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Dr.Mahendra G S
Assistant Professor, NGSMIPS
Anthelmentics
 Humans are the primary hosts for the most of helminthic infections.
 Most worms produce in human sexually by producing eggs and larvae.
 These pass out of body and infect the secondary host Imature forms
invade humans via skin or GIT and mature to adult worms with
characteristic tissue distribution.
 Worms live in hosts alimentary canal.
 Worms or larvae live in other tissues of host body like muscles, viscera,
menninges, lungs, subcutaneous tissues.
Helminthic Infections
A) INTESTINAL ROUND WORMS (NEMATODES)
 Ascaris lmubricods (common round worm)
 Enterobius vermicularis (pin worm)
 Trichuris trichuria ( whip worm)
 Strongyloids stercoralis ( thread worm)
 Ankylostoma dudenale (hook worm)
B) TAPE WORMS (CESTODES)
 Taenia saginata(Beaf) ,
 Taenia solium(Pork), Hymenolepis nana(Dwarf), diphylobothrium latum(Fish)
Humans become infected by eating raw or under cooked meat containing larvae of
infected cattle or pig which has encysted in the animal muscle tissue.
Ascaris lumbricoids ( common round worm) Hookworm whipworm
Tricuris tricura(whip worm)
Tapeworm
cysticercosis
Trichinela spiralis
Hydateid cyct
Anthelmentics agents medicinal chemistry
Mebendazole is antiparasitic medication used to treat various types of worm infections.it is
part of the benzimidazole class of drugs and works by inhibiting the synthesis of
microtubules in parasites, disrupting glucose uptake, which eventually leads to the death
of the parasite.
Mebendazole
Mechanism of Action:
Mebendazole selectively inhibits the synthesis of microtubules by binding to tubulin
within the parasites. This results in impaired glucose uptake and digestive processes
within the worm, eventually leading to its death.
Mebendazole is commonly used for the treatment of:
 Ascariasis: Infection by the roundworm Ascaris lumbricoides.
 Enterobiasis (Pinworm Infection): Caused by Enterobius vermicularis.
 Trichuriasis: Infection with the whipworm Trichuris trichiura.
 Hookworm Infections: Caused by Ancylostoma duodenale or Necator americanus.
Side Effects:
Common side effects include:
 Abdominal pain, Diarrhea, Nausea
 Less common but more serious side effects can include allergic reactions, liver
issues, and in rare cases, bone marrow suppression. Regular monitoring of liver
function and blood counts may be advised during prolonged use.
ALBENDAZOLE
 It is a broad spectrum, It is a drug of choice (primary therapeutic application)
for treatment of hydatid disease and cysticercosis.
Mechanism of action: It inhibits microtubule synthesis in nematodes(intestinal
round worms) that irreversibly impairs glucose uptake, intestinal parasites are
immobilized and die slowly
methyl N-(6-propylsulfanyl-1H-benzimidazol-2-yl)carbamate
Used to treat a variety of parasitic worm infestations. It is commonly
prescribed for conditions such as:
 Hydatid Disease (Echinococcosis): A parasitic disease caused by tapeworm
larvae.
 Neurocysticercosis: Infection caused by the pork tapeworm Taenia solium,
leading to cysts in the brain.
 Ascariasis: An infection by the roundworm Ascaris lumbricoides.
 Hookworm: Caused by worms such as Ancylostoma duodenale and Necator
americanus.
 Trichuriasis: Infection with Trichuris trichiura (whipworm).
 Strongyloidiasis: Infection by Strongyloides stercoralis.
Side Effects:
Common side effects include:
Nausea
Vomiting
 Abdominal pain
 Headache
In rare cases, more serious side effects like bone marrow suppression,
liver damage, or allergic reactions can occur, so regular monitoring of blood
counts and liver function may be necessary during prolonged treatment.
Diethylcarbamazine*
Diethylcarbamazine (DEC) is an antiparasitic medication primarily used to
treat filarial infections. It is especially effective against certain parasitic
worm infestations that cause diseases like lymphatic filariasis and loiasis.
