ANTHELMINTICS

FA R M A K O L O G I 2
 ANTHELMINTICS
Anthelmintics 
• obat yang dapat mengeluarkan cacing dari saluran GI  Vermifuge
(expel)
• membasmi cacing dewasa secara sistemik maupun yang menyerang
organ atau jaringan  Vermicide (kill)
Afinitas terhadap cacing tinggi, toks thd inang rendah

Pada tubuh inang hidup di:

• GIT
• Jaringan (larva migrasi)

Merugikan inang:
• Menghabiskan makanan
• Kehilangan darah
• sekresi toksin  merusak organ
 Cacing Patogen (Metazoa)
• Intestinal nematodes
(Ascariasis, Hookworms,
Trichuriasis, Enterobiasis,
Trichinosis, Strongyloidiasis)
• Blood and tissue nematodes
(Filariasis: W. bancrofti, B.
malayi, O. volvulus,)
Nematodes
(roundworms)
• Blood fluke (Schistosomes: S.
mansoni, S. japonicum,
S.haematobium, S. mekongi)
• Lung and liver flukes
(Paragonimus spp, Clonorchis
sinensis, Opisthorchis spp,
Fasciola hepatica)
Trematodes
(flukes)
• Taeniasis (Taenia solium
neurocysticercosis, T.
saginata)
• Diphyllobothriasis
(Diphyllobothrium latum)
• Hymenolepiasis (Hymenolepis
nana)
• Echinococcosis
(Echinococcus granulosus)
Cestodes
(flatworms and
tapeworms)
Albendazol
Benzimidazole carbamate
Spektrum luas
Absorbsi meningkat karna makanan berlemak
Dimetabolisme menjadi aktif  albendazole sulfoksida
Parasit Intraluminal  perut kosong
Parasit jaringan  makanan berlemak

MK:
menghambat sintesis mikrotubul nematoda
larvicidal : hydated disease, cysticercosis, ascariasis,
hookworm
Ovicidal: ascariasis, ancylostomiasis, trichuriasis
Penggunaan Klinis Albendazol

Ascariasis , trichuriasis,
Hydatid disease
hookworm, pinworm neurocysticercosis
(Echinococcosis)
inf.
• Dew,an>2th: SD • Aktif thd E.granulosus • +kortikosteroid
400mg • 400mg BD (dg mkn), • Symptomatic
• Ulang 2-3 h(asc) 1m parenchymal or
• 2w (pin) intraventicular cysts
Mebendazol
MK:
 blok uptake glukosa  penurunan cadangan glikogen
 Bekerja pada protein “ß tubulin” microtubular parasit
menghambat polimerisasi  penurunan pembentukan
mikrotubul.
 Mikrotubul penting untuk perkembangan larva, transport
karbohidrat, dan fungsi enzim, maintain the parasite tegument
and digestive apparatus

Absorbsi meningkat dengan makanan berlemak

 Afinitas terhadap tubulin mamalia embryotoxic
 KI ibu hamil
Mebendazol

Pharmacokinetics:
Absorpsi di GIT minimal (2-10%)  sangat efektif utk parasit di usus
75-90% oral dose  feses
t1/2 plasma : 1 h

ES:
Keluar askaris lewat mulut dan hidung  parasit lapar dan mati perlahan
Reaksi alergi, rambut rontok, granulocytopenia pada dosis tinggi
Penggunaan klinis Mebendazol
 Enterobiasis:

100mg single dose, repeated after 2-3 weeks  to kill the ova that have
develop later.
Strict hygienic measures and simultaneous treatment of all children
in the family or class is advocated to cut down autoinfection and person to
person infection
 Tapeworms:
200 mg BD for 4 consecutive days (less effective)
 Trichinella spiralis:
200 mg BD for 4 days; less effective than albendazole
 Hydatid disease
200-400 mg BD or TDS for 3-4 weeks; less effective than albendazole
  100mg chewable tab., 100mg/5mL susp.
Thiabendazole
 Aktif terhadap: round worm, hook worm, enterobius, trichuris, strongyloides

and Trichinella spiralis.

