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Common

Clinical Use
of VET Antiparasitic
By Dr. Ali Kareem Al-saidi
Bachelor veterinary medicine and surgery (BVM&S)

To Contact:
https://t.me/Vetchannel
Levamisole

Levamisole is approved for use in ruminants.


Mechanism of action:
Levamisole paralyzes worms by selectively activating nematode nicotinic
acetylcholine (ACh) receptors, allowing entry of Na+, Ca2+, for excessive
body muscle contraction, and thus induces paralysis
Therapeutic uses
Levamisole is effective against most mature GI worms and lungworms, but
it has marginal activity against Strongyloides and immature GI worms.

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Levamisole
Signs of levamisole poisoning
Include parasympathetic stimulation, convulsions, CNS depression, and
asphyxia, which is primarily the result of respiratory muscle paralysis.
Dose:
7.5 mg/kg PO
Note:
Some time mixed with Oxyclozanide l to give effect against liver fluke

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Pyrantel and morantel
Mechanism of action
Like levamisole, pyrantel, and morantel paralyze worms by causing
depolarizing neuromuscular blockade.
Therapeutic uses
 Horses: Pyrantel is effective against strongyles, ascarids, and pinworms,
but not against bots. Pyrantel tartrate is used to prevent nematodes
infestation and pyrantel pamoate is used to treat nematodes infestation.
 Dogs and cats: Pyrantel is effective against all GI nematodes, but it has
limited efficacy against whipworms.
 Ruminants: Morantel is used as a feed additive, which is effective against
stomach worms, nodular worms, and other principal intestinal worms.
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Pyrantel and morantel
Contraindications:
Because morantel and pyrantel have the same mechanism of action as
levamisole, these agents should not be used concurrently
Piperazine and pyrantel have antagonistic mechanisms of action; do not use
together.

Dose:
Dogs: 5 mg/kg PO, repeat in 3 weeks
Cats: 10 mg/kg PO, repeat in 3 weeks.
Horses: 6.6 mg (as base)/kg PO; 13.2 mg (as base)/kg for cestodes.
Cattle, Sheep & Goats: Pyrantel tartrate: 25 mg/kg PO.
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Ivermectin
Mechanism of action:
They activate the glutamate-gated chloride channels, thus inhibiting
neurotransmission in nematodes (and arthropods) to induce flaccid paralysis

Therapeutic uses and administration:


Ruminants: is effective against all major GI worms and lungworms. It is
administered at 0.2 mg/kg orally or SC, and 0.5 mg/kg topically. The pour-on
ivermectin is effective as a nematocide in cattle, but not in goats or sheep
because of poor absorption from the skin.
Horses: It is effective against bots, stomach worms, strongyles, pinworms,
and ascarids. It is administered at 0.2 mg/kg orally.

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Ivermectin
Dogs
(a) Ivermectin is effective against ascarids, hookworms, and whipworms at
0.2 mg/kg orally.
However, this dose may not be safe in some breeds (e.g., Collies) and some
individuals, and is therefore not approved for dogs.
In the dogs, being highly susceptible to ivermectin, they have a mutation of
P-glycoprotein particularly in the endothelial cells of the blood–brain barrier.
P-glycoprotein, an ATP-binding cassette transporter (or multidrug
transporter) found in the apical membrane of endothelial cells, is responsible
for drug exit from the brain. The mutation of Pglycoprotein causes retention
of drugs, particularly macrocyclic lactones, in the brain of these dogs.
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Ivermectin
Dogs
(b) Ivermectin and other macrocyclic lactones are used as heartworm
preventives and are administered to dogs once a month. For this purpose,
ivermectin is administered at 6–12 μg/kg. Macrocylic lactones eliminate L4
stage of infective larvae of Dirofilaria immitis.
(c) It is effective as a microfilaricide (50 μg/kg orally). The use of ivermectin
as a microfilaricide is extra-label. Ivermectin can be diluted with propylene
glycol, if needed.
All species:
Ivermectin is effective against all ectoparasites. It is used especially to
control mites.

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Piperazine
Mechanism of action:
Piperazine is a GABA-receptor agonist that hyperpolarizes
nematode muscle, causing flaccid paralysis of worms

Therapeutic uses:
Piperazine has a limited spectrum of action but is effective
against ascarids and nodular worms in all species; however, its use is limited
in ruminants, because ascarids are not a significant problem in this species.

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Piperazine
Dogs:
For treatment of ascarids (Note: Because larval stages in the host’s tissues
may not be affected by the drug, many clinicians recommend retreating
about 2-3 weeks after the first dose):
5 - 65 mg of base/kg PO; For pups less than 2.5 kg: 150 mg maximum.
Cats:
For treatment of ascarids (Note: Because larval stages in the host’s tissues
may not be affected by the drug, many clinicians recommend retreating
about 2-3 weeks after the first dose):
45 - 65 mg of base/kg PO; 150 mg maximum.

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Piperazine
Horses:
a) 110 mg/kg (base) PO; repeat in 3-4 weeks. Retreating at 10 week intervals
for P. equorum infections in young animals is recommended.
b) 200 mg/kg PO. Maximum of 80 grams in adults, 60 grams in yearlings, and
30 grams in foals.

Cattle, Sheep & Goats:


Because of fairly high resistance of many nematode species to piperazine, it
is rarely used alone in these species.

