Anti Amoebic Drugs

Anti amoebic Drugs
By: Dr. Kashif Iqbal

(PhD)
AMEBIASIS
Amebiasis (also called amebic dysentry) is
an infection of intestinal tract caused by
Entamoeba histolytica. The disease can be
acute or chronic, with the patients
showing varying degrees of illness, from
no symptoms to mild diarrhea to
fulminating dysentery (Dysentery in which
the symptoms are intensely acute, leading to
prostration (severe exhaust), collapse, and
often death).
The diagnosis is established by
isolating E. histolytica from fresh
feces.
Therapy is aimed not only at the
acutely ill patients but also at those
who are asymptomatic carriers,
because dormant E. histolytica may
cause future infections in the carrier
and be a potential source of infections
for others.
Protozoal infections are common
among the people in underdeveloped
tropical and subtropical countries,
where sanitary conditions, hygienic
practices and control of vectors of
transmission are inadequate.
Life cycle of
Entamoeba histolytica
Entamoeba histolytica exists in two forms:
1. Cysts form (That can survive out side the
body).
2. Trophozoites form (That are labile and don’t
persist outside the body).
Life cycle
Life cycle consists of following steps:
1. Ingestion of cysts
Cysts are ingested through feces, contaminated food or
water.
2. Formation of trophozoites
Cysts are passed into the lumen of intestine, where the
trophozoites are liberated.
3. Penetration and multiplication of trophozoites
Trophozoites are penetrated in intestinal wall and
multiply within colon wall. They either invade and
ulcerate the mucosa of large intestine or simply feed
on intestinal bacteria.
4. Systemic invasion
Large numbers of trophozoites within the
colon wall can also lead to systemic
invasion and caused liver abscess.
5. Cysts discarded
The trophozoites within the intestine are
slowly carried toward the rectum, where
they return to cyst form and are excreted
in feces.
Classification of amebicidal
drugs
According to the site where the drug is effective,
the amebicidal drugs are classified as:
• Luminal amebicides (Act on parasite in the
lumen of bowel)
• Systemic amebicides (Against amebas in
intestinal wall & liver)
• Mixed amebicides ( Against both the luminal
and systemic form of diseases).
MIXED AMEBICIDES
1. Metronidazole (Flagyl)
• Mixed amebicides are used for the treatment
of amebic infections.
• D.O.C for extraluminal amebiasis.
• Extensively used in the treatment of
infections caused by Giardia lamblia,
Trichomonas vaginalis, Anaerobic cocci, and
Anaerobic gram negative bacilli.
• Drug of choice for the treatment of
pseudomembranous colitis caused by the
anaerobic, gram positive bacillus
Clostridium difficile.
• Activated by anaerobic organisms to a
compound that damage parasite DNA.
Mechanism of action of
Metronidazole
Metronidazole is a prodrug. It requires
reductive activation of nitro group by
susceptible organism. Its selective toxicity
towards anaerobic and microaerophilic
pathogens such as E. histolytica, G. lamblia,
etc. These organisms contain electron transport
components such as ferridoxin, small Fe-S
proteins that have sufficiently negative redox
potential to donate electrons to metronidazole.
The single electron transfer forms a
highly reactive nitro radical anion
that kills susceptible organisms by
radical-mediated mechanisms that
target DNA, resulting in cell death.
Mechanism of action of
Metronidazole
Pharmacokinetics
Absorption
Metronidazole is usually given orally and it is
rapidly and completely absorbed achieving
peak plasma concentration in 1-3 hours, with
half life of about 7 hours.
Distribution
It is distributed rapidly throughout the tissues,
reaching high concentration in the body fluids,
including cerebrospinal fluid.
Metabolism
Metabolism of metronidazole occurs in liver.
Excretion
The parent drug and its metabolites are
excreted in the urine.
Contraindication:
Phenobarbital is the inducer of this enzymatic
system so it enhances the rate of metabolism
when used concomitantly. Cimetidine inhibit
this system so it prolongs the plasma half life
of metronidazole.
Clinical uses
◼ Amebiasis caused by E. histolytica
◼ Giardiasis
◼ Trichomoniasis caused by Trichomonas
vaginalis
◼ Anaerobic bacterial infections
◼ Pseudomembranous collitus
◼ Treatment of H. pylori
◼ Ulcerative gingivitis
Adverse effects:
An unpleasant metallic taste is often
experienced. The most common
adverse effects are those associated
with the gastrointestinal tract,
including nausea, vomiting, epigastric
distress, and abdominal cramps.
Urine:-dark/reddish-brown.
Which of the following drug is a
polyene?
A. Caspofungin
B. Amphotericin B
C. Nystatin
D. Griseofulvin
E. Both B & C
Which of the following drug
should be taken with cola drinks
A. Fluconazole
B. Ketoconazole
C. Itraconazole
D. Terconazole
Tick the drugs for the treatment of an
intestinal form of amebiasis:
◼ a) Metronidazole and diloxanide
◼ b) Diloxanide and streptomycin
◼ c) Diloxanide and Iodoquinol
◼ d) Emetine and metronidazole
What is diloxanide fuorate?
A. Luminal amebicide
B. Mixed
C. Systemic
Tinidazole:
Tinidazole is a second-generation
nitroimidazole that is similar to
metronidazole in spectrum of activity,
absorption, adverse effects and drug
interactions. It was approved by the U.S.
Food and Drug Administration in 2004 for
the treatment of amebiasis, amebic liver
abcess,
giardiasis and trichomoniasis but was used
outside the United States for decades prior
to approval. Tinidazole is as effective as
metronidazole, with a shorter course of
treatment, yet is more expensive than
generic metronidazole.
Iodoquinol
◼ Iodoquinol, a halogenated 8- hydroxy
quinolone.
◼ It is effective against Entamoeba histolytica,
luminal trophozite and cyst form.
◼ Side effects include rashes, diarrhea, dose-
related neuropathy, including rare optic
neuritis.
Long term use of drug should be avoided.
Paromomycin
◼ Aminoglycosides antiamebicides; alternative
agent for cryptosporidiosis.
◼ Not significantly absorbed from GIT, so
effective against the intestinal (luminal)
form of E. histolytica and tapeworm.
◼ Excreted in urine.
◼ Its antiamebic action is due to effect on cell
membranes, causing leakage and by
reducing the population of intestinal flora.
◼ Adverse effects:
➢ Gastrointestinal distress
➢ Diarrhea
SYSTEMIC AMEBICIDES
These drugs are useful in treating liver