N,N-diethyl-4-methylpiperazine-1-carboxamide
Mechanism of Action:
The mechanism of DEC is not fully understood, DEC paralyzes the parasites by interfering
with their neuromuscular system, making them easier for the immune system to destroy. It
also alters the surface structure of the worms, increasing their vulnerability to immune attack.
Diethylcarbamazine is mainly used for:
 Lymphatic Filariasis: Caused by Wuchereria bancrofti, Brugia malayi, or Brugia
timori, which can lead to elephantiasis.
 Loiasis: An infection caused by the Loa loa worm,
 Tropical Pulmonary Eosinophilia: A severe lung condition associated with filarial
infections.
Side Effects:
Common side effects include:
 Nausea
 Vomiting
 Dizziness
 Headache
Anthelmentics agents medicinal chemistry
Ivermectin
Mechanism of Action:
Ivermectin works by binding to
glutamate-gated chloride channels in the
nerve and muscle cells of invertebrates,
leading to paralysis and death of the
parasite.
Ivermectin is a widely used antiparasitic medication with broad-spectrum activity. It
is effective against a variety of parasitic infections, including those caused by
nematodes (roundworms) and ectoparasites like lice and mites.
Ivermectin is commonly Used for:
1.Onchocerciasis (River Blindness): Caused by the parasite Onchocerca
volvulus.
2.Strongyloidiasis: Caused by the parasitic worm Strongyloides stercoralis.
3.Scabies: A skin infestation caused by the mite Sarcoptes scabiei.
4.Lice: For the treatment of head lice (Pediculus humanus capitis).
5.Lymphatic Filariasis: Often used in combination with other drugs like
diethylcarbamazine or albendazole for mass drug administration.
Side Effects
Common side effects include:
Nausea
Diarrhea
Dizziness
Fatigue
In onchocerciasis, a reaction known as the Mazzotti reaction may occur,
similar to what can happen with diethylcarbamazine. This reaction involves
itching, rash, fever, and swollen lymph nodes due to the body's response to the
death of the microfilariae.

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Anthelmentics agents medicinal chemistry

  • 1. Dr.Mahendra G S Assistant Professor, NGSMIPS Anthelmentics
  • 2. Humans are the primary hosts for the most of helminthic infections. Most worms produce in human sexually by producing eggs and larvae. These pass out of body and infect the secondary host Imature forms invade humans via skin or GIT and mature to adult worms with characteristic tissue distribution. Worms live in hosts alimentary canal. Worms or larvae live in other tissues of host body like muscles, viscera, menninges, lungs, subcutaneous tissues. Helminthic Infections
  • 3. A) INTESTINAL ROUND WORMS (NEMATODES) Ascaris lmubricods (common round worm) Enterobius vermicularis (pin worm) Trichuris trichuria ( whip worm) Strongyloids stercoralis ( thread worm) Ankylostoma dudenale (hook worm) B) TAPE WORMS (CESTODES) Taenia saginata(Beaf) , Taenia solium(Pork), Hymenolepis nana(Dwarf), diphylobothrium latum(Fish) Humans become infected by eating raw or under cooked meat containing larvae of infected cattle or pig which has encysted in the animal muscle tissue.
  • 4. Ascaris lumbricoids ( common round worm) Hookworm whipworm Tricuris tricura(whip worm) Tapeworm cysticercosis Trichinela spiralis
  • 7. Mebendazole is antiparasitic medication used to treat various types of worm infections.it is part of the benzimidazole class of drugs and works by inhibiting the synthesis of microtubules in parasites, disrupting glucose uptake, which eventually leads to the death of the parasite. Mebendazole Mechanism of Action: Mebendazole selectively inhibits the synthesis of microtubules by binding to tubulin within the parasites. This results in impaired glucose uptake and digestive processes within the worm, eventually leading to its death.
