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Cestodes
Nematodes Trematodes
(flatworms and
(roundworms) (flukes)
tapeworms)
10
Pengobatan infeksi cacing
Agonist acetylcholine
Anthelmintics Target Inhibitor cholinesterase
Increase influx calcium
Neuromuscular transmission
muscle Agonist GABA
Nerve
Work on chloride ion
Neurotransmitter palsu
channel
Contoh: Piratel, piperazin, befenium,
Energy Production
Enzymes involved
Flacid paralisis
Substrate
Contoh: Mebendazol, niclosamide,
Spastic paralisis
Obat-Obat Untuk Pengobatan
Infeksi Cacing
Organisme yang menginfeksi Obat pilihan Obat
alternatif
Cacing gelang (nematoda)
Ascaris (gelang) Pir / Meb Pip, alb, atau Lev
Trichuris (cambuk) Meb Alb atau Pir
Necator (tambang) Pir / Meb Alb atau Lev
Strongyloides (benang) Tib / Ivr Alb atau Meb
E. Vermicularis (peniti/kremi) Meb / Pir Alb
Kombinasi infeksi ascaris, tricuris
dan cacing tambang Meb / Alb Alb
W. Brancofti (filariasis); B. Malayi
(filariasis); Loa loa DEC Ivr
Onchocerca volvulus Ivr DEC + Suramin
(onkosersiasis)
Obat-Obat Untuk Pengobatan
Infeksi Cacing
Organisme yang menginfeksi Obat pilihan Obat
alternatif
Cacing pipih (trematoda)
Schistosoma Pra Metrifonat
Clonorchis sinensis (pada hati) Pra Oksamnikuin
Paragonimus westermani (pada Pra Meb / Alb
paru)
Fasciola hepatica (pada hati domba) Bitionol Pra / emetin
Fasciolopsis buski (pada usus besar) Pra / niklosmid Tetrakloretilen
Cacing pita (cestoda)
T. Saginata ( pada sapi) Nik / Pra Meb
T. Solium ( pada babi) Nik / Pra
Diphyllobothrium latum ( pada Nik / Pra
ikan) Pra Nik
Hymenolepis nana (cacing pipih
kecil)
Tugas:
Benzimidazoles cari struktur molekul
1. Thiabendazole
2. Mebendazole
3. Albendazole
Pharmacokinetics
Oral absorbed, partially metabolized in liver and excreted in urine.
It metabolites: mononitroso form is carcinogenic
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Piperazine
Adverse effects
Safe and well tolerated
Nausea, vomiting, abdominal discomfort and urticaria are
occasional
Dizziness and excitement occur at high doses
Toxic doses: convulssion, death is due to respiratory
failure
Contraindicated in renal insufficiency and epileptics, but
it safe in the pregnant
Preparations
As its hexahydrate, or salts like citrate, phosphate,
adepate, all are water soluble and tasteless
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DEC
Uses
1. Filariasis:
2 mg/kg pc. 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
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DEC
Uses
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
DEC
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
The Mazzoti reaction an immune response to the antigens that are
released from dead or dying microfilariae: papular rashes, severe
itching, tachycardia and headache.
IVERMECTIN
Is an extremely potent semisynthetic derivative of the antinematodal
principle obtained from Streptomyces avermitilis.
Drug of choice for Onchocerciasis and strongyloidiasis
Alternative drug for single dose treatment of W. bancrofti, B. malayi,
Ascariasis, Enterobiasis, and trichuriasis.
Effective in visceral larva migrans
Mechanism of action
- nematodes tonic paralysis due to potentiation of GABAergic
transmission in the worm
Action through a special type of glutamate gate Cl- channel
in the susceptible worms.
* such channels are not involved in the motor control of
cestodes and trematodes, they are unaffected by ivermectin
- It has low affinity to mammalian GABA receptors and its inability
to penetrate the blood-brain barrier
8. IVERMECTIN
3. Scistosomes
- all three species can be treated with 40-75 mg/kg given once or in
divided dose in one day.
PRAZIQUANTEL
Pharmacokinetics
Rapidly absorbed from git and undergo first pass
metabolism in liver which limit its systemic bioavailability
Phenytoin, Carbamazepin, and possibly dexamethazone
induce P metabolism reduce its bioavailability
Adult Dose
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NICLOSAMIDE
1960 highly effective against cestodes: Taenia saginata, T.
solium, Diphyllobothrium latum and Hymenenolepis nana and
thread worm
Mechanism of action
- to act by inhibiting oxidative phosphorylation in
mitochondria and interfering with anaerobic generation
of ATP by the tape worm.
