Pharmacology (dra Dando)

Anti-Helminthics
30 January 08

C. Neurocysticercosis
CHEMOTHERAPY OF HELMINTHIC INFECTIONS ⇒ Therapy most appropriate for
symptomatic parenchymal or
intraventricular cysts
Albendazole
⇒ Corticosteroids + Anthelminthic drugs 
decrease inflammation caused by dying
• Broad spectrum oral anthelminthic
organism
• DOC: treatment of hydatid disease and ⇒ Albendazole: DOC because of its shorter
cysticercosis course, lower cost, improved penetration
• Also used in the treatment of pinworm and into the subarachnoid space, and
hookworm infections, ascariasis, trichuriasis, and increased drug levels when administered
strongyloidiasis with corticosteroids
⇒ Dose: 400 mg twice a day for up to 21
Chemistry and Pharmacokinetics days
• Benzimidazole carbamate D. Other Infections
• After oral administration, it is erratically absorbed ⇒ DOC for cutaneous larva migrans (400
(increased with a fatty meal) mg daily for 3 days), for visceral larva
• Rapidly undergoes 1st pass metabolism in the liver migrans (400 mg twice daily for 5 days),
to the active metabolite albendazole sulfoxide for intestinal capillariasis (400 mg
(mostly protein-bound, distributes well to tissues, daily for 10 days), for microsporidial
and enters bile, CSF, and hydatid cysts) infections (400 mg twice daily for 2
• Reaches variable maximum plasma weeks or longer) and for
concentrations about 3 hours after a 400 mg oral gnathostomiasis (400 mg twice daily for
dose 3 weeks)
• Plasma half-life: 8-12 hours ⇒ Also has activity against trichinosis (400
• Excreted in the urine mg twice daily for 1-2 weeks) and
clonorchiasis (400 mg twice daily for 1
week)
Anthelminthic Actions
⇒ Reports of effectiveness in treatment of
• Act against nematodes by inhibiting opisthorciasis, toxocariasis, and loiasis
microtubule synthesis ⇒ Conflicting reports of effectiveness in
• Larvicidal effects in hydatid disease, giardiasis and taeniasis
cystecercosis, ascariasis and hookworm infection ⇒ Included in some programs to control
• Ovicidal effects in ascariasis, ancyclostomiasis, lymphatic filariasis
and trichuriasis
Adverse Reactions, Contraindications, and
Clinical Uses Cautions
• Administered on an empty stomach when used • When used 1-3 days, nearly free of significant
against intraluminal parasites adverse effects
• Administered with a fatty meal when used against • Mild and transient epigastric distress, diarrhea,
tissue parasites headache, nausea, dizziness, lassitude, and
A. Ascariasis, Trichuriasis, and Hookworn and insomia
Pinworm Infections • Long-term use for hydatid disease: well-tolerated
⇒ adults & children > 2 y/o: single dose of but can cause abdominal distress, headaches,
400 mg orally fever, fatigue, alopecia, increases in liver
⇒ repeated for 2-3 days: heavy ascaris enzymes, and pancytopenia
infection and in 2 weeks for pinworm • After long-term therapy: Blood counts and Liver
infections Functions Studies
B. Hydatid Disease • Not for patients with known hypersensitivity to
⇒ Treatment of choice for medical therapy other benzimidazole drugs or to those with
and is a useful adjunct to surgical removal cirrhosis
or aspiration of cysts • Safety in pregnancy and in children < 2 y/o has
⇒ More active against Echinococcus not been established
granulosus than E. multilocularis
⇒ Dose: 400 mg twice daily with meals for 1 Bithionol
month or longer
⇒ Therapeutic strategy: Albendazole + • DOC: Treatment of Fascioliasis (Sheep Liver
Praziquantel  to assess response after 1 Fluke)
month or more  manage
Marco, farsi, jassie, april, viki 1 of 7
 Pharmacology – Anti-helminthics by Dra Dando
• Alternative drug in the treatment of Pulmonary
Paragonimiasis
Pharmacokinetics
