dr. Ave Olivia Rahman, M.Sc.

Bagian Farmakologi FKIK UNJA

 Penyakit cacing tambang 4A

 Strongiloidiasis 4A

 Askariasis 4A

 Skistosomiasis 4A

 Taeniasis 4A

 Gastroenteritris ec Giardiasis

4A

 Disentri basiler, disentri amuba

4A
 Helminthes :
 Intestinal nematoda : ascaris (roundworm), hookworm
(necator & ancylostoma), whipworm/trichuris, strongyloides,
pinworm/threadworm (oxyuris), trichinella.
 Tissue nematoda:wucheria, Brugia, loa-loa, onchocerca
 Trematoda flat worm: blood (schistosoma)
 Cestoda (tapeworm) : Tanium
 Protozoa: entamoeba, giardia
STRONGY Thiabendazole 25 mg/kg, twice
LOIDIASIS daily after meals
for 2 days.
Maximum dose :
3 g/day.
Albendazole 400 mg daily for 3
days
Ivermectin a single dose of
150-200 μg/kg
Early Thiabendazole 25 mg/kg twice
trichinosis daily for 7 days.
Enterobiasis
Mebendazole a single 100 mg tablet  if
needed, a second given after
2 weeks
Albendazole a single oral 400 mg dose.
Children (12- 24 months)  a
single oral 200 mg
Pyrantel pamoat a single oral dose of 11
mg/kg, to a maximum of 1 g
Ascariasis, trichuriasis, hookworm infections
Mebendazole 100 mg twice daily for 3
consecutive days (or a
single dose 500mg tablet).
Albendazole a single oral 400 mg dose.
Children (12- 24 months) 
a single oral 200 mg.
Extended 3-4 days
Ivermectin single annual dose of
ivermectin (200 μg/kg)
Pyrantel pamoat a single oral dose of 11
mg/kg, to a maximum of 1 g
schistosomia Praziquantel a single oral
sis dose of 40 mg/kg
Metrifonate 7,5-10 mg/kg on
3 occasions at
intervals of 2
weeks
Oxamniquine According area
(15-60 mg/kg
divided into 2
doses)
Intestinal Praziquantel 5-10 mg/Kg
taeniasis single dose
 Broad-spectrum anthelmintic agents
 Excellent safety profiles. Primarily mild GI
symptoms (1%)
 Include :
1. Thiabendazole
2. Mebendazole
3. Albendazole
 Has activity against most nematode worms, larval
stages and ova.
 Interfering the worm’s source of energy by different
mechanisme (inhibit fumarate-reductase system,
destroying the cytoplasmic microtubules in the
worm's intestinal cells, inhibits tubulin
polymerization  This blocks the uptake of glucose
and other nutrients)
 Absorption: Rapidly absorbed from GI tract
and skin; Tmax: 1-2 hr.
 Metabolism: Extensively hepatic
metabolised.
 Excretion: Excreted in urine (90%) and
faeces (5%)
 Side effect : gastrointestinal symptoms
 Thiabendazole has hepatotoxic potential.
 Absorption: Poorly absorbed from the GI tract.

 Distribution: Highly protein-bound (95%)

 Metabolism: Extensively hepatic; undergoes 1st-pass

elimination.

 Excretion: Mainly via faeces (as unchanged drug and

metabolites); via urine (2%, as unchanged drug and

metabolites).

 Cimetidine can increase its bioavailability

 Mebendazole does not cause significant
systemic toxicity in routine clinical use
 Contraindications : not for pregnant women
or to children < 2 years (a potent
embryotoxin and teratogen in laboratory
animals)
 Absorption in gut : variably (poor) and erratically .
Enhanced by the presence of fatty foods.
 Distribution: Widely distributed; bile, CSF,
including hydatid cysts. Protein-binding: 70%
 Metabolism: Extensive hepatic first-pass
metabolism; converted to albendazole sulfoxide.
 Excretion: Via bile; via urine (small amounts). T1/2
: 4-15 hours.
 Transient mild GI symptoms.
 Not for pregnant women teratogenic and
embryotoxic in animals (teratogenic and
embryotoxic in animals)
 The safety in children < 2 years has not
been established.
Thiabendazole Tablet kunyah 500 mg;
suspensi 500 mg/5 mL
(MINTEZOL).
Mebendazole Tablet 100 mg, 500 mg;
suspensi 100 mg/ 5 ml
(vermox 500, gavox)
Albendazole Tablet Kunyah 400 mg, 200
mg; Tab Sal Sel 400 mg;
suspensi 200 mg/5
ml (HELBEN)
 Absorption in gut : poor
 Excretion mainly in feses and 15% in urin

