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anthelmintik

pendahuluan
 Antelmintik atau obat cacing adalah obat yang digunakan untuk
memberantas atau mengurangi cacing dalam lumen usus atau jaringan
tubuh.
 Sebagian besar obat cacing efektif terhadap satu macam kelompok cacing,
sehingga diperlukan diagnosis yang tepat sebelum menggunakan obat
tertentu.
 Diagnosis dilakukan dengan menemukan cacing, telur cacing dan larva
dalam tinja, urin, sputum, darah atau jaringan lain penderita.
 Sebagian besar obat cacing diberikan secara oral yaitu pada saat makan atau
sesudah makan dan beberapa obat cacing perlu diberikan bersama pencahar.
Obat obat anticacing
 Mebendazol, Tiabendazol, Albendazol
 Piperazin, Dietilkarbamazin /DEC
 Pirantel, Oksantel
 Levamisol
 Praziquantel
 Niklosamida
 Ivermectin
 Banyak obat cacing memiliki khasiat yang efektif terhadap satu atau dua jenis
cacing saja. Hanya beberapa obat saja yang memiliki khasiat terhadap lebih
banyak jenis cacing (broad spectrum) seperti mebendazol, albendazol
 Mekanisme kerja obat cacing yaitu dengan menghambat proses penerusan
impuls neuromuskuler sehingga cacing dilumpuhkan. Mekanisme lainnya
dengan menghambat masuknya glukosa dan mempercepat penggunaan
(glikogen) pada cacing.
Albendazole
 Broad-spectrum oral anthelmintic,
 Indikasi:
 Cysticercosis
 pinworm (kremi)and hookworm infections (cacing tambang),
 ascariasis,
 trichuriasis,
 and strongyloidiasis
Dosis
 cutaneous larva migrans (400 mg daily for 3 days),
 visceral larva migrans (400 mg twice daily for 5 days),
 intestinal capillariasis (400 mg daily for 10 days),
 microsporidial infections (400 mg twice daily for 2 weeks or
longer), and
 gnathostomiasis (400 mg twice daily for 3 weeks).
 trichinosis (400 mg twice daily for 1-2 weeks) and
 clonorchiasis (400 mg twice daily for 1 week).
Side effect (SE)
 Penggunaan 1-3 hari hampir tanpa SE
 SE: Mild and transient epigastric distress, diarrhea, headache,
nausea, dizziness, lassitude, and insomnia
 In long-term use for hydatid disease, albendazole is well
tolerated, but it can cause abdominal distress, headaches,
fever, fatigue, alopecia, increases in liver enzymes, and
pancytopenia
 MOA: bersifat larvasid
Dietelcarbamazine
 Menyebabkan paralisis dan perubahan pada permukaan
membran mikrofilaria  hancur.
 Cepat diabsorpsi diusus, ekskresi lewat urin,
 70% bentuk metabolitnya.
 Dosis DEC citrate 1mgkgbb hari 1, bisa dinaikan setelah 3
hari sp 6mg/kgbb dibagi dalam dosis terbagi dan
dimaintanance selama 21 hari
 Indikasi: filariasis, Loiasis, and tropical eosinophilia.
 MOA: Dietilkarbamazin melumpuhkan mikrofilaria dan
mengubah struktur permukaannya, menggusur mereka dari
jaringan dan membuat mereka lebih rentan terhadap
kerusakan oleh mekanisme pertahanan host
 Dosis
 Filariasis: 2 - (for L loa) 3 weeks, with initial low doses to
reduce the incidence of allergic reactions to dying microfilariae.
This regimen is 50 mg (1 mg/kg in children) on day 1, three 50
mg doses on day 2, three 100 mg doses (2 mg/kg in children)
on day 3, and then 2 mg/kg three times per day to complete the
2-3 week course
Ivermectin
 Ivermectin is used only orally in humans. The drug is rapidly
absorbed, reaching maximum plasma concentrations 4 hours
after a 12 mg dose. The drug has a wide tissue distribution
and a volume of distribution of about 50 L. Its half-life is
about 16 hours. Excretion of the drug and its metabolites is
almost exclusively in the feces
 Indikasi
 A. ONCHOCERCIASIS
Treatment is with a single oral dose of ivermectin, 150 mcg/kg, with
water on an empty stomach. Doses are repeated; regimens vary from
monthly to less frequent (every 6-12 months) dosing schedules. After
acute therapy, treatment is repeated at 12-month intervals until the
adult worms die, which may take 10 years or longer. With the first
treatment only, patients with microfilariae in the cornea or anterior
chamber may be treated with corticosteroids to avoid inflammatory
eye reactions.

