Anthelminths

DR. MOZNA TALPUR

 Introduction

Human is the primary host for most helminthic

infections.
Most worms produce eggs and larva
These pass out of human body and infect secondary
host
Immature forms invade humans via skin or GIT
 Types of worms

Nematodes
 Elongated roundworms that possess a complete digestive system, including both a
mouth and an anus.
 They cause infection of intestine aswell as blood and tissues.
 Ascaris lumbricods (common)
 Enterobius vermicularis (pin worm)
 Trichris trichuria (whip worm)
 Strongyloids stercoralis (thread)
 Ankylostoma duodenale (hook worm)
For nematodes
 Direthylacarbamazine
 Ivermectin
 Mebendazole
 Pyrental [amoate
 Thiabendazole
Tape worms (cestodes)
 Flat segmented body attach to host intestine.
 Lack mouth and digestive tract
 Taenia saginata (Beef)
 Taenia solium (Pork)
For castodes
 Albendazole
 Niclosamide
Trematodes:
 Leaf shaped flatworm.
 Generally characterized by tissues they infect.
 E.g. Liver fluke, lung, blood.
Drugs for Trematodes:
 Praziquantal
 Anthelmintic modes of action
Class example MOA

Benzimidazoles Albendazole Tubulin binding and

cellular disruption
Tetrahydropyrimidine Levamisole Nicotinic-like agonists

Organophosphates Dichorvos Acetylcholine esterase

inhibitors
Piperazines Piperazine GABA agonists

Macrocyclic lactones Ivermectin GluCl- potentiators

Praziquantel Enhance Ca++

permeability
Salicylanilides Closantel Proton ionophores
 ALBENDAZOLE
(Cestode infection)

Broad spectrum
Drug of choice for treatment of hydatid disease
(ecchinococcus granulosis) and cysticercosis.
Used for the treatment of (intestinal nematodes) e.g.
ascariasis, tricurasis and strongyloidiasis, pinworm,
hookworm
 Mechanism Of Action

Inhibits microtubule synthesis, irreversibly impairs

glucose uptake, intestinal parasites are immobilized
and die slowly.

Larvicidal in: Hydatid ,cysticercosis , ascariasis and

hook worm infections.

Ovicidal in ascariasis ,hookworm , trichuriasis

 Clinical uses (albendazole)

 Used on empty stomach when used against

intraluminal parasites but with fatty meal when
against tissue parasites.

 In ascariasis ,tricurasis ,hookworm, pin worm

infection:
 Children under 2 years 400 mg orally as a single
dose repeated for 2-3 days in heavy ascariasis ,
repeated after 2-3 wks for pin worm
 Hydated diseases:
 Drug of choice ,400 mg twice with meals for 1
month or longer.
 Neurocysticercosis:
 It is controversial as it has not proved superior to
corticosteroid alone.
 It is used along with cotricosteroid to decrease the
inflammation caused by dying organism and it also reduces
the duration of course i.e. 400 mg twice daily for 21 days

 Other infections:
 Drug of choice in cutaneous and visceral larvea migrans ,
intestinal cappillariasis and others
 Adverse effects

In short term: use no significant adverse effects.

 In long term use in hydatid cyst and cysticercosis:
 Abdominal distress, headache ,fever , fatigue, alopecia ,
increased liver enzymes , pancytopenia. Blood counts and LFT
should be followed.
Not given during pregnancy and in hypersensitive
people.
 NICLOSAMIDE(Cestodes)

Second-line drug for treatment of tape worm

infections.
Mechanism of action:
Adult worm is rapidly killed by inhibition of
oxidative phosphorylation.
Pharmacokinetics:
Poorly absorbed from gut & excreted in urine.
 Clinical Uses

Treatment of most forms of tapeworms.

Not effective against cysticercosis or hydatic
disease.
Given in the morning on empty stomach.
Purgative is necessary to purge all dead segments
& prevent liberation of ova.
 Adverse effects

 Mild, infrequent and transitory GI disturbance

 Alcohol consumption should be avoided
 Not indicated in children under 2 years of age or in
pregnancy.
 MEBENDAZOLE (Nematodes)

 Synthetic benzimidazole
 Wide spectrum and safer than albendazole

Mechanism of action
 As albendazole
It kills hookworm, pin worm , ascariasis and
trichuris eggs.
 Clinical uses

 It is taken orally before or after meal tablets should be

chewed before swallowing.

