Antihelmentics

BLOCK

11

Lecturer Jubal G Abellar

MODULE

03

Date 09/05/2014

LECTURE

Antihelmentics:
I Thiabendazole
II Mebendazole
III Albendazole
IV Pyrantel
V Diethylcarbamazine
VI chemotherapy for amebiasis
A. Metronidazole
B. Diloxanide furoate
C. Paramomycin
D. Tetracycline
E.
Iodoquinol
F.
Chloroquine
G. Emetine and dehydroemetine

CASE
A 4 and 6 year old siblings were brought for check
up because of intense nocturnal pruritus at the perianal
area. There was a history of passage of flesh colored worms
2 - 3 inches in length for both of them per rectum 2
weeks ago, associated with on and off periumbilical pain.

Mechanism of Action:
suppress microtubule assembly

Inhibits secretion of parasite acetylcholinesterase

Dislodgement of worm
Side effects:
Anorexia
Headache
Vomiting
Dizziness
Hallucination
Convulsions
Cholestasis

Cutaneous larva migrans

Rectal exam revealed the above finding:

What is your impression?
How would you manage this px?
Characteristics of an Ideal Antiparasitic Agent
1.
2.
3.
4.
5.

Safe at high therapeutic doses.

Easily given preferably by oral route in single or
divided doses on the same day.
Chemically stable for long periods under climatic
conditions of use.
Ineffective as an inducer of drug resistance.
Inexpensive

MEBENDAZOLE
First Line Drug for:
1. Trichuris
2. Enterobius
3. Ascaris
4. Hookworm
5. Trichinella (together with Steroids)
6. Capillaria
Mechanism of Action:
Depletes energy stores

Disrupts cytoskeletal transport

Note! Mebendazole is not given to pregnant women
&children < 2 years old> because it is teratogenic

THIABENDAZOLE
First Line Drug for:
1. Strongyloidiasis
2. Creeping Eruption
3. Toxocara (Visceral Larva Migrans)
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Albendazole is indicated for neurocysticercosis,

echinococcosis.
PYRANTEL
Indication: Hookworn, Pinworm, Roundworm
- Must be used withOxantelto be effective against
Trichuris.

Trichuris

Hookworn rhabditiform larva

Mechanism of Action:
Depolarizing neuromuscular blocking agent by nicotinic
inactivation

Spastic paralysis

Detachment from host

Expulsion by host peristalsis

Note! Not used with Piperazine together because of
antagonistic
action
(piperazinecauses
Hyperpolarization>>>Relaxation)

Ascaris ova
Mebendazole isovicidal and kills both larva and adult
worms.
Side effects:
not significant because of poor absorption
transientabd. pain and diarrhea in massive
infestation
high dose: allergic rxns,
alopecia,agranulocytopenia, neutropenia,
hypospermia
ALBENDAZOLE

Side Effects:

Headache

Dizziness
Rash,

Fever
Mild GI symptoms
DIETHYLCARBAMAZINE

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Prevented by:
1. Adequate purging within 3-4 hours after giving the
drug clears the bowel of the dead segments before being
digested
2. Use of Praziquantel rather than Niclosamide
Cysticeruscellulosae - Praziquantel or Albendazole is the
drug of choice.
PRAZIQUANTEL
Effective for Schistosomiasis
Better cure rate than Niclosamide for H.nana
Onchocerca
Drug of Choice for:
1. Filariasis
2. Microfilariae of ONCHOCERCA but not the adult worm
Mechanism of Action:
-hyperpolarization > decrease muscular activity
- alters surface membranes rendering destruction by host
defense mechanism
Kills microfilaria in the blood but not in the nodules of
Onchocerca
Kills adult worms of Loa loa andWuchereria

Mechanism of Action:
*Alters integumental permeability to cation>>>
Influx of
Calcium >>>Muscular Spasticity
* Vacuolization and vesiculation of the parasites tegument
>> destruction
Side effects:
Transient abdominal pain, nausea, malaise , headache and
dizziness

