ANTIPROTOZOAL DRUGS
 Not used to treat clinical
 Anticoccidial drugs
 Coccidiosis
 Causes huge financial loss in animal
industry
 Impaired feed conversion
 Slow growth
 Poor carcass quality
 Therapeutic approaches
 Broilers
 Not vaccinated against coccidia
 Amprolium – nonwithdrawal drug
(administered 1 week before
slaughter)
 Layers
 Vaccinated with anticoccidial
 Sulfonamide for outbreaks
 Mammals
 Potentiated sulfonamides
 Amprolium
 Decoquinate
 Sodium ionophores
 Resistance to anticoccidial drugs
 Minimized by using two or more drugs
sequentially
 Shuttle program- different drugs
are used in one grow-out
 Rotation (switch) program-
different drugs are used in two
grow-out
1) Decoquinate
 Quinolone
 MOA
 Block DNA gyrase, thus inhibit
protein synthesis
 Pharmacokinetics
 Withdrawal period: 5 days
preslaughter in broilers
 Therapeutic uses
 Prevent coccidiosis
 Calves: E. bovis, E. zuernii
 Young goats: E. christenseni,
E. ninakohlyakimovae
 Broilers
coccidiosis
 Effective in the first sporozoite stage
(Eimeria)
 Resistance might be mounted by the
protozoa
 Toxicity
 No adverse side effects if used
properly
2) Sodium ionophores
 Preparations
 Monensin
 Salinomycin
 Lasalocid
 Used exclusively as anticoccidial drugs
 MOA
 Facilitate transport of sodium into cells
→ increase intracellular sodium
concentration → inhibit mitochondrial
functions and ATP hydrolysis
 Therapeutic uses
 Effective against Eimeria in
 Chickens
 Cattle
 Sheep
 Monensin: Cattle and sheep
 Also used as growth promoters
 Lasalocid (prevention)
 Cattle:
 Sheep
 Chicken: first generation
trophozoites and schizonts
 Salinomycin: chickens only
 Adverse effects
 Severe cardiovascular side effects:
increased intracellular influx of calcium
 Contraindications
 fatal to horses and turkeys
3) Amprolium
 Quarternary compound
 Mechanism of action
 Blocks thiamine receptors, thus no
thiamine ulitization by coccidia
 Pharmacokinetics
 Poorly absorbed after oral
administration
 No preslaughter withdrawal period
 Therapeutic uses
 Only anticoccidial used for layers and
cattle; used both for prevention and
treatment of coccidiosis
 First generation trophozoites and
schizonts
 Usually combined with sulfa drugs
  Adverse effects  Pharmacokinetics: levels can be
 Thiamine deficiency in host if given in maintained in 24 hours
increased amounts (overdosage)  Therapeutic uses
4) Nicarbazin  Combined with sulfa
 Mixture of  Coccidiosis outbreaks
 4, 4’-dinitrocarbanilide (DNC)  toxoplasmosis
 2-hydroxy-4, 6-dimethylpyrimidine  Metronidazole
(HDP)  Mechanism of action
 Mechanism of action: unknown  Metabolite disrupts DNA synthesis in
 Pharmacokinetics protozoans and bacteria
 DNC more absorbed rapidly than HDP  Pharmacokinetics
 4-day withdrawal period is required in  Absorption
broilers  Bioavailability (PO): 50-100%
 Therapeutic uses  Absorption is enhanced with food
 Prevent coccidiosis outbreaks (increased bile secretion)
 Target: second-generation  Blood level (peak) is achieved 1
trophozoites hour after administration
 Toxicity  Distribution
 Effects  Rapidly and widely distributed:
 Egg production lipidsoluble
 Bleached of brown-shelled  Metabolism and excretion
eggs  Hydroxylation and conjugation
 Mottled eggyolks (Liver)
 Poor hatchability  Excretion of metabolites and
 Impaired egg production unchanged drug: feces and urine
