28 Anthelmintics

1.
2.

Anthelmintics
Anthelmintics

1 Anthelmintics

1 Anthelmintic drugs

Benzimidazole
albendazole, mebendazole, thiabendazole
Albendazole
Albendazole broad spectrum anthelmintic
pinworm (threadworm-UK), ascariasis, trichuriasis, strongyloides
choice
hydatid disease cysticercosis

hookworm

(nematodes)
Albendazole
drug of

Anthelmintic action
albendazole
larvae stage adult
glucose uptake
stage
bind -tubulin
tubulin polymerization
microtubule-dependent glucose uptake
immobilize
larvae hydatid disease, cysticercosis, ascariasis
hookworm infection
,
therapeutic oral dose (5 mg/kg) Albendazole
(intraluminal)
albendazole
tissue
albendazole

Clinical uses
1. Ascariasis, Trichuriasis, Hookworm, Pinworm infection
,
,
,
mg
2
2. Strongyloidiasis
(threadworm-USA)
400 mg
3. Hydatid disease
Treatment of choice albendazole
400 mg
3
4. Neurocysticercosis
Albendazole drug of choice
albendazole
15 mg/kg/day
7-21
2-3
inflammatory reaction
,
, hyperthermia, convulsion

single dose 400

7-14

corticosteroids

albendazole
1-3 albendazole
mild and
transient epigastric distress, diarrhea, headache, nausea, dizziness, insomnia
hydatid disease
reversible
low grade aminotransferase elevations, gastrointestinal symptoms (nausea, vomiting, abdominal pain), alopecia,
rash, leukopenia
long term toxicity
diarrhea, anemia, hypotension, marrow depression,
liver function test abnormalities
Mebendazole
Mebendazole
Anthelmintic action
Mebendazole
albendazole

wide spectrum anthelmintics

glucose uptake

microtubule synthesis
immobilize
hookworm,

Clinical uses
Mebendazole
1. Pinworm infection (Enterobius vermicularis)
mebendazole 100 mg
cure rate 90-100%

irreversible

2. Ascaris lumbricoides, Trichuris trichiura, Hook worm

2
100 mg
2
3
2-3
cure rate 90-100 %
ascariasis trichuriasis
hookworm
species cure
rate 70-95%
3. Other infection
- Alternative drug
intestinal capillariasis (400 mg/day in divided dose
21
)
- Trichinosis
600 mg
1200-1500 mg
10
- Taeniasis
T. solium
300 mg
2
3
- Strongyloidiasis
Mebendazole alternative drug
hydatid disease
cure rate
Mebendazole

mild nausea, vomiting,

diarrhea, abdominal pain
, dizziness, hypersensitivity (rash,
urticaria)
5
hydatid disease
pruritus, rash, eosinophilia,
diarrhea, reversible neutropenia, musculoskeletal pain, fever, acute pain in cyst area
cyst leakage cyst
rupture
gastric irritation, cough, transient liver function abnormalities, alopecia,
glomerulonephritis
Niclosamide
Niclosamide

drug of choice

1-3

tape worm infection Niclosamide salicylamide derivative

metabolite niclosamide

Anthelmintic action
Niclosamide
solium

scolex (
oxidative phosphorylation Niclosamide
niclosamide
2
MgSO4
cysticercosis

proximal segment

larvae

T.
segment

Clinical uses
niclosamide
2g
3 ,
11-34
2
niclosamide
1. T. saginata, T. solium, Diphyllobothrium latum

(500 mg/ tab),

11

34
1

Niclosamide single dose 2 g (

4
500 mg) cure rate
85%
D.
latum, 95%
T. saginata T. solium
Niclosamide
cysticercosis hydatid disease
2. Hymenolepsis nana
Drug of choice praziquantel niclosamide
7
cure rate
75%
3. Other tapeworm
Hymenolepsis diminuta, Dipylidium caninum
7
4. Intestinal fluke infection
Niclosamide
alternative drug
Fasciolopsis buski, Heterophyes heterophyes
Metagonimus yokogawi
standard dose
3 dose
niclosamide
abdominal discomfort
antigen
Praziquantel
Praziquantel
infection (
cysticercosis
Praziquantel
hydatid disease

nausea, vomiting,
headache, skin rash, urticaria, vertigo

broad spectrum anthelmintic Praziquantel

)
species
trematodes
trematodes

drug of choice
cestodes

Schistosome

Fasiolopsis hepatica (sheep liver fluke)

Anthelmintic action
Praziquantel
paralysis
cell membrane permeability Calcium
contraction musculature
paralysis
praziquantel
immune response host
Praziquantel
Adult schistosomes
immature forms
cercariae
praziquantel
prophylactic effect
Praziquantel
therapeutic dose
Clinical uses
praziquantel
dose
1. Schistosomiasis

Praziquantel

2.

3.
4.

5.

6.
7.

8.

drug of choice
Schistosomiasis
20 mg/kg 3
4-6
praziquantel S. mansoni
oxamniquine
Clonorchiasis and Opisthorchiasis (Liver fluke)
25 mg/kg
3
1
Opisthoriasis
2
Clonorchiasis
100 %
Paragonimiasis (Lung fluke)
25 mg/kg
3
2
cure rate 89-100%
Taeniasis & Diphyllobothriasis
T. saginata T. solium praziquantel
10 mg/kg single dose cure rate 97-100%
D.
latum
25 mg/kg single dose
T. solium
praziquantel 2
mature segment
segment
praziquantel
cysticercosis larvae
Neurocysticercosis
Praziquantel
50 mg/kg/day
3
14
drug of choice
neurocysticercosis albendazole
H. nana
Praziquantel drug of choice
25 mg/kg single dose
1
Hydatid disease
Praziquantel
adjunct
albendazole
cyst
praziquantel
albendazole
albendazole sulfoxide
active metabolite
albendazole
Other parasites
Fasiolopsiasis (Large intestinal fluke), Metagonimiasis (Small intestinal fluke)
25 mg/kg
3
1-2

headache, dizziness, drawsiness, nausea, vomiting, lassitude, abdominal

pain, loose stools, pruritus, urticaria, arthralgia, myalgia, low-grade fever
, pruritus, skin rashes
foreign protein
praziquantel

eosinophilia

neurocysticercosis 2

1)