  • 8. Mebendazole is commonly used for the treatment of: Ascariasis: Infection by the roundworm Ascaris lumbricoides. Enterobiasis (Pinworm Infection): Caused by Enterobius vermicularis. Trichuriasis: Infection with the whipworm Trichuris trichiura. Hookworm Infections: Caused by Ancylostoma duodenale or Necator americanus. Side Effects: Common side effects include: Abdominal pain, Diarrhea, Nausea Less common but more serious side effects can include allergic reactions, liver issues, and in rare cases, bone marrow suppression. Regular monitoring of liver function and blood counts may be advised during prolonged use.
  • 9. ALBENDAZOLE It is a broad spectrum, It is a drug of choice (primary therapeutic application) for treatment of hydatid disease and cysticercosis. Mechanism of action: It inhibits microtubule synthesis in nematodes(intestinal round worms) that irreversibly impairs glucose uptake, intestinal parasites are immobilized and die slowly methyl N-(6-propylsulfanyl-1H-benzimidazol-2-yl)carbamate
  • 10. Used to treat a variety of parasitic worm infestations. It is commonly prescribed for conditions such as: Hydatid Disease (Echinococcosis): A parasitic disease caused by tapeworm larvae. Neurocysticercosis: Infection caused by the pork tapeworm Taenia solium, leading to cysts in the brain. Ascariasis: An infection by the roundworm Ascaris lumbricoides. Hookworm: Caused by worms such as Ancylostoma duodenale and Necator americanus. Trichuriasis: Infection with Trichuris trichiura (whipworm). Strongyloidiasis: Infection by Strongyloides stercoralis.
  • 11. Side Effects: Common side effects include: Nausea Vomiting Abdominal pain Headache In rare cases, more serious side effects like bone marrow suppression, liver damage, or allergic reactions can occur, so regular monitoring of blood counts and liver function may be necessary during prolonged treatment.
  • 12. Diethylcarbamazine* Diethylcarbamazine (DEC) is an antiparasitic medication primarily used to treat filarial infections. It is especially effective against certain parasitic worm infestations that cause diseases like lymphatic filariasis and loiasis. N,N-diethyl-4-methylpiperazine-1-carboxamide Mechanism of Action: The mechanism of DEC is not fully understood, DEC paralyzes the parasites by interfering with their neuromuscular system, making them easier for the immune system to destroy. It also alters the surface structure of the worms, increasing their vulnerability to immune attack.
  • 13. Diethylcarbamazine is mainly used for: Lymphatic Filariasis: Caused by Wuchereria bancrofti, Brugia malayi, or Brugia timori, which can lead to elephantiasis. Loiasis: An infection caused by the Loa loa worm, Tropical Pulmonary Eosinophilia: A severe lung condition associated with filarial infections. Side Effects: Common side effects include: Nausea Vomiting Dizziness Headache
  • 15. Ivermectin Mechanism of Action: Ivermectin works by binding to glutamate-gated chloride channels in the nerve and muscle cells of invertebrates, leading to paralysis and death of the parasite. Ivermectin is a widely used antiparasitic medication with broad-spectrum activity. It is effective against a variety of parasitic infections, including those caused by nematodes (roundworms) and ectoparasites like lice and mites.
  • 16. Ivermectin is commonly Used for: 1.Onchocerciasis (River Blindness): Caused by the parasite Onchocerca volvulus. 2.Strongyloidiasis: Caused by the parasitic worm Strongyloides stercoralis. 3.Scabies: A skin infestation caused by the mite Sarcoptes scabiei. 4.Lice: For the treatment of head lice (Pediculus humanus capitis). 5.Lymphatic Filariasis: Often used in combination with other drugs like diethylcarbamazine or albendazole for mass drug administration.
  • 17. Side Effects Common side effects include: Nausea Diarrhea Dizziness Fatigue In onchocerciasis, a reaction known as the Mazzotti reaction may occur, similar to what can happen with diethylcarbamazine. This reaction involves itching, rash, fever, and swollen lymph nodes due to the body's response to the death of the microfilariae.