Antihelmintics

Dr. Amisi
Helminthes(worms)
• Nematodes, trematodes, and cestodes are three major groups of
helminthes (worms) that infect humans.
• The worms usually infest the intestine but sometimes they may
invade the other organs.
• Most anthelmintics target eliminating the organisms from the host, as
well as controlling spread of infections
Classification of helminthes
• They are of two types:
● Nemathelminths (round bodied worms)
● Platyhelminths (flat-boddied worms)
Nematodes (Roundworms)

• The major nematode parasites of humans include the soil-transmitted

helminths (STHs; sometimes referred to as “geohelminths”) and the filarial
nematodes.
Examples of nematodes include:
• Round worms (Ascaris lumbricoides and Toxocara canis)
• Hookworms(Necator americanus, Ancylostoma duodenale)
• Whipworm (Trichuris trichiura)
• Threadworm (Strongyloides stercoralis)
• Pinworm (Enterobius vermicularis)
• Filarial worms (Wuchereria bancrofti, Brugia malayi, Brugia timori, Loa loa)
Trematodes (flukes)
Examples
• Schistosoma species (Schistosoma haematobium, Schistosoma
mansoni, Schistosoma japonicum)
Cestodes
Examples
• Taenea Solium (pork tape worm)
• Taenea saginata (beef tape worm)
• Diphylobothrium latum (fish tape worm)
Antihelmintic drugs
• Drugs used to get rid of helminths are called anthelminthic drugs
● They may be:
– Vermicide (kill)
– Vermifuge (expel)
Characteristics of ideal antihelmintics
• Orally effective in single dose
• Wide safety of margin with highest toxicity to worms
• Wide therapeutic index
• Broad spectrum activity
• Activity against mature and immature stages
• Single dose efficacy
• Ease of administration
• Economical
• Compatibility with other drugs
Drug classification
Drugs against Nematodes:
– Pyrantel pamoate
– Levamisole
– Piperazine
– Ivermectin
– Diethylcarobamazine
– Thiabendazole
Drugs against Trematodes

– Praziquantel
– Triclabendazole
Trematodes as well as cestodes

– Praziquantel
Drugs against Cestodes
– Niclosamide
Classification based on chemical structure
i. Benzimidazoles
ii. Imidathiazoles
iii. Tetrahydropyrimidines
iv. Piperazines
v. Avermectins
Benzimidazoles
• Albendazole, mebendazole, thiabendazole

Mechanism of action
• Inhibiting the assembly of the microtubules in the parasite
• Irreversibly blocking glucose uptake
Imidathiazoles
• Tetramisole
• Levamisole

Mechanism of action
The mechanism of action of levamisole as an antiparasitic agent
appears to be tied to its agonositic activity towards the L-subtype
nicotinic acetylcholine receptors in nematode muscles. This agonistic
action reduces the capacity of the males to control their reproductive
muscles and limits their ability to copulate
Tetrahydropyrimidines
• Morental, Pyrentel and Oxantel

Mechanism of action
• Act as a depolarizing, neuromuscular- blocking agent, causing release
of acetylcholine and inhibition of cholinesterase, leading to paralysis
of the worm
• The paralyzed worm releases its hold on the intestinal tract and is
expelled
Piperazines
• Piperazine salts (Phosphates, Citrate, Sulphate)

Mechanism of action
Piperazine is a GABA receptor agonist.
• Piperazines bind directly and selectively to muscle membrane GABA
receptors, presumably causing hyperpolarization of nerve endings,
resulting in flaccid paralysis of the worm. While the worm is
paralyzed, it is dislodged from the intestinal lumen and expelled live
from the body by normal intestinal peristalsis.
Avermectins
- Ivermectin
-Abamectin
-Doramectin

Mechanism of action
• Act on the glutamate-gated chloride channel receptors. Chloride
influx is enhanced, and hyperpolarization occurs, resulting in paralysis
and death of the worm
Ivermectin
• Active strongyloidiasis, and onchocerciasis (river blindness) caused by
Onchocerca volvulus (kills microfilariae but has no activity against
adult worms).
• Ivermectin is also useful in the treatment of pediculosis (lice) and
scabies.]
Praziquantel (T)
• Praziquantel is an agent of choice for the treatment of all forms of
schistosomiasis, other trematode infections, and cestode infections
such as taeniasis.

Mechanism of action
• Act by causing increased muscular activity, followed by contraction
and spastic paralysis.
Diethylcarbimazine
• Active against for filariasis caused by infection with Wuchereria
bancrofti and Brugia malayi.
• It kills the microfilariae and has activity against adult worms.
• Mechanism of action still not clear
Niclosamide
• An alternative to praziquantel for the treatment of taeniasis,
diphyllobothriasis and other cestode infections.

Mechanism of action
• It inhibits the mitochondrial phosphorylation of adenosine
diphosphate (ADP) in the parasite