Mechanism of Action
Open nonselective cation channels and induce
persistent activation of nicotinic acetylcholine
receptors, inhibits cholinesterase  spastic
paralysis of the worm.
 Transient and mild GI symptoms, headache,
dizziness, rash, and fever.
 contraindication :pregnant patients and
children < 2 years
 Pyrantel pamoate and piperazine should not
be used together (antagonistic effects on
parasites)
 Absorption: Readily absorbed from the GIT
(oral).
 Distribution: Distributes into breast milk.
 Excretion: Via urine (as metabolites).
 It produces a neuromuscular block resulting in
muscle paralysis of the worms which are
consequently dislodged and expelled in the
faeces.
 Piperazine is effective against the intestinal
Ascaris lumbricoides, Enterobius vermicularis
 Absorption: Absorbed from the GI tract (oral); peak
plasma concentrations after 4 -5hr.
 Distribution: Enters breast milk (<2%). Protein-
binding: About 93%.
 Metabolism : Extensively converted by hepatic
CYP3A4 to at least 10 metabolites.
 Excretion: Via faeces (as metabolites), via urine
(<1%). Plasma elimination half-life: 12 hr.
 Selectively binds and with high affinity to
glutamate-gated chloride ion channels 
leading to an increase in the permeability of
cell membranes to chloride ions 
hyperpolarization of the nerve or muscle cell
 death of the parasite.
 Mazzotti-like reactions to dying microfilariae (relate to
the microfilarial burden, the duration and type of filarial
infection)
 Contraindicated in conditions with an impaired blood–
brain barrier
 Not approved for use in children < 5 years and
pregnant women
 Lactating women taking the drug secrete low levels in
their milk
 Absorption: 80% of dose is rapidly absorbed from the GIT
(oral); Tmax 1-3 hr.
Distribution: CSF, enters breast milk. 80% bound to plasma
proteins.
 Metabolism: Rapid and extensive hepatic first-pass
metabolism by hydroxylation.
 Excretion: Via urine (as metabolites); elimination half-life: 1-
1.5 hr (parent drug), 4 hr (metabolites).
 Its bioavailability is reduced by inducers of hepatic CYPs,
Dexamethasone.
 It increases the cell permeability to Ca in
schistosomes  causing strong contractions
and paralysis of worm musculature 
detachment of suckers from the blood vessel
walls and to dislodgement.
 A broad spectrum of activity against
trematodes and cestodes
 Abdominal discomfort, nausea, diarrhea, headache,
dizziness, and drowsiness (transient and dose-relate)
 Safe in children over 4 years of age
 Low levels of the drug appear in the maternal milk,
 No evidence of mutagenic, carcinogenic, teratogenic.
 Contraindicated in ocular cysticercosis (irreversibly
damage the eye)
Pyrantel pamoat Kaplet 125 mg; suspensi 125 mg/5
ml (combantrin; Upixon Susp 360
(25 mg/5 mL)
Piperazine Ascarzan Sir 1 g/5 mL, Ascomin lar
oral 1 g/5 mL, Combicitrine Sir 125
mg/5 mL, Piperacyl Sir 1 g/5 mL
Diethyl (HETRAZAN tab 50, 100 mg; sirup
carbamazine 120mg/5mL)
Ivermectin Tablet 6 mg
Praziquantel Tablet 600 mg ( BILTRICIDE)
Disease Drugs
Amebiasis Metronidazole
adult dose : 500 - 750 mg orally three
times daily for 7 to 10 days.
Children dose : 35-50 mg/kg daily given
in three divided doses for 7 to 10 days.

Alternative dose for amebic liver abscess

: single oral dose 2.4 g daily for 2 days
Alternative : Tinidazole, ornidazole,
dehydroemetine and chloroquine,
Nitazoxanide
E. histolytica luminal agents : Nonabsorbed
trophozoites aminoglycoside paromomycin and the 8-
residing within hydroxyquinoline compound iodoquinol
the gut lumen.
Giardiasis Adult 250 – 500 mg three time daily for 5
– 7 days or 2 g one daily for 3 days
Children : 5 mg/kg BB 3 three times
daily for 5-7 days
A single dose of tinidazole (TINDAMAX).
Alternative, Metronidazole for 5-day,
Furazolidone
Nonabsorbed aminoglycoside
paromomycin used to treat pregnant
women.
 Metronidazole is a relatively inexpensive, highly
versatile drug
 Effective against a broad spectrum of anaerobic and
microaerophilic bacteria (gram-negative and gram-
positive bacteria, G. Lamblia, T. vaginalis , E.
Histolytica, Bacteroides, Clostridium, Helicobacter,
Campylobacter spp. , Fusobacterium, Peptococcus,
Peptostreptococcus, Eubacterium)
 Tinidazole (TINDAMAX, FASIGYN, others)
 Secnidazole (SECZOL-DS, others),
 Ornidazole (TIBERAL, others).
 Absorption: Readily absorbed from the GI tract (oral), poorly absorbed from

the vagina (intravaginal); peak plasma concentrations after 1-2 hr (oral), 5-

12 hr (rectal), 8 hr (intravaginal). May be delayed by the presence of food.

