The document discusses several new FDA-approved anti-helminthic drugs including moxidectin, triclabendazole, closantel, and emodepside. It provides details on their mechanisms of action, indications for use, and common adverse drug reactions. Moxidectin is a broad-spectrum endectocide that acts on GABA and glutamate channels. Triclabendazole is highly specific for fascioliasis and impacts worm membrane potential and proteins. Closantel acts on mitochondrial oxidative phosphorylation. Emodepside binds to receptors causing nematode paralysis. The drugs treat conditions like river blindness, liver flukes, and intestinal worms.
Asian American Pacific Islander Month DDSD 2024.pptx
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.
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