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• Antelmintik

adalah obat yang digunakan untuk terapi infeksi


dan invasi cacing parasit nematoda, trematoda
dan cestoda dalam lumen usus atau jaringan
tubuh.
 umumnya efektif terhadap satu macam
cacing

- diberikan secara oral, pada saat makan atau


sesudah makan.
Beberapa jenis obat antelmintik yang direkomendasikan
digunakan dalam Pedoman Pengendalian Kecacingan
Depkes RI 2012 antara lain Pirantel Pamoat Mebendazol
dan Albendazol.
ANTHELMINT
IK
Obat yang digunakan untuk terapi infeksi dan invasi cacing parasit
nematoda, sestoda dan trematoda dalam lumen usus atau jaringan tubuh

Penggolongan obat
• Ada 3 golongan cacing :
– Nematodes (roundworms/c. gelang)
• Intestinal nematodes (Ascariasis, Hookworms, Trichuriasis,
Enterobiasis, Trichinosis,
Strongyloidiasis)
• Blood and tissue nematodes (Filariasis: W. bancrofti, B. malayi,
O. volvulus,)
– Trematodes (flukes)
• Blood fluke (Schistosomes: S. mansoni, S. japonicum,
S. haematobium, S. mekongi)
• Lung and liver flukes (Paragonimus spp, Clonorchis sinensis,
Opisthorchis spp, Fasciola hepatica)

– Cestodes (flatworms and tapeworms/c. pita)


• Taeniasis (Taenia solium neurocysticercosis, T. saginata)
• Diphyllobothriasis (Diphyllobothrium latum)
• Hymenolepiasis (Hymenolepis nana)
• Echinococcosis (Echinococcus granulosus)
Nematodes (round worms)
• Nematode usus
– Enterobius vermicularis (pinworm)
– Ascaris lumbricoides (round worm)
– Trichuris trichiuria (whipworm)
– Hookworms
• Ancylostoma duodenale
• Necator americanus
– Strongyloides stercoralis (threadworm)
– Trichinella spiralis (cacing otot)
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 Nematode darah dan jaringan
• Filariae
 Wuchereria bancrofti.
 Obstruction of lymphatic vessels and
elephantiasis.
 Filariasis.
 Brugia malayi
 Loa loa (inflammation of skin, eye)
 Onchocerca volvulus
 (ONCHOCERCIASIS or River blindness)
Cestodes (tape worms)
 Taenia saginata
(beef tapeworm)
• Taenia solium
(pig tapeworm)
• Hymenolepis nana
(dwarf tapeworm)
• Diphyllobothrium latum
(fish tapeworm)
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Trematodes (flukes)
• Schistosoma species
(blood fluke)
S. mansoni
S. japonicum
S. haematobium
• Fasciolopsis buski
(Intestinal fluke)
• Fasciola hepatica (Sheep liver fluke)
• Clonorchis sinensis (Chinese liver fluke)
• Paragonimus westermani (Lung fluke)
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1. Mebendazol
 Merupakan antelmintik spektrum luas
 Hasil terapi yang memuaskan baru nampak setelah 3 hari
pemberian obat

 Efeknya:

- Efektif untuk mengobati ascariasis/c. gelang,


oxyuriasis/c. kremi, ankilostomiasis/c. tambang
 MK :
- menyebabkan kerusakan struktur subselular dan
menghambat sekresi asetilkolinesterase cacing
- menghambat ambilan glukosa secara ireversibel
sehingga terjadi pengosongan glikogen pada cacing
• FK : tidak larut dalam air dan rasanya enak, pemberian
oral absorpsinya buruk < 10% dan akan meningkat bila
diberikan bersama makanan berlemak, diekskresi melalui
urin

• ESO
 Mual, muntah, diare dan sakit perut ringan  sementara
 Ekspulsi (pengeluaran) cacing lewat mulut
• KI : wanita hamil trimester pertama  teratogenik pd tikus
Tidak dianjurkan untuk anak < 2 th terhentinya
aliran empedu
• Sediaan :
- Roundworm
- Hookworm 100 mg twice a day for 3 consecutive days.
- Trichuris
 Enterobiasis:
- 100 mg 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.


