Anthelmintics drugs.pdf

3,611 views 42 slides Feb 16, 2023
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About This Presentation

At the end of this e-learning session you are able to…
1. Discuss type of helminths or worm infections.
2. Explain pharmacology of Anthelminthic Drugs.

For 30+ video lecture series on Pharmacology Experiment as per PCI B Pharm Syllabus refer link given below: https://www.youtube.com/playlist?list...


Slide Content

Prof. Shaikh Abusufiyan
Assistant Professor,
AIKTC-School of Pharmacy,
New Panvel-410206
Anthelminthic Drugs
Pharma Learning Forever

At the end of this e-learning session you are able to…
A.Discuss type of helminths.
B.Explain pharmacologyof
Anthelminthic Drugs.

Activity I: Self learning of e-content

●Manyhumanharbour-->helminths(Worms)ofone
speciesoranother.
●Insomecasestheseinfection-->resultsmainlyin
discomfortanddonotcauseillhealth.eg.Threadworms
inchildren.
●Otherworminfections,suchasSchistosomiasisand
hookwormdisease-->canproduceveryserious
morbidity.

Sexual reproduction of worms:
●Most worm reproduce sexually in human host (Primary
host)
Produces egg or larvae
When passes out the body
it infect the secondary host

Type of worm infections
Those in which
1.worm lives in alimentary canal
2.worms lives in other tissue of the host body

Worm lives in alimentary canal
1. Tapeworm (Cestodes)
The usual intermediatehosts of tapeworm are
●cattle
●pigs
●and fresh water fish.
●Human become infected --> by eating raw or under
cooked meatof these animals or fishes.

2. Intestinal Round worms (Nematodes): 4 types
1. Common round worm
2. Thread worm
3. Whipe-worm
4. Hookworms

Worms lives in the host tissues
1.Trematodesorflukes:
•Infectioncausedbytrematodesorflukesis
calledasSchistosomiasis(bilharzia).
2.Tissueroundworms:areof2types
a.Guineaworms
b.Filariaeworms

a.Guineaworms
●ThegravidfemalemigratetotheS.Ctissuesoftheleg
orthefootandprotrudethroughanulcerinthe
skin.
●Thewormmaybeuptoameterinlengthandhasto
beremovedsurgically
●Orbyslowmechanicalwindningofthewormontothe
stickoveraperiodofdays.

b.Filariaeworm:
●Majorfilarialdiseasearecausedbywuchereria
whichcausedobstructionofthelymphaticvessels
producingelephantiasis.

Q&A: Activity II
Q.1 Enlist types of worm infection.
Q.2 Name worm which migrate to the S.C
tissuesof the leg or the foot and protrude
through an ulcer in the skin?
Q.3 How Filariae worm causes
elephantiasis.

Anthelmintic Drugs
●To be an effective anthelmintic drugs
●it must be able to --> penetrate the cuticle of the
worms
●or gain access--> to alimentary tract.
•Limitation: This lead to difficulties for the design of
good anthelmintic drugs.

●Somewormsareexclusively-->haemophagous
(bloodeating)whileotheraretissuegazers.
Thereforerootanddoseofanthelmintic-->is
Importantandmustbechosencarefully.

MOA of anthelmintic drugs
1.Paralysisofwormsordamageswormcuticle
Leadingtopartialdigestionorrejectionbyimmune
system.
2.Interferewith-->metabolismoftheworm

Classification
1.Forroundworm
eg.Mebendazole,Albendazole,Pyrantal,Piperazine,Levamisole,
Ivermectin.
2.Forhookworm
eg.Mebendazole,Albendazole,Pyrantal,Levamisole
3.Forthreadworm
eg.Mebendazole,Albendazole,Pyrantal,Piperazine

4. For whipworm
Eg.Mebendazole,Albendazole
5.Forfilariasis
eg.Albendazole,Ivermectin
6.Fortapeworms
Albendazole,Praziquantal

Benzimidazole
●Eg.Mebendazole, Albendazole, Thiabendazole
●Are broad spectrum agents

MOA: Polymerization
●Beta-Tubulin Microtubule
Benzimidazole
Glucose uptake by the worm

MOA:
●BenzimidazoleBindtofreebetatubulin
Andinhibititspolymerizationandthusinterferewith
Microtubulindependentglucoseuptakebytheworm.

●Theactionisselectiveonthehelminthmicrotubules
–250to400timesmorepotentinhelminththen
mammaliantissue.
●Effecttaketimetodevelop-->Wormsmaynotbe
expelledforseveraldays.

Pharmacokinetics
Absorption:
●Only10%ofdrugisabsorbedafteroral
administration.
●Fattymeal–Increasesabsorption
Metabolism:
●Rapidlymetabolisedinliver
Excretion:
●Excretedinurineandbile

Pharmacokinetics
Dose:
●Given as single daily dose--> for thread worm
●Twiceadaily-->for3daysforhookwormandround
worminfection.

Unwanted effect
●Very few
●GIT Disturbance

Q&A: Activity III
Q.1 What is the use of Ivermectin?
Q.2 Give mechanism of action of
Benzimidazole anthelmintic drugs?
Q.3 Recommend food to enhance
absorption of Benzimidazole anthelmintic
drugs.

Activity IV: Self learning of e-content

Albendazole
●Broadspectrumanthelmintics
●Afteroraladministration,itisrapidlyabsorbedand
metabolisedtosulfoxideandsulfone.
Responsibleforanthelminthicaction

●The plasma concentration of metabolites --> is 100
times greater then that of mebendazole.
Unwanted effect:
●GIT disturbance

Praziquantel:
●Highly effective broad spectrum anthelmintic drug.
●Drug of choice forall form of schistosomiasis--> used
in large scale schistosome eradication programmes.

MOA
●It apparently disturb the calcium homeostasisin the
parasite
Induces the calcium influx
Rapid and prolonged contractionof the musculature
Paralysis and death of worm

Pharmacokinetics
●Given orally -the praziquantel is well
absorbed
●Metabolised in the liver
●Metabolites are excreted in the urine
●The plasma half life –60 to 90 min.

Unwanted effects:
●GIT disturbance
●Dizziness
●Aching in muscle
●Joint skin eruption
●And low grade fever
●It is safe for pregnant and lactating women.

●Piperazine:
●Usedtotreatinfectionwithcommonroundworm
infectionandthreadworms.

MOA:
●Itirreversiblyinhibitneuromusculartransmissionin
theworms(byactinglikeGABA-theinhibitory
neurotransmitter).
leadstoparalysisofwormandtheparalysedwormare
expelledalive.

Pharmacokinetics
●Itisgivenorally-somebutnotallisabsorb
●Itispartlymetabolizedandremainderis
eliminatedunchangedviathekidney.

Unwanted effect
●GIT disturbance
●Urticaria
●Bronchospasm-occur occasionally
●Some patient experiences
●dizziness
●paraesthesia's
●vertigo
●And incoordination.

Q&A: Activity V
Q.1 Give mechanism of action of
Praziquantel?
Q.3 Recommend food to enhance
absorption of Benzimidazole anthelmintic
drugs.

Reference:
•H.PRang.MMDale,J.MRitter,R.JFlower,G
Henderson.Pharmacology,SeventhEdition.Elsevier
ChurchillLivengstonPublication.Pageno:668-672