University of Guyana

Faculty of Health Sciences

School of Medicine
Pharmacotherapeutics 1
Dr. Latoya Harris

ANTIHELMINTHS AND
MANAGEMENT OF
Group Three Members:
FILARIASIS
Hilton Chester
Kevin Hohenkirk
Anetha Jodhan
Mordesa Scott
Ravindra Singh
 INTRODUCTION
What are Heliminths?
 Helminths are worm-like parasites that survive by feeding on a
living host to gain nourishment and protection, sometimes
resulting in illness of the host.
 CLASSIFICATION

Helminths

Plathyhelminths Nemathelminths
(Flatworms) (round worms)

Cestodes Trematodes
Nematodes
(tapeworms) (flukes)
MORPHOLOGY

A micrograph showing
the morphology of a
Taenia solium tapeworm
scolex with its four
suckers, and two rows of
hooks.
 MORPHOLOGY
An adult Taenia saginata A dish of Ascaris lumbricoides
tapeworm. worms. Many grow up to 30
centimetres long.
 MODES OF TRANSMISSION
 Faecal-oral transmission of eggs or larvae passed in the faeces
of one host and ingested with food/water by another.
 e.g. ingestion of Trichuris eggs leads directly to gut infections in humans.
Transdermal transmission of
infective larvae in the soil
actively penetrating the skin and
migrating through the tissues to
the gut where adults develop and
produce eggs that are voided in
host faeces.

e.g. larval hookworms

penetrating the skin
 MODES OF TRANSMISSION

 Vector-borne transmission of larval stages taken up by blood-

sucking arthropods or undergoing amplification in aquatic
molluscs.
 e.g. Onchocerca microfilariae ingested by blackflies and injected
into new human hosts, Schistosoma eggs release miracidia to infect
snails where they multiply and form cercariae which are released to
infect new hosts.
 Predator-prey transmission of encysted larvae within prey
animals (vertebrate or invertebrate) being eaten by predators where
adult worms develop and produce eggs.
 e.g. Dracunculus larvae in copepods ingested by humans leading to guinea
worm infection, Taenia cysticerci in beef and pork being eaten by humans.
ANTI-HELMINTHICS
 Anti-helmintics are therapeutic agents used to kill (vermicide) or
expel (vermifuge) parasitic worms from the infected host. Several
of the drugs affect the nervous system of the parasite and result
in muscle paralysis. Other drugs affect the uptake of glucose and
thus energy stores.
 NEMATODES
Elongated and tapered at
ends
Possess a complete
digestive system, including
both a mouth and an anus.
They cause infections of
the intestine as well as the
blood and tissues.
LIFE CYCLE OF A NEMATODE
 ANTI-NEMATODAL DRUGS

Ivermectin Albendazole Mebendazole

Diethylcarbamazine Pyrantel pamoate

 MEBENDAZOLE/ ALBENDAZOLE

 A synthetic benzimidazole compound.

A drug of choice:
 whipworm (Trichuris trichiura),
 pinworm (Enterobius vermicularis),
 hookworms (Necator americanus and Ancylostoma
duodenale),
 roundworm (Ascaris lumbricoides).
Albendazole is the drug of choice to treat cysticercosis
(caused by Taenia solium larvae) and cystic hydatid
disease (cestode E. granulosus).
 MEBENDAZOLE/ ALBENDAZOLE

Mechanism of Action Pharmacokinetics

considerations
 Binds to and interfers with
the assembly of the parasites’ ■ Nearly insoluble in aqueous solution
microtubules and also by ■ Oral dose is absorbed, unless it is taken
decreasing glucose uptake. with a high-fat meal.
 Affected parasites are expelled ■ First-pass metabolism to inactive
with feces. compounds.
■ Half-life of about 8-12 hrs
 MEBENDAZOLE/ ALBENDAZOLE

Side Effects Contraindiction

■ Pregnant women
 Abdominal pain
■ Should not be given to children under
 Diarrhea 2 years old
 Headache ■ Should not be given to patients with
known hypersensitivity to other
 Nausea benzimidazole drugs
■ Should not be given to those with
cirrhosis.
 IVERMECTIN

 Drug of choice for the treatment of

onchocerciasis (river blindness) caused
by Onchocerca volvulus and for
cutaneous larva migrans and
strongyloidiasis.

