Farmakologi

obat anti amuba

 Metronidazole
Derivat Nitroimidazole
• Farmakokinetik • Farmakodinamik
PO absorpsi baik, Mengurangi
topical 1 g produk yg
diabsor-psi 10 x berinteraksi dg
< 250 PO
DNA berakibat
Distribusi: saliva,
kehilangan
empedu, cairan
semen, ASI, struktur helix
tulang, liver, DNA 
abses liver, menghambat
paru, sekret sintesis protein
 Farmakokinetik  Penggunaan klinik
PB < 20 %, peak Ekstra intestinal
1-2 jam t1/2 (Abses Hepar)
neonatus 25-75 treatment of
jam dewasa 6-8 choice
jam meningkat
dg gangguan Infeksi intestinal
ginjal, ESRD 21 ringan s/d sedang
jam, (colitis non
Metabolisme 30- desentri)
60% di liver Infeksi intestinal
Eliminasi: urin 20- berat (desentri)
40 tak diubah, 6-
• Reaksi • Kontraindikasi
merugikan
Alergi, kehamilan
CNS: pusing, sakit
trimester I
kepala (10%)
(tratogenik pd
GI: mual, muntah,
diare, hilang binatang)
nafsu makan
(12%)
<1%: ataxia,
kejang,
pancreatitis,xeros
tomia, vaginal
kandi-diasis,
 Antiamuba yang lain
 Diloxanide furoate (Asimptomatik)
 Iodoquinol
 Paromomycin
 Emetine & Dehydroemetine
 Tetrasiklin
 Chloroquin
 Diloxanide furoate
 Diloxanide furoate is a dichloroacetamide
derivative. It is an effective luminal
amebicide but is not active against tissue
trophozoites. In the gut, diloxanide furoate
is split into diloxanide and furoic acid;
about 90% of the diloxanide is rapidly
absorbed and then conjugated to form the
glucuronide, which is promptly excreted in
the urine. The unabsorbed diloxanide is
the active antiamebic substance.
 The mechanism of action of diloxanide
furoate is unknown. Diloxanide furoate is
considered by many the drug of choice for
asymptomatic luminal infections, but it is
no longer available in the USA. It is used
with a tissue amebicide, usually
Metronidazole, to treat serious intestinal
and extraintestinal infections
 Diloxanide furoate does not produce
serious adverse effects. Flatulence is
common, but nausea and abdominal
cramps are infrequent and rashes are
rare. The drug is not recommended in
pregnancy.
 Iodoquinol
 Iodoquinol (diiodohydroxyquin) is a
halogenated hydroxyquinoline. It is an
effective luminal amebicide that is
commonly used with metronidazole to
treat amebic infections. Its
pharmacokinetic properties are poorly
understood. Ninety percent of the drug
is retained in the intestine and
excreted in the feces
 The remainder enters the circulation,
has a half-life of 11–14 hours, and is
excreted in the urine as glucuronides.
 The mechanism of action of iodoquinol
against trophozoites is unknown. It is
effective against organisms in the
bowel lumen but not against
trophozoites in the intestinal wall or
extraintestinal tissues.
 Infrequent adverse effects include

diarrhea—which usually stops after

several days—anorexia, nausea,
vomiting, abdominal pain, headache,
rash, and pruritus.
 It should be used with caution in
patients with optic neuropathy, renal or
thyroid disease, or nonamebic hepatic
disease.
 The drug should be discontinued if it

produces persistent diarrhea or signs

of iodine toxicity (dermatitis, urticaria,
pruritus, fever).
 It is contraindicated in patients with

intolerance to iodine.
 Paromomycin
 Paromomycin sulfate is an aminoglycoside
antibiotic that is not significantly absorbed
from the gastrointestinal tract. It is used
only as a luminal amebicide and has no
effect against extraintestinal amebic
infections.
 The small amount absorbed is slowly
excreted unchanged, mainly by glomerular
filtration. However, the drug may
accumulate with renal insufficiency and
contribute to renal toxicity.
 Paromomycin is an effective luminal
amebicide that appears to have similar
efficacy and probably less toxicity than
other agents.
Emetine & Dehydroemetine
• Emetine, an alkaloid derived from ipecac,
and dehydroemetine, a synthetic analog,
are effective against tissue trophozoites of
E histolytica, but because of major toxicity
concerns they have been almost
completely replaced by metronidazole.
• The drugs are administered parenterally
because oral preparations are absorbed
erratically.
• They accumulate in tissues and are
eliminated slowly via the kidneys.
• The use of emetine and dehydroemetine is
limited to unusual circumstances in which
severe amebiasis warrants effective
therapy and metronidazole cannot be
used.
• Dehydroemetine is preferred over emetine
because of its somewhat better toxicity
profile
• The drugs should be used to treat amebic
dysentery or amebic liver abscess for the
minimum period needed to relieve severe
symptoms (usually 3–5 days).
• Emetine and dehydroemetine should be
administered subcutaneously (preferred)
or intramuscularly (but never
intravenously) in a supervised setting.
• Adverse effects are generally mild when
the drugs are used for 3–5 days but
increase with prolonged use.
• They should not be used for more than 10
days. Pain and tenderness in the area of
injection are frequent, and sterile
abscesses may develop.
• Diarrhea is common. Other adverse
effects are nausea, vomiting, muscle
weakness and discomfort, and minor
electrocardiographic changes.
• Serious toxicities include cardiac
arrhythmias, heart failure, and
hypotension.
• The drugs should not be used in patients
with cardiac or renal disease, in young
children, or in pregnancy unless absolutely
necessary.