Anti-helminthic Drugs

Introduction
• Antihelminthics are a group of antiparasitic
drugs that expel parasitic worms and other
internal parasites from the body either by
stunning or killing them and without causing
significant damage to the host. They may also
be called vermifuges (stunning) o vermicides
(killing).
• Greek word ‘Helminths mean worm’
• Helminths (worms) are multicellular organisms
 Introduction
• Helminthic infection is one of the most commonest
cause of iron deficiency anemia globally
• These infections impair child development by
constraining growth learning & school attendance
• Helminths can affect intestine as well as tissues of
other organs like skin, urinary tract, lung, liver
• We are more concerned about the helminths in
alimentary canal known as “worm infestation”
 Types of Helminthes
Roundworm (nematodes)
1. Ascaris lumbricoides (roundworm)
2. Trichuris trichura (whipworm)
3. Ancylostoma duodenale (hook worm)
4. Necator americanus (hookworm)
5. Enterobius vermicularis (pinworm)
6. Strongyloides stercoralis
(threadworm)
Flatworms
(a) Flukes (trematodes)
1. Schistosoma haematobium
2. Schistosoma japonicum
3. Clonorchis sinensis (liver fluke)
(b) Tapeworm (cestodes)
4. Taenia saginata (beef tapeworm)
5. Taenia solium (pork tapeworm)
6. Diphyllobothrium latum (fish
tapeworm)
7. Cysticercosis (pork tapeworm)
8. Hymenolepis nana (dwarf tapeworm)
9. Echinococcus granulosus (hydatid
disease)
Classification of Anti-helmintic Drugs

• According to mode of action

A. Inhibit ATP synthesis by inhibiting glucose
uptake
• Albendazole
• Mebendazole
• Thiabendazole
 Classification of Anti-helmintic Drugs
B. Paralysis of worm
• Parasitic neuromuscular blocker: Pyrantel pamote,
Levamisole, Piperazine,
• Increased influx of Chloride ion by activating
parasitic GABA: Ivermectin
• Increased permeability of cell membrane of worm
to Calcium: Praziquantel
C. Destroy scolex
• Niclosamide
 Classification of Anti-helmintic Drugs

According to types of helmintic infection

For nematodes For trematodes For cestodes
Albendazole Praziquantel Albendazole
Mebendazole Niclosamide
Triclabendazole
Diethylcarbamazine
Ivermectin
Pyrantel pamoate
Thiabendaole
Classification of Anti-helmintic Drugs