 Inhibit pertumbuhan telur dan larva, larva yang bermigrasi ke otot (T. Spiralis)

 MK=mebendazol

 Thiabendazole memiliki efek antiinflammatory, analgesic dan antipyretic 

ineffective in filariasis

 Pharmacokinetics

 Cepat diabsorbsi, dimetabolisme melalui hidroksilasi dan konjugasi

menjadi metabolit inaktif dan di ekskresi melalui urin

 Thiabendazole
Dosis
25 mg/kg/day in two divided doses taken after meals.
Tablet must be chewed

 0.5 g/tab.; 0.5g/5mL susp. (30 mL bottle)

 it used as alternative to albendazole for:

 Strongyloidiosis
Cutaneous larva migrans Give a 2 days course.
 Trichinosis – intestinal infestation If inadequate, repeat after
and larvae in muscles a gap of 2 days
Thiabendazole
Efek samping:
Mual, muntah, hilang nafsu makan, sakit kepala
Hindari mengendarai kendaraan
Gatal, sakit perut, diare
KI hamil, sakit hati dan ginjal
Diethylcarbamazine Citrate
 Obat pilihan untuk filariasis, loiasis, tropical eosinophilia

 Diberikan setelah makan

 Clinical uses: w.Bancrofti, B.malayi, B.timori, loa loa

 Loa:2w, inisial low dose (+antihistamin/kortiko) u/alergi

 50mgx1 (H-1), 50mgx3(H-2), 100mgx3(H-3), 2mg/kgx3/d~2-3w

 Kemoprofilaksis: 300mg/w (loa), 50mg/m(bancrofti,malayan

filariasis)

 MK: immobilizes microfilariae dan merubah struktur

permukaan lepas dr jaringan
 Ivermectin

 Obat pilihan untuk Strongyloidiasis, onchocerciasis (mikorfilaria)

 Obat alternatif utk W. bancrofti, B. malayi, Ascariasis, Enterobiasis,

and trichuriasis. (SD)

 MK: nematodes  tonic paralysis  potensisasi transmisi

GABAergic pada cacing  melalui Cl- channel
Tidak dapat mempengaruhi cestodes and trematodes
 afinitas rendah terhadap reseptor GABA mamalia dan tidak
dapat melewati blood-brain barrier (BBB)
 Penggunaan klinis invermectin
Onchocerciasis Strongyloidiasis lain2
• SD 150µg/kg pada • BD 200µg/kg • B.malayi
perut kosong • Immunocompromised • Mansonella ozzardi
• Dosis berulang  dosis
(setiap 6-12bln) berulang/bulan
• terapi 1 +
kortikosteroid 
mikrofilaria kornea

ES

Gatal, bengkak pada muka dan kaki

The Mazzoti reaction  respon imun terhadap antigen dari mikrofilaria

mati: gatal, sakit kepala, tachycardia

Piperazine
• 1950 ascariasis ,enterobiasis 100% cure rates; now,
second choice drug even for these worms
• MK:
• Blok transmisi neuromuskular melalui kerja antagonis ACh 
hiperpolarisasi  flaccid paralysis  cacing terlepas , hidup
• Afinitas terhadap reseptor kolinergik manusia <<

• Pharmacokinetics
• Oral absorbed, partially metabolized in liver and excreted in urine.
• It metabolites: mononitroso form  is carcinogenic
Piperazine
• ES:
• Safe and well tolerated
• Mual muntah , tidak nyaman perut, gatal
• Pusing
• Dosis toksik : kejang, kematian
• KI pada gagal ginjal dan epilepsi, aman pada ibu hamil

Penggunaan Klinis
Round worm: 4.5 g once a day for 2 cons. days;
Children 0.75 g/year of age (max 4.5 g)
It can be used during pregnancy while other drugs cannot be
used
Enterobiasis
50 mg/kg (max 2.5 g) once a day for 7 days or 75 mg/kg (max
4.5 g) single dose, repeated after 3 weeks
Pyrantel Pamoate
• Introduced in 1969, high efficacy against Ascariasis, Enterobiasis and
Ancylostomiasis
• Less active against Strongyloidiasis and inactive against Trichuris
and other worms
• Mekanisme kerja
• Aktivasi reseptor nikotinik kolinergik cacing depolarisasi
persisten  spastic paralysis.
• Toksisitas selektif  afinitas >> reseptor cacing
• Antagonis piperazine
(piperazine  hyperpolarization, flaccid paralysis)
• Only 10-15% of an oral dose is absorbed, this is partly metabolized
and excreted in urine
 Pyrantel Pamoate
• ES:
• Jarang efek samping
• Sakit kepala (jarang)
• nonirritant

