Anti Parasites

dr. Ave Olivia Rahman, M.Sc.

Bagian Farmakologi FKIK UNJA
KKI
 Kompetensi 4A:
 Penyakit cacing tambang, Strongiloidiasis, Askariasis,

Skistosomiasis, Taeniasis
 Gastroenteritris ec Giardiasis, Disentri basiler, disentri

amuba
 Vaginosis

 Cutaneus larva migran, Filariasis

 Pedikulosis kapitis, Pedikulosis pubis, Skabies

 Kompetensi 3A : Toksoplasmosis
 Kompetensi 2 : Leishmaniasis dan tripanosomiasis
 Classification of Parasites
 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 & trichomonas, leishmania &

trypanosoma, Sporozoa (toxoplasma,
isospora,cryptosporodium; plasmodium)
 Insecta :Pediculus
 Arachnida :sarcoptes scabei
Anti Helminthes :
Drugs of choice
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
Enterobiasis/oxyuris vermicularis.
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
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.
Infection Drug of choice Dose
15% Applied to the
Cutaneous larva
thiabendazole in affected area 2-3
migrans a water-soluble times daily for 5
cream base days.
(MINTEZOL)
Larva filariasis Diethylcarbamazine 6 mg/kg per day,
devided dose for 12
days. After meal
Mass Diethylcarbamazine 6 mg/kg in 24
administration administration, 12
times at weekly or
montly intervals or as a
single anual dose
Filariasis coexists Albendazole + single annual dose of
with either ivermectin ivermectin (200 μg/kg)
onchocerciasis or + a single annual dose
loiasis of albendazole (400
mg)
Filariasis W. Ivermectin single annual doses :
bancrofti , B. 400 μg/kg)
loiasis Diethylcarba initial dose : 50 mg (1 mg/kg
mazine in children) daily for 2-3
days, escalating to
maximally daily doses of 9
mg/kg in three doses for 2-3
weeks.
Onchocer Ivermectin Single oral doses 150 μg/kg,
ciasis given every 6 to 12 months
in adults and children ≥5
years
Capillaria Albendazole 400 mg/day for 10
philippinensis day .
cystic hydatid Albendazole Adult Dose :400 mg
Echinococcus given twice a day in.
granulosus Children :15 mg/kg per
day with maximum
dose 800 mg.
Treatment for 1 to 6
months
Neurocysticerc Albendazole Adult dose : 400 mg
osis caused by given twice a day.
larvalTaenia Children : 15 mg/kg per
solium day (maximum 800 mg)
in two doses for 8 to
30 days
schistosomiasis Praziquantel a single oral dose
of 40 mg/kg or
20 mg/kg three
times daily given 4
to 6 hours apart.

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 taeniasis
Praziquantel.
 Dose : 5-10 mg/Kg single dose
POSOLOGI

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)
Tablet  Kunyah 400 mg, 200
Albendazole
mg; Tab Sal Sel 400 mg;
suspensi 200 mg/5 ml
 (HELBEN)
Pyrantel Kaplet 125 mg; suspensi 125 mg/5
pamoat 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
Tablet 600 mg ( BILTRICIDE)
Praziquantel
Anti Protozoa : Drugs of choice
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 Metronidazole : 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, Furazolidone
Nonabsorbed aminoglycoside
paromomycin used to treat pregnant
women.
Trichomonia Metronidazole : A single oral dose 2 g.
sis Alternative dose : a 250-mg dose, three
times daily or a 375-mg dose given
twice daily for 7 days.
Can be repeated courses with intervals
of 4 to 6 weeks
Topical gel containing 0.75%
metronidazole or a 500- 1000 mg
vaginal suppository
Administration : metronidazole

• Tablet 250, tablet forte 500 mg

• Infus 500 mg/100 mL,
• suspensi 125mg/5ml (flagyl syrup)
• Intra vaginal : METROGEL-VAGINAL 0.75%. etc
Disease Drugs
Toxoplasmic encephalitis Antifolates pyrimethamine and
fetal infection sulfadiazine along with folinic acid
(LEUCOVORIN)
Alternative : sulfadiazine can be
substituted by clindamycin.
(For fetal infection : drug given only
after the first 12 to 14 weeks of
pregnancy) and to the newborn in
the postnatal period)
acute acquired Spiramycin
toxoplasmosis in
pregnancy (prevent
transmission to the fetus)
Disease Drugs
Cryptosporidiosis Nitazoxanide
Trypanosomiasis T. brucei Pentamidine
gambiense early-stage disease
T. brucei rhodesiense early- Suramin
stage disease.
Trypanosomiasis CNS stage Melarsoprol
Leishmaniasis Pentavalent antimony
visceral leishmaniasis Liposomal amphotericin B
Alternative : Miltefosine,
Paromomycin and pentamidine
 AntiScabies
 Scabicidal : permethrin (drug of choice), lindane,
ivermectin, crotamiton, Sulfur
 If a secondary infection (+)  antimicrobial agent
 Pruritus, itching (+)  oral antihistamine
 Crusted (+)  keratolitic
 Dosing :
◦ Permethrin cr 5%, liquid 1 %, Lotion 1 %. Single use,
may reapply in 7 days if live mites reappear
◦ Ivermectin topical lotion 0,5%, cream 1%, singe use
◦ Lindane lotion/sshampoo 1 %
◦ Crotamiton lotion/cream 10%. Only for adult patient
◦ Sulfur (5%-10%) ointment
Pharmacology of Antiparasites
 Benzimidazoles
 Thiabendazole, Mebendazol, Albendazole
 Broad-spectrum anthelmintic agents. Has activity against
most nematode worms, larval stages and ova.
 Excellent safety profiles. Primarily mild GI symptoms (1%)
 MOA : 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
Thiabendazole
 Rapidly absorbed from GI tract and skin; Tmax:
1-2 hr. Extensively hepatic metabolised,
Excreted in urine (90%) and faeces (5%)
 Side effect : gastrointestinal symptoms
 Thiabendazole has hepatotoxic potential.
Mebendazole
 Poorly absorbed from the GI tract, Highly protein-bound

