7/17/2014

Anti-Helminthic Drugs

MBCHB 3
17 July 2014

Introduction
Helminths (worms) are multicellular organisms

Over 1 billion people are infected with intestinal nematodes,

and many millions are infected with filarial nematodes, flukes,
and tapeworms

Main goals of treatment are:

control of infection
elimination of parasites (frequent reinfection in endemic areas)
controlling disease symptoms
decreasing the transmission of infection

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Roundworms (Nematodes) Drug of Choice Alternative drug

Ascaris lumbricoides Albendazole or Ivermectin,
(roundworm) pyrantel pamoate or piperazine
mebendazole
Trichuris trichiura Mebendazole or Ivermectin
(whipworm) albendazole
Necator americanus Albendazole or
(hookworm); Ancylostoma mebendazole or
duodenale (hookworm) pyrantel pamoate
Strongyloides stercoralis Ivermectin Albendazole or
(threadworm) thiabendazole
Enterobius vermicularis Mebendazole or Albendazole
(pinworm) pyrantel pamoate
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Albendazole
Albendazole, a broad-spectrum oral antihelminthic

Pharmacokinetics
Arbsoption is increased with a fatty meal
Undergoes rapid first-pass metabolism in the liver to the active
metabolite albendazole sulfoxide
Plasma half-life is 812 hours

Antihelminthic Actions
Acts against nematodes by inhibiting microtubule synthesis
Albendazole also has larvicidal effects in hydatid disease,
cysticercosis, ascariasis, and hookworm infection and ovicidal effects
in ascariasis, ancylo-stomiasis, and trichuriasis 4

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Albendazole
Clinical Uses
Administered on an empty stomach when used against intraluminal
parasites but with a fatty meal when used against tissue parasites

Ascariasis, Trichuriasis, Hookworm, and Pinworm Infections

For adults and children older than 2 years of age with ascariasis and
hookworm infections - a single dose of 400 mg orally (repeated for 2
3 days for heavy ascaris infections and in 2 weeks for pinworm
infections)

For trichuriasis - three daily 400-mg oral doses of albendazole

Albendazole
Clinical Uses
Administered on an empty stomach when used against intraluminal
parasites but with a fatty meal when used against tissue parasites
Hydatid Disease
Albendazole is the treatment of choice 400mg twice a day for one
month or more
Neurocysticercosis
Corticosteroids are usually given with the antihelminthic drug to
decrease inflammation caused by dying organisms
Albendazole - 400 mg twice a day for up to 21 days (drug of choice over
praziquantel because of its shorter course, lower cost, improved penetration into
the subarachnoid space, and increased drug levels when administered with
corticosteroids)
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Albendazole
Other Infections
Albendazole is the drug of choice in the treatment of:
cutaneous larva migrans (400 mg daily for 3 days)
visceral larva migrans (400 mg twice daily for 5 days)
intestinal capillariasis (400 mg daily for 10 days)
microsporidial infections (400 mg twice daily for 2 weeks or longer)
gnathostomiasis (400 mg twice daily for 3 weeks)

Albendazole
Adverse Drug Reactions
Mild and transient epigastric distress
Diarrhea
Headache
Nausea and dizziness
Lassitude
Insomnia
Blood counts and liver function studies should be monitored during
long-term therapy

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Mebendazole
Mebendazole is a synthetic benzimidazole that has a wide spectrum of
antihelminthic activity and a low incidence of adverse effects

Pharmacokinetics
Less than 10% of orally administered mebendazole is absorbed
half-life of 26 hours
Urine excretion
Absorption is increased if the drug is ingested with a fatty meal

Antihelminthic Actions
Acts by inhibiting microtubule synthesis
Kills hookworm, ascaris, and trichuris eggs 9

Mebendazole
Clinical Uses
Pinworm infections - 100 mg once, repeated at 2 weeks

Ascariasis, trichuriasis, hookworm, and trichostrongylus

infections - 100 mg twice daily for 3 days

Intestinal capillariasis - 200 mg twice daily for 21 or more

days

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Mebendazole
Adverse Drug Reactions
Mild nausea, vomiting, diarrhea
abdominal pain
hypersensitivity reactions (rash, urticaria)
Agranulocytosis
Alopecia
Elevation of liver enzymes
Teratogenic in animals and therefore contraindicated in pregnancy

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Praziquantel
Effective in the treatment of schistosome infections of all species
and most other trematode and cestode infections, including
cysticercosis
Pharmacokinetics
Rapidly absorbed, with a bioavailability of about 80%
80% of the drug is bound to plasma proteins
half-life is 0.81.5 hours

Antihelminthic Actions
Increase the permeability of trematode and cestode cell membranes
to calcium, resulting in paralysis, dislodgement, and death
Effective against adult worms and immature stages
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Praziquantel
Clinical Uses
Praziquantel tablets are taken with liquid after a meal; they should be
swallowed without chewing because their bitter taste can induce retching
and vomiting

Schistosomiasis
40 mg/kg per dose for two (S. mansoni and S. haematobium) or three (S.
japonicum and S. mekongi) doses at intervals of 46 hours

Clonorchiasis, Opisthorchiasis, and Paragonimiasis

Standard dosing is 25 mg/kg three times daily for 2 days

Taeniasis and Diphyllobothriasis

A single dose of praziquantel, 510 mg/kg
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Praziquantel
Neurocysticercosis
Albendazole is now the preferred drug
100 mg/kg/d in three divided doses for 1 day, then 50 mg/kg/d to
complete a 2- to 4-week course

H. nana
A single dose of 25 mg/kg is taken initially and repeated in 1 week

Hydatid Disease
In hydatid disease, praziquantel kills protoscoleces but does not
affect the germinal membrane

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Praziquantel
Adverse Reactions
headache, dizziness
drowsiness, and lassitude
nausea, vomiting, abdominal pain
loose stools, pruritus, urticaria
arthralgia, myalgia, and low-grade fever

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Flukes (Tematodes) Drug of Choice Alternative drug

Schistosoma haematobium Praziquantel Metrifonate

(bilharziasis)

Schistosoma mansoni Praziquantel Oxamniquine

Schistosoma japonicum Praziquantel

Paragonimus westermani (lung Praziquantel Bithionol

fluke)

Fasciolopsis buski (large Praziquantel or

intestinal fluke) niclosamide

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Tapeworms Drug of Choice Alternative drug

Taenia saginata (beef Praziquantel or niclosamide Mebendazole

tapeworm)

Diphyllobothrium latum Praziquantel or niclosamide

(fish tapeworm)

Taenia solium (pork Praziquantel or niclosamide

tapeworm)

Hymenolepis nana (dwarf Praziquantel

tapeworm)

Echinococcus granulosus Albendazole Praziquantel

(hydatid disease);
Echinococcus multilocularis
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Niclosamide
Niclosamide is a second-line drug for the treatment of most
tapeworm infections

Pharmacokinetics
It is minimally absorbed from the gastrointestinal tract

Antihelminthic Actions
Adult worms (but not ova) are rapidly killed by inhibition of
oxidative phosphorylation or stimulation of ATPase activity

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Niclosamide
Adverse Reactions, Contraindications, & Cautions
Infrequent, mild, and transitory adverse events:
oNausea
oVomiting
oDiarrhea
oAbdominal discomfort
oThe consumption of alcohol should be avoided on the day of
treatment and for 1 day afterward

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References
Basic and Clinical Pharmacology, 11th edition; by B G Katzung

Applied Therapeutics-Clinical Uses of drugs, 9th edition; M A Koda-

Kimble

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