ANTHELMINTICS

Solomon M. Abay (PhD)

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 Classification of parasitic worms

• Nematodes:
a. Intestinal lumen b. Inhabit tissues
• Giant round worm • Pork round worm
• Pin worm • Filariae
• Hook worm
• Whip worm
• Thread worm

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 Classification (2)
• Cestodes:
– Beef tape worm
– Pork tape worm
– Fish tape worm
• Trematodes:
– Blood fluke
– Liver fluke
– Intestinal fluke
– Lung fluke
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 NEMATODE INFESTATION [INTESTINAL]
Ascariasis (Giant round worm infestation)
• Most prevalent helminthic infestation
• Adult worm inhabit the intestine
• Serious complications can result if worms migrate into:
– Pancreatic duct
– Bile duct
– Gall bladder
– Liver
• Heavy infestation Intestinal blockade

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 Ascariasis (2)
• Drug of choice:
» Albendazole
» Mebendazole
» Pyrantel pamoate
• Alternative drug: Piperazine citrate.

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 ALBENDAZOLE
• Chemistry: benzimidazole carbamate

• Mechanism:
– Inhibition of mitochondrial fumarate reductase
– Inhibits microtubule polymerization by binding to
-tubulin  Irreversibly impairing glucose uptake
 Immobilized & slowly die

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 Albendazole (2)
• Pharmacokinetics:
– Erratically absorbed p.o.
– Rapidly undergoes 1st pass metabolism in liver to
active albendazole sulfoxide
–  absorption when taken with fatty meal
– Distributed to tissues including Bile & CSF &
enters hydatid cysts
– Excreted through bile

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 Albendazole (3)
• Therapeutic uses:
– Broad spectrum antiparasitic
1. Effective as single dose for the Rx of
• A. lumricoides
• Hookworm: A. duodenalis & N. americanus
• T. trichuria
2. Also effective against:
• E. vermicularis
• T. spiralis
3. S. sterocoralis [Invermectin is superior]
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 Albendazole (4)
4. High dose in Rx of hydatid disease
5. Useful for Rx of neurocysticercosis
– [Superior to praziquantel]
– Corticosteroids: used to control inflammatory
response

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Albendazole is well distributed into various
tissues including hydatid cysts. This
probably explains why albendazole is more
effective than mebendazole for treating
hydatid cyst disease, and possibly other
tissue-dwelling helminths.

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 Albendazole (5)
Adverse effects
• Fewer ADR when used for short term therapy
• With protracted therapy
• GI pain
• Severe head ache
• Fever
• Fatigue
• Loss of hair
•  in serum transaminase
• Leucopenia & thrombocytopenia
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 MEBENDAZOLE
• Mechanism: prevents uptake of glucose 
Immobilization & death
• drug of choice for most intestinal round worms
[pin worm, hookworm, whipworm, giant
worm]
• useful for Rx of mixed infestation
• Pharmacokinetics:
– Only 5-10 % is absorbed & rapidly metabolized

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 MEBENDAZOLE (2)
Adverse effect:
• Transient abdominal pain & diarrhea
[Massive infestation]
• Embryocytotoxic & teratogenic in rats

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 PYRANTAL PAMOATE
• Mechanism: depolarizing neuromuscular
blocker that causes spastic paralysis of
intestinal worms
• Therapeutic uses:
– Alternative to mebendazole for infestation with:
hookworm, pinworm, giant worms
• Adverse effect: serious reactions are rare
– GIT: NVD
• CNS: dizziness & drowsiness
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 PIPERAZINE CITRATE
• Mechanism: paralysis of ascaris by blocking
Ach at myoneural junction
• Therapeutic uses:
– Alternative to albendazole or mebendazole in the
Rx of ascariasis
• Adverse effect:
– NVD
– Dizziness & headache

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ENTEROBIASIS (PINWORM INFESTATION)

• Serious infections are rare but may cause

intense perianal itching
• It is readily transmissible; family members
should be treated
• Drugs of choice:
• Albendazole
• Mebendazole
• Pyrantel pamoate

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 ANCYLOSTOMIASIS & NECATORIASIS
(Hookworm infection)

• Common in rural area (barefoot)

• Adult worm attach to intestine & suck
blood chronic blood loss  progressive
anemia
– Albendazole
– Mebendazole
– Pyrantel pamoate

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 TRICHURIASIS
(WHIPWORM INFESTATION)

• Larva & adult worms inhabit large intestine

• When worm burden is large, rectal prolapse
may occur
– Mebendazole [drug of choice]
– Albendazole

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 STRONGYLOIDIASIS
(THREADWORM INFESTATION)

• Larva & adult inhabit small intestine

• Drug of choice:
• Ivermectin
• Albendazole
• Thiabendazole

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 THIABENDAZOLE

• Mechanism:
– Inhibit fumarate reductase
• Pharmacokinetics:
– Rapid absorption & metabolism
– Excreted as metabolites in the urine
• Therapeutic use: alternative drug against
– Strongyloidiasis
– Trichinellosis

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 THIABENDAZOLE (2)
• Adverse effect
– Incidence is high, most common includes:
• GIT: ANV
• Neurological: Dizziness & Drowsiness

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 NEMATODE INFESTATION (Extraintestinal)

1. TRICHINELLOSIS (PORK ROUNDWORM INFESTATION)

• Adult worm reside in intestine; Larva migrate to skeletal
muscle & become encysted
• Symptoms include:
– GI upset, Muscle pain
– Fever, Sore throat
• Drugs of choice:
– Mebendazole
– Albendazole Enteric stages of the parasite
• Prednisolone is included to reduce inflammation during
larva movement