• After ingestion, reaches peak blood levels in 4-8
hours
• Excretion via kidneys
Clinical Uses
• Dose: 30-50 mg/kg in 2-3 divided doses, given
orally after meals on alternate days for 10-15
doses
Adverse Reactions, Contraindications, and
Cautions
• Occur in up to 40% of patients
• Generally mild and transient, but occasionally
their severity requires interruption of therapy
• Includes diarrhea, abdominal cramps, anorexia,
nausea, vomiting, dizziness and headache
• Skin rashes: after a week of more of therapy 
reaction to antigens released from dying worms
• Used with caution in children < 8 y/o
Diethylcarbamazine Citrate
• DOC: Treatment of Filariasis, Loiasis and Tropical
eosinophilia
• Replaced by Ivermectin for treatment of
Onchocerciasis
Chemistry and Pharmacokinetics
• Synthetic piperazine derivative
• Marketed as a citrate salt
• Rapidly absorbed from the GIT
• After a 0.5 mg/kg dose, peak plasma levels are
reached within 1-2 hours
• Half-life: 2-3 hours in acidic urine, 10 hours in
alkaline urine
• Rapidly equilibrates with all tissues except fat
• Excretion principally in the urine as unchanged
drug and the N-oxide metabolite
• Reduce dosage in patients with persistent urinary
alkalosis or renal impairment
Anthelminthic Actions
• Immobilizes microfilariae and alters their surface
structure, displacing them from tissues and
making them more susceptible to destruction by
host defense mechanisms
• MOA against adult worms: unknown
Clinical Uses
• Should be taken after meals
A. Wuchereria bancrofti, Brugia malayi, Brugia
timori, and Loa Loa
⇒ It is the DOC foe treatment of infections
with these parasites because of its
efficacy and lack of serious toxicity
⇒ Microfilariae of all species are rapidly
killed, adult parasites killed more slowly
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 often requiring several courses of
treatment
⇒ Highly effective against adult L. loa
⇒ These infections are treated for 2 or 3
weeks (for L. loa), with initial low doses to
reduce the incidence of reaction to dying
microfialriae
⇒ 50 mg (1 mg/kg in children) on day 1,
three 50 mg doses on day 2, three 100
mg doses (2 mg/kg in children in day 3,
and then 2 mg/kg three times per day to
complete the 2-3 week course
⇒ Antihistamines: 1st few days of therapy 
limit allergic reactions and corticosteroids
should be started
⇒ May also be used for chemoprophylaxis
(300 mg weekly or 300 mg on 3
successive days each month for loiasis;
50 mg monthly for Bancroftian and
Malayan filariasis)
B. Other Uses
⇒ For tropical eosinophilia: orally, 2 mg/kg
3x daily for 7 days
⇒ Effective in Mansonella streptocerca
infections, since it kills both adults and
microfilariae
⇒ Important application: mass treatment of
W. bancrofti infections to reduce
transmission
Adverse Reactions, Contraindications, and
Cautions
• Generally mild and transient
• Headache, malaise, anorexia, weakness, nausea,
vomiting and dizziness
• Adverse effects occur as a result of the release of
proteins from dying microfilariae or adult worms
• Reactions to dying microfilariae: mild in W.
bancrofti, more intense in B. malayi and
occasionally severe in L. loa  fever, malaise,
popular rash, headache, GI symptoms, cough,
chest pain, and muscle or joint pain
• Leukocytosis is common
• Eosinophilia may increase in treatment
• Retinal hemorrhages, and rarely, encephalopathy
have been described
• Between 3rd and 12th days of treatment, local
reactions may occur in the vicinity of dying adult
or immature worms  lymphangitis with localized
swellings and flat papules
• Caution in patients with hypertension or renal
disease
Doxycycline
• Tetracycline antibiotic
• Significant macrofilaricidal activity against W.