abscesses or intestinal wall infections
caused by amebas.
Chloroquine:
◼ Used in combination with metronidazole
and diloxanide furoate to treat and
prevent amebic liver abscesses. It
eliminates trophozoites in liver abscesses.
◼ Also effective in treatment of malaria.
Emetine and Dehydroemetine:
Used as alternative agents for the treatment
of amebiasis.
◼ These inhibit protein synthesis by
blocking chain elongation.
◼ Intramuscular injection is the preferred
route.
◼ Emetine is concentrated in liver, where it
persists for a month after single dose.
◼ It is slowly metabolized and excreted,
and it can accumulate.
◼ Its half life in plasma is 5 days.
◼ The use of these, are limited by their
toxicities and close clinical observations
is necessary when these drugs are
administered.
◼ They should not be taken for more than 5
days.
◼ Dehydroemetine is only available under a
compassionate investigational new drug
protocol through the Centers of disease
Control and Prevention.
◼ The untoward effects are pain at the site
of infection, transient nausea,
cardiotoxicity, neuromuscular weakness,
dizziness, and rashes.
Some commonly used therapeutic options
for the treatment of amebiasis

Anti Amoebic Drugs

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Anti amoebic Drugs

By: Dr. Kashif Iqbal

These drugs are useful in treating liver

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