2. Albendazol
• Derivat Benzimidazol  broad spectrum activity
• MK : bekerja dengan cara berikatan dengan B-tubulin
parasit sehingga menghambat polimerisasi mikrotubulus
dan memblok pengambilan glukosa oleh larva maupun
cacing dewasa sehingga persediaan glikogen menurun
dan pembentukan ATP berkurang akibatnya cacing akan
mati
• I : cacing kremi, c. tambang, c. Askaris atau trikuris
 FK : obat cepat dimetabolisme, diekskresi melalui urin,
makanan berlemak akan meningkatkan 4x lebih besar
dibanding perut kosong.
 FD : memblok pengambilan glukosa oleh larva maupun
cacing dewasa dan pembentukan ATP berkurang 
cacing mati
 Dosis : dewasa dan anak >2 th = 400 mg dosis tunggal
diberikan bersama makanan
 KI : anak < 2 th, wanita hamil dan menyusui dan sirosis
hati
 ESO : untuk penggunaan 1-3 hari aman
- nyeri ulu hati, diare, sakit kepala, mual, lemah
pusing, insomnia

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3. Thiabendazole
• Benzimidazol (1st polyanthelmintic , 1961)  all sp. of
nematodes infesting the git – round worm, hook worm,
enterobius, trichuris, strongyloides and Trichinella spiralis.
• Also inhibits development of the eggs of worms and kills
larvae.
• Menekan perkembangan dan migrasi larva T. spiralis
• Mechanism of action  as mebendazole
• Thiabendazole has antiinflammatory, analgesic and
antipyretic actions.  contribute to the inflammatory
conditions produced by larvae or worm in tissue, however, it
is ineffective in filariasis
• Thiabdzl  inhibits dermatophytic fungi also
 FK : cepat diserap melalui usus, dalam 2 hari 90% obat
diekskresi bersama urin dalam bentuk hidroksi dan
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terkonyugasi.
 Adverse effects
- Nausea, vomiting, loss of appetite, haedache, giddiness 
most common
- It can impair alertness  driving and operation machinery
should be prohibited
- Itching, abdominal pain, diarrhoea and a variety of other
symptoms
- Neurological symptoms, bradycardia, hypotension and
liver damage are rare.
- Hypersensitivity symptoms berupa sindrom Stevens-
Johnson yang fatal dan kerusakan hati yang irreversibel juga
telah dilaporkan, dosis besar pada tikus
- It should be avoided in pregnancy, liver and kidney disease.
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 Dose
- 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)

 Uses
- Because of freq. side effects and poor patient
acceptability, thiabdzl is used only when other better
tolerated drugs are ineffective
- it used as alternative to albendazole for:
Give a 2 days
- Strongyloidiosis course.
- Cutaneous larva migrans If inadequate,
- Trichinosis – intestinal infestation repeat after a
gap of 2 days
and larvae in muscles
4. Pirantel Pamoate
• Introduced in 1969, high efficacy against Ascariasis, Enterobiasis and
Ancylostomiasis and comparable to Mebendazol
• Less active against Strongyloidiasis and inactive against Trichuris
and other worms

• MK : menghambat enzim kolinesterase, menimbulkan depolarisasi


pada otot cacing dan meningkatkan frekuensi impuls sehingga cacing
mati dalam keadaan spastik

• FK : absorpsi sedikit melalui usus, ekskresi melalui urin dan tinja

• ES : jarang, ringan dan bersifat sementara, misalnya keluhan sal.


cerna, demam dan sakit kepala

• KI : wanita hamil dan anak < 2 th, hati2 bila diberikan pada pasien dg
riwayat penyakit hati  SGOT meningkat
 Use and administration
– Ascariasis, Ancylostomiasis and Enterobiasis:
• A single dose of 10-15 mg/kg (max 1 g)
• A 3 days course for Necatoriasis and for Strongyloidiasis
 Untuk enterobiasis (c. kremi) dianjurkan mengulang dosis setelah 2 minggu

