Anthelmintic
According to the syllabus based on “PHARMACY COUNCIL OF INDIA”
“I Dedicate this work to all the
Students , Pharmacy Faculty & Family Members
Drx. Shubhanshu R.s. Jaiswal
Helminthiasis also known as Worm Infection, is any macro parasitic disease of humans & other animals in which a Part of the body is infected with parasitic worms, known as Helminths.
3. Introduction
Helminthiasis also known as Worm Infection, is
any macro parasitic disease of humans & other
animals in which a Part of the body is infected
with parasitic worms, known as Helminths.
There are numerous species of these Parasites,
which are broadly classified into tapeworms,
flukes & roundworms.
They often live in the GIT of their hosts, but
they may also burrow into other organs,
where they induce physiological damage.
4. Helminthiasis is prevalent globally about 1/3rd
of world’s population harbours them, but is
more common in developing countries with
Poorer personal and Environmental hygiene.
Causative organisms harm the host by
depriving him of food, causing blood loss,
injury to organs, intestinal or lymphatic
obstruction and by secreting toxins.
Introduction
5. Anthelmintic
Anthelmintic are the drugs that either KILL
[vermicide] Expel [vermifuge] infesting Helminths.
The choice of drug for each worm infestation is
based not only on Efficacy, but also on Lack of
Side effects/ Toxicity, Ease of administration
[preferably single dose] & low cost.
Development of resistance has not been a
problem in the clinical use of Anthelmintic.
6. Classification Of Drugs
The most Commonly used ANTHELMINTIC DRUGS
are as follows:
Mebendazole
Albendazole
Thiabendazole
Pyrantel Pamoate
Piperazine
Diethyl carbamazine citrate
Lvermectin
7. MEBENDAZOLE
It is a benzimidazole introduced in 1972. This
congener of thiabendazole became very
popular because it retained the broad-spectrum
anthelmintic activity but not the toxicity of its
predecessor.
It has produced nearly 100% cure rate/reduction
in Egg count in Roundworm,Hookworm [Both
Species].
The immobilizing and lethal action of
Mebendazole on worms is rather slow: takes
2-3 days to develop.
8. Mechanism of
Action
The Site Of Action of Mebendazole is the
Microtubular Protein ‘-Tubulin’of the Parasite.
It binds to -Tubulin of susceptible worms with
High Affinity and Inhibits its Polymerization.
Intracellular microtubules in the cells of the
worm are gradually lost.
In addition, it probably blocks glucose uptake
in the parasite and depletes it’s glycogen
stores.
9. PHARMACOKINETI
CS
Absorption of Mebendazole From
Intestines is minimal; 75-90% of an oral
dose is passed in the Faeces. The fraction
absorbed is excreted mainly as inactive
metabolites in Urine/Faeces.
10. Adverse
Effects
Diarrhoea, Nausea & Abdominal Pain have
attended it’s use in heavy infestation.
Allergic reactions, loss of hair & granulocy–
topenia have been reported with high
doses.
Vomiting, Diarrhea, Headache, Dizziness or
Drowsiness may occur.
11. Albendazole
It is a subsequently introduced congener
of Mebendazole.
Retains the Broad-Spectrum activity and
excellent tolerability of its predecessor & has
the advantage of single dose administration in
many infestations.
One dose treatment has produced cure rates
in ascariasis, hookworm (both species) &
enterobiasis which are comparable to 3 day
12. MOA PHARMACOKINETICS
The mechanism
of action of
Albendazole is
similar to that of
Mebendazole.
Absorption of
Albendazole after oral
administration is
significant, but
inconsistent . It is
enhanced when the
drug is taken with fatty
meal.
The fraction absorbed is
converted by first pass
metabolism to its
13. ADVERSE
EFFECTS
PHARMACOKINETI
CS
Gastrointestinal side
effects, Dizziness.
Prolonged use has
caused :
• Headache
• Fever
• Alopecia
• Jaundice
• and Neutropenia.