 Is a first-line agent for the treatment of

lymphatic filariasis and tropical
pulmonaryeosinophilia caused by W.
bancrofti and B. malayi.
 IVERMECTIN

Mechanism of Action Pharmacokinetics

considerations
Targets the parasite’s
glutamate-gated chloride ■ The drug is given orally.
channel receptors. ■ It does not cross the blood-brain
barrier and has no pharmacologic
Chloride influx is enhanced, effects in the CNS.
and hyperpolarization occurs, ■ Wide tissue distribution
resulting in paralysis of the ■ Rapidly absorbed by GI tract
worm. ■ Half-life of about 16hrs
 IVERMECTIN
Side Effects Contraindication
In onchocerciasis, the
killing of the microfilaria ■ Pregnant women
can result in a Mazotti-like ■ Patients with meningitis
reaction:
 fever, ■ Avoid concomitant use of Ivermectin
with drugs that enhance GABA activity
 headache,
■ Should not be given to children under 5
 dizziness, years old
 somnolence,
■ Should not be given to patients with
 hypotension impaired BBB
TREMATODES
 CESTODES
 AKA True tapeworms lack a mouth and a
digestive tract throughout their life cycle.
 Flat, segmented body
 Hermaphrodite
 Mature sexually in the definitive or final
host
 Lives in the intestines with feces
 Causes tissue and intestinal infections
LIFECYCLE OF CESTODES
 CESTODES
Type of Example Type of infection
tapeworm caused
Beef tapeworm Taenia saginata • Taeniasis
Pork tapeworm Taenia solium • Cysticercosis
• Taeniasis
Dog tapeworm Echinococcus granulosus • Echinococcosis
Fish tapeworm Diphyllobothrium latum • Diphyllobothriasis
Dwarf Tapeworm Hymenolepis nana • Hymenolepiasis
 PRAZIQUANTEL
Used to treat infections caused
worms that live in the bloodstream
and/ that lives in or near the liver .

Drug of choice for:

Trematodes e.g liver fluke,
Schistosoma infections
Cestodes e.g. Taenia solium
 PRAZIQUANTEL
Mechanism of Action Pharmacokinetics
• Leakage of intracellular Ca 2+ causing severe considerations
spasms and paralysis of the worms' muscles.
• Absorption enhanced with
food.
• Worms lose grip on intestinal wall including
tissues and veins
• High first pass metabolism
• Active against all stages of worm including
larvae • Crosses blood-brain barrier

• Worms are then either completely destroyed in • 1.5hrs half life

the intestine or passed in the stool
 PRAZIQUANTEL
Side effects Contraindications
• Nausea • Should be avoided in pregnant
• Vomiting woman.
• Abdominal pain
• Fever
• Ocular infections should not be
• Skin rashes after several days treated with Praziquantel since it
• Eosinophilia can cause damage to the eyes.
• Myalgia • Corticosteroids drastically
reduce the plasma level of
Praziquantel.
FILARIASIS
• elephantiasis, is a painful and
profoundly disfiguring disease
• all ages are affected;

• Childhood infections can manifest

later in life, causing temporary or
permanent disability

• Caused by 3 species of thread-like

nematodes
CLINICAL MANIFESTATIONS
• Acute attacks
• Adenolymphagitis (ADL) - lymphatic vessel damage that predisposes
lower limbs to bacterial infections.
• Lymphoedema and elephantiasis
• Repeated episodes of ADL leads to progression of lymphoedema
• Hydrocoele
• Fluid accumulation in Tunis vaginalis
• True filariasis hydrocoele occurs after death of adult filariasis
worms
• Chylocoele is due to accumulation of fluid after the rupture of
lymphatic vessels in scrotal cavity
TREATMENT
Endemic communities
• primary goal - eliminate microfilariae from the blood
• interrupt transmission of infection by mosquitoes.
• Studies have shown that > 5 years of MDA with preventive chemotherapy reduces
microfilariae from the bloodstream and prevents the spread of microfilariae to
mosquitoes.

• Preventive chemotherapy: given annually to an entire at-risk population:

1. albendazole (400 mg) plus ivermectin (150–200 μg/kg) or
2. diethylcarbamazine citrate (DEC) (6 mg/kg).

• MDA with albendazole (400 mg) alone should be given preferably twice per year
to stop the spread of lymphatic filariasis in areas where Loa loa is present.
TREATMENT
Individuals
1. Infected patients can be treated with one of the following regimens:a

1. single dose of a combination of albendazole (400 mg) with

ivermectin (150–200 μg/kg) in areas where onchocerciasis is co-
endemic;

2. in areas where onchocerciasis is non co-endemic, either a single

dose of a combination albendazole (400 mg) plus
diethylcarbamazine (6 mg/kg)

3. DEC (6 mg/kg) alone for 12 days.

MANAGING MORBIDITY AND PREVENTING DISABILITY
• MMDP in lymphatic filariasis require a broad strategy involving both
secondary and tertiary prevention.

• Secondary prevention includes simple hygiene measures, such as

basic skin care and exercise, to prevent ADL and progression of
lymphoedema to elephantiasis.

• For management of hydrocoele, surgery may be appropriate.

• Tertiary prevention includes psychological and socioeconomic support

for people with disabling conditions to ensure that they have equal
access to rehabilitation services and opportunities for health,
education and income.
PREVENTION

• Avoidance of mosquito bites

• through personal protection measure

• community-level vector control

• participation in MDA is the best option to prevent

lymphatic filariasis.
 SUMMARY
F.
 REFERENCE
1. World Health Organization. (2018). What is lymphatic filariasis. [online] Available at:
https://www.who.int/lymphatic_filariasis/disease/en/ [Accessed 7 Dec. 2018].