 Broilers become more prone to  Therapeutic Uses
heat stress  Giardiasis
5) Robenidine  Histomoniasis
 Effective against first generation schizonts  Babesiosis
 For the prevention of outbreaks  Trichomoniasis
 Adverse side effects  Amebiasis
 Results in unpleasant taste of broiler  Toxicity
meat  Lethargy
 Egg taste is also affected  Weakness
6) Sulfonamides  Ataxia
 Preparations  Rigidity
 Sulfadimethoxine  Anorexia
 Sulfachlorpyrazine  Vomiting
 Sulfaquinoxaline  Diarrhea
 Ethopabate (PABA antagonist but not  Reversible leukopenia
sulfa drug)  Hepatoxicity
 Therapeutic uses
 Prevention of coccidia, esp intestinal MACROCYCLIC LACTONES
than cecal - Derivatives of soil organisms
 Effective against second generation - Avermectin & Milbemycin
schizonts  MOA
7) Antifolate  Binds at the glutamate-gated chloride
 Preparations channel receptor in nematode and
 Ormetoprim arthropod nerve cells → opening of the
 Pyrimethamine channels → influx of chloride ions →
 Not approved for food animal use Flaccid paralysis + reproductive function
 Mechanism of action suppression in ticks
 Block conversion of dihydrofolate to  Not effective against trematodes and
tetrahydrofolate (inhibit thymidine cestodes!
synthesis)  Pharmacokinetics
  Well absorbed when administered  Given to pregnant sows
 PO  To prevent transmission of
 Parenterally Strongyloides ransomi to
 As pour-on formulations piglets
 Effective levels are reached in the lungs  ~80% efficacy against Trichuris
and skin (regardless of the route of suis
administration)  In horses (paste-PO)
 Route of excretion  Intramuscular injection was
 Urine used before.
 Feces  PO administration is the route
 Milk which is now approved for use
 Residues (amount) are found on the in horses.
 Muscles and kidneys: minimal  Effective against
 Liver and fat tissues: high  Trichostrongylus axei
 Effective against parasite localizing in/at  Parascaris equorum
the  Oxyuris equi
 Respiratory system  Strongylus vulgaris
 Skin  Stephanurus dentatus
 Gastrointestinal system  Dictyocaulus arnfieldi
 Contraindications  S. equinus (adult)
 Animals that are producing milk for human  Triodontophorus spp
consumption (except eprinomectin)  Habronema muscae (adult
 Avermectins and larvae)
 Commercially available avermectins  Strongyloides westeri
 Ivermectin, composition  Gastrophilus spp
 ≥90% 22,23 dihydroavermectin  Draschia megastoma
B1a  Onchocerca sp
 ≤10% of the B1b homolog  In dogs
 In ruminants (parenteral, pour-on  For Dirofilaria immitis
& PO) prevention
 Effective against  6 μg/kg, at 1 month interval
 Immature and adult stages  Collies are sensitive:reduced
of GI nematodes ability to efflux the drug from
 Adult and larval stages of the CNS
 Ostertagia (+ inhibited  Depression
L4)  Muscle weakness
 Trichostrongylus  Blindness
 Oesophagustomum  Coma
 Haemonchus  Death
 Dictyocaulus viviparis  In rats, rabbits, and mice
 Less efficacy against  Teratogenic
 Cooperia  Only at or near
 Nematodirus maternotoxic dose levels
 Pour-ons and injection  Mice: most sensitive species at
formulations 0.2-0.4 mg/kg/day
 Ectoparasites  Abamectin
 In pigs (SC)  Doramectin
 Effective against  Milbemycins
 Adult and larval stages of  Commercially available milbemycin
 Ascaris suum  Milbemycin oxime, composition
 Hyostrongylus rubidus  80% of the A4 5-