bancrofti
• Activity also seen against onchocerciasis
• Acts indirectly, by killing Wolbachia, an
intracellular bacterial symbiont of filarial parasites
Pharmacology – Anti-helminthics by Dra Dando
• May prove to be an important drug for filariasis,
both for treatment of active disease and in mass
chemotherapy campaigns
Ivermectin
• DOC: Strongyloidiasis and Onchocerciasis
• Also an alternative drug for a number
helminthic infections
Chemistry and Pharmacokinetics
• Semisynthetic macrocyclic lactone
• Mixture of: Avermectin B1a and B1b
• Derived from soil actinomycete Streptomyces
avermilitis
• Used only orally and rapidly absorbed, reaching
maximum plasma concentration 4 hours after a
12 mg dose
• Has a wide tissue distribution and a volume of
distribution of about 50L
• Half-life: 16 hours
• Excretion of drug and its metabolite: feces
Anthelminthic Actions
• Paralyze nematodes and arthropods by
intensifying GABA-mediated transmission of
signals in peripheral nerves
• In onchocerciasis, it is microfilaricidal
• It does not effectively kill the adult worms but
blocks the release of microfilariae for some
months after therapy
• With repeated doses, the drug does appear to
have a low-level macrofilaricidal action and to
permanently reduce microfilarial production
Clinical Uses
A. Onchocerciasis
⇒ Single oral dose, 150 mcg/kg, with water
on an empty stomach
⇒ Doses are repeated; regimens vary from
monthly to less frequent (every 6-12
months) dosing schedules
⇒ After acute therapy, treatment
repeated at 12-month intervals until the
adult worms die, which may take 10 years
or longer.
⇒ With the 1st treatment only, patients with
microfilariae in the cornea or anterior
chamber may be treated with
corticosteroids to avoid inflammatory eye
reactions
⇒ Ivermectin also now plays a key role
B. Stronglyloidasis
⇒ Two daily doses of 250 mcg/kg
⇒ In immunosuppresed patients with
disseminated infection, repeated
treatment is often needed,but cure may
not be possible  suppressive therapy
C. Other Parasites
⇒ Reduces microfilariae in Brugia malayi
and M. ozzardi infections but not in M.
perstans infections.
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⇒ Used with diethylcarbamazine for the
control of W. bancrofti, but it does not kill
adult worms
⇒ In loiasis, although the drug reduces
microfilaria concentrations, it can
occasionally induce severe reactions
⇒ Also effective in controlling scabies, lice,
of and cutaneous larva migrans and in
eliminating a large proportion of ascarid
worms.
Adverse Reactions, Contraindications, and
Cautions
• In strongyloidiasis, infrequent side effects include
fatigue, dizziness, nausea, vomiting, abdominal
pain, and rashes.
• In onchocerciasis, the adverse effects are
principally from the Mazotti reaction, due to the
killing of microfilariae  fever, headache,
dizziness, somnolence, weakness, rash, increased
pruritus, diarrhea, joint and muscle pains,
hypotension, tachycardia, lymphadenitis,
lymphangitis, and peripheral edema  starts on
the 1st day and peaks on the 2nd day of treatment
• Some develop corneal opacities and other eye
lesions several days after treatment  rarely
severe and generally resolve without
corticosteroid treatment
• Best to avoid concomitant use of ivermectin and
other drugs that enhance GABA activity
(barbiturates, benzodiazepines and valproic acid)
• Should not be used in pregnancy
• Safety in children younger than 5 years has not
been established
Mebendazole
• Synthetic benzimidazole
• Wide spectrum of antihelminthic activity and a
low incidence of adverse effect
Chemistry and Pharmacokinetics
is • Less than 10% of orally administered
mebendazole is absorbed
• The absorbed drug is protein-bound, rapidly
converted to inactive metabolites (1st pass in the
liver)
• Half-life: 2-6 hours
• Excretion: urine  as decarboxylated derivatives
• Absorption: increase with fatty acids
Anthelminthic Actions
• Acts by inhibiting microtubule synthesis
• Parent drug = active form
• Efficacy varies with gastrointestinal transit time,
with intensity of infection, and perhaps with the
strain of parasite
• Kills hookworm, ascaris and trichuris eggs
Clinical Uses
• For use in ascariasis, trichuriasis, hookworm and
pinworm infections
 Pharmacology – Anti-helminthics by Dra Dando
• Can be taken before or after meals, the tablets
should be chewed before swallowing
