Anthelmentics agents medicinal chemistry

Anthelmentics agents

1. Dr.MahendraG S
Assistant Professor, NGSMIPS
Anthelmentics

2. •Humansaretheprimaryhostsforthemostofhelminthicinfections.
•Mostwormsproduceinhumansexuallybyproducingeggsandlarvae.
•ThesepassoutofbodyandinfectthesecondaryhostImatureforms
invadehumansviaskinorGITandmaturetoadultwormswith
characteristictissuedistribution.
•Wormsliveinhostsalimentarycanal.
•Wormsorlarvaeliveinothertissuesofhostbodylikemuscles,viscera,
menninges,lungs,subcutaneoustissues.
HelminthicInfections

3. A) INTESTINAL ROUND WORMS (NEMATODES)
•Ascaris lmubricods(common round worm)
•Enterobius vermicularis (pin worm)
•Trichuris trichuria( whip worm)
•Strongyloidsstercoralis( thread worm)
•Ankylostomadudenale(hook worm)
B)TAPEWORMS(CESTODES)
•Taeniasaginata(Beaf),
•Taeniasolium(Pork),Hymenolepisnana(Dwarf),diphylobothriumlatum(Fish)
Humansbecomeinfectedbyeatingraworundercookedmeatcontaininglarvaeof
infectedcattleorpigwhichhasencystedintheanimalmuscletissue.

4. Ascaris lumbricoids( common round worm) Hookworm whipworm
Tricuris tricura(whip worm)
Tapeworm
cysticercosis
Trichinelaspiralis

5. Hydateidcyct

7. Mebendazoleisantiparasiticmedicationusedtotreatvarioustypesofworminfections.itis
partofthebenzimidazoleclassofdrugsandworksbyinhibitingthesynthesisof
microtubulesinparasites,disruptingglucoseuptake,whicheventuallyleadstothedeath
oftheparasite.
Mebendazole
MechanismofAction:
Mebendazoleselectivelyinhibitsthesynthesisofmicrotubulesbybindingtotubulin
withintheparasites.Thisresultsinimpairedglucoseuptakeanddigestiveprocesses
withintheworm,eventuallyleadingtoitsdeath.

8. Mebendazole is commonly used for the treatment of:
➢Ascariasis:InfectionbytheroundwormAscarislumbricoides.
➢Enterobiasis(PinwormInfection):CausedbyEnterobiusvermicularis.
➢Trichuriasis:InfectionwiththewhipwormTrichuristrichiura.
➢HookwormInfections:CausedbyAncylostomaduodenaleorNecatoramericanus.
SideEffects:
Commonsideeffectsinclude:
➢Abdominalpain,Diarrhea,Nausea
➢Lesscommonbutmoreserioussideeffectscanincludeallergicreactions,liver
issues,andinrarecases,bonemarrowsuppression.Regularmonitoringofliver
functionandbloodcountsmaybeadvisedduringprolongeduse.

9. ALBENDAZOLE
•Itisabroadspectrum,Itisadrugofchoice(primarytherapeuticapplication)
fortreatmentofhydatiddiseaseandcysticercosis.
Mechanismofaction:Itinhibitsmicrotubulesynthesisinnematodes(intestinal
roundworms)thatirreversiblyimpairsglucoseuptake,intestinalparasitesare
immobilizedanddieslowly
methylN-(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:
•HydatidDisease(Echinococcosis):Aparasiticdiseasecausedbytapeworm
larvae.
•Neurocysticercosis:InfectioncausedbytheporktapewormTaeniasolium,
leadingtocystsinthebrain.
•Ascariasis:AninfectionbytheroundwormAscarislumbricoides.
•Hookworm:CausedbywormssuchasAncylostomaduodenaleandNecator
americanus.
•Trichuriasis:InfectionwithTrichuristrichiura(whipworm).
•Strongyloidiasis:InfectionbyStrongyloidesstercoralis.

11. SideEffects:
Commonsideeffectsinclude:
•Nausea
•Vomiting
•Abdominalpain
•Headache
Inrarecases,moreserioussideeffectslikebonemarrowsuppression,
liverdamage,orallergicreactionscanoccur,soregularmonitoringofblood
countsandliverfunctionmaybenecessaryduringprolongedtreatment.

12. Diethylcarbamazine*
Diethylcarbamazine(DEC)isanantiparasiticmedicationprimarilyusedto
treatfilarialinfections.Itisespeciallyeffectiveagainstcertainparasitic
worminfestationsthatcausediseaseslikelymphaticfilariasisandloiasis.
N,N-diethyl-4-methylpiperazine-1-carboxamide
MechanismofAction:
ThemechanismofDECisnotfullyunderstood,DECparalyzestheparasitesbyinterfering
withtheirneuromuscularsystem,makingthemeasierfortheimmunesystemtodestroy.It
alsoaltersthesurfacestructureoftheworms,increasingtheirvulnerabilitytoimmuneattack.

13. Diethylcarbamazine is mainly used for:
➢LymphaticFilariasis:CausedbyWuchereriabancrofti,Brugiamalayi,orBrugia
timori,whichcanleadtoelephantiasis.
➢Loiasis:AninfectioncausedbytheLoaloaworm,
➢TropicalPulmonaryEosinophilia:Aseverelungconditionassociatedwithfilarial
infections.
Side Effects:
Common side effects include:
▪Nausea
▪Vomiting
▪Dizziness
▪Headache

15. Ivermectin
MechanismofAction:
Ivermectinworksbybindingto
glutamate-gatedchloridechannelsinthe
nerveandmusclecellsofinvertebrates,
leadingtoparalysisanddeathofthe
parasite.
Ivermectinisawidelyusedantiparasiticmedicationwithbroad-spectrumactivity.It
iseffectiveagainstavarietyofparasiticinfections,includingthosecausedby
nematodes(roundworms)andectoparasiteslikeliceandmites.

16. IvermectiniscommonlyUsedfor:
1.Onchocerciasis(RiverBlindness):CausedbytheparasiteOnchocerca
volvulus.
2.Strongyloidiasis:CausedbytheparasiticwormStrongyloidesstercoralis.
3.Scabies:AskininfestationcausedbythemiteSarcoptesscabiei.
4.Lice:Forthetreatmentofheadlice(Pediculushumanuscapitis).
5.LymphaticFilariasis:Oftenusedincombinationwithotherdrugslike
diethylcarbamazineoralbendazoleformassdrugadministration.

17. SideEffects
Commonsideeffectsinclude:
•Nausea
•Diarrhea
•Dizziness
•Fatigue
Inonchocerciasis,areactionknownastheMazzottireactionmayoccur,
similartowhatcanhappenwithdiethylcarbamazine.Thisreactioninvolves
itching,rash,fever,andswollenlymphnodesduetothebody'sresponsetothe
deathofthemicrofilariae.