FARMAKOLOGI ANTIPROTOZOA

Dr.Yani Mulyani,M.Si, Apt

Prodi S1 Farmasi
FF UBK- 2019
 PROTOZOA TAXONOMY

Sub – Kingdom Protozoa

PHYLUM PHYLUM
SARCOMASTIGOPHORA CILIOPHORA
PHYLUM
APICOMPLEXA

CLASS Class Class

Class
LOBOSEA Zoomastigophora Litostomatea
Sporozoa

Entamoeba
Trypanosoma
histolitica Plasmodium Paramecium
gambiense
vivax Caudatum
Entamoeba Trypanosoma
coli cruzi P.malariae Balantidium
coli
 ENTAMOEBA HISTOLITICA

Invasion of a person takes place when he swallows cysts with

water and food
 TRYPANOSOMES IN BLOOD
Tse-tse Flies
Kutu Triatoma
Megista

Three species are parasitic in man:

• -Trypanosoma gambiense,
• -Trypanosoma rhodesiense,
• -Trypanosoma cruzi.

Tr. Gambiense and Tr. rhodesiense cause the sleeping-sickness

(fever,anemia,enlargment of lymphatic nodes,inflammation of brain and
cerebral membranes) in man in Africa. They are found in the blood of
antilops from where they are transmitted to humans by tse-tse flies.

Tr. Cruzi is spread in South and Central America.It is transmitted to

humans by bugs “Triatoma megista” and causes chagas disease (American
Trypanosomiasis). Natural resevoirs are rats, squrrels, dogs, opossumes.
 LEISHMANIA.

It is pathogen of leishmaniasis
(cutaneous or visceral).
Leishmania tropica is the
causative agent of cutaneous
leishmaniasis which is transmitted
to humans by sand-flies of
Phlebotomus genus.
At the place of sand-flie’s sting a
red papular appears and then ulcer
forms. The ulcer cicatrizes and
forms a scar that remains after
treatment.
Leismania domovani causes visceral leishmaniosis (or Kala-azar).
The parasite attacks blood vessels, lymphatics, spleen, liver, red
bone marrow. The disease manifestes itself by fever, enlargment
of the spleen, liver, by rheumatic pains.
 LAMBLIA (GIARDIA).

It is an agent of lambliasis. The adult form

(trophozoite) has a pear shape, four pairs of
flagella, two nuclei, sucking discs and a supporting
shift-axostyle.

The parasite forms oval-shaped cysts, which are

invasional stage. It locates in the small
intestine and breaks down parental digestion.
Human being invaded by swallowing cysts with
water and food.
 TOXOPLASMA GONDII.

It causes toxoplasmosis and can be found in the forms:

• - adult forms-trophozoites,
• - cysts.

Humans ingest oocysts with meat , milk and dairy products of

animals sick with toxoplasmosis, uncooked infected eggs and
contaminated water or due to the direct contact with a cat.

Very dangerous is transplacental infection. It may cause embryo death or

birth of a cripped child. In this case trophozoite (endozoit) is invasional
stage.

Infection is often asymptomatic

TOXOPLASM
A GONDII
 PLASMODIUM.
The malarial parasites of man
include four species:
• - Pl. vivax - agent of tertian malaria,
• - Pl. malaria - agent of quartan
malaria,
• - Pl.falciparum - agent of tropical
malaria,
• - Pl.ovale – agent of tertien ovale -
malaria.
Life cycle involves sexual stage (sporogony) in the mosquito
Anopheles and asexual stage (schizogony) in man. Man is an
intermediate host and mosquito is a definitive host.
The life cycle passes 3 stages:
• a) in man:
• Exo - erythrocytic schizogony (liver phase),
• - Erythrocytic schizogony (blood phase).
• b) in mosquito:
• - Sporogony.
Clinical features of malaria include series of febrile paroxysms
followed by anemia and splenomegaly.
Life cycle of
Plasmodium
 PENGGOLONGAN OBAT
ANTIPROTOZOA

Amebiasis Leishmaniasis Toxoplasmosis Malaria Giardiasis

• Sodium • Pyrimethamine, • Metronidazol
• Metronidazole combination • Quinoline
stibogluconate • tinidazole
• Tinidazole • Pentamidine with • Anti folat • mepacrine
• Diloxanide isethionate Sulfasalazine, • Antibiotic hydrochloride
furoate klaritromisin, • Artemisin
• Amphotericine
azitromisin

Infeksi Amebiasis Infeksi Lesmania Infeksi Infeksi Infeksi Giardia

dysentri, dan yang ditularkan Toxoplasma plasmodium Lamblia
Entamoeba oleh Lalat gondii
Hytolitica
ANTI MALARIA
LIFE CYCLE OF THE MAL ARIAL PARASITE
PL ASMODIUM FALCIPARUM,
 PENGGOLONGAN OBAT

Gol. Kuinolin :
Kuinine, Kuinidine, Gol. Antibakteri :
Primakuin, Klorokuin, Sulfonamid,Tetrasiklin,
Amodiakuin, Meflokuine, Spiramisin, Azitromisin,
Halofantrin, Klindamisin, Rifampisin
primakuine,piperakuin

Gol. Antifolat : Gol. Artemisin :