• Pinworm infections: 100 mg once, repeated at 2
weeks
• Ascariasis, trichuriasis, hookworm and
trichostrongylus infections: 100 mg twice daily for
3 days (adults and children < 2y/o)
• Intestinal capillariasis: 400 mg/d in divided doses
for 21 or more days
• Trichinosis: efficacy against adult worms in the
intestinal tract and tissue larvae  3x daily with
fatty foods, at 200-400 mg/dose for 3 days and
then 400-500 mg/dose for 10 days
• For severe infections: with corticosteroids
Adverse Reactions, Contraindications, and
Cautions
• Short-term therapy for intestinal nematodes:
nearly free of adverse effects
• Mild nausea, vomiting, diarrhea and abdominal
pain
• High-dose therapy: hypersensitivity reactions
(rash, urticaria), agranulocytosis, alopecia, and
elevation of liver enzymes
• Contraindicated in pregnancy (teratogenic in
animals)
• Caution in children < 2 y/o (convulsions) and
patients with cirrhosis
• Plasma levels may be decreased with
concomitant use of Carbamazepine or
Phenytoin ; and increased by Cimetidine
Metrifonate (Trichlorfon)
• Safe, low cost, alternative drug for Schistosoma
haematobium infections
• Not active against S. mansoni or S. japonicum
Chemistry and Pharmacokinetics
• Organophosphate compound (cholinergic 
inhibit acetyl cholinesterase)
• Rapidly absorbed after oral administration
• Following the standard oral dose, peak blood
levels are reached in 1-2 hours
• Half-life: 1.5 hours
• Clearance: nonenzymatic transformation to
dichlorvos (active metabolite)
• Metrifonate ad dichlorvos: well distributed to
thetissues and are completely eliminated in 24-48
hours
Anthelminthic Actions
• Related to cholinesterase inhibition
• Temporarily paralyzes the adult worms, resulting
in their shift from the bladder venous plexus to
small arterioles of the lungs, where they are
trapped, encase by the immune system, and die
• Not effective against S. haematobium eggs
Clinical Uses
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• Single oral dose, 7.5-10 mg/kg is given 3 times at
14-day intervals
• As prophylactic agent when given monthly to
children in a highly endemic area
• Used in mass treatment programs
• In mixed infections with S. haematobium and S.
mansoni: combined with oxamniquine
Adverse Reactions, Contraindications, and
Cautions
• Mild and transient cholinergic symptoms 
nausea and vomiting, diarrhea, abdominal pain,
bronchospasm, headache, sweating, fatigue,
weakness, dizziness, and vertigo
• May begin within 30 minutes and persist up to 12
hours
• Should not be used after recent exposure to
pesticides or drugs that might potentiate
cholinesterase inhibition
• Contraindicated in pregnancy
Niclosamide
• 2nd line for treatment of most tapeworm infections
Chemistry and Pharmacokinetics
• Salicylamide derivative
• Minimally absorbed from the GIT – neither the
drug nor its metabolites have been recovered
from the blood or urine
Anthelmintic Actions
• Adult worms (but not ova) are rapidly killed,
pesumambly due to inhibition of oxidative
phosphorylation or stimulation of ATPase activity
of worms
Clinical Uses
• Adult dose: 2 g once, given in the morning on an
empty stomach
• Tablets must be chewed thoroughly and are then
swallowed with water
A. Taenia Saginata (beef tapeworm), T. solium
(pork tapeworm), Diphyllobothrium latum
(fish tapeworm)
⇒ Single 2 g dose
⇒ Cysticercosis is theoretically possible after
treatment of T. solium infections, because
viable ova are released into the gut lumen
following digestion of segments
B. Other Tapeworms
⇒ H. diminuta and Dipylidium caninum
infections are cured with a 7-day course
of treatment; a few require a second
course
⇒ Praziquantel is superior for
Hymenolepis nana (dwarf tapeworm)
infection
⇒ Not effective against cysticercosis or
hydatid disease
C. Intestinal Fluke Infections
Pharmacology – Anti-helminthics by Dra Dando
⇒ Used as an alternative drug in the
treatment of Fasciolopsis buski,
Heterophyes heterophyes, Metagonimus
yokogawai infections
⇒ Standard dose is given every other day
for 3 doses
Adverse Reactions, Contraindications, and
Cautions
• Infrequent, mild, and transitory adverse events 
nausea, vomiting, diarrhea, and abdominal
discomfort
• Consumption of alcohol should be avoided on the
day of treatment and after 1 day
• Safety not established in pregnancy and children
< 2 y/o
Oxamniquine
• Alternative to Praziquantel for treatment of S.