• Penggunaan klinis:
• Ascariasis, Ancylostomiasis and Enterobiasis:
• A single dose of 10-15 mg/kg (max 1 g)
• A 3 days course for Necatoriasis and for Strongyloidiasis

  200, 250 mg/tab.; 25, 50 mg/mL susp. (8, 10 mL bottle)

Praziquantel
• Aktivitas terhadap schistosomes, other trematodes,
cestodes and their larval forms, cysticercosis

MK:
• menyebabkan keluarnya kalsium intraselular  kontraksi
dan paralisis cacing terlepas dari dinding saluran cerna

 Tabs should be swallowed whole with some liquid during meals.

Keeping tabs in mouth may release bitter taste that can produce
nausea or vomiting.
 Praziquantel
• Pharmacokinetics
• Absorbsi cepat di GIT
• Phenytoin, Carbamazepin, and possibly dexamethazone induksi
metabolisme praziquantel menurunkan bioavailability
• melewati BBB
• T1/2 (1.5 h)
• Metabolit diekskresi lewat urin

• ES

• Rasa pahit (mual)

• Sakit perut, sakit kepala, pusing

• Utk infeksi schistosomes and visceral flukes  parasit yg mati menyebankan gatal,
urtikaria, demam

Perhatian
• tidak digunakan untuk sistiserkosis mata  menyebabkan lesi
 Penggunaan klinis Praziquantel
• Dosis dewasa = anak
- 50-100 mg/kg/d PO, 14 d
- pengobatan jangka panjang (bulan) extraparenchymal infections

1. Tapeworms
- Single dose  cure rate 90-100%
- T. saginata, T. solium: 10 mg/kg single dose in the morning
- H. nana, D. latum: 15-25 mg/kg single dose in the morning
in case of heavy infestation, re-treatment after 1 week
2. Neurocysticercosis
- 1st drug for neurocysticercosis: 50 mg/kg daily in 3 divided doses for 15 days
kills the larvae lodged in brain and other tissues. Albendazole equally and
more effective. Praziquantel and Albendazole are being used as first line base
therapy
- also effective for dermal cysticercosis, but contraindicated in ocular cycticercosis
3. Scistosomes
- all three species can be treated with 40-75 mg/kg given once or in divided dose in
one day.
Nematoda

STH (soil transmitted

helminths) ascariasis,
trichuriasis, hookworm inf. Ascaris lumbricoides
 menyerang anak 
BZAs

Obat: mebendazol(ringan),
pyrantel pamoat (parah),
Terinfeksi melalu telur di Terapi tambahan suplemen
albendazol (piperazin
makanan atau tanah besi / transfusi darah
jarang< ES neurotoksisitas,
alergi)
Nematoda
filarial LF (lymphatic filariasis)
diethylcarbamazine+albendazol/
invermectin+albendazol  target kerja: tahap
mikrofilarial yang bersikulasi di darah atau
terbawa oleh vektor antropoda

Penyebab: Wuchereria bancrofti, brugia spp.

(sistem limfatik), mansonella spp (jaringan lain)

Disebarkan oleh gigitan nyamuk

 Cestoda
Taenia saginata (cacing Taenia solium (caing
pita sapi) pita babi)

Obat albendazol,
Obat  praziquantel, praziquantel,
Daging kurang matang Infeksi
niclosamide kortikosteroid (inflamasi
dr parasit yg mati)

Cacing dewasa di usus disebabkan

oleh daging kurang matang dg
cysticerci

Cysticercosis  infeksi sistemik disebabkan

larva  neurocysticercosis (meningitis,
epilepsi
Trematoda

Schistosomiasis Obat  praziquantel

S. Haematobium, S.
Mansoni, S.
Japonicum
THE END