Helminthic infections

Cause host injury by

! nutritional depletion
!
!

ANTHELMINTIC DRUGS

Anthelmintic drugs
Helminthes
Nematodes

mechanical Injury (ie. hookworm, larvae)

eliciting an immune response (ie. hookworm
larvae in the lungs cause eosinophilic
pneumonia)

Helminthes: similar biochemical pathways to host

Benzimidazoles

Drugs
Benzimidazoles
Pyrentel pamoate
Piperazine citrate
Ivermectin
Diethylcarbamazine

bind to free -tubulin , inhibit microtubule

polymerization, inhibit glucose uptake, lack
energy

Cestodes

Niclosamide
Praziquantel

potentially teratogenic, not use in pregnancy &

<2 yr children

Trematodes

Praziquantel

Mebendazole, albendazole, thiabendazole

broad spectrum anthelmintics

Mebendazole

Albendazole

Drug of choice for many intestinal nematodes

- also kills hookworm, ascaris, and trichuris eggs
! <10% GI absorbed, low adverse effects
! chewed before swallowing
! Pinworm:100 mg once, repeated at 2 weeks
! Other nematodes: 100 mg bid for 3 days
! Good cure rate for pinworm & ascariasis
infection

!
!

affect on adult, larvicidal & ovicidal effects

used for many intestinal nematode infection &
strongyloidiasis
DOC for hydatid disease & cysticercosis
PKs: increased absorption by fatty meal , first-pass
metabolized to active metabolite albendazole
sulfoxide.

Albendazole
!

!
!
!

administered on empty stomach for intraluminal

parasites but with a fatty meal for tissue parasites
ascariasis and hookworm: 400 mg single dose
Trichuriasis: three daily 400-mg oral doses
Hydatid diseases: adjunct to surgical removal or
aspiration of cysts. 400 mg bid with meals for 1
month or longer.
Neurocysticercosis: 400 mg twice a day for up to
21 days administered with corticosteroids.

Pyrantel pamoate
!
!

!
!
!

a tetrahydropyrimidine derivative
broad-spectrum antihelminthic for intestinal nematodes
but trichuriasis or strongyloidiasis.
cause parasite paralysis by acting as a neuromuscular
blocking agent that causes release of acetylcholine and
inhibition of cholinesterase
poorly GI absorption
mild adverse effects
11 mg (base)/kg single dose, may be repeated if
indicated

Ivermectin
!
!

macrocyclic lactone, avermectin B1a & Bba mixture

DOC for strongyloidiasis and onchocerciasis
- microfilaricidal in onchocerciasis
paralyze nematodes by intensifying GABAmediated
transmission of signals in peripheral nerves
Onchocerciasis: 150 g/kg single dose. repeat doses
monthly - yearly
Strongyloidiasis: two daily doses of 200 g/kg

Thiabendazole
!

!
!

alternative drug for strongyloidiasis and cutaneous

larva migrans.
chewed before swallowing, rapidly GI absorbed
Side effects: toxic >> other benzimidazoles &
ivermectin, may cause fatal Stevens-Johnson
syndrome
strongyloidiasis: 2 days course, repeated in 1 week if
indicated
cutaneous larva migrans: cream/oral drug

Diethylcarbamazine
!
!

!
!

DOC for filariasis, loiasis, and tropical eosinophilia

immobilize microfilariae, alter their surface structure
making them more susceptible to host defense
23 week course
Antihistamines & corticosteroids may be given to
limit allergic reactions
Adverse effects: from released proteins of dying
microfilariae

Piperazine
!
!

!
!

an alternative for pinworm & ascaris infection

cause paralysis by blocking acetylcholine at the
myoneural junction
75 mg/kg OD for 2 days
mild adverse effects

"

Praziquantel
!
!

isoquinoline-pyrazine derivative
used for almost all trematode, & cestode infections
including cysticercosis.
Mechanism: increase calcium influx, resulting in
paralysis, dislodgement, and death o parasites
rapidly & well absorbed, plasma conc. increased
when taken with a high carbohydrate meal
do not chew because very bitter taste

Praziquantel
!
!

!
!

Mild and transient adverse effects

Schistosomiasis: 20 mg/kg, 2-3 doses, at 4-6 h
interval
Other trematodes: 25 mg/kg tid for 2 days for
Taeniasis & Diphyllobothriasis: 510 mg/kg, single
dose

NICLOSAMIDE
!
!
!

!
!

a salicylamide derivative for tapeworm infections,

minimally GI absorbed
rapidly kill adult worms by inhibiting oxidative
phosphorylation or stimulation of ATPase activity.
Dose: 2 g single dose, on an empty stomach
chewed thoroughly before swallowing with water