2012 Anthelminthic

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ANTHELMINTIC

DRUGS
Groups of Helminths

Cestoda (tapeworms)

Nematoda (roundworms)

Trematoda (flukes)
Helminth species Drugs
used in treatment

Ces- Taenia, diphyllobothrium Niclosamide,praziquantel


todes Echinococcus Albendazole

Nema- Ascariasis, enterobius Mebendazole, piperazine


todes Strongyloides Tiabendazole,albendazole
Trichuris,necator,ankylostoma Mebendazole
Trichinella spiralis Thiabendazole
Dracunculus medinensis Metronidazole
Wucheria,Loaloa,Brugia malayi Diethylcarbamazine
Onchocerca Ivermectin

Trema-
The Anthelmintic Drugs

Mechanism :
Damaging or killing the worm directly
Paralysing the worm
Damaging the culticle of the worm so
that host defences, such as digestion &
immune rejection, can effect the worm
Interfering with worm metabolism
Niclosamide

Mechanism of action
Blocks glucose uptake. Irreversibly damaging the
scolex. Very little absorbed from GI tract.

Adverse effects
Mild GI disturbance

Therapeutic notes
Fasted patient
Praziquantel
Mechanism of action
Increase permeability helminth plasma membrane to Ca.
Contraction & spastic paralysis vesiculation &
vacuolization damage to the tegument of the worm.
Adverse effects
Mild GI disturbance, headache, dizziness
Therapeutic notes
After meal, 3x daily for 2 days only
Piperazine
Mechanism of action
Reversible neuromuscular blocker that causes a flaccid
paralysis in worms, leading to their expulsion by GI
peristalsis.
Adverse effects
Mild GI disturbance, neurotoxic effects (dizziness)
Therapeutic notes
Single dose, 1 7 days
Benzimidazoles
Mechanism of action
Bind to a site on tubulin dimers, preventing the
polymerization of microtubules. Potent, 250-400x in
helminth than mamalian tissues.
Adverse effects
GI disturbance, headache, dizziness, hepatotoxicity
Contraindication
Pregnant woman (teratogenic, embryotoxic)
Therapeutic notes
Single dose, 1 5 days
Diethylcarbamazine
Mechanism of action
Make parasites more susceptible to host immune
defences. Kill both microfilariae in the peripheral
circulation & adult worms in the lymphatic.
Adverse effects
Mild GI disturbance, headache, lassitude
Therapeutic notes
The initial dose is started low and then increased &
maintained for 21 days
Ivermectin
Mechanism of action
Immobilizes the worm by causing tonic paralysis
of the peripheral muscle system. Potentiating
the effect of -aminobutyric acid at worms
neuromuscular junction.
Adverse effects
Ocular irritation, transient
electrocardiographic changes & somnolence.
Levamizole

Mechanism of action
Stimulates nicotinic receptors at the
neuromuscular junction & results in a spastic
paralysis, which causes faecal worm expulsion

Adverse effects
Mild nausea & vomiting

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