 Oesophagustomum spp didehydromilbemycin analog
 Metastrongylus spp  20% of the A3 5-
 Mange mites didehydromilbemycin analog
 Sucking louse  Moxidectin
 Avermectin & Moxidectin
 Potent
 Broad-spectrum at low dose levels
 Active against
 Nematodes (mature and immature)
 Hypobiotic larvae
 Arthropods
 Avermectin * milbemycin oxime
 Canine heartworm prevention
 GI roundworm prophylaxis
 Hookworm
 Ascarids
 Whipworms
IMIDAZOTHIAZOLES
 Tetramisole and Levamisole
 Tetramisole – marketed in 1965
 Levamisole
 DL-isomer of tetramisole
 Compared to tetramisole
 Decreased dosage
 Less toxic
 Broad spectrum against wide range of
GI helminths and lungworms
 Administration
 Oral
 Rapidly absorbed from the GIT
 Intramuscular
 Peak blood levels are ~ twice
compared to PO administration
 Subcutaneous
 Efficacy is better than oral
administration if used against
lungworms
 Topical
 Especially in cattle
 Slow-release bolus
 Mechanism of Action
 Ganglion stimulant of nematode nerves →
Neuromuscular paralysis of the parasite
 Efficacy as anthelmintic is based on
maximum concentration achieved than
duration of concentrations
 Not ovicidal
 Commonly used in the following species
(especially in cases of benzimidazole-
resistant parasite infection)
 Ruminants
 Mature and immature gastrointestinal
helminths
 Lungworms
 Variable efficacy against Strongyloides
 Dogs: microfilaricide (heartworm)
 Pigs
 Ascarids
 Intestinal threadworms
 Lungworms
 Nodular worms
 Kidney worms
 Poultry
 Why levamisole is used in a number of animal
species?
 Broad spectrum of activity against
nematodes
 Ease of use (due to water solubility)
 Wide margin of safety
 Lack of teratogenic effect
 Contraindications
 Should not be administered together with
OP compounds
 Increase toxic effect on the nervous
system
 Tetrahydropyrimidines
 Adverse side effect
 Inflammation at the site of SC
administration (transient)
 See tetrahydropyrimidines
 Additional effect
 Immunostimulant
 Man
 Some animals in severe diseases
ORGANOPHOSPHATES
-Dichlorvos, Trichlorfon, Haloxon,
Coumaphos
 Background
 Originally used as insecticide for sheep
and goats
 Then as ectoparasiticide
 Sheep and goats
 MOA
 Inhibit acetylcholinesterase →
neuromuscular paralysis (spastic)
 Variable susceptibility of
acetylcholinesterase
 Humans
 Host
 Parasite (different species)
 Different susceptibilities results in the
formulation of OPs that have
 Maximum effect against parasites
 Minimum toxicity against host and
humans

 How is toxicity determined in host
animals?
 Susceptibility of cholinesterase to OPs
 Rate of inhibition reversal
 Rate of inactivation of Ops
 Preparations
 Haloxon
 Safest OP for ruminants
 Used to eliminate parasites in the
 Abomasum and small intestine
(lack efficacy to parasites
found at the large intestine
 Haemonchus
 Trichostrongylus
 Cooperia
 Strongyloides
 Less but good efficacy
 Ostertagia
 Bunostomum
 Nematodirus
 Margin of safety is wide
 Administered orally in the form of
 Paste
 Drench
 Bolus
 Contraindications
 Weak animals
 Animals exposed to other
anticholinesterase agents
 Animals with gastrointestinal disorders
 Respiratory disease
 Parturition within one month
 Use of insecticides, muscle relaxants,
phenothiazine derivatives or CNS
depressants
 Margin of safety is lesser than
benzimidazoles.
