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Anthelmintic

Class
Round Worms
(Nematodes)

Benzimidazoles

Name

Route

Mebendazole

Thiabendazole

Diethylcarbamazine
Pyrantel Pamoate

Notes

Mechanism

Not well absorbed orally inc with fatty meal; Can cross
BBB and enter hydatid cyst; Plasma peak of 3-4 hours;
Broad Spectrum; Hydatid Cysts
t1/2 8-12 hrs; Bound to plasma protein; excreted in
(Enchinococcosis & Cysticercosis) URINE.
Disrupts parasitic microtubules; binds to B-tubulin
Disrupts parasitic microtubules; binds to B-tubulin; also
Broad Spectrum
Most useful Benzimidazoles.
disrupts Ox-phos and glucose uptake.
Strongylaides (threadworm);
trichinosis, dracunculus and
Most toxic/least used. Peak plasma conc. 1-2 hrs; short Metal Chelating agent (Mg2+); inhibits microtubule
capillaria
t1/2; rapidly metabolized by liver first pass;
assembly (B tubulin)

Albendazole

Ivermectin

Specific Rx

Oral Only

Onchocesca (river blindness)


Tropical roundworms (wucheria
bancrofti etc)
Broad Spectrum

Side Effects/contraindications

caution w/: Benzene allergies;


hypertension, liver cirrosis (p450
system).
Teratogen; Drug interaction with
cimetidine (p450 issues)

Sx: anorexia, dizziness, CNS sx;


p450 system; FATALITIES
Mazotti reaction (rash and muscle
Semi-synthetic LARGE; Plasma peak 4 hrs; LONG t1/2 16
pain); don't give to pregnant
hrs; Does NOT cross membranes or BBB; excreted in
Continuous stimulation of GABA receptors in worm and women or people already on
feces; can be prophylaxis.
paralyzes it. Molecular stun gun.
GABA.
Immobilizes microfilariae possibly by not letting
Synthetic; Plasma Peak 1-2 hrs; Half-Life can be affected arachidonic acid across the membrane PARALYZES
by pH (Basic will lengthen it up to 12 hrs);
worms.
Poorly absorbed orally; Most effective
Paralyzes worms through Nicotinic receptor

Flat Worms
(Trematodes &
Cestodes)

Praziquantel
Bithionol

Niclosamide

Orally
Schistosomes & all trematodes
Orally
Sheep Liver Flukes
Large dose on
empty
stomach
Tapeworms DOC

Most important one of these; Plasma Peak 1-2 hrs; liver


first pass; Crosses BBB;
Alter parasite membrane to Calcium Ions
peak plasma 4-8 hrs; halogenated
Unknown disrupts ion flow membrane shtuff.
Not used in US for humans; Not absorbed at all only
good in GI; salicylamide derivative; No plasma level

shuts down Ox-Phos and reduced ATP production

GI sx; headache (crosses BBB);


drowsiness; SPONTANEOUS
Abortions; Inflammatory reactions
(give with corticosteroids) p450
alterers

GI issues

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