mansoni infections
• Also been used extensively for mass treatment
• Not effective against S. haematobium or S.
japonicum
Pharmacokinetics
• Semisynthetic tetrahydroquinoline
• Readily absorbed orally
• Half-life: 2.5 hours
• Extensively metabolized to inactive metabolites
and excreted in the urine – up to 75% in the first
24 hours
Anthelminthic Actions
• Active against both mature and immature stages
of S. mansoni but does not appear to be
cercaricidal
• MOA: unknown
• Contraction and paralysis of the worms results in
detachment from terminal venules in the
mesentery and transit to the liver, where many
die; surviving females return to the mesenteric
vessels but cease to lay eggs.,
• Effective in instances of Praziquantel resistance
Clinical Uses
• Safe and effective in all stages of S. mansoni
disease, including advanced hepatosplenomegaly
• In the acute (Katayama) Syndrome  treatment
results in disappearance of acute symptoms and
clearance of the infection
• Less effective in children, who require higher
doses than adults
• Better tolerated with food
• In mixed schistosome infections: successful
combination with Metrifonate
Adverse Reactions, Contraindications, and
Cautions
• Mild symptoms, starting about 3 hours after a
dose and lasting for several hours
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• CNS symptoms (dizziness, headache, drowsiness
 most common), nausea and vomiting, diarrhea,
colic, pruritus, and urticaria also occur
• Infrequent adverse effects are low-grade fever, an
orange to red discoloration of the urine,
proteinuria, microscopic hematuria, and a
transient decrease in leukocytes
• Seizures: rare
• Used with caution in patients whose work or
activity requires mental alertness (no driving for
24 hours) and with those with a history of
epilepsy
• Contraindicated in pregnancy
Piperazine
• Alternative for the treatment for ascariasis
• Not recommended for other helminth infections
• Available as the hexahydrate and as a variety of
salts
• Readily absorbed, and maximum plasma levels
are reached in 2-4 hours
• Excreted unchanged in the urine in 2-6 hours, and
the excretion is complete within 24 hours
• Causes paralysis of ascaris by blocking
acetylcholine at myoneural junction; unable to
maintain their position in the host, live worms are
expelled by normal peristalsis
• Dose for Ascariasis: 75 mg/kg (maximum dose,
3.5 g) orally once daily for 2 days
• Dose for heavy infections: treatment should be
continued for 3-4 days or repeated after 1 week
• Occasionally mild adverse effects include
nauseas, vomiting, diarrhea, abdominal pain,
dizziness, and headache
• Neurotoxicity and allergic reactions are rare
• Should not be given to women during pregnancy,
to patients with impaired renal or hepatic
function, or to those with a history of epilepsy or
chronic neurologic disease
Praziquantel
• Treatment of Schistosome infections of all species
and most other trematode and cestode infections,
including cysticercosis
• Drug’s safety and effectiveness as a single oral
dose have also made it useful in mass treatment
of several infections
Chemistry and Pharmacokinetics
• Synthetic isoquinoline-pyrazine derivative
• Rapidly absorbed: 80% bioavailability after oral
administration
• Peak serum concentrations: 1-3 hours after a
therapeutic dose
• CSF concentrations of Praziquantel: 14-20% of
the drug’s plasma concentration
• 80%: bound to plasma protein
• Rapidly metabolized to inactive mono- and poly-
