Anthelminthic Drugs

By the end of the lecture, you will be able to:

• List the anthelminthic drugs of choice used for

the treatment of the following parasitic
infections:
• Taenia saginata (Tapeworm)
• Hymenolepis nana (Tapeworm)
• Describe their mechanism of action.
• Identify their distinctive toxicities.
 Introduction
Anthelminthic Drug of • Praziquantel
Choice: • Niclosamide

Alternate Drugs: • Mebendazole

 Praziquantel
Highly effective broad spectrum drug

Drug of choice for:

• Schistosomiasis
• Cysticercoids (infection with Taenia solium larvae)
• Tapeworm infections (Taenia saginata)
• Hydatidosis (Echynococcus garnulosus)
• Hymenolepis nana (dwarf tapeworm)
 Praziquantel
Acts by disrupting Ca2+ homeostasis in parasite at the
calcium channels. This induces an influx in the ion and
consequently a rapid prolonged contraction of the
musculature and eventual paralysis and death of the worm.

Praziquantel also disrupts the tegument of the parasite,

unmasking novel antigen, and as a result the parasite
become exposed to the host’s normal immune responses.
 Praziquantel
Given orally, well absorbed.

Rapid excretion in the urine- first pass effect.

A very safe drug.

Side effects are rare, transitory and of less clinical importance.

 Niclosamide
Widely used to treat:

• Tapeworm (Taenia saginata) together with praziquantel

• Hymenolepis nana (dwarf tapeworm)

Acts by inhibition of the parasite’s mitochondrial anaerobic phosphorylation

of ADP, which produces usable energy from ATP.

The scolex and the proximal segment of the worm are irreversibly damaged
by the drug, the worm then separates from the intestinal wall and expelled.
 Niclosamide
A laxative is administered before oral
administration of niclosamide

It is not lethal to ova

Unwanted effects:

• Few and transient

• Nausea and vomiting may occur
 Benzimidazoles
One of the principal anthelmintics groups.

Broad spectrum, they Include:

• Mebendazole
• Albendazole
• Thiabendazole
• Trichlabendazole

Administered orally
 Mebendazole

Synthetic benzimidazole

Used in ascariasis, trichuriasis, hookworm

and pinworm
 Benzimidazoles

Act by inhibiting the polymerization of the helminth

β-tubilin, thus interferring with microtubule-
dependent functions such as glucose uptake

Selective activity in producing activity in helminth

(250 – 400 times) than in mammalian tissue (selective
toxicity)
 Benzimidazoles
Few and transient side effects

Mebendazole may cause mild nausea, vomiting, diarrhea,

abdominal pain.

Rare side effects – hypersensitivity reactions (rash, urticaria),

agranulocytosis, alopecia, elevation of liver enzymes

Benzimedazoles should not be given to pregnant women and

children less than 2 years of age