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Eukaryote (ex.

Prokaryote (Bacteria)
Protozoa) AMEBIASIS
True nucleus with Nucleoid; with loosely
multiple organized DNA • caused by Entamoeba histolytica
ANTIPROTOZOAL DRUGS chromosomes; lacking a nuclear o Tx: metronidazole + a luminal amebicidal
with nuclear membrane and drug, such as diloxanide furoate.
membrane and mitotic apparatus o This combination provides cure rates of
mitotic apparatus greater than 90%.
With organelles No organelles
(mitochondria and
lysosomes)
Larger (80s) Smaller (70s)
ribosomes ribosomes

Luminal amebicides

• Diloxanide furoate - for tx of • Chloroquine – to treat and prevent amebic


liver abscess, also malaria
asymptomatic passers of cysts; tx of
intestinal amebiasis • MOA – amebicide – unknown
- antimalarial – alter the properties of
• - CI: pregnant women and children DNA
under 2 y/o
• SE- visual disturbances, ototoxicity
• Paromomycin- an aminoglycoside
• Tetracycline

Mixed amebicide (luminal +


Systemic amebicides MALARIA
systemic)
• Emetine • Metronidazole – selectively toxic not only • four species of the protozoal genus
• Dehydroemetine for amebae but also for anaerobic plasmodium
– both emetine and dehydroemetine organisms and for anoxic or hypoxic cells • anopheles mosquito
inhibit protein synthesis & IM is the • - forms cytotoxic compounds that bind to
preferred route proteins and DNA to result in cell death
– S/E: pain at the site of injection, • - DOC for Amebiasis
transient nausea, cardiotoxicity (eg., • - GIT irritation, metallic taste; disulfiram-
arrhythmias, congestive heart failure), like effect
neuromuscular weakness, dizziness,
and rashes

Against exoerythrocytic form/ tissue


schizontocide
• Primaquine – MOA is not completely
understood; also gametocidal for all four
plasmodia species, transmission of the
disease can be interrupted.
Against erythrocytic form/ blood Against gametocytic form
• Quinine – for chloroquine-resistant organisms;
schizonticide fetotoxic
• Chloroquine –DOC in the treatment of • Mefloquine - effective single agent for Primaquine
erythrocytic falciparum malaria, except in multidrug-resistant forms of P. falciparum • MOA – unknown
resistant strains • Pyrimethamine – blood schizonticide and • Administer drug with meals or with
sporontocide antacids
• - less effective against vivax malaria
• - acts as a strong sporonticide in the
• - also has anti-inflammatory action (also mosquito’s gut when the mosquito ingests it
used in rheumatoid arthritis and discoid with the blood of the human host
lupus erythematosus) • - inhibits folate reduction
• MOA: alters the properties of DNA • - alone is effective against P. falciparum
• - in combination with a sulfonamide, it is also
used against P. malariae

ANTHELMINTHIC DRUGS NEMATODES (round worms)


b. Mebendazole
Three major groups of helminthes (or a. Ivermectin
worms), the nematodes, trematodes and • DOC for the treatment of onchocerciasis
• DOC: whipworm, pinworm,
cestodes (river blindness) hookworm and roundworm
. antihelminthic drugs are aimed at • effective against scabies • binds to and interferes with the
metabolic targets that are present in the • The killing of the microfilaria can result in synthesis of microtubules and
parasite a Mazotti-like reaction (fever, headache, also by decreasing glucose
dizziness, somnolence, hypotension,
etc.) uptake.
• CI: pregnancy; meningitis • CI: pregnancy – embryotoxic
and teratogenic

TREMATODES (flukes)
c. Pyrantelpamoate – poorly
absorbed orally, acts as a o Praziquantel • SE: Nausea, abdominal pain,
depolarizing neuromuscular • broad spectrum of activity against headache, malaise and dizziness
blocking agent (paralyzes the trematodes (flukes) and cestodes
(tapeworms) • CI: Hypersensitivity, ocular
worm)
• causes spastic paralysis of worms
cysticercosis
d. Thiabendazole
• higher doses - tegumental damage in
- MOA - unknown
the worms, which activates host
defense mechanism

CESTODES (tapeworms)
oNiclosamide – DOC for most
cestode infection; laxative is
administered prior to oral
administration of niclosamide;
alcohol should be avoided within
1 day of niclosamide

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