MAZOTTI REACTION
Intense itching, skin rashes, enlargement and tenderness of
nodes, fever, tachycardia, and arthralgia that occurs within a
few hours after treatment of Onchocerciasis with
Diethylcarbamazine
Due to massive destruction of worms
Approach: Pretreatment with steroids or slowly increasing
the dosage to desired level or discontinue temporarily.
IVERMECTIN
Best against ONCHOCERCIASIS
kills microfilaria but little harm to adult worm
Mechanism of Action: Toxic paralysis by release and
binding of GABA
Note! Surgical incision of Onchocerca Nodules is
recommended before treatment
NICLOSAMIDE
Effective against CESTODES or TAPEWORMS
Mechanism of Action:
1. Inhibits anaerobic phosphorylation of mitochondria
2. Kills proximal worm segments and scolex but not the ova
Side Effects: well tolerated except for mild GI upset
Note: Use in Taeniasolium predisposes to CYSTICERCOSIS
Reason:Digestion of dead segments liberates walled ova into
the lumenand niclosamide does not kill the ova

OXAMNIQUINE
- alternative drug for Schistosomamansoni
- not effective for S. japonicum andhaematobium
BITHIONOL
- lung and liver flukes
METRIFONATE
- Inhibits cholinesterases
- effective for S. haematobium only
PIPERAZINE CITRATE
Choice for intestinal obstruction secondary to
Ascariasis
Useful for ascariasis and pinworms
Decompression and maintenance of fluids and
electrolytes must also be done
Causes neurotoxicity in patients with renal dysfunction, mild
GI upset, transient neuro effects &urticaria
Advantage in Ascariasis:
- Hyperpolarization Relaxation Flaccid ParalysiS
- Decreased Motility Prevents erratic migration
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Pyrantel causes spastic paralysis (possible erratic

migration)

ASCARIASIS
- In highly prevalent areas ---- deworming could be
done 3 times a year or every 4 months

- Patients to be dewormed at night will not be allowed to

eat prior.
- Do not deworm when the patient is weak or having
febrile illness.
- Ipil-ipil seeds, pineapple and papaya have deworming
properties.
- Routine deworming without fecalysis can be done
starting 1 years of age in endemic areas.
Philippine Pediatric Society (PPS) recommendation on
deworming
- Routine deworming at 1 year of age and above at
least every 6 mos
Mebendazole 500 mg -- 1 year and above
Albendazole 200 mg ----1 to 2 years old
400 mg ---above 2 years

Ascaris ova
ENTEROBIASIS
Tendency for familial occurrence
All members of household should be treated if there
is reinfection or if another member is symptomatic
Treatment should be repeated after 2 weeks because eggs
are hatched---- danger of autoinfection
HOOKWORM INFECTION
Blood loss of 0.5 ml/ worm ---- treat possible anemia
(hypochromic, microcytic)
TRICHURIASIS
Also consider possible anemia although blood loss
is not as severe as in hookworm infection
DRACUNCOLOSIS
-manual removal of worm + Metronidazole
- ginaroll
- manual removal of worm. Found at middle East, no
cases at Philippines.
POLYPARASITIC or MIXED INFECTION
Mebendazole is the preferred drug.
Note! All helminthes need treatment.
- Laboratory follow up is needed to ensure total
eradication.
- Stool exam is done 2 weeks after deworming.
- Preventive education is a must!
Preventive measures
- Hygiene
- Handwashing
- Avoid streetfoods
- Cover the wood against insects
- Storage
Myths, Beliefs or Facts?
- Do not deworm during full moon, bad weather or rainy
days.