Albendazole sulfoxide
is widely distributed in
the body, enters Brain
and is excreted in
urine with a t½ of 8.5
hours & exert
Anthelmintic activity in
tissues as well.
14. THIABENDAZOLE
It was the first benzimidazole
polyanthelminitic introduced in
1961, which covered practically
all species of Nematodes
infesting the GIT – Pinworm,
Hookworm, Roundworm.
15. MOA PHARMACOKINETICS
It also inhibits
development of
the Egg of worms
& Kill larvae.
It has
Antiinflammatory
action as well.
Since Thiabendazole
is well absorbed from
GIT, systemic adverse
effects are common.
ADVERSE
EFFECTS Nausea, vomiting.
Abdominal Pain.
Diarrhoea.
Impairment of
Alertness.
Itching.
16. PYRANTEL PAMOATE
It was Introduced in 1969 for Pinworm
infestation in Children : use soon
extended to Roundworm & Hookworm
as well.
Efficacy against Ascaris, Enterobius
and Ancylostoma is High & comparable
to that of Mebendazole.
17. Mechanism Of Action
Pyrantel Causes ACTIVATION Of
Nicotinic Cholinergic Receptors In
The Worms Resulting In Persistent
Depolarizationslowly Developing
Contracture & Spastic Paralysis.
Women's Are Then Expelled.
18. ADVERSE EFFECTS PHARMACOKINETICS
Pyrantel Pamoate is
remarkably Free of
side effects:
occasional G.I.
symptoms, Headache
and Dizziness is
reported.
Only 10-15% of an
Oral Dose of
Pyrantel Pamoate
is absorbed: This is
Partly metabolised
and excreted in
Urine.
19. PIPERAZINE
Introduced in 1950,it is a highly active drug
against Ascaris and Entrobius: achieves
90-100% cure rates.
However, because of the availability at
more convenient and better tolerated
Albendazole/Mebendazole. It is now
considered a second choice drug.
20. Piperazine causes Hyperpolarization of
Ascaris muscle by a GABA agonistic action.
Opening of CL¯ CHANNELS causes relaxation
depresses responsiveness to contractile
action of ACh. Flaccid Paralysis occurs and
worms are expelled alive.
Mechanism Of Action
21. ADVERSE EFFECTS PHARMACOKINETICS
Piperazine is safe,
but Nausea,
Vomiting, Abdominal
discomfort and
Urticarea may be felt.
Dizziness and
Excitement occurs at
high doses: Toxic
doses produce
Convulsions, Death
is due to Respiratory
A considerable
fraction of the Oral
Dose of Piperazine is
absorbed.
It is partly
metabolized in liver
and excreated in
urine.
22. Diethyl Carbamazine Citrate
Developed in 1948.
it is the first Drug for Filariasis caused
by the Nematodes Wuchereria bancrofti
[90% cases] and Brugia malayi.
23. Mechanism Of Action
Diethyl Carbamazine Citrate is Microfilaricidal.
It has a highly selective effect on microfilariae (MF). A
dose of 2 mg / kg TDS clears Mf of W. Bancrofti and B.
Malayi from peripheral Blood in 7days. The most
important action of DEC appears to be Alteration of
organelle membranes of the Mf promoting cell death.
24. ADVERSE EFFECTS PHARMACOKINETICS
Side effects are
common but
generally not serious.
Nausea
Loss of appetite
Headache
Weakness
Dizziness
are a usual
complaints.
DEC is absorbed after
oral ingestion,
distributed all over the
body, Metabolized in
liver & excreated in
urine.
Excretion is faster in a
acidic urine.
Plasma t½ of usual
clinical doses is 4-12
hours, depending on
25. Drx.SHUBHANSHU R.S. JAISWAL
E-mail: 1stsrsj@gmail.com
Contact No: 9511082401
Address:Barabanki [22500], U.P,.India.
OT Incharge
Institute Name: Mayo Institute of Medial Sciences.
Description : To do Dressing in Minor OT [Surgery Dept.].
Slideshare I’d
Shubhanshu R.S Jaiswal
https://www.slideshare.net/DrxShubhanshuRsJaisw