Medicinal chemistry-Antihelmintics agents-Pharm.D sylabus

1. ANTIHELMINTICS
BY
KENCHA SWATHI

2. INTRODUCTION
› Helmintics are parasitic to humans/animals.
› They are derived from 2 phylla
1. Platyhelminthes Cestodes(Tapeworms)
Trematodes(Fluke worms)
2.Nemathelminthes(Nematodes) –True round worms
› Infection of helminthes are called as Infestation.
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3. ANTIHELMINTICS-CLASSIFICATION
› These are the drugs that have capability to get rid(expel) off from the
body of parasitic worms or helminthes are called as antihelmintics.
Classification:
1.Phenols and its derivatives-Niclosamide,Bithionol
2.Piperazine derivatives-Piperazine citrate,Diethylcarbamazine citrate
3.Antimalarial agents- Quinacrine,Chloroquine
4.Other heterocyclic compounds-Pyrantel pamoate,Mebendazole,
Thiabendazole,Albendazole
5.Natural products-Ivermectin
6.Miscellaneous compounds-Tetrachloro ethylene, Antimony potassium
tartarate
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4. BITHIONOL NICLOSAMIDE
› Uses: Antihelmintic drug
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5. PIPERAZINE CITRATE
Uses:Antihelmintic in the treatment of pin worm (Enterobius
vermicularis) & round worm (Ascaris lubricoides) infestation.
MOA:It blocks the response of ascaris muscle to acetylcholine
causing flaccid paralysis in the worm which is dislodged from
the intestinal wall & expelled in the faeces.
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6. DIETHYL CARBAMAZINE CITRATE
Uses:It is effective against various forms of filariasis including
bancrofts,onchocerciasis ,Laviasis and ascariasis.
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7. QUINACRINE CHLOROQUINE
Uses: Antimalarial drug
Effective against worminfestation.
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8. PYRANTEL PAMOATE
Uses: In the treatment of infestations caused by pinworm and
roundworms.
MOA:It is depolarizing neuromuscular blocking agent that
causes spastic paralysis in susceptible helminthes.
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9. ALBENDAZOLE
Uses:Antihelmintic
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10. MEBENDAZOLE
Uses:Broad spectrum antihelmintic
Effective against a variety of nematode infestations like
whipworm,pinworm,roundworm and hookworm.
MOA:Irreversibly it blocks glucose uptake in susceptible
helminthes.Thereby it depletes glycogen storage in the parasite.
It will also inhibit the celldivision in nematodes.
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11. THIABENDAZOLE
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12. IVERMECTIN
Ivermectin is a member of a family of structurally complex
antibiotics produced by fermentation with a strains of
streptomyces avermytilis.
Uses:It is active against nematode infestations.
It is effective for the treatment of onchocerciasis(river
blindness) which is caused by round worm onchocera volvulus.
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13. TETRACHLORO ETHYLENE
Uses:Active against nematodes and trematodes
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14. POTASSIUM ANTIMONY TARTARATE
Uses: Used against schistosoma(blood fluke infestation)-
schistosomiasis
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15. THANK YOU
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