Diethylcarbamazine+albendazole drugs recommended for

mass treatment for filariasis eradication program.
Contraindications for deworming (treat the problem first
before deworming)
abdominal pain (severe)
profuse diarrhea
severe malnutrition
high grade fever

CHEMOTHERAPY FOR AMEBIASIS

Cases:
A. A 3 year old boy was admitted because of diarrhea for 3
days. The stool was described as watery, foul smelling,
greenish, mucoid admixed with blood streaks. There was
associated abdominal pain, fever, vomiting and tenesmus. PE
revealed sunken eyeballs, cold skin and diffuse abdominal
tenderness.
Questions:
a. Whats your clinical impression?
b. Drug of choice? Metronidazole
-Macrophages look similar with ameba.
- Stool characteristics of patient having ameba: mucoid, blood
streak, foul smelling and greenish.
- Tenesmus different from an explosive type of evacuation.
This type is pagamay-gamay.
- Sakit ang tiyan kay may ulcerations. An inflammatory form
of dysentery.
- Some are resistant to Metronidazole already. We must
know the alternative drugs. We must have an idea what to
give is it only luminal or extraluminal.
B. A 25 year old man was seen at the ER because of right
upper quadrant pain for a week. He had on and off fever
associated with weight loss and poor intake. PE revealed
tender and enlarged liver with slight icteresia. UTZ of
hepatobiliary area showed an echo-free area at the right lobe
of the liver.
An anchovy sauce like material was aspirated.
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a. Impression?
b. Medications?
- Anchovy sauce dark brown, chocolate. If anchovy sauce, it
is most likely amebic. Abscess ---> can go to the lungs rupture
---> pleural effusion
- Ameba fecal oral route ---> goes to the liver --->colitits,
diarrhea or dysentery symptoms.

numbness
(+) Disulfiram reaction with alcohol
S/Sx of disulfiram reaction: tachycardia,
hyperventilation, flushing and nausea
2. DILOXANIDE FUROATE
- choice for asymptomatic cyst passers.
- (+) cyst but no s/sx.
3. PAROMOMYCIN
-an Aminoglycoside.Not significantly absorbed
MECHANISM OF ACTION: Amebicidal by causing leakage of
cell membrane and by reducing population of intestinal flora
like Tetracycline. (*intestinal flora gives food to the amebacausing microbes)
- alternative drug for diloxanide in asymptomatic
carriers.
4.TETRACYCLINE
avoid using in children

Luminal amebicides
- Diloxanide
- Paromomysin
- Tetracyclin - avoid discoloration if primary teeth below 8
years old children
Metronidazole is both luminal and systemic. Together with
Emetine, Dehydroemetine and Fluoroquine

5. IODOQUINOL
-recommended as an intestinal amebicide and for
asymptomatic carrier: caused an epidemic of
subacutemyelooptic neuropathy. (*doc is not so sure is ara pa
nisa market)
Etofamide (Kitnos) faster. Used if patient is not improving
with Metronidazole and who dont want the taste of it. More
expensive.

If theres abscess or amebic dysentery already: give

Metronidazole.

6. CHLOROQUINE
-used to eliminate trophozoites in liver abscesses like
Emetine and Dehydroemetine. Effective for
extraintestinalamebasis

1. METRONIDAZOLE
-toxic for ameba, anaerobic organisms, giardia,
trichomonasand surgical cases (pseudomonas).
-choice for symptomatic and invasive amebiasis although
effective against cysts and trophozoites.
-asymptomaticamebiasis has cysts at intestines but no
signs of infection. A carrier.
MECHANISM OF ACTION:
a. its nitro group serves as an electron acceptor binds
to the protozoans ferrodoxin - like, low redox
potential electron transport protein forms reduced
cytotoxic compound
b. impairs the ability of DNA to function as a template
(distributed well throughout the body tissues and
fluids)
Side effects:
nausea
vomiting
epigastric distress
abdominal cramps
metallic taste
dizziness, vertigo

7. EMETINE and DEHYDROEMETINE

-alternative agents
MECHANISM OF ACTION: inhibit protein synthesis by
blocking translocation of peptide chain.
- INTRAMUSCULAR - preferred route = more side
effects. Used in amebic abscess.
Emetine concentration in the liver and persist for a month
after a single dose :
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 Use is limited by toxicities

Dehydroemetine is less toxic
Untoward effects:
1. Pain at injection site
2. Nausea
3. Cardiotoxicity
4. Neuromuscular weakness
5. Dizziness
6. Rashes
Educate patient about:
1. Frequent handwashing
2. Proper food preparation and handling
3. Sanitary toilet

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