ANTHELMINTIC DRUGS

RAMLA KASHIF
 WHAT ARE ANTHELMINTIC?

• Anthelmintic, any drug that acts against infections caused

by parasitic worms (helminths).

• Helminths can be divided into three groups: cestodes

or tapeworms; nematodes or roundworms; and
trematodes or flukes.
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• The helminths differ from other infectious organisms in that they have a complex

body structure.

• They are multicellular and have partial or complete organ systems (e.g., muscular,

nervous, digestive, and reproductive).

• Several of the drugs used to treat worm infections affect the nervous system of the

parasite and result in muscle paralysis.

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• Other drugs affect the uptake of glucose and thus energy stores.
• No anthelmintic is completely effective, completely without toxic effect
upon the host or equally active against all worms.
HELMINTHS
 CHEMOTHERAPY OF HELMINTIC
INFECTIONS

FOR NEMATODES FOR TREMATODES

• Diethylcarbamazine • Praziquantel
• Ivermectin

• Mebendazole
FOR CESTODES
• Albendazole
• Pyrantel pamoate
• Niclosamide
• Thiabendazole
 DRUGS FOR TREATMENT OF NEMATODES

• Nematodes are elongated roundworms that possess a complete digestive system.

• They cause infections of the intestine as well as the blood and tissues.

• Treatment of roundworms is complicated by the fact that some live in

blood, lymphatics, and other tissues and thus require use of drugs that are

absorbed from the intestinal tract and penetrate into tissues. Others are

found primarily or solely in the intestinal tract (intestinal nematodes).

 MEBENDAZOLE

• A synthetic benzimidazole compound.

• First-line agent for the treatment of infections caused by whipworms,
pinworms, hookworms and roundworms.
 MECHANISM OF ACTION

• It acts by inhibiting the assembly of the microtubules in the parasite

and also by irreversibly blocking glucose uptake.

• Affected parasites are expelled in the feces.

 ADVERSE EFFECTS
• Diarrhea
• Stomach pain, discomfort, or swelling
• Nausea
• Vomiting
• Loss of appetite
• Should be avoided in pregnancy (contraindicated)
 PYRANTEL PAMOATE

• Also effective in treatment of infections caused by roundworms,

pinworms and hookworms.

• It is poorly absorbed orally .

 MECHANISM OF ACTION
• It exerts its effect in the intestinal tract.
• Acts as a depolarizing, neuro-muscular-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.
 ADVERSE EFFECTS

• Nausea
• Vomiting
• Diarrhea
 THIABENDAZOLE

•A synthetic benzimidazole, a potent broad-spectrum anthelmintic

agent.

• Current use is limited to the topical treatment of cutaneous larva

migrans (creeping eruption).

• Largely replaced by other agents because of its toxic effects.

 IVERMECTIN

• Ivermectin is a broad-spectrum anti-parasitic agent, traditionally

against parasitic worms and other multicellular parasites.

• It is mainly used in humans in the treatment of river blindness and

other worm infestations like head lice, scabies, strongyloidiasis and
lymphatic filariasis (elephantiasis).
LYMPHATIC FILARIASIS
 MECHANISM OF ACTION

• Ivermectin targets the glutamate-gated chloride channel receptors.

• Chloride influx is enhanced and hyperpolarization occurs, resulting in
paralysis and death of the worm.
 PHARMACOKINETICS
• Given orally.
• Does not readily cross BBB.
• Biological half-life 18 hours
• Metabolized by liver
CONTRA-INDICATIONS:
• In pregnancy.
 ADVERSE EFFECTS

• Fever
• Headache
• Dizziness
• Somnolence
• Hypotension
 DIETHYLCARBAMAZINE

• Diethylcarbamazine is the drug of choice of filariasis caused by infection with

Wuchereria bancrofti and Brugia malayi.
• It kills the microfilariae and has activity against adult worms.
• In countries where filariasis is endemic, a combination of anti-filarial drugs(either
diethylcarbamazine and albendazole or ivermectin and albendazole) may be
used as preventive chemotherapy.
 PHARMACOKINETICS

• Rapidly absorbed after oral administration with meals.

• Excreted mainly in urine.

• ADVERSE EFFECTS:
• Fever
• Nausea/vomiting
• Arthralgia
• Headache
 CONTRA-INDICATIONS

• Diethylcarbamazine can accelerate blindness and cause severe Mazotti reactions

in patients with onchocerciasis so should be avoided in patients with this disorder.
 DRUGS FOR THE TREATMENT OF
TREMATODES

• The trematodes (flukes) are leaf-shaped flatworms.

• They are generally characterized by the tissues they infect for
example, liver, lung, intestinal or blood.
 PRAZIQUANTEL

• Drug of choice for the treatment of all forms of schistosomiasis,other trematode

infections and cestode infections such as taeniasis.
• Praziquantel is also used off-label in the treatment of cysticercosis caused by Taenia
solium larvae.
 MECHANISM OF ACTION

• Permeability of the cell membrane to calcium is increased ,causing contracture and

paralysis of parasite.

PHARMACOKINETICS:
• Rapidly absorbed after oral administration and distributes into CSF.
• Extensively metabolized by liver and excreted in the urine.
 ADVERSE EFFECTS

• Dizziness
• Malaise
• Headache
• GI upset
 DRUG-INTERACTION

• Grapefruit and grapefruit juice may interact with praziquantel and lead to potentially
dangerous effects.
• Dexamathasone, phenytoin, rifampin and carbamazepine may increase the
metabolism of praziquantel.
• Cimetidine increases praziquantel levels.
 CONTRA-INDICATIONS

• Praziquantel is contra-indicated for the treatment of ocular cysticercosis because

destruction of the organism in the eye may cause irreversible damage.
 DRUGS FOR THE TREATMENT OF
CESTODES

• The cestodes or true tapeworms typically have a flat, segmented body and attach to
the host’s intestine.
• Tapeworms lack a mouth and a digestive tract throughout their life cycle.
 NICLOSAMIDE

• Niclosamide is alternative to praziquantel for the treatment of

taeniasis, diphyllobothriasis and other cestode infections.
• It inhibits the mitochondrial phosphorylation of adenosine diphosphate (ADP) in the
parasite, making it lethal for the cestode’s scolex and segments but not for the ova.
• Anaerobic metabolism may also be inhibited.
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• A laxative is administered prior to oral administration to purge the bowel of all dead
segments and to enhance digestion and liberation of the ova.
• Alcohol should be avoided within 1 day of niclosamide use.
 ALBENDAZOLE

• Albendazole is an another benzimidazole.

• It is effective against most nematodes known.
• Its primary therapeutic application is in the treatment of cestodal infestations such as
cysticercosis and hydatid disease caused by larval stage of Echinococcus
granulosus.
• It inhibits micro-tubule synthesis and glucose uptake in nematodes.
 PHARMACOKINETICS

• Albendazole is erratically absorbed after oral administration but absorption is

enhanced by a high-fat-meal.
• Distributes widely including CSF.
• Undergoes extensive first-pass metabolism, including formation of an active
sulfoxide.
• Excreted in bile.
 ADVERSE EFFECTS

• Headache
• Nausea
• Risk of hepatotoxicity (treatment of hydatid disease 3 months)
• Agranulocytosis (rarely)
• Pancytopenia (rarely)