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Benzimidazoles (BZDs)
BZDs include albendazole, fenbendazole, oxfendazole, oxibendazole, and
febantel (a pro-BZD that is converted to fenbendazole and oxfendazole in
animals).

Mechanism of action:
BZDs inhibit microtubule synthesis in nematode cells by interfering with
polymerization of β-tubulins (Figure 16-3). BZDs do not affect microtubule
synthesis in animal cells, this is why these drugs are relatively safe in
animals. Care should be exercised for some of the BZDs (albendazole) if the
animal is in the first one-third of pregnancy.

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Benzimidazoles (BZDs)

Therapeutic uses:
Ruminants: Albendazole ,fenbendazole , and oxfendazole are effective
against major GI worms (in both the adult and larval stages).
In addition, they are effective against lungworms.
However, they are ineffective against filariae.

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Benzimidazoles (BZDs)
Horses: Fenbendazole, oxfendazole, and oxibendazole are effective against
strongyles, but have limited activity against immature strongyles.
They are not very effective against migrating larvae of Strongylus vulgaris
and S. edentatis, and thus need elevated, multiple doses to treat these
parasites.
They are effective against Oxyuris, Trichostronylus, and Parascaris. They have
limited activity against Strongyloides, Habronema, and Dictyocaulus; and
thus may need elevated doses to treat these parasites.
They are not effective against Gasterophilus.

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Benzimidazoles (BZDs)
Dogs and cats: Fenbendazole and febantel (in Drontal©R Plus) are
effective against ascarids, hookworms, and whipworms in both adult and
larva forms.
Administration & dose:
BZDs are administered orally. In general, one single dose in cattle and horses, and three to
five consecutive daily dosages in carnivores and omnivores.
Cattle: For susceptible parasites:
a) 10 mg/kg PO
b) 7.5 mg/kg PO; 15 mg/kg PO for adult liver flukes
Note: BZDs have ovicidal activity on nematodes. In addition, production of eggs by
nematodes is inhibited within 1 hour of BZD administration.
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Niclosamide

Niclosamide is highly effective against most of the tapeworm


species in companion animals.
However, it has poor efficacy against Dipylidium spp. and E.
granulosus.
This drug is also effective for the treatment of common
tapeworms in ruminants such as Moniezia spp. and Thysanosoma
spp.
In horses it may be used for the treatment of Anoplocephala spp.

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Niclosamide

It may be administered as either suspension by oral or


intraruminal routes in ruminants or as tablets for oral treatment
in companion animals.
Niclosamide administration in fasted animals increases its
efficacy. Its oral administration, at doses of 100–157 mg/kg,
produced only low plasma concentrations, which correlates with
low gastrointestinal (GI) absorption and the wellknown safety of
the drug

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Niclosamide

Interestingly, niclosamide has been identified as a potential


anticancer agent due to its inhibitory effects on multiple
intracellular signaling pathways. The signaling molecules in those
pathways may be over-expressed, constitutively active, or
mutated in different cancer cells. Consequently, a number of in
vitro and in vivo studies have reported on the anticancer
effectiveness of niclosamide, used either alone or in combination
with other antineoplastic agents.

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Salicylanilides

This family includes fasciolicidal drugs of similar chemical


structure sharing the same mode of action. The most extensively
used salicylanilides (closantel, rafoxanide, and oxyclozanide) are
described here.

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Salicylanilides
Closantel
Is highly effective for the treatment of adult flukes and shows
good activity against immature specimens aged 6–8 weeks. It is
not effective against earlier stages.
At an oral dosage of 10 mg/kg, its efficacy is more than 92%
against 8-week-old and adult F. hepatica.
It is less active against younger stages of this parasite, that is 70–
77% efficacy for 6-week-old flukes migrating in the liver.
It is also effective (94.6–97.7%) against 8-week-old Fascioloides.
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Salicylanilides
Rafoxanide
Its principal use is as an adulticide for F. hepatica and F. gigantica.
A single therapeutic dose (7.5 mg/kg) in sheep provides nearly
100% for 12-week-old flukes of F. hepatica, 86–99% for 6-week-
old flukes, and 50–98% forN4-week-old specimens of this
parasite.
At elevated doses (10–15 mg/kg), rafoxanide shows high activity
against 4-week-old flukes.

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Salicylanilides
Rafoxanide
The same dosages reach similar efficacies against F. hepatica in
cattle.
The reliable efficacy of this drug against 4- and 6-week-old flukes
gives rafoxanide an advantage over strictly adulticidal drugs in the
treatment of acute fasciolosis.

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Salicylanilides
Rafoxanide
In this case, the administration might be repeated after 3 weeks
to eliminate maturing flukes that may have escaped the earlier
treatment.
In addition, this anthelmintic is also indicated for the treatment of
haemonchosis, bunostomosis, and sheep nasal bots (Oestrus
ovis).

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Salicylanilides
Oxyclozanide
Oxyclozanide was introduced over 40 years ago for use against adult fluke
infections in ruminants.
It has been also used against tapeworms (Moniezia spp.) in sheep and cattle.
This anthelmintic is marketed as an oral drench containing oxyclozanide only
or in combination with levamisole hydrochloride or oxfendazole. It is also
formulated as a powder to be incorporated in the feed.
The recommended dose rates are 10–15 mg/kg for cattle and 15 mg/kg for
sheep and goats.

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