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


5. Piperazine
• Introduced 1950, highly active against ascariasis and
enterobiasis 100% cure rates; now, second choice drug
even for these worms
• MK : mengganggu permeabilitas membran sel terhadap
ion yang berperan dalam mempertahankan potensial
istirahat sehingga menyebabkan hiperpolarisasi dan
supresi impuls spontan disertai paralisis pada cacing
• FK : penyerapan di sal. Cerna baik, ekskresi melalui urin
• ES : mempunyai batas keamanan yang lebar  aman
• KI : dapat memperkuat efek kejang pada pasien
epilepsi tidak boleh diberikan pada pasien epilepsi,
gangguan hati dan ginjal
• Sediaan : sirup 1 g/5 ml
• USES
– 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
6. LEVAMIZOLE, TETRAMIZOLE
• Tetramizole was developed in the late 1960s, it is racemic;
its levo isomer (levamizole) was found to be more active
and is preferred now.
• Both are active against many nematodes, but use is
restricted to ascariasis and ancylostomiasis, because
action on other worms is poor
• It kills strongyloides larvae, but adult worms are not
sensitive
• It interference with carbohydrate metabolism
• Preparations: 50, 150 mg/tab.; 50 mg/5mL syrup
• Kini digunakan sebagai terapi ajuvan penyakit imunologik
termasuk keganasan
• Uses
- Ascariasis: a single dose of levamizole 50mg for children 10-19kg
bw, 100mg for 20-39kg bw, and 150mg for >40kg bw and adult 
90% cure rates
- Owing to good tolerance and low dose used in mass treatment of
round worm
- It is an alternative drug for A. duodenale: 2 doses at 12h interval 
70-90% cure rate; it is less efficacious against necatoriasis
- others:
 Levamizole is an immunomodulator  restores depressed T cell
function.
• Adverse effects
– 1 or 2 doses used in helminthiasis are well tolerated
– Incidence of nausea, abdominal pain, giddiness, fatigue,
drowsiness or insomnia are low. 25
7. DIETHYLCARBAMAZINE CITRATE (DEC)
• Develop in 1948, it the only drug available for filarialis.

• MK : menurunkan aktivitas otot sehingga parasit seakan-akan


mengalami paralisis dan menyebabkan perubahan pada permukaan
membran mikrofilaria sehingga lebih mudah dihancurkan oleh sistem
imun tubuh.

• Oral  absorbed, distributed all over the body (Vd= 3-5 L/kg),
metabolized in liver and excreted in urine. Excreted is faster in acidic
urine. Plasma t1/2 of usual clinical doses is 4-12 h.

• DEC has highly selective effect on microfilaria (Mf).

• A dose of 2 mg/kg TDS clears Mf of W. bancrofti and B.malayi from


peripheral blood in 7 days. However, Mf in nodules and transudates
are not killed.
• Uses
1. Filariasis:
- 2 mg/kg TDS produces rapid symptomatic relief; Mf disappear
from blood and patient become non infective to mosquitoes in 7
days; however, the adult worm survives in the lymphatics and gives
rise to intermittent microfilaria and symptoms. Prolonged
treatment with different schedules  radical cure
- A total dose of 72-126 mg/kg spread over 12 days to several weeks
 satisfactory
- > 1 courses are needed with a gap of 3-4 weeks

- Elephantiasis (chronic lymphatic obstruction) is not


affected by DEC
• Uses
2. Tropical eosinophilia
- DEC 4 mg/kg BD-TDS: improved signs and symptoms of eosinophilic
lung or tropical eosinophilia

3. Loa loa and O. volvulus: small doses 25-50 mg initially

 Preparations
50, 100 mg tab., 120mg/5mL syr., 50mg/5mL pediatric syr.;
inj. 200mg DEC + CPZ maleate 5 mg and lignocaine 20mg in 10 mL vial
• Adverse effects
– Nausea, loss of appetide, headache, weakness and
dizziness  are common but generally not serious.
– A febrile reaction with rash, pruritus, enlargement of
lymph nodes and fall of BP may occurs due to mass
destruction of Mf and adult worms  mild to severe.
• The reaction can be minimized by
– starting with a low doses (0.5 mg/kg)
• Given an antihistaminics and/or Corticosteroids
– Leukocytosis and mild albuminuria are also noted
– The Mazzoti Reaction  very common side effect
and may be fatal
Doxycyclin
• Doxycycline digunakan sebagai kombinasi dengan Kina
dan Primakuin sebagai terapi lini kedua malaria
falciparum, dapat juga digunakan sebagai terapi profilaksis
malaria falciparum
• Dosis untuk terapi Malaria :
Terapi lini kedua malaria falciparum (kombinasi dengan
Kina dan Primakuin)
Usia > 15 th : 2x 3,5 mg/kgBB/hari
Usia 8-14 th : 2x 2,2 mg/kgBB/hari
Sebagai Profilaksis : 100 mg/hari diberikan 1-2 hari
sebelum bepergian sampai 4 minggu setelah kembali

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Tetracycline
• Digunakan sebagai kombinasi dengan Kina dan
Primakuin sebagai terapi lini kedua malaria falciparum.
• Dosis untuk Malaria : 4x 4-5 mg/kgBB/dosis

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