Pirimetamin, Trimetropim, Artemisin,Artemer,
Proguanil, Klorprokuanil Artesunat
 ME CH ANI SME ACT I ONSOF ANT I MAL AR I A ON
DI FFE R ENT P H ASE S OF
T H E PAR ASI T E L I FE CY CL E :

1. Blood Schizontocidal Drugs:

• influence on Erythrocytic Schizonts

2. Tissue Schizontocidal Drugs:

• influence on Tissue Schizonts:
• a) Effective against Pre-Erythrocytic
• (primary tissue form);
• b) Effective against Exo-Erythrocytic
• (secondary tissue form).
3. Gametocytocidal drugs:
• influence on sexual forms 17
 Menghambat dihidrofolat menghambat sintesis
reduktase asam dihydrofolic
Contoh : Pirimetamin Contoh : Sulfonamid,
sulfodoksin

Golongan Antifolat Golongan Antibakteri

Mekanisme
kerja

Golongan Kuinolin
Golongan Artemisin

Menghambat polimerisasi heme, yang

Menghambat degradasi
substansi terakhir menjadi beracun untuk
hemoglobin
skizon
Contoh : artemeter
Contoh : klorokuin, kuinine, primaquine
Colour atlas of pharmacology
 TATALAKSANA PENGOBATAN

Malaria tanpa komplikasi

Malaria pada ibu hamil

Malaria berat

DIRJEN pengendalian penyakit dan kesehatan DEPKES RI.2008.pedoman penatalaksanaan

pengobatan malaria di indonesia; Jakarta
 TATAL AK SANA P E NG OB ATAN MAL AR I A B E R AT

DIRJEN pengendalian penyakit dan kesehatan DEPKES RI.2008.pedoman

penatalaksanaan pengobatan malaria di indonesia ; jakarta
Tatalaksana pengobatan malaria tanpa komplikasi
 Tatalaksana pengobatan malaria pada ibu hamil

DIRJEN Pengendalian Penyakit dan Kesehatan DEPKES RI.2008.Pedoman

Penatalaksanaan Pengobatan Malaria di Indonesia ; Jakarta
 CHEMOPROPHYLAXIS OF MALARIA
Area Antimalarial Adult prophylactic
tablets dose
Chloroquine Chloroquine 150mg base Two
resistance tablets weekly
present PLUS Proguanil 100 mg Two
tablets daily
OR Mefloquine 250 mg One
tablet weekly
Chloroquine Chloroquine 150mg base Two
resistance tablets weekly
absent OR Proguanil 100 mg Two
tablets daily
 CHEMOPROPHYLAXIS OF
MALARIA
• Chemoprophylaxis is begun 1 week before entering
the malarious area and is continued until 4 weeks
after leaving it.
• It is also important to avoid anopheline
mosquitoes, which bite at night. Long sleeves and
trousers should be worn outside the house.
Repellent creams and sprays can be used.
Screened windows, the use of a mosquito net and
burning repellent coils or tablets also reduce the
risk.
AMEBIASIS
 AMEBIASIS

Amebiasis adalah penyakit parasit yang manifestasinya pada saluran pencernaan yang spesifik.

Penyebab : Entamoeba histolytica

Serangan : hampir secara eksklusif yaitu menelan

kista Entamoeba histolytica yang ditemukan dalam
makanan atau air yang terkontaminasi makanan
CLASSIFICATION OF ANTIAMEBIC
DRUGS:

systemic Luminal Mixed

• Tinidazole • Diloxanide • luminal and

• metronidazole furoate systemic
• Chloroquine • Iodoquinol
• Emetine • Paromomycin
• Dehydroemetine • They act on the
• They are parasites in the
effective against lumen of the
amebas in the bowel only
intestinal wall
and liver.
 MEKANISME KERJA METRONIDAZOLE

Buka BNF 76 Hal 533

Buka Goodman 687
 PHARMACOKINETICS
• Metronidazole is completely and rapidly absorbed after oral
administration.
• For the treatment of amebiasis, it is usually administered with a
luminal amebicide, such as iodoquinol or paromomycin.
• This combination provides cure rates of greater than 90%.
• Metronidazole distributes well throughout body tissues and
fluids.
• Therapeutic levels can be found in vaginal and seminal fluids,
saliva, breast milk, and cerebrospinal fluid (CSF).
• Metabolism of the drug depends on hepatic oxidation of the
metronidazole side chain by mixed- function oxidase, followed
by glucuronidation.
• The drug accumulates in patients with severe hepatic disease.
 ADVERSE EFFECTS

• Dry mouth
• Metallic taste in the mouth and,
Commonly
• Nausea occurs
• Headache

• Vomiting, Diarrhea, insomnia, weakness, dizziness, thrush, dysuria, dark urine,

paraesthesias, and neutropenia are infrequently encountered.
• Pancreatitis along with CNS symptoms eg, ataxia, encephalopathy, and seizures are
rarely seen.
 DRUG INTERACTION

• Metronidazole has a disulfiram like effect when taken with alcohol.

• It potentiates the anticoagulant effect of coumarin (warfarin) type of anticoagulants.
• Phenytoin & phenobarbitone may increase the elimination of the drug, while
cimetidine decreases plasma clearance by manipulating with the hepatic cytochrome
enzymes.
• Lithium + metronidazole  lithium toxicity