hydroxylated products after a 1st pass in the liver
• Half-life: 0.8-1.5 hour
Pharmacology – Anti-helminthics by Dra Dando
• Excretion: via kidneys and bile
• Increase plasma concentration with increase
carbohydrate diet or with Cimetidine
• Bioavailability is markedly reduced with some
antiepileptics (phenytoin, carbamazepine) or
with corticosteroids
Anthelmintic Actions
• Paralysis, dislodgement and death  by
increasing the permeability of trematodes and
cestodes cell membranes to calcium
• Effective against adult worms and immature
stages
• Prophylactic effect against cercarial infection
Clinical Uses
• Taken with liquid after a meal
• Swallowed without chewing because their bitter
taste can induce retching and vomiting
A. Schistosomiasis
⇒ DOC for all forms of schistosomiasis
⇒ Dose: 20 mg/kg for 2 or 3 doses at
intervals of 4-6 hours
⇒ Effective in adults and children and is
generally well tolerated by patients in the
hepatosplenic stage of advanced disease
⇒ For S. mansoni drug resistance:
Oxamniquine
⇒ As chemoprophylaxis: not established
B. Clonorchiasis, Opisthorchiasis, and
Paragonimiasis
⇒ Dose: 25 mg/kg 3x for 1 day results in
nearly 100% cure rates for clonorchiasis
and opisthorchiasis
⇒ A 2 day course provides 90-100% cure
rates for pulmonary paragonimiasis
C. Taeniasis and Diphyllobothriasis
Pyrantel Pamoate
⇒ Single dose: 5-10 mg/kg
⇒ Does not kill eggs  larvae of T. solium
released from eggs in the large bowel
could penetrate the intestinal wall and
give rise to cysticercosis
D. Neurocysticercosis
⇒ Similar efficacy to Albendazole
(preferred drug)
⇒ Dose: 50 mg/kg/d in 3 divided doses for
14 days or longer
⇒ Has diminished bioavailability when taken
concurrently with a corticosteroid
E. H. nana
⇒ DOC for H. nana infections and the 1st
drug to be highly effective
⇒ Single dose of 25 mg/kg is taken initially
and repeated in 1 week
F. Hydatid Disease
⇒ Kills protoscoleces but does not affect the
germinal membrane
⇒ Being evaluated as an adjunct with
albendazole pre- and postsurgery
⇒ Enhances the plasma concentration of
albendazole sulfoxide
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G. Other Parasites
⇒ Fasciolopsiasis, Metagonimiasis, and other
forms of heterophyiasis  Limited trials at
dosage of 25mg/kg 3x a day for 1-2 days
⇒ Not effective for fascioliasis, however,
even at dosages as high as 25 mg/kg 3x
daily for 3-7 days
Adverse Reactions, Contraindications, and
Cautions
• Mild and transient adverse effects are common
• Begin within several hours after ingestion and
may persist for hours to 1 day
• Most frequent: headache, dizziness, drowsiness,
and lassitude
• Others include nausea, vomiting, abdominal pain,
loose stools, pruritus, urticaria, arthralgia,
myalgia and low-grade fever
• Mild and transient elevation of liver enymes
• Several days after starting: low-grade fever,
pruritus, and skin rashes (macular and urticarial),
sometimes associated with worsened eosinophilia
 due to realease of proteins from dying worms
• In neurocysticercosis, neurologic abnormalities
may be exarcebated by inflammatory reactions
around dying parasites  use with
Corticosteroids to decrease the inflammatory
reaction
• Contraindicated in ocular cysticercosis (parasite
destruction in the eye may cause irreparable
damage)
• Avoid: pregnant, children < 4 y/o
• Patients should not drive during therapy and
should be warned regarding activities requiring
particular physical coordination or alertness 
