tablets
Pastes (e.g., Ivermectin for horses)
Injectable solutions

Anthelmintics
Avoidance of drug resistance
Careful diagnosis of worm infestation
By means of faecal examination
Or clinical signs manifested by the animal
Optimal withdrawal period

1. Benzimidazoles
Constitute the most frequently used group of
broad spectrum vermicidal drugs
Thiabendazole
Albendazole
Fenbendazole
Oxfendazole
Mebendazole
Triclabendazole
Cambendazole

Pro-drugs
Febental----- Fenbendazole & Oxibendazole
Netobimin ----- Albendazole
Bind to -tubulin (a structural protein) and
block the polymerization of tubulin into
microtubulin
Continual depolymerization at the other end
leads to complete breakdown of microtubules

Blockage of cell division


Inhibition of mitochondrial fumerate
reductase enzyme & blockage of glucose
transport
Broad spectrum anthelmintic drugs with
excellent efficacy against all helminth
endoparaistes
Triclabendazole is very effective against all
stages of Fasciola

Triclabendazole has no anticestodal and


antinematodal action
Fenbendazole is also effective against canine
Giardiasis
Thiabendazole also possesses anti-fungal
action
Albendazole is widely used for the treatment
of Hydatidosis, Cysticercosis

They are more useful in divided doses than a


single dose
More effective in ruminants and horses
Alteration in -tubulin structure that reduces
the affinity for binding to Benzimidazoles
Thiabendazole can occasionally cause
vomiting and diarrhea in dogs
Dachshands are more susceptible

Teratogenicity in sheep---- Oxfendazole,


Albendazole and Febantel

2. Macrocyclic lactones
Avermectins (including Ivermectin,
Doramectin, Abamectin and Selamectin)
Milbimycins (which include Moxidectin and
Milbemycin oxime)

Produced by streptomyces and Avermectins


are isolated from streptomyces avermitilis
Binding to Glutamate receptors (associated
with Cl- channels) triggers chloride ion influx
(as a result of opening of Cl- channels)
Hyperpolarization of parasite neuron,
paralysis and death of target parasites
Also bind to GABA-gated Cl- channels and
cause hyperpolarization

Ivermectin is well absorbed (>90%) from GIT


after oral administration in simple stomach
animals
In ruminants the ruminal inactivation reduces
the bioavailability to only 25-30%
The injectable preparations of Ivermectin
should be administered only through S/C
route in species other than horses (in which
it is given exclusively through oral route

Known as endectocides
Active against endoparasites including
Nematodes
Lung worms
Immature heart worms
Ectoparasites
Cattle grubs
Mange mites
Lice
Horn flies
No activity against cestodes and trematodes

Adverse effects
Collie breed of dogs
Manifested by ataxia, salivation, mydriasis,
tremors, paresis, recumbency and coma
Intravenous administration of Physostigmine
Hypersensitivity reaction to dead parasites

3. Imidathiazoles
Levamisole, Tetramisole & Butamisole
Autonomic ganglionic stimulants
(cholinomimetics)
Cause activation of parasympathetic nervous
system
Blocking of fumerate reductase and
succinate oxidase enzymes

Interfere with carbohydrate metabolism of


parasites
Immuno-stimulatory action
Potentiate the organophosphate intoxication
Broad spectrum nematocidal drugs
Effective against adult as well as larval GI
round worms, lung worms, heart worm (dogs)
and kidney worms

Ineffective against tapeworms and flatworms

Clinical signs of toxicity:


Hypersalivation
Miosis (reduction of papillary diameter)
Frequent urination
Diarrhea

Broncho-constriction
Muscle tremors
Death (from asphyxia due to respiratory
muscle paralysis)
Horses and dogs are more susceptible to
adverse effects
Intoxication can be treated with Atropine &
Hexamethonium

4. Tetrahydropyrimidines
Pyrentel, Morentel and Oxantel
Act as depolarizing neuromuscular blockers
Paralysis of susceptible organisms
Slow expulsion of parasites from the host body
Active against adult & larval nematodes residing
in the lumen or on the mucosal surface

Less effective against larvae that dwell inside


the mucosa (e.g., arrested osteretagia larvae)
Have no anti-cestodal & anti-trematodal action
(except when used at high doses in horses)
Safe for use during pregnancy & lactation
Emesis may sometimes occur in dogs receiving
therapeutic doses of Pyrentel

5. Organophosphates:
Inhibit acetylcholinesterase enzyme
Thus indirectly enhance the level of
acetylcholine
Interference with neuromuscular transmission
Trichlorfon, Dichlorvos & Coumaphos

Trichlorfon
Active against some nematodes of ruminants
Mainly used to treat ectoparasitic infestation

Drug interactions:

Anti-cholinesterase agents
Muscle relaxants
Aminoglycosides
Imidathiazoles

Organophosphate intoxication
Accidental overdosage
Licking of topically applied drug
Muscarinic signs (salivation, lacrymation &
diarrhea)
Nicotinic signs (muscle tremors & respiratory
paralysis)

Nervous signs (hyperexcitation, ataxia and


seizures)

Treatment:
Atropine + Pralidoxime
Organophosphates have been replaced by
much safer and broad spectrum anthelmintics

6. Isoquinolones (Praziquantel)
Increases the cell membrane permeability
causing rapid calcium influx

Instantaneous contraction & spastic paralysis


of parasites
Affected worms loose grip over the intestinal
mucosa and are expelled
Also produces irreversible focal destruction of
protective integument
Complete or partial disintegration of worms
after being attacked by the hosts proteolytic
enzymes

Primarily a broad spectrum anticestodal drug


Has flukicide action against lung, gut, blood
& liver flukes in dogs
Has no activity against nematodes
Safest anticestodal drug
No teratgenic or embryotoxic effects

7. Salicylanilides
Niclosamide, Oxyclozanide and Refoxanide
Inhibit mitochondrial oxidative
phosphorylation
Interfere with anaerobic ATP generation

Niclosamide
Primarily used as an anticestodal drug

Oxyclozanide
Mainly effective against adult flukes

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