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 Extra-intestinal (2)
2. WUCHERERIASIS & BRUGLASIS
(Lymphatic filarial infestation)
• W. bancrofti & B. malayi invade the
lymphatic system
• Heavy infestation  lymphatic
destruction  Elephantiasis
• Drug of choice: Diethylcarbamazine

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 DIETHYLCARBAMAZINE
• Mechanism:
• 1st the drug reduces muscular activity 
parasite dislodges from site of attachment
• 2nd by altering the surface properties of the
parasites  more vulnerable to attack by
host defenses
• Pharmacokinetics:
– Readily absorbed & extensively metabolized

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 DIETHYLCARBAMAZINE (2)
• Therapeutic uses:
– Drug of choice for filarial infestations
• Destroys microfilariae of W.bancrofti, B.malayi & Loa
loa
• Kills also adult females of these species.
• Adverse effects
– Reactions caused directly by DEC are minor:
• Headache
• Dizziness
• NV
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 DIETHYLCARBAMAZINE (3)
• Occurring secondary to death of the parasite are
more serious:
– Rash
– Intense itching
– Encephalitis
– Fever
– Tachycardia
– Lymphadenitis
– Leukocytosis
– Proteinuria
• These can be decreased by pre-treatment with
glucocorticoids

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 Extra-intestinal (3)
3. ONCHOCERCIASIS (River blindness)
• Heavy infestation causes:
– Dermatologic
• Nodules
• Pruritic dermatitis
– Opthalmic
• Occular lesions, caused by infiltration & death of
microfilariae  optic neuritis, optic atrophy,
blindness
– The drug of choice is Ivermectin

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 IVERMECTIN
• Mechanism: disrupts nerve traffic & muscle
function in target parasite
• Opening of cell surface Cl- channel

• Hyperpolarization

• Causes paralysis followed by death
• Pharmacokinetics:
– Administered p.o.
– t1/2 =16hrs
– Metabolize in liver

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 IVERMECTIN (2)

• Therapeutic uses:
– Rx of onchocerciasis
– Rx of intestinal strongyloidiasis
• Used extensively in veterinary medicine

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 IVERMECTIN (3)
• Adverse effects:
– Mazotti reaction when used for onchocerciasis
– Principal symptoms are:
• Pruritis
• Rash
• Fever
• Lymph node tenderness
• Bone & joint pain
• Due to allergic & inflammatory response to death of
microfilariae
• No data on pregnant women; teratogenic in mice,
rats, rabbits [cleft palate]
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 CESTODE INFESTATIONS
1. TAENIASIS [beef & pork tape worm]
• Acquired by eating undercooked beef or
pork that contains tapeworm larvae
• Treated by:
– Praziquantel
– Niclosamide

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 CESTODE (2)
2. DIPHYLLOBOTHRIASIS [Fish tapeworm
infestation]
• acquired by ingestion of undercooked fish
that is infested with tapeworm larvae
• worms are killed by:
– Praziquantel
– Niclosamide

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 NICLOSAMIDE

• Mechanism: inhibits mitochondrial oxidative

phosphorylation in tapeworm  cessation of
ATP production  death
• Therapeutic uses:
– Alternative to praziquantel in Rx of Cestode
infestation.

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 NICLOSAMIDE (2)
• treating infections caused by T. saginata (beef
tapeworm), T. solium (pork tapeworm), and D.
latum (fish tapeworm)
• With H. nana (dwarf tapeworm), a longer
treatment course (up to 7 days) is necessary.
• Adverse effects
– Absorption is poor  systemic ADR is minimal
– GIT: ANV

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 PRAZIQUANTEL
• Mechanism: absorbed by helminthes
• At low concentration  spastic paralysis 
detachment of worms
• At high concentration  disruption of the
tegument of the worm  rendered
vulnerable to lethal effect of host defenses

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 PRAZIQUANTEL (2)
• Pharmacokinetics:
– Readily absorbed from GIT
– Extensive hepatic metabolism
– Metabolites excreted in urine
– Concentration is reduced by phenytoin or
carbamazepine; and increased by cimetidine.

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 PRAZIQUANTEL (3)
• Therapeutic uses:
– Active against cestodes and trematodes

Flukes: Tapeworms :
S. haematobium, D. latum,
S. mansoni, H. nana,
S. japonicum T. saginata,
other flukes, such as T. solium
Paragonimus
westermani

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 PRAZIQUANTEL (4)
• Adverse effects:
– Relatively free of toxicity
• Nausea, vomiting, and abdominal discomfort.
– due to the liberation of helminth proteins
from dead worms

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 TREMATODE INFESTATION
1. Schistosomiasis (blood fluke infestation)
• Has acute & chronic phases
• Acute: Chronic:
Fever Intestinal polyps
Lymphadenitis hepatospleenomegaly
Anorexia
Malaise Portal hypertension
Muscle pain
Rash

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 Schistosomiasis (2)
• For both acute & chronic phase, praziquantel is the
drug of choice

Metrifonate
• Metrifonate: alternative to praziquantel to S.
hematobium
• organophosphorous
• The active metabolite, dichlorvos, inactivates
acetylcholinesterase
• Contraindicated:
– Pregnancy,
– Previous insecticide exposure, or
– With depolarizing neuromuscular blockers.
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 2. FACILIASIS (Liver fluke infestation)
• Parasites inhabit the biliary tract
• Symptoms include:
– Anorexia, Mild fever, Fatigue
– Itching in the region of the liver
• Praziquantel is not effective
• Bithionol is the alternative

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 3. FASCIOLOPSIASIS
(Intestinal fluke infestation)
• Adult worms inhabit the small intestine
• Disruption of bowel function may occur
– Constipation & diarrhea
• Massive infestation  bowel obstruction
• Praziquantel is Rx of choice

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Thank you

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