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Introduction:
• Anti-helminthics are drugs either kill (vermicide) or expel
(vermifuge) infesting helminthics (worms).
• In the human body, GIT is the abode of many helminthics, but
some also live in tissues, or their larvae migrate into tissues.
• They harm the host by depriving him of food, causing blood
loss, injury to organs, intestinal or lymphatic obstruction and by
secreting toxins.
FDAapproved new drugs:
• Moxidectin
• Triclabendazole
• Closantel
• Emodepside
Moxidectin
• Potent, broad-spectrum endectocide.
• Semi-synthetic methoxine
• Moxidectin has a longer half-life in adipose tissue than ivermectin because of
its liposolubility.
• MOA:
Selectively binds to GABA-A and glutamate-gated chloride ion channels
(which are vital for the function of invertebrate nerve and muscle cells).
It presents activity against the parasite but it does not kill them.
Once moxidectin is bound, there is an increased permeability leading to an
influx of chloride ions and flaccid paralysis of the parasite
Indication:
 River blindness (Onchocerca volvulus): 8 mg orally, taken once
as a single dose.
ADR:
 Headache
 Hypotension
 Hyponatremia
 Eosinophilia
 Pruritus
Triclabendazole
• Narrow spectrum agent and unique among benzimidazole in its highly
specific activity against Fascioliasis.
MOA:
Triclabendazole are absorbed by the outer body covering of the mature and immature
worms.
Causing reduction in the resting membrane potential, inhibition of tubulin function
(changes at position 82 (glutamic acid) and position 91 (threonine)) as well as protein
and enzyme synthesis necessary of survival.
This metabolic disturbances leads to an inhibition of motility, inhibition of
spermatogenesis and egg/embryonic cells.
Indication:
Fascioliasis (total dose of 20 mg/kg-10 mg/kg doses given on Days 1
and 3).
ADR:
 Yellow skin or eyes
 Abdominal pain (expulsion of dye worms)
 Vomiting
 Indigestion
Closantel
 Closantel is a broad-spectrum antiparasitic agent used against several species and
developmental stages of trematodes, nematodes and arthropods.
MOA:
Decouples the mitochondrial oxidative phosphorylation
Leads to inhibition of ATP synthesis
Seems to occur through supression of the activity of succinate dehydrogenase and fumarate
reductase .
Cause death of the parasite
Indication:
 Fasciola hepatica (liver fluke).
ADR:
 Difficulty breathing
 Swelling of face, lips, toungue..etc
 Rashes
 Red swollen blisters or peeling skin with or without fever
 Wheezing
Emodepside:
 Broad spectrum, Semisynthetic compound whose precursor is a metabolite of the
fungus Mycelia sterile.
 potent antihelminthic drug used in combination with praziquantel
MOA:
Drug bind to the lactrophilin receptor presynaptically
Which activates a complex signal transmission cascade that eventually results in the
release of inhibitory neuropeptides into the synaptic gap
Resulting ion influx that occurs postsynaptically results in the inhibition of pharyngeal
pump function that leads to paralysis and death of susceptible nematodes
Indication:
 River blindness (onchocerciasis).
 Treatment of intestinal nematodes.
 To control Hookworm, roundworm, and Tapeworm Infection in Cats.
ADR:
 Hair loss
 Nervousness
 Salivation
 Eye irritation
 Tremor
Neurocysticercosis:
 Neurocysticercosis is a preventable parasitic infection caused by larval cysts
(enclosed sacs containing the immature stage of a parasite) of the pork
tapeworm (Taenia solium).
 Larval cysts in the brain cause a form of cysticercosis
called neurocysticercosis which can lead to seizures.
Treatment:
 Albendazole is now preferred over praziquantel; bec-
ause:
 Course of treatment is shorter (8-15 days)
 Cheaper
 High cure rate
 Corticosteroids enhance absorption
REFERENCE:
 http://what-when-how.com/medical-microbiology-and-infection/tissue-
helminths-parasitology-medical-microbiology-and-infection/
 https://www.emro.who.int/health-topics/helminthiasis/index.html
 Goodman and Gilman’s, The pharmacological basis of therapuetics,
12TH edition, Page number: 1444-1459
 https://www.slideshare.net/ParasuramanParasuraman/anthelmintic-
drugs
 https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020666s005
s006lbl.pdf
 https://www.mdpi.com/1422-0067/21/14/4957
 https://go.drugbank.com/drugs/DB11431
 https://medlineplus.gov/druginfo/meds/a619048.html
 https://pubmed.ncbi.nlm.nih.gov/33674322/
ANTI-HELMINTHICS KD.pptx

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ANTI-HELMINTHICS KD.pptx

  • 1.
