Antihelmintics Drugs

DR.NAZISH

Antihelmintic agents

Drugs for nemtodes :

Diethylcarbamazine
Ivermectin
Mebendazole
Pyrantal pamoate
Thiabendazole
Drugs for trematodes :
Praziquantal , Oxamniquine
Bithionol
, Metrifonate
Drugs for cestodes :
Albendazole
Niclosamide

Overview
3 major groups of helminths(worms) that
infects humans are:
Nematodes (roundworms, whipworm,
pinworms, threadworms ,hookworms)
Trematod (flukes)
Cestodes (tapeworms)

Drugs for treatment of Nematodes

Mebendazole :

Synthetic benzimidazole compound and wide spectrum

antihelminthic, less adverse effects.
Drug of choice in the treatment of infections by
whipworm ,pinworm, hookworms, roundworms.
Half life 2-6 hours.
Absorption is increased if drug is ingested with fatty meal.
Underoes first pass metabolism and excreted mainly in
urine .
The drug acts by inhibiting microtubule synthesis.
Contraindicated in pregnancy.(embryotoxic and
teratogenic) and should b given with caution in cirrhosis
and children of 2 years.

Clinical uses:
Ascariasis(round worms) trichuriasis
(whipworm), hookworms
disease(ancylostoma duodenale, nectar
americanus), pinworm
disease(enterobiasis).
Adverse effects:
Short term therapy free of side effects.
Mild nausea, vomiting, diarrhea
,abdominal pain.
High dose therapy--- hypersenstivity
reactions(rash, urticaria, alopecia,
agranulocytosis, elevated liver enzymes.)

Pyantal pamoate
Broad spectrum antihelminthic,
Highly effective for Pinworm, Ascariasis and
Trichostrongylus Orientalis infection.
A tetrahydropyrimidine derivative
Poor absorption from GIT
The drug is a neuromuscular blocking agent that
causes release of acetycholine and inhibition of
cholinestrase ,this results in paralysis of worms
followed by expulsion.
Adverse effects:are infrequent, mild and transient.
Nausea,vomiting,diarrhea,abdominal
cramps,dizziness,drowsiess,headche,insomnia,rash
fever,weakness.
Caution : in liver dysfunctioning patient

Thiabendazole

A benzimidazole compound .
Rapidly absorbed after ingestion.
Half-life 1.2 hrs.
Completely metabolized in liver and excreted in
urine.
Dose should be given after meals.
Adverse effects : dizziness, anorexia,
nausea, vomiting, epigastric pain, abdominal
cramps, diarrhea, pruritis, headche, drowziness
and neuropsychiatric symptoms,Irreversible
liver failure and fatal stevens johnson
syndrome.
Contra : pregnancy or hepatic or renal disease.

Ivermectin
Drug of choice for river blindness and threadworm
infection.
Used orally only in humans and rapidly absorbed.
Half life is about 16 hours. Excretion is through feces.
Drug Targets the parasites glutamate-gated chloride
receptors. chloride influx is increased &
hyperpolarization occurs, resulting in paralysis of the
worms.
Clinical uses: onchocerciasis, stongyloidiasis, scabies,
Adverse effects: fatigue, dizziness, nausea, vomiting,
abdominal pain ,rashes ,fever ,headche, pruritis,
hypotension, tachycardia, lymphadenitis and
peripheral edema.
Contra : pregnancy.

Diethylcarbamazine
Drug of choice in the treatment of filariasis, loiasis,
tropical eosinophilia .
A synthetic piperazine derivative.
Rapidly absorbed from GIT,half life---1-2 hrs if
acidic urine.
Drug should b taken after meals.
Urinary alkalosis and renal impairment may require
dosage reduction.
Clinical uses: Wuchereria Bancrofti, brugia malai.
Adverse effects: fever, rash, mayalgia
,leukocytosis, anorexia,nausea,vomiting,
proteinuria,joint pain,
Caution: hypertension or renal disease.

Drugs for the treament of Trematodes

Praziquantal:
Drug of choice of all forms of schistosomiasis and
cysticercosis.
Permeability of the cell membrane is increased,causing
contractures and paralysis of the parasite.
Synthetic isoquinoline pyrazine derivative
Peak serum concentration are reached 1-3 hours after
therapeutic dose.
Half life is 0.8-1.5 hrs
Excretion is mainly via kidneys and bile.
Clinical uses:
paragonimasis,taeniasis,neurocuysticercosis,h.nana, hydatid
disease.
Contra :ocular cysticercosis.
Drug interaction: phenytoin,carbamazepine, dexamethasone.

Bithionol
Used in treatment of lung
fluke( pul.paragonimiasis) and sheep liver
fluke (fascioliasis ).
Excretion is via kidneys.
Severe effects needs interruption of
therapy.
adverse effects:
Diarrhea ,nausea , vomiting ,anorexia,
skin reaction, dizziness headche.
Caution: in children

Drugs for the treatment of Cestodes

Niclosamide:
Second line drug for most tapeworm infections.
Drug should be given in morning on an empty
stomach.
Adult worms are rapidly killed due to inhibition
of oxidative phosphorylation or stimulation of
ATPase activity.
Clinical uses;( beef ,pork,fish,dog tapeworm),
Cycticercosis .
Adverse effects:mild nausea , vomiting ,
diarrhea,and abdominal discomfort.
Contra : alcohol

Albendazole
A broad spectrum oral antihelimintics and drug of choice
for hydatid disease and cysticercosis.
It is a benzimidazole carbamate.
Half life---8-12 hrs
Excreted in urine
Should b given empty stomach when used against
intraluminal parasite but with fatty meal when used
against tissue parasite.
Clinical uses: ascariasis , trichuriasis, hookworm,
pinworm infections, hydatid disease, neurocysticercosis.
Adverse effects: insomnia, diarrhea, lassitude, nausea,
long term (pancytopenia ,alopecia, liver enzymes
increased).
Contra : hypersenstivity to albendazole, pregnancy,
children under 2 yrs.

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