 Adverse side effects
 Toxicity (additive)
 Acute: SLUD syndrome (due to
cholinergic stimulation)
 Chronic:
 Demyelination resulting in chronic
neurotoxicity
 Acute death due to
 Respiratory paralysis
 Cardiovascular arrest
 Antidote for OP poisoning
 Atropine
 2-PAM / pralidoxime
 OP and man
 Op is absorbed well thorugh intact skin
(high lipid solubility)
 Interacts with a lot of drugs
 Rapidly degraded in the body
 Tissue residues are dangerous to man
(withdrawal period should be observed)
 Sprays, collars and washes of OP for
small animals- hazardous to children when
ingested, inhaled or in contact
 OP and fish
 Fish are susceptible to toxicity
 Water pollution (due to careless disposal
of OP) results in fish kill
1. Dichlorvos
a) High volatility (versatile OP)
b) Can be formulated into pellets and
released slowly as it passes through the
GIT
i. Increased concentration against
parasites along the GIT
ii. Increased safety
iii. Host can detoxify small amounts
iv. Drug in the feces can kill fly larvae
c) Efficacy + trichlorfon
i. Effective aginst
1. Bots
2. Ascarids
3. Other intestinal helminths
4. Trichlorfon must be converted
into dichlorvos to be effective.
d) Specific therapeutic uses
i. Pigs, dogs and cats
1. Whipworms
2. Nodular worms
3. Strongyloides
4. Hookworms
5. Ascarids
6. Little or no effect against
migrating larvae of ascarids and
hookworms
ii. Horses
1. Bots
2. Strongyles
3. Ascarids
4. Pinworms
2. Trichlorfon  Strongid-T® 
a) Specific therapeutic uses  Strongid-P® 
i. Used mainly in horses  Nemex® 
1. Bots, ascarids, oxyurids  Drontal® 
ii. Has efficacy in small animals and  Heartgard®
ruminants  Embonate
iii. Spectrum of activity is similar to  Formulations
dichlorvos  For oral administration
iv. One of the safest Ops  Suspension
v. Can be used in fishponds
 Paste
3. Coumaphos
 Drench
a) Specific therapeutic uses
 Tablets
i. For cattle
 Aqueous solutions
1. Stomach worms
 Spectrum (Effective against)
2. Whipworms
 Ascarids
3. Cooperia
 Large and small strongyles
ii. Incorporated in the feed to improve
 Pinworms
safety
 Oxantel
TETRAHYDROPYRIMIDINES
 Phenol analog of phenols
- pyrantel, oxantel, morantel
 Combined with pyrantel in some
preparations (for dogs and man)
 Pyrantel and Morantel
 To be effective against whipworms
 MOA
 Depolarizing neuromuscular blockade:
 Morantel
inducing paralysis in parasites
 Methyl ester of pyrantel
 MOA of antinematodal drugs
 Ruminants: safer and more effective than
pyrantel
 Pyrantel
 Sheep: absorbed rapidly from the
 First introduced as a broadspectrum GI
 Abomasum
anthelmintic agent
 Upper small intestine
 Sheep
 Liver: site of metabolism
 Cattle
 Metabolites are excreted in the urine
 Horses
 Dogs
 Morantel + Pyrantel
 Pigs
 High efficacy against
 Preparations
 Adult gut worms
 Tartrate
 Larval stages in the lumen or on the
 Well absorbed in dogs and pigs
mucosal surface (x arrested larvae)
 Less well by ruminants
 No withholding periods in some countries
 Metabolism is rapid
 Excretion  Contraindication
 Metabolites: Urine (fast)  Levamisole
 Unchanged: Feces (esp. in  Resistance
ruminants)  There is a crossresistance among
 For horses Strongid-C®  pyrantel, morantel, and levamisole.
 For pigs Banminth®  Adverse Reaction
 Pamoate salt  Parasympathetic stimulation
 Poor solubility in water  Convulsions
 Reduced absorption from the gut  CNS depression
(advantage)  Asphyxia- the result of respiratory muscle
 Allows drug to be effective paralysis.
against parasites found at the
lower end of the small intestine
 Effective in horses and dogs