2)

neurologic reactions
inflammatory reactions
headache, meningismus, nausea, vomiting, mental changes, seizures
48-72
analgesics, antiemetics, diuretics, anticonvulsants

Pyrantel pamoate
Pyrantel pamoate broad spectrum anthelmintic
pinworm (Enterobius
vermicularis), ascaris
Trichostrongylus orientalis (
nematode
)
hookworm
N. americanus
Pyrantel pamoate
trichuriasis strongyloides
analog pyrantel pamoate oxantel pamoate
trichuriasis
broad spectrum anthelmintics
Anthelmintic action
Pyrantel
Acetylcholine
tissue

depolarizing neuromuscular blocking agent

cholinesterase
paralysis

Pyrantel

Clinical uses

standard dose 11 mg/kg (maximum 1 g)

1. Enterobius vermicularis (pinworm)
single dose
2 4 cure rate
95 %
2. Ascaris lumbricoides (roundworm)
single dose
2
cure rate 85-100%
3. Hookworm and T. orientalis
single dose
A. duodenale T. orientalis
90% cure rate
N. americanus infection
moderate or heavy infection (
2000 1
)
3
Species
pyrantel pamoate
3
6

Mild
cramps, dizziness, drawsiness, headache, insomnia, rash, fever, weakness
Piperazine
Piperazine
tartrate

piperazine hexahydrate

Anthelmintic action
Piperazine
(ascaris)
neuromuscular transmission
neurotransmitter
paralysis
Piperazine therapeutic dose

nausea, vomiting, diarrhea, abdominal

piperazine salt

citrate, phosphate, adipate,

paralysis
block Acetylcholine myoneural junction
reversible
GABA
inhibitory

Clinical uses
- Piperazine alternative drugs
Ascaris
75 mg/kg/day (maximum 3.5 g)
2
cure rate
90 %
heavy infection
3-4
1
piperazine
piperazine
pinworm
7
- Piperazine
hook worm infection, trichuriasis strongyloidiasis
nausea, vomiting, diarrhea, abdominal pain, dizziness, headache
somnolence, dizziness, ataxia, seizures, chorea, visual disturbance
Piperazine
fever, edematous skin reaction, bronchospasm)

serum sickness like syndromes (

Diethylcarbamazine
Diethylcarbamazine
synthetic piperazine derivative
51% Diethylcarbamazine
drug of choice
filariasis (
loa) tropical eosinophilia
Anthelmintic action
Diethylcarbamazine immobilize microfilariae
defense mechanism host

urticaria,

citrate salt
active base
W. bancrofti
B. malayi), loiasis (Loa

surface structure
adult worm

microfilariae

Clinical uses
Diethylcarbamazine
1. W. bancrofti, B. malayi, Loa loa, B. timori
diethylcarbamazine drug of choice
serious
toxicity Microfilariae
adult parasite
course
2
mg/kg
3
W. bancrofti
allergic reaction microfilariae
2 mg/kg
, 2 mg/kg
2 2mg/kg
3
2 mg/kg
L. loa B.malayi
antihistamine
4-5
diethylcarbamazine
microfilariae
3-4
diethylcarbamazine
prophylaxis 300 mg
1
300 mg
3
loiasis 50 mg
bancroftian malayan filariasis
2. Onchocera volvulus
drug of choice ivermectin
diethylcarbamazine
microfilariae
reaction
Diethylcarbamazine microfilariae
adult stage
Diethylcarbamazine
onchoceriasis
suramin
adult
worm
3. Tropical eosinophilia
diethylcarbamazine
2 mg/kg
7
4. Mass therapy
Diethylcarbamazine
W. bancrofti
1 dose
12
1)
2-4
weakness, nausea, vomiting, dizziness, sleepiness
2)

headache, malaise, anorexia,

foreign protein

Katzung BG, ed. Basic and clinical pharmacology, 8th ed. New York: Lange medical books/McGraw-Hill;
2001.
Rang HP, Dale MM, Ritter JM, Pharmacology. 4th ed. Edinburgh: Churchill Livingstone; 2000.
Edwards CRW, Bouchier IAD, Haslett C, Chilvers ER. Davidsons Principles and practice of Medicine. 17th ed.
Edinburgh. Churchill Livingstone; 1995.

r
1.
Benzimidazole Albendazole, Mebendazole, Thiabendazole
microtubule-dependent glucose uptake
.
.
2.
intestinal tapeworm
pork tapeworm, beef tapeworm, fish tapeworm
cysticercosis
dwarf tapeworm
MgSO4
.
.
3. Praziquantel
calcium permeability cell membrane
paralysis

4.

tapeworm

niclosamide

.
.
5. Oxaminiquine drug of choice
blood fluke
.
.
6.
Praziquentel
neurocysticercosis

7.

8.

9.

10.

praziquentel

inflammatory reaction

.
pyrantel pamoate
piperazine
2
cholinesterase
ACh
.
.
Ivermectin
GABA transmission
hyperpolarization
.
.
Praziquentel
hydatid cyst
praziquentel
albendazole
albendazole
.
.
Niclosamide
oxidative phosphorylation
.
.

chloride channel

hydatid cyst

10