Antiprotozoal Agents: PHR Sangita

ANTIPROTOZOAL
AGENTS
Phr Sangita
ANTIPROTOZOAL DRUGS
 These are drugs useful in infection caused by
the protozoa Entamoeba Histolytica.
 Amoebic cysts reaching the intestine
transform into trophozoites which either live
on the surface of colonic mucosa forms cysts
that pass into the stools and serve to
propagate the disease or invade the mucosa
form amoebic ulcers and cause acute
dysentery with blood and mucus in stool
 Occasionally the trophozoites pass into the
blood stream, reach the liver by portel vein
and cause amoebic liver absecess.
CLASSIFICATION
 Tissue amoebicides : They attain high concentration in
blood and tissues following oral or parenteral
administration
 For both intestinal and extraintestinal amoebiasis:
Nitroimidazoles : metronidazole , Tinidazole
 Alkaloids: Emetine
 For extraintestinal amoebiasis only: chloroquine
 Luminal amoebicides : They are poorly absorbed after oral

adminstration, hence attain high concentration in the bowel.
They act on cysts and trophozoites present close to the mucosa
 Amides : diloxanide furoate
 8-hydroxyquinolines: Quiniodochlor
 Antibiotics: tetracycline
 Therapeutic agents are classified as mixed,
luminal or systemic amoebicides according to
the site where the drug is effective.
 Luminal amebicides act on the parasite in
the lumen of the bowel, whereas systemic
agents are effective against amebiae in the
intestine wall and the liver.
MIXED AMEBICIDE : METRONIDAZOLE
 Amebiasis is generally treated with the

combination of metronidazole plus a luminal
amebicial drug, such as diloxanide furoate.
This combination provides cure rates of
greater than 90%.
 Metronidazole also has important
antibactericala activity.
Mode of action
 It is selective toxic not only for amoebae but
also for anaerobic organisms ( including
bacteria). Some anaerobic protozoan
parasites ( including amebae) possess
ferrodoxin – like low redox- potential,
electron transport proteins that participate
in metabolic electron removal reactions.
 The nitro group of metronidazole is able to
remove as an electron acceptor forming
reduced cyctotoxic compounds that binds to
proteins and DNA causing break and damage
microbial DNA resulting in cell death.
P.K:
 It is completely and rapidly absorbed after oral administration and
poorly bound to plasma protein

 It diffuses well into the tissues including brain
 It is metabolised in the liver and excreted in urin
 For treatment: It is administered with luminal amaebicide such as
diloxanide furoate.

 ADR:
 Common : GIT- nausea, vomiting epigastric distress and abdominal
cramps.
 Allergic reactions: skin rashes, urticaria,itching, flushing
 An unpleasant metallic taste is often experienced.
 Other effects include oral moniliasis( yeast infection of the mouth)
 dizziness, vertigo, numbness, headache
 if taken with alcohol, disulfiram like effect.
 Dose : amebiasis : adult – 500mg -750mg TDS for 10 days

Child- 35-50mg/kg in 3 divided dose for 10days
USES
 Amoebiasis : metronidazole 400-800mg tds
for 7 days
 Trichomonas vaginitis:
 Anaerobic infections: lung abscess, pelvic
inflammatory disease, brain abscess
 Guinea worm infection
LIMINAL AMEBICIDES: DILOXANIDE
FUROATE
 It is highly effective luminal amoebicide:
directly kills trophozoites responsible for
production of cysts, diloxanide furoate is
useful in the treatment of aymptomatic
possess of cysts.
 used along with tissue amebicide
metronidazole to treat serious intestinal and
extraintestinal infection.
 ADR: flatulence, nausea, abdominal cramps,

rashes.
MOA;
 After oral administration diloxanide furoate
is hydrolysed to diloxanide and furoic acid in
the intestinal mucosa and the diloxanide is
about 90% absorbed. However the
unabsorbed drug is the active amoebicide.
Dose :
 Adult; 500mgTDS for 10days
 Child; 20mg/kg TDS for 10days
 CI: pregnant women, child <2yrs.

