Anthelmintics Vineeth

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Anthelmintics

VINEETH M KRISHNAN
ROLL NO: 153
MEBENDAZOLE
MECHANISM OF ACTION
● MEBENDAZOLE binds to β-tubulin of susceptible
worms with high affinity and inhibits its polymerization.
Intracellular microtubules in the
cells of the worm are gradually lost.
● In addition, it probably blocks glucose uptake in the parasite
and depletes its glycogen stores.
ADVERSE EFFECTS
● Incidents of expulsion of Ascaris
from mouth or nose have occurred, probably due
to starvation of the parasite and their slow death.
● Allergic reactions, loss of hair and granulocytopenia have been
reported with high doses.
Uses

Uses and administration Mebendazole is


available as: MEBEX, WORMIN 100 mg chewable tab and
100 mg/5 ml suspension. MEBENDAZOLE 100 mg tab. The
dose
and duration of treatment is the same for children
above 2 years as for adults; ½ dose for 1–2
yr age.
Albendazole
MECHANISM OF ACTION
● Albendazole has weak microfilaricidal action, kills cysticerci,
hydatid larvae, ova of ascaris/ hookworm and is also effective in
cutaneous larva migrans.
● The mechanism of action of albendazole is similar to that of
mebendazole.
ADVERSE EFFECTS

Prolonged use, as in hydatid or in cysticercosis, has caused headache,


fever, alopecia, jaundice and neutropenia
USES
● For intestinal worms it should be given on empty stomach, while for
cysticercosis, hydatid and cutaneous larva migrans it should be given
with a fatty meal
● Ascaris, hookworm, Enterobius and Trichuris: a single dose of 400 mg
(for adults and children above 2 yrs, 200 mg for 1–2 yr age). Three day
treatment may be needed in heavy trichuriasis.
● • Tapeworms and strongyloidiasis: 400 mg daily for 3 consecutive days.
● Trichinosis: Three day treatment expels the adult worm from intestine,
but has limited effect on larvae that have migrated to muscles.
Pyrantel pamoate
MECHANISM OF ACTION
Pyrantel causes activation of nicotinic cholinergic receptors in the
worms resulting in persistent depolarization → slowly developing
contracture and spastic paralysis. Worms are then expelled
ADVERSE EFFECTS
● Pyrantel pamoate is remarkably free of side effects
● occasional gastrointestinal symptoms like headache and dizziness is
reported
USES
● For Ascaris, Ancylostoma and Enterobius: a single dose of 10 mg/kg is
recommended. A 3 day course for Necator and for Strongyloides has
been suggested.
● No fasting, purging or other preparation of the patient is needed
Piperazine
MECHANISM OF ACTION
Piperazine causes hyperpolarization of Ascaris muscle by a GABA agonist
action. Opening of Cl¯ channels causes relaxation and depresses
responsiveness to contractile action of ACh. Flaccid paralysis occurs and
worms are expelled alive
ADVERSE EFFECTS
● Piperazine is safe, but nausea, vomiting, abdominal discomfort and urticaria
may be felt.
● It is contraindicated in renal insufficiency and in epileptics
USES
● For roundworm infestation 4g once a day for 2 consecutive days;
children 0.75 g/year of age (max. 4 g) is considered curative.
● It can be used during pregnancy while other drugs cannot be used
Levamisole
MECHANISM OF ACTION
The ganglia in worms are stimulated causing tonic paralysis and expulsion of
live worms
ADVERSE EFFECTS
One or two doses used in helminthiasis are well tolerated. Incidence of side
effects—nausea, abdominal pain, giddiness, fatigue, drowsiness or insomnia
is low.
USES
● Ascariasis—Single dose 150 for adults, 100 mg for children 20–39 kg
body weight, 50 mg for 10–19 kg.
● Ancylostomiasis—Two doses at 12 hour intervals.
● It is less effective against Necator
WORM FIRST CHOICE ALTERNATIVE
DRUGS DRUG
ROUNDWORM Mebendazole, Albendazole Piperazine, Levamisole
Ascaris lumbricoides Pyrantel Ivermectin

HOOKWORM Pyrantel, Mebendazole Levamisole


Ancylostoma duodenale Albendazole
Necator americanus

PINWORM Pyrantel, Mebendazole Piperazine


Enterobius vermicularis Albendazole

PORK ROUNDWORM Albendazole Mebendazole


Trichinella spiralis

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