B. STRONGYLOIDIASIS
Treatment consists of two daily doses of 200 mcg/kg. In
immunosuppressed patients with disseminated infection, repeated
treatment is often needed, but cure may not be possible.
 Adverse reaction/adverse effect (AE)
 In strongyloidiasis treatment, infrequent side effects include
fatigue, dizziness, nausea, vomiting, abdominal pain, and rashes.
In onchocerciasis treatment, the adverse effects are principally
from the Mazotti reaction, due to killing of microfilariae.
The reaction includes fever, headache, dizziness, somnolence,
weakness, rash, increased pruritus, diarrhea, joint and muscle
pains, hypotension, tachycardia, lymphadenitis, lymphangitis,
and peripheral edema. This reaction starts on the first day and
peaks on the second day after treatment. The Mazotti reaction
occurs in 5-30% of persons and is generally mild, but it may be
more frequent and more severe in individuals who are not long-
term residents of onchocerciasisendemic areas
levamizole
 Dosis tunggal digunakan untuk Ascaris Trichostrongylus,
efektifitas sedang A.duodenale dan rendah untuk N.americanus
 - Cara kerja : meningkatkan aksi potensial dan menghambat
transmisi neuromukularcacing paralisis..
 - Absorpsi oral cepat dan lengkap. 60% obat diekskresi
bersama ureum.
mebendazole
 Efektif mengobati cacing gelang, cacing kremi, cacing
tambang dan T.trichiura,cacing pita.
 - Kerjanya merusak subseluler dan menghambat sekresi
asetilkolinesterase cacing, menghambat ambilan glukosa.
 - Absorpsi oral buruk (10%), dari yg diabsorbsi 90% terikat
protein. ekskresi terutama lewat urin dalam dalam bentuk
utuh.
 Mebendazole mungkin bertindak dengan menghambat
sintesis mikrotubulus.
 Obat membunuh telur cacing tambang, ascaris, dan Trichuris
 Dosis dewasa & anak > 2th 2-3 x 100mg
 SE/AE
 Short-term mebendazole therapy for intestinal nematodes is nearly
free of adverse effects. Mild nausea, vomiting, diarrhea, and
abdominal pain have been reported infrequently. Rare side effects,
usually with high-dose therapy, are hypersensitivity reactions (rash,
urticaria), agranulocytosis, alopecia, and elevation of liver enzymes.

Mebendazole is teratogenic in animals and therefore contraindicated


in pregnancy. It should be used with caution in children younger than
2 years of age because of limited experience and rare reports of
convulsions in this age group. Plasma levels may be decreased by
concomitant use of carbamazepine or phenytoin and increased by
cimetidine. Mebendazole should be used with caution in patients with
cirrhosis
Niridazole
 Efektif untuk S. haematobium dan S. mansoni.
 - Ekskresinya dalam bentuk metabolit melalui urine dan tinja.
 - Hati Hati-hati pada penderita gangguan fungsi hati, ginjal
dan darah.
 KI niridazole:
 Defisiensi enzym G6PD
METRIFONATE (TRICHLORFON)