- Injured by niclosamide, the tape worm are partly digested
in the intestine.
- In case of T. solium, digested of dead segments can
be hazardous, because the ova released from them
develop into larvae in the intestine, penetrate its
wall and cause visceral cysticercosis
NICLOSAMIDE
Regimen for tape worm
Niclosamide (0.5 g tab.) after light breakfast, 2 tablets
chewed, swallowed with water, followed by another 2
tablets after 1h (total 2g);
Total dose for children 2-6 yrs is 1g
A saline purge is given 2h after the later dose to wash off the
worm
The scolex should be searched in the stools to be sure that
the worm will not grow again
NICLOSAMIDE
Regimen for tape worm
* For H. nana, the 2g dose is repeated daily for 5 days
needed because the cycticerci of H. nana (which are not
affected by niclosamide) develop in jejunal villi of the same
host and worm appear in the intestinal lumen after 4 days.
However, no purgative is required.
Treatment may have to be repeated after 10 days
NICLOSAMIDE
Adverse effects
Niclosamide is tasteless and non irritating
Minimally absorbed from git no systemic tox. occurs.
It is well tolerated minor abdominal symptoms
Malaise, pruritus and light headache are rare.
Safe during pregnancy and in patient with poor health
Kesimpulan
Obat-Obat Untuk Pengobatan
Infeksi Cacing
Organisme yang menginfeksi Obat pilihan Obat
alternatif
Cacing gelang (nematoda)
Ascaris (gelang) Pir / Meb Pip, alb, atau Lev
Trichuris (cambuk) Meb Alb atau Pir
Necator (tambang) Pir / Meb Alb atau Lev
Strongyloides (benang) Tib / Ivr Alb atau Meb
E. Vermicularis (peniti/kremi) Meb / Pir Alb
Kombinasi infeksi ascaris, tricuris
dan cacing tambang Meb / Alb Alb
W. Brancofti (filariasis); B. Malayi
(filariasis); Loa loa DEC Ivr
Onchocerca volvulus Ivr DEC + Suramin
(onkosersiasis)
Obat-Obat Untuk Pengobatan
Infeksi Cacing
Organisme yang menginfeksi Obat pilihan Obat
alternatif
Cacing pipih (trematoda)
Schistosoma Pra Metrifonat
Clonorchis sinensis (pada hati) Pra Oksamnikuin
Paragonimus westermani (pada Pra Meb / Alb
paru)
Fasciola hepatica (pada hati domba) Bitionol Pra / emetin
Fasciolopsis buski (pada usus besar) Pra / niklosmid Tetrakloretilen
Cacing pita (cestoda)
T. Saginata ( pada sapi) Nik / Pra Alb/Meb
T. Solium ( pada babi) Nik / Pra
Diphyllobothrium latum ( pada Nik / Pra
ikan) Pra Nik
Hymenolepis nana (cacing pipih
kecil)
No Obat MK Penggunaan
1 Thiabendazole Penghambatan produksi Nematoda : strongyloidiasis
energi (penghambatan dan trichinosis
enzim fumarat reduktase)
2 Mebendazole Penghambatan produksi Nematoda : Cacing kremi,
energi (mengganggu ambilan gelang, tambang, pita,
glukosa ) cambuk
3 Albendazole Penghambatan produksi askaris, kremi, tambang dan
energi (menghambat trikuriasis , Strongiloidiasis,
ambilan glukosa , Neurosistiserkosis
menurunkan pembentukan
ATP)
4 Pirantel activation worm nicotinic Nematoda : Kremi, gelang,
Pamoat cholinergic receptors cambuk
persistent
depolarization spastic
paralysis
5 Piperazin blocks neuromuscular Nematoda : Gelang, kremi
transmission
hyperpolarization
flaccid paralysis
No Obat MK Penggunaan
6 Dietilkarbamazin Penurunan kegiatan otot dan Nematoda : Filariasis,
(DEC) kemudian melumpuhkan loa-loa, O. volvulus
mikrofilaria.
7 Ivermectin GABAergic transmission in Nematoda :
the worm tonic paralysis Onchocerciasis and
strongyloidiasis
Trematoda dan
cestoda tdk efektif
8 Praziquantel Increases membrane Schistosomiasis &
permeability to calcium Taenia.
paralysis
Fasciola hepatica tdk
efektif
9 Niklosamid act by inhibiting oxidative cestodes: Taenia
phosphorylation ATP tape saginata, T. solium,
worm decrease Diphyllobothrium
latum and
Hymenenolepis nana
and thread worm
Terimakasih