 Pinworm infection: 100 mg as a single dose, to be repeated

after 2-3 weeks.

 Ascaris lumricoides , trichuris trichura , hookworm and

trichstrongtlus; 100 mg /twice daily for 3 days to repeated
in 2-3 weeks

 in adults and children over 2 years cure rate is 90-100 %

except hook worm but there occurs marked reduction
Trichinosis: It has limited efficacy against adult
worm.200-300 mg for 3 days ,then 400-500 mg for
10 days with fatty meal and co-administration with
corticosteroids in sever infection
 Adverse effects and precautions:

No adverse effects in short term therapy. Mild GI

disturbance.

With high dose: Hypersensitivity reactions,

agranulocytosis , alopecia ,elevation of liver enzymes .

Used with caution under 2ys of age may cause convulsion

in this group.

Enzyme inducers and inhibitors affect plasma level of the

drug.

Hepatic parenchymal disease

 Thiabendazole(Nematodes)

 Mechanism as other benzimidazole

 Chelating agent and form stable complexes with metals

including iron, but does not bind with calcium.

 Rapidly absorbed

 Half- life of 1-2 hrs

 Completely metabolized in liver and 90% is excreted in

urine

 Can also absorbed through skin

 Clinical uses
Should be given after meals and tablets should be
chewed
Strongyloidal infections
In cutaneous larva migrans.
Thiabendazole cream is applied topically or drug
can be given orally for 2 days.
 Adverse Effects & Contraindications

More toxic than other benzamidazoles

GI disturbances
Pruritus ,headache, drowsiness, psychoneurotic
symptoms.
Irreversible liver failure.
Fatal Stevens –Johnson syndrome
Not used in young children , pregnancy, hepatic and
renal diseases.
 PYRANTEL PAMOATE(nematodes)

 Broad spectrum
Pharmacokinetics:
 Poorly absorbed orally
 Half of the drug is excreted unchanged in the feces.
Mechanism of action:
 Neuromuscular blocking drug leads to paralyses of worms

 Effective against luminal organisms (mature or

immature forms).
 Not effective against migratory stages in the tissues
or against ova
 Clinical uses

Pin worm given orally with or without food.

Ascariasis
Hookworm

Adverse Effects
 Infrequent mild GI disturbance
 Drowsiness , headache ,insomnia.

 Rash ,fever

Contraindications
 Pregnancy
Children under 2 years of age
 DIETHYL CARBAMAZINE( nematodes )

Drug of choice for the treatment of filariasis and

tropical eosinophilia.
Pharmacokinetics:
Rapidly absorbed from gut
Half- life is 2-3 hours
The drug should be given after meals
It is excreted in urine as unchanged or metabolite.
Dosage is reduced in urinary alkalosis and renal
impairment.
 Mechanism Of Action

Immobilizes microfilariae and alters their surface

structure ,displacing them from tissues & making them
susceptible to destruction by host defense mechanism
Adverse rection:
Fever , malaise, papular rash, headache, GI disturbance, cough.
Chest, muscle, joint pain
Leucocytosis
Retinal hemorrhage
Encephalopathy
Lymphangitis and lymphadenopathy.
*It is not teratogenic
 Contraindications & Cautions

*Hypertension

*Renal disease

*patient with lymphangitis

Patients suspected of malaria
 IVERMECTIN(nematodes)

Drug of choice for treatment of filaria &

strongyloidiasis
It is a macrocyclic lactone ring
Given only orally
Rapidly absorbed
Does not cross BBB.
Half- life is 16 hrs
Excretion in urine & feces.
Mechanism Of Action:
 Paralyzenematodes by intensifying GABA-
mediated transmission of signals in peripheral
nerves.
Clinical uses:
 Drug of choice for cutaneous larva migrans &
strongyloidiasis.
 Onchocerciasis

 It is also used for scabies , lice .

 Filariasis (it is microfilaricidal).

 Adverse Effects

Fatigue, dizziness, GI disturbance

Killing of microfilaria result in a Mazotti reaction
(fever, headache, dizziness, somnolence,
hypotension , tachycardia, peripheral edema)
Corneal opacities & other eye lesions.
 Contraindications & Cautions

Concomitant use with other drugs that enhance

GABA
e.g Barbiturates, benzodiazepines, valproic acid.
Pregnancy
Meningitis
Children under 5 years of age.