Anthelmintics Agents
Anthelmintics are drugs that either kill
(vermicide) or expel (vermifuge) infesting
helminths.
Helminths harm the host by depriving him
of food, causing blood loss, injury to organs,
intestinal or lymphatic obstruction and by
secreting toxins.
The choice of drug for each worm
infestation is based not only on efficacy, but
also on lack of side effects/toxicity, ease of
administration and low cost.
Classification
• Benzimidazoles: Albendazole,
Mebendazole, Thiabendazole
• Imidazo thiazole: Levamisole
• Vinyl pyrimidines: Pyrantel
pamoate
• Piperazines: Diethylcarbamazine
citrate, Piperazine citrate
• Amide: Niclosamide
• Natural Products: Ivermectin
Mebendazole
This benzimidazole derivative has broad-
spectrum anthelmintic activity.
Mebendazole has produced nearly 100%
cure rate/reduction in egg count in
roundworm, hook worm (both species),
Enterobius and Trichuris infestations.
Prolonged treatment has been shown to
cause hydatid cysts in the liver. Treatment
after resection (cutting) of the cyst may
prevent its regrowth.
The immobilizing and lethal action of
mebendazole on worms is rather slow: takes
2–3 days to develop.
Mechanism of action: it appears to act
on microtubular protein ‘β-tubulin’ of the
parasite. It binds to β-tubulin of susceptible
worms with high affinity and inhibits its
polymerization.
In also, blocks glucose uptake in the
parasite, inhibits some mitochondrial
enzymes and depletes its glycogen stores.
Hatching of nematode eggs and their
larvae are also inhibited.
Pharmacokinetics: absorbed from intestines.
An oral dose is excreted in the faeces.
Adverse effects At low doses: Diarrhoea,
nausea and abdominal pain.
At high doses: Allergic reactions, loss of
hair and granulocytopenia.
Incidents of expulsion of worms from
mouth or nose have occurred, probably due
to starvation of the parasite and their slow
death.
Contraindication during pregnancy.
Uses:
For Roundworm 100 mg twice a day for 3
consecutive
For Hookworm 7 days.
Pin worm (Enterobius) 100 mg single
dose, repeated after 2-3 weeks.
Hydatid disease: 200-400 mg BD or TDS
for 3-4 weeks.
Albendazole
It is a congener of mebendazole with
broad-spectrum activity and excellent
tolerability of its predecessor
(mebendazole), and has the advantage of
single dose administration in many
infestations. One dose treatment has
produced cure rates in roundworm, and
hookworm.
The mechanism of action of albendazole is
similar to that of mebendazole.
Pharmacokinetics: inconsistent absorption
after oral administration.
Absorption is enhanced when the drug is
taken with fatty meal. It is converted to
sulfoxide active metabolite, which enters
brain and others tissue. It is excreted in
urine.
Side effects Albendazole is well tolerated;
headache, fever, dizziness, alopecia,
jaundice and neutropenia.
Uses No preparation or post drug fasting/
purging is required. For intestinal worms it
should be given on empty stomach.
• For Roundworm, hookworm, Enterobius
and Trichuris: a single dose of 400 mg
(for adults and children above 2 yrs; 200
mg for 1–2 yr age) is suffcient.
• Tapeworms: 400 mg twice daily for 3
consecutive days. It is a second choice
drug to praziquantel and niclosamide for
tapeworm infestation.
• Trichinosis: Three day treatment with 400
mg twice daily expels the adult worm
from intestine.
• Hydatid disease: 400 mg BD for 4 weeks,
repeat after 2 weeks, up to 3 courses.
Albendazole use in pregnant women is
contraindicated.
Levamisole, Tetramisole
Tetramisole, is racemic mixture. Its levo
isomer (levamisole) was found to be more
active and preferable. Both are active
against roundworm.
Mechanism of action: They are vermifuge,
causing paralysis and expulsion of live
worms by stimulation of ganglia in worms.
Interference with carbohydrate metabolism
(inhibition of fumarate reductase) may
also be contributing to paralysis.
Levamisole is an immunomodulator as
well: restores depressed T cell function. It
was used as a disease modifying drug in
rheumatoid arthritis and as an adjunct in
malignancies.
Adverse effects: Nausea, abdominal pain,
giddiness, fatigue, drowsiness or insomnia is
low.
Pyrantel pamoate
It was introduced in 1969 for roundworm
and hookworm infestation in children.
Mechanism of action: It activates nicotinic
cholinergic receptors in the worms
resulting in persistent depolarization and
spastic paralysis. Worms are then expelled.
Cholinergic receptors in mammalian skeletal
muscle have very low affinity for pyrantel
pamoate.
Pharmacokinetics: low oral absorption. this
is partly metabolized and excreted in urine.
Adverse effects: g.i.t symptoms, headache
and dizziness.
Use: No fasting, purging or other
preparation of the patient is required.
Piperazine
It is a highly active drug against Ascaris and
Enterobius. However, it is not frequently
used now because of availability of more
convenient and better tolerated albendazole
/mebendazole.
Mechanism of action: Piperazine act as a
GABA agonistic leads to opening of Cl¯
channels. Hyperpolarization causes
relaxation and depresses responsiveness to
contractile action of ACh. Flaccid paralysis
occurs and worms are expelled alive. They
recover if placed in piperazine free medium.
Therefore, often a purgative (senna) is given
with it, but is not mandatory. Side effects: have been mild—pruritus,
Pharmacokintics: Well absorbed orally, giddiness, nausea, abdominal pain,
partly metabolized in liver and excreted in constipation, lethargy and transient ECG
urine. Changes.
Side effect: At low doses: nausea, vomiting, Safety of ivermectin in pregnant
abdominal discomfort and urticarial. women and young children is not
At high doses: Dizziness and excitement established
occur at high doses; toxic doses produce
convulsions; death is due to respiratory
failure.
Contraindication in renal insuffciency and
in epileptics, but is safe in the pregnant.
Dose: For roundworm infestation 4 g once a
day for 2 consecutive days.
Combination of any other anthelmintic
(except piperazine) with a purgative in the
same formulation is banned in India.

Ivermectin It is an extremely potent

semisynthetic derivative of the
antinematodal principle obtained from
Streptomyces avermitilis. Ivermectin is the
drug of choice for single dose treatment of
onchocerciasis and strongyloidosis.
It has been used as add-on drug to
albendazole/mebendazole in heavy
trichuriasis. Certain insects, notably scabies
and head lice are killed by ivermectin.
Mechanism of action: It activates
glutamate gated Cl¯ channel leads to
hyperpolarization. Hyperpolarization causes
tonic paralysis and expulsion of worms.
Potentiation of GABAergic transmission
in the worm has also been observed.
Ivermectin used for filariasis and
onchocerciasis.
Ivermectin is the only drug effective orally
in scabies and pediculosis.