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Anthelmintics

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by

Mostafa Nabil

on 13 May 2016

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Transcript of Anthelmintics

ANTHELMENTICS
Thiobendazole
Albendazole
Ivermectin
Pyrantel pamoate

Piprazin

Helminthes

Vermicide
Vermifuge
Charachters of Ideal anthelmentics
Orally Active
Effective in Single Dose
Inexpensive
Safe to man . Toxic to worm
* Block Glucose uptake due to inhibiting microtubules synthesis Anthelmentics



Prevelance
* Block Glucose uptake due to inhibiting microtubules synthesis Anthelmentics

Mebendazole

Synthetic benzimidazole
Wide Spectrum
Low Adverse effect

PharmacoKinetics :
Absorbtion in intestine.
Only 10 % is absorbed
The absorbed dose rabidly converted in metabolites ( First Pass in liver ) 2-6 h half life
75-90 % of dose passed in feaces
Dose :
100 mg Tablet / Chewable tablt / /5ml suspension
More effective than albendazole in tichuraisis
DOC :

Pin worm , Hook worm ( Ancylostoma ) , Round worms Ascariasis.
Side Effects :

Nausea , Vimiting , diarrhea , abdominal pain
High Dose : Rash urticaria , elevation in Liver enzymes
Contraindicated in pregnancy ( teratogenic )
used with aution in children under 2 years as may cause convulsions
oral Broad spectrum anthelmentic agent
DOC in hydatid disease & custicercosis
Also effective againest Pin worm , hook worm , round worm , whip worm , thread worm
Dose :
Taken with fatty meal with tissue parasite ( it's metabolite albendazole sulfoxide is highly active )
weak action againest microfilaria
400 mg oral for adults & children over 2 years for 2-3 days in Ascaris , Trichuraisis , Hook worm & pin worm infections
Help in Surgical removal of Hydatid cysts, 400 mg twice daily with meals for 1-6 months
Also in
Cutaneous larva migrain ( 400 mg daily for 3 days )
viscral larva migrain ( 400 mg twice daiy for 5 days )

Pharmacokinetics :

Erraticaly absorbed ofter oral adminstration but inhanced with heavy fat meal.
Metabolized in liver & excreted in urine
t 1/2
: 8.5 h

Side ُEffects :
Almost free
But mild epigastric distress, diarrhea , headache , nausea were reported
In long term cause Elevation in Liver enzymes
Given with caution in Liver & Kidney patients
Contra indicated in pregnanacy

*Effective against Thread worm, cutanous larva migrain , early stage of trichinosis
PK :
water insoluble but available for oral absorption
hydroxylated in liver and excreted in urin

MOA :
as mebendazole but have anti inflamatory effect which help in
inflamation of cutanous larva migration.

SE :

Nausea , Vomiting , Loss of appetite , Headache



MOA :

activates nicotinic cholinergic receptors leading to persistant depolarization which cause spastic paralysis.

PK:

Poor oral absorption
Inestinal tract is the site of effect

SE:
Mild Nausea , Headache , Vomiting
Effective against round worms , hook worms , pin worms
MOA :
Cause HyperPolarization of worm mucle by GABA Agonist action cause Chloride channel opening So decrease Contraction to Ach
Orally Active
Metabolized in liver & excreted in urin

SE :

Almost Safe
In high doses cause Dizziness
Toxicity cause death due to convulsions & respiratory faliure
*
CI
in Renal dysfunction

ٍ
SAFE IN PREGNANCY !!
Niclosamide

SAFE IN PREGNANCY
MOA :
inhibit oxidative phosphorylation in mitochondria & Ulter priduction of areobic ATP
DOC :

Cestodes (Tape Worm)
SE :
Minor Abdominal Symptoms

MOA :
Acts via Special type of glutamate gated Cl-Channel These Channel only in invertebrae >> So not effective on man or Fluks or tap worm
Increase GABA Activity
Cause paralysis of Worm Muscle
PK :
absorbed orally , Well distributed ( not to CNS ) , Half life 48 - 60 H
Dose :
0.2 mg per Kg with 400 mg albendazole in Flaria Infection.
0.2 per Kg single dose in Strongyloids
SE :

Nasuea , Vomiting , Pruritus .

THANK YOU

Refrences:
http://jama.jamanetwork.com/article.aspx?articleid=338112
http://www.ncbi.nlm.nih.gov/pubmed/127396
http://tmedweb.tulane.edu/pharmwiki/doku.php/albendazole
http://www.drugs.com/mtm/albendazole.html
Praziquantel
DOC :
Trematodes Schistosomasis
MOA :
Increase cell wall permeability to Ca++ causing Pralysis

PK:
Rabid Oral Absorbtion
Metabolized in liver & excreted in urine


CI:
Ocular Cysticercosis ( Eye Destruction)
Full transcript