 Distribution: Protein-binding: <20%. Widely distributed in body tissues and

fluids (bile, bone, breast milk, cerebral abscesses, CSF, liver and liver

abscesses, saliva, semenal fluid, vaginal secretions, crosses the placenta and

rapidly enters fetal circulation.

 Metabolism: Hepatic via side-chain oxidation and glucuronide formation.

 Excretion: Mainly via urine (as metabolites); via faeces (small amounts).

Elimination half-life: 8 hr; longer in neonates and severe hepatic impairment

 Metronidazole is converted to reduction
products that interact with DNA to cause
destruction of helical DNA structure and
strand leading to a protein synthesis
inhibition and cell death in susceptible
organisms..
 Trichomoniasis, Amaebiasis, Giardiasis

 Metronidazole intravenously  A loading dose of 15

mg/kg is followed 6 hours later by a maintenance dose

of 7.5 mg/kg every 6 hours, usually for 7 to 10 days.

 Prophylaxis of postoperative mixed bacterial infections

 Bacterial vaginosis.

 Infection H. Pylori  combination metronidazole with

other antibiotics and a proton pump inhibitor

 Clostridium difficile infection  250-500 mg
orally three times daily for 7 to 14 days (or
even longer)
 Control colonic Crohn’s disease  750 mg
three times daily for prolonged periods may be
necessary
 Headache, nausea, dry mouth, metallic taste,
vomiting, diarrhea, and abdominal distress.
 Furry tongue, glossitis, and stomatitis 
associated with an exacerbation of candidiasis.
 Neurotoxic effects  dizziness, vertigo,
encephalopathy, convulsions, incoordination,
paresthesias and ataxia  discontinuation of
metronidazole.
 Pricipitate CNS signs of lithium toxicity in patients
receiving high doses of lithium.

 Drug that inhibit hepatic microsomal metabolism (ex.

Cimetidine)  Plasma levels of metronidazo

 Coumadin anticoagulants  prolong the prothrombin

time

 Patients with severe hepatic disease  reduced dosage

 Metronidazole and disulfiram or any disulfiram- like drug

should not be taken together  confusional and
psychotic states
• Tablet 250, tablet forte 500 mg
• Infus 500 mg/100 mL,
• suspensi 125mg/5ml (flagyl syrup)
• Intra vaginal : METROGEL-VAGINAL 0.75%. etc
 Nitazoxanide and its active metabolite, tizoxanide

(desacetyl-nitazoxanide), inhibit the growth of sporozoites

and oocytes of C. parvum and inhibit the growth of the

trophozoites of G. intestinalis, E. histolytica, etc

 activity against the intestinal helminths: Hymenolepsis

nana, Trichuris trichura, Ascaris lumbricoides, Enterobius

vermicularis, Ancylostoma duodenale, Strongyloides
stercoralis, and the liver fluke Fasciola hepatica.
Clostridium spp. and H. pylori
 Absorption : good
 Bioavailability after an oral dose is excellent,
Tmax 1 to 4 .
 Distribution : 99.9% bound to plasma
proteins.
 Excretion : urine, bile, and feces,
 Treatment of G. intestinalis infection in children
under the age of 12
 Treatment of diarrhea in children under 12
caused by cryptosporidia
 For children 12 - 47 months : 100 mg every 12
hours for 3 days;
 for children 4 - 11 years : 200 mg every 12
hours for 3 days
 Abdominal pain, diarrhea, vomiting, and
headache
 A greenish tint to the urine
 In pregnancy, itazoxanide is considered a
category B
1. Ana, 5 tahun, 15 kg, dibawa ibunya berobat
ke dokter dengan keluhan gatal di daerah
anus pada malam hari. Nafsu makan
menurun dan berat badan tidak naik. Dari
hasil pemeriksaan ditemukan telur cacing di
daerah anus. Berikan resep obat cacing
untuk ana?
2. Toni, 5 tahun dibawa ke dokter oleh ibunya
karena diare. Diare berlangsung 3 hari ini,
5x/hari. Tidak ada demam. Sebelumnya telah
diberikan oralit dan preparat zinc tapi tidak
ada perbaikan. Dari hasil pemeriksaan feses
didapatkan histolika. Berikan resep untuk
pasien ini?