According to spectrum of drugs

Broad Spectrum Narrow Spectrum
Albendazole Piperazine
Mebendazole
Pyrantel pamoate
Praziquantel
Levamisol
 Albendazole
• Broad-spectrum oral antihelminthic, is a benzimidazole
carbamate
• Absorption is enhanced by the presence of fatty foods
• Rapidly undergoes first pass metabolism in the liver to
active metabolite albendazol sulfoxide
• Sulfoxide is mostly protein bound, distributes well to
tissues and enters bile, cerebrospinal fluid, and hydatid
cysts
• Plasma half life 8-12 hours
• Albendazole metabolites are excreted in the urine.
 Albendazole
• Mechanism of action
 Inhibit
– Microtubule polymerization by binding to ß-
tubulin of parasite
– Mitochondrial fumarate reductase
 Reduce glucose transport
 Uncoupling of oxidative phosphorylation
 Albendazole
• Therapeutic uses
1. Safe and highly effective against GI nematodes (Ascaris
lumbricoides, Trichuris trichiura, Enterobiasis vermicularis
and hookworms)
2. Cystic hydatid disease caused by Echinococcus granulosus
3. Alveolar echinococcous caused by Echinococcus
multilocularis
4. Neurocysticercosis caused by larval forms of Taenia solium
5. Empiric therapy to treat those who return from the
tropics with persistent unexplained eosinophilia
 Albendazole
• Adverse effects for short term use
1. Mild and transient epigastric distress
2. Diarrhea
3. Nausea
4. Dizziness
5. Lassitude
6. Insomnia
 Albendazole
Adverse effects for Long term use
(in case of the treatment for hydatid disease)
1. Abdominal distress
2. Headache
3. Fever
4. Fatigue
5. Alopecia
6. Increases in liver enzymes
7. Pancytopenia
 Albendazole
Cautions
Blood count
Liver function
Contraindication
Children below 2 years
Pregnancy
Known hypersensitivity to other benzimidazole
drug
Liver cirrhosis
 Mebendazole
• Synthetic benzimidazole
• Wide spectrum of antihelminthic activity
• Low systemic bioavailability (22%) due to poor absorption
and rapid first-pass metabolism at the intestinal wall and in
the liver
• Less than 10% of orally administered mebendazole is
absorbed
• Absorbed portion of mebendazole is about 95% bound to
plasma protein and extensively metabolized
• Excreated through bile
• Mechanism of action is same as albendazole
 Mebendazole
Therapeutic uses
• More prepherable in children.
• First line agent for the treatment of infections caused by ascariasis,
trichuriasis, hookworm and pinworm  
• For treatment of enterobiasis 100 mg tablet single dose, if the
patient is not cured a second dose shouldbe given after 3 weeks
• For control of ascariasis, trichuriasis, or hookworm infection, the
recommended regimen is 100 mg of mebendazole twice daily for
three consecutive days. If the person is not cured 3 weeks after
treatment, a second course should be given.  
• For intestinal capillariasis, 200 mg twice daily for 21 or more days
• In case of trichinosis 200 mg twice daily for 4 days.
 Mebendazole
Adverse effects
• Mild nausea
• Vomiting
• Diarrhea
• Abdominal pain
Contraindication
• Children below 2 years
• Pregnancy
 Levamisole
• Levamisole is a imidazole derivatives
cholinergic anthelminthic
• Quickly absorbed from GIT
• Plasma half life 4 hours
• Extensively metabolized in liver
 Levamisole
• Levamisole is a potent muscle and nerve L-subtype
selective nicotinic acetylcholine receptor channel
agonist. Opening of these channels produces
depolarization, calcium entry, and an increase in
sarcoplasmic calcium, producing spastic muscle
contraction, resulting in passive elimination of the
worms.
• Another mechanism is it also inhibit fumarate
reductase and hence succinate production what are
the main source of ATP
 Levamisole
Therapeutic uses
1. Excellent activity against ascaris lumbricoides
2. low to moderate efficacy against trichuris trichiura and
hookworm infections
3. Also been used for its immunomodulatory effects in cancer
Adverse effects
4. Severe adverse effect as agranulocytosis occur at high
dosages used for immunotherapy
5. Adverse effects for single low dosages are minor include
nausea, vomiting, headache, dizziness, or abdominal pain
 Pyrantel Pamoate
• Is the drug of choice for children below 2 years of
age
• Is a tetrahydropyrimidine derivative broad-
spectrum anthelminthic
• Poorly absorbed from the gastrointestinal tract
• Effective against mature and immature forms of
active luminal organism
• Major portion of the administered dose is
excreated through feces.
 Pyrantel Pamoate
Mechanism of action
• It is a depolarizing neuromuscular blocking
agents. Open nonselective cation channels and
inducepersistent activation of nicotinic
acetylcholine receptors and spastic paralysis of
the worm.
• It release of acetylcholine and inhibits
cholinesterase this results in paralysis of worms,
followed by expulsion.
 Pyrantel Pamoate
Therapeutic uses
1. Is an alternative to mebendazole or
albendazole for treatment of ascariasis and
enterobiasis.
2. Effective in the treatment of infections
caused by roundworms, pinworms, and
hookworms (ankylostoma duodenale,
necator americanus)
 Pyrantel Pamoate
Adverse effects
Nausea, vomiting, diarrhea, abdominal cramps
Dizziness, drowsiness, headache, insomnia
Rash
Fever and weaknessCaution
Caution
Patients with liver dysfunction should be used
with caution as transient aminotransferase
elevated.
 Available Preparation in Bangladesh
Drug Preparation Dose
Albendazole Tablet 400 mg
Suspension 200 mg/5 ml
Mebendazole Tablet 100 mg
Suspension 100 mg/5 ml
Levamisol Tablet 40 mg
Suspension 40 mg/5 ml
Pyrantel pamoate Suspension 50 mg/ml