dizziness and drowsiness
• Broad spectrum anthelminthic
• Highly effective for the treatment of pinworm,
ascaris, and trichostrongylus orientalis infections
• Moderately effective against both species of
hookworm
• Not effective in trichuriasis or strongyloidiasis
• Oxantel pamoate: analog of pyrantel used as
treatment of trichuriasis
• 2 drugs combined (pyrantel land oxantel): broad-
spectrum
Chemistry and Pharmacokinetics
• Tetrahydropyrimidine derivative
• Poorly absorbed form the GIT
• Active mainly against luminal oraganisms
• Peak plasma levels are reached in 1-3 hours
• Over-half of the administered dose is recovered
unchanged in the feces
Anthelminthic Actions
• Effective against mature and immature forms of
susceptible helminthes within the intestinal tract
Pharmacology – Anti-helminthics by Dra Dando Page 7 of 7

but not against migratory stages in the tissues or
against ova
• A neuromuscular blocking agent that causes
release of acetylcholine and inhibition of
cholinesterase  results in paralysis, which is
followed by expulsion of worms
Clinical Uses
• Dose: 11 mg/kg (maximum, 1 g) orally once with
or without food
• For pinworm: dose is repeated in 2 weeks
• For ascariasis: single dose  85-100% cure rates
 treatment should be repeated if eggs are found
2 weeks after treatment
• For hookworm infections: single dose is effective
against light infections, but not for heavy
infections, esp. with N. americanus  3-day
course is necessary to reach 90% cure rates 
course treatment can be repeated in 2 weeks
Adverse Reactions, Contraindications, and
Cautions
• Infrequent, mild and transient  nausea,
vomiting, diarrhea, abdominal cramps,
drowsiness, headache, insomnia, rash, fever, and
weakness
• Caution: patient with liver dysfunction  because
of low, transient aminotransferase elevations
• Experience with the drug in pregnant women and
children younger than 2 years of age is limited
• For strongyloides infection: treatment is for 2
days
• For hyperinfection syndrome: standard dose is
continued twice daily for 5 -7 days
• For cutaneous larva migrans: cream can be
applied topically or the oral drug can be given for
2 days (Albendazole  preffered, less toxic)
Adverse Reactions, Contraindications, and
Cautions
• Much more toxic than other benzimidazoles or
ivermectin
• Common adverse effects: dizziness, anorexia,
nausea and vomiting
• Less frequent problems: epigastric pain,
abdominal cramps, diarrhea, pruritus, headache
and drowsiness, and neuropsychiaitric symptoms
• Fatal Steven-Johnson syndrome and irreversible
liver failure
• Limited in children weighing less than 15 kg
• Not be used in pregnancy or in the presence of
hepatic or renal disease

Thiabendazole

• Alternative to Ivermectin for the treatment of

Strongyloidiasis and cutaneous larval migrans

Chemistry and Pharmacokinetics

• Benzimidazole compound
• Chelating agent that form stable complexes with
metals like iron, it does not bind calcium
• Rapidly absorbed after ingestion
• With standard dose, drug concentrations in
plasma peak within 1-2 hours
• Half-life: 1.2 hours
• Almost completely metabolized in the liver to 5-
hydroxy form
• 90% excreted in the urine in 48 hours, largely as
glucuronide or sulfonate conjugate
• Can also be absorbed from the skin

Anthelminthic Actions
• Probably the same as that of other
benzimidazoles
• Has ovicidal effects for some parasites

Clinical Uses
• Dose: 25 mg/kg (maximum 1.5 g) twice after
meals
• Tablets should be chewed