  • 2. Introduction: • Anti-helminthics are drugs either kill (vermicide) or expel (vermifuge) infesting helminthics (worms). • In the human body, GIT is the abode of many helminthics, but some also live in tissues, or their larvae migrate into tissues. • They harm the host by depriving him of food, causing blood loss, injury to organs, intestinal or lymphatic obstruction and by secreting toxins.
  • 3.
  • 4.
  • 5.
  • 6.
  • 7. FDAapproved new drugs: • Moxidectin • Triclabendazole • Closantel • Emodepside
  • 8. Moxidectin • Potent, broad-spectrum endectocide. • Semi-synthetic methoxine • Moxidectin has a longer half-life in adipose tissue than ivermectin because of its liposolubility. • MOA: Selectively binds to GABA-A and glutamate-gated chloride ion channels (which are vital for the function of invertebrate nerve and muscle cells). It presents activity against the parasite but it does not kill them. Once moxidectin is bound, there is an increased permeability leading to an influx of chloride ions and flaccid paralysis of the parasite
  • 9. Indication:  River blindness (Onchocerca volvulus): 8 mg orally, taken once as a single dose. ADR:  Headache  Hypotension  Hyponatremia  Eosinophilia  Pruritus
  • 10. Triclabendazole • Narrow spectrum agent and unique among benzimidazole in its highly specific activity against Fascioliasis. MOA: Triclabendazole are absorbed by the outer body covering of the mature and immature worms. Causing reduction in the resting membrane potential, inhibition of tubulin function (changes at position 82 (glutamic acid) and position 91 (threonine)) as well as protein and enzyme synthesis necessary of survival. This metabolic disturbances leads to an inhibition of motility, inhibition of spermatogenesis and egg/embryonic cells.
  • 11. Indication: Fascioliasis (total dose of 20 mg/kg-10 mg/kg doses given on Days 1 and 3). ADR:  Yellow skin or eyes  Abdominal pain (expulsion of dye worms)  Vomiting  Indigestion
  • 12. Closantel  Closantel is a broad-spectrum antiparasitic agent used against several species and developmental stages of trematodes, nematodes and arthropods. MOA: Decouples the mitochondrial oxidative phosphorylation Leads to inhibition of ATP synthesis Seems to occur through supression of the activity of succinate dehydrogenase and fumarate reductase . Cause death of the parasite
  • 13. Indication:  Fasciola hepatica (liver fluke). ADR:  Difficulty breathing  Swelling of face, lips, toungue..etc  Rashes  Red swollen blisters or peeling skin with or without fever  Wheezing
  • 14. Emodepside:  Broad spectrum, Semisynthetic compound whose precursor is a metabolite of the fungus Mycelia sterile.  potent antihelminthic drug used in combination with praziquantel MOA: Drug bind to the lactrophilin receptor presynaptically Which activates a complex signal transmission cascade that eventually results in the release of inhibitory neuropeptides into the synaptic gap Resulting ion influx that occurs postsynaptically results in the inhibition of pharyngeal pump function that leads to paralysis and death of susceptible nematodes
  • 15. Indication:  River blindness (onchocerciasis).  Treatment of intestinal nematodes.  To control Hookworm, roundworm, and Tapeworm Infection in Cats. ADR:  Hair loss  Nervousness  Salivation  Eye irritation  Tremor
  • 16. Neurocysticercosis:  Neurocysticercosis is a preventable parasitic infection caused by larval cysts (enclosed sacs containing the immature stage of a parasite) of the pork tapeworm (Taenia solium).  Larval cysts in the brain cause a form of cysticercosis called neurocysticercosis which can lead to seizures. Treatment:  Albendazole is now preferred over praziquantel; bec- ause:  Course of treatment is shorter (8-15 days)  Cheaper  High cure rate  Corticosteroids enhance absorption
  • 17. REFERENCE:  http://what-when-how.com/medical-microbiology-and-infection/tissue- helminths-parasitology-medical-microbiology-and-infection/  https://www.emro.who.int/health-topics/helminthiasis/index.html  Goodman and Gilman’s, The pharmacological basis of therapuetics, 12TH edition, Page number: 1444-1459  https://www.slideshare.net/ParasuramanParasuraman/anthelmintic- drugs  https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020666s005 s006lbl.pdf  https://www.mdpi.com/1422-0067/21/14/4957  https://go.drugbank.com/drugs/DB11431  https://medlineplus.gov/druginfo/meds/a619048.html  https://pubmed.ncbi.nlm.nih.gov/33674322/