MEDICINAL AGENTS

Lecture No : 15PD305
Anti-protozoal agents
Course Leader
Mrs. Dhanashree N

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 INTRODUCTION

• Antiprotozoal agents (Anti amoebic agents) : These agents are

chemical agents used in treatment of amoebiasis caused by entamoeba
histolytica.
• Types of Amoebiasis include
• Intestinal Amoebiasis : Characterized by dysentery and abdominal
cramps.
• Extra-Intestinal Amoebiasis : Liver
• Cutaneous Amoebiasis : Lungs, Spleen, Rarely Brain

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MODE OF INFECTION

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MODE OF INFECTION

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CLASSIFICATION OF ANTI-
AMOEBICIDES
• Luminal -It is active only against intestinal forms of amoeba. Ex:-
Diloxanide furoate.

• Systemic -. These agents have been employed primarily to treat

severe amoebic dysentery or hepatic abscesses. Ex : Dihydroemetine,
Choro -quinine

• Mixed -These agents are active against both intestinal and systemic
forms of amoeba. Eg :- Metronidazole, tinidazole, and ornidazole.

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CLASSIFICATIONS

1. Ipecacuanha alkaloids : Emetine, Dihydro-emetine

2. Nitroimidazole derivatives : Metronidazole, Tinidazole, Ornidazole
3. Diloxanide furonate
4. 8-Hydroxyquinoline : Di-iodohydroxyquinine, iodoquinol
5. Chloroquine
6. Carbarsone

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IPECAC ALKALOIDS

• The alkaloids emetine and dihydro-emetine are obtained by

separation from extracts of ipecac.
• They occur as levorotatory, light-sensitive white powders that are
insoluble in water.
• The alkaloids readily form water-soluble salts. Solutions of the
hydrochloride salts intended for intramuscular injection should be
adjusted to pH 3.5 and stored in light-resistant containers.
• Both are amoebicidal
• Available in the powder form
• Probably acts by inhibiting protein synthesis by Chain elongation.
• Useful in systemic amoebiasis.

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EMETINE AND DIHYDRO-EMETINE

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5- NITRO-IMIDAZOLES

• Metronidazole

• Tinidazole

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METRINDAZOLE

• Mixed amebicide, drug of choice for systematic &

intestinal amoebiasis.
• MOA: NO2 group accepts electron from ETC & diverts
the normal ETC pathway.
• The reduced metronidazole cause loss of helical structure
of DNA by breaking the strand resulting in cell Death.

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TINDAZOLE (TINDAMAX)(SPORINEX)

• Used in infections caused by amoebae giardia and trichomonas

preferred in metronidazole tolerance cases.
• It is of value in variety of bacterial infections.
• A part of combination therapy for Helicobacter pylori eradication.
• Side – effects : Nausea, vomiting, headache, increased blood pressure,
flushing and shortness of breath specially with intake of alcohol.
• Plasma Half-life : 12-14 Hrs.

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SYNTHESIS OF METRINDAZOLE

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SYNTHESIS OF TINDAZOLE

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ORNIDAZOLE

• Used for protozoal infections.

• Active against anaerobic bacteria including Pepto streptococcus
clostridium bacteriodes fragilis, prevotella, porphysomanas,
Tusbacterium, entamoebia histolytics, trichomonas vaginates and
grardia lambia.
• Also given along with ofloxacin to cure periodontitis, diarrhoea,
dysentery, gingivitis and pelvic inflammation disease.
• MOA : NO2 is reduced to active NH2 group which interferes with the
formation of microbial DNA loss of helical structure and DNA
breakdown.

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SECNIDAZOLE

• Selective for many anaerobic gram +ve and gram ve bacteria &
protozoa like trichomonas,
• Entamoeba giardia & bacteroides fragiles.

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DILOXANIDE FUROANATE
(FURAMIDE/ EUTAMIDE)
• It undergoes amide hydrolysis before exerting amoebicidal effect.
• Non-polar esters are more potent.
• Used in the treatment of asymptomatic carriers of E. Histolytica,.
• White crystalline powder, administered orally.

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8-HYDROXY QUINOLINE DERIVATIVES

• Yellowish micro-crystalline substance, light sensitive.

• Recommended for acute and chronic intestinal amoebiasis.
• Not effective in extraintestinal amoebiasis.
• Should not be used routinely for travellers diarrhoea, due to high
incidence of topic neuropathy.

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CLIOQUINOL(Vioform)

• Spongy , light sensitive, yellowish white powder is soluble in H2O.

• Initially used as a substitute for iodoform for many skin conditions
like eczema, psoriasis etc,
• Used as 3% ointment / cream for Trichomonas vaginalis.
• Best used for topical treatment for fungal infections( Athlete’s foot &
Jock itch).
• Also useful for intestinal amoebiasis.

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Carbarsone

• It is an organo-arsenic compound
• Used as anti-protozoal drug for treatment of amoebiasis and other
infections (histomoniasis)

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