Systemic amebicide : Emetine and
dyhydroemetine
 These are alternative agents for the treatment

of amebiasis.
 Emetine is a potent and directly acting
amoebicide—kill trophozoites but no effect on
cysts.
 They inhibit protein synthesis by blocking
intrarribosomal translocation of tRNA-
aminoacid complex
 Emetine are irritant, bitter in taste and
nauseating hence cannot be administered
orally. They are addministered through s.c, i.m
route.
 Dehydroemetine is probably less toxic than
emetine. So dehydroemetine used more than
emetine.
 It is slowly metabolized and excreted and can
accumulate. Its half life is 5 days. Clinical
observation is necessary when these drugs are
used
 ADR: pain at the site of injection, N,

cardiotoxicity , neuromuscular weakness,
dizziness, rashes.
 Dose : 60mg OD for 5day[ NMT 10days]

 CI: renal and cardiac patients, in young
children, pregnant women.
Nitroimidazole ( Metronidazole and
TInidazole)
 Drugs of choice for extraluminal amebiasis

 It kills trophozoites but not cysts
 Effectively eradicates intestinal and
extraintestinal tissue infections
 Completely absorbed after oral
administration
MOA:
 Disruption of DNA synthesis as well as nucleic acid
synthesis
 Bactericidal , amebicidal properties
 ADR: metallic taste, N, V, diarrhea, abdominal

cramps, dry mouth, insomnia, thrust
 DI: phenytoin, Phenobarbital  increase

elimination of nitroimidazole
Avoid alcohol during or 3 days after.
 Dose of Tinidazole :
 Amebiasis adult 2gm daily for 2-3days
 Child  50-60mg/kg for 5days
 Giardiasis -- adult 2gm single dose
Leishmaniacide
 There are three types of leishmaniasis:

cutaneous, mucocutaneous and visceral.
 Leishmaniasis is transmitted from animal to
humans by bite of infected sandflies. The
treatment of leishmaniasis is difficult becoz
the effective drugs are limited by their
toxicities.
 Drugs like sodium stibogluconate are used for
conventional therapy.
DRUGS USED ARE:
 Antimonial : sodium stibogluconate
 Diamidine : pentamidine
 Antifungal drugs: amphotericin B
ketoconazole
others : miltefosine
paromomycin
allopurinol
Sodium stibogluconate:
 Drug of choice for KALA-AZAR
 First line agents for cutaneous and visceral
leishmaniasis
 Not absorbed orally, excreted in urine
 Administered by I.V or IM route
ADR: fever, headache, myalgias, arthralgias and

rashes
 Dose :
 20mg/kg IV/IM OD for 20days ( cutaneous)
 20mg/kg IV/IM OD for 28days ( visceral and
mucocutaneous)
Antigiardial drugs
 Giardia lambia is the most commonly diagnosed
intestinal parasite. It invades the mucosa and
causes diarrhoea requiring treatment.

Quinacrine
 Acridine derivative primarily used to treat
Giardiasis but also effective against tapeworm,
malaria and leishmaniasis.
 MOA: bind to membrane phospholipids, blocking
phospholipase A2 activity.
 ADR: dizziness, headache,vomiting,
pigmentation of skin
 CI: pregnancy
Drugs for Trypanosomiasis
 It is fatal disease caused by species of trypanosomiasis.

 African sleeping sickness and American sleeping
sickness.
 In African sleeping sickness, the causative organisms
trypanosome brucei gambiense and trypamosoma
brucei rhosiense initially live and grow in the blood.
The parasites invades the CNS causing an inflammation
of the brain and spinal cord that produces the
characteristic lethargy and eventually continous sleep.
 Suramin
 Melarsoprol
 Nifurtimox
 Pentamidine isethionate
Nifurtimox
 It found use only in the treatment of acute
T.cruzi infection ( chagas disease)
 Suppressive not curative
 MOA: undergoes reduction and generates
intracellular oxygen radical ( hydrogen
peroxide)—highly reactive and toxic to
organism.
 ADR: N,V,bdominal pain, fever,insomnia.
 Dose : adult 8-10mg/kg/day in four divided
dose for 90-120days orally.
Sumarin
 It is sulphated napthylamine used early
treatment and prophylaxis of African
trypanosomiasis
 Not absorbed orally so given in IV route
 Half life is 90days
 ADR: hemolytic anemia, fever , chronic

diarrhea
 Dose –300mg initially then 1gm on days
1,3,7,14,21 days

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ANTIPROTOZOAL

 For extraintestinal amoebiasis only: chloroquine

 Luminal amoebicides : They are poorly absorbed after oral

 Amebiasis is generally treated with the

poorly bound to plasma protein

 Dose : amebiasis : adult – 500mg -750mg TDS for 10 days

 ADR: flatulence, nausea, abdominal cramps,

 CI: pregnant women, child <2yrs.

 These are alternative agents for the treatment

 ADR: pain at the site of injection, N,

 Dose : 60mg OD for 5day[ NMT 10days]

 Drugs of choice for extraluminal amebiasis

 ADR: metallic taste, N, V, diarrhea, abdominal

 DI: phenytoin, Phenobarbital  increase

 There are three types of leishmaniasis:

ADR: fever, headache, myalgias, arthralgias and

 It is fatal disease caused by species of trypanosomiasis.

 ADR: hemolytic anemia, fever , chronic

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