(95%), Extensively hepatic metabolism; undergoes 1st-

pass elimination, Mainly excreted via faeces, urine (2%)

 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)
 Albendazole
 Absorption in gut variably (poor) and erratically; Enhanced
by the presence of fatty foods. Widely distributed; bile, CSF,
including hydatid cysts. Protein-binding: 70%, Extensive
hepatic first-pass metabolism. Excretion Via bile & urine
(small amounts). T1/2 : 4-15 hours.
 Transient mild GI symptoms.
 Not for pregnant women teratogenic and embryotoxic in
animals
 The safety in children < 2 years has not been established
Pyrantel Pamoate
 Absorption in gut poor , Excretion mainly in feses and 15% in
urin
 MOA : 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)
 Piperazine
 Readily absorbed from the GIT (oral). Distributes into
breast milk.Excretion via urine
 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


 Diethylcarbamazine
 Readily absorbed from the GI tract (oral); skin (topical);
conjunctiva (optical). Tmax : 1-2 hours after a single oral dose.
Widely distributed in tissues. rapid and extensive metabolism.
(Active metabolite : diethylcarbamazine- N-oxide). Excretion via
Urine
 Alkalinizing the urine can elevate its bioavaibility
 Dosage reduction for people with renal dysfunction or sustained
alkaline urine.
 Active against the microfilariae and adult worms of W. bancrofti,
B. malayi, B. timori and Loa loa but only against the microfilariae
of O. volvulus. It is also used in treatment of toxocariasis.
 Side Effects & Precautions
 Side effect : anorexia, nausea, headache, vomiting
(high doses)
 Usually disappear within a few days despite
continuation of therapy.
 Contraindicated for the treatment of onchocerciasis
causes severe reactions related to microfilarial
destruction  Pretreatment with glucocorticoids and
antihistamines
 Ivermectin
 Absorbed from the GI tract (oral); peak plasma
concentrations after 4 -5hr. Enters breast milk (<2%).
Protein-binding: About 93%. Extensively converted by
hepatic CYP3A4 to at least 10 metabolites. Excretion via
faeces & urine (<1%). T1/2 : 12 hr.
 MOA : 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.
 Side Effects & Precautions.

 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
 Praziquantel
 80% of dose is rapidly absorbed from the GIT (oral); Tmax 1-3 hr.
Distribution: CSF, enters breast milk, 80% bound to plasma
proteins. Rapid and extensive hepatic first-pass metabolism by
hydroxylation. Excretion via urine
 Bioavailability reduced by inducers of hepatic CYPs,
Dexamethasone.
 MOA : increases the cell permeability to Ca  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
 Side Effects & Precautions

 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)
 METRONIDAZOLE
 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)

 MOA : interact with DNA to cause destruction of helical DNA

structure and strand protein synthesis inhibition  cell death

Analog ...
 Tinidazole (TINDAMAX, FASIGYN, others)
 Secnidazole (SECZOL-DS, others),
 Ornidazole (TIBERAL, others).
 Pharmacokinetics
 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).

 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.

Side Effects & Precautions

 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.
 Drug Interaction
 Pricipitate CNS signs of lithium toxicity in patients receiving high
doses of lithium.
 Drug that inhibit hepatic microsomal metabolism (ex. Cimetidine)
 Plasma levels of metronidazol
 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
 Other Drugs
 ANTIHELMIINTHES : NICLOSAMIDE, LEVAMISOLE,
SURAMIN, METRIFONATE, OXAMNIQUINE
 ANTIPROTOZOA : DILOXANIDE, MEGLUMIE
ANTIMONIATE, PENTAMIDINE,
DEHYDROEMETINE, MELARSOPROL, LEVAMISOLE,
AMPHOTERICIN, EFLORNITHINE, MILTEFOSINE,
NITAZOXANIDE
 BENZYL BENZOATE, PERMETHRIN

TERIMA KASIH
 M enu lis Res ep

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. . Ny. W, 38 tahun mengeluh keputihan dan gatal didaerah kelaminnya.
Sekret berwarna kekuningan dan berbau. Dari hasi pemeriksaan
didapatkan kemerahan di daerah vagina. Dokter melakukan pemeriksaan
laboratorium terhadap sekret vagina. Berikan resep untuk Ny. W?
3. . Toni, 5 tahun, 20 kg dibawa ke dokter oleh ibunya karena diare. Diare
berlangsung 3 hari ini, 5x/hari. Tidak ada demam. Tidak ada dehidrasi.
Sebelumnya telah diberikan oralit dan preparat zinc tapi tidak ada
perbaikan. Dari hasil pemeriksaan feses didapatkan histolika. Berikan
resep untuk pasien ini?