 Metrifonate is a safe, low-cost alternative drug for the


treatment of Schistosoma haematobium infections.
 It is not active against S mansoni or S japonicum
 Metrifonate, an organophosphate compound, is rapidly
absorbed after oral administration. Following the standard
oral dose, peak blood levels are reached in 1-2 hours; the
half-life is about 1.5 hours.
 Clearance appears to be through nonenzymatic
transformation to dichlorvos, its active metabolite.
 Metrifonate and dichlorvos are well distributed to the tissues
and are completely eliminated in 24-48 hours
 MOA: cholinesterase inhibitionparalisis
 S haematobium,: a single oral dose of 7.5-10 mg/kg is given
three times at 14-day intervals.
 Adverse Reactions, Contraindications,
 mild and transient cholinergic symptoms, including nausea and
vomiting, diarrhea, abdominal pain, bronchospasm, headache,
sweating, fatigue, weakness, dizziness, and vertigo. These
symptoms may begin within 30 minutes and persist up to 12
hours.
Metrifonate should not be used after recent exposure to
insecticides or drugs that might potentiate cholinesterase
inhibition.
 Metrifonate is contraindicated in pregnancy
Drugs with definite risk of haemolysis
in most G6PD-deficient individuals
 Dapsone dan sulphones lain
 Methylthioninium chloride (methylene blue)
 Niridazole
 Nitrofurantoin
 Primaquin
 Primaquine African and Asian people)
 Quinolones (including ciprofloxacin, moxifloxacin, nalidixic
acid, norfloxacin, and ofloxacin)
 Sulphonamides (including co-trimoxazole; some
sulphonamides, e.g. sulfadiazine)
Drugs with possible risk of haemolysis
in some G6PD-deficient individuals
 Aspirin
 Clorokuin
 Menadion
 Probenezid
 Quinidine
Piperazine
 - Efektif terhadap Efektif terhadap A.lumbricoides dan
E.vermicularis.
 - Kerjanya menyebabkan blokade respon otot cacing terhadap
asetilkolin paralisis dan cacing mudah dikeluarkan oleh
peristaltik usus.
 - Absorpsi melalui saluran cerna, ekskresi melalui urine.
 KI relatif: hepatic impairment ; renal impairment ; epilepsy;
pregnancy
 Side-effects
 nausea, vomiting, colic, diarrhoea, allergic reactions including
urticaria, bronchospasm,
 Jarang:arthralgia, fever, Stevens-Johnson syndrome and
angioedema; rarely dizziness, muscular incoordination ;
drowsiness, nystagmus, vertigo, blurred vision, confusion
Pirantel pamoat
 Untuk cacing gelang, cacing kremi dan cacing tambang.
 - Kerjanya menimbulkan depolarisasi pada otot cacing dan
meningkatkan frekuensi imfuls, menghambat enzim
kolinesterase.
 - Absorpsi melalui usus tidak baik, ekskresi sebagian besar
bersama tinja, <15% lewat urine.
 Side effect: (ringan, jarang &sementara jika obat di stop): GI
disturbances( nausea, vomiting, tenesmus, anorexia,
diarrhea, abdominal cramps, and gastralgia)
Prazikuantel
 Efektif terhadap Cestoda dan Trematoda, seperti
S. mansoni &. S. japonicum.
 - Kerjanya :memblok depolarisasi junctionmelepaskan
asetylkholin&menghambat kholinesterasestimulasi
reseptor nikotinicparalisis spastik cacing lepas dari
tempatnya.
 - Absorpsi oral baik, ekskresi sebagian besar bersama urine.
 Side effect: headache, exacerbation of neurologic
signs and symptoms such as seizures, increased CSF
protein concentrations and anticysticercal IgG
levels, arachnoiditis, meningism, hyperthermia, and
intracranial hypertension, mual. muntah dll
Tiabendazole
 Efektif terhadap strongyloidiasis, askariasis, oksiuriasis dan
larva migrans kulit
 Kerjanya menghambat enzim fumarat reduktase cacing dan
enzim asetilkolinesterase cacing cacing mati.
 - Absorpsi lewat usus, 90% obat diekskresi bersama urine.
 Dosis:
 The standard dosage, 25 mg/kg (maximum, 1.5 g) twice daily,
should be given after meals. Tablets should be chewed. For
strongyloides infection, treatment is for 2 days. Cure rates are
reportedly 93%. A course can be repeated in 1 week if
indicated. In patients with hyperinfection syndrome, the
standard dose is continued twice daily for 5-7 days. For
cutaneous larva migrans, thiabendazole cream can be applied
topically or the oral drug can be given for 2 days (although
albendazole is less toxic and therefore preferred).
 Adverse Reactions, Contraindications, & Cautions

Thiabendazole is much more toxic than other benzimidazoles or


ivermectin, so other agents are now preferred for most
indications. Common adverse effects include dizziness, anorexia,
nausea, and vomiting. Less frequent problems are epigastric pain,
abdominal cramps, diarrhea, pruritus, headache, drowsiness, and
neuropsychiatric symptoms. Irreversible liver failure and fatal
Stevens-Johnson syndrome have been reported.

Experience with thiabendazole is limited in children weighing less


than 15 kg. The drug should not be used in pregnancy or in the
presence of hepatic or renal disease